Optimal polymer mixtures for gastric retentive tablets
DC CAFC
First Claim
1. A controlled-release tablet for releasing a drug into at least a portion of a region defined by the stomach and the upper gastrointestinal tract, said tablet comprising a solid monolithic matrix with said drug dispersed therein, said matrix comprising a combination of poly(ethylene oxide) and hydroxypropyl methylcellulose at a weight ratio that causes said matrix to swell upon contact with gastric fluid to a size large enough to provide gastric retention, wherein;
- said drug has a solubility in water that exceeds one part of said drug per ten parts of water, by weight, and wherein;
said poly(ethylene oxide) has a viscosity average molecular weight of from about 2,000,000 to about 10,000,000 daltons, and wherein said hydroxypropyl methylcellulose has a viscosity of from about 4,000 centipoise to about 200,000 centipoise, measured as a 2% solution in water.
7 Assignments
Litigations
2 Petitions
Accused Products
Abstract
Unit dosage form tablets for the delivery of pharmaceuticals are formed of the pharmaceutical dispersed in a solid unitary matrix that is formed of a combination of poly(ethylene oxide) and hydroxypropyl methylcellulose. The combination offers unique benefits in terms of release rate control and reproducibility while allowing both swelling of the tablet to effect gastric retention and gradual disintegration of the tablet to clear the tablet from the gastrointestinal tract after release of the drug has occurred.
267 Citations
19 Claims
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1. A controlled-release tablet for releasing a drug into at least a portion of a region defined by the stomach and the upper gastrointestinal tract, said tablet comprising a solid monolithic matrix with said drug dispersed therein, said matrix comprising a combination of poly(ethylene oxide) and hydroxypropyl methylcellulose at a weight ratio that causes said matrix to swell upon contact with gastric fluid to a size large enough to provide gastric retention, wherein;
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said drug has a solubility in water that exceeds one part of said drug per ten parts of water, by weight, and wherein;
said poly(ethylene oxide) has a viscosity average molecular weight of from about 2,000,000 to about 10,000,000 daltons, and wherein said hydroxypropyl methylcellulose has a viscosity of from about 4,000 centipoise to about 200,000 centipoise, measured as a 2% solution in water. - View Dependent Claims (2, 3, 4, 5, 10, 11, 12, 13, 14, 15, 16, 18)
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6. A controlled-release tablet for releasing a drug into at least a portion of a region defined by the stomach and the upper gastrointestinal tract, said tablet comprising a solid monolithic matrix with said drug dispersed therein, said matrix comprising a combination of poly(ethylene oxide) and hydroxypropyl methylcellulose at a weight ratio that causes said matrix to swell upon contact with gastric fluid to a size large enough to provide gastric retention, wherein;
said drug has a solubility in water that is less than one part of said drug per ten parts of water, by weight, said poly(ethylene oxide) has a viscosity average molecular weight of from about 100,000 to about 5,000,000 daltons, and said hydroxypropyl methylcellulose has a viscosity of from about 1,000 centipoise to about 100,000 centipoise, measured as a 2% solution in water. - View Dependent Claims (7, 8, 9, 17, 19)
Specification
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- Resources
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Current AssigneeAssertio Therapeutics, Inc. (Assertio Holdings, Inc.)
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Original AssigneeDepomed Incorporated (Assertio Holdings, Inc.)
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InventorsBerner, Bret, Gusler, Gloria, Chau, Mei, Padua, Aimee
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Primary Examiner(s)Webman, Edward J.
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Application NumberUS10/029,134Publication NumberTime in Patent Office908 DaysField of Search424/486, 424/480, 424/468, 424/488, 514/866, 514/635, 514/722.3, 514/781US Class Current424/468CPC Class CodesA61K 9/0065 Forms with gastric retentio...A61K 9/2031 obtained otherwise than by ...A61K 9/2054 Cellulose; Cellulose deriva...A61P 1/00 Drugs for disorders of the ...A61P 1/04 for ulcers, gastritis or re...A61P 1/06 Anti-spasmodics, e.g. drugs...A61P 31/04 Antibacterial agentsA61P 35/00 Antineoplastic agents
