Sustained release capsule

Claim 2

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 0.01% to 90% of an active drug ingredient which is a weak acid, neutral, or a weak base; (b) from 5% to 96% of polyvinylpyrrolidone; and (c) from 4% to 40% of carboxyvinylpolymer; wherein said polyvinylpyrrolidone and said carboxy­vinylpolymer occur substantially entirely in separate particles of said particulate mixture.

Claim 3

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 0.01% to 90% of an active drug ingredient which is a weak acid, neutral, or a weak base; (b) from 5% to 96% of polyvinylpyrrolidone; and (c) from 4% to 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.

Claim 4

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 0.01% to 90% of an active drug ingredient which is a weak acid, neutral, or a weak base; (b) from 5% to 96% of polyvinylpyrrolidone; and (c) from 4% to 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.

Claim 5

A capsule of Claim 1 or process of Claim 2, wherein said first particulate mixture comprises from 10% to 70% of said first active drug ingredient, from 10% to 70% of polyvinylpyrrol­idone and from 5% to 25% of carboxyvinylpolymer.

Claim 6

A capsule or process of Claim 3 wherein said carboxy­vinylpolymer has a molecular weight of at least 1,250,000, and said capsule shell is a hard gelatin capsule shell which is soluble in gastric juice.

Claim 7

A process or capsule of Claim 3 or Claim 4 wherein said particulate mixture comprises polyvinylpyrrolidone having a molecular weight of from 7,000 to 700,000, and from 7% to 10% of carboxyvinylpolymer having a molecular weight of 3,000,000, said carboxyvinylpolymer being a polyacrylic acid cross-linked with 1% of polyallyl sucrose having an average of 5.8 allyl groups for each molecule of sucrose.

Claim 8

A combination sustained release/rapid release pharma­ceutical capsule for oral administration comprising, in a capsule shell which is soluble in a gastrointestinal juice: (1) a first layer of a first particulate mixture comprising: (a) from 0.01% to 90% of a first active drug ingredient which is a weak acid, neutral, or a weak base; (b) from 5% to 96% of polyvinylpyrrolidone; and (c) from 4% to 40% of carboxyvinylpolymer; wherein said polyvinylpyrrolidone and said car­boxyvinylpolymer occur substantially entirely in separate particles of said first particulate mixture; (2) a second layer of a second particulate mixture comprising a second active drug ingredient.

Claim 9

A combination sustained release/rapid release pharma­ceutical capsule for oral administration comprising, in a capsule shell which is soluble in a gastrointestinal juice: (1) a first layer of a first particulate mixture comprising: (a) from 0.01% to 90% of a first active drug ingredient which is a weak acid, neutral, or a weak base; (b) from 5% to 96% of polyvinylpyrrolidone; and (c) from 4% to 40% of carboxyvinylpolymer; wherein said polyvinylpyrrolidone and said car­boxyvinylpolymer occur substantially entirely in separate particles of said first particulate mixture; (2) a second layer of a second particulate mixture comprising a second active drug ingredient.

Claim 10

A process for producing a combination sustained release/rapid release pharmaceutical capsule for oral administration comprising the steps of: (1) preparing a first particulate mixture comprising: (a) from 0.01% to 90% of a first active drug ingredient which is a weak acid, neutral, or a weak base; (b) from 5% to 96% of polyvinylpyrrolidone; and (c) from 4% to 40% of carboxyvinylpolymer; wherein said polyvinylpyrrolidone and said car­boxyvinylpolymer occur substantially entirely in separate particles of said first particulate mixture; (2) preparing a second particulate mixture comprising a second active drug ingredient; and (3) filling, into a capsule shell which is soluble in a gastrointestinal juice, a first layer of said first particulate mixture, and a second layer of said second particulate mixture.

Claim 11

A process for producing a combination sustained release/rapid release pharmaceutical capsule for oral administration comprising the steps of: (1) preparing a first particulate mixture comprising: (a) from 0.01% to 90% of a first active drug ingredient which is a weak acid, neutral, or a weak base; (b) from 5% to 96% of polyvinylpyrrolidone; and (c) from 4% to 40% of carboxyvinylpolymer; wherein said polyvinylpyrrolidone and said car­boxyvinylpolymer occur substantially entirely in separate particles of said first particulate mixture; (2) preparing a second particulate mixture comprising a second active drug ingredient; and (3) filling, into a capsule shell which is soluble in a gastrointestinal juice, a first layer of said first particulate mixture, and a second layer of said second particulate mixture.

Claim 12

A capsule of Claim 6 or process of Claim 7 wherein said first particulate mixture comprises from 10% to 70% of said first active drug ingredient, from 10% to 70% of polyvinylpyrrolidone, and from 5% to 25% of carboxyvinylpolymer.

Claim 13

A capsule or process of Claim 8 wherein said first and second active drug ingredients are the same active drug ingredi­ent, said carboxyvinylpolymer has a molecular weight of at least 1,250,000, and said capsule shell is a hard gelatin capsule shell which is soluble in gastric juice.

Claim 14

A capsule or process of Claim 8 or Claim 9 wherein said first particulate mixture comprises said polyvinylpyrrolidone having a molecular weight of from 7,000 to 700,000, and from 7% to 10% of carboxyvinylpolymer having a molecular weight of 3,000,000, said carboxyvinylpolymer being a polyacrylic acid cross-linked with 1% of polyallyl sucrose having an average of 5.8 allyl groups for each molecule of sucrose.