Claims for Patent: 4,798,725

Summary for Patent: 4,798,725

Title:	Sustained release capsule
Abstract:	The invention involves a sustained release pharmaceutical capsule for oral administration comprising, in a capsule shell, a particulate mixture comprising an active drug ingredient which is a weak acid, neutral, or a weak base, polyvinylpyrrolidone, and carboxyvinylpolymer.
Inventor(s):	Patel; Vikram S. (Norwich, NY)
Assignee:	Norwich Eaton Pharmaceuticals, Inc. (Norwich, NY)
Application Number:	06/874,732
Patent Claims:	1. A sustained release pharmaceutical capsule for oral administration comprising a particulate mixture, in a capsule shell which is soluble in a gastrointestinal juice, said particulate mixture comprising: (a) from about 0.01% to about 90% of an active drug ingredient which is a weak acid, neutral, or a weak base; (b) from about 5% to about 96% of polyvinylpyrrolidone; and (c) from about 4% to about 40% of carboxyvinylpolymer; wherein said polyvinylpyrrolidone and said carboxyvinylpolymer occur substantially entirely in separate particles of said particulate mixture. 2. The capsule of claim 1 wherein said particulate mixture comprises from about 10% to about 70% of polyvinylpyrrolidone. 3. The capsule of claim 1 wherein said particulate mixture comprises from about 15% to about 60% of polyvinylpyrrolidone. 4. The capsule of claim 2 wherein said particulate mixture comprises from about 5% to about 25% of carboxyvinylpolymer. 5. The capsule of claim 3 wherein said particulate mixture comprises from about 10% to about 70% of said active drug ingredient and from about 5% to about 15% of carboxyvinylpolymer. 6. The capsule of claim 2 wherein said particulate mixture comprises from about 10% to about 70% of said active drug ingredient and from about 7% to about 10% of carboxyvinylpolymer. 7. The capsule of claim 4 wherein said carboxyvinylpolymer has a molecular weight of at least about 1,250,000, and said capsule shell is a hard gelatin capsule shell which is soluble in gastric juice. 8. The capsule of claim 5 wherein said carboxyvinylpolymer has a molecular weight of about 3,000,000 and is a polyacrylic acid cross-linked with about 1% of polyallyl sucrose having an average of about 5.8 allyl groups for each molecule of sucrose. 9. The capsule of claim 6 wherein said carboxyvinylpolymer has a molecular weight of about 3,000,000 and is a polyacrylic acid cross-linked with about 1% of polyallyl sucrose having an average of about 5.8 allyl groups for each molecule of sucrose. 10. The capsule of claim 8 wherein said polyvinylpyrrolidone has a molecular weight of from about 7,000 to about 700,000. 11. A process for producing a sustained release pharmaceutical capsule for oral administration comprising the steps of: (1) preparing a particulate mixture, said particulate mixture comprising: (a) from about 0.01% to about 90% of an active drug ingredient which is a weak acid, neutral, or a weak base; (b) from about 5% to about 96% of polyvinylpyrrolidone; and (c) from about 4% to about 40% of carboxyvinylpolymer; wherein said polyvinylpyrrolidone and said carboxyvinylpolymer occur substantially entirely in separate particles of said particulate mixture. (2) filling said particulate mixture into a capsule shell which is soluble in a gastrointestinal juice. 12. The process of claim 11 wherein said particulate mixture comprises from about 10% to about 70% of said active drug ingredient, from about 10% to about 70% of polyvinylpyrrolidone, and from about 5% to about 15% of carboxyvinylpolymer. 13. The process of claim 12 wherein said carboxyvinylpolymer has a molecular weight of at least about 1,250,000, and said capsule shell is a hard gelatin capsule shell which is soluble in gastric juice. 14. The process of claim 11 wherein said particulate mixture comprises from about 10% to about 70% of said active drug ingredient, from about 10% to about 70% of polyvinylpyrroline having a molecular weight of from about 7,000 to about 700,000, and from about 7% to about 10% of carboxyvinylpolymer having a molecular weight of about 3,000,000, said carboxyvinylpolymer being a polyacrylic acid cross-linked with about 1% of polyallyl sucrose having an average of about 5.8 allyl groups for each molecule of sucrose.