Discrete Particles In Supporting Matrix Patents (Class 424/469)
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Publication number: 20020006438Abstract: 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: ApplicationFiled: September 25, 1998Publication date: January 17, 2002Inventors: BENJAMIN OSHLACK, MARK CHASIN, HUA-PIN HUANG
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Patent number: 6338857Abstract: The invention provides a sustained release composition free of food effect comprising: (c) a core comprising carbamazepine; and (d) a functional coating comprising, based on the weight of the coating, from 30 to 80% of a gastroresistant polymer and from 10 to 40% of a hydrophilic silicon dioxide. The invention also provides a method for alleviating food effect in a carbamazepine pharmaceutical composition.Type: GrantFiled: May 26, 2000Date of Patent: January 15, 2002Assignee: Pharma Pass LLCInventor: Pawan Seth
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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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Publication number: 20010048945Abstract: Pharmaceutical compositions that enable the release of a physiologically active substance over a prolonged period of time following administration to a patient are described. The pharmaceutical compositions are provided by encapsulation of a physiologically active substance into a matrix comprising biodegradable polymers and lipids. The rate of release of the physiologically active substance from the pharmaceutical composition is controlled by varying the ratio of the polymer to the lipid. The compositions can be stored in an aqueous suspension or as a solid dosage form. The physiologically active substances include small molecules, peptides, proteins, nucleic acids and vaccines. The biodegradable polymers include homopolymers, or random or block copolymers. The lipids include phospholipids, cholesterol and glycerides.Type: ApplicationFiled: May 17, 2001Publication date: December 6, 2001Applicant: SkyePharma, Inc., a California corporationInventor: Mantripragada Bhima Sankaram
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Publication number: 20010046980Abstract: The present invention relates to the field of cancer, and in particular hormone dependent cancers including, but not limited to prostate, breast, endometrial, ovarian, thyroid, bone, and testis. The present invention also relates to the use of steroid analogues, and in particular analogues of &Dgr;5-androstene-3-&bgr;, 17&agr;-diol, and its epimer &Dgr;5-androstene-3-&bgr;, 17&bgr;-diol for the treatment and prevention of cancer.Type: ApplicationFiled: February 26, 2001Publication date: November 29, 2001Inventor: Roger M. Loria
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Patent number: 6319518Abstract: A composition comprising gelatin and a polysaccharide which is degradable by a colonic enzyme and, optionally, with an aldehyde and/or a polyvalent metal ion and/or an additional polysaccharide, which is not degraded or disintegrated in the upper gastrointestinal tract, thereby rendering the active substance loaded therein to be selectively delivered to the colon and to be effectively released in the colon.Type: GrantFiled: August 29, 1997Date of Patent: November 20, 2001Assignee: Samyang CorporationInventors: Seung-Seo Lee, Sung-Bum La, Chang-Baeg Lim, Sujung Lee, Bo-Youn Seo, Chaul-Min Pai
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Patent number: 6306439Abstract: The present invention relates to administration forms having a relatively long gastric residence time, in the preparation of which mixtures of polymers containing lactam groups and polymers containing carboxyl groups are used, and which are distinguished both by marked swelling properties and by high dimensional stability in the swollen state.Type: GrantFiled: May 9, 1997Date of Patent: October 23, 2001Assignee: Bayer AktiengesellschaftInventors: Gunther Penners, Klemens Lustig, Jörg Petersen-von Gehr
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Patent number: 6306438Abstract: A stabilized sustained release oral solid dosage form which includes an effective amount of tramadol or a pharmaceutically acceptable salt thereof dispersed in a matrix of a hydrophobic material comprising a wax-like substance which was melted or softened during the preparation of the matrix, is cured at a temperature from about 35° C. to about 65° C. for a time period from about 4 to about 72 hours, such that the formulation, when subjected to in-vitro dissolution after exposure to accelerated storage conditions of at least one month at 40° C./75% RH, releases an amount of tramadol which does not vary at any given dissolution time point by more than about 20% of the total amount of tramadol released when compared to in-vitro dissolution conducted prior to subjecting the dosage form to the accelerated storage conditions.Type: GrantFiled: July 2, 1998Date of Patent: October 23, 2001Assignee: Euro-Celtique, S.A.Inventors: Benjamin Oshlack, Hua-Pin Huang, Mark Chasin, Paul Goldenheim
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Patent number: 6306427Abstract: The invention relates to a composition, in pellet form, useful for the nutritional and/or medicinal supplementation of ruminants and a method for admixing the pellets with foodstuff. The pellet contains granules of one or more active ingredients/principles protected against degradation in toe rumen and one or more binding agents capable of being solubilized, crosslinked or melted. Optionally, the pellet may also contain an unprotected active ingredient for release in the rumen. The pellet may further contain a disintegrating agent and/or filler.Type: GrantFiled: February 1, 1993Date of Patent: October 23, 2001Assignee: Rhone-Poulenc Nutrition AnimaleInventors: Claude Annonier, Pierre Autant, Jacques Ruel, Hugues Porte, Jean-Claude Laffay, Alain Sabatier
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Patent number: 6296842Abstract: The invention relates to a sustained release composition and methods of forming and using said composition for the sustained release of biologically active agent. The sustained release compositions of the invention comprise a biocompatible polymer and a biologically active agent characterized by a porous center and a less porous outer layer wherein the center and outer layer consist of essentially the same materials. The sustained release compositions can be prepared by annealing at least a substantial portion of the exterior surface of a polymer/active agent matrix. The compositions which have been annealed exhibit a decrease in the release of agent over the first 24 hours following administration (i.e., reduced burst) and as a result can show an increase in the duration of sustained release thereby providing increased therapeutic benefits.Type: GrantFiled: August 10, 2000Date of Patent: October 2, 2001Assignee: Alkermes Controlled Therapeutics, Inc.Inventors: Warren E. Jaworowicz, James I. Wright
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Patent number: 6296873Abstract: A zero-order sustained-release delivery system for delivery of carbamazepine or a derivative thereof. A polymeric matrix formulation of carbamazepine comprises hydrophilic polymer or hydrophilic/hydropholic polymer mixture which permits carbamazepine or carbamezepine derivative to be released from the polymer matrix in zero-order release kinetics.Type: GrantFiled: March 31, 2000Date of Patent: October 2, 2001Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Ifat Katzhendler, Michael Friedman
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Patent number: 6294201Abstract: This invention relates to an orally administered osmotic drug release system that consists of a shell and a core containing a pharmaceutically active substance, as well as a process for its production. The invention relates further to an osmotic drug release system for use as a drug in human beings and animals, as well as the use of the osmotic drug release system in the production of a drug for the treatment and/or prevention of illnesses in human beings and animals.Type: GrantFiled: April 25, 2000Date of Patent: September 25, 2001Assignee: Bayer AktiengesellschaftInventors: Stefan Kettelhoit, Ranga-Rao Kanikanti, Erich Brendel, Claus Weisemann, Ernst Chantraine, Michael Eisele, Patrick Bosché
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Patent number: 6287693Abstract: 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: GrantFiled: February 25, 1998Date of Patent: September 11, 2001Inventors: John-Claude Savoir, Juan Angeles, Aurelio De Gyves, Abraham Gomez
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Patent number: 6284273Abstract: The present invention is concerned with a solid slow release oral pharmaceutical dosage unit resistant to amylase which comprises a solid dosage unit made up of an admixture of a therapeutic dosage of an orally effective pharmaceutical product, an optional polysaccharide or polyol, and cross-linked high amylose starch, wherein the cross-linking of the high amylose starch has been carried out with a covalent or non-covalent cross-linking agent with from about 0.1 g to about 30 g of cross-linking agent per 100 g of high amylose starch.Type: GrantFiled: February 24, 1998Date of Patent: September 4, 2001Inventors: Vincent Lenaerts, Francois Chouinard, Mircea Alexandru Mateescu, Pompilia Ispas-Szabo
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Publication number: 20010018070Abstract: Drugs are formulated as unit oral dosage forms by incorporating them into polymeric matrices comprised of hydrophilic polymers that swell upon imbibition of water to a size that is large enough to promote retention of the dosage form in the stomach during the fed mode. The oral formulation is designed for gastric retention and controlled delivery of an incorporated drug into the gastric cavity, and thus administered, the drug is released from the matrix into the gastric fluid by solution diffusion. The swollen polymeric matrix, having achieved sufficient size, remains in the gastric cavity for several hours if administered while the patient is in the fed mode, and remains intact long enough for substantially all of the drug to be released before substantial dissolution of the matrix occurs. The swelling matrix lowers the accessibility of the gastric fluid to the drug and thereby reduces the drug release rate.Type: ApplicationFiled: March 29, 1999Publication date: August 30, 2001Inventors: JOHN W. SHELL, JENNY LOUIE-HELM, MICHELINE MARKEY
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Patent number: 6280771Abstract: Dosage forms prepared by solid free form fabrication (SFF) provide release of medicament in multiple phases.Type: GrantFiled: February 20, 1998Date of Patent: August 28, 2001Assignees: Therics, Inc., Massachusetts Institute of TechnologyInventors: Donald Monkhouse, Jaedeok Yoo, Jill K. Sherwood, Michael J. Cima, Esteban Bornancini
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Patent number: 6277405Abstract: The invention provides a micronized fenofibrate composition. The micronized fenofibrate composition has a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or with 0.025M sodium lauryl sulfate. The composition can further comprise hydrophilic polymers, surfactants, hydrosoluble carriers, outer phases or layers, or other pharmaceutically acceptable excipients. The immediate-release fenofibrate composition is preferably in the form of a tablet or in the form of granules inside a capsule.Type: GrantFiled: May 18, 2000Date of Patent: August 21, 2001Assignee: Labaratoires Fournier, S.A.Inventors: André Stamm, Pawan Seth
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Patent number: 6277406Abstract: The invention deals with the use of low temperature and low humidity conditions during the storage and shaping of “flash-dose” tablet compositions. The compositions may be rendered substantially non-amorphous before tablet formation.Type: GrantFiled: October 8, 1997Date of Patent: August 21, 2001Assignee: Fuisz Technologies Ltd.Inventors: Richard C. Fuisz, Tushar K. Misra, Pradeepkumar P. Sanghvi
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Patent number: 6274174Abstract: The present inventors have made studies for the purpose of establishing a process for preparing controlled-release preparations which can rapidly release 99% or more of a slightly soluble medicament (which has by itself shows a slow dissolution rate) in the upper part of the small intestine. As a result, the inventors have succeeded in establishing a process comprising carrying a slightly soluble medicament which has a slow intestinal dissolution rate on aggregates of the spherical microparticles of a multivalent metal alginate, in which each of the secondary particles (i.e., the aggregates) has a specific surface area ranging from 1 to 280 m2/g. This success leads to the accomplishment of the present invention.Type: GrantFiled: June 30, 1999Date of Patent: August 14, 2001Assignees: Nisshinbo Industries, Inc., Freund Industrial Co., Ltd.Inventors: Takeshi Hom-ma, Nagayoshi Myo, Takaya Sato, Hironobu Nanbu
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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: 6267986Abstract: This invention relates to a process for the preparation of a controlled release pharmaceutical composition comprising two discrete zones wherein the first discrete zone comprises therapeutically effective amount of pseudoephedrine or its pharmaceutically acceptable salt as active ingredient and the second discrete zone comprises a therapeutically effective amount of a long-acting antihistamine selected from the group consisting of loratadine, azatidine, fexofenadine, terfenadine, cetirizine, astemizole, and levocabastine, or their pharmaceutically acceptable salt as active ingredient.Type: GrantFiled: September 24, 1999Date of Patent: July 31, 2001Assignee: Ranbaxy Laboratories LimitedInventors: Girish Kumar Jain, Ashok Rampal, Himadri Sen
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Publication number: 20010008640Abstract: The present invention provides a bilayer structure for encapsulating multiple containment units. These containment units can attach or contain therapeutic or diagnostic agents that can be released through the bilayer structure. A suitable example of such a containment unit is a unilamellar or multilamellar vesicle.Type: ApplicationFiled: February 8, 2001Publication date: July 19, 2001Applicant: The Regents of the University of CaliforniaInventors: Joseph A. Zasadzinski, Scott Walker, Michael Kennedy
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Patent number: 6261601Abstract: A pharmaceutical composition in the form of tablets or capsules provides a combination of temporal and spatial control of drug delivery to a patient for effective therapeutic results. The pharmaceutical composition comprises a drug, a gas generating component, a swelling agent, a viscolyzing agent, and optionally a gel forming polymer. The swelling agent belongs to a class of compounds known as superdisintegrants (e.g., cross-linked polyvinylpyrrolidone or sodium carboxymethylcellulose). The viscolyzing agent initially and the gel forming polymer thereafter form a hydrated gel matrix which entraps the gas, causing the tablet or capsule to be retained in the stomach or upper part of the small intestine (spatial control). At the same time, the hydrated gel matrix creates a tortuous diffusion path for the drug, resulting in sustained release of the drug (temporal control). A preferred once daily ciprofloxacin formulation comprises 69.9% ciprofloxacin base, 0.34% sodium alginate, 1.03% xanthan gum, 13.Type: GrantFiled: September 14, 1998Date of Patent: July 17, 2001Assignee: Ranbaxy Laboratories LimitedInventors: Naresh Talwar, Himadri Sen, John N. Staniforth
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Patent number: 6251431Abstract: A biodegradable insect repellant that breaks down in the presence of water to minimize solid waste, comprising a water soluble substrate substantially comprising foamed vegetable starch, and cedar oil carried in the substrate. The substrate is preferably made of corn and or potato starch. The cedar oil may be from about 0.01 to about 10 times the weight of the substrate. A coloring agent may optionally be provided in the cedar oil to impart color to the insect repellant. Because the substrate is made from a water soluble starch, it dissolves in water leaving little or no solid waste.Type: GrantFiled: June 1, 1993Date of Patent: June 26, 2001Assignee: Chemia CorporationInventor: Norman A. Van Rees
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Patent number: 6248359Abstract: The present invention provides a simple multi-tablet system for the treatment of urinary incontinence with oxybutynin. Particular embodiments of the invention provide a first tablet that releases oxybutynin over a short period of time, e.g. less than six hours, and a second tablet that releases oxybutynin over an extended period of time, e.g., eighteen to twenty-four hours, to maintain therapeutically effective levels oxybutynin in the mammal for a period of about twenty four hours. Unlike other systems, this system is easily adaptable to compensate for patient to patient variability in response to oxybutynin therapy. The invention also provides a method of treating urinary incontinence with the above system and a kit comprising various first and second tablets to rapidly develop a patient's preferred dosing regimen, i.e., the dosing regimen which provides the greatest therapeutic benefit and/or least amount or severity of side effects.Type: GrantFiled: January 5, 2000Date of Patent: June 19, 2001Assignee: Laboratorios Phoenix U.S.A., Inc.Inventor: Joaquina Faour
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Patent number: 6248358Abstract: A bioadhesive tablet wherein the active ingredient may be protected from water or the surrounding environment, thereby protecting it from metabolism or from other degradation caused by moisture, enzymes, or pH effects, and making it bioavailable only at a controlled rate. The active ingredient may be protected from moisture during the manufacturing process and more importantly may be protected from moisture and the immediate septic environment until after the patient has applied the tablet, and then only at a slow and controlled rate. It is by this process of progressive hydration that the active ingredient remains protected for many hours after administration. It is also by the process of progressive hydration that controlled and sustained release is achieved because only that part of the active ingredient that is the hydrated (aqueous) fraction of the tablet is available for absorption (bioavailable).Type: GrantFiled: August 23, 1999Date of Patent: June 19, 2001Assignee: Columbia Laboratories, Inc.Inventors: William J. Bologna, Howard L. Levine, Philippe Cartier, Dominique de Ziegler
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Patent number: 6238697Abstract: Methods and formulations for making extended release bupropion hydrochloride tablets using direct compression, and tablets formed thereby, are provided which combine bupropion hydrochloride, binders such as polyethylene oxide or hydroxypropyl cellulose, a filler such as lactose, glidants and lubricants under low shear conditions to form hard, chip-resistant tablets which exhibit improved cohesiveness and are easily and reproducibly formed without adhering to the compression punches and dies.Type: GrantFiled: December 21, 1998Date of Patent: May 29, 2001Assignee: Pharmalogix, Inc.Inventors: Vijai Kumar, Kevin Scott McGuffy
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Patent number: 6238698Abstract: An oral preparation, comprising at least one pharmaceutical active compound in a matrix which is swellable in aqueous medium, which is released from the matrix into the aqueous medium in a delayed manner on swelling thereof, while the matrix is largely resistant to disintegration during the release process, it is characterized in that it is a layered tablet with layers adhering to one another, of which at least one layer is the swellable matrix layer and at least another layer is an auxiliary and/or excipient layer, and in that the swellable matrix layer contains an amount of crosslinked amylose.Type: GrantFiled: July 27, 1999Date of Patent: May 29, 2001Assignee: LTS Lohmann Therapie-Systeme GmbHInventor: Karsten Cremer
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Patent number: 6228398Abstract: The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component compnsimg a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition.Type: GrantFiled: May 8, 2000Date of Patent: May 8, 2001Assignee: Elan Corporation, PLCInventors: John G. Devane, Paul Stark, Niall M. M. Fanning
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Patent number: 6221392Abstract: The invention is directed to a hard tablet that can be stored, packaged and processed in bulk. Yet the tablet dissolves rapidly in the mouth of the patient with a minimum of grit. The tablet is created from an active ingredient mixed into a matrix of a nondirect compression filler and a relatively high lubricant content.Type: GrantFiled: December 16, 1999Date of Patent: April 24, 2001Assignee: Cima Labs Inc.Inventors: Rajendra K. Khankari, John Hontz, Sara J. Chastain, Leo Katzner
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Patent number: 6221393Abstract: The present invention relates to a delayed-release pharmaceutical composition which is in the form of tablets prepared by direct tableting and consisting of at least one active principle and a matrix which gives the said composition its delayed-release effect, characterized in that the said matrix consists at least in part of pregranulated polysaccharides of high molecular weight and of synthetic or natural origin.Type: GrantFiled: October 22, 1999Date of Patent: April 24, 2001Assignee: Rhodia ChimieInventors: Jean-Pierre Collaueri, Guillaume Conrath, Paul-Joël Derian, Gabriel Gousset, Frédéric Mauger
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Patent number: 6210714Abstract: A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.Type: GrantFiled: February 14, 2000Date of Patent: April 3, 2001Assignee: Euro-Celtique S.A.Inventors: Benjamin Oshlack, Mark Chasin
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Patent number: 6207188Abstract: This invention relates to a novel form of the sodium salt of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole, known under the generic name omeprazole sodium salt. This invention also relates to processes for its preparation of omeprazole sodium form B which is thermodynamically stable, as well as pharmaceutical compositions containing it and its use in the treatment of gastrointestinal disorders.Type: GrantFiled: June 29, 1998Date of Patent: March 27, 2001Assignee: AstraZeneca ABInventors: Anders Gustavsson, Kristina Kjellbom, Ingvar Ymén
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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: 6203817Abstract: Transdermal compositions, devices, and methods for the administration of a drug at reduced skin irritation levels are disclosed. More particularly, this invention relates to novel methods, compositions, and devices for the reduction or elimination of irritation or sensitization caused by an irritating or sensitizing drug when it is delivered transdermally. According to a preferred embodiment, transdermal administration of a drug salt of a non-zwitterionic drug is disclosed wherein the drug salt comprises a combination of surface activity and a low octanol-water partition coefficient. Such drug salts have been found to reduce irritation or sensitization to the drug being delivered while achieving therapeutically effective transdermal fluxes.Type: GrantFiled: June 5, 1998Date of Patent: March 20, 2001Assignee: ALZA CorporationInventors: Michel J. N. Cormier, Peter E. Daddona, Juanita A. Johnson
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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: 6194005Abstract: The invention concerns a method for preparing a modified release of active principle. The method comprises the steps of mixing a powder composed of active principle, adjuvant or combinations thereof while heating and fluidizing in order to obtain individual grains, liquefying a lipid matrix agent composed of partial esters of alcohol with at least one fatty acid, coating the powder by spraying from 1 to 15% by weight of the final composition liquid lipid matrix agent over the individual grains, the spraying air pressure, and optionally the spraying rate varying throughout the coating operation and lowering the temperature of the combined product to allow the lipid matrix agent to solidify around the grains.Type: GrantFiled: March 23, 1999Date of Patent: February 27, 2001Assignee: Gattefosse, S.A.Inventors: Nabil Farah, Philippe Barthelemy, Joseph Joachim
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Patent number: 6190697Abstract: The effervescent formulation elation in the form of granules or of a tablet contains, in addition to the effervescent base, at least one water-soluble or at least suspendable plant extract whose particles are coated with at least one oily, fatty or waxy substance. At least one emulsifier and/or at least one antifoam may be present in the coating and/or as a further component of the mixture, in particular applied as a further component of the mixture to a pharmaceutically permissible filler as carrier. The individual phases are prepared by a procedure in which the plant extract or the filler is heated—preferably in a granulator, in particular in a vacuum granulator—and wet or mixed with a melt or solution of the oily, fatty or waxy substance or at least one emulsifier and/or at least one antifoam and then dried—preferably in a vacuum—and sieved to the desired particle size.Type: GrantFiled: October 26, 1998Date of Patent: February 20, 2001Inventors: Gerhard Gergely, Irmgard Gergely, Thomas Gergely, Stefan Gergely
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Patent number: 6187339Abstract: The invention concerns a solid pharmaceutical composition comprising less than 7% by weight of an oil or oily substance, a low dosage active ingredient, and a water insoluble non-cross-linked polymeric excipient capable of binding water and having a mean particle size greater than 150 &mgr;m. The composition can be obtained by a simple procedure comprising mixing the water insoluble non-cross-linked polymeric excipient capable of binding water and the active ingredient, which is dissolved or dispersed in an oil or an oily substance, in an aqueous dispersion thereof, or in water.Type: GrantFiled: October 17, 1995Date of Patent: February 13, 2001Assignee: Akzo Nobel N.V.Inventors: Pieter de Haan, Henrika Gerardina Maria Poels-Janssen
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Oral pharmaceutical dosage forms comprising a proton pump inhibitor and an antacid agent or alginate
Patent number: 6183776Abstract: An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more antacid agents or an alginate in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer and an optional separating layer in between the proton pump inhibitor and the enteric coating. The fixed formulation is in the form of multilayered tablets, sachets or multiple unit tableted dosage forms. The multiple unit dosage form is most preferred. The new fixed formulation is especially useful in the treatment of disorders associated with dyspepsia such as heartburn.Type: GrantFiled: February 13, 1997Date of Patent: February 6, 2001Assignee: Astra AktiebolagInventors: Helene Depui, Agneta Hallgren -
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: 6165512Abstract: The invention relates to compositions useful for making taste-masked oral dosage forms which can be easily processed and which disintegrate rapidly when placed in the mouth. The compositions include coated liquiflash particles and shearform floss particles. Tablets are preferred dosage forms.Type: GrantFiled: October 30, 1998Date of Patent: December 26, 2000Assignee: Fuisz Technologies Ltd.Inventors: Djelila Mezaache, Michael G. Raiden, Pradeepkumar P. Sanghvi, Scott J. Szedlock
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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: 6162466Abstract: The present invention provides a pharmaceutical preparation in tablet form, where the active ingredient is an anti-epileptic medication, preferably a sustained release formulation, and most preferably a sustained release formulation where the active ingredient is carbamazepine. The product consists of carbamazepine particles coated with a single hydrophobic layer and is in a disintegrating tablet form.Type: GrantFiled: April 15, 1999Date of Patent: December 19, 2000Assignee: Taro Pharmaceutical Industries Ltd.Inventors: Daniela Licht, Marina Zholkoysky, Roman Kaplan, Michael Friedman, Abraham Yacobi, Yechiel Golander, Dan Moros, Barrie Levitt
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Patent number: 6162465Abstract: The invention relates to a method for the determination of dose-level characteristics, such as physicochemical properties, functionality and/or quality, of a multiple unit system comprising a plurality of individual subunits (12). A number of said subunits (12) are individually analysed for obtaining precise characteristics for each individually analysed subunit (12). Said dose-level characteristics of the multiple unit system are determined based the thus-obtained precise characteristics for each individually analysed subunit (12). The invention also relates to an industrial process in which this method is used, and to the use of the claimed method in a process for designing a multiple unit system formulation product.Type: GrantFiled: June 30, 1998Date of Patent: December 19, 2000Assignee: Astra AktiebolagInventors: Staffan Folestad, Johan Gottfries, Arne Torstensson, Gunnar Zackrisson, Goran Ostling
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Patent number: 6156339Abstract: This invention relates to a process for the preparation of an oral solid rapidly disintegrating dosage form of a pharmaceutically active substance which has an unacceptable taste which process comprises: (i) forming a solution or a suspension in a solvent of a water soluble or water dispersible carrier, a filler and the pharmaceutically active substance with the unacceptable taste in association with a lipid, the weight ratio of the pharmaceutically active substance to the lipid being in the range of from 1:1 to 1:10 and the weight ratio of the carrier to the lipid being in the range of from 5:1 to 1:15; (ii) forming discrete units of the suspension or solution; and (iii) removing the solvent from the discrete units under conditions whereby unit dosages are formed comprising a network of carrier/filler carrying a dosage of the pharmaceutically active substance in association with the lipid; oral solid rapidly disintegrating dosage forms prepared by such a process are also provided.Type: GrantFiled: August 10, 1999Date of Patent: December 5, 2000Assignee: R.P. Scherer CorporationInventors: Leon Grother, Michael Hall, Douglas Bryans, Richard Green, Patrick Kearney
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Patent number: 6149943Abstract: The present invention provides a core of predominately microcrystalline cellulose, on which an active drug is layered onto the core via solution coating. The coated particles have a narrower particle size distribution than coated granules provided by other processes. An optional final coating of a pharmaceutically acceptable polymeric coating is provided to provide tastemaking or controlled release, and protection of the drug-layered particles.Type: GrantFiled: November 2, 1999Date of Patent: November 21, 2000Assignee: McNeil-PPC, Inc.Inventors: Daniel McTeigue, Indukumar G. Shah, Karen Swider, David W. Wynn
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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: 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: 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