Discrete Particles In Supporting Matrix Patents (Class 424/469)
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Patent number: 6524618Abstract: An extended-release matrx formulation capable of being directly compressed into tablets comprising metformin hydrochloride blended with specific excipients. The excipients used in the formulation enhance the flow and compaction properties of the drug and insure that the formulation is directly compressible into a tablet containing about 100 mg to about 800 mg, preferably about 250 mg to about 750 mg, of metformin hydrochloride in unit dosage form. Each tablet produced by direct compression of the formulaton has the desired hardness and dissolution characteristics such that the drug is released in the body of the subject over an extended period of time.Type: GrantFiled: June 12, 2001Date of Patent: February 25, 2003Inventors: Vijai Kumar, Kevin Scott McGuffy
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Publication number: 20030035838Abstract: Microparticles and nanoparticles prepared from oppositely charged polymers are provided in which a drug is incorporated into the core and is conjugated to one polymer by a Schiff-base crosslink. The particles are suitable for use in injectable formulations in which the rate of release of the drug through the particle shell is slowed as compared to noncrosslinked drugs. Enzymatically degradable polymers can be incorporated in otherwise hydrolytically stable particles to provide drug release at particular sites within the body where the enzyme of interest is present.Type: ApplicationFiled: September 27, 2002Publication date: February 20, 2003Applicant: NanoDelivery, Inc.Inventor: Ales Prokop
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Patent number: 6521261Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.Type: GrantFiled: October 16, 2001Date of Patent: February 18, 2003Assignee: Edward Mendell Co., Inc.Inventors: Bob E. Sherwood, John H. Staniforth, Edward A. Hunter
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Patent number: 6517866Abstract: Sustained release dosage forms of sertraline which release sertraline at a rate between 1 mgA/hr and 40 mgA/hr. The dosage forms may exhibit an initial delay period during which sertraline is released at a rate less than 1 mgA/hr.Type: GrantFiled: September 7, 1999Date of Patent: February 11, 2003Assignee: Pfizer Inc.Inventors: Mary Tanya Am Ende, William John Curatolo, Hylar Lewis Friedman, Dwayne Thomas Friesen, Scott Max Herbig, Ravi Mysore Shankar, James Blair West
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Patent number: 6517868Abstract: Disclosed herein is a tableted oral extended release dosage form comprising a plurality of granules of an effective amount of a pharmaceutically active compound, at least one amino acid, and an intragranular polymer in which the granule is dispersed within a hydrophilic extragranular polymer matrix which is more rapidly hydrating than the intragranular polymer. The amino acid is selected for hydropathy characteristics depending on solubility characteristics of the active compound.Type: GrantFiled: November 30, 2001Date of Patent: February 11, 2003Inventors: A. Reza Fassihi, Thomas Dürig
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Publication number: 20030026839Abstract: 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: ApplicationFiled: January 2, 2002Publication date: February 6, 2003Applicant: Euro-Celtique S.A.Inventors: Benjamin Oshlack, Mark Chasin, Hua-Pin Huang
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Patent number: 6514531Abstract: The present invention relates to controlled-release dosage forms of zolpidem or salts thereof adapted to release zolpidem over a predetermined time period, according to a biphasic profile of dissolution, where the first phase is an immediate release phase and the second phase is a prolonged release phase and particular embodiments thereof intended to avoid abuse.Type: GrantFiled: July 16, 2001Date of Patent: February 4, 2003Assignee: Sanofi-SynthelaboInventors: Gérard Alaux, Gareth Lewis, Frédéric Andre
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Patent number: 6500457Abstract: Novel pharmaceutical dosage forms provide for pulsatile delivery of an antiarrhythmic agent that releases the drug in spaced apart “pulses.” The dosage forms are comprised of first, second and optional 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, granules, or particles or may comprise a single tablet with the first, second and optional third dosage units incorporated therein, or a “coated core” dosage form. Methods of treatment using the pharmaceutical dosage forms are provided as well.Type: GrantFiled: August 14, 2000Date of Patent: December 31, 2002Assignee: Peirce Management, LLCInventors: Kamal K. Midha, Mark Hirsh, Whe-Yong Lo
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Patent number: 6492488Abstract: A method for forming polyacrylic acid granules and granules prepared therefrom, wherein the granules are flowable, have comparable swelling characteristics and provide comparable tablet properties to powdered polyacrylic acid, have increased bulk density and contain minimal amounts of very small particles that can cause dusting and static adherence. The granules are used to prepare controlled-release tablets, especially for pharmaceutical purposes. The tablets prepared from granules obtained by the method of present invention have superior controlled release properties.Type: GrantFiled: June 10, 1999Date of Patent: December 10, 2002Assignee: PMD Holdings Corp.Inventors: Daniel James Adams, David William Weaver
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Patent number: 6488962Abstract: The retention of oral drug dosage forms in the stomach is improved by using swellable dosage forms that are shaped in a manner that will prevent them from inadvertently passing through the pylorus as a result of being in a particular orientation. The planar projection of the shape is one that has two orthogonal axes of different lengths, the longer being short enough to permit easy swallowing prior to swelling while the shorter is long enough within one-half hour of swelling to prevent passage through the pylorus.Type: GrantFiled: June 20, 2000Date of Patent: December 3, 2002Assignee: DepoMed, Inc.Inventors: Bret Berner, Jenny Louie-Helm
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Publication number: 20020176888Abstract: A controlled-release oral dosage formulation of a salt-forming active ingredient, wherein the active ingredient is present as at least two different salts in a solid aggregation state, wherein the two different salts have different water solubility and release the active ingredient in-vitro at different release rates, provided that oral dosage formulations are excluded which comprise a resin carrying a sulfonate group and a resin carrying a carboxyl group and which contain an active ingredient in a form fixed to these resins.Type: ApplicationFiled: February 28, 2002Publication date: November 28, 2002Inventors: Johannes Bartholomaeus, Iris Ziegler
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Patent number: 6485759Abstract: Botanical Combination therapies for treating AIDS and immune-deficient patients include therapeutically effective doses of five medicinal plants of Thailand. First combination, ayurvedic composition 1, consists of ground and spray-dried plant extracts Houttuynia cordata, Combretum quadrangulare, Mimusops elengi, Randia siamensis, and Borassus flabellifer in the varied amount. Drug mixture is administered one capsule twice daily. Second combination therapy consists of ayurvedic composition 1 (one capsule twice daily) plus one capsule of ayurvedic composition 2 twice daily. Ayurvedic composition 2 is powder of Houttuynia cordata extract in varied amounts. Ayurvedic composition 3 consists of dried extracts of five plant materials in fixed amounts. Ayurvedic composition 4 is dried extract of Houttuynia cordata 100 mg.Type: GrantFiled: July 12, 2001Date of Patent: November 26, 2002Assignee: The Government Pharmaceutical Organization Research and Development InstituteInventors: Kim Chantara, Krisana Kraisintu
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Patent number: 6485743Abstract: The present invention relates to a method and composition of an oral preparation of itraconazole, an excellent azole antifungal drug. More particularly, it relates to an oral preparation of itraconazole having improved bioavailability, which is prepared by following steps of: i) dissolving itraconazole and bydrophilic polymer with solvent, ii) spray-drying said mixture, and iii) preparing the solid dispersions for oral preparation. The solid dispersions prepared in this invention may be useful in preparing tablets, granules and other oral dosage forms.Type: GrantFiled: June 29, 2000Date of Patent: November 26, 2002Assignee: Choongwae Pharma CorporationInventors: Jae-Young Jung, Kye-Hyun Kim, Sang-Heon Lee, Ji-Woong Hong, Jong-Woo Park, Kyu-Hyun Lee
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Patent number: 6482434Abstract: A method for reducing certain effects associated with a negative calorie balance in a human includes the step of administering conjugated linoleic acid to a human in an amount effective to reduce at least one of the effects.Type: GrantFiled: April 4, 2000Date of Patent: November 19, 2002Assignee: Wisconsin Alumni Research FoundationInventors: Michael W. Pariza, Richard L. Atkinson, Jr.
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Publication number: 20020168338Abstract: Devices useful in the delivery of DNA encoding neurotrophic agents, anti-fibrotic agents, and related compositions are disclosed herein for use in the treatment of central and/or peripheral nervous system injury. Methods of making and using the disclosed devices and DNA are also described. In various embodiments, the invention also discloses compositions and devices that may further include a targeting agent, such as a polypeptide that is reactive with an FGF receptor (e.g., bFGF), or another ligand that binds to cell surface receptors on neuronal cells, or a support cell. The invention also discloses methods of promoting neuronal survival and regeneration via transfection of an axon as it grows through a device or composition of the present invention, or via transfection of a repair cell.Type: ApplicationFiled: October 23, 1998Publication date: November 14, 2002Inventor: ANDREW BAIRD
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Publication number: 20020164372Abstract: The present invention relates to controlled release delivery of biologically active molecules from a solid composition prepared by exposure of the molecules to an organic compound. For instance, the organic compound is an organic solvent, such as an alcohol (e.g., preferably a lower alcohol, such as methanol, ethanol, isopropanol, n-propanol, n-butanol, isobutanol, t-butanol, etc.), a mixture of alcohols, an aldehyde, a ketone, a hydrocarbon (saturated or unsaturated), or an aromatic hydrocarbon. The solvent can be a mixture of different organic solvents, or the resulting formulation can be a mixture of, e.g., different lyophilized preparations, such as may be used to control the release profile of the resulting admixture.Type: ApplicationFiled: December 31, 2001Publication date: November 7, 2002Inventor: Sidney Pestka
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Publication number: 20020164373Abstract: A solid, oral, controlled release dosage form comprising a therapeutically effective amount of an opioid compound, or a salt thereof, a matrix-forming polymer and an ionic exchange resin.Type: ApplicationFiled: February 27, 2002Publication date: November 7, 2002Inventor: Ann M. Maloney
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Patent number: 6475521Abstract: A biphasic controlled release delivery system for pharmaceuticals which have high water solubility, such as the antidiabetic metformin HCl salt, is provided which provides a dosage form that has prolonged gastric residence so that a dosing regimen of at least one gram metformin, once daily, may be achieved while providing effective control of plasma glucose.Type: GrantFiled: September 16, 1999Date of Patent: November 5, 2002Assignee: Bristol-Myers Squibb Co.Inventors: Peter Timmins, Andrew B. Dennis, Kiren A. Vyas
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Publication number: 20020160046Abstract: The present invention provides a time-release dosage form for delivering an acid-labile pharmaceutical, such as omeprazole, into the upper portion of the gastrointestinal tract downstream of the stomach. The dosage form includes a drug-containing core surrounded by an inert time-release coating that delays release of the drug from the core until expiration of a certain time period after administration, generally 0.5-5.0 hours or 1-3 hours. When the gastrointestinal fluid contacts the core, the drug is released rapidly into the GI tract. The dosage form does not contain an enteric coating. The dosage form can also include one or more additional coatings exterior to the time-release coating to provide delivery of an immediately released loading dose of the acid-labile drug or another drug.Type: ApplicationFiled: November 21, 2001Publication date: October 31, 2002Inventors: Joseph R. Robinson, James W. McGinity
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Patent number: 6468959Abstract: There is provided a plural dosage form for peptide pharmaceuticals comprising a matrix of gelatin or gelatin derivative having distributed therein the peptide pharmaceutical in particular insulin, as well as, pharmaceutically conventional carriers and additives. By selection of the appropriate gelatin the pharmaceutical is liberated in the small intestine or the large intestine so that is not enzymatically degraded anymore by peptidases.Type: GrantFiled: April 5, 1994Date of Patent: October 22, 2002Assignee: ALFATEC-Pharm GmbHInventors: Jens-Christian Wunderlich, Ursula Schick, Jurgen Freidenreich, Jurgen Werry
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Patent number: 6468976Abstract: The present invention relates to a novel monohydrate form of 1-(N2-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl)-L-proline known under the generic name lisinopril. Further, the present invention also relates to the use of the novel monohydrate form of lisinopril for the treatment of hypertension and other cardiovascular diseases, pharmaceutical compositions containing it as well as processes for the preparation of the novel monohydrate form of lisinopril.Type: GrantFiled: September 10, 2001Date of Patent: October 22, 2002Assignee: AstraZeneca ABInventor: John Brown
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Patent number: 6462022Abstract: The present invention relates to a pharmaceutical composition comprising lisinopril and dibasic calcium phosphate dihydrate (DCPD), produced by a process comprising mixing lisinopril and DCPD with a specific surface area of less than 1.5 m2g−1. The use of large particle sized DCPD in a lisinopril formulation/composition has the effect of reducing the amount of the lisinopril degradation product DKP that is formed, thereby increasing the shelf-life of tablets formulated with the larger sized DCPD, particularly those with low doses of lisinopril.Type: GrantFiled: September 24, 2001Date of Patent: October 8, 2002Assignee: AstraZeneca ABInventors: Ronald John Roberts, David Brandon Bowen
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Publication number: 20020132002Abstract: A sustained release pharmaceutical formulation is disclosed. The formulation comprises a water soluble medicament and a polymer mixture comprising a first component of about 80 weight percent polyvinylacetate combined with about 20 weight percent polyvinyl pyrrolidone, of the total weight of the first component, combined with a second component of a cellulose ether polymer.Type: ApplicationFiled: February 27, 2002Publication date: September 19, 2002Inventors: Jose Gutierrez-Rocca, Saul Rios
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Patent number: 6451345Abstract: The present invention provides taste-masked microcapsules of Linezolid or the like (any member of the orally effective oxazolidinone or macrolide antibiotics), suitable for oral administration as a suspension, a fast-disintegrating, effervescent or chewable tablet, and more specifically relates to such oral dosage forms in which the bitter taste of Linezolid contained therein is masked by a combination of microencapsulation by solvent coacervation and subsequent functional membrane coating on said microcapsules. The taste-masked granules thus obtained release less than 5%, most preferably less than 3%, at a pH of 4.0 to 6.0 (pH of the saliva) but rapidly release (as a burst) at pHs of the upper intestinal tract. The taste-masked granules are optionally blended with other pharmaceutically acceptable excipients and filled into unit dose containers or compressed into fast-disintegrating/effervescent/chewable tablets.Type: GrantFiled: February 17, 2000Date of Patent: September 17, 2002Assignee: Eurand Pharmaceuticals Ltd.Inventors: Phillip J. Percel, Krishna S. Vishnupad, Gopi M. Venkatesh
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Publication number: 20020119194Abstract: The invention relates to pharmaceutical forms for oral administration in the form of tablets, film-coated tablets, pellets or granules comprising at least 88% of mesna, produced by granulation with up to 15% of water, based on the amount of solid employed, and also tablets, film-coated tablets, pellets or granules comprising at least 80% of mesna, produced by direct compression or compaction. without the use of organic solvents.Type: ApplicationFiled: October 19, 2001Publication date: August 29, 2002Inventors: Jurgen Rawert, Werner Sarlikiotis
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Publication number: 20020110590Abstract: Preparations comprising a capsule, tablet or other dosage form containing a core of different types of DFMO are provided. These preparations are capable of providing for the direct and constant delivery of DFMO to the entire GI tract or just the colon and rectum. The DFMO-containing granules include granules specially formulated to achieve rapid DFMO release, and granules formulated to achieve slower DFMO release and/or granules formulated for gastric, enteric or colorectal release. Methods of using the preparations to flood the GI tract with relatively constant levels of DFMO may thus be provided. The ratio of the (+) to the (−)-enantiomeric forms of DFMO in the granules will be controlled so as to enhance the pharmacological profile and reduce toxicity of the preparation relative to racemic DFMO. Preparations and methods for achieving systemic delivery as well as direct colon delivery of DFMO are also described.Type: ApplicationFiled: August 10, 2001Publication date: August 15, 2002Applicant: Ilex Oncology, Inc.Inventors: Ze?apos;ev Shaked, James McGinity
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Publication number: 20020102300Abstract: A solid, oral, controlled release pharmaceutical dosage form comprising a pharmaceutically active ingredient having a solubility in water of greater than 1 gm in 250 ml water at 25° C., the active ingredient dispersed in a matrix wherein the dosage form provides, as tested by the Ph. Eur. Basket method at 100 rpm 900 ml aqueous buffer (pH 6.5) containing 0.05% w/w Polysorbate 80 at 37° C., an essentially zero order rate of release of the pharmaceutically active ingredient over a period of 8 hours, the amount of pharmaceutically active ingredient released over eight hours being in the range of 15% to 45%, and when tested in a group of at least five healthy humans the median tmax, based on blood sampling at half hourly intervals, is in the range of from about 2.5 to about 6 hours, and the ratio of mean Cmax to the mean plasma level at 24 hours is in the range of about 1.5 to about 3.5.Type: ApplicationFiled: February 5, 2002Publication date: August 1, 2002Inventors: Ronald Brown Miller, Stewart Thomas Leslie, Sandra Theresc Antoinette Malkowska, Derek Allan Prater, Trevor John Knott, Hassan Mohammad
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Publication number: 20020098232Abstract: Novel pharmaceutical dosage forms provide for pulsatile delivery of an antiarrhythmic agent that releases the drug in spaced apart “pulses.” The dosage forms are comprised of first, second and optional 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, granules, or particles or may comprise a single tablet with the first, second and optional third dosage units incorporated therein, or a “coated core” dosage form. Methods of treatment using the pharmaceutical dosage forms are provided as well.Type: ApplicationFiled: August 14, 2001Publication date: July 25, 2002Inventors: Kamal K. Midha, Mark Hirsh, Whe-Yong Lo
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Patent number: 6419960Abstract: The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.Type: GrantFiled: December 16, 1999Date of Patent: July 16, 2002Assignee: Euro-Celtique S.A.Inventors: Thinnayam N. Krishnamurthy, Andrew Darke
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Patent number: 6419952Abstract: A dosage form comprising a gelatin capsule formed with a composite wall and containing a liquid, active agent formulation where the wall comprises a barrier layer formed over the external surface of the gelatin capsule, an expandable layer formed over the barrier layer and a semipermeable layer formed over the expandable layer is described. The dosage forms and methods provide for the conversion of standard gelatin, liquid formulation capsules into controlled, release dosage forms that permit the controlled release of the active agent into the environment of use over time.Type: GrantFiled: May 25, 2001Date of Patent: July 16, 2002Assignee: Alza CorporationInventors: Patrick S. -L. Wong, Liang C. Dong, Jiansheng Wan
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Patent number: 6414050Abstract: Compositions comprising an admixture of a biofunctional polymer substrate and a biofunctional material substrate adapted for use in or in association with the human or animal body, cultivated or uncultivated living matter and methods for making and using thereof are disclosed. The biofunctional material substrate retains bioactivity in the admixture. As disclosed, the compositions may be made by a process which comprises contacting a mixture of the substrates or their precursors with a supercritical fluid under supercritical conditions of reduced viscosity to plasticise and swell the biofunctional polymer substrate and under conditions of physical blending to distribute the biofunctional material substrate throughout the biofunctional polymer substrate, and releasing the supercritical fluid under subcritical conditions. Also disclosed are biofunctional polymer matrices and methods of making and using thereof.Type: GrantFiled: January 10, 2000Date of Patent: July 2, 2002Assignee: University of NottinghamInventors: Steven Melvyn Howdle, Vladimir Popov
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Publication number: 20020076438Abstract: A high drug load spheronized beadlet is provided wherein said beadlet comprises about 80% to 100% by weight of an acid labile medicament, preferably didanosine, about 0% to about 10% by weight of a disintegrant, and about 0% to about 10% by weight of a binder selected from the group consisting of sodium carboxymethylcellulose, hydroxypropylmethylcellulose, potassium alginate, and partially pregelatinized corn starch. A high drug load pharmaceutical composition, comprising the beadlet, with an enteric coating disposed thereon, is also provided.Type: ApplicationFiled: November 16, 2001Publication date: June 20, 2002Inventors: Ismat Ullah, Gary J. Wiley
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Patent number: 6399096Abstract: A solid, oral controlled release pharmaceutical dosage form has a water-soluble active ingredient dispersed in a matrix and releases the active ingredient at such a rate upon administration that the median tmax is 2.5 to 6 hours and the ratio of mean Cmax to mean plasma level of the active ingredient at 24 hours is in the range of 1.5 to 3.5.Type: GrantFiled: July 27, 1998Date of Patent: June 4, 2002Assignee: Euro-Celtique S.A.Inventors: Ronald Brown Miller, Stewart Thomas Leslie, Sandra Therese Antoinette Malkowska, Derek Allan Prater, Trevor John Knott, Hassan Mohammad
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Patent number: 6399100Abstract: Controlled release oral pharmaceutical preparations are provided which comprise a therapeutically effective amount of tiagabine or a pharmaceutically acceptable salt thereof dispersed in a rate controlling polymeric matrix comprising at least one rate controlling polymer. The preparation can be formulated into oral dosage forms such as tablets or multiparticulates which provide therapeutically effective plasma levels of tiagabine for a period of at least 12 hours, preferably 24 hours or more. The preparation can provide tiagabine mean plasma concentrations equal to or greater than 50% of the maximum plasma concentration for at least 10 hours, preferably 14 hours, most preferably 16 hours or more.Type: GrantFiled: July 31, 1998Date of Patent: June 4, 2002Assignee: Elan Corporation, plcInventors: Maurice Joseph Anthony Clancy, Kenneth Iain Cumming, Michelle Caulfield
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Patent number: 6391338Abstract: The present invention is a method of preparing a system for delivering a bio-affecting agent and the composition prepared thereby. The invention includes forming a molecular dispersion of the bio-affecting agent in an increased energy state in a water-soluble polymer which is compatible with the bio-affecting agent. As a consequence of transforming the bio-affecting agent to an increased-energy condition and freezing it in such condition in a water-soluble polymer, the bio-affecting agent is made available (“bio-available”) to a bio-system upon dissolution of the polymer. This method and composition has been found extremely effective for delivery of otherwise substantially non-soluble drugs and other bio-affecting ingredients.Type: GrantFiled: August 21, 1998Date of Patent: May 21, 2002Assignee: Biovail Technologies Ltd.Inventors: Steven E. Frisbee, Garry L. Myers, Richard C. Fuisz, Andrea S. Blake, Robert K. Yang
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Publication number: 20020054907Abstract: 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 comprising 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: ApplicationFiled: May 7, 2001Publication date: May 9, 2002Inventors: John G. Devane, Paul Stark, Niall M. M. Fanning
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Publication number: 20020044968Abstract: Controlled release, discrete, solid particles which contain an encapsulated and/or embedded component such as a heat sensitive or readily oxidizable pharmaceutically, biologically, or nutritionally active component are continuously produced without substantial destruction of the matrix material or encapsulant. A release-rate controlling component is incorporated into the matrix to control the rate of release of the encapsulant from the particles. The additional component may be a hydrophobic component or a high water binding capacity component for extending the release time. The plasticizable matrix material, such as starch, is admixed with at least one plasticizer, such as water, and at least one release-rate controlling component under low shear mixing conditions to plasticize the plasticizable material without substantially destroying the at least one plasticizable material and to obtain a substantially homogeneous plasticized mass.Type: ApplicationFiled: February 13, 2001Publication date: April 18, 2002Applicant: General Mills, Inc.Inventor: Bernhard H. van Lengerich
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Patent number: 6372255Abstract: A multi-layer tablet for the instant and prolonged release of active substances comprises at least two layers where the first outer layer comprises a mixture of excipients and an active substance, allowing for the immediate release of the active substance within the first layer, and a second layer, arranged in contact with the first layer. The second layer comprises a nonbiodegradable inert porous polymeric matrix in which an active substance is dispersed, allowing for the prolonged release of the active substance within the second layer.Type: GrantFiled: June 21, 2000Date of Patent: April 16, 2002Assignee: Merck Patent GesellschaftInventors: Olivier Saslawski, Laurence Orlando
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Patent number: 6365185Abstract: The present invention relates to tablets which are time-controlled to release active agent at different rates in different regions of the digestive tract in order to maintain a substantially constant concentration in the blood. In one embodiment, a new modified release drug delivery system, for once a day peroral use, consisting of a solid core comprising an active agent together with a hydrogel, with the solid core being coated with a semi-permeable, self-destructing membrane which is optionally drilled to provide a release orifice, and then optionally further coated with the same or different active agent material. The device delivers the active agent in a substantially constant effective dose for the duration of the transit through the stomach and small intestine, followed by accelerated release when reaching the large intestine.Type: GrantFiled: March 26, 1999Date of Patent: April 2, 2002Assignee: University of CincinnatiInventors: Wolfgang A. Ritschel, Mukul A. Agrawal
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Patent number: 6365184Abstract: An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more NSAIDs in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of an enteric coating layered tablet, a capsule or a multiple unit tableted dosage form. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of gastrointestinal side-effects associated with NSAID treatment.Type: GrantFiled: December 23, 1999Date of Patent: April 2, 2002Assignee: AstraZeneca ABInventors: Helene Depui, Per Lundberg
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Patent number: 6365180Abstract: The present invention relates to novel, liquid and semi-solid pharmaceutical compositions which can be administered in liquid form or can be used for preparing capsules containing such pharmaceutical compositions. Also provided are methods of using and processes for preparing the pharmaceutical compositions of the present invention.Type: GrantFiled: July 16, 1999Date of Patent: April 2, 2002Inventors: Glenn A. Meyer, Laura A. Trespidi, Edward S. Wilson, Christy M. Clark, Ashok J. Desai, Frederick D. Sancilio
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Patent number: 6358533Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.Type: GrantFiled: January 4, 2001Date of Patent: March 19, 2002Assignee: Edward Mendell, Co., Inc.Inventors: Bob E. Sherwood, John H. Staniforth, Edward A. Hunter
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Patent number: 6358531Abstract: A method is provided for preparing shells, concentric shells or porous, homogenous gels from alkali borate glass particles at low temperatures (i.e. room temperature or less than above 100° C.). The alkali borate glass particles contain one or more cations such as aluminum which react with an aqueous solution containing an anion such as hydroxide to form an aqueous insoluble material having a solubility limit of less than about 0.01 wt. percent. The resulting shells or gels may be used in many different applications such as a filler in resins, as filters, precursors for nano-sized powders, as thin surface films or catalyst support media. The resulting shells or gels may also have a chemotherapeutic drug added thereto, following which the resulting product is administered to a mammal and the insoluble material is dissolved form the product in vivo through administration of chelating agent.Type: GrantFiled: February 1, 1999Date of Patent: March 19, 2002Assignee: The Curators of the University of MissouriInventors: Delbert E. Day, Samuel D. Conzone
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Publication number: 20020031550Abstract: A controlled release formulation of an acetonitrile compound and its use in the treatment and/or prophylaxis of certain disorders.Type: ApplicationFiled: September 19, 2001Publication date: March 14, 2002Applicant: SmithKline Beecham Corporation and SmithKline Beecham p.l.c.Inventors: Joseph Peter Sauer, Susan Marie Milosovich, William Thomas Muldoon, James Albert Napper, Laurence Rousseau
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Patent number: 6352722Abstract: Derivatized carbohydrates are provided which can be used to form a variety of materials including solid delivery systems. The derivatized carbohydrates are generally carbohydrates, wherein at least a portion of the hydroxyl groups on the carbohydrate are substituted with a branched hydrophobic chain, such as a hydrocarbon chain, via, for example, an ether or ester linkage. The solid delivery systems can be used for delivery and release of a variety of substances, and are, for example, in the form of tablets for oral administration, or in the form of powders, microspheres or implants for intravenous, intradermal, transdermal, pulmonary or other route of administration. The derivatized carbohydrates can be processed to form a solid matrix having a substance, such as a therapeutic agent, incorporated therein. In one embodiment, the solid matrix is provided in a solid dose form which is capable of releasing a therapeutic substance in situ at various controlled rates.Type: GrantFiled: December 22, 1998Date of Patent: March 5, 2002Assignee: Quadrant Holdings Cambridge LimitedInventor: Julian A. Blair
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Patent number: 6348216Abstract: Provided herein are compositions and methods of making compositions of ibuprofen in combination with a narcotic analgesic. Specifically provided is a pharmaceutical tablet composition comprising ibuprofen; a narcotic analgesic; colloidal silicon dioxide; a filler selected from the group consisting of microcrystalline cellulose and powdered cellulose; a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, and sodium starch glycolate; a binder consisting of an akylhydroxy methylcellulose; a starch; and a lubricant.Type: GrantFiled: June 10, 1997Date of Patent: February 19, 2002Assignee: Knoll Pharmaceutical CompanyInventors: Gregory P. Kushla, Jin-Wang Lai, Gerald P. Polli
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Publication number: 20020015729Abstract: There is provided a controlled release formulation including an inner core comprising, or coated with, a drug, which drug possesses (a) a free acid group which can be converted into an alkali metal salt and (b) a pKa in the rnage 2.0 to 9.0, which inner core is subsequently coated with a rate-controlling membrane that determines drug release, wherein the drug is present as a salt that displays higher solubility at pH 4.5 to 8.0 than the corresponding compound containing a free acid group.Type: ApplicationFiled: May 6, 1999Publication date: February 7, 2002Inventor: PETER JAMES WATTS
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Publication number: 20020015732Abstract: A formulation of a 5&agr;-reductase inhibitor for oral administration, which comprises a composition obtained by grinding a mixture of an azasteroid, a water-soluble polymer and a disintegrant.Type: ApplicationFiled: August 4, 1998Publication date: February 7, 2002Inventors: FUSAO USUI, YUKO OHUCHI, AKIRA KUSAI
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Patent number: 6340475Abstract: 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: GrantFiled: March 29, 1999Date of Patent: January 22, 2002Assignee: DepoMed, Inc.Inventors: John W. Shell, Jenny Louie-Helm, Micheline Markey
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Patent number: 6340476Abstract: Novel pharmaceutical dosage forms provide for pulsatile delivery of methylphenidate, i.e., release encapsulated drug in spaced apart “pulses.” The dosage forms are comprised of first, second and optionally third dosage units, with each dosage unit having a different drug release profile. The dosage forms may comprise capsules housing compressed tablets or drug-containing beads or particles, or may comprise a single tablet with the first, second and optionally third dosage units each representing an integral and discrete segment thereof. Methods of treatment using the pharmaceutical dosage forms are provided as well.Type: GrantFiled: April 6, 2000Date of Patent: January 22, 2002Assignee: Armaquest, Inc.Inventors: Kamal K. Midha, Theodore L. Iorio, Shubha Chungi