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PCT - WORLD PATENTS IN PHARMACEUTICAL EXCIPIENTS PUBLISHED FROM 1990 TO 2007


FORMULATIONS OF 5-HT3 RECEPTOR ANTAGONISTS WITH POLYORTHOESTER FOR USE IN THE PREVENTION OF ACUTE AND DELAYED CHEMOTHERAPY- INDUCED NAUSEA AND VOMITING (CINV)

(WO2007133752) 22.11.2007 A61K 47/10 A.P. PHARMA, INC.
A pharmaceutical composition for the sustained release of an effective amount of a selective 5-hydroxytryptamine 3 (5-HT3) receptor antagonist for the prevention, reduction or alleviation of acute and delayed chemotherapy-induced nausea and vomiting (CINV) following a course of emetogenic chemotherapy, wherein the composition is administered by subcutaneous injection, the composition comprising a 5-HT3 receptor antagonist, a semi-solid delivery vehicle and a pharmaceutically acceptable liquid excipient; wherein the composition, when administered in a single dosage, provides a controlled release of the 5-HT3 receptor antagonist and prolonging the release of the 5- HT3 receptor antagonist that tracks the profile of the incidence of vomiting.
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A METHOD FOR OBTAINING A PHARMACEUTICAL COMPOSITION COMPRISING AN ACTIVE AGENT ZIPRASIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

(WO2007126322) 08.11.2007 A61K 9/14 PLIVAKRAKËW, ZAKLADY FARMACEUTYCZNE S.A.
The present invention discloses a method for obtaining a pharmaceutical composition comprising an active agent ziprasidone or a pharmaceutically acceptable salt thereof, to improve solubility and thus bioavailability of the drug, whereby the active agent is slugged together with one or more pharmaceutically acceptable excipients. In preferred embodiment the active agent is slugged with solubilizing agent and optionally with additional diluent and/or lubricant. Preferably ziprasidone hydrochloride or ziprasidone hydrochloride monohydrate are used as the active agent. Preferably a hydrophilic excipient chosen from alkyl cellulose derivatives, starch derivatives, poly(oxy)ethylene derivatives, polyvinyl derivatives or glyceryl derivatives is u...
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FLUID DISPENSING SYSTEM, METHODS AND PRODUCTS

(WO2007117173) 18.10.2007 G05D 11/02 CLOSED JOINT STOCK COMPANY 'BIOCAD'
A system for dispensing fluid includes a first fluid circuit for circulating a first fluid, a fluid supply for supplying a second fluid, and a second fluid circuit for mixing the first and second fluids. The first fluid can be hydrophobic and the second fluid can be aqueous. The mixture can be an emulsion. The first fluid can be a suppository base, and the second fluid can include an active pharmaceutical ingredient. The system can dispense the mixed fluids to a mold for forming a suppository.
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NOVEL COMPOSITIONS FOR HAIR DISORDERS AND PROCESS OF PREPARATION THEREOF

(WO2007113851) 11.10.2007 A61Q 7/00 PANACEA BIOTEC LTD.
Novel compositions for hair loss prevention and/or hair growth promotion comprising at least active agent preferably derived from natural source such as from the plant Vernonia sp., either alone or in combination with other active agent(s) and optionally one or more excipient(s) are provided. The process for the extraction of hair growth promoting agent and preparation of compositions comprising such active agent are also described. The novel composition is preferably in the form of an oral or topical preparation such as tablet, capsule, liquid solution or suspension, cream, gel, lotion or spray and is useful against hair disease(s)/disorder (s) and/or other associated disorders particularly in the management of testosterone induced androgen...
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STABILIZED COMPOSITIONS CONTAINING ALKALINE LABILE DRUGS

(WO2007112286) 04.10.2007 A61K 9/20 AUXILIUM PHARMACEUTICALS, INC.
A stabilized bioadhesive composition containing an alkaline labile drug and a method for its preparation are provided. In one aspect, the composition is a hot-melt extruded (HME) composition comprising a preformed excipient mixture comprising an acidic component and an alkaline thermoplastic matrix-forming material, e.g. polymer. The excipient mixture is formed before blending with an alkaline labile drug. The blend is then hot-melt extruded to form the HME composition. By so doing, the acidic component is able to neutralize or render moderately acidic the excipient mixture. This particular process has been shown to substantially reduce the degradation of an alkaline labile drug during hot-melt extrusion. The excipient mixture softens or me...
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ANTIBIOTIC COMPOSITIONS OF MODIFIED RELEASE AND PROCESS OF PRODUCTION THEREOF

(WO2007110875) 04.10.2007 A61K 31/43 PANACEA BIOTEC LTD.
Novel modified release pharmaceutical compositions wherein the composition comprises at least one antibiotic(s) preferably amoxicillin or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof either alone or in combination with other antibiotic(s) as active ingredient, with at least one release modifying agent(s) for controlling the release of the beta lactam antibiotic optionally with one or more other pharmaceutically acceptable excipient(s) is provided, wherein the dosage form provides a release of not more than about 60 % of the antibiotic in about 30 minutes and not less than about 70 % of the antibiotic after 8 hours when subjected to in vitro dissolution study or when...
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CONTROLLED RELEASE FORMULATION OF TOLTERODINE

(WO2007109357) 27.09.2007 A61K 9/50 TEVA PHARMACEUTICAL INDUSTRIES LTD.
The invention encompasses stable multiparticulate pharmaceutical compositions of tolterodine having at least one pharmaceutically acceptable excipient and at least two populations of multiparticulates each population having tolterodine or a salt thereof and the ratio of the populations is from 90:10 to 10:90 by weight, wherein after storage for 1 month at 40 ░C and 75 % relative humidity the difference between the dissolution profile at 4 hours is no more than about 5 % when compared to the dissolution profile at the time of manufacture.
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LIQUID AND SOLID DOSAGE FORMULATIONS CONTAINING DATES (PHOENIX DACTYLIFERA)

(WO2007107787) 27.09.2007 None KHAN, Karrar Ahmad
Oral liquid and solid dosage formulations comprise a homogeneous dispersion of date material in a finely divided form. The formulation may be of nutritional and/or therapeutic value. Alternatively, the processed dates in the liquid and solid form may function purely as an excipient, in particular as an agent capable of improving the palatability of a pharmaceutically active substance with an unpleasant taste. The liquid formulation may be prepared by dispersing stoned, but otherwise whole date material in water, and subjecting the dispersion to homogenisation. The solid dose formulation preferably takes the form of granules, a tablet or a lozenge, and is preferably prepared by a process that involves the formation of a homogeneous dispersio...
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PHARMACEUTICAL COMPOSITION CONTAINING A CENTRAL OPIOID AGONIST, A CENTRAL OPIOID ANTAGONIST, AND A PERIPHERAL OPIOID ANTAGONIST, AND METHOD FOR MAKING THE SAME

(WO2007088489) 09.08.2007 None HARROGATE HOLDINGS
A pharmaceutical composition for treating or preventing a disease, condition or symptoms thereof in a warm-blooded animal including a human, includes a therapeutically effective amount of an opioid agonist exhibiting potential pharmacologically addictive properties in warm blooded animals including humans; a side-effect reducing agent present in amounts sufficient to at least substantially neutralize the adverse side effects of the opioid agonist; an opioid antagonist present in a sequestered form in amounts sufficient to block the pharmacological effect of the opioid agonist upon release from the sequestered form; and a pharmaceutically acceptable carrier.
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NOVEL PHARMACEUTICAL COMPOSITIONS AND PROCESS OF PREPARATION THEREOF

(WO2007086078) 02.08.2007 A61K 9/24 PANACEA BIOTEC LTD.
Novel pharmaceutical compositions comprising at least one active agent(s) or its pharmaceutically acceptable salts, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof; at least one permeation enhancer(s); at least one adsorbent(s) and at least one bioadhesive polymer(s); optionally at least one acid soluble polymer(s) and optionally one or more other pharmaceutically acceptable excipient(s) are provided. Preferably the compositions are in the gastro-adhesive modified release form and/or fast disintegrating dosage form which release the active agent(s) over an extended period of time. Also provided are processes of preparation of such novel compositions and methods of using them.
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FILM CONTAINING COMPOSITIONS

(WO2007076466) 05.07.2007 A61K 8/02 COLGATE-PALMOLIVE COMPANY
An oral care, personal care or cleansing composition with a carrier comprising a functional material and at least two polymers. One polymer has a greater solubility in water than the other polymer; one of the polymers may be water-soluble and the other polymer water-insoluble. The polymers are selected and apportioned to provide at least one of the following: (1) a desired stability of the film in the composition. (2) a desired rate of disintegration of the film during use of the composition, and (3) a desired rate of delivery of the functional material during use of the composition.
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PHARMACEUTICAL PRODUCT COMPRISING POROUS SILICON

(WO2007071915) 28.06.2007 A61K 9/16 pSiMEDICA LIMITED
The present invention relates to a pharmaceutical product comprising porous silicon, a beneficial substance, and an excipient, the beneficial substance being located in at least some of the pores of the porous silicon, and the excipient having a structure and composition such that it has a melting point between 25 C and 45 C. The invention allows improved control over the release of a beneficial substance from porous silicon.
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HUMAN ALPHA-DEFENSINS INHIBIT INTERLEUKIN-1BETA RELEASE

(WO2007065128) 07.06.2007 A61K 38/17 AUBURN UNIVERSITY
Human ?-defensins are inhibitors of interleukin-l? post transitional processing and release. Interleukin-l? is a key cytokine involved in the initiation and amplification of the 5 inflammatory process, including the inflammation of diseases such as Crohn's Disease and Ulcerative Colitis. Particularly, human neutrophil defensin-1 (HNP-I) produced mainly by neutrophils, and human ?-defensin 5(HD-5) produced by Paneth cells has been found to block interleukin-l? post transitional processing and release. Thus, a pharmaceutical composition and method for treating inflammation in the mammalian tissues is herein disclosed. The pharmaceutical composition is a therapeutic supplementation of a metabolic pathway to reduce inflammat...
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SUSTAINED-RELEASE FORMULATION OF ZONISAMIDE

(WO2007062228) 31.05.2007 A61K 9/00 OREXIGEN THERAPEUTICS, INC.
Pharmaceutical formulations comprise sustained-release zonisamide. Methods of preparing such pharmaceutical formulations involve intermixing zonisamide with a suitable excipient configured to control the dissolution profile of the zonisamide. Methods of treatment involve administering the pharmaceutical formulations to patients in need of such treatment.
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COMPOSITION AND ITS USE FOR THE MANUFACTURE OF A MEDICAMENT FOR TREATING, PROPHYLACTICALLY TREATING, PREVENTING CANCER AND/OR INFECTIONS IN THE URINARY TRACT

(WO2007054373) 18.05.2007 A61K 9/16 NOLABS AB
A composition is provided that allows for treatment of cancer, prophylactic treatment, and treatment of infection in the urinary tract. The composition comprises a nitric oxide (NO) eluting polymer that elutes nitric oxide (NO) in a therapeutic dose. The nitric oxide (NO) eluting polymer may be integrated with a carrier material, such that said carrier material, in use, regulates and controls the elution of said therapeutic dosage of nitric oxide (NO). The nitric oxide (NO) eluting polymer may be provided as a Solution or Suspension. Furthermore, a manufacturing method for said composition is disclosed, as well as uses of said composition in the urinary tract.
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PHARMACEUTICAL COMPOSITIONS COMPRISING POLYMERIC BINDERS WITH NON- HYDROLYSABLE COVALENT BONDS AND THEIR USE IN TREATING CELIAC DISEASE

(WO2007053935) 18.05.2007 A61K 31/74 UNIVERSITE DE MONTREAL
A pharmaceutical composition comprising a polymeric binder including a high molecular weight synthetic polymer having a backbone constituted of non hydrolysable covalent bonds, said polymer being able to form electrostatic bonds at a pH lower than the isoelectric point of gluten and peptides derived from the degradation of gluten, and being able to bind to gluten or peptides derived from the degradation of gluten in the gastrointestinal tract, and a pharmaceutically acceptable carrier. Methods of using the polymeric binder for binding gluten or a peptide derived from the degradation of gluten, for decreasing the degradation of gluten into toxic peptides or for decreasing interaction of gluten or peptides derived from the degradation of glut...
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NOVEL DISPERSIBLE TABLET COMPOSITION

(WO2007052289) 10.05.2007 A61K 47/38 RUBICON RESEARCH PVT LTD.
The present invention relates to a novel dispersible tablet composition, which comprises of a pharmacologically active ingredient and at least one excipient, which reduces the sedimentation rate of active ingredient. This invention further relates to a process for the preparation of a dispersible tablet of a pharmacologically active ingredient.
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STABLE COATED PHARMACEUTICAL FORMULATION OF OLANZAPINE AND PROCESS FOR PREPARING THE SAME

(WO2007049304) 03.05.2007 A61K 9/00 JUBILANT ORGANOSYS LIMITED
Disclosed herein are stable solid coated oral formulations of olanzapine and the process of preparation thereof. The formulation comprising effective amount of olanazpine and pharmaceutically acceptable excipient, wherein said formulation is coated with stabilized coating employing a selective polymer selected from hydroxypropyl methyl cellulose phthalate, polyvinyl acetate phthalate, cellulose acetate phthalate, hydroxypropyl methyl cellulose acetate succinate, polyvinyl alcohol, vinyl acetate copolymer, pullulan gum or zein or in combination thereof.
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TRAZODONE COMPOSITION FOR ONCE A DAY ADMINISITIATION

(WO2007048220) 03.05.2007 A61K 9/22 LABOPHARM INC.
The invention relates to a once a day formulation of trazodone or a trazodone derivative. The formulation contains trazodone or a trazodone derivative and a controlled release excipient so that, once administered orally, the trazodone or the trazodone derivative is maintained at a therapeutic plasma concentration from at least 1 hour to at least 24 hours after initial administration. After administration, the initial therapeutic action takes effect within the first hour and lasts at least about 24 hours. This therapeutic effect remains relatively and substantially stable for the remaining period of 24 hours. The formulations can be used for treating depression and/or sleeping disorders.
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METHODS OF ADMINISTERING RAPAMYCIN ANALOGS WITH ANTI-INFLAMMATORIES USING MEDICAL DEVICES

(WO2007047473) 26.04.2007 A61F 2/00 ABBOTT LABORATORIES
A medical device comprising a supporting structure capable of including or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient may include one or more therapeutic agents or substances, with the carrier including a coating on its surface, and the coating including the therapeutic substances, such as, for example, drugs. Supporting structures suitable for use include, but are not limited to, coronary stents, peripheral stents, catheters, arterio-venous grafts, by- pass grafts, and drug delivery balloons used in the vasculature. Drugs that are suitable for use in this invention include, but are not limited to, This drug can be used in combination with another drug including those selected from anti-prolifer...
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COMPOSITIONS AND METHODS OF ADMINISTERING RAPAMYCIN ANALOGS WITH PACLITAXEL USING MEDICAL DEVICES

(WO2007047416) 26.04.2007 A61F 2/00 ABBOTT LABORATORIES
Systems and compositions comprising paclitaxel and a second drug, such as rapamycin, analogs, derivatives, salts and esters thereof are disclosed, as well as methods of delivery wherein the drugs have effects that complement each other. Medical devices comprising supporting structures capable of including or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient can contain one or more therapeutic agents or substances, with the carrier preferably including a coating on the surface thereof, and the coating including the therapeutic substances, such as, for example, drugs. Supporting structures for the medical devices that are suitable for use in this invention include coronary stents, peripheral stents, cat...
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COMPOSITIONS, SYSTEMS, KITS, AND METHODS OF ADMINISTERING RAPAMYCIN ANALOGS WITH PACLITAXEL USING MEDICAL DEVICES

(WO2007046935) 26.04.2007 A61F 6/06 ABBOTT LABORATORIES
A system and compositions including zotarolimus and paditaxel are disclosed, as well as methods of delivery, wherein the drugs have effects that complement each other. Medical devices are disclosed which include supporting structures that include at least one pharmaceutically acceptable carrier or excipient, which carrier or excipient can include one or more therapeutic agents or substances, with the carrier including at least one coating on the surface thereof, and the coating associated with the therapeutic substances, such as, for example, drugs. Supporting structures for the medical devices that are suitable for use in this invention include, but are not limited to, coronary stents, peripheral stents, catheters, arterio-venous grafts, b...
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INHALATORY PHARMACEUTICAL COMPOSITIONS IN FORM OF DRY POWDERS, SOLUTIONS OR SUSPENSIONS

(WO2007045689) 26.04.2007 A61K 9/72 ERATECH S.r.l.
Inhalatory pharmaceutical composition comprising a drug, a soluble excipient and a surfactant, characterized by: - said soluble excipient is present in an amount between 10% and less than 100% by weight; - the weight ratio between said surfactant and said drug is between 0.01 and 10; - the particle size of at least 50% of the particles of said powder is below 5 Ám; - the bulk density db of said powder is between 0.1 and 0.3 g/cc; - the tapped density dt o f said powder is between 0.15 and 0.7 g/cc; - the ratio db/dt is between 0.2 and 0.65.
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PHARMACEUTICAL COMPOSITION COMPRISING POLYSACCHARIDES FROM ANGELICA GIGAS NAKAI FOR PREVENTION AND TREATMENT OF CANCER DISEASE

(WO2007037627) 05.04.2007 A61K 31/715 KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
Disclosed is a pharmaceutical composition for prevention and treatment of cancers, comprising Angelan, a polysaccharide isolated from Angelica gigas Nakai, as an active ingredient, and a pharmaceutically acceptable carrier, excipient or diluents. In detail, Angelan is excellent in the inhibition of cancer cell growth and the suppression of attachment and invasion of cancer cells to extracellular matrix, thereby inhibiting metastasis of cancer cells. In addition, when Angelan is taken in combination with an existing anticancer drug such as doxorubicin, synergic anticancer effects can be obtained.
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CONTROLLED RELEASE DOSAGE FORMULATION OF DULOXETINE

(WO2007034503) 29.03.2007 A61K 9/28 CADILA HEALTHCARE LIMITED
The preset invention provides a controlled release dosage form of duloxetine comprising a homogenous core comprised of duloxetine or its pharmaceutically acceptable salts, pharmaceutically acceptable polymeric carrier, solubility enhancer, a hydrophobic component, a hydrodynamic diffusion enhancer, a viscolyzing agent and pharmaceutically acceptable excipients; a entering coat on said core and a barrier layer between said core and the enteric coat.
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CHITOSAN-SILICON DIOXIDE COPRECIPITATE AND USE AS EXCIPIENT IN SOLID DOSAGE FORMS

(WO2007025715) 08.03.2007 A61K 47/02 THE JORDANIAN PHARMACEUTICAL MANUFACTURING CO.
Chitosan silicone dioxide coprecipitate composition, method of production thereof, pharmaceutical composition comprising the chitosan silicone dioxide coprecipitate composition and use of the chitosan silicone dioxide coprecipitate composition for manufacturing a sustained or immediate release formulation.
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COMPOUNDS FOR PHOTOCHEMOTHERAPY

(WO2007023398) 01.03.2007 A61K 41/00 UNIVERSITE DE GENEVE
Enzyme-activatable photosensitizing polymer conjugates are disclosed for photochemotherapeutic treatment of human diseases and disorders, bacteriologic or virologic indications, cosmetic applications and other pathologic situations. These polymer conjugates may comprise a polymer carrier, a photosensitizer, a quencher, a targeting molecule and/or a biocompatibilizing unit. These macromolecular conjugates may be designed to guide to the target tissue a photosensitizing agent in an inactive, non -phototoxic form. However, upon entering the target environment, in which certain enzymes are presently active, the conjugate may release its photosensitizers in its fully active form, resulting in a highly localized activation of the photoactive agent...
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BIFUNCTIONAL PROTEIN ANCHORS

(WO2007011216) 25.01.2007 A61P 35/00 APPLIED NANOSYSTEMS B.V.
The invention relates to the areas of immunology and vaccine delivery. More specifically, it relates to a bacterial vaccine delivery technology with built-in immunostimulatory properties which allows the immobilization of any antigen of interest, without prior antigen modification. Provided is an antigen-loaded immunogenic carrier complex comprising at least one bifunctional polypeptide attached to an immunogenic carrier, said bifunctional polypeptide comprising a peptidoglycan binding domain (PBD) through which the polypeptide is attached to said carrier, fused to an antigen binding domain (ABD) to which at least one antigen of interest is bound. Also provided is a pharmaceutical (e.g. vaccine) composition comprising an antigen-loaded immu...
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NOVEL PHARMACEUTICAL MODIFIED RELEASE DOSAGE FORM CYCLOOXYGENASE ENZYME INHIBITOR

(WO2007010559) 25.01.2007 A61K 9/20 PANACEA BIOTEC LTD.
Pharmaceutical modified release dosage form comprising at least one cyclooxygenase enzyme inhibitor or its pharmaceutically acceptable salts, esters, prodrugs, solvates, hydrates, or derivatives thereof as active agent, with a pharmaceutically acceptable carrier for controlling the release of the cyclooxygenase enzyme inhibitor is provided. The dosage form preferably provides a release of not more than about 60 % of the cyclooxygenase enzyme inhibitor in 1 hour and not less than about 75 % of the cyclooxygenase enzyme inhibitor after 12 hours when tested in accordance with the dissolution method (I) described herein employing Distilled water with 2.0 % Sodium lauryl sulphate as the dissolution medium or in accordance with the dissolution me...
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MODIFIED-RELEASE COMPOSITION OF AT LEAST ONE FORM OF VENLAFAXINE

(WO2006130843) 07.12.2006 A61K 9/20 BIOVAIL LABORATORIES INTERNATIONAL S.R.L.
The present invention relates to a modified release composition of at least one form of venlafaxine, which is a delayed controlled release composition. The composition comprises a core comprising at least one form of venlafaxine selected from the group consisting of venlafaxine, an active metabolite of venlafaxine, a pharmaceutically acceptable salt of venlafaxine, a pharmaceutically acceptable salt of an active metabolite of venlafaxine, and combinations thereof, less than 10% of a gelling agent and a pharmaceutically acceptable excipient. The composition further comprises a modified release coating which substantially surrounds the core which provides a delayed controlled release of the at least one form of venlafaxine.
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ORAL DOSAGE FORMS COMPRISING PROGESTERONE AND METHODS OF MAKING AND USING THE SAME

(WO2006128057) 30.11.2006 A61K 9/48 DURAMED PHARMACEUTICALS, INC.
The present invention relates to an oral pharmaceutical dosage form comprising micronized progesterone, an edible oil, an absorbing disintegrant, and a hydrophilic excipient. Particularly, the invention relates to a pharmaceutical dosage form wherein the dosage form is in a powder form and is contained in a pharmaceutically acceptable capsule. The present invention is also directed toward methods of making the dosage form, methods of using the dosage form, and kits comprising the dosage form.
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COMPRESSED PHARMACEUTICAL COMPOSITION COMPRISING COATED PELLETS AND A DIRECT COMPRESSION MIXTURE, AND METHOD OF PREPARATION THEREOF

(WO2006127637) 30.11.2006 A61K 9/26 ACTAVIS GROUP HF
A compressible mixture prepared from a waxy filler, cellulose filler, or a mixture thereof and a disintegrant is disclosed for the preparation of compressed pharmaceutical compositions containing coated pellets. The resulting compressed compositions exhibit substantially the same dissolution profiles as the pellets in the absence of the compressible mixture.
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SUSTAINED RELEASE MICROPARTICLES FOR PULMONARY DELIVERY

(WO2006124446) 23.11.2006 A61K 9/00 NEKTAR THERAPEUTICS
A composition of microparticles for delivery to the pulmonary system provides sustained release of a pharmaceutical agent. The microparticles comprise a lipid structural matrix comprising a multilamellar structure of lipid bilayers having lipid chains ordered in an L?L phase. The lipid matrix at least partially encapsulates the pharmaceutical agent at a bilayer interface formed between head groups of adjacent lipid layers. The microparticles are prepared by heating a precursor formulation comprising a solvent, matrix-forming excipient and pharmaceutical agent to a temperature above the liquid-crystalline transition temperature Tc of the matrix-forming excipient and below the melting or denaturation point of the pharmaceutical agent. The...
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PHARMACEUTICAL COMPOSITIONS COMPRISING OF ARSENOUS ACID, ITS SODIUM SALT AND ITS DERIVATIVES INTENDED FOR THE TREATMENT OF UROGENITAL CANCER AND ITS METASTASIS

(WO2006121280) 16.11.2006 A61K 33/36 KOMIPHARM INTERNATIONAL CO., LTD.
The present application relates to pharmaceutical compositions and methods for treatment of urogenital diseases and bone metastasis in a human, which pharmaceutical composition contains an effective amount of arsenous acid alkaline or earth alkaline metal salt and/or a pharmaceutically acceptable adjuvant. According to the present invention, the alkaline arsenous acid metal salt is sodium meta-arsenita(AsO2Na) or potassium meta-arsenite(AsO2K). The effective amount of arsenous acid alkaline or earth alkaline metal salt is 0.0001-1500 mg/kg, preferably 1- 1000 mg/kg, more preferably 1-150 mg/kg, and most preferably 50-100 mg/kg of body weight/day. The administration form of the pharmaceutical compositions of the invention is preferably oral, ...
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INHALATION DEVICE CONTAINING PLURAL DOSES OF A PHARMACEUTICAL COMPOSITION

(WO2006117353) 09.11.2006 A61K 31/46 BOEHRINGER INGELHEIM INTERNATIONAL GMBH
The invention relates to an inhalation device comprising plural of doses of a pharmaceutical composition in powder form, wherein the pharmaceutical composition comprises one or more, preferably one, anticholinergic^, optionally in combination with a pharmaceutically acceptable excipient.
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ORALLY DISINTEGRATING PHARMACEUTICAL TABLET FORMULATIONS OF OLANZAPINE

(WO2006115770) 02.11.2006 A61K 9/20 TEVA PHARMACEUTICALS USA, INC.
This invention provides orally disintegrating pharmaceutical tablet formulations comprising per tablet the following ingredients in the following percentages by weight: olanzapine as an active ingredient in an amount from about 2.5% to about 10%; mannitol in an amount from about 75% to about 95%; a disintegrating agent in an amount from about 1.0% to about 10%; and one or more excipient in a total amount of about 0.1% to about 10%. This invention also provides a method of treating a patient in need of treatment with olanzapine which comprises administering to the patient a therapeutically effective dose of the above pharmaceutical tablet formulations. Finally, this invention provides a method of producing the above pharmaceutical tablet for...
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CELLULOSIC FILMS INCORPORATING A PHARMACEUTICALLY ACCEPTABLE PLASTICIZER WITH ENHANCED WETTABILITY

(WO2006115712) 02.11.2006 A61K 9/20 EASTMAN CHEMICAL COMPANY
An enteric coating for a solid pharmaceutical carrier or substrate wherein the enteric coating includes a cellulosic polymeric material selected from selected from the group consisting of hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, methyl cellulose, ethyl cellulose, cellulose acetate, cellulose acetate butyrate, cellulose acetate phthalate, cellulose acetate succinate, cellulose acetate propionate, cellulose acetate trimellitate, hydroxypropylmethyl cellulose phthalate, hydroxypropylmethyl cellulose succinate, hydroxypropylmethyl cellulose acetate succinate, cellulose acetate succinate butyrate, cellulose acetate succinate propionate, carboxymethylcellulose sodium, cellulose butyrate, and mixtures thereo...
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PHARMACEUTICAL DOSAGE FORMS COMPRISING A LIPID PHASE

(WO2006115463) 02.11.2006 A61K 47/14 GALENICA TECHNOLOGY AB
A tablet for oral administration comprises a lipid phase, comprised to 80% by weight or more by a mixture of (a) triglyceride, (b) mono- or/and diglyceride, and (c) cell membrane lipid; (d) one or more pharmacologically active agents dissolved or dispersed in the lipid phase; (e) water and/or ethanol; and (f) an absorption controlling amount of particulate pharmaceutical excipient. Also disclosed are granules, a suppository for rectal administration, and a capsule filled with the granules . Methods for preparing the tablet, the suppositoriy and the granules are also disclosed as well as uses of the granules and a method for coating them.
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BENZIMIDAZOLE FORMULATION

(WO2006105798) 12.10.2006 A61K 9/28 NYCOMED DANMARK APS
A dry manufacturing process for the production of a pharmaceutical formulation of a benzimidazole and an alkaline substance is described. A tablet is compressed directly from a dry powder or a dry particulate matter avoiding any liquid or excipient conventionally used as a wet binder. The manufacturing process has the advantage of being simple and cost efficient. At the same time an expensive drying step is superfluous. The resulting pharmaceutical formulation has a good stability and a good dissolution profile.
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PHARMACEUTICAL PREPARATION COMPRISING PERINDOPRIL ERBUMINE AND METHOD OF PREPARATION AND STABILISATION THEREOF

(WO2006101462) 28.09.2006 A61K 9/16 VULM, a.s.
The subject matter of the invention is a pharmaceutical preparation comprising perindopril erbumine in a stable form within the rage 1 to 40 % by weight and at least one excipient and/or a mixture of excipients within the range 1 % - 99 % by weight, whereas at least one excipient is a substance of basic character maintaining pH 7.1 to 14. The subject matters of the invention are also a method of preparing, stabilising and packing of an oral pharmaceutical preparation in the dosage form of tablets, and/or coated tablets, and/or capsules which is used as an oral therapeutic of hypertension. The principle of manufacturing method consists in preparation of a compound comprising an alkalising excipient by dry mixing of powder components, and/or ...
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TRANSPORT OF NANO- AND MACROMOLECULAR STRUCTURES INTO CYTOPLASM AND NUCLEUS OF CELLS

(WO2006089668) 31.08.2006 A61K 47/48 LUDWIG-MAXIMILIANS-UNIVERSIT─T
The present invention refers to novel conjugate molecules and their use or the transport of nano- and macromolecular structures into cells and/or the nucleus. More particularly, the present invention refers to conjugate molecules containing a carrier, preferably thiopyridyl moieties, and a cargo moiety. Thereby, the thiopyridyl moiety is bound to the cargo moiety to act as a carrier, particularly for efficient intracellular and/or intranuclear delivery of drugs, nano-or macromolecular structures, etc.. The novel conjugate molecules are provided for the manufacture of a medicament for gene therapy, apoptosis, or for the treatment of diseases such as cancer, autoimmune diseases or infectious diseases.
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METHOD AND DEVICE FOR OPHTHALMIC ADMINISTRATION OF ACTIVE PHARMACEUTICAL INGREDIENTS

(WO2006082588) 10.08.2006 B05B 3/08 PHARMALIGHT INC.
Disclosed is the use of a mist of a pharmaceutical composition for ophthalmic delivery of a protein or peptide active pharmaceutical ingredient, a related method of treatment and a device useful in implementing the use and method. Disclosed is also the use of a mist for ophthalmic delivery of a pharmaceutical composition including a highly irritating penetration enhancer and an ophthalmically acceptable carrier, a related method of treatment and a device useful in implementing the use and method. Disclosed is also a device for ophthalmic administration configured to direct a mist of a pharmaceutical composition to the eye only when the eye is open. Disclosed is also a self-sterlizing device for ophthalmic administration. Disclosed is also a...
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A PHARMACEUTICAL COMPOSITION CONTAINING OLANZAPINE AS THE ACTIVE AGENT AND A PROCESS FOR THE PREPARATION THEREOF

(WO2006081779) 10.08.2006 A61K 9/20 ZENTIVA, A.S.
A pharmaceutical composition containing, as the active agent, olanzapine and further a filler and auxiliary substances, in the form of tablet obtainable by direct tabletting, the core of the tablet containing olanzapine in an amount of 0.5 to 20 w.% and a pharmaceutically acceptable filler in an amount of 35 to 99 w.%, preferably up to 95 w.%, with the particle sizes ranging from 10 to 1000 Ám, preferably from 50 to 400 Ám, the core being optionally coated, in which case the coating contains 1 to 10 w.% of polyethyleneglycol after drying. The pharmaceutically acceptable filler is selected from the series of microcrystalline cellulose, lactose, the polyalcohols mannitol or sorbitol, calcium hydrogenphosphate, and a combination of...
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PHARMACEUTICAL COMBINATION PREPARATION FOR ORAL DELIVERY FOR THE TREATMENT OF DIABETES MELLITUS

(WO2006080630) 03.08.2006 A61K 9/28 HANDOK PHARMACEUTICALS CO., LTD.
Disclosed are a combined pharmaceutical preparation for oral delivery for treatment of diabetes mellitus, comprising a) an inner layer comprising metformin or a pharmaceutically acceptable salt thereof, a swellable polymer and a pharmaceutically acceptable excipient, b) a drug- free intermediate layer comprising a water-soluble polymer, and c) an outer layer comprising glimepiride and a releasing controller; and a method for preparing the same.
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STABLE PHARMACEUTICAL FORMULATIONS OF ZONISAMIDE AND METHODS FOR THEIR MANUFACTURE

(WO2006078948) 27.07.2006 A61K 31/423 TEVA PHARMACEUTICAL INDUSTRIES LTD.
One of the embodiments of the present invention is directed toward a process for preparing a stable zonisamide pharmaceutical composition, comprising subjecting zonisamide to wet granulation with a granulation liquid to form a granulated mixture as the stable zonisamide pharmaceutical composition, wherein the granulation liquid is selected from purified water, alcohol and mixtures thereof. The stable zonisamide pharmaceutical composition can be used to fill capsule shells to prepare stable zonisamide capsules. Another embodiment of the invention concerns a for preparing a stable zonisamide pharmaceutical capsule, comprising (i) forming an intimate mixture with zonisamide powder and an effective amount of at least one pharmaceutically accept...
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ZINC-CONTAINING TREATMENTS FOR HYPERPHOSPHATEMIA

(WO2006072054) 06.07.2006 A61K 31/315 GENZYME CORPORATION
A method of treating hyperphosphatemia in a subject comprises the step of administering to the subject an effective amount of a pharmaceutically acceptable zinc salt. A pharmaceutical composition comprises a pharmaceutically acceptable carrier, a pharmaceutically acceptable zinc salt; and a phosphate sequestrant. In one embodiment, the phosphate sequestrant is selected from a pharmaceutically acceptable lanthanum, calcium, magnesium and iron salt. In another embodiment, the phosphate sequestrant is an amine polymer, wherein the molar ratio of a zinc ion of the ion salt to amine nitrogen atoms in the amine polymer is 0.1-3.0. The invention also includes a pharmaceutical composition comprising a pharmaceutically acceptable carrier; a pharmace...
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BILAYER TABLETS OF OXCARBAZEPINE FOR CONTROLLED DELIVERY AND A PROCESS OF PREPARATION THEREOF

(WO2006070406) 06.07.2006 A61K 9/24 J.B. CHEMICALS &PHARMACEUTICALS LTD
The present invention describes a bilayer tai et comprising (a) an immediate release first layer comprising an effective amount of oxcarbazepine and at least one pharmaceutically acceptable excipient and (b) a controlled release second. layer comprising an effective amount of oxcarbazepine and pharmaceutically acceptable excipients wherein total amount of oxcarbazepine impurities is less than or equal to about 2 % by weight. The present invention describes process for preparation of a controlled release bilayer tablets that is capable of delivering oxcarbazepine from one layer immediately followed by controlled delivery of oxcarbazepine from matrix forming layer. The present invention also describes process for preparation of oxcarbazepine ...
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PHARMACEUTICAL COMPOSITIONS OF AMORPHOUS ATORVASTATIN AND PROCESS FOR PREPARING SAME

(WO2006059224) 08.06.2006 A61K 9/16 WARNER-LAMBERT COMPANY LLC
Solid pharmaceutical compositions containing atorvastatin are disclosed. The compositions include a solid dispersion of amorphous atorvastatin and one or more optional pharmaceutically acceptable excipients. The solid dispersion is prepared by mixing crystalline atorvastatin with a melt-processible polymer and an optional stabilizer and an optional plasticizer at a temperature sufficiently high to soften or melt the polymer and to melt or dissolve the crystalline atorvastatin in the polymer, thereby forming a dispersion of amorphous atorvastatin.
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PHARMACEUTICAL PRODUCT

(WO2006055928) 26.05.2006 A61K 8/02 SMITHKLINE BEECHAM CORPORATION?
A pharmaceutical and pharmaceutical-like product is provided. The product provides a plurality of components having active agents that are delivered in a single delivery entity or vehicle. The product allows for selective control of the release rates of each of the active agents while still being delivered in a single product.
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SPONTANEOUSLY DISPERSIBLE PHARMACEUTICAL COMPOSITIONS

(WO2006050123) 11.05.2006 A61K 9/107 NOVARTIS AG
A spontaneously dispersible pharmaceutical composition comprising a poorly soluble drug and a carrier medium comprising (1) a lipophilic component, (2) a surfactant, and optionally (3) a hydrophilic component, wherein at least one of the components (1) to (3) is solid at room temperature. A particularly useful hydrophilic component in the system is a polymer that is solid at room temperature, e.g., solid PEG.
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TABLETS COMPRISING A POORLY COMPRESSIBLE ACTIVE AGENT AND TOCOPHEROL POLYETHYLENEGLYCOL SUCCINATE (TPGS)

(WO2006047067) 04.05.2006 A61K 9/16 EASTMAN CHEMICAL COMPANY
A solid composition suitable for forming into a tablet includes a pharmaceutically active substance in an amount sufficient to provide a therapeutic effect when administered; from 0.2 to 15 weight %, based on the total weight of the composition, of a water-soluble preparation of a fat- soluble vitamin; and from 10 to 80 weight %, based on the total weight of the composition, of an excipient. Another aspect of the present invention is method for making the solid composition.
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ANTIFUNGAL COMPOSITION APPLICABLE TO BODY TISSUE, PREFERABLY NAILS

(WO2006042324) 20.04.2006 A61K 9/08 QLT USA INC.
The present invention provides a non-water soluble, film-forming composition which adheres to body tissue and forms a pharmaceutical carrier to provide localized delivery of an antifungal agent to a treatment site. The composition will typically include: (a) an alkyl cellulose; (b) a hydroxyalkyl cellulose; (c) a pharmaceutically acceptable polar protic solvent; (d) an antifungal agent selected from the group of naftifine, ciclopirox, terbinafine, pharmaceutically acceptable salts thereof, and combinations thereof; (e) an glycol ether; (f) an antipruritic agent selected from the group of camphor, menthol, butamben picrate, metacresol, benzyl alcohol, camphorated metacresol, juniper tar, phenol, phenolate sodium, resorcinol, camphorated meta...
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PHARMACEUTICAL COMPOSITION AND METHOD FOR TREATING A JOINT CAPSULE ARTHROPATHY

(WO2006039704) 13.04.2006 A61K 31/38 JANSSEN PHARMACEUTICA, N.V.
A pharmaceutical composition for use in treating a joint-capsule arthropathy comprising an effective amount of one or more of a locally administered, optionally encapsulated therapeutic agent in admixture with a hyaluronic acid delivery vehicle and a method for use thereof in treating a joint-capsule arthropathy by intra-articular injection.
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A METHOD FOR PRODUCING ORAL SOLID DOSAGE FORM AND ORAL SOLID DOSAGE FORM PREPARED THEREBY

(WO2006034661) 06.04.2006 A61K 9/20 PLIVA-LACHEMA a.s.
The invention relates to a method for producing an oral solid dosage form capable of instantaneous release of the active substance which is a sparingly water-soluble antiestrogen, particularly tamoxifen citrate, characterized in that the antiestrogen is pre-mixed with a water-insoluble and/or alcohol-insoluble filler and optionally with at least one further pharmaceutically acceptable excipient, 80 % of particles of the filler or its mixture with at least one further pharmaceutically acceptable excipient being smaller than 355 micrometers and at most 10 % of these particles being smaller than 40 micrometers, whereupon the triturate obtained is mixed with a water-insoluble and/or alcohol-insoluble filler and with a water-soluble and/or alcoh...
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SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION

(WO2006032089) 30.03.2006 A61K 9/58 SMART DRUG SYSTEMS INC
A sustained release mini-implant including a silicone support material; and a pharmaceutically active composition carried in or on the silicone support rod; the pharmaceutically active composition including at least one pharmaceutically active component; and optionally a carrier therefor; the mini-implant providing a predetermined threshold blood level of pharmaceutical active for treatment of a selected indication.
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ORAL PHARMACEUTICAL COMPOSITION FOR TARGETED TRANSPORT OF A PLATINUM COMPLEX INTO THE COLORECTAL REGION, METHOD FOR PRODUCING AND USE AS MEDICAMENT THEREOF

(WO2006029579) 23.03.2006 A61K 31/282 PLIVA-LACHEMA A.S.
The invention relates to an oral pharmaceutical composition for targeted transport of a platinum complex into the colorectal region, characterized in that it comprises a mixture of platinum complex of general formula (I) wherein A each independently is an -NH3 group or an amino group containing 1 to 18 carbon atoms, B each independently is a halogen atom, a hydroxy group or a COOR group wherein R each independently is hydrogen atom or an alkyl, alkenyl, aryl, aralkyl, alkylamino or alkoxy group containing 1 to 10 carbon atoms or functional derivatives of these groups, and X each independently is a halogen atom or a monocarboxylate group containing 1 to 20 carbon atoms, or X together form a dicarboxylate group containing 2 to 20 carbon atoms...
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MULTIPARTICULATES OF PREFERABLY AN OPIOID, AND METHOD OF MANUFACTURING USING EXTRUSION

(WO2006024881) 09.03.2006 A61K 9/16 EURO-CELTIQUE S.A.
Extrusion of a mix containing a pharmaceutically active agent can be achieved using a plasticising excipient in an amount sufficient to act as plasticiser and also act as lubricant, thereby avoiding the need for inclusion of a lubricant. The invention provides multiparticulates with controlled release properties, substantially free of lubricant. The present invention is preferably directed to extruded multiparticulates containing an opioid such as oxycodone, an ammonium methacrylate copolymer such as Eudragit« RSPO, a plasticising excipient such as preferably stearyl alcohol and a water permeability modifier such as preferably Eudragit« RLPO. The obtained multiparticulates show a release rate profile which is pH- independent.
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COSMETIC OR PHARMACEUTICAL COMPOSITION FOR SKIN CARE

(WO2006023710) 02.03.2006 A61K 6/00 INFINITY2 HEALTH SCIENCES, INC.
The present invention relates to a cosmetic or pharmaceutical composition to reduce skin damage caused by aging and/or the environment. The composition can include a genus Centipeda plant extract, a trace metal source (such as a copper source) which can be in a skin absorbing form in an amount effective for activating or enhancing superoxide dismutase enzyme, and a carrier suitable for topical administration. The compound may alternatively include a genus Centipeda plant extract and a low molecular weight transporter and an ion-pair delivery system including a donating composition and an accepting composition, wherein the donating composition and the accepting composition are combined to form a bound ion-pair, and a carrier suitable for top...
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INTRANASAL DELIVERY OF ANTIPSYCHOTIC DRUGS

(WO2006023497) 02.03.2006 A61K 9/12 UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
An intranasal pharmaceutical composition is provided that comprises an antipsychotic drug, such as haloperidol, and a liquid vehicle. Methods of manufacture and administration of the composition are provided as well as methods of treatment of various psychotic episodes, diseases and/or disorders.
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PHARMACEUTICAL MULTILAYER TABLET FOR CONTROLLED RELEASE OF ACTIVE INGREDIENTS WITH HIGHLY PH-DEPENDENT SOLUBILITY

(WO2006010640) 02.02.2006 A61K 9/24 SANOFI-AVENTIS
The present invention relates to a pharmaceutical controlled release multilayer tablet comprising at least two layers, at least one active ingredient with highly pH-dependent solubility, at least one pharmaceutically acceptable pH maintaining excipient and at least one pharmaceutically acceptable matrix forming excipient, characterized in that said at least one active ingredient with highly pH-dependent solubility and said at least one pharmaceutically acceptable pH maintaining excipient are respectively comprised in at least one distinct layer.
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PHARMACEUTICAL COMPOSITION COMPRISING TIBOLONE AND PROCESS FOR PROCUDING THE SAME

(WO2005117899) 15.12.2005 A61K 31/57 CIPLA LIMITED
A pharmaceutical composition comprises tibolone, a water-solute starch and optionally a further pharmaceutical acceptable carrier. Preferred compositions comprise an inclusion complex of tibolone and a water-soluble starch, in particular cyclodextrin. A process for making a tablet comprising a composition of the invention comprises mixing tibolone cyclodextrin, a carrier and disintegrant; granulating with a binder; lubricating the granules with a lubricating agent; and compressing the granules to form tablets. In another embodiment, a process for making a composition of the invention comprises adding solvent to a premix comprising tibolone and a cyclodextrin; blending the ingredients to allow the complex to form; and formulating the blend a...
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COMPOSITIONS COMPRISING FLAVONOIDS AND TOCOTRIENOLS AND METHODS THEREOF

(WO2005115378) 08.12.2005 A61P 9/10 KGK SYNERGIZE INC
Disclosed in certain embodiments is a pharmaceutical formulation, such as a tablet, gel capsule, solution, liquid, suspension or emulsion, comprising a pharmaceutical ingredient comprising an active agent combination comprising flavonoids and tocotrienols in a ratio of about 75:25 to about 95:5 and at least one pharmaceutical acceptable excipient. The flavonoids may comprise naringenin, hesperetin, nobiletin or tangeretin. The tocotrienols may comprise alpha-tocotrienol, gamma- tocotrienol or delta-tocotrienol. The formulations may be used to lower total cholesterol, triacylglycerols, LDL cholesterol and Apo B.
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NOVEL EXTENDED RELEASE COMPOSITION OF VENLAFAXINE HYDROCHLORIDE CONTAINING POLYVINYL ACETATE

(WO2005112901) 01.12.2005 A61K 9/28 LUPIN LTD.
Extended release pharmaceutical composition of Venlafaxine hydrochloride comprising a pharmaceutically acceptable capsule containing minitablets. The minitablets comprise from about 20% to about 70% by weight effective amount of Venlafaxine hydrochloride, polyvinyl acetate, one or more pharmaceutically acceptable excipients. The minitablets have diameter from about 1 mm to 5 mm and are coated with a release controlling composition.
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METHOD OF USE OF CARBOXYLATED POLYSACCHARIDES TOPICALLY ON THE EYEBALL

(WO2005110430) 24.11.2005 A61K 31/70 MICHIGAN STATE UNIVERSITY
The use of chemically modified dicarboxy polysaccharides for the topical treatment of the eyeball are described. The modified polysaccharides provide a carrier in solutions for the treatment of the eyeball to obtain a timed release.
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DRY POWDER PHARMACEUTICAL COMPOSITION, ITS PREPARATION PROCESS AND STABLE AQUEOUS SUSPENSION OBTAINED FROM SUCH COMPOSITION

(WO2005102283) 03.11.2005 A61K 9/16 ERATECH S.R.L.
Pharmaceutical composition in a dry powder form comprising at least one hydrophobic active principle, at least one water-soluble excipient and at least one surfactant, wherein the particles in said dry powder state have a Volume Mean Diameter VMDd greater than the Volume Mean Diameter VMDwof particles in a suspension obtained from said pharmaceutical composition at standard conditions of dispersion in a water-medium. It is also disclosed a process to prepare such dry composition and an extemporaneous suspension for inhalation therapy obtainable from said dry composition.
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PHARMACEUTICAL COMPOSITIONS COMPRISING AN AMPHIPHILIC STARCH

(WO2005099674) 27.10.2005 A61K 9/20 VECTURA LIMITED
The present invention relates to controlled or sustained release solid pharmaceutical compositions, to pharmaceutical excipients for use in the manufacture of such compositions and to methods of producing such compositions and excipients. The controlled or sustained release excipients include a release controlling excipient comprising an amphiphilic starch.
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PHARMACEUTICAL COMPOSITION AND METHOD FOR THE TRANSDERMAL DELIVERY OF MAGNESIUM

(WO2005091872) 06.10.2005 A61F 13/00 BRIERRE, Barbara, T.
The present invention relates to a method and transdermal pharmaceutical composition for preventing magnesium deficiency or imbalances associated with magnesium deficiency including diabetes, hypertension, high cholesterol, cardiac arrhythmias, acute myocardial infarction, arteriosclerosis, atherosclerosis, preeclampsia, dysautonomia, mitral valve prolapse, asthma, constipation, irritable bowel syndrome, migraines, muscle spasms and cramping, premenstrual syndrome, osteoporosis, kidney stones, chronic fatigue syndrome, and fibromyalgia. The transdermal pharmaceutical composition includes a therapeutically effective amount of a pharmaceutically acceptable salt of magnesium and a pharmaceutically acceptable carrier. A therapeutically effectiv...
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BIOAVAILABLE SOLID DOSAGE FORMS OF METAXALONE

(WO2005087204) 22.09.2005 A61K 9/20 SPIREAS, Spiridon
Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin« 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin« tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a non...
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PHARMACEUTICAL COMPOSITION CONTAINING PLATINUM COMPLEX AS ACTIVE SUBSTANCE AND METHOD OF MANUFACTURING THEREOF

(WO2005077357) 25.08.2005 A61K 9/16 PLIVA-LACHEMA A.S.
The invention relates to a pharmaceutical composition containing as active substance a platinum complex of general formula (I), wherein A, A', B, B', X and X' have specific meanings, in a mixture with at least one pharmaceutically acceptable excipient, this composition being characterized in that it is a granulate of particle size less than 0.5 mm, prepared by wet granulation of water-wetted mixture of tetravalent platinum complex of general formula (I), at least one neutral saccharide and at least one natural and/or modified polysaccharide, and is optionally contained in a capsule or a sachet or is optionally compressed into a tablet, the surface of the granulate, capsule or tablet being coated with a layer of at least one pharmaceutically...
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SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS OF A HIV PROTEASE INHIBITOR

(WO2005063209) 14.07.2005 A61K 9/107 TIBOTEC PHARMACEUTICALS LTD.
The present invention relates to pharmaceutical formulations of (3R,3aS,6aR)--hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate, salts, esters, polymorphic and pseudopolymorphic forms thereof, which are self- microemulsifying drug delivery systems and comprise as carrier a lipophilic phase, one or more surfactants, a hydrophilic solvent and a nucleation inhibitor.
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PHARMACEUTICAL COMPOSITIONS COMPRISING LERCANIDIPINE

(WO2005053689) 16.06.2005 A61K 31/44 LIFECYCLE PHARMA A/S
A controlled release pharmaceutical composition comprising lercanidipine dissolved or dispersed in a solid vehicle at ambient temperature, thus forming a solid dispersion, achieves delayed release of lercanidipine over an extended period of time, reduced food effect and increased bioavailability compared to commercially available lercanidipine containing products.
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PHARMACEUTICAL COMPOSITIONS COMPRISING DANAZOL

(WO2005053660) 16.06.2005 A61K 9/14 LIFECYCLE PHARMA A/S
A controlled release pharmaceutical comprising danazol has the property of slow release of danazol over an extended period of time and markedly increased bioavailability compared to commercially available danazol-containing products. The pharmaceutical composition comprises danazol dissolved in a solid vehicle or carrier and is especially suitable for oral solid dosage forms. The composition significantly reduces food effect and may reduce side effects.
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AZITHROMYCIN DOSAGE FORMS WITH REDUCED SIDE EFFECTS

(WO2005053650) 16.06.2005 A61K 9/16 PFIZER PRODUCTS INC.
An oral dosage form comprising azithromycin and an effective amount of an alkalizing agent. Preferably, said oral dosage form comprises an effective amount of an alkalizing agent and an azithromycin multiparticulate wherein said multiparticulate comprises azithromycin, a mixture of glyceryl monobehenate, glyceryl dibehenate and glyceryl tribehenate, and a poloxamer. Typically, the oral dosage form includes any suitable oral dosing means such as a powder for oral suspension, a unit dose packet or sachet, a tablet or a capsule.Additionally disclosed is an oral suspension comprising azithromycin, an effective amount of an alkalizing agent and a vehicle. Preferably, the azithromycin is in multiparticulate form wherein said multiparticulate comp...
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IMPROVED ANTIPERSPIRANT METHODS AND COMPOSITIONS

(WO2005051337) 09.06.2005 A61K 8/81 THE PROCTER &GAMBLE COMPANY
An antiperspirant compositions and corresponding methods of application wherein the compositions comprise a) a skin-adhering system comprising i) a skin-adhering polymer, ii) one or more volatile solvents; b) antiperspirant active; c) thickening agent; and d) an anhydrous carrier in an amount sufficient to provide enhanced substantivity of antiperspirant actives.
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FIBER RICH FRACTION OF TRIGONELLA FOENUM-GRACEUM SEEDS AND ITS USE AS A PHARMACEUTICAL EXCIPIENT

(WO2005049211) 02.06.2005 A23L 1/308 RUBICON RESEARCH PRIVATE LIMITED
A novel solvent free process of obtaining an insoluble fiber rich fraction from Trigonella Foenum-graceum seeds is disclosed. The multifunctional fiber rich fraction (FRF) and highly purified FRF are useful as excipients for pharmaceutical dosage forms for various routes of administration. These excipients can be used as binder, disintegrant, filler, dispersing agent, coating agent, film forming agent, thickener and the like, for preparation of variety of dosage forms. FRF and highly purified FRF can also be used in a controlled release, targeted release and other specialized delivery systems, as well as in food and cosmetics formulation.
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BIODEGRADABLE OXIDIZED CELLULOSE ESTERS AND THEIR USES AS MICROSPHERES

(WO2005047339) 26.05.2005 A61K 9/16 UNIVERSITY OF IOWA RESEARCH FOUNDATION
A new cellulose excipient, OCCAE, suitable for use as a binder, filler, and/or disintegrant in the development of solid dosage forms and as a bodying agent or a drug carrier in the preparation of topical formulations is described. The cellulose excipient is formed by reacting an oxidized cellulose ester with an alcohol in the presence of a catalyst. The invention also describes the formation of controlled release microspheres using OCCAE and/or oxidized cellulose esters that may be used to control the release of drug in a patient over a time period of several hours to several days.
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GAMMA-TOCOPHEROL THERAPY FOR RESTENOSIS PREVENTION

(WO2005039443) 06.05.2005 A61F 2/02 MEDLOGICS DEVICE CORPORATION
A stent is provided in combination with delivery of a tocopherol agent, and in particular a des-methyl tocopherol agent, and further beneficially a gamma-tocopherol agent, so as to reduce restenosis along the vessel or other lumenal wall where the stent is implanted. In particular applications, the stent is an endolumenal stent, and more specific beneficial applications is an endovascular stent, and the gamma-tocopherol elutes from a coating or carrier coupled with the stent. Certain combinations are provided with the des-methyl-tocopherol or phytyl substituted chromanol, e.g. gamma-tocopherol, combined with an additional agent such as an anti-restenosis agent, e.g. sirolimus, tacrolimus, everolimus, or paclitaxel, in order to provide syner...
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MODIFIED RELEASE COMPOSITIONS COMPRISING TACROLIMUS

(WO2005020993) 10.03.2005 A61K 9/16 LIFECYCLE PHARMA A/S
A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.
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PHARMACEUTICAL DESMOPRESSIN COMPOSITION AS SOLID DOSAGE FORM AND METHOD FOR MANUFACTURING THEREOF

(WO2005011640) 10.02.2005 A61K 9/20 FERRING B.V.
The invention relates to a novel pharmaceutical composition as a solid dosage form comprising desmopressin, or a pharmaceutically acceptable salt thereof, as a therapeutically active ingredient together with a pharmaceutically acceptable excipient, diluent or carrier, or mixture thereof, wherein the pharmaceutical composition is composed of a compressed granulate and contains lubricant in an amount of from 0.05 to less than 0.50 percent by weight of said pharmaceutical composition.
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CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION

(WO2004108162) 16.12.2004 A61K 9/20 BIOKEY, INC.
Embodiments of the invention generally provide pharmaceutical drug compositions, methods of preparing oral drug compositions, such as extended release dosage compositions, and methods for treating infection. More particularly, the invention relates to formulations containing a drug and a carrier material. In one aspect, the invention provides a pharmaceutical formulation including a therapeutically active agent, from about 0.1% to about 4.9% by weight of a pharmaceutically acceptable polymer, and from about 0.1% to about 30% by weight of a pharmaceutically acceptable acid, wherein the pharmaceutical composition have a zero order release profile of the therapeutically active agent. In another aspect, the invention provides methods for prepar...
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DRUG DELIVERY SYSTEMS FOR TUMOR TARGETING NGR-MOLECULES AND USES THEREOF

(WO2004105782) 09.12.2004 A61K 9/127 G. GASLINI CHILDREN'S HOSPITAL
The present invention relates to targeted delivery systems for delivering therapeutic agents to tumor. The invention further relates to methods of delivering a therapeutic agent to a tumor for the prevention and treatment of cancer by killing tumor cells and tumor associated endothelial cells. In particular, the present invention provides a tumor-targeted drug delivery system comprising a NGR-containing molecule linked to a delivery vehicle encapsulating a therapeutic agent, preferably a drug, such as a cytotoxic agent or a chemotherapeutic agent. Specifically, the delivery systems of the present invention are capable of delivering an increased amount of therapeutic agent to a tumor as compared to other delivery systems. In particular, the ...
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PHARMACEUTICAL COMPOSITION BASED ON AGONIST OF BENZODIAZEPINE

(WO2004105767) 09.12.2004 A61K 9/00 SIGMA PHARMA LTDA.
The present invention describes the use of pharmaceutical compounds in pharmaceutical compositions for sublingual administration, including as active ingredient thereof, an agonist of the central receptor of benzodiazepinics chosen among diazepam, lorazepam, bromazepam, triazolam, alprazolam, flunitrazepam, nitrazepam and midazolam maleate, in a mixture with a pharmaceutical excipient consisting of, at least, 70% of the weight of the final formulation containing 40 - 45% by weight of lactose, 15- 27% by weight of sorbitol and 12 - 16% by weight of cellulose.
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NASAL FORMULATIONS INCLUDING A TOPICAL DECONGESTANT AND A TOPICAL CORTICOSTEROID AND THEIR USE IN TREATMENT OF OBSTRUCTIVE SLEEP APNEA

(WO2004105731) 09.12.2004 A61K 31/137 TEDOR PHARMA, INC.
A pharmaceutical formulation is provided for nasal drug administration of a topically administrable decongestant, a topically administrable corticosteroid and a pharmaceutically acceptable carrier, and may optionally include further carriers, therapeutic extenders, and the like. Such formulations may also optionally further include a therapeutically active member selected from the group consisting of a topical antibiotic, a topical antihistamine (preferably a non-sedating antihistamine), a leukotriene D4 antagonist, a 5-lipoxygenase inhibitor, and a FLAP antagonist, or a pharmaceutically acceptable salt thereof. In addition, methods for using the formulation to treat decongestant/corticosteroids-responsive conditions, diseases or disorders ...
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COMPOSITIONS FOR INDUCING IMMUNE RESPONSES

(WO2004098509) 18.11.2004 A61K 39/21 CHIRON CORPORATION
The invention provides, inter alia, immunogenic compositions comprising a first antigen, at least two adjuvants, wherein a first adjuvant comprises a polymer derived from poly(lactides) and/or poly (lactide-co-glycolides), and wherein a second adjuvant comprises an imidazoquinoline, wherein said first antigen is encapsulated within, adsorbed or conjugated to, co-lyophilized or mixed with said first adjuvant, and a pharmaceutically acceptable excipient, wherein said composition elicits a cellular immune response when administered to a vertebrate subject. The invention also provides methods of producing immunogenic compositions, methods for producing a cytotoxic-T lymphocyte (CTL) response in a vertebrate subject, and methods of immunization.
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PHARMACEUTICAL COMPOSITION CONTAINING RIBAVIRIN AS ACTIVE SUBSTANCE AND METHOD OF MANUFACTURING THEREOF

(WO2004096187) 11.11.2004 A61K 9/16 PLIVA-LACHEMA a.s.
The invention relates to a pharmaceutical composition which is a freely flowing granulate prepared using the wet granulation of a mixture, wetted with water, of ribavirin, at least one pharmaceutically acceptable filler selected from the group including cellulose and its derivatives and carbonates, phosphates, sulfates and silicates of metals, and optionally at least one pharmaceutically acceptable excipient, and also a method of the manufacture thereof. The pharmaceutical composition according to the invention ensures the perfect stability of the composition, even in case of a high ratio of the active substance in it, and the immediately release of the active substance from a dosage form, when administered orally in the form of capsules or...
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SOLID DOSAGE FORM COMPRISING DESMOPRESSIN

(WO2004096181) 11.11.2004 A61K 9/20 FERRING B.V.
The present invention relates to a novel pharmaceutical composition as a solid dosage form comprising desmopressin as a therapeutically active ingredient, and to a method for manufacturing thereof. The invention relates to a pharmaceutical composition as a solid dosage form comprising desmopressin, or a pharmaceutically acceptable salt thereof, as a therapeutically active ingredient together with a pharmaceutically acceptable excipient, diluent or carrier, or mixture thereof, wherein at least one of said excipient, diluent and carrier is a substance selected from a monosaccharide, disaccharide, oligosaccharide and a polysaccharide, wherein the said substance has an average particle size in the range of from 60 to 1 000 Ám. A method ac...
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SOLID DRUG FORMULATION AND DEVICE FOR STORAGE AND CONTROLLED DELIVERY THEREOF

(WO2004096176) 11.11.2004 A61K 9/00 BOSTON SCIENTIFIC SCIMED INC.
Devices and methods are provided for the storage and controlled release of a solid form of a drug. The device comprises a body portion; one or more reservoirs located in and defined by the body portion; a solid matrix which comprises a drug and which is contained in each of the one or more reservoirs; and one or more excipient materials dispersed throughout pores or interstices within the solid matrix and substantially filling any space not otherwise occupied by the solid matrix within each of the one or more reservoirs, wherein the excipient material enhances stability of the drug while stored in the one or more reservoirs or enhances release of the drug from each reservoir. In an alternative embodiment, the device provides for the storage...
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ORAL PHARMACEUTICAL DELIVERY SYSTEM WITH IMPROVED SUSTAINED RELEASE

(WO2004096150) 11.11.2004 A61K 9/20 SHEAR/KERSHMAN LABORATORIES, INC.
A solid oral delivery system having improved sustained release properties made of at least one lipid, dry particles including at least one pharmaceutical, and at least one filler, wherein the dry particles are continuously coated by the lipid and form a homogeneous suspension with the lipid, wherein the suspension, when melted, exhibits thixotropic and/or pseudoplastic properties, wherein the suspension is formed into the desired dose by molding or pouring the suspension when in a liquid or semi-liquid state. The process for preparing the present delivery system by melting the lipid, blending the dry particles which include the pharmaceutical, at least one filler and, optionally, flavorings with the melted lipid, and pouring or molding the ...
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PHARMACEUTICAL COMPOSITION CONTAINING PLATINUM COMPLEX AS ACTIVE SUBSTANCE AND METHOD OF MANUFACTURING THEREOF

(WO2004087126) 14.10.2004 A61K 9/16 PLIVA-LACHEMA A.S.
The invention relates to a pharmaceutical composition containing the platinum complex of formula (I) as an active substance where A, A', B, B', X and X' have specific meanings, in a mixture with at least one pharmaceutically acceptable excipient, characterized in that it is formed of a granulate with particles smaller than 0.5 mm in size prepared by wet granulation of a mixture of platinum complex of tetravalent platinum of formula (I) wetted by water, at least one neutral saccharide and at least one native and/or modified polysaccharide, being optionally contained in a capsule or a sack or being optionally pressed into the form of a tablet, while the surface of the granulate, the capsule or the tablet is optionally coated with a layer of a...
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OIL-CONTAINING, ORALLY ADMINISTRABLE PHARMACEUTICAL COMPOSITION FOR IMPROVED DELIVERY OF A THERAPEUTIC AGENT

(WO2004087052) 14.10.2004 A61K 9/48 LIPOCINE, INC.
The present invention relates to oral pharmaceutical compositions and methods for improved delivery of therapeutic agents, e.g., lipid- regulating agents. Compositions of the present invention include a carrier, where the carrier contains a combination of a triglyceride and at least two surfactants, at least one of which is hydrophilic. Upon dilution with an aqueous medium, the composition forms a clear, aqueous dispersion. The invention also pertains to methods for treating lipid disorders such as hypercholesterolemia, hypertriglyceridemia, and mixed dyslipidemia by oral administration of the compositions provided.
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PHARMACEUTICAL COMPOSITIONS FOR NASAL DELIVERY

(WO2004075824) 10.09.2004 A61K 9/00 BRITANNIA PHARMACEUTICALS LIMITED
According to the invention there is provided a powdered pharmaceutical formulation suitable for nasal delivery which is a freeze- dried blend of active material and excipient(s) containing: 0.5 - 50 % by wt of active material 50 - 99.5 % by wt of excipient(s), and in which at least 0.1 % by wt of the blend is an amorphous state, which can be directly obtained by freeze drying without the need for milling and without containing the pronounced low particles defined as finings. Such powders retain free-flowing properties on storage, are physically and chemically stable and are readily soluble.
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SEMI-SOLID IMMEDIATE-RELEASE ORAL FORMULATIONS COMPRISING AN ANTICANCER HYDROPHOBIC AGENT, A POLYGLYCOLISED GLYCERIDE AND A HYDROPHILIC CARRIER

(WO2004073592) 02.09.2004 A61K 9/48 PHARMACIA ITALIA S.P.A.
The present invention relates to a pharmaceutical composition suitable for oral administration, in the form of semisolid matrix, comprising an active ingredient poorly soluble in water and present in a quantity of from 15 to 45% by weight of the percent composition of the pharmaceutical composition; a surfactant agent constituted by a polyglycolised glyceride; and a pharmaceutically acceptable hydrophilic carrier.
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SUGAR-FREE ORAL TRANSMUCOSAL SOLID DOSAGE FORMS AND USES THEREOF

(WO2004069198) 19.08.2004 A61K 9/00 CEPHALON, INC.
The present invention is directed to oral solid dosage forms. The solid dosage forms are sugar-free, and comprise a pharmaceutical agent and a suitable pharmaceutically acceptable excipient. Preferably, the solid dosage forms of the present invention are bioequivalent to a sugar- containing solid dosage form. Bioequivalence is preferably obtained by incorporating an ionizing agent, more preferably in the form of a buffer system, into the solid dosage forms, in an amount sufficient to maintain a portion of the pharmaceutical agent, upon dissolution of said composition in saliva, in an ionized state.
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OSTEOGENIC COMPOSITION

(WO2004067027) 12.08.2004 A61K 31/4015 THE UNIVERSITY OF ZURICH
The present invention relates to pharmaceutical composi-tions containing a synergistic amount of at least one bone morphogenetic protein (BMP) and a synergistic amount of at least one pyrrolidone optionally in a pharmaceutically acceptable carrier, such as a biodegradable polymer. The present invention further relates to methods of treating or-thopaedic and dental, including periodontal, diseases by simultaneously administering a synergistic amount of at least one bone morphogenetic protein (BMP) and a syner-gistic amount of at least one pyrrolidone optionally in a pharmaceutically acceptable carrier to patients in need of such treatment.
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ORAL CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION CONTAINING METAXALONE AS ACTIVE AGENT

(WO2004066981) 12.08.2004 A61K 9/00 SUN PHARMACEUTICAL INDUSTRIES LIMITED
The present invention provides an oral controlled release pharmaceutical composition comprising metaxalone, a pharmaceutically acceptable release rate controlling excipient, and pharmaceutically acceptable excipients, wherein the oral controlled release pharmaceutical composition provides peak plasma levels at a time of about 3 hours or more after oral administration of the composition.
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MODIFIED RELEASE FORMULATIONS OF SELECTIVE SEROTONIN RE-UPTAKE INHIBITORS

(WO2004058229) 15.07.2004 A61K 9/20 BIOVAIL LABORATORIES INC.
A modified release pharmaceutical composition for oral administration, suitable for once daily dosing, comprising a form of at least one selective serotonin re-uptake inhibitor (SSRI) selected from the group consisting of SSRIs, racemic mixtures thereof, enantiomers thereof, pharmaceutically acceptable salts thereof, and combinations thereof in combination with at least one pharmaceutically-acceptable excipient wherein the pharmaceutical composition exhibits the following in vitro dissolution profile when measured using the USP Paddle Method at 100 rpm in 900 mL of a buffered medium having a pH between about 5.5 and about 7.5 at 37.0 ▒ 0.5 ░C: (a) between about 0% and about 50% (by wt) of the form of the at least one SSRI is rele...
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FILM COATED TABLET COMPRISING AN EXTRACT OF RED VINE LEAVES

(WO2004058227) 15.07.2004 A61K 9/20 BOEHRINGER INGELHEIM INTERNATIONAL GMBH
The invention relates to a film coated tablet comprising the following constituents: a) at least 50 % by weight of a dried extract of red vine leaves, which is obtainable by extraction of red vine leaves with water and drying; b) up to 50 % by weight of an excipient consisting essentially of at least one binder, at least one disintegrant, at least one filler, and a lubricant; and c) a tablet film consisting essentially of a film former, a plastiziser, a coating agent and optionally a coloring agent.Furthermore, the invention relates to an aqueous extract of red vine leaves is obtainable by a method comprising the steps of: a) collecting red vine leaves at a point of time when the content in flavonoids has reached an optimum; b) drying and c...
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COMPOSITIONS AND METHODS OF DELIVERY OF PHARMACOLOGICAL AGENTS

(WO2004052401) 24.06.2004 A61K 47/18 AMERICAN BIOSCIENCE, INC.
The present invention relates to a pharmaceutical composition comprising a pharmaceutical agent and a pharmaceutically acceptable carrier, which carrier comprises a protein, for example, human serum albumin and/or deferoxamine. The human serum albumin is present in an amount effective to reduce one or more side effects associated with administration of the pharmaceutical composition. The invention also provides methods for reducing one or more side effects of administration of the pharmaceutical composition, methods for inhibiting microbial growth and oxidation in the pharmaceutical composition, and methods for enhancing transport and binding of a pharmaceutical agent to a cell.
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PHARMACEUTICAL COMPOSITIONS FOR THE PULMONARY DELIVERY OF AZTREONAM

(WO2004052333) 24.06.2004 A61K 9/19 PARI GMBH
The invention relates to pharmaceutical compositions for the delivery of therapeutic compounds to the respiratory system. More in particular, it deals with improved formulations of an antibiotic compound to prevent and treat bacterial infections of the respiratory system. The invention provides a solid pharmaceutical composition for the preparation of an aerosolizable liquid for inhalatin, comprising an effective amount of aztreonam and a basic excipient, wherein the ratio of aztreonam to the basic excipient is selected to yield a solution with a pH of about 3.5 to 5.5 when dissolved in water at an aztreonam concentration of about 30 to 200 mg/ml. Furthermore, the invention provides a pharmaceutical kit for the preparatin of an aerosolizabl...
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PHARMACEUTICAL COMPOSITIONS HAVING A MODIFIED VEHICLE

(WO2004045646) 03.06.2004 A61K 31/545 PHARMACIA &UPJOHN COMPANY LLC
A composition comprising: (a) one to three bioactive agents; and (b) a vehicle comprising; (i) a modified liquid carrier, and (Ř) an un- modified liquid carrier wherein the ratio by volume of the modified liquid carrier to the un-modified liquid carrier is between 0.00001:99.99999 to less than 0.01:99.99, that provide the composition with predictable sustained-release properties and wherein immediately after manufacture of the composition, said composition can be administered to a host such that the one to three bioactive agents are released to the host on a sustained basis.
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GASTRIC ACID SECRETION INHIBITING COMPOSITION

(WO2004035090) 29.04.2004 A61K 9/00 OREXO AB
An oral pharmaceutical dosage form comprises pharmacologically effective amounts of an acid-susceptible proton pump inhibitor and an H2 receptor antagonist in combination with at least on pharmacologically acceptable excipient which causes a delayed release and/or an extended release of the proton pump inhibitor. The H2 receptor antagonist is included in the dosage form in such a way that it is rapidly released after administration. This dosage form is suitable for the treatment of conditions associated with an excessive secretion of gastric acid and provides a suitable combination of a rapid onset and a long-lasting duration of the effect. The invention also relates to a method for manufacturing such a dosage form and to a method for the t...
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METHODS OF DRUG DELIVERY USING SULPHATED CHITINOUS POLYMERS

(WO2004018010) 04.03.2004 A61K 31/727 CHITOGENICS, INC.
The present invention provides methods and compositions for delivering a therapeutic agent across a membrane that has limited permeability for the therapeutic agent. The method includes delivering the therapeutic agent to the membrane in a composition which includes a sulphated chitinous polymer as a primary carrier.
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PRAMIPEXOLE ONCE-DAILY DOSAGE FORM

(WO2004010999) 05.02.2004 A61K 9/20 PHARMACIA CORPORATION
An orally deliverable pharmaceutical composition comprises a therapeutically effective amount of pramipexole or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipients, said composition exhibiting at least one of (a) an in vitro release profile wherein on average no more than about 20% of the pramipexole is dissolved within 2 hours after placement of the composition in a standard dissolution test; and (b) an in vivo pramipexole absorption profile following single dose administration to healthy adult humans wherein the time to reach a mean of 20% absorption is greater than about 2 hours and/or the time to reach a mean of 40% absorption is greater than about 4 hours. The composition is useful for ora...
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PACKAGING AND DISPENSING OF RAPID DISSOLVE DOSAGE FORM

(WO2004009445) 29.01.2004 A61J 3/07 KOSMOS PHARMA
An oral dosage delivery vehicle comprising an edible film including a uniformly distributed active ingredient, wherein said film comprises dosage units releasably joined by one or more weakened sections, which permit said dosage units to be detached from said film.
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INTRANASAL PHARMACEUTICAL COMPOSITIONS COMPRISING AN ANTIHISTAMINE AND A LEUKOTRIENE INHIBITOR

(WO2003101434) 11.12.2003 A61K 9/00 BHATTACHARYA, Sampad
A pharmaceutical composition in the intranasal delivery to the nasal mucosa for prevention and treatment of symptoms of allergic rhiities and problems like nasal polyps comprising of Loratadine or Desloratadine which are potent antihistamine and solubilised at pharmaceutically acceptable pH of 4 to 8 which does not cause any irritation in the nose and permits the application of potent antihistamine at the site of action the nasal mucosa in lesser doses and without any side effect with immediate onset of action. Montelukast Sodium in combination with Loratadine would be very effective and gives some effect as intranasal steroids that without any side effects. Addition of pharmaceutical acceptable delivery vehicle help in forming intranasal a...
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BIGUANIDE FORMULATIONS

(WO2003099214) 04.12.2003 A61K 9/16 ANDRX CORPORATION
In certain embodiments, the invention is directed to a pharmaceutical dosage form consisting essentially of a single phase matrix comprising metformin; or a pharmaceutically acceptable salt thereof and at least one controlled release excipient; said dosage form providing a mean Tmax of metformin from about 3 to about 12 hours after administration to human patients.
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USE OF COMPLETELY LINEAR SHORT CHAIN ALPHA-GLUCANS AS A PHARMACEUTICAL EXCIPIENT

(WO2003097017) 27.11.2003 A61K 9/20 NATIONAL STARCH AND CHEMICAL INVESTMENT HOLDING COPORATION
This patent pertains to a tablet comprising as a binder a low amylose starch, which has been fully debranched using isoamylase and the method of making such tablet. Such binders are useful in any tabletting method, including direct compression, and can be used as a replacement for microcrystalline cellulose.
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MATERIALS AND METHODS FOR PREVENTION AND TREATMENT OF RNA VIRAL DISEASES

(WO2003092618) 13.11.2003 A61K 38/51 UNIVERSITY OF SOUTH FLORIDA
The subject invention concerns a method of inhibiting an RNA virus infection within a patient by increasing the amount of 2-5 oligoadenylate (2-5 AS) activity within the patient. Preferably, the preventive and therapeutic methods of the present invention involve administering a nucleotide encoding 2-5 AS, or at least one catalytically active fragment thereof, such as the p40, p69, p100 subunits to a patient in need thereof. The present inventors have determined that overexpression of 2-5AS causes a reduction in epithelial cell damage, reduction in infiltration of mononuclear cells in the peribronchiolar and perivascular regions, and reduction in thickening of the septa in the lungs. Levels of chemokines, such as MIP1-?, are also reduced...
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PHARMACEUTICAL COMPOSITIONS COMPRISING A DECONGENSTANT AND FURTHER ACTIVE INGREDIENTS FOR TREATING COUGH AND FLU

(WO2003089007) 30.10.2003 A61K 31/137 ADCOCK INGRAM INTELLECTUAL PROPERTY (PROPRIETARY) LIMITED
A pharmaceutical composition comprises a combination of a decongestant such as phenylephrine, pseudoephedrine or phenylpropanolamine or a pharmaceutically acceptable salt or derivative thereof, and at least one other active ingredient selected from a non-steriodal anti- inflammatory, an anti-histamine, a local anaesthetic, an antiseptic anaesthetic and a cough suppressant, and a pharmaceutically acceptable carrier. The pharmaceutical composition, which is provided in the form of a lozenge, tablet, capsule, mouthwash, gargle or spray, in particular a lozenge, is suitable for the symptomatic relief of cough and flu, including but not limited to that associated with sore throats and congested nasal passages.
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MELOXICAM SUPPOSITORIES CONTAINING E.G. POLYETHYLENGLYCOL

(WO2003082297) 09.10.2003 A61K 9/00 BOEHRINGER INGELHEIM INTERNATIONAL GMBH
The present invention relates to a suppository essentially consisting of the active ingredient meloxicam or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient.
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HIGHLY AQUEOUS LIQUID CARRIER FORMULATIONS

(WO2003082242) 09.10.2003 A61K 47/26 BATTELLEPHARMA, INC.
Disclosed is a liquid carrier vehicle for a dissolved or suspended pharmaceutically active agent administered to a patient via inhalation of an aerosol where the aerosol is produced by an electrohydrodynamic spraying device and where the liquid carrier vehicle comprises: a. from about 50% V/V to about 100% V/V water; b. from about 0% to about 40% V/V ethanol; c. from about 0% to about 30% V/V of a co-solvent; d. from about 0.5% to about 10% V/V of a pharmaceutically acceptable excipient; and e. from about 0.05% W/V to about 10% W/V of a derivatized carbohydrate surfactant; wherein said liquid carrier has a resistivity of from about 25ohm m to about 8000 ohm m and a surface tension of from about 20 dyne/cm to about 40 dyne/cm. Also disclosed...
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ANALGESICS FOR NASAL ADMINISTRATION

(WO2003080022) 02.10.2003 A61K 9/00 IONIX PHARMACEUTICALS LIMITED
An analgesic and a delivery agent are combined in a pharmaceutical composition such that, on introduction into the nasal cavity of a patient to be treated, the analgesic may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration, Cther, of 0.2 ng/ml or greater which is maintained for a duration Tmaint of at least 2 hours. The analgesic may be an opioid analgesic or a non-steroidal anti- inflammatory drug.
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DRUG DOSE-FORM AND METHOD OF MANUFACTURE

(WO2003068604) 21.08.2003 A61K 9/00 WEIBEL, Michael, K.
Disclosed is a novel solid dosage unit, preferably in the form of a film or thin troche, containing at least one pharmaceutical agent, and its method of manufacture, which involves introduction of a fluid containing at least one non-volatile material, such as a polymeric film forming substance, a volatile carrier and at least one pharmaceutical agent into a depression or cavity comprising the major element of the packaging film for the finished dosage unit (s), and removing the volatile carrier from the cavity by exposure to radiant energy, whereby the remaining non-volatile residue comprises the desired dosage unit. The packaging film can be subsequently lidded by conventional sealing methods to produce packaged dosage units wh...
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PHARMACEUTICAL COMPOSITION COMPRISING N- ((1-N-BUTYL-4-PIPERIDINYL) METHYL)-3, 4-DIHYDRO-2H- (1, 3) OXAZINO (3, 2-A) INDOLE-10-CARBOXAMIDE OR SALT AND PROCESS THEREFOR COMPRISING DRY GRANULATION

(WO2003068193) 21.08.2003 A61K 9/16 GLAXO GROUP LIMITED
The invention provides a process for preparing a pharmaceutical composition comprising N-[1-nbutyl-4-piperidinyl)methyl]-3,4-dihydro-2H- [1,3]oxazino[3,2-a]indole-10-carboxamide (SB 207266) (piboserod) or a pharmaceutically acceptable salt thereof in combination with one or more pharmaceutically acceptable excipients, the process comprising forming part or all of the SB 207266 or the salt thereof into granules by a dry granulation process. The process is preferably a roller compaction process, preferably followed by milling to a suitable particle size. The granules are usually of increased particle size and/or compacted compared to the SB 207266 or the salt thereof. Preferably, the SB 207266 or the salt thereof is present in the composition ...
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COMPOSITIONS AND METHODS FOR TREATING PAIN USING CYCLOOXYGENASE-1 INHIBITORS

(WO2003068159) 21.08.2003 A61K 31/00 WAKE FOREST UNIVERSITY
The present invention discloses a method of eliciting an analgesic effect in a subject in need thereof comprising intrathecally administering to the subject a therapeutically effective amount of a cyclooxygenase 1 inhibitor or pharmaceutically acceptable salt thereof in a preservative- free pharmaceutically acceptable carrier. The present invention further discloses pharmaceutical compositions comprising a cylcooxygenase 1 inhibitor or a pharmaceutically acceptable salt thereof and an adjuvant such as an adrenergic agonist, opioid analgesic, local anesthetic, and calcium channel blocker, and combinations thereof in a preservative-free pharmaceutically acceptable carrier. Kits comprising a composition comprising a cyclooxygenase 1...
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DRY GRANULATED FORMULATIONS OF AZITHROMYCIN

(WO2003063838) 07.08.2003 A61K 9/20 PFIZER PRODUCTS INC.
This invention relates to a pharmaceutical formulation, in the form of a tablet, sachet or powder for suspension dosage form, which comprises dry granulated particles of a non-dihydrate form of azithromycin and, optionally, one or more pharmaceutically acceptable excipients. Preferably, the pharmaceutical formulation is a tablet containing between about 40%, by weight, to about 85% , by weight, non-dihydrate azithromycin. More preferably, the pharmaceutical formulation contains non-dihydrate azithromycin selected from the forms B, D, E, F, G, H, J, M, N, 0, P, Q, R, or mixtures thereof. Even more preferably, the invention relates to a pharmaceutical formulation wherein the dosage of azithromycin is 250 mgA, 500 mgA, 600 mgA or 1000 mgA. The...
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DNA DOSAGE FORMS

(WO2003061636) 31.07.2003 A61K 9/14 GLAXO GROUP LIMITED
The present invention relates to efficient devices for administration of DNA based pharmaceutical agents into mammalian skin. In a particularly preferred aspect of the present invention there is provided devices for administration of DNA vaccines into the skin of the mammal, and preferably into human skin. The present invention provides a microneedle DNA pharmaceutical agent delivery device having at least one skin-piercing element which comprises a support member coated with a solid reservoir medium containing, in solid solution or suspension within it, the DNA pharmaceutical agent, and a stabilising agent that inhibits the degradative effects of free radicals. Preferably the solid pharmaceutical reservoir medium coated onto such dev...
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SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION

(WO2003061634) 31.07.2003 A61K 9/00 SMART DRUG SYSTEMS INC
A sustained release composition including at least one growth and/or reproduction-associated pharmaceutical component; analogue thereof or derivative thereof; and a non-silicone pharmaceutical carrier therefor, in a unit dosage form.
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SIMVASTATIN DOSAGE FORMS

(WO2003055467) 10.07.2003 A61K 9/28 SYNTHON B.V.
The present invention relates to a pharmaceutical tablet composition comprising an effective amount of simvastatin and at least one pharmaceutically acceptable excipient, wherein said composition exhibits a pH within the range of 5.0 to 7.5.
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RADIOOPAQUE SUSTAINED RELEASE PHARMACEUTICAL SYSTEM

(WO2003051335) 26.06.2003 A61K 9/00 SMART DRUG SYSTEMS INC
An at least partially radio-opaque sustained release delivery apparatus including a sustained release support material; a pharmaceutically active composition carried in or on the sustained release support material; and a material which renders the delivery apparatus at least partially radio-opaque; the pharmaceutically active composition including at least one pharmaceutically active component; and optionally carrier therefor; the pharmaceutically active component being present in amounts of from approximately 30 % to 75 % by weight, based on the total weight of the sustained release delivery apparatus; the radio-opaque material being carried in the support material, and/or in the pharmaceutically active composition.
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ANTIMUSCARINIC AEROSOL

(WO2003039464) 15.05.2003 A61K 31/00 PHARMACIA &UPJOHN COMPANY
The present invention concerns the use of antimuscarinic agents for the treatment of urinary disorders. The invention provides a method of treating urinary disorder in a mammal, including man, comprising administering to said mammal, in need of such a. treatment, a therapeutically effective amount of an antimuscarinic agent, or solvate or prodrug thereof, said administration being performed by inhalation or insufflation.
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VAGINALLY ADMINISTERD ANTI-DYSRHYTHMIC AGENTS FOR TREATING PELVIC PAIN AND INFERTILITY

(WO2003037381) 08.05.2003 A61K 9/00 COLUMBIA LABORATORIES (BERMUDA) LIMITED
The invention relates to a pharmaceutical composition for relieving pelvic pain or infertility associated with uterine dysrhythmia. The composition includes a locally-administered anti-dysrhythmic treating agent and a bioadhesive extended-release carrier. The composition may be delivered in an extended release formulation that includes a bioadhesive, water-swellable , water-insoluble, cross-linked polycarboxylic acid polymer, such as polycarbophil. The treating agent may be a local anesthetic, such as lidocaine. The invention also relates to a method of treating or preventing pelvic pain, or treating or improving infertility, by inserting a mixture of an anti-dysrhythmic treating agent and a bioadhesive carrier into the vagina of the patien...
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DELIVERY SYSTEM FOR PHARMACEUTICAL, NUTRITIONAL AND COSMETIC INGREDIENTS

(WO2003035094) 01.05.2003 A61K 35/78 NATREON INC.
A stable, water-soluble delivery system which is a purified Shilajit composition obtained by extraction of native Shilajit, preferably containing at least 40% by weight of a carrier which is purified fulvic acid, characterized by having a sponge-like structure punctured by voids of about 200-1000 A in diameter, and a Mn molecular weight of about 700-2500; and an effective amount of an active pharmaceutical, nutritional or cosmetic ingredient added to said carrier and filling voids therein.
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COMPOSITIONS COMPRISING HYDROXYAPATITE USEFUL FOR THE ADMINISTRATION OF THERAPEUTIC AGENTS

(WO2003030943) 17.04.2003 A61K 9/00 THE UNIVERSITY OF BRITISH COLUMBIA
Compositions and methods for in vivo delivery of pharmaceutically active agents associated with hydroxyapatite (HAP). Compositions comprising a pharmacologically active agent and HAP in a pharmaceutically acceptable carrier, the composition providing controlled release of the pharmacologically active agent when introduced into the body. The pharmaceutically acceptable carrier can be a polymer paste or gel which may contain a second pharmacologically active agent. Methods of making and administering a controlled release compositions for the delivery of a pharmacologically active agent, such as a nucleic acid, in combination with a polycationic polymer and in a pharmaceutically acceptable carrier, to a mammal in a pharmaceutically effective a...
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FLASHMELT ORAL DOSAGE FORMULATION

(WO2003030868) 17.04.2003 A61K 9/00 BRISTOL-MYERS SQUIBB COMPANY
There is provided granules for the production of improved flash- melt pharmaceutical oral dosage forms. In addition to one or more medicaments, the granules are composed of an excipient combination consisting of a superdisintegrant (of two or more agents selected from the group consisting of crospovidone, croscarmellose sodium, sodium, sodium starch glycolate, low-substituted hydroxypropyl cellulose or pregelatinized starch), a dispersing agent, a distributing agent, and a binder and may also include other conventional ingredients such as sweetening and flavoring agents. The subject granules are advantageous in that they are stable and can be prepared without the aid of solvents and without the need for special environments or handling. Dosa...
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SUSTAINED RELEASE PHARMACEUTICAL COMPOSITIONS

(WO2003028653) 10.04.2003 A61K 9/16 GLAXO GROUP LIMITED
A sustained release pharmaceutical composition having a plurality of multi-component pharmaceutical particles having a medicament/excipient matrix, the medicament/excipient fraction including a substantially hydrophilic medicament fraction and a substantially hydrophilic excipient fraction, the pharmaceutical particles being coated with at least one pharmaceutically acceptable coating material wherein the pharmaceutical particles exhibit a substantially linear dissolution profile and a duration of efficacy over at least a 12 hour period.
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MEDICAL DEVICES CONTAINING RAPAMYCIN ANALOGS

(WO2003022807) 20.03.2003 A61L 27/54 ABBOTT LABORATORIES
A medical device comprising a supporting structure capable of containing or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient may contain one or more therapeutic agents or substances, with the carrier preferably including a coating on the surface thereof, and the coating containing the therapeutic substances, such as, for example, drugs. Supporting structures for the medical devices that are suitable for use in this invention include, but are not limited to, coronary stents, peripheral stents, catheters, arterio-venous grafts, by-pass grafts, and drug delivery balloons used in the vasculature. Drugs that are suitable for use in this invention include, but are not limited to Formula (I). This drug can ...
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OILY THIXOTROPIC FORMULATIONS

(WO2003022254) 20.03.2003 A61K 9/48 F. HOFFMANN-LA ROCHE AG
The present invention relates to a novel thixotropic oily vehicle comprising from 0.2% to 5% (w/w) of a colloidal silica and from 0.2% to 5% (w/W) of a hydrophilic polymer in an edible oil. The interaction between the hydrophylic polymer and the colloidal silicon dioxide in the above concentration ranges enables to keep the amount of the latter component at a low concentration, by nevertheless conferring on the solution enough thixotropy and a low viscosity under shear. The invention also relates to capsules filled with the above fill mass.
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COMBINATORIAL TYPE (SEVERAL VEHICLES WITHIN A HOUSING) CONTROLLED RELEASE DRUG DELIVERY DEVICE

(WO2003022252) 20.03.2003 A61K 9/16 INTELLIPHARMACEUTICS CORP.
The present invention is a controlled release delivery device. The device comprises more than one vehicle comprising up to 60% by wgt active agent; up to 60% by wgt amino acid; up to 60% by wgt buffer; and up to 70% by wgt polymer. The vehicle(s) are provided within a housing.
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PREPARATION OF SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION

(WO2003022242) 20.03.2003 A61K 9/00 SMART DRUG SYSTEMS INC
A sustained release apparatus including a silicone support material; and a pharmaceutically active composition carried in or on the silicone support material; the pharmaceutically active composition including at least one pharmaceutically active component; and optionally a carrier therefor; the pharmaceutically active component being present in amounts of from approximately 30 % to 75 % by weight, based on the total weight of the sustained release apparatus.
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A METHOD OF TREATING BENIGN GYNAECOLOGICAL DISORDERS AND A DRUG DELIVERY VEHICLE FOR USE IN SUCH A METHOD

(WO2003017973) 06.03.2003 A61K 9/00 PANTARHEI BIOSCIENCE B.V.
One aspect of the present invention is concerned with a method of treating a benign gynaecological disorder in a female mammal using a drug delivery vehicle, said benign gynaecological disorders being selected from the group consisting of uterine leiomyomas, endometriosis, adenomyosis, functional menorrhagia and metrorrhagia, the method comprising intravaginal administration of the drug delivery vehicle to the female mammal suffering from the benign gynaecological disorder, said drug delivery vehicle containing a selective estrogen enzyme modulator (SEEM), wherein the method provides the SEEM in a therapeutically effective dosage to prevent or reduce symptoms of said benign gynaecological disorder, said SEEM being selected from the group co...
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SUSTAINED RELEASE DELIVERY SYSTEM

(WO2003009833) 06.02.2003 A61K 31/365 SMART DRUG SYSTEMS INC
A sustained release apparatus including at least one sustained release mini tablet implant;the or each mini tablet implant including a pharmaceutically active composition including at least one pharmaceutically active component; and a carrier therefor; the, or each implant together, being of significantly reduced size and/or payload relative to an equivalent immediate release treatment.
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ANTIHISTAMINE FORMULATIONS FOR SOFT CAPSULE DOSAGE FORMS

(WO2003007920) 30.01.2003 A61K 9/48 R.P. SCHERER TECHNOLOGIES, INC.
The invention herein relates to pharmaceutical composition containing loratadine and derivatives thereof which is suitable for use in soft capsule dosage forms. A pharmaceutical composition according to the invention comprises loratadine and derivatives thereof in a pharmaceutically effective amount; and a solvent system comprising a mixture of medium chain fatty acids. The loratadine compositions exhibit good solubility and storage stability while maintaining bioavailability of the drug. The compositions also permit high concentrations of solubilized loratadine per total fill volume and thereby permit the use of smaller capsules to deliver the same dosage of drug.
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PHARMACEUTICAL FORMULATION FOR THE INTRAMUSCULAR ADMINISTRATION OF FULVESTRANT

(WO2003006064) 23.01.2003 A61K 31/565 ASTRAZENECA AB
The invention relates to a sustained release pharmaceutical formulation adapted for administration by injection containing the compound fulvestrant, 7 a-[9-(4,4,5,5,5-pentafluoropentylsulphiny1)nony1]oestra- 1,3,5(10)-triene-3,17 ▀-diol, at concentration of at least 100mg/ml in solution in a ricinoleate vehicle which additionally comprises at least one alcohol and a non-aqueous ester solvent which is miscible in the ricinoleate vehicle.
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ORAL ADMINISTRATION OF 6-HYDROXY-OXYMORPHONE FOR USE AS AN ANALGESIC

(WO2003004032) 16.01.2003 A61K 9/20 ENDO PHARMACEUTICALS, INC.
In a method of treating pain, a patient is administered a pharmaceutical composition of 6-hydroxy oxymorphone in an amount sufficient to induce analgesia. In one embodiment, the pharmaceutical composition is administered orally. Any known or later developed method of oral delivery may be used. To achieve the desired analgesic effect, blood plasma levels of 6-hydroxy oxymorphone are raised to at least approximately 0.2 ng/mL. Most preferably blood plasma levels of 6-hydroxy oxymorphone range at least 0.3 ng/mL during treatment. Administration of compositions containing 6- hydroxy oxymorphone, and one or more carriers, diluents, and excipients in an amount sufficient to induce analgesia is also contemplated.
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LOW SALT FORMS OF POLYALLYLAMINE

(WO2002085378) 31.10.2002 A61K 31/785 GENZYME CORPORATION
Disclosed is a pharmaceutical composition comprising a stable polyallylamine hydrochloride polymer in which between about 4 % to about 12 % by weight of the polymer is a chloride anion and a pharmaceutically acceptable carrier or diluent.
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A NOVEL COATING FOR A SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION

(WO2002085335) 31.10.2002 A61K 9/20 NOSTRUM PHARMACEUTICALS INC.
The present invention is directed to a coating composition for coating a solid dosage form of a medicament, where the coating composition controls the release of the medicament, said coating composition comprising (a) at least 50% (w/w) by dry weight of a water insoluble polymer insoluble in both acidic, basic and neutral pH, present in the form of an aqueous latex dispersion, (b) a water soluble non-polymeric component present in a weight ratio of about 5 to about 50% (w/w) by dry weight of the coating, having a molecular weight of less than about 15,000 daltons and water solubility in excess of 5 grams per 100 grams of water at room temperature at 1 atm pressure, said water soluble non-polymeric component being organic and either solid or...
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FAST DISINTEGRATING MELOXICAM TABLET

(WO2002085331) 31.10.2002 A61K 9/20 BOEHRINGER INGELHEIM INTERNATIONAL GMBH
The present invention relates to a fast disintegrating tablet comprising meloxicam or a pharmaceutically acceptable salt thereof, starch or various starches, glidant and at least one additional excipient.
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GUM BASE AND GUM MANUFACTURING USING PARTICULATED GUM BASE INGREDIENTS

(WO2002071860) 19.09.2002 A23G 4/00 L.A. DREYFUS CO.
A particulated gum base comprises particulated elastomer ingredients and particulated spray congealed ingredients having a size of less than or equal to about 1 millimeters. A method of making a particulate blend gum base comprises the steps of providing at least one first gum base ingredient having a softening point of less than about 130 ░F, providing a second gum base ingredient, combining at least the first and second gum base ingredients to form a combined ingredient having a particulate form, blending at room temperature the combined ingredient with a third gum base ingredient to form the powder blend gum base, the powder blend gum base comprising at least an elastomer, a softener, an antitack ingredient and a filler. An improved met...
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CARRIER SYSTEMS COMPRISING VITAMIN B12 - BIODEGRADABLE MICRO PARTICULATE CONJU GATES FOR PERORAL DELIVERY OF DRUGS, PEPTIDES/PROTEINS AND VACCINES

(WO2002067995) 06.09.2002 A61K 9/16 COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
The invention relates to a novel complex for oral delivery of drugs, therapeutic protein / peptides and vaccines which are loaded in a Vitamin B┐12? (VB┐12?) coupled particulate carrier system with spacers in between, the carrier system with spacers having a formula VB┐12? - R'/R'-N wherein, R' or R' is spacer and/or agents for derivatization of VB┐12? to provide either NH┐2? or COOH or SH groups, and N is the micro or nano particle carriers for the delivery of injectable drugs, therapeutic protein/peptides and vaccines.
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METHOD OF PRODUCING POROUS TABLETS WITH IMPROVED DISSOLUTION PROPERTIES

(WO2002055061) 18.07.2002 A61K 9/00 PARTICLE AND COATING TECHNOLOGIES, INC.
A method of producing a fast-dissolving pharmaceutical delivery device of moderate strength. The delivery device is a fully formed tablet composed of readily available sugars, strength polymers and a volatilizable excipient along with an active ingredient and optional flavorings. The tablet as made will disintegrate in an aqueous medium such as saliva in under 15 seconds, making mastication unnecessary or at least requiring only one or two bites on the tablet. Essential to the invention is the easily obtainable particle size ranges of the sugars and the volatilizable excipient which promotes optimum release and tablet strength. The invention also allows for effective taste masking of the active ingredient with standard particle coating tech...
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SOLID POLYUNSATURATED FATTY ACID COMPOSITIONS

(WO2002045681) 13.06.2002 A61K 9/14 S.L.A. PHARMA AG
A particulate omega-3 polyunsaturated fatty acid composition suitable for use as a medicament or foodstuff additive is obtained by acid precipitation from a basic dispersion or solution comprising an omega-3 polyunsaturated fatty acid, salt or ester, metabolite or other pharmacologically acceptable derivative thereof and a polymeric pharmaceutical excipient which may be a polymethacrylate or a polysaccharide or ether, ester or other derivative thereof.
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PHARMACEUTICAL FORMULATIONS COMPRISING PACLITAXEL, DERIVATIVES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

(WO2002043765) 06.06.2002 A61K 9/107 TRANSFORM PHARMACEUTICALS, INC.
The invention concerns paclitaxel solubilizers and formulations thereof with a high propensity to dissolve paclitaxel. The formulations of the invention reduce or obviate the need for the disadvantageous excipient Cremophor$m(3) EL. The formulations of the invention are useful for administering paclitaxel, its derivatives, or pharmaceutically acceptable salts or such derivatives to patients in need thereof. The formulations of the invention are suitable for parenteral, oral, local, or transdermal administration to mammals including humans, particularly for intravenous delivery.
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STABLE, AEROSOLIZABLE SUSPENSIONS OF PROTEINS (E.G. INSULIN, DNASE) IN ETHANOL

(WO2002043695) 06.06.2002 A61K 38/28 BATELLE MEMORIAL INSTITUTE
Stable suspensions of a biologically active protein are disclosed that are suited for aerosol delivery to the lungs of a patient in need of treatment, which comprise particles of biologically active protein suspended in ethanol. In a preferred embodiment, the invention describes a stable suspension of insulin useful for aerosol delivery to the lungs of a patient in need of treatment comprising particles of a pharmaceutically effective amount of insulin suspended in ethanol. A method of delivering a therapeutically effective amount of a protein to the respiratory tract Of a patient is described which comprises producing an aerosol of a stable liquid suspension of a protein using an electrohydrodynamic spraying means wherein the liquid suspen...
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COMPOSITIONS AND METHODS FOR REDUCING GNRH-INDUCED BONE LOSS

(WO2002030451) 18.04.2002 A61K 38/18 ATOSSA HEALTHCARE, INC.
Compositions, and methods for administering such compositions, are provided to reduce GnRH-induced bone loss. The compositions are a pharmaceutically acceptable formulation comprising a therapeutically effective amount of GnRH and a bone growth promoting agent. The GnRH and bone growth promoting agent are typically formulated with a pharmaceutically acceptable carrier and administered in an amount sufficient to treat, to prevent, or to reduce the symptoms of, a sex steroid hormone-responsive condition in a patient. The GnRH and bone growth promoting agent can be administered prophylactically or to treat existing sex steroid hormone-responsive conditions in patients by a variety of administration modes, including intramuscular, intravenous, ...
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PHARMACEUTICAL VEHICLE

(WO2002028435) 11.04.2002 A61K 8/04 SOLTEC RESEARCH PTY LTD.
This invention relates to vehicles for the percutaneous delivery of at least one pharmaceutically active agent to the epidermis. In particular this invention relates to pharmaceutical compositions directed to the treatment of skin diseases, more particularly those containing salicylic acid. More specifically, a hydroalcoholic vehicle for percutaneous delivery of an active agent to the epidermis, said vehicle comprising lower alcohol, water and wax-surfactant, said wax surfactant being one, or a combination of compounds selected from the group consisting of acyl glutamates, phosphoric acids or salts, acyl isethionates, alkyl ether sulfates, alkyldibenzylmethylammonium salts, heterocyclic ammonium salts, tetraalkylammonium salts, ethoxylated ...
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POWDERED/MICROFIBRILLATED CELLULOSE

(WO2002022172) 21.03.2002 A61K 9/16 UNIVERSITY OF IOWA RESEARCH FOUNDATION
A new cellulose excipient suitable for use as a binder, filler, and/or disintegrant in the development of solid dosage forms and as a bodying agent or a drug carrier in the preparation of topical formulations is described. The cellulose excipient is formed by soaking a source of cellulose in an aqueous alkali metal hydroxide solution. The cellulose is then regenerated, washed, and optionally hydrolyzed with a dilute mineral acid. The cellulose excipient is also useful as an aqueous dispersion in topical formulations and in the manufacture of cellulose beads.
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COMPOSITIONS FOR TREATING SEXUAL DYSFUNCTION, CONTAINING AN NO- DONOR AND AN ANTIOXIDANT

(WO2002019999) 14.03.2002 A61K 31/375 SACKS, Meir, S.
Methods for treating sexual dysfunction are disclosed. The methods generally comprise the administration of an NO donor and an antioxidant; the active ingredients can be administered topically to the genitals of the patient. The methods allow for localized NO delivery through topical application of the present compounds, while minimizing, if not preventing, damage associated with peroxynitrite formation. Compositions comprising L- arginine, or a derivative thereof and an antioxidant in a pharmaceutical carrier suitable for application to the genitals is also disclosed.
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MODIFIED RELEASE FORMULATION

(WO2002019990) 14.03.2002 A61K 9/20 ASTRAZENECA AB
A pharmaceutical modified release formulation comprising a pharmacologically active substance and a modified water-soluble polysaccharide, which modified water-soluble polysaccharide is obtainable by: a) forming a precipitate of a water-soluble polysaccharide by contacting a solution of the water-soluble polysaccharide with a solvent in which the polysaccharide is poorly soluble or insoluble; or b) milling a water-soluble polysaccharide. The modified water-soluble polysaccharides provide modified release formulations with high tablet hardness. Also claimed are a process for preparing the modified release formulation, and the use of the modified water-soluble polysaccharides as an excipient in a pharmaceutical formulation.
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APPARATUS FOR TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE AND ASSOCIATED METHOD

(WO2002018001) 07.03.2002 A61M 15/00 PNEUMOFLEX SYSTEMS, L.L.C.
An apparatus and method for treatment of a patient having a pulmonary disease involving chronic obstruction of the airways includes a container having therein a chamber containing a composition of L-tartrate in a pharmaceutically acceptable carrier; an opening connected to the chamber so as to provide an outlet thereof, the opening sized for producing droplets of a predetermined size range responsive to the composition being motivated from the chamber through the opening; and a source of motivating force connected with the chamber so as to motivate the compositions through the opening to thereby cause nebulization of the composition. A treatment kit comprises the container described and a mouthpiece connectable to the container so as to be ...
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TRANSDERMAL PHARMACEUTICAL DELIVERY COMPOSITION

(WO2002017881) 07.03.2002 A61K 9/06 QUEEN MARY &WESTFIELD COLLEGE
A pharmaceutically delivery system is described comprising a pharmaceutically active agent and acidified nitrite as an agent to produce local production of nitric oxide at the skin surface. The dosage form may be in any pharmaceutically acceptable carrier means and comprises an acidifying agent adapted to reduce the pH at the environment. In one embodiment, a barrier consisting of a membrane allows diffusions of the anaesthetic and nitrite ions while preventing direct contact of the skin and acidifying agent.
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SOLID DISPERSION OF IPRIFLAVONE FOR ORAL ADMINISTRATION AND ITS MANUFACTURING METHODS

(WO2002013790) 21.02.2002 A61K 9/14 KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
This invention relates to an ipriflavone-containing pharmaceutical agent for oral administration with improved bioavailability, wherein ipriflavone is solid-dispersed in the presence of a water-soluble polymer, an absorption fortifier, and an excipient while the crystal of said pharmaceutical agent is prepared in an amorphous form at the same time so that said ipriflavone can be enclosed in said water soluble polymer, and thus even a little amount as well as lower number of dosage of said ipriflavone pharmaceutical agent can increase the effective blood concentration of said ipriflavone pharmaceutical agent and the solubility for the body fluid in the gastrointestinal tract, thereby remarkably improving the bioavailability of said agent whi...
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IMPROVED SOLID PHARMACEUTICAL DOSAGE FORMULATION OF HYDROPHOBIC DRUGS

(WO2002013762) 21.02.2002 A61K 9/20 DELSYS PHARMACEUTICAL CORPORATION
A novel solid pharmaceutical dosage formulation of hydrophobic drugs is disclosed, which provides enhanced dissolution and improved bioavailability. The hydrophobic drug is deposited electrostatically on the base substrate. The dosage form may include any pharmaceutically acceptable additive, disposed within a carrier that is segregated from, but in contact with, the deposit. Figure No. 1 depicts an isometric view of a product comprising a strip package containing a plurality of unit forms in accordance with the prior art.
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LIQUID FORMULATION OF METFORMIN

(WO2002011716) 14.02.2002 A61K 9/00 RANBAXY SIGNATURE LLC
The present invention is directed to a liquid formulation of metformin or its pharmaceutically acceptable salts thereof. The liquid pharmaceutical composition comprises a therapeutically effective amount of metformin or its pharmaceutically acceptable salt, in a liquid carrier, which may also include a sweetener that does not increase the blood glucose level of a subject after ingestion thereof. In one embodiment, it may also include alkyl hydroxyethyl-cellulose, and/or a polyhydroxy alcohol. In another embodiment, the carrier may contain a sweetener, mineral acid, and bicarbonate salt maintained at a pH of 4.0 to 9.0. It is useful for treating hyperglycemia and diabetes.
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FORMULATIONS OF MOMETASONE AND A BRONCHODILATOR FOR PULMONARY ADMINISTRATION

(WO2002011711) 14.02.2002 A61K 31/57 LONGWOOD PHARMACEUTICAL RESEARCH, INC.
A pharmaceutical formulation is provided for pulmonary drug administration of a bronchodilator, a corticosteroid and an optional pharmaceutically acceptable carrier. In addition, methods for using the formulation to treat bronchodilator/corticosteroid-reponsive conditions, diseases or disorders are provided, as are drug delivery devices and dosage forms for housing and/or dispensing the formulations.
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METHOD FOR THE DETECTION OF APOPTOSIS BY DETERMINING APOPTOSIS- SPECIFIC MARKERS RELEASED INTO AN EXTRACELLULAR MEDIUM THROUGH CELLULAR RELEASE MECHANISMS

(WO2002008752) 31.01.2002 A61K 38/00 EVOTEC OAI AG
A method for the detection of apoptosis by determining presence, amount, or activity of apoptosis-specific markers released from at least one cell undergoing apoptosis into an extracellular medium through cellular release mechanisms is disclosed. The extracellular medium includes body fluids, in particular urine, inflammatory fluid, serum, liquor, or cell culture medium, wherein samples are preferably taken from humans or animals. The method can be used for the diagnosis and/or for therapy control of diseases and/or processes associated with increased apoptosis. It can also be used for therapy control of diseases associated with decreased apoptosis. Additionally, a method is disclosed for the identification of apoptosis-modulating substance...
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NOVEL AEROSOL FORMULATION CONTAINING A POLAR FLUORINATED MOLECULE

(WO2002003958) 17.01.2002 A61K 47/24 ASTRAZENECA AB
The present invention relates to a stable pharmaceutical aerosol formulation intended for inhalation. The formulation contains an active substance, an aerosol propellant, a polar flurorinated molecule and an excipient. The preferred propellant is HFA 134a or HFA 227 or a mixture thereof.
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CROSS-LINKED HIGH AMYLOSE STARCH FOR USE IN CONTROLLED-RELEASE PHARMACEUTICAL FORMULATIONS AND PROCESSES FOR ITS MANUFACTURE

(WO2002002084) 10.01.2002 A61K 9/00 LENAERTS, Vincent
The present invention relates to a novel form of cross-linked high amylose starch and process for its manufacture. Such cross-linked high amylose starch is useful as an excipient in a controlled-release pharmaceutical formulation when compressed with a pharmaceutical agent(s) in a tablet. Such cross-linked high amylose starch is prepared by (a) cross-linking and chemical modification of high amylose starch, (b) gelatinization, and (c) drying to obtain a powder of said controlled release excipient. In a preferred embodiment, such cross-linked high amylose starch is prepared in following steps: (1) granular cross-linking and additionally chemical modification (e.g., hydroxypropylation) of high- amylose starch; (2) thermal gelatinization of th...
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SEMI-SOLID DELIVERY VEHICLE AND PHARMACEUTICAL COMPOSITIONS

(WO2001085139) 15.11.2001 A61K 47/34 ADVANCED POLYMER SYSTEMS, INC.
A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.
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MODIFIED RELEASE FORMULATIONS CONTAINING A HYPNOTIC AGENT

(WO2001078725) 25.10.2001 A61K 9/16 SYNTHON B.V.
Hypnotic pharmaceutical compositions are made from pellets and exhibit a modified release. Zolpidem or a pharmaceutically acceptable salt thereof is a typical hypnotic. The pellets are preferably spherical and exhibit a dissolution profile that includes 60 % of the hypnotic agent being release from the pellet not earlier than 5 minutes from the start of a specified in vitro dissolution test. Although the modified release profile can include 50 % of the hypnotic agent being released not earlier than 15 minutes after the start of the dissolution test, the pellet preferably does not contain a release rate controlling excipient or coating. Instead, microcrystalline cellulose and the active constitute the majority of the pellet, e.g. 90 % or mor...
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LOCAL DRUG DELIVERY

(WO2001070274) 27.09.2001 A61K 47/48 NEDERLANDSE ORGANISATIE VOOR TOEGEPAST- NATUURWETENSCHAPPELIJK ONDERZOEK TNO
A method for local therapeutic intervention, which provides long- term retention of a highly concentrated drug within the target tissue after local delivery. The invention uses in particular the structural components of tissue as a high capacity carrier/support for accumulation of a high concentration of the drug, providing a rather uniform distribution of the bound drug throughout the tissue. A concentrated drug is to be delivered in the locus of pathology, which drug comprises a therapeutic effector moiety coupled to an affinity vehicle moiety, which affinity vehicle is capable of binding to an abundant structural component of the extracellular matrix of the target tissue, providing long-term retention of the therapeutic effector therein. ...
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LIPID CARRIER

(WO2001066086) 13.09.2001 A61K 9/48 LIPOCORE HOLDING AB
The invention refers to a lipid carrier composition for controlled release of a bioactive substance, which comprises at least one triglyceride oil, and at least one polar lipid selected from the group consisting of phosphatidylethanolamine and monohexosylceramide, and ethanol, which is charactrised in that the carrier composition has the ability to form a cohesive structure, which structure is retained in an aqueous environment. The invention also refers to a pharmaceutical composition consisting of said lipid carrier and a bioactive substance dissolved or dispersed in the carrier, preferably an injectable composition.
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FULVESTRANT FORMULATION

(WO2001051056) 19.07.2001 A61K 31/565 ASTRAZENECA AB
The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7$g(a)-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)- triene-3,17$g(b)-diol, more particularly to a formulation adapted for administration by injection containing the compound 7$g(a)-[9-(4,4,5,5,5- pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17$g(b)-diol in solution in a ricinoleate vehicle which additionally comprises at least one alcohol and a non-aqueous ester solvent which is miscible in the ricinoleate vehicle.
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METHOD FOR PREPARING SOLID DELIVERY SYSTEM FOR ENCAPSULATED AND NON-ENCAPSULATED PHARMACEUTICALS

(WO2001049272) 12.07.2001 A61K 9/00 SHEAR/KERSHMAN LABORATORIES, INC.
The present invention is an oral drug delivery system for delivering unpalatable pharmaceuticals, wherein the pharmaceutical delivery system comprises a lipid, dry particles including at least one pharmaceutical and at least one filler, and a surfactant, wherein the dry particles are continuously coated by the lipid and form a suspension with the lipid, making the pharmaceutical more palatable.
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METHODS FOR PREPARING PHARMACEUTICAL FORMULATIONS

(WO2001045741) 28.06.2001 A61K 31/00 GLAXO GROUP LIMITED
The invention relates to pharmaceutical formulations and methods for preparing pharmaceutical formulations of histamine releasers. The present invention provides methods for determining the concentration of physiologically acceptable excipient for use in the formulations of invention. The present invention also provides methods for suppressing pharmaceutically-induced histamine release by administering to an animal, the formulations of the present invention. A kit useful for preparing pharmaceutical formulations of histamine releasers is also provided.
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EXTENDED RELEASE ORAL DOSAGE COMPOSITION

(WO2001045676) 28.06.2001 A61K 9/20 SCHERING CORPORATION
A compressed bilayer solid composition comprising (a) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable excipient and (b) a sustained release second layer comprising an effective amount of a nasal decongestant and a pharmaceutically acceptable sustained release agent wherein the composition contains less than about 2 % of desloratadine decomposition products is disclosed.
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RADIATION SENSITIVE LIPOSOMES

(WO2001039744) 07.06.2001 A61K 9/00 THE ARIZONA BOARD OF REGENTS on behalf of THE UNIVERSITY OF ARIZONA
The present invention relates to a radiation sensitive liposome, and the use of this liposome as carrier for therapeutic and diagnostic agent(s). In particular, the invention encompasses a liposomal delivery system, comprising a stable liposome-forming lipid and a polymerizable colipid, a fraction of which polymerizable colipid polymerizes upon exposure to ionizing radiation, thereby destabilizing the liposomal membrane. Destabilization of liposomes allows for leakage of liposomal contents. The present invention further contemplates methods of diagnosing and treating conditions and diseases that are responsive to liposome- encapsulated or associated agents.
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SOLID CARRIERS FOR IMPROVED DELIVERY OF ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS

(WO2001037808) 31.05.2001 A61K 9/16 LIPOCINE, INC.
The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and t...
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INJECTION VEHICLE FOR POLYMER-BASED FORMULATIONS

(WO2001028591) 26.04.2001 A61K 9/16 GENENTECH, INC.
The invention provides injection vehicles suitable for administering particulate suspensions, such as polymer-based formulations, as well as associated pharmaceutical formulations, articles of manufacture, and kits. Other aspects of the invention included methods for producing and administering pharmaceutical formulations. The injection vehicles of the invention are superior to conventional injection vehicles in that they include a pseudoplastic composition that improves injectability, which facilitates delivery of the desired dose. The injection vehicles of the invention also allow the use of smaller-bore needles than are usually necessary to inject polymer-based formulations, reducing the pain associated with injection of such formulation...
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PHARMACEUTICAL COMPOSITION FOR TREATMENT OF MUCOSAL EPITHELIAL ULCERATION AND/OR EROSION

(WO2001028515) 26.04.2001 A61K 31/65 L═F-HLAUP EHF. BIO-GELS PHARMACEUTICALS INC.
A bioadhesive pharmaceutical composition for treatment of mucosal epithelial ulceration and/or erosions, said composition comprising: (i) a bioadhesive substance; (ii) a biologically active substance having MMP inhibitory activity; and (iii) an optional physiologically acceptable vehicle; said bioadhesive substance and optional physiologically acceptable vehicle being selected to release the biologically active substance in a therapeutic amount into the epithelia of the mucosa without affecting the normal flora thereof; use of the composition for the manufacture of a medicament for treating mucosal ulceration and/or erosion; a method of treating mucosal epithelial ulceration and/or erosion in a mammal; and a method of delivering a biologica...
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PHARMACEUTICAL FORMULATIONS CONTAINING POORLY SOLUBLE DRUG SUBSTANCES

(WO2001024801) 12.04.2001 A61K 9/20 SANOFI-SYNTHELABO
A method for preparing pharmaceutical formulations of poorly soluble drug substances in the form of concentrated solutions for filling soft gelatin capsules and solid dispersions and suspensions for filling hard gelatin capsules and compressing into tablets is provided. Pharmaceutical formulations of poorly soluble drug substances are also disclosed. The formulations include the sodium salt of the poorly soluble drug substance, a conversion aid such as PEG, polysorbate, a sugar alcohol (e.g. mannitol or xylitol), propylene glycol or transcutol, and, in some cases an excipient, such as dicalcium phosphate dihydrate, lactose monohydrate, or microcrystalline cellulose.
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ANTI-INFLAMMATORY PHARMACEUTICAL FORMULATIONS

(WO2001024778) 12.04.2001 A61K 9/24 NORTON HEALTHCARE LTD.
An oral pharmaceutical dosage form including a mixture of a delay release formulation of a non-steroidal anti-inflammatory drug (NSAID) and a mixture containing a prostaglandin and one or more excipients.
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CONTROLLED RELEASE ORAL DOSAGE SUITABLE FOR ORAL ADMINISTRATION

(WO2001015665) 08.03.2001 A61K 9/20 NOSTRUM PHARMACEUTICALS, INC.
The present invention is directed to a pharmaceutical composition, preferably in the form of a tablet comprising a therapeutically effective amount of a medicament in a carrier comprising a water insoluble polymer and a water-insoluble inorganic salt.
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CONTROLLED RELEASE FROM COPOLYMERS OF ACRYLIC OR METHACRYLIC ACID/L-DOPA, ACRYLIC OR METHACRYLIC ACID/L-$G(A)-METHYL DOPA, ACRYLIC OR METHACRYLIC ACID/CARBIDOPA AND THEIR COMBINATIONS

(WO2001010378) 15.02.2001 A61K 31/198 FUNDAă├O OSWALDO CRUZ - FIOCRUZ
The invention relates to site directed drug delivery systems providing a controlled release of L-dopa, carbidopa or L-alpha-methyldopa and/or their combinations which eliminates or at least reduces the deleterious side effects of these drugs. Biologically active copolymers having directional characteristics to the digestive mucous tissue comprise L-dopa, carbidopa or L-alpha-methyldopa chemically combined with biologically acceptable poly(acrylic acid) or poly(methacrylic acid). The copolymers are obtained by a process comprising the steps of: (a) reacting L-dopa, carbidopa or L-alpha-methyldopa with a chlorination agent; (b) bringing into reaction the product of step (a) and poly(acrylic acid) or poly(methacrylic acid) in the presence of a...
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TASTE MASKED PHARMACEUTICAL LIQUID FORMULATIONS

(WO2001003698) 18.01.2001 A61K 9/00 ORTHO-MCNEIL PHARMACEUTICAL, INC.
A liquid composition for oral administration comprising a pharmaceutically active medicament coated with a taste masking effective amount of a polymer blend of (a) dimethylaminoethyl methacrylate and neutral methacrylic acid ester (MM/MAE) and (b) a cellulose ester, in an aqueous vehicle, wherein the polymer weight ratio of the cellulose ester to the MM/MAE is about 40:60 to about 90:10, preferably about 60:40. The liquid composition utilizes a 'reverse enteric coating' which is soluble in the acid pH's of the stomach, generally about 1.0 to 4.0, but relatively insoluble at the non-acidic pH's of the mouth. The coatings provide for rapid release and absorption of the drug, which is generally desirable in the case of liquid dosage forms.
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COMBINATION THERAPY FOR TREATING HYPERCHOLESTEROLEMIA

(WO2000069446) 23.11.2000 A61K 31/785 GELTEX PHARMACEUTICALS, INC.
The invention relates to methods for treating hypercholesterolemia and atherosclerosis, and reducing serum cholesterol in a mammal. The methods of the invention comprise administering to a mammal a first amount of a bile acid sequestrant compound which is an unsubstituted polydiallylamine polymer and a second amount of an HMG Co-A reductase inhibitor compound. The first and second amounts together comprise a therapeutically effective amount. The invention further relates to pharmaceutical compositions useful for the treatment of hypercholesterolemia and atherosclerosis, and for reducing serum cholesterol. The pharmaceutical compositions comprise a combination of a first amount of an unsubstituted polydiallylamine polymer compound and a seco...
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COMBINATION THERAPY FOR TREATING HYPERCHOLESTEROLEMIA

(WO2000069445) 23.11.2000 A61K 31/785 GELTEX PHARMACEUTICALS, INC.
The invention relates to methods for treating hypercholesterolemia and atherosclerosis, and reducing serum cholesterol in a mammal. The methods of the invention comprise administering to a mammal a first amount of a bile acid sequestrant compound which is an unsubstituted polydiallylamine polymer and a second amount of a cholesterol-lowering agent. The first and second amounts together comprise a therapeutically effective amount. The invention further relates to pharmaceutical compositions useful for the treatment of hypercholesterolemia and atherosclerosis, and for reducing serum cholesterol. The pharmaceutical compositions comprise a combination of a first amount of an unsubstituted polydiallylamine polymer compound and a second amount of...
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PHARMACEUTICAL COMPOSITIONS FOR TREATING MALARIA

(WO2000067699) 16.11.2000 A61K 31/44 ARCH CHEMICALS, INC.
The present invention is directed to pharmaceutical compositions and methods for treating a patient suffering from malaria. The pharmaceutical composition of the invention includes a therapeutically effective amount of pyrithione, pyrithione chelate, pyrithione disulfide, pyridine-2-ones, pyridine-2-thiones, or pyrithione salt, and a pharmaceutically acceptable carrier. The pharmaceutical composition of the invention is preferably administered to the patient in a non-oral form, such as a dermal patch, topical cream, anal suppository, intravenous injection, or nasal inhalant, in order to minimize the breakdown of the active ingredients and provide maximum therapeutic benefit to the patient.
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A PHARMACEUTICAL COMPOSITION OF CONCENTRATES FOR MICROEMULSION AND SELF-EMULSIFYING DRUG DELIVERY SYSTEM

(WO2000066140) 09.11.2000 A61K 38/13 PHARMASOLUTIONS, INC.
The present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of cyclosporin in association with a pharmaceutical carrier, said carrier comprising a drug solubilizing effective amount of a fatty acid having 6-22 carbon atoms and a non-ionic surfactant.
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COMPOSITION CONTAINING OPIOID ANTAGONISTS AND SPRAY DISPENSER

(WO2000062757) 26.10.2000 A61K 9/00 BRITANNIA PHARMACEUTICALS LIMITED
A spray applicator is disclosed for administering an opioid antagonist selected from naloxone and/or naltrexone. The applicator is capable of delivering single or multiple doses of the antagonist through a projecting delivery portion which is shaped or dimensioned for introduction into the nose or mouth. A pharmaceutical composition for nasal or oral administration is also disclosed which comprises an opioid antagonist, such as naloxone and/or naltrexone, and which comprises a water-susceptible solid carrier admixed with the opioid antagonist.
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FAST-DISPERSING DOSAGE FORMS CONTAINING FISH GELATIN

(WO2000061117) 19.10.2000 A61K 9/00 R.P. SCHERER CORPORATION
The invention disclosed herein relates to a pharmaceutical composition comprising a carrier and an active ingredient, wherein the carrier is fish gelatin and the composition is a fast-dispersing dosage form designed to release the active ingredient rapidly on contact with a fluid. In one embodiment, the composition is designed for oral administration and releases the active ingredient rapidly in the oral cavity on contact with saliva. The fish gelatin can be obtained from cold water fish sources and is preferably the non-gelling, non-hydrolyzed form. A process for preparing such a composition and a method of using fish gelatin in a fast dispersing dosage form are also provided.
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FORMULATION COMPRISING TESTOSTERON UNDECANOATE AND CASTOR OIL

(WO2000059512) 12.10.2000 A61K 9/48 AKZO NOBEL N.V.
Disclosed is a pharmaceutical formulation in the form of a capsule for oral administration comprising testosterone undecanoate as an active ingredient dissolved in a pharmaceutically acceptable liquid carrier, characterised in that the liquid carrier comprises at least 50 % by weight of castor oil. The choice of castor oil as the liquid carrier, in conjunction with the choice of testosterone undecanoate as the androgen, makes for a solution which can comprise about 200-250 mg/ml of TU. This is a novel achievement for any orally administerable solution of testosterone. The solution may also contain a lipophilic surfactant such as lauroglycol.
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ORAL PHARMACEUTICAL COMPOSITIONS CONTAINING LONG-CHAIN TRIGLYCERIDES AND LIPOPHILIC SURFACTANTS

(WO2000059482) 12.10.2000 A61K 9/107 R.P. SCHERER CORPORATION
The invention disclosed herein relates to liquid pharmaceutical compositions for oral administration which contain a drug or active ingredient dissolved in a liquid vehicle or carrier in which the liquid vehicle comprises a glyceride of a long chain fatty acid having from 14 to 22 carbon atoms and a lipophilic surfactant having an HLB of less than 10. Compositions of the invention provide increased drug or active ingredient stability and contain a liquid vehicle which is less reactive with the drug or active ingredient than free fatty acids. In one embodiment, the liquid pharmaceutical compositions contain testosterone undecanoate, a long chain triglyceride, and lauroglycol. The compositions can be orally administered and formulated in soft...
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OPIOID AGONIST IN A FAST DISPERSING DOSAGE FORM

(WO2000051539) 08.09.2000 A61K 9/00 R.P. SCHERER TECHNOLOGIES, INC.
This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, an opioid ($g(m) receptor) agonist, such as fentanyl, or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for preparing such a composition and the use of such a composition as an analgesic, for the treatment of chronic pain and/or breakthrough pain, as an anesthetic premedication, for the induction of anesthesia, as a sedative and/or for the treatment of anxiety are also provided.
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PHARMACEUTICAL COMPOSITION OF HYDROPHOBICALLY MODIFIED HEDGEHOG PROTEINS AND THEIR USE

(WO2000045848) 10.08.2000 A61K 47/48 CURIS, INC.
The object of the invention is to provide a pharmaceutical composition of a hydrophobically modified hedgehog protein containing a biocompatible carrier, wherein the carrier binds the hedgehog protein as an active folded structure and can release it locally in vivo in an active form in a delayed manner. Such formulations are particularly suitable for the repair of bone and cartilage defects and can also be used to repair neuronal defects or for a systemic delivery. The object is achieved by a pharmaceutical composition of a hydrophobically modified hedgehog protein which is characterised in that this composition contains hydrophobically modified hedgehog proteins and a biodegrable protein or a proteolytic degradation product thereof as a ca...
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BUCCAL DRUG DELIVERY SYSTEM FOR USE IN MALE CONTRACEPTION

(WO2000042942) 27.07.2000 A61K 9/00 PLACE, Virgil, A.
A buccal dosage unit is provided for administering a contraceptive composition to fertile mammalian males. The buccal dosage unit comprises an androgenic agent and a progestin in a polymeric carrier that bioerodes and provides for delivery of the active agents throughout a predetermined drug delivery period that is preferably in the range of approximately 8 to 24 hours.
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SUSTAINED RELEASE FORMULATION WITH REDUCED MOISTURE SENSITIVITY

(WO2000040205) 13.07.2000 A61K 9/20 COPLEY PHARMACEUTICAL INC.
A sustained release pharmaceutical formulation is provided that has reduced sensitivity to moisture and thus enhanced storage stability. The formulation comprises a tablet containing a pharmacologically active agent and a carrier selected from the group consisting of solid polyethylene glycols, ingestible waxes, and mixtures thereof, with a carrier consisting essentially of a mixture of a solid polyethylene glycol and an ingestible wax preferred. Active agents include analgesics, particularly tramadol hydrochloride. Therapeutic methods are provided as well.
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APPARATUS AND PROCESS FOR PREPARING CRYSTALLINE PARTICLES

(WO2000038811) 06.07.2000 A61K 9/16 GLAXO GROUP LIMITED
There is provided according to the present invention a process for preparing crystalline particles, especially particles of a pharmaceutical or carrier substance suitable for inhalation therapy, in addition to an apparatus for the preparation of such particles.
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WATER-INSOLUBLE DRUG DELIVERY SYSTEM

(WO2000037050) 29.06.2000 A61K 9/107 THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
The present invention provides a drug delivery system comprising a water-insoluble drug, a water-miscible organic solvent for the water- insoluble drug, a surfactant, and water, as well as a process for preparing the same. This invention further provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and such a drug delivery system. In addition, the present invention provides a method of delivering a drug to a host by administering to the host the drug delivery system of the present invention.
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SUSTAINED RELEASE TABLET CONTAINING HYDROCOLLOID AND CELLULOSE ETHER

(WO2000033818) 15.06.2000 A61K 9/20 NOSTRUM PHARMACEUTICALS, INC.
The present invention is directed to a solid sustained release pharmaceutical tablet for administering to a host, comprising a therapeutically effective amount of a pharmaceutically active ingredient and a sustained release carrier therefor, said sustained release carrier comprising (a) a hydrocolloid selected from the group consisting of xanthan gum, guar gum, and alginic acid or a pharmaceutically acceptable salt thereof, and (b) a cellulose ether, said hydrocolloid and cellulose ether being present in synergistic effective amount to retard release of said pharmaceutically active ingredient, said hydrocolloid being present in amount ranging from about 0.3 % to about 7.0 % by weight of the tablet and said cellulose ether being present in a...
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COMPOSITIONS COMPRISING CEFUROXIME AXETIL

(WO2000030647) 02.06.2000 A61K 9/14 BIOCHEMIE GESELLSCHAFT M.B.H.
Cefuroxime axetil in a non-gelatinous form on contact with an aqueous liquid, e.g. in the form of a solid solution in a polymer or in the form of a solid dispersion on a carrier, e.g. useful for the production of pharmaceutical compositions comprising cefuroxime axetil as an active ingredient and the use of cefuroxime axetil in the manufacture of an oral dosage form which does not exhibit an adverse food effect.
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A PROCESS FOR THE PREPARATION OF SUSPENSIONS OF DRUG PARTICLES FOR INHALATION DELIVERY

(WO2000025746) 11.05.2000 A61K 9/10 CHIESI FARMACEUTICI S.P.A.
The invention is directed to a process for the preparation of suspensions of drug particles for inhalation delivery, said process providing particles of optimised particle size and distribution homogeneously dispersed in the carrier. The process, which is also suitable for the preparation of sterile suspensions, includes the step of homogenising and micronising the formulation in a turboemulsifier provided with a high-potency turbine, optionally followed by a treatment in a high- pressure homogeniser. A further aspect of the invention is directed to a process for preparing micronised sterile beclomethasone dipropionate by gamma-irradiation.
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FORMULATIONS OF FEXOFENADINE

(WO2000021510) 20.04.2000 A61K 9/00 WEST PHARMACEUTICAL SERVICES DRUG DELIVERY &CLINICAL RESEARCH CENTRE, LTD.
The present invention provides a composition comprising (i) fexofenadine or a pharmaceutically acceptable salt thereof and (ii) a pharmaceutical excipient that increases the solubility of the fexofenadine or salt in water. The pharmaceutical excipient is preferably a cyclodextrin.
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PHARMACEUTICAL COMPOSITIONS COMPRISING IBUPROFEN AND DOMPERIDONE

(WO2000007570) 17.02.2000 A61K 9/00 THE BOOTS COMPANY PLC
A stable pharmaceutical composition comprising a mixture of (i) an ibuprofen medicament; (ii) a domperidone medicamement; and (iii) a carrier material characterized in that the carrier material is substantially free of povidone and comprises at least one diluent combined with at least one release modifying agent.
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A STABLE ORAL PHARMACEUTICAL COMPOSITION CONTAINING A SUBSTITUTED PYRIDYLSULFINYL BENZIMIDAZOLE

(WO1999061022) 02.12.1999 A61K 9/48 RANBAXY LABORATORIES LIMITED
A pharmaceutical composition which is stable and suitable for oral administration to a patient comprises a mixture of a substituted pyridyl sulfinyl benzimidazole having gastric acid secretion inhibitory activity (such as omeprazole, lansoprazole, or pantoprazole), and a pharmaceutically acceptable carrier. The carrier comprises a polymer having vinyl pyrrolidone monomeric units, such as polyvinylpyrrolidone or a vinyl pyrrolidone-vinyl acetate copolymer. Surprisingly, it has been found that the vinylpyrrolidone polymer acts as a stabilizing excipient on the substituted pyridyl sulfinyl benzimidazole so that the composition need not include any alkaline components to prevent degradation of the active ingredient. In a preferred embodiment, t...
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LAYERING PROCESS AND APPARATUS THEREFOR

(WO1999061006) 02.12.1999 A61K 9/16 EURAND INTERNATIONAL S.P.A.
The invention concerns a process and apparatus for applying a layer to a pharmaceutical unit such as a seed or tablet which comprises: (a) coating the unit with particles of drug and/or excipient; the unit and the particles optionally being at different electrical potentials such that electrostatic attraction occurs between them; (b) applying to the unit a binding solution; and (c) drying.
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PRO-DRUG CONJUGATES FOR THE TREATMENT OF STROKE AND OTHER ISCHAEMIC CONDITIONS

(WO1999053908) 28.10.1999 A61K 31/00 UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
A prodrug represented by the Formula (I): A - X - B, wherein A comprises a carrier that selectively effects release of B at hypoxic sites in the brain; X comprises a cleavable linker; and B comprises at least one active moiety of a therapeutic agent for the treatment of stroke or other ischaemic conditions.
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PAROXETINE COMPOSITIONS

(WO1999048499) 30.09.1999 A61K 9/20 SMITHKLINE BEECHAM PLC
Paroxetine is adsorbed on a carrier to form a free-flowing powder useful for capsule filling or for tablet formation; and used in therapy to treat depression.
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NICOTINE INHALER

(WO1999045902) 16.09.1999 A61K 9/00 SLUTSKY, Art
A method of producing a nicotine medicament for use in an inhaler comprises combining a nicotine formulation, a sugar and a liquid carrier including water to produce a flowable mixture and drying the flowable mixture at conditions to produce particles of the nicotine medicament suitable for delivery to the alveoli and lower airways of the person. Also disclosed is a nicotine medicament made by the method. The nicotine composition produced by this method is a composite particle suitable for tobacco replacement or withdrawal therapy.
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POLYMERIC CARRIER

(WO1999036100) 22.07.1999 A61K 9/16 EFRAT BIOPOLYMERS LTD.
The invention provides a polymeric carrier for delivery of a bioactive or bioreactive molecule, comprising a stereocomplex of at least one biocompatible stereoselective polymer and a bioactive or bioreactive molecule.
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SMALL PEPTIDES AND METHODS FOR TREATMENT OF ASTHMA AND INFLAMMATION

(WO1999025372) 27.05.1999 A61K 38/00 HISTATEK, LLC
A pharmaceutical composition is described as an admixture of a pharmacological carrier and a peptide having the formula: f-Met-Leu-X. X is selected from the group consisting of Tyr, Tyr-Phe, Phe-Phe and Phe-Tyr. Also described are methods for inhibiting the degranulation of mast cells and for treating inflammation in a patient, for example, where the inflammation is a result of a disease selected from the group consisting of asthma, rheumatoid arthritis and anaphylaxis. In addition, methods are described for inhibiting the release of cytokines in a patient, for inhibiting the release of histamines in a patient, for inhibiting the release leukotrienes in a patient, for reducing adhesion, migration and aggregation of lymphocytes, eosinophils ...
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SECRETORY LEUKOCYTE PROTEASE INHIBITOR DRY POWDER PHARMACEUTICAL COMPOSITIONS

(WO1999017800) 15.04.1999 A61K 38/00 AMGEN INC.
The present invention relates to the pulmonary administration of a therapeutic protein by means of powdered pharmaceutical composition suitable for inhalation therapy. In particular the invention relates to dry powder formulations of secretory leukocyte protease inhibitor (SLPI) for pulmonary delivery. Exemplary pharmaceutical compositions contain SLPI and a pharmaceutically acceptable carrier in the form of a dry powder which is typically less than about 10 % by weight water. About 50 % to 95 % by mass of the powder comprises particles or agglomerates of particles having a diameter within the range of from about 1.0 microns to about 8 microns, with a mass median diameter ranging from about 3.0 microns to about 6 microns.
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PHARMACEUTICAL PREPARATION COMPRISING CLODRONATE AS ACTIVE INGREDIENT AND SILICIFIED MICROCRYSTALLINE CELLULOSE AS EXCIPIENT

(WO1999015155) 01.04.1999 A61K 9/20 LEIRAS OY
The object of the invention is a pharmaceutical preparation for oral use, especially a tablet, which as its active ingredient contains a pharmacologically acceptable salt of dichloromethylene bisphosphonic acid, i.e. a clodronate, especially disodium clodronate, and which as an excipient contains silicified microcrystalline cellulose. Further objects of the invention are a process for the manufacture of said pharmaceutical preparation, and the use of silicified microcrystalline cellulose for the manufacture of said pharmaceutical preparation.
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HIGH AND LOW LOAD FORMULATIONS OF IGF-I IN MULTIVESICULAR LIPOSOMES

(WO1999012522) 18.03.1999 A61K 9/127 DEPOTECH CORPORATION
Disclosed are multivesicular liposomes (MVLs) containing IGF-I with substantially full bioavailability, wherein the loading of the IGF-I into the liposomes is modulated by adjusting the osmolarity of the aqueous component into which the agents are dissolved prior to encapsulation. In the making of MVLs, the process involves dissolving the IGF-I, an osmolarity excipient, and a pH modifying agent sufficient to solubilize the IGF-I in a first aqueous component used during manufacture of the MVLs. To increase the loading of the IGF-I, the osmolarity of the aqueous component used during manufacture of the MVLs is reduced, whereas the osmolarity of the aqueous component is increased to obtain the low load formulations. The rate of release of the ...
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PHARMACEUTICAL COMPOSITION CONTAINING MIDAZOLAM

(WO1999009989) 04.03.1999 A61K 9/00 R. P. SCHERER LIMITED
This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, midazolam or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for the preparation of such a composition and the use of such a composition for the induction of anaesthesia, anaesthetic pre-medication, sedation, conscious sedation, the treatment of anxiety, the induction of hypnosis and/or amnesia, the treatment and/or prophylaxis of epileptic fits and/or convulsions and the relaxation of skeletal muscle are also provided.
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SOLID PHARMACEUTICAL DOSAGE FORMS IN FORM OF A PARTICULATE DISPERSION

(WO1999008660) 25.02.1999 A61K 9/14 WARNER-LAMBERT COMPANY
Solid particulate dispersions of pharmaceutical agents in a matrix of a water-soluble polymer exhibiting good aqueous dissolution enhanced bioavailability. The method of the invention utilizes water-soluble polymers such as polyvinylpyrrolidone, hydroxypropyl cellulose or hydroxypropylmethyl cellulose as carriers. The invention provides for mixing or extracting the active ingredients in solid particulate form with the polymeric carrier at a temperature at which the polymer softens, or even melts, but the drug remains solid or crystalline. The drug particules thus become coated and produce a product that is matrix coated, i.e. a particulate dispersion.
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ORAL SOLID PHARMACEUTICAL COMPOSITIONS CONTAINING NICORANDIL FOR A MODULATED RELEASE AND THE PROCESS FOR THEIR PREPARATION

(WO1999007370) 18.02.1999 A61K 9/20 BIOMEDICA FOSCAMA INDUSTRIA CHIMICO-FARMACEUTICA S.P.A.
This application describes an oral pharmaceutical composition in a solid form for a modulated release of Nicorandil, containing an appropriate quantity of a glyceride of a saturated aliphatic fatty acid containing a number of carbon atoms equal to or greater than 18 as a pharmaceutically acceptable excipient; a process for its preparation, and a use in drugs for oral administration.
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COMPOSITIONS, KITS, AND METHODS FOR INHIBITING CEREBRAL NEUROVASCULAR DISORDERS AND MUSCULAR HEADACHES

(WO1999003473) 28.01.1999 A61K 9/00 ASTRA AKTIEBOLAG
Compositions, methods and kits for inhibiting a cerebral neurovascular disorder or a muscular headache in a human patient are disclosed. Also disclosed are uses of a long-acting local anesthetic ingredient for manufacturing a medicament comprising the long-acting local anesthetic ingredient for use in inhibiting a cerebral neurovascular disorder in a human patient. The methods comprise intranasally administering to the patient a pharmaceutical composition comprising a local anesthetic, and preferably a long-acting local anesthetic ingredient. A composition useful for practicing the methods of the invention is described which comprises at least one local anesthetic in a pharmaceutically acceptable carrier, wherein the composition is formulat...
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ANTIGEN DELIVERY SYSTEM COMPRISING MONOGLYCERIDE OR DIGLYCERIDE DERIVATIVES AS ADJUVANT

(WO1999002186) 21.01.1999 A61K 9/00 LYFJA RËUN HF, THE ICELANDIC BIO PHARMACEUTICAL GROUP
Adjuvants for administration, particularly for mucosal administration, of an antigen, are described, as well as compositions comprising the described adjuvant in combination with an antigen and a physiologically acceptable vehicle. Methods of eliciting and enhancing an immune response utilizing the adjuvant compositions of the invention are also described. The adjuvant comprises mono- or diglycerides containing at least one water soluble polymer, e.g. poly oxyethylene (PEG┐2-30?). The antigen can be bound to the adjuvant. The adjuvant may be used in the treatment of plants as well.
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TARGETED LIPOSOMAL CONSTRUCTS FOR DIAGNOSTIC AND THERAPEUTIC USES

(WO1999001110) 14.01.1999 A61K 9/127 SDG, INC.
This invention provides a liposomal construct for delivering a diagnostic or therapeutic agent to a mammal comprising a liposomal carrier, a diagnostic or therapeutic agent entrapped within or associated with said liposomal carrier and a sequestering agent distributed within said liposomal carrier to reduce leakage of the diagnostic or therapeutic agent from the liposomal construct prior to delivery.
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DEVICE AND METHOD FOR TREATMENT OF DYSMENORRHEA

(WO1998056323) 17.12.1998 A61F 6/08 UMD, INC.
Methods, devices, and compositions for treatment of dysmenorrhea comprise an intravaginal drug delivery system containing an appropriate pharmaceutical agent incorporated into a pharmaceutically acceptable carrier whereby the pharmaceutical agent is released into the vagina and absorbed through the vaginal mucosa to provide relief of dysmenorrhea. The drug delivery system can be a tampon device (42), vaginal ring, pessary, tablet, suppository, vaginal sponge, bioadhesive tablet, bioadhesive microparticle, cream lotion, foam, ointment, paste solution, or gel. The system delivers a higher concentration to the muscle of the uterus, the primary site for the dyskinetic muscle contraction, which is the pathophysiologic cause of dysmenorrhea.
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STABILIZED TIBOLONE COMPOSITIONS

(WO1998047517) 29.10.1998 A61K 9/16 AKZO NOBEL N.V.
The invention pertains to a pharmaceutical dosage unit, such as a tablet or a capsule, comprising an effective amount of tibolone (generally of from 0.1 to 10 % by weight) and a starch-containing pharmaceutically acceptable carrier (also denoted as basic granulate), wherein the carrier contains of from 10 to 100 % by weight of the starch. Thus a more stable tibolone formulation is obtained, allowing dry storage and lower doses of active ingredient.
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TIMED-RELEASE LOCALISED DRUG DELIVERY BY PERCUTANEOUS ADMINISTRATION

(WO1998040118) 17.09.1998 A61B 17/34 ADVANCED RESEARCH &TECHNOLOGY INSTITUTE
Devices and methods are disclosed for the percutaneous administration of a composition to a desired $i(in vivo) location. The composition comprises a biologically active substance and a pharmaceutically acceptable carrier. The pharmaceutically acceptable carrier is preferably non-solid and a polymer, which is preferably capable of being transformed into a gel, thus allowing timed-released delivery of the substance. A preferred use for this invention is to provide local delivery of biologically active substances for the prevention of restenosis following angioplasty or other blood vessel injury.
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MULTIPLE SITE DELIVERY OF ADENOVIRAL VECTOR FOR THE INDUCTION OF ANGIOGENESIS

(WO1998032859) 30.07.1998 A61K 38/19 CORNELL RESEARCH FOUNDATION, INC.
The present invention provides a method for enhancing the level of perfusion of blood to a target tissue, treating a target tissue suffering from or at risk of suffering from ischemic damage, inducing angiogenesis in a target tissue, and/or inducing collateral blood vessel formation in a target tissue affected by or at risk of being affected by a vascular occlusion. The present inventive method comprises administering to the target tissue a dose of a pharmaceutical composition comprising (a) a pharmaceutically acceptable carrier and (b) an adenoviral vector comprising a DNA encoding an angiogenic peptide, such that the level of perfusion of blood to the target tissue is enhanced, the dose has a therapeutic or prophylactic effect on the targ...
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PHARMACEUTICAL COMPOSITION HAVING HIGH BIOAVAILABILITY AND METHOD FOR PREPARING IT

(WO1998031360) 23.07.1998 A61K 9/16 PHARMA PASS
The invention provides a composition comprising: (a) an inert hydrosoluble carrier covered with at least one layer containing an active ingredient except fenofibrate in a micronized form having a size less than 20 $g(m)m, a hydrophilic polymer and, optionally, a surfactant, the polymer making up at least 10 % by weight of (a); and (b) optionally one or several outer phase(s) or layer(s). The invention also provides a method for preparing said composition.
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CO-PROCESSED MICROCRYSTALLINE CELLULOSE AND CALCIUM CARBONATE

(WO1998024841) 11.06.1998 A61K 9/20 FMC CORPORATION
Particulate pharmaceutical tablet excipient compositions comprising co-processed microcrystalline cellulose and particulate USP calcium carbonate having a particle size distribution of 7 to 22 $g(m)m wherein the range of calcium carbonate to microcrystalline cellulose is 70:30 to 90:10.
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METHOD AND APPARATUS FOR RAPID $i(IN SITU) ANALYSIS OF PRESELECTED COMPONENTS OF HOMOGENEOUS SOLID COMPOSITIONS, ESPECIALLY PHARMACEUTICAL COMPOSITIONS

(WO1998020325) 14.05.1998 G01N 21/71 NATIONAL RESEARCH COUNCIL OF CANADA
A method and apparatus for rapid $i(in situ) spectroscopic analysis of preselected components of homogeneous solid chemical compositions, especially pharmaceutical products. The apparatus comprises a high-power pulsed laser (10) whose beam is focused on the material (18), typically a tablet or the powder prior to compaction into the tablet, which generally consists of an active ingredient (e.g. a drug) and a filler material (cellulose, glucose, lactose, etc.). The pulsed laser beam vaporizes a small volume of the pharmaceutical product and produces a plasma having an elemental composition which is representative of the pharmaceutical product. The atomic composition of the vaporized material is analyzed with an optical spectrometer (24). As ...
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FATTY ACID ESTERS OF LACTIC ACID SALTS AS PERMEATION ENHANCERS

(WO1998018417) 07.05.1998 A61K 9/70 THERATECH, INC.
A transdermal drug delivery system which enhances the delivery of the drug comprises a composition containing, as an enhancer, one or more C ┐5? to C┐21? fatty acid esters of a lactic acid salt. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant contained in a penetration-enhancing vehicle comprising 0.25 to 50% w. of the fatty acid ester of a lactic acid salt enhancer in a suitable pressure sensitive adhesive carrier vehicle formed from an aqueous emulsion based pressure sensitive adhesive.
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PHARMACEUTICAL GEL PREPARATION APPLICABLE TO MUCOSAL SURFACES AND BODY TISSUES

(WO1998017252) 30.04.1998 A61K 9/00 VIROTEX CORPORATION
The present invention relates to a non water-soluble pharmaceutical carrier gel which adheres to mucosal surfaces and body tissues upon application and forms a film, providing protection and delivery of pharmaceutical to the site of application, surrounding body tissues, and bodily fluids. The gel comprises a volatile or diffusing nonaqueous solvent and at least one non water-soluble alkyl cellulose or hydroxyalkyl cellulose. A bioadhesive polymer may also be added. The gel provides an effective residence time with ease of use. The residence time may be adjusted by adding a component which acts to adjust the kinetics of erodability of the carrier.
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IMMUNOMODULATORY FORMULATION

(WO1998010747) 19.03.1998 A61K 9/127 GALENA AS
Pharmaceutical compositions especially for internal application, in a form of drug delivery systems which create the lyotropic liquid crystals when in contact with aqueous phase. The pharmaceutical compositions consist of: (A) hydrophobic active ingredient with immunomodulatory effect from a group of N-methylated cyclic undecapeptides or macrolide antibiotics, in quantity 1,0-35,0 weight % in a carrier medium containing (B) at least one absorption promoter allowing for contact of the drug with a biological membrane or passing of the drug through in quantity 1-40 weight %; (C) nonlipidic vehicle containing at least one of the below-mentioned substances: (C1) surfactant or mixed surfactant with HLB > 9, in quantitiy 1-80 weight %; (C2) lipoph...
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CONTROLLED RELEASE MICROPARTICLES WITH A HYDROPHOBIC MATERIAL

(WO1998007412) 26.02.1998 A61K 9/16 ALKERMES CONTROLLED THERAPEUTICS, INC.
A pharmaceutical composition and a method of forming said composition for the sustained release of biologically active agent. The pharmaceutical composition of the invention comprises (a) a sustained release delivery device consisting essentially of (i) a drug delivery device having a biologically active agent disposed within said device and characterized by a plurality of interior spaces, and (ii) a hydrophobic material wherein said material is contained within a substantial number of interior spaces of the drug delivery device as to have a beneficial effect and (b) a pharmaceutical carrier. Alternatively, the pharmaceutical composition of the invention is in the substantial absence of a pharmaceutical carrier. The method of the invention ...
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CONTROLLED RELEASE TABLET

(WO1997048385) 24.12.1997 A61K 9/20 TEMPLE UNIVERSITY OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
A controlled release tablet including a pharmaceutical agent and an excipient. The excipient includes at least about 60 % of a water swellable polymer and a lubricant. The water swellable polymer is chosen such that the swelling rate of the polymer is equal to the dissolution rate of the swollen polymer. The excipient may also include such other ingredients as diluents, fillers, binders, solubilizers, emulsifiers, and other pharmacologically inactive compounds. The polymer is chosen with the pharmaceutical agent in mind such that the tablet will be fully dissolved at the same time that the last of the pharmaceutical agent is released.
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COMPOSITION AND SYSTEM FOR IONTOPHORETIC TRANSDERMAL DELIVERY OF DRUGS

(WO1997047353) 18.12.1997 A61K 9/00 NOVAGENT OY J─RNSTRÍM, Risto HIRVONEN, Jouni
The present invention relates to a pharmaceutical composition for the controlled iontophoretic transdermal delivery of a drug comprising a combination of a drug and an electrically conductive carrier, wherein the administration of the drug to the patient is intended to be enhanced by leading an electrical current from said composition to the patient's skin. According to the invention the electrically conductive carrier is a textile fiber with an ion exchanger group grafted thereto. According to a preferred embodiment the drug is tacrine or its pharmaceutically acceptable salt. The invention further concerns a system for the iontophoretic transdermal delivery of a drug to a patient. In this system, the pharmaceutical composition (22) is atta...
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SUSTAINED RELEASE OXYCODONE FORMULATIONS WITH NO FED/FAST EFFECT

(WO1997045091) 04.12.1997 A61K 9/16 EURO-CELTIQUE, S.A. OSHLACK, Benjamin CHASIN, Mark
A solid controlled release, oral dosage form, the dosage form comprising a therapeutically effective amount of oxycodone or a salt thereof together with a sustained release carrier which causes the formulation to preferentially release the drug in low pH (e.g., gastric fluid) is bioavailable and does not exhibit a fed/fast effect.
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SUSTAINED RELEASE EXCIPIENT

(WO1997026865) 31.07.1997 A61K 9/20 EDWARD MENDELL CO., INC. BAICHWAL, Anand
A sustained-release formulation for use in oral solid dosage forms includes from about 10 to about 40 percent or more by weight galactomannan gum; from about 1 to about 20 percent by weight of an ionizable gel strength enhancing agent and an inert pharmaceutical filler.
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SUSTAINED-RELEASE DRUG DELIVERY SYSTEM

(WO1997019677) 05.06.1997 A61K 9/20 PHARMAVENE, INC.
A sustained-release pharmaceutical composition comprising a highly soluble pharmaceutical agent, such as selegiline, in a pharmaceutical carrier comprising a hydrophilic polymer dispersed in a hydrophobic matrix. A hydrophilic microenvironment is created in a hydrophobic matrix by incorporating hydrophilic polymers within a hydrophobic matrix. Optionally, a binder, preferably a polyhydroyxlated compound, can also be added.
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PROMPT-RELEASE PHARMACEUTICAL COMPOSITIONS

(WO1997018798) 29.05.1997 A61K 9/00 RECORDATI S.A. CHEMICAL AND PHARMACEUTICAL COMPANY
The present invention is represented by a prompt-release pharmaceutical composition, suitable in particular for oral use, comprising: a) a plurality of nuclei having dimensions between 50 and 500 'mu'm, selected among microcrystals of the active ingredient and microgranules containing at least one active ingredient and at least one pharmaceutically acceptable excipient; b) a lipidic coating comprising a lipidic material sprayed in the melted state onto the said nuclei, and optionally at least one hydrophilic additive; c) a vehicle comprising one or more pharmaceutically acceptable excipients. The coated micronuclei can form a suspension which can be reconstituted by the patient immediately before use by simply adding the suspending phase, o...
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CONTROLLED RELEASE FORMULATION (ALBUTEROL)

(WO1997016172) 09.05.1997 A61K 9/20 EDWARD MENDELL CO., INC.
A sustained release pharmaceutical formulation and methods of making and using the same are provided. The sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional hydrophobic material and/or hydrophobic coating, and a medicament for sustained oral administration.
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PHARMACEUTICAL GRANULES

(WO1997010810) 27.03.1997 A61K 9/16 SMITHKLINE BEECHAM SEIYAKU KK AKIYAMA, Hidero MATSUMOTO, Zene UENO, Takashi
A high speed agitation granulator method of preparing a substantially spherical granule for pharmaceutical use comprising a medicament for pharmaceutical use, wherein the medicament has an aqueous solubility of 0.01 to 0.30 g/ml, which method comprises introducing a mixture of medicament and excipients composing at least 5 % crystalline cellulose into the granulator and spraying on water or a mixture of ethanol and water as binder solution; a substantially spherical granule for pharmaceutical use comprising famciclovir and 5 % or more crystalline cellulose, together with an optional coating; and a sachet containing a unit dose of famciclovir in the form of such granules.
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ORAL FAST-DISSOLVING COMPOSITIONS FOR DOPAMINE AGONISTS

(WO1997006786) 27.02.1997 A61K 9/00 R.P. SCHERER LIMITED JOHNSON, Edward, Stewart CLARKE, Anthony GREEN, Richard, David
This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, a dopamine agonist, characterised in that the composition is in the form of a fast- dispersing dosage form designed rapidly to release the active ingredient in the oral cavity. Such compositions which further comprise an anti-emetic and/or an opioid antagonist are also provided. A process for preparing such compositions, the use of such compositions for the treatment and/or evaluation of Parkinson's disease and products and kits for the administration of a dopamine agonist and the co-administration of a dopamine agonist and an anti-emetic and/or opioid antagonist are also provided.
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PHARMACEUTICAL COMPOSITIONS OF CONJUGATED ESTROGENS AND METHODS FOR THEIR USE

(WO1997004753) 13.02.1997 A61K 9/20 DURAMED PHARMACEUTICALS, INC.
This invention relates to novel pharmaceutical compositions and methods for their preparation containing conjugated estrogens for the treatment of peri-menopausal, menopausal and post-menopausal disorders in women. The novel pharmaceutical compositions comprise a carrier base material and conjugated estrogens formed into a solid unit dosage form possessing a regular incremental release of the medicament upon oral administration. Further, the invention comprises the combination of conjugated estrogens with progestogens in a solid, shaped dosage unit. Specifically, the invention comprises the use of an organic excipient such as high molecular weight hydroxyalkyl alkylcelluloses. The use of an organic excipient such as hydroxypropylmethylcellu...
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PHARMACEUTICAL COMPOSITIONS OF CONJUGATED ESTROGENS AND METHODS FOR THEIR USE

(WO1997004752) 13.02.1997 A61K 9/20 DURAMED PHARMACEUTICALS, INC.
This invention relates to novel pharmaceutical compositions containing conjugated estrogens for the treatment of peri-menopausal, menopausal and post-menopausal disorders in women. The novel pharmaceutical compositions comprise a carrier base material and conjugated estrogens formed into a solid unit dosage form possessing a regular incremental release of the medicament upon oral administration. Further, the invention comprises the combination of conjugated estrogens with progestogens in a solid, shaped dosage unit. Specifically, the invention comprises the use of an organic excipient such as high molecular weight hydroxyalkyl alkylcelluloses. The use of an organic excipient such as hydroxypropylmethylcellulose in a stable, solid dosage for...
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NOVEL FORMULATION FOR PEPTIDE RELEASE

(WO1997000693) 09.01.1997 A61K 9/00 PEPTIDE TECHNOLOGY LIMITED WALSH, John, Desmond TRIGG, Timothy, Elliot
A pharmaceutical and/or veterinary formulation comprising deslorelin and an excipient, the formulation being characterised in that, in vitro, it releases deslorelin into phosphate buffered saline, as hereinbefore described, at 37 ░C at a rate of about 2-80 'mu'g/day for at least 200 days. The formulation may be used for prevention of reproductive function, particularly in dogs and cats, and for the treatment, particularly in humans, of prostate and breast cancer and other diseases and conditions where suppression of testosterone or estradiol levels is beneficial.
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PURIFIED GALACTOMANNAN AS AN IMPROVED PHARMACEUTICAL EXCIPIENT

(WO1996040163) 19.12.1996 A61K 9/20 CIBUS PHARMACEUTICAL, INC.
Disclosed is a substantially anhydrous, powdered, galactomannan composition consisting essentially of a galactomannan hydrocolloid exhibiting about 50 % to about 90 % by weight of anhydromannose residues and about 10 % to about 50 % by weight anhydrogalactose residues; less than about 1 % by weight of protein material and less than about 3 % of other nonaqueous impurities. This material is useful for preparing pharmaceutical compositions both in the substantially anhydrous form but preferably in a hydrated form which includes about 5-15 % by weight water. The pharmaceutical compositions comprise a therapeutically effective amount of a drug, the hydrated powdered galactomannan composition and optionally other pharmaceutically-acceptable exci...
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ORAL ACYCLOVIR DELIVERY

(WO1996040144) 19.12.1996 A61K 9/107 PHARMAVENE, INC.
A pharmaceutical preparation for oral acyclovir delivery comprising a stable, hydrophobic emulsion comprising continuous phase of a hydrophobic material selected from the group consisting of a long chain carboxylic acid or ester or alcohol thereof dispersed in an aqueous phase or having a hydrophilic discontinuous phase dispersed in a hydrophobic phase of a long chain carboxylic acid or alcohol thereof. The emulsion with acyclovir is incorporated into a pharmaceutical carrier suitable for oral delivery.
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CONTINUOUS FLUOROCHEMICAL MICRODISPERSIONS FOR THE DELIVERY OF PHARMACEUTICAL AGENTS

(WO1996040053) 19.12.1996 A61K 9/00 ALLIANCE PHARMACEUTICAL CORP. TREVINO, Leo, A. DELLAMARY, Luis, A. TARARA, Thomas, E. WEERS, Jeffry, G. RANNEY, Helen, M.
A method for preparing a pharmaceutical microdispersion exhibiting enhanced bioavailability, including the steps of providing a thermodynamically stable pharmaceutical composition comprising at least one pharmaceutical agent incorporated in a physiologically acceptable liquid carrier, the liquid carrier comprising one or more lipophilic solvents such as fluorochemicals and preferably at least one nonfluorinated co-solvent, and combining the stable pharmaceutical composition with an amount of at least one miscible diluent sufficient to initiate phase separation of the pharmaceutical agent from the pharmaceutical composition wherein a microdispersion of the pharmaceutical composition is formed. Also disclosed are microdisperse pharmaceutical ...
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CHEMOTHERAPEUTIC COMPOSITIONS

(WO1996038186) 05.12.1996 A61K 31/765 CHEMEQ PTY. LIMITED MELROSE, Graham, John, Hamilton
The present invention relates to the treatment of gastrointestinal disease and/or cancer, and a method of weight gain, via the ingestion of polymeric compositions in humans, animals or birds in need of said treatment. The invention provides methods for the treatment of cancer, the treatment and/or prevention of gastrointestinal disease and/or infection and/or diarrhoea, and a method for increasing weight gain in humans, animals or birds comprising administering to said humans, animals or birds an effective amount of a pharmaceutical or veterinary composition or feed additive, comprising an effective amount of a polymer and/or copolymer, having the repeating polymeric unit (I) wherein R is H or alkyl, usually C1 to C4, or this unit in hydrat...
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ORAL INSULIN DELIVERY

(WO1996037215) 28.11.1996 A61K 9/107 PHARMAVENE, INC.
A pharmaceutical preparation for oral insulin delivery comprising a stable, hydrophobic emulsion comprising continuous phase of a hydrophobic material selected from the group consisting of a long chain carboxylic acid or ester or alcohol thereof dispersed in an aqueous phase or (ii) having a hydrophilic discontinuous phase dispersed in a hydrophobic phase of a long chain carboxylic acid or alcohol thereof. The emulsion with insulin is incorporated into a pharmaceutical carrier suitable for oral delivery.
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ARTIFICIAL SKIN CONTAINING AS SUPPORT BIOCOMPATIBLE MATERIALS BASED ON HYALURONIC ACID DERIVATIVES

(WO1996033750) 31.10.1996 A61K 35/12 FIDIA ADVANCED BIOPOLYMERS S.R.L. SORANZO, Carlo ABATANGELO, Giovanni CALLEGARO, Lanfranco
Artificial human skin comprising: a) microperforated membrane based on a hyaluronic acid derivative, on which keratinocytes have been seeded and cultured, b) an underlying non-woven tissue based on a hyaluronic acid derivative wherein fibroblasts have been seeded and left to proliferate. The artificial human skin according to the present invention can be therefore advantageously used in medicine, in surgery, in diagnostics and as a vehicle for preparing a controlled release medicament. Lastly, this artificial human skin can be frozen to -80 ░C or placed in liquid nitrogen and stored, so that a tissue bank can be created.
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TAMPER EVIDENT PHARMACEUTICAL DOSAGE FORM

(WO1996033702) 31.10.1996 A61K 9/48 R.P. SCHERER CORPORATION TANNER, Keith ORANGE, Kelly
A dosage form for pharmaceuticals, nutrient supplements and food products which is nontoxic and suitable for introduction into mammalian bodies comprising soft elastic gelatin capsule containing a colorless clear liquid carrier and an active ingredient. The capsule is rendered particularly tamper evident by color neutralizing its inherent amber/yellow color with edible dyes and pigments.
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CONTROLLED RELEASE FORMULATION FOR WATER SOLUBLE DRUGS IN WHICH A PASSAGEWAY IS FORMED IN SITU

(WO1996033700) 31.10.1996 A61K 9/00 ANDRX PHARMACEUTICALS, INC.
A controlled release pharmaceutical tablet is disclosed which is based on: (a) a compressed core which contains: i) a medicament; ii) from 5 to 20 % by weight of a water soluble osmotic agent based on the total weight of the compressed core; iii) a water soluble pharmaceutically acceptable polymeric binder; iv) a conventional pharmaceutical excipient; and (b) a dual layer membrane coating around said core which consists essentially of: i) a first inner coating layer for sustained release of the medicament, said inner coating layer consisting essentially of a plasticized water insoluble pharmaceutically acceptable polymer and a pharmaceutically acceptable water soluble polymer, and; ii) a second outer coating layer for immediate release of a...
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CONTROLLED RELEASE INSUFFLATION CARRIER FOR MEDICAMENTS

(WO1996031198) 10.10.1996 A61K 9/14 EDWARD MENDELL CO., INC.
Controlled release powder insufflation formulations are disclosed. The powder formulation includes cohesive composites of particles containing a medicament and a controlled release carrier which preferably includes one or more polysaccharide gums of natural origin.
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CONTROLLED RELEASE TABLET

(WO1996026718) 06.09.1996 A61K 9/20 TEMPLE UNIVERSITY OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
A controlled release tablet including a pharmaceutical agent and an excipient. The excipient includes at least about 50 % of a water swellable polymer and a lubricant. The water swellable polymer is chosen such that the swelling rate of the polymer is equal to the dissolution rate of the swollen polymer. The excipient may also include such other ingredients as diluents, fillers, binders and other pharmacologically inactive compounds. The polymer is chosen with the pharmaceutical agent in mind such that the tablet will be fully dissolved at the same time that the last of the pharmaceutical agent is released.
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PHARMACEUTICAL EXCIPIENT HAVING IMPROVED COMPRESSIBILITY

(WO1996022080) 25.07.1996 A61K 9/20 EDWARD MENDELL CO., INC. STANIFORTH, John, N. SHERWOOD, Bob, E. HUNTER, Edward, A.
A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression. Figure graphically shows a comparison of the tensile strength of tablets prepared in accordance with the invention and prior art tablets. Dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and an effective amount of a surfactant, which, in preferred embodiments is an anionic surfactant present in amounts ranging from about 0.1 % to about 0.5 %, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and surfactant are in intimate association with each other. One preferred anionic surfactant utilized in the novel ex...
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PHARMACEUTICAL EXCIPIENT HAVING IMPROVED COMPRESSIBILITY

(WO1996021429) 18.07.1996 A61K 9/20 EDWARD MENDELL CO., INC.
A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1 % to about 20 % silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.
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NSAID DELIVERY EMPLOYING A POWDERED HYDROCOLLOID GUM OBTAINABLE FROM HIGHER PLANTS

(WO1996016639) 06.06.1996 A61K 9/20 CIBUS PHARMACEUTICAL, INC.
An oral-delivery pharmaceutical composition for reducing the gastric irritation effect of an NSAID in the upper GI tract of a mammal. The composition includes (a) a mucosal protective amount of a pharmaceutically-acceptable hydrocolloid gum obtainable from higher plants, (b) a dispersion-enhancing amount of another excipient and (c) a therapeutically-effective amount of an NSAID. Also disclosed is a process for preparing the composition and a method for reducing the gastric irritation effect of the NSAID by administering the composition. Also, disclosed is a composition particularly useful for preparing an aqueous suspension.
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SUSTAINED-RELEASE DRUG DELIVERY EMPLOYING A POWDERED HYDROCOLLOID GUM OBTAINABLE FROM HIGHER PLANTS

(WO1996016638) 06.06.1996 A61K 9/20 CIBUS PHARMACEUTICAL, INC.
An oral-delivery pharmaceutical composition for achieving sustained release of a drug in a mammal. The composition includes (a) a suitable amount of a pharmaceutically-acceptable hydrocolloid gum obtainable from higher plants (e.g., about 20 % - 90 % by weight), (b) another excipient (e.g., about 5 % - 30 % by weight) that aids in sustained release and (c) a therapeutically-effective amount of a drug. Preferably the mean particle size of the gum is about 150'mu' or less. Also disclosed is a process for preparing the composition and a method for achieving sustained release of a drug by administering the composition to a subject in need thereof.
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METHODS AND MEANS FOR DRUG ADMINISTRATION

(WO1996005840) 29.02.1996 A61K 31/5575 PHARMACIA AB STJERNSCHANTZ, Johan SEL╔N, G÷ran
Method and means for delivery of drugs to the optic nerve head and the region surrounding it which comprises contacting the surface of the eye with an effective amount of a drug for treatment of said nerve head and a physiologically acceptable prostaglandin or prostaglandin derivative for enhancing delivery of the drug to the nerve head, in an opththalmologically acceptable carrier.
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PREDNISOLONE METASULPHOBENZOATE PREPARATION FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE

(WO1996004918) 22.02.1996 A61K 9/16 FLEXPHARM LIMITED SPEIRS, Christopher, James
The dissolution at pH 6.5 of prednisolone metasulphobenzoate or a pharmacologically acceptable salt thereof from a non-disintegratable solid enteric composition comprising the prednisolone metasulphobenzoate in an excipient matrix is increased by the presence in the matrix of a rheological modifying agent, especially croscarmellose, in an amount of at least 5 percent by weight of the composition but insufficient to cause disintegration. Preferably the composition is in the form of pellets coated with an enteric coating which is substantially insoluble below pH 7 and contained in a capsule or tablet coated with an enteric coating which is soluble at a pH in the range pH 5.5 to pH 7. The coated capsules and tablets are for use in the treatmen...
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SOLID DELIVERY SYSTEMS FOR CONTROLLED RELEASE OF MOLECULES INCORPORATED THEREIN AND METHODS OF MAKING SAME

(WO1996003978) 15.02.1996 A61K 9/14 QUADRANT HOLDINGS CAMBRIDGE LIMITED ROSER, Bruce, Joseph COLACO, Camilo JERROW, Mohamed, Abdel, Zahra BLAIR, Julian, Alexander KAMPINGA, Jaap WARDELL, James, Lewis DUFFY, John, Alistair
The present invention encompasses solid dose delivery systems for administration of guest substances. Preferred delivery systems are suitable for delivery of bioactive materials to subcutaneous and intradermal, intramuscular, intravenous tissue, the delivery system being sized and shaped for penetrating the epidermis. The delivery systems comprise a vitreous vehicle loaded with the guest substance and capable of releasing the guest substance in situ at various controlled rates. The present invention further includes methods of making and using the solid dose delivery systems.
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PHARMACEUTICAL COMPOSITIONS, MAINLY VAGINAL SUPPOSITORY, CONTAINING MANY DIFFERENT ACTIVE INGREDIENTS

(WO1996003135) 08.02.1996 A61K 9/00 MILANKOVITS, M▀rton
The invention relates to pharmaceutical preparations, vaginal suppositories, ointments, solutions, painting solutions, vaginal drops, talc powders, etc. containing many different active ingredients. The basis of the invention is that the pharmaceutical preparation according to the invention contains at least three from the following components: a) an antibiotic, preferably chloramphenicol or erythromycin; b) sulphonamide, preferably sulfadiamidin; c) clotrimazol (bis-phenyl-(2-chlorophenyl)-1- imidazolyl-methane) or natamycin or nystatin; and d) nitro-metronidazol, that is metronidazol or tinidazol or nimorazol, together with an appropriate carrier; in given case together with borax and inactive ingredients and/or carriers and/or additives k...
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HEPARIN-BINDING PROTEIN FOR THE TREATMENT OF SEPSIS AND PROCESSES FOR ITS PREPARATION

(WO1995028949) 02.11.1995 A61K 38/00 NOVO NORDISK A/S FLODGAARD, Hans, Jakob, Hem RASMUSSEN, Poul, Baad
Pharmaceutical composition for the prevention or treatment of diseases or conditions associated with induction of the cytokine cascade by lipopolysaccharide (LPS), the composition comprising a heparin-binding protein (HBP) which, in glycosylated form, has an apparent molecular weight of 28 kD (as determined by SDS-PAGE under reducing conditions), the protein being produced in the azurophil granules of polymorphonuclear leukocytes, together with a pharmaceutically acceptable carrier or diluent. The heparin-binding protein is produced in host cells containing a DNA sequence encoding N-terminally extended HBP or encoding HBP preceded by and fused to a DNA sequence encoding another protein. Also disclosed is a process wherein the culture medium...
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ONCE-A-DAY METOPROLOL ORAL DOSAGE FORM

(WO1995028917) 02.11.1995 A61K 9/20 EDWARD MENDELL CO., INC. BAICHWAL, Anand, R. McCALL, Troy, W.
A sustained release oral solid dosage form of metoprolol pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, a cationic cross-linking agent. The formulation provides release of metoprolol for at least about 24 hours. Methods of preparation and methods of treatment using the preparations of the invention are also disclosed.
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SUSTAINED RELEASE EXCIPIENT

(WO1995028916) 02.11.1995 A61K 9/20 EDWARD MENDELL CO., INC. BAICHWAL, Anand, R. McCALL, Troy, W.
A sustained-release excipient for use in oral solid dosage forms includes from about 15 to about 30 percent or more by weight heteropolysaccharide gum; an effective amount of a cationic cross-linking agent capable of cross-linking the heteropolysaccharide in an environment of use; and an inert pharmaceutical filler.
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DELIVERY SYSTEMS FOR HYDROPHOBIC DRUGS

(WO1995024893) 21.09.1995 A61K 9/48 R.P. SCHERER LIMITED LACY, Jonathan, Ernest EMBLETON, Jonathan, Kenneth
There is provided a carrier for hydrophobic drugs, and pharmaceutical compositions based thereon, which carrier comprises a digestible oil and a pharmaceutically acceptable surfactant component for dispersing the oil in vivo upon administration of the carrier, which comprises a hydrophilic surfactant, said surfactant component being such as not to substantially inhibit the in vivo lipolysis of the digestible oil.
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COPROCESSED GALACTOMANNAN - GLUCOMANNAN

(WO1995017831) 06.07.1995 A23C 19/076 FMC CORPORATION
A composition comprising: (A) a coprecipitate consisting essentially of: (a) a galactomannan, with (b) a glucomannan; and (B) optinally, a gelling agent admixed with the formed coprecipitate. Preferably, the galactomannan is locust bean gum, the glucomannan is derived from konjac, and the gelling agent is carrageenan. In another embodiment, this invention comprises a method for preparing a coprecipitate of a galactomannan with a glucomannan, such method comprising: (A) mixing a galactomannan with an aqueous medium (optionally accompanied by heat and/or agitation) to form a galactomannan sol; (B) mixing a glucomannan in similar manner with the same or another volume of the aqueous medium to form a glucomannansol; (C) comixing the galactomann...
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EXPULSION OF MATERIAL FROM A DELIVERY DEVICE

(WO1995017172) 29.06.1995 A61K 9/48 R.P. SCHERER CORPORATION STEVENS, Howard, Norman, Ernest RASHID, Abdul BAKHSHAEE, Massoud BINNS, Julie, Stephanie MILLER, Christopher, Jon
A delivery device for delivering an active substance (12) to a patient at a predetermined time after administration comprises a male hydrogel plug (2) engaged in the neck (4) of a female body (6). An expandible excipient (10) such as a hydrogel powder or a pharmaceutical disintegrant in powder, slug or tablet form is provided beneath the active substance. In contact with an aqueous medium, the excipient absorbs water and swells such as to rapidly expel the active substance and effectively deliver it from the device.
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SUSTAINED RELEASE FORMULATIONS FOR 24 HOUR RELEASE OF METOPROLOL

(WO1995013055) 18.05.1995 A61K 9/20 EDWARD MENDELL CO., INC.
A sustained release oral solid dosage form of metoprolol pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, a cationic cross-linking agent, and metoprolol provides release of metoprolol for at least about 24 hours. In certain embodiments, the sustained release formulation further includes a hydrophobic material.
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DESFERRIOXAMINE ORAL DELIVERY SYSTEM

(WO1995011690) 04.05.1995 A61K 9/16 EMISPHERE TECHNOLOGIES, INC. MILSTEIN, Sam, J. BARANTSEVITCH, Evgueni, N.
Modified amino acids and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. The modified amino acids are preparable by reacting single amino acids or mixtures of two or more kinds of amino acids with an amino modifying agent such as benzene sulfonyl chloride, benzoyl chloride, and hippuryl chloride. The modified amino acids may form encapsulating microspheres in the presence of the active agent under sphere-forming conditions. Alternatively, the modified amino acids may be used as a carrier by simply mixing the amino acids with the active agent. The preferred acylated amino acid carrier is salicyloyl-phenylalanine. The modified amino acids are particularly useful in delivering biologicall...
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SENNA DOSAGE FORM

(WO1995011032) 27.04.1995 A61K 9/28 THE PROCTER &GAMBLE COMPANY
This invention relates to a pharmaceutical laxative composition in unit dosage form, for peroral administration of sennosides to a human or other animal subject, comprising a safe and effective amount of sennosides in a rapidly dissolving matrix; and a proximal colonic delivery carrier which effects release of said sennosides substantially near the junction between the small intestine and the colon or within the colon of said subject. This invention also involves methods for providing laxation for humans and other animals in need thereof by peroral administration of such compositions.
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A NOVEL PHARMACEUTICAL FOR ORAL ADMINISTRATION COMPRISING PROGRESTERONE AND A POLYETHYELENE GLYCOL TOGETHER WITH AN EXCIPIENT

(WO1995005807) 02.03.1995 A61K 9/20 NOVO NORDISK A/S GRAM, Karen, Susanne JENSEN, Annelise
A pharmaceutical composition for oral administration of progesterone may, conveniently, contain a PEG, and a further excipient selected from the group comprising a starch, a cellulose, pecting, and tragacanth.
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DELAYED RELEASE CARNITINE

(WO1995005168) 23.02.1995 A61K 9/50 SHUG, Austin, L. GULBRANDSEN, Carl, E.
A sustained release, orally administered pharmaceutical composition comprising carnitine and an acceptable pharmaceutical excipient is described for the treatment of carnitine deficiency and other carnitine responsive conditions. The sustained release formulation avoids the characteristic problems of gastrointestinal invitation, dumping in the urine and bacterial degradation attendant previously known oral formulations of carnitine.
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NEW PHARMACEUTICAL COMPOSITIONS FOR TOPICAL USE CONTAINING HYALURONIC ACID AND ITS DERIVATIVES

(WO1995003786) 09.02.1995 A61K 9/12 FIDIA ADVANCED BIOPOLYMERS S.R.L. BENEDETTI, Luca CALLEGARO, Lanfranco
Provided is a pharmaceutical composition, comprising a pharmaceutically effective amount of an acidic polysaccharide and/or a derivative thereof, a gaseous vehicle, and a pharmaceutically acceptable carrier or excipient. Said acidic polysaccharide or derivative thereof can be hyaluronic acid, a pharmaceutically acceptable salt of hyaluronic acid, a partial or total ester of hyaluronic acid with an alcohol, a partial or total intermolecular ester of hyaluronic acid, a partial or total intramolecular ester of hyaluronic acid, a cross-linked ester of hyaluronic acid, an alginic acid ester, an ester of carboxymethylcellulose, an ester of carboxymethylchitin, an ester of carboxymethyl starch, a gellan ester, a cross-linked gellan ester, a pectic...
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METHOD FOR MAKING FREEZE DRIED DRUG DOSAGE FORMS

(WO1995001782) 19.01.1995 A61K 9/20 R.P. SCHERER CORPORATION WONG, Sang, K. KEARNEY, Patrick
The present invention discloses an improved technique for preparing a rapidly dispersing pharmaceutical tablet of a granular therapeutic agent which has both relatively low solubility and relatively large particle size. Xanthan gum is added to a liquid admixture of solvent, carrier components, and the granular therapeutic agent. The xanthan gum not only facilitates suspension of the granular therapeutic agent in the liquid admixture, but, more surprisingly, does so without adversely affecting the dispersion qualities and texture of the tablet in the patient's mouth upon administration.
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PREPARATION OF MICROPARTICLES AND METHOD OF IMMUNIZATION

(WO1994027718) 08.12.1994 A61K 9/16 O'HAGAN, Derek, Thomas McGEE, John, Paul DAVIS, Stanley, Stewart
The present invention describes a method for producing microparticles useful in the formulation of pharmaceutical compositions. The present invention further describes a method of immunizing a mammal against diseases comprising administering to a mammal an effective amount of antigen containing microparticles. In particular, the present invention describes a method of potentiating an immune response in a mammal comprising administering an effective amount of a pharmaceutical composition to a mammal. The present invention further describes a vaccine comprising a pharmaceutical composition containing said microparticles. An antigen delivery system comprising microparticles containing entrapped antigens is further described by the present inve...
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POLYMERIC X-RAY CONTRAST COMPOSITIONS CONTAINING IODINATED POLYMERIC BEADS

(WO1994025075) 10.11.1994 A61K 49/04 STERLING WINTHROP INC.
Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material in combination with a divalent cation capable of forming a coating on the gastrointestinal tract and iodinated polymeric, water-insoluble beads having a particle size of from about 0.01 to about 1000mu wherein said iodinated polymeric beads comprise a polymer containing repeating units of formula (I) wherein A is a repeating organic unit in the backbone chain of the polymer; and X is an organic moiety containing or iodinated aromatic group and a hydrophilic group, said moiety having an iodine content within the range of from about 40 to about 80 weight percent based on the molecular weight of X, in a pha...
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READILY AVAILABLE KONJAC GLUCOMANNAN SUSTAINED RELEASE EXCIPIENT

(WO1994015643) 21.07.1994 A61K 9/20 FMC CORPORATION
A solid dosage form, such as a pharmaceutical tablet, containing a rapidly hydratable konjac glucomannan sustained release excipient such as clarified konjac, cryogenically ground konjac and plasticized konjac. The method of making the tablets by compressing excipient and pharmaceutically active ingredient as dry powders.
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PROCESS FOR PREPARING CONTROLLED RELEASE PHARMACEUTICAL FORMS AND THE FORMS THUS OBTAINED

(WO1994014421) 07.07.1994 A61K 9/20 DIOLAITI, Luigi MOTTA, Giuseppe
An improved process for preparing controlled release pharmaceutical forms comprises exposing a mixture comprising one or more excipients and one or more active ingredients compatible with each other and with said excipients to mechanical or electromechanical actions for a well established time and within a wide range of frequencies to give tablets, matrices or mono or multilayered films. Said forms can be optionally crushed to give a granulate or powder. Depending on the employed excipient, a delayed or rapid but always controllable release of the active ingredient can be attained.
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NON-AQUEOUS LIQUID POWDER

(WO1994014403) 07.07.1994 A61K 8/58 SAFE &DRY COMPANY, INC.
This invention discloses a dusting body powder which is applied as a lotion or a cream and which then evaporates to a powder. By applying it as a lotion or cream, all cracks and pores of the skin are filled. By virtue of the volatility of the cyclic silicone fluid containing delivery vehicle and its evaporation, a powder results which leaves no greasy residue on the skin. The liquid powder according to the present invention comprises a purified starch powder mixed with a volatile cyclomethicone silicone fluid, preferably in equal amounts by weight.
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PHARMACEUTICAL POWDER COMPOSITION CONTAINING NON-IONIC CELLULOSE ETHER DERIVATIVE AND A CHITIN-DERIVED POLYMER

(WO1993024149) 09.12.1993 A61K 9/00 THE PROCTER &GAMBLE COMPANY KOOCHAKI, Patricia, Elaine
A pharmaceutical composition in powder form comprising a drug and a pharmaceutically-acceptable carrier, the carrier comprising a non-ionic cellulose ether derivative and a chitin-derived polymer. The pharmaceutical composition provides a high availability of the active ingredient and displays improved adhesion characteristics.
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OIL-IN-WATER EMULSIONS OF POSITIVELY CHARGED PARTICLES

(WO1993018852) 30.09.1993 A61K 8/06 YISSAM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM BENITA, Simon ELBAZ, Efrat
An oil-in-water emulsion useful as a delivery vehicle of hydrophobic ingredients such as pharmaceutical drugs and cosmetic active agent; wherein the emulsion particles have a net positive charge (i.e. a positive zeta potential).
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COMPOSITION AND METHOD FOR IMPROVING ORAL BIOAVAILABILITY OF CARBAMAZEPINE

(WO1993010794) 10.06.1993 A61K 31/55 UNIVERSITY OF FLORIDA
The invention provides compositions for use in improving the oral bioavailability of carbamazepine comprising, in oral dosage form, a therapeutically effective amount of carbamazepine complexed with cyclodextrin selected from the group consisting of hydroxypropyl and hydroxyethyl derivatives of $g(b)- and $g(g)-cyclodextrin, the complex comprising at least 2 molecules of cyclodextrin per molecule of carbamazepine; and a non-toxic pharmaceutically acceptable carrier therefor. Also provided are compositions comprising, in oral dosage form, a therapeutically effective amount of carbamazepine in an aqueous solution comprising from about 20 % to about 50 % cyclodextrin selected from the group consisting of hydroxypropyl and hydroxyethyl derivati...
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METHOD FOR THE PREPARATION OF PROLONGED-RELEASE ORAL PHARMACEUTICAL FORMS CONTAINING ACTIVE SUBSTANCES HAVING A SOLUBILITY DEPENDENT UPON THE pH VALUE

(WO1993000889) 21.01.1993 A61K 9/16 L.C. PHARCHEM LTD. CONTE, Ubaldo GIUNCHEDI, Paolo
A method is described which permits the release of a pharmaceutical product having weakly basic characteristics so as to be very soluble in an acid pH and virtually insoluble in a basic pH, at a constant rate, independently of the pH conditions in which the pharmaceutical product and the pharmaceutical form obtained from the latter are found. The method consists in the preparation of pellets composed of an active principle, a swellable polymeric material and a gastroresistant polymeric material. By carrying these pellets in a natural or synthetic polymeric material which is gellable and hydrophilic, or in a lipophilic polymeric or non-polymeric material, it is possible to obtain modified-release pharmaceutical forms which are capable of rel...
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TOPICAL 5-FLUOROURACIL PRODRUG COMPOSITION AND METHOD

(WO1992017180) 15.10.1992 A61K 31/505 UNIVERSITY OF FLORIDA
A pharmaceutical composition in unit dosage form adapted for topical administration to a human or non-human animal in need thereof comprising a pharmacologically effective amount of a prodrug of 5- fluorouracil having formula (I), wherein R1 and R2 may be the same or different and are selected from the group consisting of H, R3CO- and R4-O- CO with the proviso that both R1 and R2 may not be H; or a non-toxic pharmaceutically acceptable salt, adduct, oxide or other derivative thereof; a pharmaceutically acceptable, topically administratable carrier therefor; and a method for topically applying the composition. R3 and R4 comprise groups such that the prodrug (1) has an enhanced delivery across topical membranes and (2) hydrolyzes after delivery...
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A SINGLE DOSE VACCINATION SYSTEM

(WO1992017165) 15.10.1992 A61K 9/00 CSL LIMITED
The invention provides a pharmaceutical or veterinary implant, which when parenterally administered releases a pulse of at least one biologically active material at a controllable time interval after implantation. The implant comprises the biologically active material; an excipient comprising at least one water soluble material and at least one water insoluble material; and a polymer film coating adapted to rupture at a predetermined period of time after implantation, and wherein the excipients and polymers are biocompatible. The biologically active material is selected from the group consisting of antigens, antibodies, hormones, growth promotants, antibiotics, nutrients, minerals and vitamins. Preferably the excipient comprises a combinati...
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THE USE OF 5-AMINOSALICYLIC ACID IN THE TREATMENT OF IRRITABLE BOWEL SYNDROME - DIARRHEAL PHASE OR TYPE (IBS-D)

(WO1992016214) 01.10.1992 A61K 9/00 NORWICH EATON PHARMACEUTICALS INC.
Treatment for a human or other mammal afflicted with IBS-D, comprising the topical delivery to the intestinal tract of said human or other mammal, preferably the large intestine, of a safe and effective amount of a pharmaceutical composition consisting essentially of the 5-ASA active ingredient and pharmaceutically acceptable excipients. Said topical delivery is preferably accomplished by the oral administration to said human or other mammal of a delayed-release composition consisting essentially of said 5-ASA active ingredient and a pharmaceutically acceptable excipient.
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THE USE OF 5-AMINOSALICYLIC ACID IN THE TREATMENT OF IRRITABLE BOWEL SYNDROME - DIARRHEAL PHASE OR TYPE (IBS-D)

(WO1992016206) 01.10.1992 A61K 9/00 NORWICH EATON PHARMACEUTICALS INC.
Treatment for a human or other mammal afflicted with IBS-D, comprising the topical delivery to the intestinal tract of said human or other mammal, preferably the large intestine, of a safe and effective amount of a pharmaceutical composition consisting essentially of the 5-ASA active ingredient and pharmaceutically-acceptable excipients. Said topical delivery is preferably accomplished by the oral administration to said human or other mammal of a delayed-release composition consisting essentially of said 5-ASA active ingredient and a pharmaceutically- acceptable excipient.
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COMPOSITION FOR SOLID PHARMACEUTICAL PREPARATIONS CONTAINING VITAMIN D3 DERIVATIVE AND PROCESS FOR PREPARATION THEREOF

(WO1991016899) 14.11.1991 A61K 9/20 SUMITOMO PHARMACEUTICALS CO., LTD. WISCONSIN ALUMNI RESEARCH FOUNDATION
A composition for solid pharmaceutical preparations containing a vitamin D3 derivative capable of permitting the derivative to be uniformly distributed in the composition while being stabilized. The composition contains an excipient consisting of mannitol and sugar, a degradative agent consisting of hydroxypropyl cellulose, and a binder consisting of polyvinyl pyrrolidone and hydroxypropylmethyl cellulose.
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ERIODICTYON DRUG DELIVERY SYSTEMS

(WO1991014441) 03.10.1991 A61K 9/00 PARNELL PHARMACEUTICALS, INC.
Methods, compositions and systems are provided for delivering a drug to the skin or mucosa. The invention involves the use of eriodictyon fluid extract as an excipient in compositions and systems for administering drugs topically, transdermally or transmucosally. The invention also relates to methods of using eriodictyon fluid extract to reduce skin or mucosal irritation and as a moisturizer.
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TRANSDERMAL DRUG DELIVERY COMPOSITION

(WO1990008553) 09.08.1990 A61K 9/70 ABBOTT LABORATORIES MOU-YING, Fu, Lu HO-WAH, Hui
Pharmaceutical compositions having enhanced membrane permeability that comprise a therapeutically active ingredient, a penetration enhancer, a solubilizing agent and a solvent vehicle. These compositions are useful in oral and transdermal applications.
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DIRECTLY COMPRESSIBLE SUSTAINED RELEASE EXCIPIENT

(WO1990003165) 05.04.1990 A61K 9/20 EDWARD MENDELL CO., INC.
A free-flowing directly compressible granulation useful as a slow release pharmaceutical excipient is disclosed. The excipient includes a hydrophilic matrix which includes a heteropolysaccharide and a polysaccharide material capable of cross-linking the heteropolysaccharide, and an inert diluent.
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PCT - World Patents in Excipients, Delivery and Release of Pharmaceutical
Compositions and Actives Published from 1990 to 2007
World  Patents Published  in 2008
 
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WORLD PATENTS IN EXCIPIENTS, DELIVERY AND RELEASE OF PHARMACEUTICAL ACTIVES PUBLISHED FROM 1990 TO 2007
This list includes patent documents published by the World Intellectual Property Organization (WIPO). The list was retrieved by searching the claims section of all patent applications. Salient
search terms included pharmaceutical formulations, excipients, strips, gums, cellulose, lozenge, tablets, capsules, suppositories; solid dosage, nasal inhalation; time, control or sustained
drug release; polysaccharides, polymeric excipients, hyaluronic acid, micro- and nano-spheres, carbomer, povidone, polyacrylates, polymerthacrylates; emulsions; enemas, vaginal, rectal,
nasal, ocular or buccal administration of medications, etc.