Sustained Or Differential Release Patents (Class 424/457)
Containing discrete coated particles pellets, granules, or beads (Class 424/458)
  • Ovulation triggering drugs
    Patent number: 6407057
    Abstract: The invention relates to medicaments for initiating ovulation comprising LH in an administrable form which ensures an increase in LH plasma levels for a period of some 40 to 60 hours.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: June 18, 2002
    Assignee: Applied Research System ARS Holding N.V.
    Inventor: Jean-Claude Emperaire
  • Anticonvulsant containing composition for treating neuropathic pain
    Patent number: 6406716
    Abstract: The effectiveness of an anticonvulsant such as gabapentin for alleviating neuropathic pain is potentiated by a nontoxic antagonist for the N-methyl-D-aspartate receptor or nontoxic substance that blocks a major intracellular consequence of N-methyl-D-aspartate receptor activation.
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: June 18, 2002
    Assignee: Endo Pharmaceuticals Inc.
    Inventors: Frank S. Caruso, Fredrick L. Minn, John W. Lyle
  • Treatment of H. pylori associated gastroduodenal disease
    Patent number: 6406703
    Abstract: The application discloses a method for the treatment of Heliobacter infection in a mammalian host, which comprises administration to said infected host of an immunologically effective amount of one or more Heliobacter antigen(s), optionally in association with a mucosal adjuvant.
    Type: Grant
    Filed: July 5, 2000
    Date of Patent: June 18, 2002
    Assignees: CSL Limited, The University of New South Wales
    Inventors: Christopher Vincent Doidge, Adrian Lee
  • Discoloration-resistant vitamin composition
    Patent number: 6403119
    Abstract: The invention disclosed herein includes a vitamin composition encapsulated in a soft or hard shell capsule, said vitamin composition comprising water soluble vitamin particles suspended in a fill liquid, wherein said water soluble vitamin particles are coated with a material that is substantially insoluble in the fill liquid and the shell of the capsule, but soluble in the gastrointestinal tract of a mammal, and the coated water soluble vitamin particles are of a size that are suitable for encapsulating as a suspension in said capsule. The invention also includes a process for manufacturing the same. Vitamin containing capsules according to this invention are discoloration-resistant.
    Type: Grant
    Filed: May 4, 2000
    Date of Patent: June 11, 2002
    Assignee: R. P. Scherer Technologies, Inc.
    Inventors: Richard Charles Oppenheim, Hung Cam Truong
  • Extended release formulation of venlafaxine hydrochloride
    Patent number: 6403120
    Abstract: 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 fiber 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: Grant
    Filed: September 12, 2001
    Date of Patent: June 11, 2002
    Assignee: Wyeth
    Inventors: Deborah M. Sherman, John C. Clark, John U. Lamer, Steven A. White
  • Pharmaceutical compositions
    Patent number: 6399104
    Abstract: A dry powder layering process for preparing pharmaceutical compositions of the leukotriene antagonist zafirlukast. The process forms coated beads suitable for sprinkling on to food and drink.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: June 4, 2002
    Assignee: AstraZeneca UK Limited
    Inventors: Joseph R Creekmore, Susan J Corvari
  • EPIDURAL ADMINISTRATION OF THERAPEUTIC COMPOUNDS WITH SUSTAINED RATE OF RELEASE
    Publication number: 20020065506
    Abstract: A drug delivery system provides sustained-release delivery of therapeutic biologically active compounds administered epidurally. In the preferred embodiment the biologically active compound is an opioid, which is encapsulated within the non-concentric internal aqueous chambers or bilayers of multivesicular liposomes. The opioid is released over an extended period of time when the liposomes are introduced epidurally as a single dose for sustained analgesia.
    Type: Application
    Filed: September 16, 1997
    Publication date: May 30, 2002
    Applicant: SkyePharma, Inc.
    Inventors: ANDRAS GRUBER, SHARAD B. MURDANDE, TAEHEE KIM, SINIL KIM
  • Pharmaceutical formulation comprising a 2- [(2-pyridinyl) methyl] sulfinyl benzimidazole having anti-ulcer activity and a process for the preparation of such formulation
    Patent number: 6391342
    Abstract: Oral pharmaceutical formulation comprising granules having an inert core coated with a layer, comprising a 2-[[(2-pyridinyl)methyl]sulfinyl]benzimidazole having anti-ulcer activity, a disintegrant and a surfactant in a matrix of a melt coating substance essentially consisting of one or more esters of glycerol and fatty acids, a separating layer and an enteric coating layer, and a process for the preparation of such formulation using a melt coating technique for the preparation of the benzimidazole containing layer.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: May 21, 2002
    Assignee: A/S GEA Farmaceutisk Fabrik
    Inventors: Kristian Lund Henriksen, Helle Kann, Karen Eichstedt Sørensen, Søren Bols Pedersen
  • Inorganic-polymer complexes for the controlled release of compounds including medicinals
    Patent number: 6391336
    Abstract: This invention relates generally to the production and use of inorganic-polymer complexes for the controlled release of compounds including medicinals. The inorganic compound used is advantageously calcium sulfate-hemihydrate. The invention includes a composition for the controlled release of an active agent comprising: a) a hydrated or crystallized inorganic compound, and b) a matrix polymer which slows the release of the active agent, wherein the composition is a solid matrix due to the hydration or crystallization of the inorganic compound. Further included is a composition for the controlled release of an active agent comprising: a) a hydrated or crystallized inorganic compound, and b) a complexing agent which forms a salt or conjugate with the active agent, wherein the composition is a solid matrix due to the hydration or crystallization of the inorganic compound.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: May 21, 2002
    Assignee: Royer Biomedical, Inc.
    Inventor: Garfield P. Royer
  • Microcapsule and method of making the same
    Patent number: 6391288
    Abstract: A microcapsule of the present invention is characterized in that it encapsulate oil droplets having average particle size of 0.01 to 3 &mgr;m and its capsulating agent is a hydrophilic polymer gelling agent. The main component of the capsulating agent is preferably a hydrophilic polymer gelling agent which hardens by heating and cooling, and, in particular, agar or carrageenan. In the making method of the present invention, a microcapsule can be made efficiently due to no loss in the inner oil phase, and its particle size can easily be controlled. The microcapsule is excellent in shearing-resistance, store stability. Also, if the fracture strength of the microcapsule is within a specific range, a microcapsule which releasing characteristic of encapsulated oil droplets when applied is immediately-, gradually- or non-releasing can be obtained.
    Type: Grant
    Filed: July 26, 2000
    Date of Patent: May 21, 2002
    Assignee: Shiseido Co., Ltd.
    Inventors: Kazuyuki Miyazawa, Isamu Kaneda, Toshio Yanaki
  • Sustained-release microgranules containing diltiazem as active principle
    Patent number: 6383516
    Abstract: Novel forms of sustained-release microgranules (LP) containing diltiazem are disclosed. The microgranules consist of a neutral granular carrier coated with an active layer including diltiazem or a pharmaceutically acceptable salt thereof as the active principle, a surfactant and a binder, and an outer layer providing sustained release of the active principle (layer LP).
    Type: Grant
    Filed: January 11, 2001
    Date of Patent: May 7, 2002
    Assignee: Laboratoires des Produits Ethiques Ethypharm
    Inventors: Patrice Debregeas, Gérard Leduc, Pascal Oury, Pascal Suplie
  • Biodegradable glass compositions and methods for radiation therapy
    Patent number: 6379648
    Abstract: A nonradioactive glass in particulate form adapted for radiation therapy in a mammal comprise a biodegradable rare earth-lithium borate glass material of a specified composition which, upon being subjected to an effective amount of neutron irradiation, will produce a beta or gamma emitting radioisotope, the radioisotope being distributed throughout the glass material, the glass upon being introduced into a body fluid for radiation therapy being adapted to react therewith causing the radioisotope to form an insoluble compound on the surface of the glass material which is retained in the glass material and thereby prevented from escaping from the treatment site. Radioactive glasses and methods for carrying out radiation therapy with such radioactive glasses are also disclosed.
    Type: Grant
    Filed: February 1, 1999
    Date of Patent: April 30, 2002
    Assignee: The Curators of the University of Missouri
    Inventors: Delbert E. Day, James E. White
  • Method for increasing tissue perfusion by co-administration of an agent that increases cGMP synthesis and an agent that inhibits cGMP degradation
    Publication number: 20020048599
    Abstract: A method for increasing tissue perfusion with blood by the co-administration of an agent that increases cGMP synthesis and an agent that inhibits cGMP degradation in the cells of the blood vessel walls or in blood cells. The method comprises, for example, the co-administration of therapeutically effective amounts of a statin and dipyridamole, especially a timed-release formulation of dipyridamole.
    Type: Application
    Filed: October 16, 2001
    Publication date: April 25, 2002
    Inventor: Thomas H. Mueller
  • Process for producing aqueous solution of fumaric acid
    Patent number: 6375974
    Abstract: A process for obtaining an aqueous fumaric acid solution which is useful in stably obtaining a large amount of aqueous fumaric acid solution. A column is packed with solid fumaric acid and then water is passed through the column, thereby giving an aqueous fumaric acid solution. Water is usually passed in the reverse direction. The solid fumaric acid may be in the form of tablets containing 70% by weight or more of fumaric acid. The aqueous fumaric acid solution thus obtained has a pH value of about 1 to 4. A urinal, etc. is treated with a fumaric acid-containing deodorizing agent to thereby efficiently deodorize nitrogen-containing bad-smelling components over a long period of time. A solid deodorizing agent containing fumaric acid, which has an extremely low solubility and a low dissolution rate in water, is placed on a urinal to deodorize the same.
    Type: Grant
    Filed: December 23, 1999
    Date of Patent: April 23, 2002
    Assignee: Mitsui Takeda Chemicals, Inc.
    Inventors: Toshio Ito, Yukio Tanaka
  • Copolymer and process for preparing the same
    Patent number: 6372880
    Abstract: A copolymer having a weight-average molecular weight of 1,000 to 100,000 which comprises, as repeating structure units, both of a succinimide unit represented by the structural formula (1) and a hydroxycarboxylic acid unit represented by the structural formula (2) wherein R is a methyl group or a hydrogen atom, and a process for preparing a copolymer which comprises a polymerization step of heating a mixture of aspartic acid and a cyclic ester compound.
    Type: Grant
    Filed: December 23, 1998
    Date of Patent: April 16, 2002
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hosei Shinoda, Yukiko Asou, Hiroaki Tamatani
  • Microparticles which controllably release olfactorily active substances, methods of using same and processes for preparing same
    Patent number: 6368633
    Abstract: Described are flavor composition, flavor component, perfume composition and perfume component-containing microparticles which are particulate matrices composed of: (a) an olfactorily active component (e.g., perfume component); (b) silica; and (c) a saccharide composition which is a mixture of mannitol and maltose. The microparticles are useful in augmenting, enhancing and/or imparting aroma and/or taste (over relatively long periods of time in a controllably releasable manner) to perfume compositions, perfumed articles (e.g., deodorancy and antiperspirant sticks), foodstuffs, chewing gums, beverages and the like. Also described is a process for preparing the above-mentioned microparticles using, in sequence, (1) adsorption of the olfactorily active material onto silica followed by (2) a blending/extrusion step followed by (3) at least one particularization step.
    Type: Grant
    Filed: May 14, 2001
    Date of Patent: April 9, 2002
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Wen Chin Lou, Keith J. McDermott, Shmuel David Shefer, Adi Shefer, John M. Teffenhart, Chee-Teck Tan, Jerome I. Lindauer, Leslie C. Smith
  • Sustained-release preparation
    Publication number: 20020031545
    Abstract: Disclosed is a sustained-release preparation comprising 1) a polymer of lactic acid having a weight-average molecular weight of about 25,000 to about 60,000 and 2) a physiologically active substance, and which releases the physiologically active substance over a period of at least about 5 months; the sustained-release preparation shows an almost continuous zero order release of the physiologically active substance over a period of as long as about 5 months.
    Type: Application
    Filed: March 7, 2000
    Publication date: March 14, 2002
    Inventors: Hiroaki Okada, Yayoi Douken
  • Oral calcitonin pharmaceutical compositions and methods of making the same
    Patent number: 6352974
    Abstract: The present invention relates to novel compositions, in particular to compositions comprising calcitonin or a fragment or conjugate thereof and to methods for preparing such compositions. It also relates to oral formulations comprising the compositions and to shelf stable formulations of calcitonin or a fragment or conjugate thereof.
    Type: Grant
    Filed: September 21, 1999
    Date of Patent: March 5, 2002
    Assignee: Eurand International S.p.A.
    Inventors: Matteo Ghirri, Marco Zema
  • Extended release formulation
    Publication number: 20020025339
    Abstract: 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 fiber 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: Application
    Filed: September 12, 2001
    Publication date: February 28, 2002
    Applicant: American Home Products Corporation
    Inventors: Deborah M. Sherman, John C. Clark, John U. Lamer, Steven A. White
  • Apatite-coated solid composition
    Patent number: 6344209
    Abstract: An apatite-coated solid composition which contains a biodegradable polymer and an apatite-coated solid composition which contains a biodegradable polymer and a medicinal substance have properties of sustained release and of osteoconductive activity.
    Type: Grant
    Filed: October 20, 1999
    Date of Patent: February 5, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kazuhiro Saito, Tetsuo Hoshino
  • Methylphenidate modified release formulations
    Patent number: 6344215
    Abstract: A pharmaceutical MR (modified release) multiparticulate dosage form such as a capsule (once-a-day MR Capsule) of Methylphenidate indicated for the treatment of children with attention deficit hyperactivity disorder (ADHD), capable of delivering a portion of the dose for rapid onset of action and the remainder of the dose in a controlled manner for about 12 hours, is composed of a multitude of multicoated particles made of two populations of drug layered beads, IR (immediate release) and ER (extended release) Beads. The IR beads preferably are made by layering an aqueous solution comprising a drug and a binder on to non-pareil sugar spheres and then applying a seal coat to the drug coated cores. The ER Beads are made by applying an extended release coating of a water insoluble dissolution rate controlling polymer such as ethylcellulose to IR Beads.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: February 5, 2002
    Assignee: Eurand America, Inc.
    Inventors: Marie J. Bettman, Phillip J. Percel, Dan L. Hensley, Krishna S. Vishnupad, Gopi M. Venkatesh
  • METHOD FOR PRODUCING SUSTAINED-RELEASE FORMULATIONS
    Publication number: 20020013273
    Abstract: Methods for preparing biodegradable microparticles are provided. Also provided are microparticles prepared by the method which include IGF-1 entrapped therein. The microparticles allow for controlled release of IGF-1 and other polypeptides over prolonged periods of time.
    Type: Application
    Filed: November 6, 1998
    Publication date: January 31, 2002
    Inventors: BRET SHIRLEY, MANINDER HORA, DEREK O'HAGAN, MANMOHAN SINGH
  • Pharmaceutical dosage form for pulsatile delivery of methylphenidate
    Patent number: 6340476
    Abstract: 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: Grant
    Filed: April 6, 2000
    Date of Patent: January 22, 2002
    Assignee: Armaquest, Inc.
    Inventors: Kamal K. Midha, Theodore L. Iorio, Shubha Chungi
  • SUSTAINED RELEASE HYDROMORPHONE FORMULATIONS EXHIBITING BIMODAL CHARACTERISTICS
    Publication number: 20020006438
    Abstract: The invention is related to a solid sustained release once-a-day oral dosage form comprising hydromorphone or a pharmaceutically acceptable salt thereof together with a sustained release carrier, the dosage providing a relatively rapid rise in plasma concentration to an initial early peak concentration, followed by a second broader peak with plateau plasma concentrations.
    Type: Application
    Filed: September 25, 1998
    Publication date: January 17, 2002
    Inventors: BENJAMIN OSHLACK, MARK CHASIN, HUA-PIN HUANG
  • Melt-extrusion multiparticulates
    Patent number: 6335033
    Abstract: A unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: January 1, 2002
    Assignee: Euro-Celtique, S.A.
    Inventors: Benjamin Oshlack, Hua-Pin Huang, Mark Chasin
  • ORAL PULSED DOSE DRUG DELIVERY SYSTEM
    Publication number: 20010055613
    Abstract: 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: Application
    Filed: October 21, 1998
    Publication date: December 27, 2001
    Inventors: BETH A. BURNSIDE, XIAODI GUO, KIMBERLY FISKE, RICHARD A. COUCH, RONG-KUN CHANG, DONALD J. TREACY, CHARLOTTE M. MCGUINNESS, EDWARD M. RUDNIC
  • PROCESS FOR PREPARING FAST DISPERSING SOLID ORAL DOSAGE FORM
    Publication number: 20010055611
    Abstract: 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: Application
    Filed: June 17, 1999
    Publication date: December 27, 2001
    Inventors: RICHARD GREEN, PATRICK KEARNEY
  • Solid medicament form with active agent distributed in flat polymer fragments
    Patent number: 6333048
    Abstract: In a solid medicament form for the peroral application of active agents containing a uniform distribution of active agent in a polymer material, the polymer material is in the form of flat fragments.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: December 25, 2001
    Assignee: LTS Lohmann Therapie-Systeme GmbH
    Inventors: Bodo Asmussen, Walter Müller, Karsten Cremer
  • Sustained release medicinal compositions
    Patent number: 6328979
    Abstract: The present invention relates to sustained-release pharmaceutical compositions for ionic pharmaceutically active substances (excluding ionic prostanoic acid derivatives) containing ionic compounds having opposite charges to those of the active substances and increasing hydrophobicity of the active substances. More specifically, the invention relates to sustained-release pharmaceutical compositions comprising the ionic pharmaceutically active substances and the ionic compounds having opposite charges to those of the active substances and increasing hydrophobicity of the active substances that contain hydrophobic groups in the molecule thereof. The pharmaceutical composition of the invention can exhibit excellent sustained release effect of the active substance, irrespective of water solubility possessed by the ionic pharmaceutically active substances.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: December 11, 2001
    Assignee: Yamanouchi Pharmaceuticals, Co. Ltd.
    Inventors: Noboru Yamashita, Akira Takagi, Masataka Katsuma, Katsumi Saito, Yuuki Takaishi, Tatsuo Yasuda, Yutaka Takahashi, Mitsuo Mitomi
  • Delivery system to modulate immune response
    Patent number: 6328967
    Abstract: 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: Grant
    Filed: March 12, 1998
    Date of Patent: December 11, 2001
    Assignee: Allergenics, Inc.
    Inventor: Roberto L. Rivera
  • Combination of zinc ions and vitamin C and method of making
    Patent number: 6316008
    Abstract: Compositions for oral use containing at least one zinc compound, at least one amino acid, a source of ascorbic acid which does not appreciably associate with zinc ions, and a base material. The compositions provide for slow release of zinc upon dissolution in the mouth. The amino acid provides the zinc compound(s) with a palatable taste and no aftertaste. The source of ascorbic acid provides Vitamin C without interacting with zinc and forming unpalatable by-products. A method for making such compositions is also described.
    Type: Grant
    Filed: September 3, 1998
    Date of Patent: November 13, 2001
    Inventor: John C. Godfrey
  • Method for treatment of anxiety and depression
    Patent number: 6312717
    Abstract: An improved method of treatment for anxiety and/or depression provides a quicker and more robust anxiolytic/antidepressant activity to a patient suffering from depression. The method comprises the concurrent administration of effective doses of certain azapirones, such as buspirone, given in a manner that suppresses formation of the 1-(2-pyrimidinyl)piperazine metabolite; and a 5-HT1A autosomal receptor antagonist, such as pindolol.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: November 6, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: Perry B. Molinoff, Geoffrey C. Dunbar
  • Pharmaceutical preparation in form of coated capsule releasable at lower part of digestive tract
    Patent number: 6309666
    Abstract: A pharmaceutical preparation in the form of a coated capsule which can release contents of a capsule at a lower part of the digestive tract comprising (a) a hard capsule containing at least an acidic substance, (b) a polymer film soluble at low pH which is formed on a surface of said hard capsule, and (c) an enteric coating film which is formed on a surface of said polymer film soluble at low pH. According to the pharmaceutical preparation of the present invention, any kind of a medicament can be delivered to any desired site between the upper part of the small intestine and the lower part of the large intestine in the digestive tract by controlling the amount of polymer(s) used for the polymer film soluble at low pH and/or by selecting the kind of the polymer film soluble at low pH and/or the acidic substance without any complicated requirements for each medicament.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: October 30, 2001
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Harumi Hatano, Takahiro Ito, Takashi Ishibashi, Hiroyuki Yoshino, Masakazu Mizobe
  • MELT-EXTRUSION MULTIPARTICULATES
    Publication number: 20010033865
    Abstract: A unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.
    Type: Application
    Filed: July 22, 1999
    Publication date: October 25, 2001
    Inventors: BENJAMIN OSHLACK, HUA-PIN HUANG, MARK CHASIN
  • Pharmaceutical composition comprising cyclosporin solid-state microemulsion
    Patent number: 6306434
    Abstract: A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.
    Type: Grant
    Filed: June 1, 2000
    Date of Patent: October 23, 2001
    Assignee: Chong Kun Dang Corp.
    Inventors: Chung Il Hong, Jung Woo Kim, Nam Hee Choi, Hee Jong Shin, Su Geun Yang, Jae Hyun Kim, Jong Lae Lim, Chong Kook Kim
  • Enteric coated pharmaceutical compositions
    Patent number: 6306900
    Abstract: 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: Grant
    Filed: October 23, 2000
    Date of Patent: October 23, 2001
    Assignee: Novartis AG
    Inventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
  • Oral pharmaceutical preparation embedded in an oily matrix and methods of making the same
    Patent number: 6306435
    Abstract: The present invention relates to an oral pharmaceutical preparation which contains an acid or base labile pharmaceutical ingredient which is embedded in an oily matrix which is controlled at neutral pH. The oily matrix-embedded pharmaceutical ingredient is encapsulated and then being coated by an enteric coating. The enteric coating enables the pharmaceutical ingredient to reach the small intestine for absorption. The oily matrix has the advantages of avoiding acidic or basic conditions. It can also isolate moisture and oxygen so as to allow for greater absorption and bioavailability of the pharmaceutical ingredient in vivo.
    Type: Grant
    Filed: June 26, 2000
    Date of Patent: October 23, 2001
    Assignee: Yung Shin Pharmaceutical Industrial Co. Ltd.
    Inventors: Gan-Lin Chen, Wen-Yi Hsu
  • Sustained release oxycodone formulations with no fed/fast effect
    Publication number: 20010031278
    Abstract: A solid controlled release, oral dosage form, the dosage form comprising a therapeutically effective amount of oxycodone or a salt thereof together with a sustained release carrier which causes the formulation to preferentially release the drug in low pH (e.g., gastric fluid) is bioavailable and does not exhibit a fed/fast effect.
    Type: Application
    Filed: April 5, 2001
    Publication date: October 18, 2001
    Inventors: Benjamin Oshlack, Mark Chasin
  • Pharmaceutical product
    Patent number: 6303143
    Abstract: A substrate is roboticaly picked up at a station and transported to a measuring station to measure the distance to a reference. The substrate is aligned to a robot before measurement. The measured substrate is then transported to a pharmaceutical or diagnostic powder/grain deposition station where the powder/grains are controllably deposited on the substrate to predetermined thicknesses over a plurality of powder/grain collection zones. The deposited powder/grains are then measured to determine the thickness and area covered by the deposited powder/grains at each collection zone. The substrate is then transported to a lamination station and each collection zone of powder/grains is welded to a cover substrate. The system remembers which collection zones are out of specification so that they can be later selectively discarded.
    Type: Grant
    Filed: June 10, 1998
    Date of Patent: October 16, 2001
    Assignees: Sarnoff Corporation, Delsys Pharmaceutical Corporation
    Inventors: Suggy S. Chrai, Ramaswamy Murari, Eugene Samuel Poliniak, Hoi Cheong (Steve) Sun, Nitin Vithalbhai Desai, Dominic Stephen Rosati, Nalin Kumar, William Ronald Roach, Lawrence Harrison Hammer, Peter David Southgate, Bawa Singh, Howard Christopher Rivenburg, David Keller, Peter John Zanzucchi, Aaron William Levine, Prince Lal
  • Preparations with controlled release
    Patent number: 6303144
    Abstract: A controlled release preparation containing at least one kind of a pharmaceutically active ingredient, a male piece and a female piece, the pieces fitting together to enclose the active substance therein, wherein the male piece is made from a material that gels in the intestinal juice, is disclosed. In a preferable mode, the male piece contains an ethyl acrylate-methyl methacrylate-trimethylammonioethyl methacrylate chloride copolymer and a methacrylic acid-ethyl acrylate copolymer. In a preferable mode, the female piece is made from a water insoluble polymer. In a preferable mode, the dosage form is a tablet or a capsule.
    Type: Grant
    Filed: August 10, 2000
    Date of Patent: October 16, 2001
    Assignee: Welfide Corporation
    Inventor: Tomoyuki Omura
  • Controlled release lipoic acid
    Publication number: 20010028896
    Abstract: 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: Application
    Filed: January 5, 2001
    Publication date: October 11, 2001
    Inventor: Edward A. Byrd
  • Controlled release metformin formulations
    Publication number: 20010024659
    Abstract: Sustained release pharmaceutical formulations comprising an antihyperglycemic drug or a pharmaceutically acceptable salt thereof are disclosed. The formulations provide therapeutic plasma levels of the antihyperglycemic drug to a human patient over a 24 hour period after administration.
    Type: Application
    Filed: November 29, 2000
    Publication date: September 27, 2001
    Applicant: Andrx Corporation
    Inventors: Chih-Ming Chen, Xiu Xiu Cheng, Steve Jan, Joseph Chou
  • Orally administrable opioid formulations having extended duration of effect
    Patent number: 6294195
    Abstract: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: September 25, 2001
    Assignee: Purdue Pharma L.P.
    Inventors: Benjamin Oshlack, Mark Chasin
  • Slow-release matrix pellets and the production thereof
    Patent number: 6290990
    Abstract: Slow-release matrix pellets with a spherical or lenticular shape and uniform maximum diameters in the range from 0.5 to 4 mm, composed of a) 0.1-87% by weight of at least one biologically active compound, b) 5-50% by weight of at least one water-insoluble polymer, c) 5-45% by weight of at least one lipophilic component as plasticizer for polymer b), d) 3-40% by weight of a natural or semisynthetic gel former, e) 0-50% by weight of one or more conventional formulation aids.
    Type: Grant
    Filed: October 17, 1996
    Date of Patent: September 18, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Sven Grabowski, Joerg Rosenberg, Axel Sanner
  • PHARMACEUTICAL COMPOSITIONS COMPRISING MONOAMINE OXIDASE B INHIBITORS
    Publication number: 20010021722
    Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as an active ingredient, a monoamine oxidase B inhibitor, characterised in that the composition is formulated to promote pre-gastric absorption of said monoamine oxidase B inhibitor. A process for preparing such a composition and the use of such a composition for the treatment of Parkinson's disease, the treatment and/or prophylaxis of depression and the treatment and/or prophylaxis of Alzheimer's disease are also provided.
    Type: Application
    Filed: November 17, 1997
    Publication date: September 13, 2001
    Inventors: FRANCESCA, MARY BREWER, EDWARD STEWART JOHNSON, ANTHONY CLARKE
  • Process for producing sustained-release preparation by in-water drying
    Patent number: 6287587
    Abstract: The present invention is to provide sustained-release microcapsules which contains high amount of a drug, suppresses initial release and shows stable release, and the production method of which comprises adding a physiologically active substance to biodegradable polymer in an organic solvent containing a fat and oil (in particular, vitamin E) and dispersing and emulsifying the mixture.
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: September 11, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takada Shigeyuki, Taira Keiko, Iwasa Susumu
  • Stable shaped particles of crystalline organic compounds
    Patent number: 6287693
    Abstract: The present invention provides storage stable, shaped particles of allotropic organic compounds. The particles of the present invention can be shaped according to the desired application. Preferred shapes of such particles are microspheres, particularly those having diameters of about 1 to about 1,000 microns. The stable shaped particles of the present invention are particularly well-suited to the fabrication of pharmaceutical formulations, particularly where sustained release and uniform bioavailability are desired. The storage stable particles are formed by a solid state crystallization of allotropic organic compounds. The solid state crystallization process of the present invention affords a means for achieving a storage stable crystalline form of said allotropic compound without loss or deterioration of the original particle dimensions.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: September 11, 2001
    Inventors: John-Claude Savoir, Juan Angeles, Aurelio De Gyves, Abraham Gomez
  • Biomedical assay device
    Patent number: 6287595
    Abstract: The present invention provides an integrated structural unit that includes a diagnostic form that includes at least one active ingredient that is present in an amount that advantageously does not vary by more than about five percent from a predetermined target amount. In one embodiment, the unit form comprises a substrate, a deposit that is disposed on the substrate, and a spreading layer that overlies the deposit and is used to retain and spread a sample of liquid which is to be assayed. The deposit comprises a powder, including the active ingredient(s). The diagnostic form is created via a dry powder deposition apparatus that electrostatically deposits the powder on the substrate utilizing an electrostatic chuck and charged powder delivery apparatus.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: September 11, 2001
    Assignee: Delsys Pharmaceuticals Corporation
    Inventors: Zvi Loewy, Dennis Lee Matthies
  • Localized delivery of factors enhancing survival of transplanted cells
    Patent number: 6281015
    Abstract: Growth factors and/or angiogenic factors are administered in combination with dissociated cells to be transplanted, preferably in microspheres with the cells on or in a polymeric matrix, to enhance survival and proliferation of the transplanted cells. Examples demonstrate that epidermal growth factor (EGF) was incorporated into microspheres fabricated from a copolymer of lactic and glycolic acid using a double emulsion technique, the incorporated EGF was steadily released over one month in vitro, and it remained biologically active, as determined by its ability to stimulate DNA synthesis, division, and long-term survival of cultured hepatocytes. EGF-containing microspheres were mixed with a suspension of hepatocytes, seeded onto porous sponges, and implanted into the mesentery of two groups of Lewis rats, to demonstrate efficacy in vivo.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: August 28, 2001
    Assignees: Children's Medical Center Corp., Massachusetts Institute of Technology
    Inventors: David J. Mooney, Robert S. Langer, Joseph P. Vacanti
  • Extended release formulation of venlafaxine hydrochloride
    Patent number: 6274171
    Abstract: 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: Grant
    Filed: January 20, 2000
    Date of Patent: August 14, 2001
    Assignee: American Home Products Corporation
    Inventors: Deborah M. Sherman, John C. Clark, John U. Lamer, Steven A. White