Claims
- 1. The method of preparing an oral antidiabetic pharmaceutical composition containing an antidiabetic benzoic acid as the active ingredient, which comprises dissolving
- (a) an acidic antidiabetic benzoic acid with a basic excipient, or
- (b) an amphoteric antidiabetic benzoic acid with a basic or acidic excipient, or
- (c) a basic antidiabetic benzoic acid with an acidic excipient
- and polyvinylpyrrolidone in an inert polar solvent, where the molar ratio of benzoic acid to basic or acidic excipient is less than 1:1 and the ratio of benzoic acid to polyvinylpyrrolidone is from about 1:0.5 to 1:10 parts by weight, and evaporating the resulting solution to dryness.
- 2. The method of claim 1, where said benzoic acid is -Ethoxy-4-{2-oxo-2-[(.alpha.-isobutyl-2-piperidino-benzyl)-amino]ethyl}-benzoic acid.
- 3. The method of claim 1, where said benzoic acid is -[N-(.alpha.-phenyl-2-piperidino-benzyl)-aminocarbonylmethyl]benzoic acid.
- 4. The method of claim 1, where said benzoic acid is 4-[N-(2-Piperidino-.alpha.-propylbenzyl)-carbamoylmethyl]benzoic acid.
- 5. The method of claim 1, where said basic excipient is ethylenediamine or L-lysine, and said acidic excepient is sulfuric acid, phosphoric acid or tartaric acid.
- 6. The method of claim 1, which comprises dissolving 2-Ethoxy-4-{2-oxo-2-[(.alpha.-isobutyl-2-piperidino-benzyl)-amino]ethyl}-benzoic acid with a basic or acidic excipient in an inert polar solvent, where the molar ratio of said benzoic acid to basic or acidic excipient is less than 1:1, dissolving polyvinylpyrrolidone in the resulting solution, the ratio of said benzoic acid to polyvinylpyrrolidone being about 0.5 to 1:10 parts by weight, and evaporating the solution thus obtained to dryness.
- 7. The method of claim 1, where the molar ratio of said benzoic acid to basic or acidic excipient is about 1:1.1 to 110.
- 8. The method of claim 1, where said conventional pharmaceutical excipient includes an additional solubilizing agent.
- 9. An oral antidiabetic pharmaceutical composition consisting essentially of a conventional pharmaceutical excipient and the evaporation residue of a solution of an effective antidiabetic amount of an acidic, amphoteric or basic antidiabetic benzoic acid, a basic or acidic excipient and polyvinylpyrrolidone in an inert polar solvent, where the molar ratio of benzoic acid to basic or acidic excipient is less than 1:1 and the ratio of benzoic acid to polyvinylpyrrolidone is about 1:0.5 to 1:10 by weight.
- 10. A composition of claim 9, where said benzoic acid is 2-Ethoxy-4-{2-oxo-2-[(.alpha.-isobutyl-2-piperidino-benzyl)-amino]-ethyl}-benzoic acid.
- 11. A composition of claim 9, where said benzoic acid is 4-[N-(.alpha.-phenyl-2-piperidino-benzyl)-aminocarbonylmethyl]benzoic acid.
- 12. A composition of claim 9, where said benzoic acid is 4-[N-(2-Piperidino-.alpha.-propylbenzyl)-carbamoylmethyl]benzoic acid.
- 13. A composition of claim 9, where said basic excipient is ethylenediamine or L-lysine, and said acidic excepient is sulfuric acid, phosphoric acid or tartaric acid.
- 14. A composition of claim 9, where the molar ratio of said benzoic acid to basic or acidic excipient is from 1:1.1 to 1:10.
- 15. A composition of claim 9, wherein said conventional pharmaceutical excipient includes additional solubilizing agent.
- 16. The method of claim 1, wherein the evaporation residue is combined with a conventional pharmaceutical excipient to produce the desired oral antidiabetic pharmaceutical composition.
- 17. The method of claim 6 wherein the evaporation residue is combined with a conventional pharmaceutical excipient to produce the desired oral antidiabetic pharmaceutical composition.
Priority Claims (1)
Number |
Date |
Country |
Kind |
3320582 |
Jun 1983 |
DEX |
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Parent Case Info
This is a continuation-in-part of copending application Ser. No. 615,892, filed May 31, 1984 now U.S. Pat. No. 4,696,815, issued Sept. 29, 1987.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
3708481 |
Kufter |
Jan 1973 |
|
4696815 |
Schepky |
Sep 1987 |
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