Organic Coatings Patents (Class 424/475)
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Patent number: 6599532Abstract: The present invention provides an osmotic device containing controlled release alprazolam in the core optionally in combination with an anti-psychotic agent, in a rapid release external coat. A wide range of anti-psychotic agents can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One preferred embodiment of the osmotic device includes an external coat that has been spray coated rather compression coated onto the device. The device with spray coated external core is smaller and easier to swallow than the similar device having a compression coated external coat. The device is useful for the treatment of depression, anxiety or psychosis related disorders.Type: GrantFiled: January 8, 2001Date of Patent: July 29, 2003Assignee: Osmotica Corp.Inventors: Joaquina Faour, Juan A. Vergez
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Patent number: 6576260Abstract: Disclosed herein is sustained-release formulations of tramadol comprising tramadol saccharinate coated with at least one sustained-release coating. The sustained release formulations may also contain tramadol in non-sustained release form, and other pharmaceutically acceptable excipients. Also disclosed are methods of preparation of and methods of treatment using the inventive formulations.Type: GrantFiled: February 28, 2002Date of Patent: June 10, 2003Assignee: Gruenenthal GmbHInventors: Johannes Bartholomaeus, Heinrich Kugelmann, Iris Ziegler
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Patent number: 6572888Abstract: A controlled release formulation of lipoic acid is disclosed. The lipoic acid is combined with excipient materials in such a way that those materials provide for gradual release of the lipoic acid in a manner which makes it possible to substantially increase the period of time over which therapeutic levels of lipoic acid are maintained relative to a quick release formulation. These features make it possible to use lipoic acid to reduce serum glucose levels and maintain those levels over time thereby obtaining a range of desired therapeutic results.Type: GrantFiled: January 5, 2001Date of Patent: June 3, 2003Assignee: Medical Research InstituteInventor: Edward A. Byrd
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Patent number: 6569457Abstract: A high drug load enteric coated pharmaceutical composition is provided which includes a core in the form of a tablet and which is comprised of a medicament which is sensitive to a low pH environment of less than 3, such as ddl, and having an enteric coating formed of methacrylic acid copolymer and a plasticizer. The tablets may be of varying sizes and may be orally ingested individually or a plurality of tablets sufficient to attain a desired dosage may be encapsulated in a dissolvable capsule. The tablets have excellent resistance to disintegration at pH less than 3 but have excellent drug release properties at pH greater than 4.5. A novel method of making said pharmaceutical composition is also disclosed.Type: GrantFiled: May 25, 2001Date of Patent: May 27, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Ismat Ullah, Gary J. Wiley
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Patent number: 6569456Abstract: The present invention provides an osmotic device containing controlled release diltiazem in the core in combination with a rapid release ACE inhibitor, or diuretic, in an external coat. The delivery device of the invention can also be a chronotherapeutic osmotic device that provides a delayed and controlled release of diltiazem and a delay and rapid release of an ACE inhibitor or diuretic. A wide range of ACE inhibitors or diuretics can be used in this device. Particular embodiments of the invention provide osmotic devices having predetermined release profiles. One specific embodiment of the osmotic device includes an external coat that has been spray coated rather than compression coated onto the device. The device with spray coated external core is smaller and easier to swallow than the similar device having a compression coated external coat. The device is useful for the treatment of blood pressure or hypertension related disorders.Type: GrantFiled: January 5, 2001Date of Patent: May 27, 2003Assignee: Osmotica Corp.Inventors: Joaquina Faour, Juan A. Vergez
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Patent number: 6555136Abstract: Novel pharmaceutical dosage forms provide for pulsatile delivery of methylphenidate, i.e., release encapsulated drug in spaced apart “pulses.” The dosage forms are comprised of first, second and optionally third dosage units, with each dosage unit having a different drug release profile. The dosage forms may comprise capsules housing compressed tablets or drug-containing beads or particles, or may comprise a single tablet with the first, second and optionally third dosage units each representing an integral and discrete segment thereof. Methods of treatment using the pharmaceutical dosage forms are provided as well.Type: GrantFiled: November 13, 2001Date of Patent: April 29, 2003Assignee: PharmaQuest, Ltd.Inventor: Kamal K. Midha
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Patent number: 6537582Abstract: 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 prostaqlandin and one or more excipients.Type: GrantFiled: November 14, 2001Date of Patent: March 25, 2003Assignee: Norton Healthcare Ltd.Inventors: Austen John Woolfe, Siobhan Greene, Gordon McIntyre, Nitin Vadilal Sheth
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Patent number: 6531155Abstract: Granular materials are obtainable by pressing mixtures of at least one pulverulent, rheology-modifying, carboxyl-containing polymer as main component and at least one oil-soluble component.Type: GrantFiled: July 6, 1998Date of Patent: March 11, 2003Assignee: BASF AktiengesellschaftInventors: Christian Schade, Robert Heinz, Thekla Börs, Hans-Ulrich Wekel
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Patent number: 6521256Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyanot carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonyl-methyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.Type: GrantFiled: February 19, 2002Date of Patent: February 18, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tadashi Makino, Tetsuro Tabata, Shin-Ichiro Hirai
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Patent number: 6517868Abstract: Disclosed herein is a tableted oral extended release dosage form comprising a plurality of granules of an effective amount of a pharmaceutically active compound, at least one amino acid, and an intragranular polymer in which the granule is dispersed within a hydrophilic extragranular polymer matrix which is more rapidly hydrating than the intragranular polymer. The amino acid is selected for hydropathy characteristics depending on solubility characteristics of the active compound.Type: GrantFiled: November 30, 2001Date of Patent: February 11, 2003Inventors: A. Reza Fassihi, Thomas Dürig
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Patent number: 6509038Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.Type: GrantFiled: November 19, 1998Date of Patent: January 21, 2003Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Elvire Colette Baert, Geert Verreck, Dany Thoné
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Patent number: 6503535Abstract: The invention provides a process for coating a branded pharmaceutical dosage form for the purpose of covering any embossed or printed matter or any colored coating by the application of an amount of a sugar based coating which is sufficient to obscure any identifying indicia without compromising the stability or releasability of the drug that is contained in the dosage form.Type: GrantFiled: January 4, 2001Date of Patent: January 7, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: Michael L. Cappola
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Patent number: 6500459Abstract: A pharmaceutical composition for controlled onset and sustained release of an active ingredient, said composition comprising: (i) a core comprising: (a) an active ingredient; (b) a hydrophilic carrier; (c) a hydrodynamic diffusion enhancer; and optionally (d) conventional pharmaceutically acceptable excipients selected from the group consisting of binders, fillers and lubricants and combinations thereof; and (ii) a functional coating membrane surrounding said core.Type: GrantFiled: July 21, 1999Date of Patent: December 31, 2002Inventors: Harinderpal Chhabra, Shyamal K. Sarkar
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Publication number: 20020192283Abstract: A coating for masking or reducing the detectable presence of certain characteristic odor or odors, taste or tastes of pharmaceutical preparations, particularly Valerian extracts, is described. The coating comprises from one to three coating compartments, in any combination or as a single-layer amalgam. The first coating compartment comprises a hydroxyalkyl cellulose and an anti-tackiness agent. The second coating compartment may comprise a sugar and at least one anti-tackiness agent. The third coating compartment may comprise a methacrylate copolymer, a hydroxyalkyl cellulose and an anti-tackiness agent.Type: ApplicationFiled: May 14, 2002Publication date: December 19, 2002Inventors: I-Lan T. Sue, Pou-Hsiung Wang
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Patent number: 6475493Abstract: The present invention describes an aqueous pharmaceutical coating formulation which can be used for coating core elements containing one or more medicaments to achieve controlled release. The coated pharmaceutical formulation provides a release of medicaments in a controlled manner at highly acidic environment such as that of stomach and shows relatively faster release in media with basic pH such as that of the intestine. The coating composition is a heterogenous mixture which comprises (a) at least 75% by weight of a water insoluble polymer which is insoluble in both acidic as well as basic pH; and (b) 1 to 25% by weight of an enteric polymer which is substantially insoluble in water at a pH below 4.5 and which is substantially soluble in water at a pH between above about 6.0, said enteric polymer and water insoluble polymer being present in an amount effective to control the release of said medicament.Type: GrantFiled: August 30, 2000Date of Patent: November 5, 2002Assignee: Norstrum Pharmaceuticals, Inc.Inventor: Nirmal Mulye
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Publication number: 20020160048Abstract: A film-coated tablet containing talsaclidine comprising:Type: ApplicationFiled: January 22, 2002Publication date: October 31, 2002Inventors: Karoline Bechtold-Peters, Thomas Friedl, Michael Walz
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Patent number: 6461639Abstract: This invention relates to a controlled-release combination drug product comprising troglitazone, e.g. its hydrochloride, and a biguamide, e.g. metformin. In particular, the product comprises a core of metformin, at least a portion thereof has a layer or coat thereon of troglitazone.Type: GrantFiled: February 15, 2001Date of Patent: October 8, 2002Assignee: Aeropharm Technology, Inc.Inventors: Akwete L. Adjei, Yaping Zhu, Anthony J. Cutie
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Patent number: 6451342Abstract: This invention relates to a controlled release combination drug product comprising troglitazone, e.g. its hydrochloride, and a biguamide, e.g. metformin. In particular, the product comprises a core of metformin, at least a portion thereof has a layer or coat thereon of troglitazone.Type: GrantFiled: February 15, 2001Date of Patent: September 17, 2002Assignee: Aeropharm Technology IncorporatedInventors: Akwete L. Adjei, Yaping Zhu, Anthony J. Cutie
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Patent number: 6451343Abstract: Controlled release dosage forms useful in the treatment and/or prophylaxis of dementia, including Alzheimer's disease, in mammals, and for enhancing amyloid precursor protein processing along a non-amyloidogenic pathway in patients suffering from, or at risk of developing, Alzeimer's disease.Type: GrantFiled: August 30, 2000Date of Patent: September 17, 2002Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Robert Glinecke, William Muldoon, Susan Marie Milosovich, Joseph Sauer, Laurence Rousseau
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Patent number: 6447797Abstract: It has been discovered that certain phosphoinositides demonstrate antibacterial activity. Particularly, these phosphoinositides have been discovered to prevent the adhesion of H. influenzae onto the nasopharyngeal cells of mammals, and, in particular, humans. Phosphoinositides useful with the present invention have the following formula: wherein R1 and R2 are selected from the group consisting of hydrogen and monounsaturated and saturated fatty acids having a carbon chain length of C6 to C20 and R1 and R2 can be the same or different; and R3 to R7 are selected from the group consisting of hydrogen or a phosphate moiety with at least two of R3 to R7 being a phosphate moiety; and hydrates and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 19, 2001Date of Patent: September 10, 2002Assignee: Abbott LaboratoriesInventors: Shie-Ming Hwang, Yung-Sheng Huang, Jim-Wen Liu, Pradip Mukerji, Steven Neal Anderson, Jonathan A. Meulbroek
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Patent number: 6444218Abstract: The present invention provides an improved soft chewable multivitamin tablet in which vitamin C is separated from calcium pantothenate and/or minerals such as iron, copper, zinc and mixtures thereof in a core or multilaminate form and a process for preparing the same. The soft chewable multivitamin tablet of the present invention maintains its stability over a long-storage time in terms of the content and potency of vitamins while overcoming the problems of incompatibility, bad mouthfeel and palatability.Type: GrantFiled: June 8, 2001Date of Patent: September 3, 2002Assignee: Sam-A-Pharmaceuticals Co. Ltd.Inventors: Yoon Dong Han, Jong Bum Park
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Patent number: 6440450Abstract: The present invention provides an improved soft chewable multivitamin tablet in which vitamin C is separated from calcium pantothenate and/or minerals such as iron, copper, zinc and mixtures thereof in a core or multilaminate form and a process for preparing the same. The soft chewable multivitamin tablet of the present invention maintains its stability over a long-storage time in terms of the content and potency of vitamins while overcoming the problems of incompatibility, bad mouthfeel and palatability.Type: GrantFiled: May 19, 1999Date of Patent: August 27, 2002Assignee: Sam-Pharmaceutical Co., Ltd.Inventors: Yoon Dong Han, Jong Bum Park
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Publication number: 20020115718Abstract: A process for preparing divalproex sodium tablets is provided. The process comprises preparing a neutralized divalproex sodium solution by combining divalproex sodium, having a sodium valproate and a valproic acid moiety, with an aqueous solvent and a base, e.g., sodium hydroxide, the base being in sufficient amount to ensure neutralization of the valproic acid moiety of the divalproex sodium. The neutralized divalproex sodium solution is sprayed onto a pharmaceutically acceptable carrier, and processed to obtain divalproex sodium tablets.Type: ApplicationFiled: February 16, 2001Publication date: August 22, 2002Applicant: Andrx CorporationInventors: Chih-Ming Chen, Boyong Li
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Patent number: 6432448Abstract: An edible, hardenable coating composition containing microcrystalline cellulose and carrageenan and either a strengthening polymer, a plasticizer or both. The coating composition of the present invention may be applied to pharmaceutical and veterinary solid dosage forms, confectionery, seeds, animal feed, fertilizers, pesticide tablets, and foods and provides an elegant prompt release coating which does not retard the release of active ingredients from the coated substrate.Type: GrantFiled: January 27, 2000Date of Patent: August 13, 2002Assignee: FMC CorporationInventors: Michael Augello, Sheila M. Dell, Domingo C. Tuason, James J. Modliszewski, Thomas A. Ruszkay, David E. Werner
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Publication number: 20020090395Abstract: 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.Type: ApplicationFiled: October 7, 1999Publication date: July 11, 2002Inventors: AUSTEN JOHN WOOLFE, SIOBHAN GREENE, GORDON MCINTYRE
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Publication number: 20020086057Abstract: This invention relates to new stable oral pharmaceutical formulations prepared by covering an nucleus formed by a core with a first hydrophobic polymer layer, a second layer coating the first layer, wherein said second layer comprises one or more labile pharmaceutical compounds in one or more acceptable hydrophobic excipients, and an optional third enteric polymer layer.Type: ApplicationFiled: November 9, 2001Publication date: July 4, 2002Inventors: Debra Alida Odink, I-Lan Sue, Gary Conard Visor
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Patent number: 6399100Abstract: Controlled release oral pharmaceutical preparations are provided which comprise a therapeutically effective amount of tiagabine or a pharmaceutically acceptable salt thereof dispersed in a rate controlling polymeric matrix comprising at least one rate controlling polymer. The preparation can be formulated into oral dosage forms such as tablets or multiparticulates which provide therapeutically effective plasma levels of tiagabine for a period of at least 12 hours, preferably 24 hours or more. The preparation can provide tiagabine mean plasma concentrations equal to or greater than 50% of the maximum plasma concentration for at least 10 hours, preferably 14 hours, most preferably 16 hours or more.Type: GrantFiled: July 31, 1998Date of Patent: June 4, 2002Assignee: Elan Corporation, plcInventors: Maurice Joseph Anthony Clancy, Kenneth Iain Cumming, Michelle Caulfield
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Patent number: 6387410Abstract: 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.Type: GrantFiled: January 7, 2000Date of Patent: May 14, 2002Assignee: Norton Healthcare LtdInventors: Austen John Woolfe, Siobhan Greene, Gordon McIntyre, Nitin Vadilal Sheth
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Patent number: 6380234Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.Type: GrantFiled: August 8, 2001Date of Patent: April 30, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tadashi Makino, Tetsuro Tabata, Shin-Ichiro Hirai
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Patent number: 6372252Abstract: The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about six-to-one (6:1), more preferably a range of about three-to-two (3:2) to about four-to-one (4:1), and most preferably about two-to-one (2:1), by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release guaifenesin tablet which has two portion: the first portion comprises an immediate release formulation of guaifenesin and the second portion comprises a sustained release formulation of guaifenesin as described above.Type: GrantFiled: April 28, 2000Date of Patent: April 16, 2002Assignee: Adams Laboratories, Inc.Inventors: Ralph W. Blume, Robert D. Davis, Donald Jeffrey Keyser
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Patent number: 6368627Abstract: A pharmaceutical composition for oral adminstration comprising a film-coated solid dosage form including 3-[2-(dimethylamino)ethyl]-N-methyl-1H-indole-5-methanesulphonamide or a pharmaceutically acceptable salt or solvate thereof as active ingredient. The film-coated solid dosage forms are of use in the treatment of conditions associated with cephalic pain, in particular migraine.Type: GrantFiled: January 13, 2000Date of Patent: April 9, 2002Assignee: Glaxo Group LimitedInventors: Anthony John Phillips, Ian Keith Winterborn, John Malcolm Padfield
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Publication number: 20020034546Abstract: A pharmaceutical composition is provided which is useful for cholesterol lowering and reducing the risk of a myocardial infarction, which includes a statin, such as pravastatin, lovastatin, simvastatin, atorvastatin, cerivastatin or fluvastatin, in combination with aspirin, in a manner to minimize interaction of aspirin with the statin and minimize side effects of aspirin. A method for lowering cholesterol and reducing risk of a myocardial infarction employing such composition is also provided.Type: ApplicationFiled: April 2, 2001Publication date: March 21, 2002Inventors: Ismat Ullah, Nemichand B. Jain
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Patent number: 6331316Abstract: A high drug load enteric coated pharmaceutical composition is provided which includes a core in the form of a tablet and which is comprised of a medicament which is sensitive to a low pH environment of less than 3, such as ddl, and having an enteric coating formed of methacrylic acid copolymer and a plasticizer. The tablets may be of varying sizes and may be orally ingested individually or a plurality of tablets sufficient to attain a desired dosage may be encapsulated in a dissolvable capsule. The tablets have excellent resistance to disintegration at pH less than 3 but have excellent drug release properties at pH greater than 4.5. A novel method of making said pharmaceutical composition is also disclosed.Type: GrantFiled: April 14, 2000Date of Patent: December 18, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Ismat Ullah, Gary J. Wiley
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Patent number: 6326028Abstract: This invention relates to coatings employed to coat medicinal tablets. Such tablets include but are not limited to small pellet(s) of medication to be taken orally. In particular this invention relates to the use of alginates and/or gellan gum, mixtures thereof and the like as tablet coatings. More in particular, this invention relates to the use of alginate and gellan gum as tablet coatings for tablets which are useful for humans including coating(s) on medicinal tablets and to a process for making such coatings.Type: GrantFiled: October 30, 1998Date of Patent: December 4, 2001Assignee: Monsanto CompanyInventors: Thierry Nivaggioli, George Colegrove, John Flanagan
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Publication number: 20010044474Abstract: A controlled release dosage form for sertraline has a core comprising a sertraline-containing composition and a water-swellable composition wherein the water-swellable composition is in a separate region within the core. A coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. In one embodiment, the dosage form releases sertraline to the use environment at an average rate of 6 to 10 wt % per hour from the second to the twenth hour after introduction to a use environment and less than about 25 wt % for the first two hours and at least 70 wt % by the twelfth hour, where the percentages correspond to the mass of drug released from the tablet divided by the total mass of drug originally present in the tablet.Type: ApplicationFiled: December 20, 2000Publication date: November 22, 2001Inventors: William J. Curatolo, Kenneth C. Waterman, Avinash G. Thombre, Michael B. Fergione, Michael C. Roy, Leah E. Appel, Danni Supplee, Dwayne T. Friesen, Mark B. Chidlaw, Ronald A. Beyerinck
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Patent number: 6319512Abstract: The present intention relates to an implant for the controlled release of at least one pharmaceutically active principle comprising a core containing at least one active principle and a sheath surrounding said core, wherein said sheath is composed of at least one polymeric film applied around said core. It also relates to a process for the preparation of such an implant, characterised by the production of a core containing at least one active principle, preparation of at least one polymeric film, application of the polymeric film(s) around said core by juxtaposition and/or superposition thereof, and sterilisation of the implant thus obtained.Type: GrantFiled: February 23, 2000Date of Patent: November 20, 2001Assignee: Debio Recherche Pharmaceutique SAInventors: Alexandra Rothen-Weinhold, Robert Gurny, Piero Orsolini, Frédéric Heimgartner
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Patent number: 6306900Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.Type: GrantFiled: October 23, 2000Date of Patent: October 23, 2001Assignee: Novartis AGInventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
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Patent number: 6296874Abstract: This invention relates to a combination drug product comprising troglitazone, e.g. its hydrochloride, and a biguamide, e.g. metformin. In particular, the product comprises a core of metformin, at least a portion thereof has a layer or coat thereon of troglitazone.Type: GrantFiled: October 31, 2000Date of Patent: October 2, 2001Assignee: Aeropharm Technology IncorporatedInventors: Anthony J. Cutie, Akwete L. Adjei
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Patent number: 6296875Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.Type: GrantFiled: June 7, 2000Date of Patent: October 2, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Tadashi Makino, Tetsuro Tabata, Shin-Ichiro Hirai
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Patent number: 6294200Abstract: Pharmaceutical tablet, capable of delivering the active substance or the active substances, according to a predeterminable release profile, comprising a core with an external partial coating in which said core consists of 3 layers, wherein the upper layer contains an amount of the active substance with suitable excipients, the intermediate layer consists of polymeric material with retarding barrier function and the lower layer contains the remaining amount of the active substance with suitable excipients and said external coating consists of controlled permeability polymeric materials, applied by compression to the lower surface and to the lateral surface of the core.Type: GrantFiled: February 4, 1997Date of Patent: September 25, 2001Assignee: Jagotec AGInventors: Ubaldo Conte, Lauretta Maggi
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Patent number: 6284275Abstract: A controlled release pharmaceutical tablet containing antihyperglycemic drug and a hypoglycemic drug that does not contain an expanding or gelling polymer layer and comprising a core containing the antihyperglycemic drug and the hypoglycemic drug, a semipermeable coating membrane surrounding the core and at least one passageway in the membrane to allow the drugs to be released from the core.Type: GrantFiled: June 9, 2000Date of Patent: September 4, 2001Assignee: Andrx Pharmaceuticals, Inc.Inventors: Chih-Ming Chen, Xiu Xiu Cheng, Joseph Chou, Steve Jan
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Patent number: 6274173Abstract: An oral pharmaceutical composition comprises an acid-labile irreversible proton pump inhibitor in pellet or tablet form, wherein the irreversible proton pump inhibitor is at least partly in slow-release form. On combined administration with an anti-microbially-active ingredient, the composition is distinguished by imparting an enhanced action of rapid onset against disorders caused by Helicobacter.Type: GrantFiled: December 15, 1999Date of Patent: August 14, 2001Assignee: BYK Gulden Lomberg Chemische Fabrik GmbHInventors: George Sachs, Rango Dietrich
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Patent number: 6262115Abstract: A composition and a dosage form are disclosed comprising oxybutynin alone/or accompanied by another drug indicated for therapy. A method is disclosed for administering oxybutynin alone/or accompanied by a different drug or for administering oxybutynin and a different drug according to a therapeutic program for the management of incontinence alone, and for other therapy.Type: GrantFiled: March 29, 1999Date of Patent: July 17, 2001Assignee: ALZA CoporationInventors: George V. Guittard, Francisco Jao, Susan M. Marks, David J. Kidney, Fernando E. Gumucio
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Publication number: 20010007678Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.Type: ApplicationFiled: November 19, 1998Publication date: July 12, 2001Inventors: LIEVEN ELVIRE COLETTE BAERT, GEERT VERRECK, DANY THONE
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Patent number: 6251432Abstract: Dosage form unit is provided to deliver one or more beneficial agents into a fluid, such as liquid enteral nutritional product. The dosage form unit includes a core containing at least one beneficial agent, preferably a marker dye, which is dispersible in the fluid. The core also contains a compatible binding agent to bind the beneficial agent together. Additional components of the core may include a plasticizer, a standard flow agent, a lubricant, additional tableting aids and at least one hydrophilic agent. A latex coating encases the core. The latex coating includes a mixture containing a substantially hydrophobic base material, preferably formed from an emulsion of cellulose acetate microspheres, which is capable of defining a matrix-type membrane, and at least one hydrophilic component being dispersible in the fluid. A dispersible beneficial agent is preferred as one of the hydrophilic components of the latex coating to allow immediate release of the beneficial agent therefrom.Type: GrantFiled: July 1, 1999Date of Patent: June 26, 2001Assignee: Abbott LaboratoriesInventors: Terrence B. Mazer, Joseph E. Walton, Barbara S. Arnholt, Monty L. Evans, Ronita K. Geckle, Daniel Hamilton, John J. Kropczynski, Jr., Frank A. Murawski, Larry G. Tucker, Sherri A. Walker, Michael V. Walsh, Rhonda Cole Walsh
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Patent number: 6248758Abstract: A pharmaceutical formulation comprising a benzimidazole derivative as active ingredient, and as excipients, at least one cyclodextrin and at least one amino acid.Type: GrantFiled: September 8, 1999Date of Patent: June 19, 2001Assignee: Hexal AGInventors: Karin Klokkers, Marion Kutschera, Wilfried Fischer
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Patent number: 6248359Abstract: The present invention provides a simple multi-tablet system for the treatment of urinary incontinence with oxybutynin. Particular embodiments of the invention provide a first tablet that releases oxybutynin over a short period of time, e.g. less than six hours, and a second tablet that releases oxybutynin over an extended period of time, e.g., eighteen to twenty-four hours, to maintain therapeutically effective levels oxybutynin in the mammal for a period of about twenty four hours. Unlike other systems, this system is easily adaptable to compensate for patient to patient variability in response to oxybutynin therapy. The invention also provides a method of treating urinary incontinence with the above system and a kit comprising various first and second tablets to rapidly develop a patient's preferred dosing regimen, i.e., the dosing regimen which provides the greatest therapeutic benefit and/or least amount or severity of side effects.Type: GrantFiled: January 5, 2000Date of Patent: June 19, 2001Assignee: Laboratorios Phoenix U.S.A., Inc.Inventor: Joaquina Faour
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Patent number: 6224911Abstract: This invention is directed to a process for the preparation of enteric coated pharmaceutical dosage forms. This invention is further directed to the aqueous enteric coating dispersions suitable for use in the process and the enteric coated pharmaceutical dosage forms prepared by the process.Type: GrantFiled: January 18, 1995Date of Patent: May 1, 2001Assignee: Syntex (U.S.A.) LLCInventors: Zakauddin T. Chowhan, Patrick H. Vo
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Patent number: 6221395Abstract: It is described a new method for the preparation of pharmaceutical tablets carrying poorly soluble in water principle; this method allows to obtain tablets with fast and/or slow release of the active principle. The peculiar feature is the fact that the poorly soluble in water active principle (es: nifedipine) is treated with a surfactant, during the granulation phase or whatever during the preparation process; the obtained product, subjected to a compression, produces pharmaceutical tablets which show high bioavailability of the carried active principle. This procedure can be used to prepare polymeric matrixes (with modified release), formed by tablets with one or more layers. The procedure of manufacture and the characteristics of the new finished tablet are described.Type: GrantFiled: September 1, 1998Date of Patent: April 24, 2001Assignee: Jagotec AGInventors: Lauretta Maggi, Ubaldo Conte, Pascal Grenier, Guy Vergnault, Robert Zimmer
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Patent number: 6210714Abstract: A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.Type: GrantFiled: February 14, 2000Date of Patent: April 3, 2001Assignee: Euro-Celtique S.A.Inventors: Benjamin Oshlack, Mark Chasin