Sustained Or Differential Release Patents (Class 424/457)
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Patent number: 6270787Abstract: An osmotic delivery system has a membrane plug retention mechanism which can also be used to control the delivery rate of a beneficial agent from the osmotic delivery system. The osmotic delivery device includes an implant capsule containing a beneficial agent and an osmotic agent. Holes are formed along a side wall of the implant capsule at an open end of the capsule. When the membrane plug is inserted into the open end of the capsule the membrane material swells into the holes in the capsule side wall creating a large frictional force which prevents expulsion of the membrane plug. A beneficial agent delivery rate of the osmotic delivery system is controllable by varying the size and number of the holes to change the amount of exposed surface area of the membrane plug. An increase in the surface area of the membrane plug exposed to the exterior environment causes a corresponding increase in the liquid permeation rate of the membrane and thus, increases the beneficial agent delivery rate.Type: GrantFiled: December 22, 1998Date of Patent: August 7, 2001Assignee: ALZA CorporationInventor: Rupal Ayer
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Patent number: 6270795Abstract: A method of making a microparticle that contains DNA coding for a polypeptide is described in which a solvent extraction method is used and solvent extraction takes place at elevated temperature. Oral administration of the microparticle leads to its expression. DNA coding for an immunogen is for stimulating antibody formation in a recipient and DNA coding for a non-immunogenic polypeptide is for gene therapy applications. DNA is incorporated into the microparticle without destruction of its function.Type: GrantFiled: May 15, 1998Date of Patent: August 7, 2001Assignee: Microbiological Research AuthorityInventors: David Hugh Jones, Graham Henry Farrar, James Christopher Stephen Clegg
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Patent number: 6270796Abstract: A prefilled, unifying dispensing container of at least two different medication dosage units comprising a regimen for the treatment of rhinitis, indicia for distinguishing the dosage units, and coordinating instructions. The medications may be contained in bottles, blister packages, or pouches. Medications include antihistamine and nasal decongestant. One dosage is for administration when sedation is not desired and the other is for administration when stimulation is not desired.Type: GrantFiled: October 29, 1998Date of Patent: August 7, 2001Inventor: Robert E. Weinstein
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Patent number: 6270797Abstract: One aspect of the invention resides in a monolithic sustained release composition of glipizide for patients with non-insulin dependent diabetes mellitus that exhibits a breakdown after ingestion by a patient in conformity with a zero-order kinetic. The present invention provides a composition of a glipizide and a hydrocolloid forming agent and optimally other auxiliary excipients for the sustained release of glipizide. It is preferable that the hydrophilic material comprises at least 50% by weight of the composition. The present invention is also directed to the process for producing the composition. One aspect of this process includes the steps of granulating glipizide, a hydrophilic material and a diluent, drying the granulated product and lubricating the product with a flow regulating agent and lubricant.Type: GrantFiled: May 18, 2000Date of Patent: August 7, 2001Assignee: USV LimitedInventors: Suresh Kumar Gidwani, Purushottam Singnurkar, Prashant Kumar Tewari
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Patent number: 6267969Abstract: Unit-of-use reagent compositions and methods for preparing such reagent compositions are disclosed. The reagent composition comprises one or more reagents which are necessary for a specific binding assay and which are incorporated in a porous material which is encapsulated in a carrier matrix. The unit-of-use reagent composition can be lyophilized to avoid the need for cold storage of the reagent composition.Type: GrantFiled: June 21, 1994Date of Patent: July 31, 2001Assignee: Abbott LaboratoriesInventor: Sharon M. Devereaux
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Patent number: 6264941Abstract: This invention provides improved devices and methods for long-term, stable expression of a biologically active molecule using a biocompatible capsule containing genetically engineered cells for the effective delivery of biologically active molecules to effect or enhance a biological function within a mammalian host. The novel capsules of this invention are biocompatible and are easily retrievable. This invention specifically provides improved methods and compositions which utilize cells transfected with recombinant DNA molecules comprising DNA sequences coding for biologically active molecules operatively linked to promoters that are not subject to down regulation in vivo upon implantation into a mammalian host. Furthermore, the methods of this invention allow for the long-term, stable and efficacious delivery of biologically active molecules from living cells to specific sites within a given mammal.Type: GrantFiled: January 25, 1999Date of Patent: July 24, 2001Assignee: Neurotech S.A.Inventors: Edward E. Baetge, Joseph P. Hammang, Frank T. Gentile, Mark D. Lindner, Shelley R. Winn, Dwaine F. Emerich
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Publication number: 20010008638Abstract: The present invention relates to an oral dosage delivery form which is effective in increasing the testosterone levels in humans. In a preferred embodiment, the composition comprises a mixture of four (4) prohormones, three (3) anti-estrogen agents and at least one (1) enteric coating. The inventive prohormone/anti-estrogen time-release dosage form allows the prohormone/anti-estrogen ingredients to be released over an extended period of time so as to provide for a sustained elevated blood serum testosterone level.Type: ApplicationFiled: July 14, 1999Publication date: July 19, 2001Inventor: BRIAN J. WILDING
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Patent number: 6261599Abstract: Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques disclosed.Type: GrantFiled: July 23, 1999Date of Patent: July 17, 2001Assignee: Euro-Celtique, S.A.Inventors: Benjamin Oshlack, Mark Chasin, Hua-Pin Huang, David Sackler
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Patent number: 6254889Abstract: The present invention relates to a solid dispersion and a solid dispersion dosage form which comprise a xanthine derivative represented by the following formula (I) or a pharmacologically allowable salt thereof and a polymer. (In the above formula, R1 and R2 are the same or different, and represent substituted or unsubstituted lower alkyl groups, and Q represents a hydrogen atom or a hydroxyl group.Type: GrantFiled: March 26, 1997Date of Patent: July 3, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Makoto Kigoshi, Tomoaki Masada, Yasuhiko Ueno, Yasuhiro Ishikawa, Eiji Hayakawa
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Patent number: 6254882Abstract: A method and composition are disclosed utilizing the pure (S) isomer of salmeterol which is a potent bronchodilator with reduced adverse effects, having a better selectivity for &bgr;2 receptors than the corresponding R enantiomer or the racemate.Type: GrantFiled: September 16, 1997Date of Patent: July 3, 2001Assignee: Sepracor Inc.Inventor: Thomas P. Jerussi
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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: 6251427Abstract: A pharmaceutical capsule composition for oral administration exhibiting controllable, satisfactory release profiles of both loratadine and pseudoephedrine or its salts, which comprises: (a) a plurality of rapid-release pellets (pellets A), each pellet containing (i) a therapeutically effective amount of loratadine, (ii) pseudoephedrine or a pharmaceutically acceptable salt thereof, and (iii) one or more pharmaceutically acceptable excipients; and (b) a plurality of extended-release pellets (pellets B), each pellet containing (i) pseudoephedrine or a pharmaceutically acceptable salt thereof and (ii) one or more pharmaceutically acceptable excipients, which are coated with a water-insoluble polymer in an amount ranging from 2 to 30 wt % and a wet-blocking agent selected from the group consisting of magnesium stearate, talc, fatty acid ester and a mixture thereof in an amount ranging from 2 to 30 wt %, based on the total weight of pellets B.Type: GrantFiled: February 22, 2000Date of Patent: June 26, 2001Assignee: Yuhan CorporationInventors: Hyun-Soo Kim, Young-Joon Park, Hang-Bum Jo
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Patent number: 6251434Abstract: Preparations of non-steroidal analgesics with antipyretic and antiinflammatory effect are obtainable by extrusion and shaping of a melt, comprising, besides one or more active ingredients, a mixture of a) 40-99.5% by weight of a homopolymer of N-vinylpyrrolidone with a Fikentscher K value of 30, b) 0.25-59.75% by weight of a water-soluble copolymer of N-vinylpyrrolidone, and c) 0.25-10% by weight of one or more physiologically acceptable salts of sodium or potassium, where the stated amounts are based on the total of components a), b) and c).Type: GrantFiled: July 15, 1998Date of Patent: June 26, 2001Assignee: BASF AktiengesellschaftInventors: Jörg Breitenbach, Joerg Rosenberg
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Patent number: 6248363Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.Type: GrantFiled: November 23, 1999Date of Patent: June 19, 2001Assignee: Lipocine, Inc.Inventors: Mahesh V. Patel, Feng-Jing Chen
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Patent number: 6235302Abstract: The present invention relates to a regenerated cellulose based sponge material with an inner viscose fiber reinforcement having a staple fiber length of 5-50 mm and impregnated with a biocide agent. Also disclosed is a regenerated cellulose based sponge material with an inner cotton fiber reinforcement having a staple fiber length of 5-50 mm and impregnated with a biocide agent. The coagulation and regeneration takes place in a bath that has a pH of 13 or higher and which includes Glauber's salt, NaOH and water.Type: GrantFiled: March 31, 1999Date of Patent: May 22, 2001Assignee: Kalle Nalo GmbH & Co. KGInventors: Leo Mans, Klaus-Dieter Hammer
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Patent number: 6228395Abstract: 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: GrantFiled: November 25, 1998Date of Patent: May 8, 2001Assignee: Laboratories des Produits Ethiques EthypharmInventors: Patrice DeBregeas, Gérard LeDuc, Pascal Oury, Pascal Suplie
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Patent number: 6221333Abstract: 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: GrantFiled: February 1, 1999Date of Patent: April 24, 2001Assignee: The Curators of the University of MissouriInventors: Delbert E. Day, James E. White
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Patent number: 6221390Abstract: A novel pharmaceutical combination is described, together with a method of making the same and a method of treating hypertensive patients using the same, wherein (1) the pharmaceutically active antihypertensive agent and citric acid and (2) the pharmaceutically active antikaliuretic agent and a nonionic surfactant are mixed, either together or separately, to form an essentially homogenous combination composition, and only thereafter blending with excipients to form the novel combination composition in solid dosage form.Type: GrantFiled: August 25, 1997Date of Patent: April 24, 2001Assignee: Barr Laboratories, Inc.Inventors: Salah U. Ahmed, Gandha Naringrekar
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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: 6214381Abstract: A pharmaceutical composition useful for treating ocular conditions, such as glaucoma. In particular, the pharmaceutical composition is a sustained release oral dosage composition for relieving intraocular pressure comprising methazolamide and a high molecular weight binder, wherein the composition provides sustained rate of methazolamide release in an in vitro drug release profile. A filler and a lubricant may also be included.Type: GrantFiled: September 8, 1998Date of Patent: April 10, 2001Assignee: Effcon, Inc.Inventors: Eddie R. Burklow, Jeffrey S. Kiel, Jeffrey H. Ping
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Patent number: 6211393Abstract: Silicon compound of general formula a), in which A, B, C, D are radicals which are different from OH and are covalently bonded to Si; two or three of these bond that are linked to Si are Si—O—C, Si—S—C or Si—N—C type bonds and are hydrolyzable in vivo, forming Si—OH bonds that are biologically active especially when in contact with living tissue, the A and D bonds of formula b) being invariably hydrolyzable; at least one of the hydrolyzable bonds corresponds to an acyloxy, aryloxy or vinyloxy radical; at least one of the compounds obtained after hydrolysis of the hydrolyzable bonds is a stabilizer, and the non-hydrolyzable bonds, which are of the Si—C type, correspond to hydrocarbon or fluorocarbon radicals for which Si is not directly linked to the phenyl ring.Type: GrantFiled: July 22, 1996Date of Patent: April 3, 2001Assignee: Exsymol S.A.M.Inventors: Marie Christine Seguin, Jean Gueyne, Jean-Francois Nicolay, Andre Franco
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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: 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: 6200600Abstract: Novel devices for the controlled release of active materials especially pharmaceuticals comprise a capsule formed from two separable pieces at least part of the capsule walls is water permeable. The capsule contains a water sensitive material which on contact with water causes the two pieces to separate. In the preferred embodiment the devices comprise a generally cylindrical tube closed at one or both ends by a water swellable plug. The devices find particular application as oral dosage forms for use in man.Type: GrantFiled: December 15, 1994Date of Patent: March 13, 2001Assignee: BTG International LimitedInventor: Abdul Rashid
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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: 6197340Abstract: A controlled release formulation of lipoic acid is disclosed. The lipoic acid is combined with excipient materials in such a way that those materials protect the lipoic acid from chemical degradation in the gastrointestinal tract and provide for gradual release of the lipoic acid. These combined 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 results.Type: GrantFiled: April 8, 1999Date of Patent: March 6, 2001Assignee: Medical Research InstituteInventors: Edward A. Byrd, Rajiv Janjikhel
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Patent number: 6194000Abstract: Disclosed is a method for the therapeutic treatment of pain related to wind up in a human or animal. The method of the invention is practiced by administering to the subject an effective amount of an analgesic pharmaceutical composition which includes a NMDA receptor antagonist in an immediate release form combined with an NMDA receptor antagonist in a sustained release form. The immediate release form and sustained release forn are present in sufficient amounts to diminsh or abolish wind up.Type: GrantFiled: April 17, 1998Date of Patent: February 27, 2001Assignee: F.H. Faulding & Co., LimitedInventors: Ian Keith Smith, Grant Wayne Heinicke
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Patent number: 6190702Abstract: A sustained-release preparation containing a bioactive polypeptide is prepared using a starting material containing a lyophilized product of an aqueous solution or suspension of the bioactive polypeptide in a non-ionic surfactant. The lyophilized product is dispersed in an oil phase, which further contains a biocompatible, biodegradable polymer.Type: GrantFiled: May 30, 1997Date of Patent: February 20, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigeyuki Takada, Tomofumi Kurokawa, Susumu Iwasa
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Patent number: 6187338Abstract: The analgesic effectiveness of tramadol is significantly enhanced by administering tramadol prior to, with or following the administration of an analgesia enhancer which is a nontoxic NMDA receptor blocker and/or a nontoxic substance that blocks at least one major intracellular consequence of NMDA receptor activation.Type: GrantFiled: February 22, 1999Date of Patent: February 13, 2001Assignee: Algos Pharmaceutical CorporationInventors: Frank S. Caruso, Fredrick L. Minn, John W. Lyle
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Patent number: 6183779Abstract: A pharmaceutical composition is provided for the oral administration of an NSAID and a prostaglandin. The composition is a solid dosage form wherein the NSAID is enterically coated and the prostaglandin is present along with an effective stabilizing amount of a prostaglandin stabilizing agent such as hydroxypropyl methylcellulose or polyvinylpyrrolidone. Exemplary dosage forms are bilayer tablets in which the prostaglandin is misoprostol and the NSAID is diclofenac, piroxicam, or a pharmaceutically acceptable salt thereof. Methods for using the composition to treat NSAID-responsive conditions, disorders and diseases are provided as well.Type: GrantFiled: March 22, 1999Date of Patent: February 6, 2001Assignee: Pharmascience Inc.Inventors: Aomar Ouali, Abul Kalam Azad
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Patent number: 6183780Abstract: The invention relates to an Oral Delayed Immediate Release formulation comprising a compressed core containing one or more active substances surrounded with a coating, wherein release of active substance from the core is caused by rupture of the coating after a definite lag-time, said core comprising one or more immediate release carriers and having no substantial swelling properties upon exposure to gastrointestinal fluids. The invention further relates to formulations containing an Immediate Release formulation combined with one or more Oral Delayed Immediate Release formulations with different lag-times and to a method of preparing an Oral Delayed Immediate Release formulation.Type: GrantFiled: September 19, 1997Date of Patent: February 6, 2001Assignee: Duphar International Research B.V.Inventors: Paulus M. Van Balken, Jules A. C. Elbers, Henderik W. Frijlink, Wienman E. Philips
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Patent number: 6174873Abstract: Disclosed are compositions including an adenosine analog, wherein the composition comprises a dosage form suitable for oral (co)administration. Also disclosed are compositions including adenosine analogs, wherein the composition is in a dosage form including a pill, capsule, lozenge, or tablet, and compositions including adenosine analogs, wherein the composition is in a dosage form comprising a liquid. Additionally disclosed are methods of administering the inventive composition, and kits including the inventive compositions.Type: GrantFiled: November 4, 1998Date of Patent: January 16, 2001Assignee: SuperGen, Inc.Inventor: Simeon M. Wrenn, Jr.
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Patent number: 6174547Abstract: A dosage form is disclosed comprising a drug formulation that self-emulsifies in said dosage form.Type: GrantFiled: July 14, 1999Date of Patent: January 16, 2001Assignee: ALZA CorporationInventors: Liang-Chang Dong, Steven Espinal, Patrick S. L. Wong
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Patent number: 6171615Abstract: A stable sustained release theophylline formulation is prepared by incorporating theophylline into a semi-solid matrix comprising polyglycolized glycerides (GELUCIRE® excipient) and a mixture of nucleation enhancers. Theophylline is admixed with molten GELUCIRE to make the sustained release formulation. The nucleation enhancer composition is then incorporated in the admixture to make the sustained release formulation resistant to changes in dissolution upon aging. Orally administrable compositions are prepared by filling gelatin capsules with the formulation. The polyglycolized glycerides (GELUCIRE) and the nucleation enhancer composition also can be used as an excipient system for preparing sustained release pharmaceutical compositions.Type: GrantFiled: July 6, 1998Date of Patent: January 9, 2001Assignees: Gattefoss{acute over (e)}, SmithKline Beecham Corp.Inventors: Pascale Roussin, Sarma Duddu
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Patent number: 6172250Abstract: A process for the preparation of biologically active silicon compounds by hydrolysis of a precursor which produces a compound which prevents the formation of polymers from the silicon hydrolyzed bonds.Type: GrantFiled: July 16, 1996Date of Patent: January 9, 2001Assignee: Exsymol S.A.M.Inventors: Marie-Christine Seguin, Jean Gueyne, Jean-Francois Nicolay, Andre Franco
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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: 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: 6165503Abstract: In the formation of capsules having a polyanionic polysaccharide core and a polycationic polysaccharide membrane layer, improved binding of the polycationic polysaccharide is achieved by including polyvalent ions, especially calcium ions, at the membrane forming step.Type: GrantFiled: July 1, 1998Date of Patent: December 26, 2000Assignee: FMC Biopolymer A.S.Inventors: Olav G.ang.ser.o slashed.d, .O slashed.ivind Skaugrud, Peter Dettmar, Gudmund Sj.ang.k-Braek, Ian Jolliffe
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Patent number: 6162463Abstract: An extended release formulation of diltiazem which is suitable for once-daily oral administration comprises a quantity of a quick release preparation of diltiazem or a pharmaceutically active salt thereof, mixed with a quantity of a slow release (or delayed release) preparation of diltiazem or a pharmaceutically active salt thereof. The quick release preparation used obtains a maximal release of diltiazem within approximately 1-2 hours after administration, and then falls toward baseline levels. The delayed release preparation individually shows a maximal release of diltiazem at between approximately 6-8 hours after administration.Type: GrantFiled: April 28, 1998Date of Patent: December 19, 2000Inventor: Arnold S. Lippa
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Patent number: 6162467Abstract: A process for the manufacture of particles comprises mechanically working a mixture of a drug and a hydrophobic and/or hydrophilic fusible carrier in a high speed mixture so as to form agglomerates, breaking the agglomerates to give controlled release particles and optionally continuing the mechanical working with the optional addition of a low percentage of the carrier or diluent.Type: GrantFiled: August 9, 1999Date of Patent: December 19, 2000Assignee: Euro-Celtique, S.A.Inventors: Ronald Brown Miller, Stewart Thomas Leslie, Sandra Therese Antoinette Malkowska, Derek Allan Prater, Trevor John Knott, Joanne Heafield, Deborah Challis
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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: 6143328Abstract: Sustained release pharmaceutical formulations containing morphine, or a pharmaceutically acceptable salt thereof, as active ingredient, suitable for administration on a once daily basis, are disclosed. In a first aspect, an orally administrable sustained release unit dosage form gives a peak plasma level at 1.0 to 6 hours after administration. In a second aspect, the formulation provides a W.sub.50 for the M-6-G metabolite for morphine of between 4 and 12 hours. A third aspect concerns the pharmaceutical unit dosage form obtained by compressing multiparticulates comprising a pharmaceutically active substance in a matrix of hydrophobic fusible material having a melting point of from 35 to 150.degree. C.Type: GrantFiled: March 8, 1999Date of Patent: November 7, 2000Assignee: Euro-Celtique, S.A.Inventors: Joanne Heafield, Trevor John Knott, Stewart Thomas Leslie, Sandra Therese Antoinette Malkowska, Ronald Brown Miller, Derek Allan Prater, Kevin John Smith
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Patent number: 6136327Abstract: Preferential delivery via electrotransport of a preferred isomeric form of a pharmaceutically active chiral compound from a mixture of the isomeric forms of said compound is provided. A method of decreasing the delivery via electrotransport of a less preferred isomer of a drug is also provided. Drug delivery devices suitable for such preferential delivery and methods of making the same are also provided.Type: GrantFiled: December 1, 1997Date of Patent: October 24, 2000Assignee: ALZA CorporationInventors: Suneel K. Gupta, Gayatri Sathyan, Rama Padmanabhan
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Patent number: 6132768Abstract: An oral pharmaceutical composition of a reversible proton pump inhibitor in pellet or tablet form, wherein the reversible proton pump inhibitor is at least partly in slow-release form, is distinguished, on combined administration with an antimicrobially-active ingredient, by an enhanced action of rapid onset against disorders caused by Helicobacter.Type: GrantFiled: July 5, 1995Date of Patent: October 17, 2000Assignee: BYK Gulden Lomberg Chemische Fabrik GmbHInventors: George Sachs, Rango Dietrich
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Patent number: 6117450Abstract: The method of making a solid drug with controlled effective ingredient delivery for oral administration includes selecting a predetermined number of at least three of four compressed compositions containing an effective ingredient or effective ingredient combination defined by their release profile of effective ingredient and/or effective ingredient combination. The solid drug or medicinal preparation is formed according to known methods requiring only comparatively small apparatus expense and minimal time. Perorally administered solid drugs are made by this process which can provide widely varying pharmaceutically-required release profiles of effective ingredients or effective ingredient combinations, for example delayed release, uniformly maintained release or pulsatile release adjusted to fit a special rhythm.Type: GrantFiled: April 24, 1998Date of Patent: September 12, 2000Assignee: JENAPHARM GmbH & Co. KGInventors: Michael Dittgen, Sabine Fricke, Carsten Timpe, Hagen Gerecke, Annette Eichardt
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Patent number: 6113935Abstract: A suspension of microcapsules in an organic liquid, the microcapsules containing an aqueous phase, is produced by interfacial polymerization in the presence of a proton transfer catalyst of a water-in-oil emulsion in which the aqueous phase contains a urea/formaldehyde or melamine/formaldehyde prepolymer.Type: GrantFiled: December 19, 1997Date of Patent: September 5, 2000Assignee: ZENECA LimitedInventors: Maurius Rodson, Herbert B. Scher
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Patent number: 6113943Abstract: 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: GrantFiled: October 31, 1997Date of Patent: September 5, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Okada, Yayoi Douken
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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: 6103264Abstract: A process for preparing a controlled release composition with a controlled release matrix and containing a pharmaceutically active ingredient, which comprises granulating the active ingredient with a molten matrix material or with a matrix material while it is being melted and with optional additional inactive materials at a first elevated temperature, then cooling and screening the granulate, forming a fluidized bed of the resulting material at a second elevated temperature, and recovering the resulting product; and the product formed by the process.Type: GrantFiled: July 7, 1998Date of Patent: August 15, 2000Assignee: Arzneimittelwerk Dresden GmbHInventors: Torsten Hoffmann, Klaus Liebold, Joachim Wolf, Heiko Schumacher