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WORLD PATENTS IN PHARMACEUTICAL EXCIPIENTS AND FORMULATIONS GRANTED IN 2009


Title: CROSS-LINKED DEXTRIN AS A TABLET DISINTEGRANT/EXCIPIENT

Publication No: WO2009/153798
Pub. Date - Int. Class - Applicant: - 23.12.2009 - A61K 9/20 - NATCO PHARMA LIMITED
Disintegrants are the essential components of a tablet. Cross-linking of dextrin with epichlorohydrin induces hydrophobization in hydrophilic dextrin. This in turn gives good swelling power in water. Dextrin is cross-linked with various ratios of epichlorohydrin to dextrin by weight. Cross-linking is done from 5-50% ratio of epichlorohydrin. The swelling capacity is highest with 20% cross-linking. The cross-linked dextrin is evaluated for disintegrating action by preparation of paracetamol tablets by wet granulation method and folic acid tablets by direct compression technique. In wet granulation technique, tablets prepared using 20% cross-linked dextrin disintegrated in less than one minute and by direct compression technique tablet disint...


Title: ANTIVIRAL COMPOSITIONS, METHODS OF MAKING AND USING SUCH COMPOSITIONS, AND SYSTEMS FOR PULMONARY DELIVERY OF SUCH COMPOSITIONS

Publication No: WO2009/143011
Pub. Date - Int. Class - Applicant: - 26.11.2009 - A61K 9/72 - NOVARTIS AG
A pharmaceutical composition comprises particles comprising an antiviral active, wherein the particles have a mass median aerodynamic diameter from about 1 m to about 7 m and a bulk density less than about 1.0 g/cm3. A pharmaceutical composition comprises a powder including an effective amount of antiviral and pharmaceutically acceptable excipient, wherein the powder comprises particles comprising having a mass median aerodynamic diameter from about 1 m to about 7 m, and a bulk density less than about 1.0 g/cm3. Also provided are pharmaceutical compositions comprising combinations of two or more antiviral actives. Also provided are unit dosage forms, methods of making and usi...


Title: CLONIDINE FORMULATIONS IN A BIODEGRADABLE POLYMER CARRIER

Publication No: WO2009/129460
Pub. Date - Int. Class - Applicant: - 22.10.2009 - A61K 31/4162 - WARSAW ORTHOPEDIC, INC.
Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.


Title: SINGLE DOSAGE PHARMACEUTICAL FORMULATION COMPRISING EPROSARTAN MESYLATE

Publication No: WO2009/124983
Pub. Date - Int. Class - Applicant: - 15.10.2009 - A61K 9/16 - LEK PHARMACEUTICALS D.D.
A dry formulation or granulation of eprosartan mesylate is described which comprises eprosartan mesylate in particulate form with a particle size, wherein at least 65 v/v % eprosartan mesylate particles fall in a particle size range of from 2 to 27 m. In another aspect, a dry formulation or granulation of eprosartan mesylate comprises eprosartan mesylate combined with an excipient which at least comprises a PEG having molecular weight in the range of 400 to 20000 and mannitol. Further described is a single dosage pharmaceutical formulation such as tablet obtained from such a dry formulation or granulation of eprosartan mesylate by direct compression or dry granulation. A dry formulation or granulation of eprosartan mesylate, or a pro...


Title: NUCLEASE COMPOSITIONS, METHODS OF MAKING AND USING SUCH COMPOSITIONS, AND SYSTEMS FOR PULMONARY DELIVERY OF SUCH COMPOSITIONS

Publication No: WO2009/120619
Pub. Date - Int. Class - Applicant: - 01.10.2009 - A61K 9/16 - NOVARTIS AG
A powder composition comprises particles including a nuclease, wherein the particles have a mass median aerodynamic diameter ranging from about 1 m to about 5 m. A pharmaceutical composition comprises a powder including an effective amount of nuclease and pharmaceutically acceptable excipient, wherein the powder comprises particles comprising less than 40 wt% of nuclease and having a mass median aerodynamic diameter ranging from about 1 m to about 5 m. Unit dosage forms, spray drying methods, and methods of treatment are also included.


Title: MULTILAYERED PHARMACEUTICAL COMPOSITIONS AND PROCESSES THEREOF

Publication No: WO2009/118763
Pub. Date - Int. Class - Applicant: - 01.10.2009 - A61K 9/52 - PANACEA BIOTEC LIMITED
The present invention relates to multilayered pharmaceutical compositions comprising at least one or more agents each selected from same or different classes having a low dose, comprising at least one polymer(s) or enteric polymer that predominantly controls or delays the release of at least one active agent(s) and optionally one or more pharmaceutically acceptable excipient(s).


Title: DELAYED RELEASE COMPOSITIONS OF DULOXETINE

Publication No: WO2009/118756
Pub. Date - Int. Class - Applicant: - 01.10.2009 - A61K 9/36 - LUPIN LIMITED
A delayed release dosage form comprising core comprising duloxetine or its pharmaceutically acceptable salts or derivatives thereof, optionally, other pharmaceutically acceptable excipient(s) thereof; intermediate layer; and enteric layer; wherein the dosage form comprises one/more dissolution enhancer(s), wherein the enteric layer comprises one/more enteric polymers other than hydroxypropylmethyl acetate succinate. A process of preparing a delayed release dosage comprising mixing pharmaceutically acceptable excipients with duloxetine or its pharmaceutically acceptable derivatives thereof; granulating the product of previous step compressing the granulate formed in previous step to form core, coating said core with intermediate layer follow...


Title: AGGLOMERATES OF SUCRALOSE AND POLYOLS, AND THEIR USE IN CHEWING GUMS

Publication No: WO2009/108842
Pub. Date - Int. Class - Applicant: - 03.09.2009 - A23L 1/0526 - TATE &LYLE TECHNOLOGY LTD
The invention provides co-agglomerates of sucralose and a polyol, wherein the co- agglomerate comprises grains of polyol onto which sucralose has been dried, as well as methods for making such co-agglomerates. In general, the methods comprise contacting a dry powder of polyol with a liquid solution of sucralose in a food acceptable solvent under conditions which moisten, but not dissolve the polyol powder, to form a moist mixture, and drying the moist mixture to form a co-agglomerate comprising grains of agglomerated polyol onto which sucralose has been dried. Also provided are artificial sweetener carriers comprising bentonite which comprise sucralose. The invention features pharmaceutical, cosmetic, and food compositions, especially chewi...


Title: MODIFIED RELEASE FORMULATIONS OF HMG COA REDUCTASE INHIBITORS

Publication No: WO2009/095934
Pub. Date - Int. Class - Applicant: - 06.08.2009 - A61K 9/20 - LUPIN LIMITED
Modified release formulations of HMG Co-A reductase inhibitors, which provide reduced incidence of rhabdomyolysis, renal toxicity and other side effects by increasing hepatic bioavailability and decreasing systemic availability upon oral administration. The modified release pharmaceutical formulation comprises a therapeutically effective amount of HMG CoA reductase inhibitor or a pharmaceutically acceptable salt(s), polymorph(s), solvate(s), hydrate(s), prodrug or metabolite thereof, one ore more release modifying agent(s) and one or more pharmaceutically acceptable excipient(s), wherein the modified release formulation provides reduced incidence of adverse effects and improved efficacy when compared to the immediate release formulation upo...


Title: PHARMACEUTICAL COMPOSITIONS

Publication No: WO2009/095395
Pub. Date - Int. Class - Applicant: - 06.08.2009 - A61K 9/32 - BIOVAIL LABORATORIES INTERNATIONAL SRL
The present invention relates to a pharmaceutical composition comprising a tablet core comprising a combination of actives selected from the group consisting of bupropion hydrochloride and escitalopram oxalate, bupropion hydrobromide and citalopram hydrochloride, bupropion hydrobromide and escitalopram oxalate, and bupropion hydrobromide and quetiapine fumarate, and at least one pharmaceutically acceptable excipient, and a control-releasing coat surrounding the tablet core, wherein said composition surprisingly provides for a synchronous release of the combination of active agents in-vitro. The once-daily pharmaceutical composition surprisingly also provides for enhanced absorption of bupropion hydrobromide when a...


Title: DELAYED RELEASE PHARMACEUTICAL COMPOSITION OF DULOXETINE

Publication No: WO2009/092129
Pub. Date - Int. Class - Applicant: - 30.07.2009 - A61K 31/381 - ALPHAPHARM PTY LTD
A pharmaceutical composition comprising duloxetine or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipient(s) characterised in that the duloxetine has a D90 particle size of 2 to 40 m.


Title: A SLOW-RELEASE FORMULATION BASED ON AN ASSOCIATION OF GLYCOGEN AND ALGINATE

Publication No: WO2009/083561
Pub. Date - Int. Class - Applicant: - 09.07.2009 - A61K 31/00 - AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
The present invention relates to a controlled-release pharmaceutical formulation comprising at least one active ingredient dispersed in a matrix comprising at least one slow-release excipient comprising an association of at least one glycogen and at least one alginate with alkaline-earth metal salts, and a process for its preparation. The invention also relates to a slow-release excipient comprising an association of at least one glycogen and at least one alginate with alkaline-earth metal salts, and the process for its preparation, and its use for the preparation of slow-release pharmaceutical formulations.


Title: STABILIZED PREPARATION CONTAINING COENZYME Q10 AND PROCESS FOR PREPARATION THEREOF

Publication No: WO2009/061105
Pub. Date - Int. Class - Applicant: - 14.05.2009 - A61K 9/30 - CJ CHEILJEDANG CORPORATION
A pharmaceutical agent of stabilized Coenzyme QlO and a method for the preparation thereof are provided. The agent may be a coated tablet composed of a bare tablet containing at least one vitamin and/or mineral ingredient in combination with a carrier and at least one coating layer containing Coenzyme QlO. In the agent, Coenzyme QlO is present in a film coating layer separated from the bare tablet comprising vitamins and/or minerals and thus is prevented from being unstabilized by the vitamins and/or minerals. In addition, the film coating layer of Coenzyme QlO is protected from conditions of the external environment such as water, temperature and light, by a protective layer.


Title: A CONTROLLED-RELEASE PARTIAL GLYCINE AGONIST COMPOSITION FOR USE WITH LEVODOPA IN PARKINSON'S DISEASE AND METHOD OF USE

Publication No: WO2009/059242
Pub. Date - Int. Class - Applicant: - 07.05.2009 - A01N 43/58 - LAZARUS THERAPEUTICS, INC.
A pharmaceutical composition comprises partial glycine agonist in a controlled release formulation for once a day administration to subjects with Parkinson's disease. The composition includes a controlled release material comprising a partial glycine agonist, a sustained release component, and at least one pharmaceutically acceptable excipient, wherein the composition upon initial administration of one dose provides a mean plasma concentration of the partial glycine agonist of at least 10 g/mL and not more than 30 g/mL within one hour of administration and continues to provide a mean plasma concentration of the partial glycine agonist of not more than 30 g/mL for 12 - 16 hours. The partial glycine agonist is administered in a dose eff...


Title: NOVEL COLON TARGETED MODIFIED RELEASE BIOADHESIVE FORMULATION OF 5-AMINO SALICYLIC ACID OR ITS SALTS AND METABOLITES THEREOF

Publication No: WO2009/047802
Pub. Date - Int. Class - Applicant: - 16.04.2009 - A61K 9/20 - LUPIN LIMITED
The present invention relates to a colon targeted modified release bioadhesive pharmaceutical composition of 5-amino salicylic acid or a pharmaceutically acceptable salt or enantiomer or polymorph or metabolites thereof, one or more hydrophilic or hydrophobic release controlling agent (s) and pharmaceutical acceptable excipient (s), and the process of preparing it.


Title: ORAL CONTROLLED RELEASE COMPOSITION OF CARVEDILOL

Publication No: WO2009/047800
Pub. Date - Int. Class - Applicant: - 16.04.2009 - A61K 9/62 - LUPIN LIMITED
An oral controlled release pharmaceutical composition comprising a carvedilol or a pharmaceutically acceptable salt(s) thereof. The oral controlled release pharmaceutical composition comprises a core comprising a therapeutically effective amount of carvedilol or a pharmaceutically acceptable salt(s) thereof and/or other pharmaceutically acceptable excipient thereof; and a functional coating comprising one or more pH dependent polymer(s), water soluble pore forming agent and/or other pharmaceutically acceptable excipient(s) thereof.


Title: HIGH DOSE SOLID UNIT ORAL PHARMACEUTICAL DOSAGE FORM OF MYCOPHENOLATE SODIUM AND PROCESS FOR MAKING SAME

Publication No: WO2009/047799
Pub. Date - Int. Class - Applicant: - 16.04.2009 - A61K 31/343 - PANACEA BIOTEC LIMITED
Provided are high dose solid unit oral pharmaceutical dosage form compositions comprising mycophenolate sodium as active agent in an amount of from greater than about 720 mg to about 1500 mg, preferably from about 800 mg to about 1440 mg calculated as mycophenolic acid, and one or more pharmaceutically acceptable excipient(s). Particularly the dosage form compositions are meant for once-a-day or twice-a-day administration and provide the active agent in an extended release form which is released in a sustained manner in-vivo for a prolonged duration. The invention is also directed to process of manufacturing the high dose formulations, and prophylactic and/or therapeutic methods of using such dosage forms. The composition of the present inv...


Title: PHARMACEUTICAL COMPOSITION

Publication No: WO2009/043395
Pub. Date - Int. Class - Applicant: - 09.04.2009 - A61K 9/00 - STI PHARMACEUTICALS LTD.
According to the invention a pharmaceutical composition suitable for pulmonary administration comprising at least one cannabinoid, at lease one local anaesthetic and a pharmaceutical acceptable carrier, diluent or excipient is provided. Furthermore, the addition of a local anaesthetic to a composition suitable for pulmonary administration allows and improves the delivery and bioavailability of an accurate dose and also of repeated doses of cannabinoids. The term 'cannabinoid', for the purpose of this invention, includes all major and minor cannnabinoids found in natural cannabis and hemp material that can be isolated and reproduced by synthetic means. This includes delta-9-Tetrahydrocannabinol (THC), delta-8-Tetrahydrocannabinol, Cannabidio...


Title: USE OF MELANOCYTE-STIMULATING HORMONE RELEASE-INHIBITING FACTOR AS A THERAPEUTIC AGENT IN THE TREATMENT OF PSEUDOMONAS AERUGINOSA INFECTION

Publication No: WO2009/039993
Pub. Date - Int. Class - Applicant: - 02.04.2009 - A61K 38/06 - mondoBIOTECH Laboratories AG
The present invention is directed to the use of the peptide compound Pro-Leu-Gly-NH2 as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Pro-Leu-Gly-NH2 optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/o...


Title: USE OF BAND 3 PROTEIN (824-829) AND/OR MELANOCYTE-STIMULATING HORMONE RELEASE-INHIBITING FACTOR AS A THERAPEUTIC AGENT IN THE TREATMENT OF PSEUDOMONAS AERUGINOSA INFECTION

Publication No: WO2009/039992
Pub. Date - Int. Class - Applicant: - 02.04.2009 - A61P 25/28 - MONDOBIOTECH LABORATORIES AG
The present invention is directed to the use of the peptide compound Tyr-Val-Lys-Arg-Val-Lys-OH as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquide buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Tyr-Val-Lys-Arg-Val-Lys-OH optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.


Title: MATRIX DOSAGE FORMS OF VARENICLINE

Publication No: WO2009/027786
Pub. Date - Int. Class - Applicant: - 05.03.2009 - A61K 31/498 - PFIZER INC.
The present invention provides matrix dosage form comprising varenicline or a pharmaceutically acceptable salt thereof, at least one high molecular weight water soluble polymer; and at least one water-insoluble, hydrophilic excipient.


Title: LIQUID FORMULATION OF G-CSF CONJUGATE

Publication No: WO2009/027437
Pub. Date - Int. Class - Applicant: - 05.03.2009 - C07K 17/08 - BIOGENERIX AG
The present invention relates to a liquid pharmaceutical composition comprising a granulocyte colony stimulating factor polypeptide conjugated with a polymer, the composition having a pH value in the range of 4.5 to 5.5. The composition further comprises a surfactant and optionally one or more other pharmaceutically acceptable excipients. Further, the composition of the invention is free from tartaric acid or salts thereof and from succinic acid and salts thereof as buffering agents and does not contain amino acids as stabilizer. The composition has a good storage stability and is especially useful for the prophylaxis and treatment of disorders and medical indications where granulocyte colony stimulating factor preparations are considered a...


Title: CONTROLLED RELEASED COMPOSITIONS

Publication No: WO2009/021127
Pub. Date - Int. Class - Applicant: - 12.02.2009 - A61K 9/22 - NEUROGEN CORPORATION
Provided are controlled-release compositions that include a therapeutically effective amount of adipiplon and a pharmaceutically acceptable carrier. The controlled-release compositions can be a formulation with multiple components, e.g., layers or particles which release adipiplon at different rates. Also provided are methods for inducing sleep and for treating CNS disorders, which methods include administering an effective amount of a controlled-release adipiplon composition to a patient.


Title: NUCLEIC ACID-LIPOPOLYMER COMPOSITIONS

Publication No: WO2009/021017
Pub. Date - Int. Class - Applicant: - 12.02.2009 - A61K 9/19 - EGEN, INC.
Compositions, methods, and applications that increase the efficiency of nucleic acid transfection are provided. In one aspect, a pharmaceutical composition may include at least about 0.5 mg/ml concentration of a nucleic acid condensed with a cationic lipopolymer suspended in an isotonic solution, where the cationic lipopolymer includes a cationic polymer backbone having cholesterol and polyethylene glycol covalently attached thereto, and wherein the molar ratio of cholesterol to cationic polymer backbone is within a range of from about 0.1 to about 10, and the molar ratio of polyethylene glycol to cationic polymer backbone is within a range of from about 0.1 to about 10. The composition further may include a filler excipient.


Title: CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION OF TOLPERISON HYDROCHLORIDE

Publication No: WO2009/013552
Pub. Date - Int. Class - Applicant: - 29.01.2009 - A61K 9/20 - RICHTER GEDEON NYRT.
The present invention relates to tolperison hydrochloride containing pharmaceutical compositions with controllable release of active agent and to a process for the preparation thereof. The controlled release pharmaceutical composition according to the invention comprises multiple granule cores formed with a natural anionic polymer and a lipophil excipient, a hydrophilic matrix-forming excipient which surrounds the cores, and other pharmaceutically acceptable excipients.


Title: PHARMACEUTICAL COMPOSITIONS FOR GASTROINTESTINAL DRUG DELIVERY

Publication No: WO2009/008006
Pub. Date - Int. Class - Applicant: - 15.01.2009 - A61K 9/16 - LUPIN LIMITED
A novel pharmaceutical composition, which comprises a therapeutically effective amount of active principle(s) or a pharmaceutically acceptable salt or enantiomer or polymorph thereof, optionally one or more release controlling agent(s) and pharmaceutical acceptable excipient(s) thereof, wherein the composition is formulated to increase the residence time of the said pharmaceutical composition and/or active principle(s) in the gastrointestinal tract. A novel pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/fast release and the other is controlled release. A pharmaceutical composition comprising at least two entities wherein one entity is an immediate release/ fast release and the other is...


Title: PHARMACEUTICAL COMPOSITIONS OF RIFAXIMIN

Publication No: WO2009/008005
Pub. Date - Int. Class - Applicant: - 15.01.2009 - A61K 9/20 - LUPIN LIMITED
A pharmaceutical composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s) and release controlling agent(s). Pharmaceutical composition of rifaximin comprising: at least two entities wherein one entity is an immediate release or fast release and the other is controlled release. The pharmaceutical composition in the form of multilayer tablet comprising, at least one layer comprising, therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s); said layer providing controlled release rifaximin; and at least one layer which ....

 

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WORLD PATENTS IN EXCIPIENTS, DELIVERY AND RELEASE OF PHARMACEUTICAL ACTIVES PUBLISHED IN 2009
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.