Nifedipine-containing solid preparation composition

• US 4,412,986 A
• Filed: 04/16/1981
• Issued: 11/01/1983
• Est. Priority Date: 06/07/1977
• Status: Expired due to Term

• Current Assignee: Bayer AG
• Original Assignee: Yamanouchi Pharmaceutical Co., Ltd. (Astellas Pharma Incorporated)
• Inventors: Ohmura, Tadayoshi, Kawata, Hiroitsu, Soeishi, Yoshiaki, Yano, Katsuhiko, Higuchi, Saburo, Matsumura, Mikio
• Primary Examiner(s): Robinson, Douglas W.
• Application Number:
  US06/254,882
• Time in Patent Office: 929 Days
• Field of Search: 424/266, 424/80, 424/362
• US Class Current: 514/356
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/2004 Excipients; Inactive ingredients

Abstract

A novel nifedipine-containing solid pharmaceutical preparation composition comprising a mixture of nifedipine and at least one 1st(a) substance selected from polyvinyl pyrrolidone, methyl cellulose, hydroxypropyl cellulose and hydroxypropylmethyl cellulose; a mixture of nifedipine, at least one 1st(b) substance selected from polyvinyl pyrrolidone, urea, citric acid mannitol, succinic acid, methyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose and amino acid, and at least one 2nd substance selected from a surface active agent, polyethylene glycol, propylene glycol, glycerol, a glycerol fatty acid ester and a vegetable oil; or a mixture of nifedipine, the 1st(b) substance, the 2nd substance and calcium lactate.

The composition of this invention can increase the bioavailability of nifedipine and makes it possible to provide a nifedipine-containing pharmaceutical preparation which has small bulk and can be easily administered.

Claims

1. A nifedipine-containing solid composition comprising a coprecipitate (a) of nifedipine and (b) about 1 to 20 times its weight of a member selected from the group consisting of polyvinylpyrrolidone, methylcellulose, hydroxypropylcellulose and hydroxypropylmethylcellulose.

2. A composition according to claim 1, wherein (b) is present in about 1 to 10 times the weight of (a).

3. A composition according to claim 1, wherein (b) is polyvinylpyrrolidone.

4. A composition according to claim 1, wherein (b) is methylcellulose.

5. A composition according to claim 1, wherein (b) is hydroxypropylcellulose.

6. A composition according to claim 1, wherein (b) is hydroxypropylmethylcellulose.

7. A composition according to claim 1, further containing (c) about 0.1 to 10 parts per part by weight of (a) of at least one compound selected from the group consisting of an anionic surface active agent, a nonionic surface active agent, polyethylene glycol, propylene glycol, glycerol, a glycerol fatty acid ester and a vegetable oil.

8. A composition according to claim 7, wherein (c) is sodium lauryl sulfate.

9. A composition according to claim 7, wherein (c) is polyethylene glycol.

10. A composition according to claim 1, further containing (d) about 0.1 to 10 parts per part by weight of (a) of at least one member selected from the group consisting of aluminum silicate and calcium lactate.

11. A method of effecting coronary vascular dilation with high bioavailability in humans and animals which comprises orally administering a therapeutically effective amount of the composition claimed in claim 1.

12. A method of effecting coronary vascular dilation with high bioavailability in humans and animals which comprises orally administering a therapeutically effective amount of the composition claimed in claim 7.

13. A method of effecting coronary vascular dilation with high bioavailability in humans and animals which comprises orally administering a therapeutically effective amount of the composition claimed in claim 11.

14. A composition according to claim 1 in the form of a tablet of less than 400 mg.

15. A composition according to claim 1 in the form of a tablet of less than 250 mg.