Ethyl Cellulose Patents (Class 424/495)
  • Rapidly disintegrating coated pellets with delayed release
    Patent number: 6379706
    Abstract: The invention concerns pharmaceutical forms of administration that are in the form of pellets which contain a retarding agent in which the release rate of the active substance is not delayed or is substantially identical compared to corresponding pellets that contain no retarding agent. The release rate of these rapidly disintegrating pellets is at least about 90% within a time period of 30 minutes. In addition the present invention also concerns processes for the production these pellets.
    Type: Grant
    Filed: January 31, 2001
    Date of Patent: April 30, 2002
    Assignee: Roche Diagnostics GmbH
    Inventors: Michaela Opitz, Hendrik Von Burën, Rolf-Dieter Gabel, Geoffrey Lee
  • Stabilized pharmaceutical composition and its production
    Patent number: 6380234
    Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: April 30, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tadashi Makino, Tetsuro Tabata, Shin-Ichiro Hirai
  • Composition comprising a crystallographically stable, amorphous cephalosporin and processes for the preparation thereof
    Publication number: 20020037322
    Abstract: Processes are provided for the preparation of orally administrable, yellow and powdery compositions essentially consisting of particles composed of a homogeneous mixture of an amorphous Cefditoren pivoxil substance with a water soluble high-molecular additive. These compositions can be produced by dissolving crystalline Cefditoren pivoxil substance and the water-soluble high-molecular additive in an aqueous solution of an acid, then neutralizing the resultant solution, to co-precipitate the product, and drying the thus precipitated product, followed by recovering the product in the form of the above-mentioned particles.
    Type: Application
    Filed: November 26, 2001
    Publication date: March 28, 2002
    Inventors: Masahiro Onodera, Masamichi Sukegawa, Kiyoshi Yasui, Tatsuo Watanabe, Toyomi Sato, Yasushi Murai, Katsuharu Iinuma
  • Pharmaceutical excipient having improved compressibility
    Patent number: 6358533
    Abstract: 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: Grant
    Filed: January 4, 2001
    Date of Patent: March 19, 2002
    Assignee: Edward Mendell, Co., Inc.
    Inventors: Bob E. Sherwood, John H. Staniforth, Edward A. Hunter
  • METHOD AND COMPOSITION FOR TREATMENT OF INFLAMMATORY CONDITIONS
    Publication number: 20020002154
    Abstract: Methods of treating inflammation of the gastrointestinal tract and/or systemic or local inflammation by administering a steroid anti-inflammatory or a non-steroid anti-inflammatory drug in conjunction with polyunsaturated fatty acids or their derivatives and optionally also a pharmacologically active antioxidant and compositions for practicing these methods are described.
    Type: Application
    Filed: February 8, 1999
    Publication date: January 3, 2002
    Inventors: POL-HENRI GUIVARC'H, GARY ROBINSON
  • Controlled release formulation
    Patent number: 6326027
    Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: December 4, 2001
    Assignee: Euro-Celtique S.A.
    Inventors: Ronald Brown Miller, Sandra Therese Antoinette Malkowska, Walter Wimmer, Udo Hahn, Stewart Thomas Leslie, Kevin John Smith, Horst Winkler, Derek Allan Prater
  • Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer
    Patent number: 6316031
    Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: November 13, 2001
    Assignee: Purdue Pharma LP
    Inventors: Benjamin Oshlack, Frank Pedi, Jr., Mark Chasin
  • Sustained release pharmaceutical preparation
    Patent number: 6312728
    Abstract: The present invention pertains to a sustained release drug delivery system which comprises a core of active ingredient, an enteric coating, a second coating of active ingredient and lastly a readily gastric-soluble protective coating. In another embodiment, the sustained release drug delivery system comprises a core of active ingredient, an enteric coating; a second coating of active ingredient; a second enteric coating and a third coating of active ingredient The sustained release dosage form of this invention is useful for pharmaceutically active ingredients that have limited aqueous solubility, especially phenytoin sodium, and other pH dependent soluble drugs.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: November 6, 2001
    Assignee: Cascade Development, Inc.
    Inventors: Elliott Beiman, Fred Landsman
  • Enteric coated pharmaceutical compositions
    Patent number: 6306900
    Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: October 23, 2001
    Assignee: Novartis AG
    Inventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
  • Pharmaceutical formulations for acid labile substances
    Patent number: 6296876
    Abstract: This invention in general relates to novel pharmaceutical compositions for acid labile substances as well as for methods of making such. Specifically, the invention provides a pharmaceutical composition comprising about 1 to 75% by weight acid labile compound, up to about 5% by weight disintegrant, at least one protector coat layer used to separate and protect the acid labile substance from acid reacting groups and gastric juice, and at least one enteric coat layer which surrounds the protector coating layer and ensures delivery of over 80% the acid labile substance to the small intestine.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: October 2, 2001
    Inventors: Isa Odidi, Amina Odidi
  • Method for producing a granule
    Patent number: 6296875
    Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.
    Type: Grant
    Filed: June 7, 2000
    Date of Patent: October 2, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Tadashi Makino, Tetsuro Tabata, Shin-Ichiro Hirai
  • Controlled release encapsulated substances
    Publication number: 20010021404
    Abstract: Novel encapsulated substances which remain largely encapsulated in aqueous medium during a heat-treatment and only dissolve during a subsequent cooling phase can be prepared by processes for the preparation of spherical cores and subsequent coating with one or more hydrophobic shells and a shell of modified cellulose.
    Type: Application
    Filed: March 7, 2001
    Publication date: September 13, 2001
    Inventors: Jens Uhlemann, Birgit Schleifenbaum
  • Oral pharmaceutical composition with delayed release of active ingredient for pantoprazole
    Patent number: 6274173
    Abstract: An oral pharmaceutical composition comprises an acid-labile irreversible proton pump inhibitor in pellet or tablet form, wherein the irreversible proton pump inhibitor is at least partly in slow-release form. On combined administration with an anti-microbially-active ingredient, the composition is distinguished by imparting an enhanced action of rapid onset against disorders caused by Helicobacter.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: August 14, 2001
    Assignee: BYK Gulden Lomberg Chemische Fabrik GmbH
    Inventors: George Sachs, Rango Dietrich
  • Sachet formulations
    Patent number: 6270804
    Abstract: Bioaffecting sachets, or powders, containing coated liquiflash microspheres and partially recrystallized shearform floss particles are disclosed. The sachets give organoleptically acceptable properties, including a pleasing mouthfeel, when orally ingested.
    Type: Grant
    Filed: October 30, 1998
    Date of Patent: August 7, 2001
    Assignee: Biovail Technologies Ltd.
    Inventors: John J. Getz, Steven E. Frisbee, Tushar K. Misra, John R. Sisak, Pradeepkumar P. Sanghvi
  • Methods for preventing crystal growth and particle aggregation in nanoparticulate compositions
    Patent number: 6267989
    Abstract: The present invention is directed to methods for preventing crystal growth and particle aggregation in nanoparticulate compositions. The methods comprise reducing a nanoparticulate composition to an optimal effective average particle size. The resultant nanoparticulate compositions exhibit prolonged particle size stability and minimal crystal growth, even following exposure to elevated temperatures.
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: July 31, 2001
    Assignee: Klan Pharma International Ltd.
    Inventors: Elaine Liversidge, Greta A. Gottardy, Linden Wei
  • Method for encapsulating reactive dental agents
    Patent number: 6258343
    Abstract: A method for encapsulating a water soluble reactive agent in an alkyl cellulosic polymer to provide an encapsulated product from which leaching of the reactive agent into an aqueous dentifrice containing another compound reactive with the agent is prevented or controlled, said method comprising the steps of (a) uniformly dispersing the reactive agent in the alkyl cellulose and a solvent for the polymer to form a paste; (b) casting the paste onto a sheet forming substrate; (c) grinding and subdividing the sheet having the reactive agent encased therein into particles of a predetermined size; (d) washing the particles with water to remove any encased agent exposed by the grinding; and, (e) drying the particles of encapsulated reactive agent.
    Type: Grant
    Filed: August 15, 2000
    Date of Patent: July 10, 2001
    Assignee: Colgate-Palmolive Company
    Inventors: Alexander P. Kiczek, Sr., Mike Wong
  • FORMULATIONS FOR THERAPEUTIC AGENTS ABSORBED THROUGH MUCOUS MEMBRANES
    Publication number: 20010006617
    Abstract: Particulate crystalline therapeutic substances are formulated with stabilizers to enhance contact between the crystalline therapeutic substances and the mucosal membranes to provide extended therapeutic effect.
    Type: Application
    Filed: March 11, 1997
    Publication date: July 5, 2001
    Inventors: GARY G. LIVERSIDGE, W. MARK EICKHOFF, KATHLEEN J. ILLIG, PRAMOD SARPOTDAR, STEPHEN B. RUDDY
  • Controlled release tramadol
    Patent number: 6254887
    Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.
    Type: Grant
    Filed: July 10, 1996
    Date of Patent: July 3, 2001
    Assignee: Euro-Celtique S.A.
    Inventors: Ronald Brown Miller, Stewart Thomas Leslie, Sandra Therese Antoinette Malkowska, Kevin John Smith, Walter Wimmer, Horst Winkler, Udo Hahn, Derek Allan Prater
  • Programmed release ambroxol—HCl dosage forms
    Patent number: 6251429
    Abstract: Programmed-release ambroxol·HCl pharmaceutical dosage forms, adopted to maintain a therapeutically effective plasma level thereof for about 24 hours, comprise a plurality of inert core microgranules of a variety of particle sizes ranging from 0.3 to 1.2 mm, such inert core microgranules being coated with alternating microlayers of (1) micronized ambroxol hydrochloride active agent and (2) delayed-release film material, such coated microgranules including an external microlayer of delayed-release film material, and such coated mi.crogranules having particle sizes ranging from 0.6 to 1.5 mm.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: June 26, 2001
    Assignee: Therapicon slr
    Inventors: Paolo Alberto Veronesi, Anna Maria Veronesi
  • Controlled release dosage form of [R-(Z)]-alpha-(methoxyimino)-alpha-(1-azabicyclo[2.2.2.]oct-3-yl)acetonitrile monohydrochloride
    Publication number: 20010003588
    Abstract: A controlled release formulation of an acetonitrile compound and its use in the treatment and/or prophylaxis of certain disorders.
    Type: Application
    Filed: January 12, 2001
    Publication date: June 14, 2001
    Applicant: SmithKline Beecham Corporation
    Inventors: Joseph Peter Sauer, Susan Marie Milosovich, William Thomas Muldoon, James Albert Napper, Laurence Rousseau
  • Controlled-release composition
    Patent number: 6245351
    Abstract: A controlled-release composition comprising a drug-containing core coated with a coating composition containing a water-insoluble substance and a swellable polymer having no basic groups which is capable of maintaining an almost constant drug concentration in plasma over an extended period of time to ensure sustained drug action in the body.
    Type: Grant
    Filed: March 4, 1997
    Date of Patent: June 12, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Eiji Nara, Yohko Akiyama, Kenji Nakamura
  • Controlled release oral dosage form of ketoprofen
    Patent number: 6238703
    Abstract: A controlled release analgesic dosage form comprising: a core comprising an analgesic and binding agent; and a coating comprising an enteric polymer, a water insoluble second polymer and a lubricant.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: May 29, 2001
    Assignee: Andrx Pharmaceuticals, Inc.
    Inventors: Steve Jan, Xiu Xiu Cheng, Chih-Ming Chen
  • Fast decomposing pellets
    Patent number: 6224909
    Abstract: The invention concerns pharmaceutical forms of administration that are in the form of pellets which contain a retarding agent in which the release rate of the active substance is not delayed or is substantially identical compared to corresponding pellets that contain no retarding agent. The release rate of these rapidly disintegrating pellets is at least about 90% within a time period of 30 minutes. In addition the present invention also concerns processes for the production these pellets.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: May 1, 2001
    Assignee: Roche Diagnostics GmbH
    Inventors: Michaela Opitz, Hendrik Von Büren, Rolf-Dieter Gabel, Geoffrey Lee
  • Rapidly releasing and taste-masking pharmaceutical dosage form
    Patent number: 6221402
    Abstract: A rapidly-releasing and taste-masking pharmaceutical dosage form and a process for preparing such oral dosage form are disclosed.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: April 24, 2001
    Assignee: Pfizer Inc.
    Inventors: Akinori Itoh, Toshiyuki Niwa
  • Pharmaceutical excipient having improved compressibility
    Patent number: 6217909
    Abstract: 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: Grant
    Filed: November 12, 1999
    Date of Patent: April 17, 2001
    Assignee: Edward Mendell Co., Inc.
    Inventors: Bob E. Sherwood, John H. Staniforth, Edward A. Hunter
  • Prompt-release oral pharmaceutical compositions for extemporaneous suspensions
    Patent number: 6214386
    Abstract: A pharmaceutical composition suitable for preparing an extemporaneous suspension, that promptly releases active agents or ingredients (drugs) is disclosed. These compositions comprise an active agent in microgranule form. The microgranules containing the active agent are coated with a film coating mixture containing at least one lipid material and an optional hydrophilic additive. The coating envelopes the microgranules but does not impart a controlled release property to the composition, and affords prompt release thereof once ingested.
    Type: Grant
    Filed: November 22, 1996
    Date of Patent: April 10, 2001
    Assignees: Recordati, S.A., Chemical and Pharmaceutical Co.
    Inventors: Giancarlo Santus, Roberto Golzi
  • Gastroretentive controlled release microspheres for improved drug delivery
    Patent number: 6207197
    Abstract: There is provided a drug delivery composition for the controlled release of an active agent in the stomach environment over a prolonged period of time, which comprises a microsphere comprising an active ingredient in the inner core of the microsphere and (i) a rate controlling layer of a water insoluble polymer and (ii) an outer layer of a bioadhesive agent in the form of a cationic polymer.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: March 27, 2001
    Assignee: West Pharmaceutical Services Drug Delivery & Clinical Research Centre Limited
    Inventors: Lisbeth Illum, He Ping
  • Oral dosage for the controlled release of analgesic
    Patent number: 6197347
    Abstract: 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: Grant
    Filed: June 29, 1998
    Date of Patent: March 6, 2001
    Assignee: Andrx Pharmaceuticals, Inc.
    Inventors: Steve Jan, Xiu Xiu Cheng, Chih-Ming Chen
  • Entric-coated pharmaceutical compositions
    Patent number: 6172107
    Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: January 9, 2001
    Assignee: Novartis AG
    Inventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
  • Orally administrable nifedipine pellet and process for the preparation thereof
    Patent number: 6168806
    Abstract: The present invention relates to a fast-release as well as a prolonged release type of nifedipine pellets and the process for the preparation thereof. The fast-release type of nifedipine pellets comprises a particulate core which is covered by a nifedipine coating layer. The particulate core comprises water-soluble or water-insoluble excipient(s) and a pharmacologically acceptable carrier. The nifedipine coating layer comprises an effective amount of nifedipine dissolved in organic solvent(s). This nifedipine coating layer can further be mixed with a suspension which comprises an adhesive, an emulsifier, and a dispersant. The preferred composition of the fast-release type of nifedipine includes 20-70% of the particulate core, 3-15% of nifedipine, 1-20% of emulsifier, 1-20% of adhesive, and 1-30% of dispersant.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: January 2, 2001
    Inventors: Fang-Yu Lee, Shan-Chiung Chen, Han-Chiang Kuo
  • Dosage forms containing taste masked active agents
    Patent number: 6165512
    Abstract: 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: Grant
    Filed: October 30, 1998
    Date of Patent: December 26, 2000
    Assignee: Fuisz Technologies Ltd.
    Inventors: Djelila Mezaache, Michael G. Raiden, Pradeepkumar P. Sanghvi, Scott J. Szedlock
  • Methods of enhancing repair, healing and augmentation of tissues and organs
    Patent number: 6165514
    Abstract: Tissue and organ repair, healing and augmentation are enhanced by administering pharmaceutically acceptable group IIIa element-containing compounds in amounts sufficient to provide therapeutic levels of the elements. Group IIIa element-containing compounds mimic the beneficial biological effects of endogenous growth factors to induce cells responsible for repair, healing and augmentation of tissues and organs. Group IIIa element-containing compounds are suitable for a variety of applications such as wound healing, bone fracture repair, treatment of dermatologic conditions and successful bonding of implanted tissue grafts and prostheses.
    Type: Grant
    Filed: December 29, 1998
    Date of Patent: December 26, 2000
    Assignee: The Hospital for Special Surgery
    Inventors: Richard Bockman, Peter Guidon
  • Method of treating humans with opioid formulations having extended controlled release
    Patent number: 6143322
    Abstract: Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. of from about 12.5% to about 42.5% (by wt) opioid released after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of said opioid analgesic obtained in-vivo occurs from about 2 to about 8 hours after administration of the dosage form.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: November 7, 2000
    Assignee: Purdue Pharma L.P.
    Inventors: Richard Sackler, Robert Kaiko, Paul Goldenheim
  • Taste-masked microcapsule compositions and methods of manufacture
    Patent number: 6139865
    Abstract: A taste-masked microcapsule composition for administration of a drug is provided. The composition comprises microcapsules of drug and a substantially water-insoluble polymeric material, typically a cellulosic polymer. The microcapsule composition may be incorporated into any number of pharmaceutical formulations, including chewable tablets, effervescent tablets, powders, liquid dispersions, and the like. A method for masking the taste of drugs is also provided, involving a phase separation coacervation technique in which drug is coated with relatively high levels of a polymeric material. These high coating levels give rise to effective taste masking, while nevertheless allowing targeted release of drug, so that the drug is released shortly after passage through the mouth.
    Type: Grant
    Filed: October 1, 1997
    Date of Patent: October 31, 2000
    Assignee: Eurand America, Inc.
    Inventors: David R. Friend, Steve Ng, Rafael E. Sarabia, Thomas P. Weber, Jean-Marie Geoffroy
  • Flavor-masked pharmaceutical compositions
    Patent number: 6136347
    Abstract: The invention relates to flavor-masked pharmaceutical compositions for oral administration, their preparation and their use as medicaments.The new pharmaceutical preparations according to the invention make it possible to administer pharmaceutical active substances having very unpleasant organoleptic properties such as, for example, very bad taste, even in liquid form.
    Type: Grant
    Filed: May 24, 1996
    Date of Patent: October 24, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Norbert Pollinger, Johannes Michaelis, Klaus Benke, Roland Rupp, Manfred Bucheler
  • Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer
    Patent number: 6129933
    Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.
    Type: Grant
    Filed: July 24, 1997
    Date of Patent: October 10, 2000
    Assignee: Purdue Pharma LP
    Inventors: Benjamin Oshlack, Mark Chasin, Frank Pedi, Jr.
  • Extended release acetaminophen particles
    Patent number: 6126967
    Abstract: 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: Grant
    Filed: September 3, 1998
    Date of Patent: October 3, 2000
    Assignee: Ascent Pediatrics
    Inventors: Emmett Clemente, Aloysius O. Anaebonam, Robert W. Mendes, Abdel A. Fawzy, Eric M. Morrel
  • Process for producing stabilized pharmaceutical composition
    Patent number: 6123962
    Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R.sup.2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R.sup.3 and R.sup.5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R.sup.4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: September 26, 2000
    Assignee: Takeda Chemical Industries, Inc.
    Inventors: Tadashi Makino, Tetsuro Tabata, Shin-Ichiro Hirai
  • Fatty ester combinations
    Patent number: 6117452
    Abstract: The thermoforming of compositions containing active agents is carried out by processing compositions containing certain fatty esters in combination.
    Type: Grant
    Filed: August 12, 1998
    Date of Patent: September 12, 2000
    Assignee: Fuisz Technologies Ltd.
    Inventors: Nils Ahlgren, Joseph Cascone, Joan Fitzpatrick, Steven E. Frisbee, John Getz, Mark R. Herman, Bernard M. Kiernan, Barbara Montwill, Ed O'Donnell, Desiree Pereira, Pradeepkumar P. Sanghvi
  • Seeded microcapsules for use in tablets, pharmaceutical agents and nutritional compounds
    Patent number: 6110501
    Abstract: A microcapsule having a core, a shell and seeds fully or partially embedded in said shell. The core and seeds are active substances which preferably function as a leavening agent. The shell is composed of either a water soluble or meltable natural polymer, including vegetable waxes. When the shell is ruptured, the active substances will react with each other and the dough mixture thereby producing a leavening effect and/or dough conditioning effect in baked goods.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: August 29, 2000
    Assignee: Verion Inc.
    Inventors: Bruce K. Redding, Jr., Jerome Harden
  • Pharmaceutical excipient having improved compressibility
    Patent number: 6106865
    Abstract: A composition, comprising (a) microcrystalline cellulose; and (b) a compressibility augmenting agent which (i) physically restricts the proximity of the interface between adjacent cellulose surfaces; or (ii) inhibits interactions between adjacent cellulose surfaces; or (iii) accomplishes both (i) and (ii) above, is disclosed. The composition is in the form of agglomerated particles of microcrystalline cellulose and the compressibility augmenting agent in intimate association with each other.
    Type: Grant
    Filed: March 10, 1998
    Date of Patent: August 22, 2000
    Assignee: Edward Mendell Co., Inc.
    Inventors: John N. Staniforth, Edward A. Hunter, Bob E. Sherwood
  • Pharmaceutical excipient having improved compressibility
    Patent number: 6103219
    Abstract: 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: Grant
    Filed: December 17, 1997
    Date of Patent: August 15, 2000
    Assignee: Edward Mendell Co., Inc.
    Inventors: Bob E. Sherwood, John H. Staniforth, Edward A. Hunter
  • Opioid formulations having extended controlled release
    Patent number: 6103261
    Abstract: Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer at 37.degree. C. from about 12.5% to about 42.5% (by weight) active agent released after 1 hour, from about 25% to about 55% (by weight) active agent released after 2 hours, from about 45% to about 75% (by weight) opioid analgesic released after 4 hours and greater than about 60% (by weight) opioid analgesic released after a hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of active agent obtained in-vivo between about 2 and about 8 hours after administration of the dosage form.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: August 15, 2000
    Assignee: Purdue Pharma LP
    Inventors: Mark Chasin, Benjamin Oshlack, Frank Pedi, Jr.
  • Croscarmellose taste masking
    Patent number: 6099865
    Abstract: The present invention describes the use of croscarmellose sodium to coat bitter-tasting active agents in a manner that will mask the bitter taste of these materials, taste masked pharmaceutical compositions in which the particles of pharmaceutically active agent are coated with croscarmellose sodium, taste masked pharmaceutical tablets made therefrom, in which the rapid disintegration of tablets that is imparted by croscarmellose sodium is preserved, and to a method for preparing such coated particles by preparing them in a fluidized bed coating process.
    Type: Grant
    Filed: June 11, 1999
    Date of Patent: August 8, 2000
    Assignee: FMC Corporation
    Inventors: Michael Augello, Sheila M. Dell, George E. Reier, Howard J. Stamato, Lynn M. DiMemmo
  • H.sub.2 -Receptor antagonist and antacid composition
    Patent number: 6090412
    Abstract: A solid pharmaceutical composition for oral administration comprising a histamine H.sub.2 -receptor antagonist, a low neutralizing capacity antacid, and a high neutralizing capacity antacid coated with a pH-independent and water-insoluble polymer base, which composition improves the condition of a patient promptly after administration and sustains the effects for an extended period of time in the treatment of digestive disorders on which suppression of gastric acid secretion is effective.
    Type: Grant
    Filed: May 26, 1998
    Date of Patent: July 18, 2000
    Assignee: Yamaouchi Pharmaceutical Co., Ltd.
    Inventors: Yoshimi Hashimoto, Hiroyoshi Shiozawa, Hideyuki Kishimoto, Yoichi Setoguchi
  • Solid substances comprising valproic acid and sodium valproate
    Patent number: 6077542
    Abstract: Substances that are solid at 25.degree. C. are obtained by dissolving sodium valproate in heated valproic acid and cooling the resultant solution. The resulting solid substances can easily be processed into solid pharmaceutical dosage forms.
    Type: Grant
    Filed: July 31, 1997
    Date of Patent: June 20, 2000
    Inventor: Bernard Charles Sherman
  • Oral pharmaceutical composition with delayed release of active ingredient for pantoprazole
    Patent number: 6068856
    Abstract: An oral pharmaceutical composition of pantoprazole in pellet or tablet form, wherein the pantoprazole is at least partly in slow-release form, is distinguished, on combined administration with an antimicrobially-active ingredient, by an enhanced action of rapid onset against disorders caused by Helicobacter.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: May 30, 2000
    Assignee: BYK Gulden Chemische Fabrik GmbH
    Inventors: George Sachs, Rango Dietrich
  • Compositions comprising hemostatic compounds and bioabsorbable polymers
    Patent number: 6056970
    Abstract: Solid, fibrous bioabsorbable hemostatic compositions containing a bioabsorbable polymer and a hemostatic compound, methods for making the hemostatic compositions, and methods for using the hemostatic compositions are disclosed.
    Type: Grant
    Filed: May 7, 1998
    Date of Patent: May 2, 2000
    Assignee: Genzyme Corporation
    Inventors: Keith E. Greenawalt, Julia B. Gershkovich
  • Enteric-coated pharmaceutical compositions of mycophenolate
    Patent number: 6025391
    Abstract: Disclosed are pharmaceutical compositions which have been modified to release pharmaceutically acceptable mycophenolate salts in the upper part of the intestinal tract and methods of treatment using the pharmaceutical compositions.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: February 15, 2000
    Assignee: Novartis AG
    Inventors: Barbara Haeberlin, Ching-Pong Mak, Armin Meinzer, Jacky Vonderscher
  • Pharmaceutical compositions containing dipyridamole or mopidamol and acetylsalicylic acid or the physiologically acceptable salts thereof, processes for preparing them and their use in treating clot formation
    Patent number: 6015577
    Abstract: The specification describes a pharmaceutical combination consisting of dipyridamole or mopidamol and acetylsalicylic acid or the physiologically acceptable salts thereof, processes for preparing this pharmaceutical combination and the use thereof for the controlled prevention of clot formation.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: January 18, 2000
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eisert, Peter Gruber