Discrete Particles In Supporting Matrix Patents (Class 514/965)
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Patent number: 6413534Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of preventing prostate carcinogenesis comprising the steps of administering to a human subject having a precancerous precursor of prostate adenocarcinoma, a pharmaceutical preparation comprising a chemopreventive agent to prevent, prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.Type: GrantFiled: September 12, 2000Date of Patent: July 2, 2002Assignee: The University of Tennessee Research CorporationInventors: Mitchell S. Steiner, Sharan Raghow
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Patent number: 6413535Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of preventing prostate carcinogenesis comprising the steps of administering to a human subject having a precancerous precursor of prostate adenocarcinoma, a pharmaceutical preparation comprising a chemopreventive agent to prevent, prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.Type: GrantFiled: September 12, 2000Date of Patent: July 2, 2002Assignee: The University of Tennessee Research CorporationInventors: Mitchell S. Steiner, Sharan Raghow
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Patent number: 6410043Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of preventing prostate carcinogenesis comprising the steps of administering to a human subject having a precancerous precursor of prostate adenocarcinoma, a pharmaceutical preparation comprising a chemopreventive agent to prevent, prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.Type: GrantFiled: September 12, 2000Date of Patent: June 25, 2002Assignee: The University of Tennessee Research CorporationInventors: Mitchell S. Steiner, Sharan Raghow
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Patent number: 6406689Abstract: Compositions and methods are provided which can be utilized in active immunization as a prophylactic treatment or a therapeutic treatment for tumors. The compositions are employed as injectable tumor vaccines or as preparations for intratumoral administration and are capable of stimulating immune responses to specific tumor antigens. The tumor vaccines are composed of an antigenic cellular material including a plurality of inactivated tumor cells or tumor cell portions, a depot material, and an immunostimulant adsorbed to the depot material. The depot material with absorbed immunostimulant is mixed with the tumor cells or tumor cell portions to form the vaccine compositions. The preparations for intratumoral administration include the depot material adsorbed immunostimulant without the antigenic cellular material. The immunostimulant adsorbed to the depot material permits release of biologically active quantities of the immunostimulant over a period of time rather than all at once.Type: GrantFiled: March 3, 1999Date of Patent: June 18, 2002Inventors: Frank W. Falkenberg, Oliver C. Krup
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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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Patent number: 6391341Abstract: The present invention relates to multi-unitary pharmaceutical preparations containing piroxicam for oral administration. Such pharmaceutical preparations are stable pellet pharmaceutical preparations containing piroxicam and they comprise an amount of active ingredient of between 5 and 50 mg, an inert core with spherical symmetry and a diameter of 600-850 &mgr;m, constituted by inert excipients, coated with an active layer containing piroxicam in micronized form and various pharmaceutically acceptable inert excipients, mixed in appropriate proportions in order to allow the adequate disaggregation of the formulations and dissolution of the active ingredient, coated in it turn with an insulating layer of a polymeric nature and soluble in water, this layer being coated finally with a gastroresistant or enteric layer of a minimum thickness of 20 &mgr;m. This invention also refers to the process for the preparation of said pharmaceutical preparations.Type: GrantFiled: May 30, 2000Date of Patent: May 21, 2002Inventors: Carla Patricia Goncalves Mendes, Maria Julia Caeiro Ramalho de Oliveira
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Patent number: 6368632Abstract: Method of treating warm blooded animals suffering from psychotic disorders. The method includes administering a pharmaceutically effective amount of sustained-release microparticles that include risperidone, or a pharmaceutically acceptable acid addition salt thereof, and a biodegradable and biocompatible polymeric matrix.Type: GrantFiled: May 26, 2000Date of Patent: April 9, 2002Assignees: Janssen Pharmaceutica, Alkermes Controlled Therapeutics Inc. IIInventors: Jean Mesens, Michael E. Rickey, Thomas J. Atkins
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Patent number: 6368630Abstract: The present invention relates to a composition for the modulated release of a biologically active agent. The composition comprises a biocompatible polymeric matrix, a biologically active agent which is dispersed within the polymeric matrix, and a metal cation component which is separately dispersed within the polymeric matrix, whereby the metal cation component modulates the release of the biologically active agent from the polymeric matrix. The present invention also relates to a method for modulating the release of a biologically active agent from a biocompatible polymeric matrix, comprising the steps of dissolving a biocompatible polymer in a solvent to form a polymer solution and also separately dispersing a metal cation component and a biologically active agent within the polymer solution.Type: GrantFiled: March 23, 1999Date of Patent: April 9, 2002Assignee: Alkermes Controlled Therapeutics, Inc.Inventors: Howard Bernstein, Yan Zhang, M. Amin Khan, Mark A. Tracy
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Publication number: 20020037309Abstract: 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: ApplicationFiled: March 7, 2001Publication date: March 28, 2002Applicant: Alkermes Controlled Therapeutics, Inc.Inventors: Warren E. Jaworowicz, James I. Wright
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Patent number: 6346518Abstract: The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula and the pharmaceutically acceptable acid addition salt forms thereof, processes for preparing said stereoisomeric forms, the complexes thereof with cyclodextrin derivatives, pharmaceutical compositions comprising said complexes and methods of preparing said complexes and pharmaceutical compositions.Type: GrantFiled: January 26, 1995Date of Patent: February 12, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Jean Louis Mesens, Jozef Peeters
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Patent number: 6340671Abstract: The invention relates to certain stable microsphere compositions containing a fat, a wax or a mixture thereof; an active ingredient selected from LL-F28249&agr;-&lgr; compounds, 23-oxo or 23-imino derivatives of LL-F28249&agr;-&lgr; compounds, milbemycin compounds and avermectin compounds; an antioxidant and, optionally, an oil, a semi-soft fat, a fatty acid derivative or mixture thereof. The invention also relates to a method for introducing and maintaining levels of the active compound in the blood of warm-blooded animals for extended periods of time and for the prevention or treatment of infections and infestations caused by helminths, nematodes, acarids and endo- and ectoparasitic arthropods in warm-blooded animals by the parenteral administration of compositions of the invention.Type: GrantFiled: June 22, 1994Date of Patent: January 22, 2002Assignee: American Cyanamid CompanyInventors: Susan Mancini Cady, William David Steber, Phillip Wayne Hayes, Mary Ehlers Doscher, Kurt Allen Schwinghammer
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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: 6245740Abstract: The present invention relates to the preparation of polyol/thickened oil suspensions containing a biologically active agent, for the sustained delivery of the biologically active agent. The described protein/glycerol/oil suspensions show sustained release of protein, e.g., G-CSF, of up to at least one week.Type: GrantFiled: December 23, 1998Date of Patent: June 12, 2001Assignee: Amgen Inc.Inventors: Merrill Goldenberg, Daxian Shan, Alice Beekman
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Patent number: 6228894Abstract: A softgel-compatible composition containing retinol comprises retinol-impregnated microparticles. The composition may include an optionally thickened silicone oil, or may include an emulsion comprising a silicone oil. Ascorbic acid may be present as ascorbic acid-impregnated microparticles and/or within the emulsion. Such compositions are compatible with softgels, and may also be used in other dispensing containers, such as sachets, tubes, and airless pumps.Type: GrantFiled: March 19, 1999Date of Patent: May 8, 2001Assignees: Enhanced Derm Technologies, Inc., R. P. Scherer CorporationInventors: Marie A. Rinaldi, Subhash J. Saxena, Paul C. Tutschek
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Patent number: 6221853Abstract: The invention relates to a lactulose-based medicinal product, characterized by the incorporation of anhydrous lactulose into a coating vehicle, which is also anhydrous, consisting of a mixture of pharmaceutically acceptable purified paraffinic hydrocarbons, this vehicle having a melting point of about 37° C.±4° C. It is, in particular, dosed so as to allow the administration of 3 to 5 g per day to an adult, in particular in a single dosage intake.Type: GrantFiled: October 21, 1998Date of Patent: April 24, 2001Inventors: Odette M. Salsarulo, Gerard Salsarulo
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Patent number: 6203813Abstract: The present invention provides an opiate antagonist implant which is an admixture of an opiate antagonist, in either acid or base form, and a pharmaceutically acceptable carrier. The admixture is uniformly compressed into a subcutaneously implantable pellet which is effective to release levels of the opiate antagonist over desired amounts of time when subcutaneously implanted in a patient to effectively inhibit the effects of a number of addictive drugs.Type: GrantFiled: October 9, 1998Date of Patent: March 20, 2001Inventor: Lance L. Gooberman
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Patent number: 6204255Abstract: Non-deliquescent formulation comprising or consisting of sodium valproate and cyclodextrin having a molar ratio of sodium valproate to cyclodextrin within the range of from 1:0.01 to 1:0.09.Type: GrantFiled: May 24, 1999Date of Patent: March 20, 2001Assignee: Hexal AGInventor: Karin Klokkers
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Patent number: 6200590Abstract: A phased-release suppository delivery system is disclosed wherein microscopic polymeric “nanospheres” ladened with one or more active agents are homogeneously incorporated within a pharmaceutically acceptable suppository base. The preparation of the “nanospheres” allows the spheres to be transported, substantially intact, across fenestrated membranes such as the capillary membranes of the rectum. The method of preparation of the “nanospheres” allows for the controlled release of active agent(s) only after a substantial number of the spheres have been transported across the capillary membrane of the rectum or other body cavity and have been taken up into the systemic circulation system.Type: GrantFiled: August 10, 1998Date of Patent: March 13, 2001Assignee: Naphcare, Inc.Inventor: John Graham Eley
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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: 6136343Abstract: A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.Type: GrantFiled: December 8, 1998Date of Patent: October 24, 2000Assignee: Edward Mendell Co., Inc.Inventor: Anand R. Baichwal
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Patent number: 6126967Abstract: An extended release acetaminophen composition comprises a plurality of discrete particles containing acetaminophen which, when contained within a gelatin capsule and assayed in a USP Apparatus I rotating basket at 50 rpm in 900 mL of phosphate buffer at pH 5.8 and 37.degree. C., exhibits about 40 percent to about 53 percent acetaminophen dissolution at one-half hour, about 50 percent to about 68 percent dissolution at 45 minutes, about 57 percent to about 77 percent acetaminophen dissolution at one hour, and about 82 percent to about 92 percent acetaminophen dissolution at two hours. After six hours, the contemplated extended release acetaminophen composition exhibits substantially complete dissolution. A process for treating a human patient with the extended release acetaminophen composition is also disclosed.Type: GrantFiled: September 3, 1998Date of Patent: October 3, 2000Assignee: Ascent PediatricsInventors: Emmett Clemente, Aloysius O. Anaebonam, Robert W. Mendes, Abdel A. Fawzy, Eric M. Morrel
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Patent number: 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: 6083532Abstract: Depot drug formulations include the pharmaceutical itself and a three component release rate controlling matrix composition. The three components of the matrix composition are (1) a pH dependent gelling polymer such as an alginate component, (2) an enteric polymer component, such as Eudragit.RTM. L or S, and (3) a pH independent gelling polymer, such as hydroxy propyl methyl cellulose or polyethylene oxide. The drug release rate can be adjusted by changing the amount of one or more of these components of the composition.Type: GrantFiled: December 5, 1997Date of Patent: July 4, 2000Assignee: Duramed Pharmaceuticals, Inc.Inventors: Guohua Zhang, Prasad Pinnamaraju, Muhammad Ali
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Patent number: 6080429Abstract: A method for drying microspheres in a fluidized bed is provided, along with a composition comprising microspheres dried by that method.Type: GrantFiled: November 7, 1997Date of Patent: June 27, 2000Assignee: Genentech, Inc.Inventors: Jeffrey L. Cleland, Andrew J. S. Jones, Michael Frank Powell
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Patent number: 6074634Abstract: The present invention provides an composition for attracting noctuid and/or other lepidopteran species. Liquid and solid formulations are provided, along with methods for their use, for controlling or eliminating noctuid and/or other lepidopteran species, and/or protecting plants susceptible to noctuid and/or other lepidopteran species damage.Type: GrantFiled: October 5, 1998Date of Patent: June 13, 2000Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Juan D. Lopez, Jr., Ted N. Shaver, Kenneth R. Beerwinkle, Peter D. Lingren
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Patent number: 6069137Abstract: This invention relates to treatment of traveller's diarrhea, including diarrhea caused by enterotoxigenic E. coli (ETEC), using oligosaccharide compositions which bind E. coli heat-labile toxin (LT) and/or one or more serotypes of enterotoxigenic E. coli organisms. More specifically, the invention concerns neutralization and removal of LT associated with traveller's diarrhea. This invention also relates to prevention of ETEC from colonizing the intestinal tract and inducing disease.Type: GrantFiled: April 30, 1998Date of Patent: May 30, 2000Assignee: Synsorb Biotech, Inc.Inventors: Louis D. Heerze, Glen D. Armstrong
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Patent number: 6046177Abstract: Sulfoalkyl ether cyclodextrin (SAE-CD) based controlled release pharmaceutical formulations are provided by the present invention. The present solid pharmaceutical formulations consist of a core comprising a physical mixture of one or more SAE-CD derivatives, an optional release rate modifier, a therapeutic agent, a major portion of which is not complexed to the SAE-CD, and an optional release rate modifying coating surrounding the core. The present formulations are advantageously easier to prepare than other SAE-CD based formulations in the art yet provide similar or improved effectiveness. The SAE-CD derivative is used to modify the bioavailability and/or rate of bioabsorption of therapeutic agents. Multi-layered, osmotic pump, coated, and uncoated tablet, minitablet, pellet, micropellet, particle, powder, and granule dosage forms are disclosed herein.Type: GrantFiled: January 13, 1999Date of Patent: April 4, 2000Assignee: Cydex, Inc.Inventors: Valentino J. Stella, Roger A. Rajewski, Venkatramana M. Rao, James W. McGinity, Gerold L. Mosher
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Patent number: 6020002Abstract: The present invention is a method and a dosage unit for delivery of a controlled-release system. The dosage unit is a quick dissolve unit which can be prepared by mixing uncured shearform matrix and a controlled-release system, either molding or compacting a unit dosage form and curing the shearform matrix. The controlled-release systems used in the present invention include instantaneous release components, delayed release components, sustained release components, and combinations thereof.Type: GrantFiled: November 5, 1997Date of Patent: February 1, 2000Assignee: Fuisz Technologies Ltd.Inventors: Garry L. Myers, Gerald E. Battist, Richard C. Fuisz
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Patent number: 5993805Abstract: Microparticles of a water-soluble material, which are smooth and spherical, and at least 90% of which have a mass median particle size of 1 to 10 .mu.m, and which carry a therapeutic or diagnostic agent can successfully be used in dry powder inhalers to deliver the said agent.Type: GrantFiled: June 7, 1995Date of Patent: November 30, 1999Assignee: Quadrant Healthcare (UK) LimitedInventors: Andrew D. Sutton, Richard A. Johnson, Peter J. Senior, David Heath
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Patent number: 5985354Abstract: Two or more hydrophilic polymers that are not soluble in each other at a particular concentration and temperature, but which have a positive spreading coefficient in solution, are used to form multi-layered polymeric microspheres. The multi-layer microspheres produced by the method are distinguished by extremely uniform dimensioned polymer layers and actual incorporation of a substance to be delivered into the polymer layers. In the preferred embodiment of the method, two polymers are dissolved in an aqueous solvent, the substance to be incorporated is dispersed or dissolved in the polymer solution, the mixture is suspended in an organic solvent or polymer/water mixture and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer.Type: GrantFiled: June 7, 1995Date of Patent: November 16, 1999Assignee: Brown University Research FoundationInventors: Edith Mathiowitz, Jules S. Jacob, Donald E. Chickering, III, Kathleen Jo Pekarek
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Patent number: 5977313Abstract: Platelet substitutes, comprising fibrinogen, or analogous products useful in therapy, which further comprise an insoluble carrier to which is bound an essentially non-degraded active protein including the sequence Arg-Gly-Asp. Such conjugates can be made by a conjugation process comprising 0.01 to 2.5% by weight active fibrinogen, and no more that 50% inactive fibrinogen.Type: GrantFiled: October 17, 1997Date of Patent: November 2, 1999Assignee: Quadrant Healthcare LimitedInventors: David Heath, Sarah Margaret Middleton, Roy Harris, Nicola Jane Church
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Patent number: 5942244Abstract: A tablet for the local and slow release of herbal medication into the oral cavity of a subject. Also provided is a method of making the tablet and a method of using the tablet. The tablet includes a pharmaceutically effective amount of a herbal medication, a polymeric matrix material such as ethyl cellulose, a release enhancer such as PEG 4000 and a filler such as lactose. The tablet is characterized by long dissolution times of up to 120 minutes.Type: GrantFiled: July 31, 1997Date of Patent: August 24, 1999Assignee: Farmo-Nat Ltd.Inventors: Michael Friedman, Orna Levin, Yochanan Forman, Doron Friedman
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Patent number: 5928667Abstract: A drug delivery device comprising a single phase matrix of a rigid polymer and a flexible polymer, useful for sustained release of a pharmaceutically active ingredient, as well as a method for employing the same, are disclosed.Type: GrantFiled: November 25, 1996Date of Patent: July 27, 1999Assignee: University of MarylandInventors: Joel Rosenblatt, Vivek Shenoy
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Patent number: 5916790Abstract: The present invention generally relates to novel encapsulation compositions and methods. In particular, the invention relates to stabilized microcapsule compositions which comprise a layer of a crosslinked, mixed functionality, polymer matrix, and methods for their preparation. The encapsulated compositions may comprise the crosslinked polymer matrix layer as an inner layer, an outer layer, or an intermediate layer of an overall encapsulated composition. The compositions will generally also comprise a biological material, e.g., cells, proteins, and the like, encapsulated within the composition. The compositions and methods of the invention are useful in a variety of applications, including cell culturing and transplant therapy.Type: GrantFiled: March 3, 1995Date of Patent: June 29, 1999Assignee: Metabolex, Inc.Inventor: Karl C. Enevold
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Patent number: 5912017Abstract: A method for preparation of multi-layer polymeric microspheres formed from any degradable or non-degradable polymers which are not soluble in each other at a particular concentration, but which have a positive spreading coefficient in solution. The multi-layer microspheres produced by the method are distinguished by extremely uniform dimensioned layers of polymer and actual incorporation of the substance to be delivered into the polymer layers. In the preferred embodiment of the method, two polymers are dissolved in a volatile organic solvent, the substance to be incorporated is dispersed or dissolved in the polymer solution, the mixture is suspended in an aqueous solution and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer. In another embodiment, solvent is removed by spray drying.Type: GrantFiled: July 1, 1992Date of Patent: June 15, 1999Assignee: Massachusetts Institute of TechnologyInventors: Edith Mathiowitz, Robert S. Langer
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Patent number: 5912015Abstract: The present invention relates to a composition for the modulated release of a biologically active agent. The composition comprises a biocompatible polymeric matrix, a biologically active agent which is dispersed within the polymeric matrix, and a metal cation component which is separately dispersed within the polymeric matrix, whereby the metal cation component modulates the release of the biologically active agent from the polymeric matrix. The present invention also relates to a method for modulating the release of a biologically active agent from a biocompatible polymeric matrix, comprising the steps of dissolving a biocompatible polymer in a solvent to form a polymer solution and also separately dispersing a metal cation component and a biologically active agent within the polymer solution.Type: GrantFiled: April 7, 1998Date of Patent: June 15, 1999Assignee: Alkermes Controlled Therapeutics, Inc.Inventors: Howard Bernstein, Yan Zhang, M. Amin Khan, Mark A. Tracy
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Patent number: 5910322Abstract: Pharmaceutical formulations for oral administration, comprising a matrix which comprises a .beta.-lactam antibiotic optionally in combination with a .beta.-lactamase inhibitor, granules in a delayed release form dispersed within the matrix, which comprise a .beta.-lactam antibiotic optionally in combination with a .beta.-lactamase inhibitor, the overall tablet formulation including a .beta.-lactam antibiotic and a .beta.-lactamase inhibitor.Type: GrantFiled: October 2, 1997Date of Patent: June 8, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Ernest Lionel Gilbert Rivett, Francis Walter Grimmett, Michael William Hartnell
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Patent number: 5900425Abstract: The invention relates to pharmaceutical preparations having controlled release of active compound and to processes for their preparation, in particular for poorly soluble active compounds having problematic bioavailability.Type: GrantFiled: September 19, 1997Date of Patent: May 4, 1999Assignee: Bayer AktiengesellschaftInventors: Venkata-Rangarao Kanikanti, Wolfgang Muck, Andreas Ohm, Peter Kurka, Gerd Toppel
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Patent number: 5891470Abstract: A softgel formulation containing retinol comprises a soft gelatin shell and a fill material within that shell containing retinol-impregnated microparticles. The fill material may be an optionally thickened silicone oil, or may be an emulsion comprising a silicone oil. Ascorbic acid may be present as ascorbic acid-impregnated microparticles and/or within the emulsion.Type: GrantFiled: April 17, 1998Date of Patent: April 6, 1999Assignees: Advanced Polymer Systems, Inc., R.P. Scherer CorporationInventors: Marie A. Rinaldi, Subhash J. Saxena, Paul C. Tutschek
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Patent number: 5880150Abstract: An antimicrobial agent comprising allyl isothiocyanate (AIT) packaged in a packaging material having a structure wherein part of the pores of a porous packaging substrate is filled with, or said pores are partially or entirely narrowed by a resin impervious to AIT vapor, and a method for controlling the AIT vapor release speed comprising enclosing AIT in the above-mentioned packaging material. According to the present invention, the AIT vapor release speed can be controlled, whereby enabling sustained release of AIT vapor and persistent effect of antimicrobial action. In addition, the antimicrobial agent of the present invention can be widely applied to food industries and various other fields where breeding and reproduction of deleterious microorganisms pose problems, since it is economical, compact and easy to use.Type: GrantFiled: July 10, 1995Date of Patent: March 9, 1999Assignees: The Green Cross Corporation, Rengo Co., Ltd.Inventors: Masao Fujita, Kiyoshi Kamei, Kiyoko Kawazu, Yuichi Mizukami, Yasushi Sekiyama
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Patent number: 5879713Abstract: Delivery of bioactive molecules such as nucleic acid molecules encoding a protein can be significantly enhanced by immobilization of the bioactive molecule in a polymeric material adjacent to the cells where delivery is desired, where the bioactive molecule is encapsulated in a vehicle such as liposomes which facilitates transfer of the bioactive molecules into the targeted tissue. Targeting of the bioactive molecules can also be achieved by selection of an encapsulating medium of an appropriate size whereby the medium serves to deliver the molecules to a particular target. For example, encapsulation of nucleic acid molecules or biologically active proteins within biodegradable, biocompatible polymeric microparticles which are appropriate sized to infiltrate, but remain trapped within, the capillary beds and alveoli of the lungs can be used for targeted delivery to these regions of the body following administration to a patient by infusion or injection.Type: GrantFiled: January 23, 1997Date of Patent: March 9, 1999Assignee: Focal, Inc.Inventors: Laurence A. Roth, Stephen Jack Herman
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Patent number: 5874418Abstract: Sulfoalkyl ether-cyclodextrin (SAE-CD) based pharmaceutical formulations are provided by the present invention. These formulations comprise SAE-CD derivatives and a therapeutic agent, a major portion of which is not complexed to the SAE-CD. The present formulations are advantageously easier to prepare than other SAE-CD based formulations in the art yet provide similar or improved effectiveness. The SAE-CD derivative can be used to modify the bioavailability and/or rate of bioabsorption of therapeutic agents.Type: GrantFiled: May 5, 1997Date of Patent: February 23, 1999Assignee: Cydex, Inc.Inventors: Valentino Stella, Roger A. Rajewski, James W. McGinity
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Patent number: 5869094Abstract: A solid form of oral administration of isosorbide 5-mononitrate with a controlled, pH-independent release of the active substance in the gastro-intestinal tract is constituted by a pellet coated with a depot layer and a release prolonging lacquer layer. The lacquer layer contains ethyl cellulose and polymethacrylate in a weight ratio from 3:1 to 3:2. The new form of administration is characterized in that it is less costly to produce.Type: GrantFiled: January 24, 1997Date of Patent: February 9, 1999Assignee: BYK Gulden Lomberg Chemische Fabrik GmbHInventors: Cornelia Alida Maria Van Egmond, Andre Pullen, Sibo Wytse De Jong, Adrianus Petrus De Jong, Jan Bron
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Patent number: 5866619Abstract: A colonic delivery system for delivering a drug to the colon is provided. The system comprises a drug in combination with a matrix, wherein the matrix comprises a saccharide-containing polymer. According to the invention, the matrix is resistant to chemical and enzymatic degradation in the stomach and small intestine. The matrix is degraded in the colon by bacterial enzymatic action, and the drug is released. The system is useful for targeting drugs to the colon in order to treat colonic disease. The system is also useful for enteric administration of drugs such as proteins and peptides which are otherwise degraded in the stomach and small intestine.Type: GrantFiled: November 26, 1997Date of Patent: February 2, 1999Assignees: Perio Products Ltd., Yissum Research Development Company of the Hebrew University of JerusalemInventors: Amnon Sintov, Abraham Rubinstein
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Patent number: 5866163Abstract: The present invention is a method of preparing rapidly dissolving comestible units such as tablets. The present invention also includes an apparatus for making the comestible units and the units themselves. The product prepared in accordance with the present invention can include active ingredients and is capable of dissolving in the mouth of the consumer within several seconds. The unit dosage forms prepared in accordance with the present invention are particularly useful as antacids and as a delivery vehicle for biologically active ingredients, especially those which are ideally combined with antacid ingredients in order to ameliorate the effects of antacid environment.Type: GrantFiled: December 19, 1996Date of Patent: February 2, 1999Assignee: Fuisz Technologies Ltd.Inventors: Garry L. Myers, Gerald E. Battist, Richard C. Fuisz
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Patent number: 5861387Abstract: Methods of treatment and prevention of estrogen-related diseases, and of fertility control, include low dose (e.g. less than 50 nanomolar serum concentration) administration of certain anabolic steroids, progestins and other substantially non-masculinizing androgenic compounds. Sustained release formulations substantially free of organic solvent, and sustained release formulations for maintaining low serum levels of androgen are disclosed.Type: GrantFiled: June 7, 1995Date of Patent: January 19, 1999Assignee: Endorecherche Inc.Inventors: Fernand Labrie, Martin Lepage
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Patent number: 5853746Abstract: Methods and compositions are provided for the treatment and repair of defects in the cartilage or bone of humans and other animals as in full-thickness defects in joints. To induce cartilage formation, a defect in cartilage is filled with a matrix having pores sufficiently large to allow cartilage repair cells to populate the matrix. The matrix contains an anti-angiogenic agent that serves as a functional barrier to prevent vascularization and bone growth into the cartilage area. The matrix filling the defect in cartilage may also contain a proliferation agent and a chemotactic agent, and a transforming factor in an appropriate delivery system. A functional barrier between the bone and cartilage areas of a full-thickness defect may also be created by heat-treating the areas of bleeding to form a transient tissue barrier which prevents blood vessels and associated cells from penetrating from the bone area into the cartilage area.Type: GrantFiled: June 28, 1996Date of Patent: December 29, 1998Assignee: Robert Francis ShawInventor: Ernst B. Hunziker
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Organic/inorganic gels for delivering controlled quantities of active compounds in aqueous solutions
Patent number: 5846555Abstract: The invention concerns a composite gel comprising an inorganic matrix containing a fibrous inorganic polymer in which an active organic compound is dispersed.The invention also concerns a device comprising the gel and a process for delivering a controlled quantity of active organic compound in an aqueous solution.The invention applies to the prevention of biological growth in aqueous solutions used domestically, agriculturally or industrially, in particular in the solutions used in photographic processing.Type: GrantFiled: September 5, 1996Date of Patent: December 8, 1998Assignee: Eastman Kodak CompanyInventors: Olivier Jean Christian Poncelet, Danielle Marie Henriette Wettling, Jeannine Rigola -
Patent number: 5846563Abstract: A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.Type: GrantFiled: April 18, 1997Date of Patent: December 8, 1998Assignee: Edward Mendell Co., Inc.Inventor: Anand R. Baichwal
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Patent number: 5840714Abstract: Inclusion Complexes of Racemic Ibuproxam and of Optically Active Ibuproxam with Cyclodextrin Derivatives, Process for the Preparation Thereof, Pharmaceutical Preparations Containing these Inclusion Complexes or Containing Optically Active S-(+)-Ibuproxam, and Use ThereofThere are disclosed novel inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic cyclodextrin derivatives and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone. Further a process for preparing S-(+)-ibuproxam and inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic derivatives of .beta.-cyclodextrin and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone, is disclosed.Disclosed are also pharmaceutical compositions containing these inclusion complexes or optically active S-(+)-ibuproxam.Type: GrantFiled: February 20, 1996Date of Patent: November 24, 1998Assignee: LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.Inventors: Janko Zmitek, Katarina Verhnjak, Darja Fercej-Temeljotov, Mateja Kovacic, Anton Lavric, Breda Bole-Vunduk