Containing Polysaccharide (e.g., Cellulose Sugars, Etc.) Patents (Class 424/461)
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Publication number: 20010055611Abstract: Process is provided for preparing an oral solid rapidly disintegrating freeze-dried dosage form of a pharmaceutically active substance having an unacceptable taste, wherein prior to freeze drying, a suspension of uncoated or coated coarse particles of a pharmaceutically active substance in a carrier material is cooled to reduce the viscosity and minimize release of the active substance during processing, as well as beyond the point of disintegration of the form in the mouth, to minimize bad taste from the drug.Type: ApplicationFiled: June 17, 1999Publication date: December 27, 2001Inventors: RICHARD GREEN, PATRICK KEARNEY
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Publication number: 20010055613Abstract: A multiple pulsed dose drug delivery system for pharmaceutically active amphetamine salts, comprising an immediate-release component and an enteric delayed-release component wherein (1) the enteric release coating has a defined minimum thickness and/or (2) there is a protective layer between the pharmaceutically active amphetamine salt and the enteric release coating and/or (3) there is a protective layer over the enteric release coating. The product can be composed of either one or a number of beads in a dosage form, including either capsule, tablet, or sachet method for administering the beads.Type: ApplicationFiled: October 21, 1998Publication date: December 27, 2001Inventors: BETH A. BURNSIDE, XIAODI GUO, KIMBERLY FISKE, RICHARD A. COUCH, RONG-KUN CHANG, DONALD J. TREACY, CHARLOTTE M. MCGUINNESS, EDWARD M. RUDNIC
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Publication number: 20010055612Abstract: This invention relates to a 24 hour extended release dosage formulation and unit dosage form thereof of venlafaxine hydrochloride, an antidepressant, which provides better control of blood plasma levels than conventional tablet formulations which must be administered two or more times a day and further provides a lower incidence of nausea and vomiting than the conventional tablets. More particularly, the invention comprises an extended release formulation of venlafaxine hydrochloride comprising a therapeutically effective amount of venlafaxine hydrochloride in spheroids comprised of venlafaxine hydrochloride, microcrystalline cellulose and, optionally, hydroxypropylmethylcellulose coated with a mixture of ethyl cellulose and hydroxypropylmethylcellulose.Type: ApplicationFiled: June 19, 2001Publication date: December 27, 2001Applicant: American Home Products Corporation Five Giralda FarmsInventors: Deborah M. Sherman, John C. Clark, John U. Lamer, Steven A. White
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Publication number: 20010051184Abstract: The compound curcumin, derived from turmeric, inhibits phosphorylase kinase and, by doing so, exhibits a number of physiological effects related to the control of inflammation and cellular proliferation. However, curcumin is effective only when in solution. Curcumin is almost completely insoluble in water or in oils, but is soluble in alcohols. Accordingly, a method for treating inflammation in a mammal comprising administering curcumin in a solution containing at least one alcohol to a mammal to detectably inhibit the activity of phosphorylase kinase in the blood of the mammal or in a tissue of the mammal. The alcohol is preferably ethanol, 1-propanol, or 2-propanol; most preferably, it is ethanol. Instead of curcumin, a curcumin derivative or curcuminoid can be administered.Type: ApplicationFiled: May 20, 1999Publication date: December 13, 2001Inventor: MADALENE C.Y. HENG
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Patent number: 6328967Abstract: A microsphere containing an immunogen bound to an inert particle having a mesh size of greater than about 35 mesh for site-specific release and induction of an immune response. The immune response may be an overall enhanced T lymphocyte immune response or a selective response. The physical and chemical characterigticg and/or modes of administration of the microsphere may be engineered to increase TH1 lymphocytes for treatment of cancer or infectious disease. The microencapsulated immunogen has an enteric coating for oral administration.Type: GrantFiled: March 12, 1998Date of Patent: December 11, 2001Assignee: Allergenics, Inc.Inventor: Roberto L. Rivera
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Publication number: 20010043945Abstract: A pharmaceutical composition is provided containing an admixture of phenytoin sodium and an erodible matrix which extends the release of the phenytoin sodium over about a two hour period. The erodible matrix comprises binder(s) and diluent(s) which control the release of drug from the pharmaceutical composition. The erodible matrix can further comprise an alkaline pH modifier.Type: ApplicationFiled: May 11, 2001Publication date: November 22, 2001Applicant: MYLAN PHARMACEUTICALS INC.Inventors: William J. Addicks, Joseph P. Duda, Daniel A. Snider, Kerry R. Benson
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Patent number: 6316031Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.Type: GrantFiled: December 22, 1999Date of Patent: November 13, 2001Assignee: Purdue Pharma LPInventors: Benjamin Oshlack, Frank Pedi, Jr., Mark Chasin
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Publication number: 20010033866Abstract: Pharmaceutical composition capable of releasing a therapeutically effective dose of active agent, e.g., rivastigamine, in a time-controlled manner.Type: ApplicationFiled: March 27, 2001Publication date: October 25, 2001Inventors: Jorg Ogorka, Oskar Kalb, Rajen Shah, Satish Chandra Khanna
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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: 6303581Abstract: Methods and kits for removing, treating or preventing head lice infestations in patients in need of such treatment are disclosed and include topically applying to the lice-infested area an effective amount of a driable pediculostatic agent for a time sufficient to immobilize the lice, drying the agent onto the application site and removing the dried agent, thereby removing the lice and nits.Type: GrantFiled: April 25, 2001Date of Patent: October 16, 2001Inventor: Dale L. Pearlman
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Patent number: 6297033Abstract: A system for nitrate removal from aquariums, both fresh water and marine aquariums, by means of permeable polymeric beads which contain a combination of fermentative and denitrifying bacteria and a carbon source. Preferred beads are beads made from sodium alginate or chitosan. The bacteria, in the presence of the carbon source, are able to reduce nitrate to nitrogen gas. Bacteria which are not harmful to fish are used. The porous beads used in the process are novel and part of the invention.Type: GrantFiled: March 5, 1998Date of Patent: October 2, 2001Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Jaap Van Rijn, Amos Nussinovitch, Joseph Tal
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Patent number: 6284269Abstract: Pharmaceutical compositions containing enolic carboxamide type antiinflammatory agent meloxicam that exhibit improved wettability, aqueous solubility, dissolution behaviour over a broad range of pH, and that are prepared by crystal structure modification of the drug through dry or wet mechanical homogenization with two further components—one of them is selected from a group of oligo—and dissolution improving, or alkalizing agent. The application of the formulations according to the present invention results in an improved biovailability and effectiveness of meloxicam.Type: GrantFiled: May 10, 2000Date of Patent: September 4, 2001Assignee: Hexal AGInventors: Andreas Struengmann, Brigitte Freudensprung, Karin Klokkers
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Patent number: 6274171Abstract: This invention relates to a 24 hour extended release dosage formulation and unit dosage form thereof of venlafaxine hydrochloride, an antidepressant, which provides better control of blood plasma levels than conventional tablet formulations which must be administered two or more times a day and further provides a lower incidence of nausea and vomiting than the conventional tablets. More particularly, the invention comprises an extended release formulation of venlafaxine hydrochloride comprising a therapeutically effective amount of venlafaxine hydrochloride in spheroids comprised of venlafaxine hydrochloride, microcrystalline cellulose and, optionally, hydroxypropylmethylcellulose coated with a mixture of ethyl cellulose and hydroxypropylmethylcellulose.Type: GrantFiled: January 20, 2000Date of Patent: August 14, 2001Assignee: American Home Products CorporationInventors: Deborah M. Sherman, John C. Clark, John U. Lamer, Steven A. White
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Patent number: 6274170Abstract: Compounds comprising multi-vitamins, zinc and an anti-platelet aggregating agent for the treatment of atherosclerotic cardiovascular disease (ASCVD) are disclosed. The compounds are provided in dosage form, and preferably include selected amounts of ascorbic acid, folic acid, vitamin E, vitamin B6 and vitamin B12. The anti-platelet aggregating agent preferably comprises aspirin. A protective coating is preferably provided between the aspirin and the other vitamin and mineral constituents. The dosages are effective in the treatment of ASCVD, and possess extended shelf lives.Type: GrantFiled: February 18, 1999Date of Patent: August 14, 2001Inventors: Richard Heibel, John J. Abbott
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Patent number: 6270804Abstract: Bioaffecting sachets, or powders, containing coated liquiflash microspheres and partially recrystallized shearform floss particles are disclosed. The sachets give organoleptically acceptable properties, including a pleasing mouthfeel, when orally ingested.Type: GrantFiled: October 30, 1998Date of Patent: August 7, 2001Assignee: Biovail Technologies Ltd.Inventors: John J. Getz, Steven E. Frisbee, Tushar K. Misra, John R. Sisak, Pradeepkumar P. Sanghvi
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Patent number: 6265384Abstract: Methods and kits for removing, treating or preventing head lice infestations in patients in need of such treatment are disclosed and include topically applying to the lice-infested area an effective amount of a driable pediculostatic agent for a time sufficient to immobilize the lice, drying the agent onto the application site and removing the dried agent, thereby removing the lice and nits.Type: GrantFiled: January 25, 2000Date of Patent: July 24, 2001Inventor: Dale L. Pearlman
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Patent number: 6258846Abstract: The present disclosure relates to novel nutritional compositions containing linoleic acid and/or linolenic acid which optimize child neurological development and provide improved nutritional support for women prior to and during lactation. The nutritional compositions are intended for use by women to optimize infant neurological development and provide improved nutritional support for women prior to, during and after lactation.Type: GrantFiled: June 1, 1999Date of Patent: July 10, 2001Assignee: Drugtech CorporationInventors: Marc S. Hermelin, R. Saul Levinson, George Paradissis
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Patent number: 6251429Abstract: Programmed-release ambroxol·HCl pharmaceutical dosage forms, adopted to maintain a therapeutically effective plasma level thereof for about 24 hours, comprise a plurality of inert core microgranules of a variety of particle sizes ranging from 0.3 to 1.2 mm, such inert core microgranules being coated with alternating microlayers of (1) micronized ambroxol hydrochloride active agent and (2) delayed-release film material, such coated microgranules including an external microlayer of delayed-release film material, and such coated mi.crogranules having particle sizes ranging from 0.6 to 1.5 mm.Type: GrantFiled: January 30, 1995Date of Patent: June 26, 2001Assignee: Therapicon slrInventors: Paolo Alberto Veronesi, Anna Maria Veronesi
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Patent number: 6251879Abstract: A delivery system is provided to reduce methane production in animals or to improve the weight gain of an animal. Embodiments include a delivery system comprising a volatile and/or water soluble antimethanogenic agent with cyclodextrin or a cyclodextrin-like compound.Type: GrantFiled: June 14, 1999Date of Patent: June 26, 2001Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Christopher May, Alan Lindsay Payne, Philip Laurence Stewart, John Alexander Edgar
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Patent number: 6245351Abstract: A controlled-release composition comprising a drug-containing core coated with a coating composition containing a water-insoluble substance and a swellable polymer having no basic groups which is capable of maintaining an almost constant drug concentration in plasma over an extended period of time to ensure sustained drug action in the body.Type: GrantFiled: March 4, 1997Date of Patent: June 12, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Eiji Nara, Yohko Akiyama, Kenji Nakamura
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Patent number: 6228355Abstract: The invention provides a method and compositions for controlling food borne enteric bacterial pathogens in poultry populations. The incidence of the colonization of poultry by enteropathogenic bacteria, and/or the populations of enteropathogenic bacteria within colonized poultry, may by substantially reduced by providing particles of an expanded matrix material to the locus or vicinity of the animals, particularly during the period of feed removal prior to slaughter. The method and compositions are particularly useful for the control of Salmonella species, enteropathogenic Escherichia coli, and Campylobacter species.Type: GrantFiled: June 13, 2000Date of Patent: May 8, 2001Assignee: The United States of America as represented by the Secretary of AgricultureInventors: James A. Byrd, II, Larry H. Stanker, Donald E. Corrier
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Patent number: 6214385Abstract: A controlled absorption diltiazem pellet formulation for oral administration comprises a core having diltiazem or a pharmaceutically acceptable salt thereof as the active ingredient. The core is surrounded by a coating which has only a single layer which is comprised of a relatively major proportion of talc and relatively minor proportion of sodium lauryl sulfate admixed with a minor proportion of a pharmaceutically acceptable film-forming, first polymer permeable to water and diltiazem, and a major proportion of a pharmaceutically acceptable film-forming, second polymer that is less permeable to water and diltiazem than the first polymer. The core and the coating layer both exclude organic acids. The composition of the coating layer as well as the proportion of core to coating layer are effective to permit release of the diltiazem allowing controlled absorption following oral administration.Type: GrantFiled: November 23, 1999Date of Patent: April 10, 2001Inventors: Grant W. Heinicke, Angelo Lepore, Angelo M. Morella
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Patent number: 6214621Abstract: The invention relates to an ionic conjugate, which is stable in a biological medium, and which is comprised of a particle vector with at least one cationic, nonliquid, hydrophilic nucleus and of polyanionic oligonucleotides. The invention further concerns the pharmaceutical compositions containing these conjugates and the use of a particle vector to carry the oligonucleotides to the cells.Type: GrantFiled: September 30, 1999Date of Patent: April 10, 2001Assignee: Biovector Therapeutics, S.A.Inventors: Didier Betbeder, Roger Kravtzoff, Ignacio de Miguel, Sophie Sixou, Pamela Pavco, Thale Jarvis
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Patent number: 6207198Abstract: A composition, particularly adapted for oral administration, containing omeprazole, and a method for preparing the composition, are disclosed. The composition, being exempt of alkaline-reacting compounds, contains a core constituted of nuclei and said benzimidazole, the nuclei and benzimidazole being compressed together, an intermediate layer, and an enteric layer.Type: GrantFiled: August 3, 1998Date of Patent: March 27, 2001Assignee: Schwarz Pharma AGInventor: Pawan Seth
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Patent number: 6207718Abstract: A composition of a hedgehog protein which includes as an additive cyclodextrin, a non-ionic detergent, an anionic saccharide and/or ionic salt containing zinc ions, magnesium ions, calcium ions and/or sulfate ions is especially stable at room temperature.Type: GrantFiled: August 2, 1999Date of Patent: March 27, 2001Assignee: Ontogeny, Inc.Inventor: Apollon Papadimitriou
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Patent number: 6200602Abstract: The invention provides a drug delivery composition for colonic delivery comprising a polar drug, an absorption promoter which (a) comprises a mixture of a fatty acid having 6 to 16 carbon atoms or a salt thereof and a dispersing agent, or (b) comprises a mixture of mono/diglycerides of medium chain fatty acids and a dispersing agent, and means adapted to release the polar drug and absorption promoter in the colon following oral administration. A preferred fatty acid is capric acid or a salt thereof. Colon specific delivery can be achieved by providing the composition in a capsule, tablet or pellet which is coated with a material which dissolves in the small intestine or is degraded by the conditions in the colon.Type: GrantFiled: March 30, 1998Date of Patent: March 13, 2001Assignee: West Pharmaceutical Services Drug Delivery & Clinical Research Centre LimitedInventors: Peter James Watts, Lisbeth Illum
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Patent number: 6197347Abstract: An oral dosage form that provides for the controlled release of an analgesic wherein the dosage form comprises a core containing an analgesic that is coated with a mixture of an enteric polymer, a water insoluble polymer and a lubricant.Type: GrantFiled: June 29, 1998Date of Patent: March 6, 2001Assignee: Andrx Pharmaceuticals, Inc.Inventors: Steve Jan, Xiu Xiu Cheng, Chih-Ming Chen
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Patent number: 6180661Abstract: Spontaneously dispersible concentrates capable of forming ultramicroemulsions are described. The concentrates include esters of formula (I) and (II): wherein (a) R1, R3, R4, and R5 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R2 is glucose:(1,2); (b) R2, R3, R4, and R5 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R1 is glucose:(1,3); (c) R2, R3, R4, and R5 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R1 is rhamnose:(1,4); or (d) R2, R3, R4, and R5 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R1 is rutinose:(1,5); wherein (a) R1, R2, and R4 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene and R3 is rhamnose:(11,7); or (b) R2 and R4 each independently represents a C6-22 alkyl, a C6-22 alkenyl or a C6-22 alkapolyene, R1 is methyl, and R3 is rutinose:(11,8).Type: GrantFiled: January 21, 1998Date of Patent: January 30, 2001Assignee: Marigen, S.A.Inventors: Carl Eugster, Conrad Hans Eugster
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Patent number: 6172107Abstract: 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: December 22, 1999Date of Patent: January 9, 2001Assignee: Novartis AGInventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
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Patent number: 6165495Abstract: A drug delivery system comprising a dissolvable solid portion (10) having an outer (12) and inner surface (14) and a cavity (16) for receiving fluid. The cavity (16) is surrounded by, and contained within, the solid portion (10). Both the solid portion (10) and the cavity (16) are supported by a handle (20). A method of administering a drug is also disclosed.Type: GrantFiled: October 23, 1996Date of Patent: December 26, 2000Inventor: Mildred Blankenship
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Patent number: 6165513Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.Type: GrantFiled: June 10, 1998Date of Patent: December 26, 2000Assignee: The Procter & Gamble Co.Inventors: Richard John Dansereau, Petrus Jakobus Bekker
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Patent number: 6162471Abstract: A prethickened hydrolytic beverage useful in rehydrating and regaining electrolytic balance with those suffering from dysphagia. Said beverage comprises water, a carbohydrate source, a modified food starch, various electrolytes and other minor ingredients.Type: GrantFiled: November 19, 1999Date of Patent: December 19, 2000Assignee: Hormel Foods CorporationInventor: Kathie L. Sheldon
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Patent number: 6159499Abstract: The present invention relates to a composition, particularly adapted to oral administration, substantially free of alkaline-reacting compounds. The composition comprises (a) a core containing an acid-labile benzimidazole active principle, where the core comprises a plurality of nuclei and the active principle mixed together and then compressed together, and where the active principle is not in the form of an alkaline salt; (b) an intermediate layer; and (c) an enteric layer; provided that omeprazole is not the benzimidazole active principle. A process for preparing the composition is also disclosed.Type: GrantFiled: October 20, 1998Date of Patent: December 12, 2000Assignee: Pharma Pass LLCInventor: Pawan Seth
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Patent number: 6159501Abstract: An oral pharmaceutical modified release multiple-units composition for the administration of an analgesically effective amount of an opoid. The composition comprises at least two fractions wherein individual units containing an opoid are coated with a sustained release coating. A first fraction is adapted to relatively fast release while a second fraction is adapted to a delayed release. Such compositions make possible to obtain both a relatively fast onset of the analgesic effect and the maintenance of analgesically active plasma concentration for a relatively long period of time. The invention further relates to a process for the preparation of a composition according to the invention.Type: GrantFiled: June 22, 1998Date of Patent: December 12, 2000Assignee: Nycomed Danmark A/SInventor: Annette Skinhoj
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Patent number: 6156347Abstract: The present invention relates to controlled/extended release oral dosage forms of chromium picolinate. Chromium picolinate is a common and effective biologically active form of chromium. As such, it has beneficial nutritional and therapeutic effects including improved insulin metabolism and lipid lowering activity.The controlled dosage form of the present invention can be provided in various ways, including matrix formulations such as matrix tablets or multiparticulate formulations like micro capsules or coated pellets put into hard gelatin capsules. This provides effective drug delivery for extended periods of time, at relatively stable, optimal plasma peak values, with minimal undesirable side effects.The invention provides effective controlled/extended release oral dosage formulations of chromium picolinate and processes for their preparation.Type: GrantFiled: January 21, 1998Date of Patent: December 5, 2000Assignee: Bio-Dar Ltd.Inventors: Yoav Blatt, Oded Friedman, Eugene Kimelman, Avner Rotman
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Patent number: 6143322Abstract: Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. of from about 12.5% to about 42.5% (by wt) opioid released after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of said opioid analgesic obtained in-vivo occurs from about 2 to about 8 hours after administration of the dosage form.Type: GrantFiled: April 8, 1997Date of Patent: November 7, 2000Assignee: Purdue Pharma L.P.Inventors: Richard Sackler, Robert Kaiko, Paul Goldenheim
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Patent number: 6139877Abstract: The present invention relates to a novel pharmaceutical form, in the form of spheroids, containing tiagabine as active principle. The invention also covers the process for the preparation of such spheroids and multiparticulate pharmaceutical preparations, such as tablets, containing these spheroids. These pharmaceutical preparations are intended for the delivery of the spheroids they contain, and are characterized by the absence of an adverse effect on the release profile of the tiagabine contained in the spheroids following a possible compression step.Type: GrantFiled: November 23, 1998Date of Patent: October 31, 2000Assignee: Laboratoires des Produits Ethiques EthypharmInventors: Patrice Debregeas, Gerard Leduc, Pascal Oury, Pascal Suplie
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Patent number: 6132772Abstract: The present invention relates to extended-release solid oral dosage forms of a drug having low solubility in water are obtained by dissolving the drug in polyethylene glycol having a mean molecular weight of at least 1000 and adding thereto a hydrophilic gel-forming polymer.Type: GrantFiled: July 31, 1997Date of Patent: October 17, 2000Inventor: Bernard Charles Sherman
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Patent number: 6129933Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.Type: GrantFiled: July 24, 1997Date of Patent: October 10, 2000Assignee: Purdue Pharma LPInventors: Benjamin Oshlack, Mark Chasin, Frank Pedi, Jr.
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Patent number: 6126967Abstract: An extended release acetaminophen composition comprises a plurality of discrete particles containing acetaminophen which, when contained within a gelatin capsule and assayed in a USP Apparatus I rotating basket at 50 rpm in 900 mL of phosphate buffer at pH 5.8 and 37.degree. C., exhibits about 40 percent to about 53 percent acetaminophen dissolution at one-half hour, about 50 percent to about 68 percent dissolution at 45 minutes, about 57 percent to about 77 percent acetaminophen dissolution at one hour, and about 82 percent to about 92 percent acetaminophen dissolution at two hours. After six hours, the contemplated extended release acetaminophen composition exhibits substantially complete dissolution. A process for treating a human patient with the extended release acetaminophen composition is also disclosed.Type: GrantFiled: September 3, 1998Date of Patent: October 3, 2000Assignee: Ascent PediatricsInventors: Emmett Clemente, Aloysius O. Anaebonam, Robert W. Mendes, Abdel A. Fawzy, Eric M. Morrel
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Patent number: 6120787Abstract: A method of preparing parenterally administrable sustained release microparticles, which comprises preparing core particles in an aqueous medium that is essentially free from organic solvent, a biologically active substance being entrapped therein during or after said preparation, drying the core particles and coating the same with a release-controlling polymer by air suspension technique so as to create a shell on the core particles without any detrimental exposure of the active substance to organic solvent. Microparticles obtainable by such a method also are provided.Type: GrantFiled: April 17, 1998Date of Patent: September 19, 2000Assignee: Biogram ABInventors: Nils-Ove Gustafsson, Timo Laakso, Peter Fyhr, Monica Jonsson
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Patent number: 6110494Abstract: A sustained release cisapride oral dosage formulation suitable for once-daily administration comprises a plurality of mini-tablets containing cisapride or a salt thereof with an organic acid and capable of releasing cisapride at different sites along the gastrointestinal tract. The mini-tablets include a proportion of immediate release tablets and a proportion of tablets which release cisapride in response to the pH environment at a given site in the distal regions of the gastrointestinal tract and which include cisapride or a salt thereof embedded in a matrix of hydrophilic polymer, said matrix being coated with a pH dependent polymer, the formulation having a Cmax/Cmin ratio under steady state conditions of 2:1 or less as evidenced by a substantially flat plasma profile in vivo.Type: GrantFiled: December 22, 1997Date of Patent: August 29, 2000Assignee: Elan Corporation, plcInventors: Maurice Joseph Anthony Clancy, Kenneth Iain Cumming
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Patent number: 6096337Abstract: Liquisolid systems are acceptably flowing and compressible powdered forms of liquid medications. According to the concept of liquisolid systems, liduid lipophilic drugs, or water-insoluble solid drugs dissolved in suitable non-volatile solvents, may be converted into free-flowing and readily compressible powders by a simple admixture with selected powder excipients referred to as the carrier and coating materials. Various grades of microcrystalline or amorphous cellulose may be used as carriers, whereas very fine particle size silica powders may be used as coating materials.Type: GrantFiled: August 19, 1998Date of Patent: August 1, 2000Inventors: Spiridon Spireas, Sanford M. Bolton
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Patent number: 6086918Abstract: Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by virtue of an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition includes an absorption enhancer and a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.Type: GrantFiled: August 19, 1998Date of Patent: July 11, 2000Assignee: Unigene Laboratories, Inc.Inventors: William Stern, James P. Gilligan
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Patent number: 6077533Abstract: An oral dosage form of morphine is formulated by powder-layering an homogeneous mixture of morphine sulfate and hydrous lactose impalpable onto inert beads to obtain a multiparticulate product. A plurality of the powder-layered beads may be administered either in immediate release form or in an extended release form by coating with a hydrophobic material. In addition, multi-particulate oral dosage forms containing therapeutically effective agents containing a plurality of pharmaceutically acceptable inert beads powder-layered with homogeneous mixture of a therapeutically effective agent and hydrous lactose impalpable are also disclosed. A method of preparing the dosage forms as well as a method preparing spheroids containing the homogeneous mixture of therapeutically effective agent and hydrous lactose impalpable are also disclosed.Type: GrantFiled: January 12, 1998Date of Patent: June 20, 2000Assignee: Purdue Pharma L.P.Inventors: Benjamin Oshlack, Frank Pedi
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Patent number: 6066333Abstract: Control of inflammation is achieved by control of the level and/or activity of the enzyme heme-oxygenase (HO). A HO inducer is anti-inflammatory (FIG. 14) and used to treat inflammation, such as chronic inflammatory diseases. A HO inhibitor promotes inflammation and is used to treat immunosuppressed conditions. Alternative, or additional, control of heme-oxygenase activity is achieved by control of nitric oxide levels, elevated levels promoting inflammation.Type: GrantFiled: March 21, 1997Date of Patent: May 23, 2000Assignee: William Harvey Research LimitedInventors: Dean Willis, Adrian Richard Moore, Derek Albert Willoughby
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Patent number: 6056949Abstract: The present invention relates to a process for the preparation of spherical or substantially spherical, practically dust-free aromatic and odoriferous granulated material which is free-flowing, mechanically stable and has a narrow grain-size distribution.Type: GrantFiled: April 6, 1998Date of Patent: May 2, 2000Assignee: Givaudan Roure (International) SAInventors: Heini Menzi, Matthias Perren, Rudolf Ringgenberg
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Patent number: 6054145Abstract: Disclosed is a process for the preparation of pharmaceutical dosage units containing as an active substance of from 0.005 to 1.0% by weight of micronised Org 30659, comprising (a) a mixing step comprising bringing into association the active substance and a suitable carrier to form a mixture, and (b) a granulating step in which the mixture is granulated to form agglomerates or granules by wetting the mixture with a binder liquid, the wetting being conducted under agitation, characterised in that the granulation step (b) is conducted so as to exert on the granules a shear force which does not exceed the tensile strength of the agglomerates or granules. The process leads to granules and tablets having an excellent content/uniformity.Type: GrantFiled: March 12, 1999Date of Patent: April 25, 2000Assignee: Akzo Nobel, N.V.Inventors: Herman Vromans, Hendrika Gerardina Maria Poels-Janssen
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Patent number: 6039958Abstract: A stabilized live vaccine containing a varicella virus and a stabilizer, wherein the vaccine is substantially free of Ca.sup.2+ ions and Mg.sup.2+ ions is described. This stabilized live vaccine is excellent in storage stability and heat resistance. Also described is an improved stabilizer for a live varicella vaccine, comprising at least gelatin or hydrolyzed gelatin, each being substantially free of Ca.sup.2+ ions and Mg.sup.2+ ions. The stabilizer can advantageously be used to stabilize a live vaccine containing a varicella virus. The substantial freedom of Ca.sup.2+ ions and Mg.sup.2+ ions can be attained by masking Ca.sup.2+ ions and Mg.sup.2+ ions present in a live vaccine containing a varicella virus and a stabilizer, with a chelating reagent, or by using as a stabilizer gelatin and/or a gelatin derivative after being purified to remove Ca.sup.2+ ions and/or Mg.sup.2+ ions contained therein.Type: GrantFiled: October 28, 1998Date of Patent: March 21, 2000Assignee: The Research Foundation for Microbial Diseases of Osaka UniversityInventors: Kuniaki Koyama, Juichiro Osame
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Patent number: 6033687Abstract: A controlled absorption diltiazem pellet formulation for oral administration comprises a core having diltiazem or a pharmaceutically acceptable salt thereof as the active ingredient. The core is surrounded by a coating which has only a single layer which is comprised of a relatively major proportion of talc and relatively minor proportion of sodium lauryl sulfate admixed with a minor proportion of a pharmaceutically acceptable film-forming, first polymer permeable to water and diltiazem, and a major proportion of a pharmaceutically acceptable film-forming, second polymer that is less permeable to water and diltiazem than the first polymer. The core and the coating layer both exclude organic acids. The composition of the coating layer as well as the proportion of core to coating layer are effective to permit release of the diltiazem allowing controlled absorption following oral administration.Type: GrantFiled: April 7, 1999Date of Patent: March 7, 2000Assignee: F.H. Faulding & Co.Inventors: Grant W. Heinicke, Angelo Lepore, Angelo M. Morella