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Claims for Patent: 5,731,000

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Claims for Patent: 5,731,000

Title: Stabilized pharmaceutical composition containing bupropion
Abstract:This application discloses a method of inhibiting degradation of the antidepressant bupropion hydrochloride in a solid pharmaceutical formulation, so that the pharmaceutical formulation will maintain at least 80% of its initial bupropion potency after one year.
Inventor(s): Ruff; Michael David (Greenville, NC), Kalidindi; Sanyasi Raju (Edison, NJ), Sutton, Jr.; Joel Elmore (Greenville, NC)
Assignee: Glaxo Wellcome Inc. (Rtp, NC)
Application Number:08/586,916
Patent Claims: 1. A pharmaceutical composition in solid form comprising bupropion hydrochloride and a pharmaceutically acceptable stabiliser in an effective stabilising mount, in which the composition contains at least about 80% w/w of undegraded bupropion hydrochloride after storage for 6 weeks at about 40.degree. C. and 75% relative humidity and in which an aqueous solution of the stabiliser in a concentration of about 6% w/w has a pH of about 0.9 to about 4, the stabiliser being selected from an organic acid, a carboxylic acid, an acid salt of an amino acid and sodium metabisulphite.

2. A pharmaceutical composition in solid form comprising bupropion hydrochloride and a pharmaceutically acceptable stabiliser in an effective stabilising mount, in which the composition contains at least about 80% w/w of undegraded bupropion hydrochloride after storage for 6 weeks at about 50.degree. C. and 27% relative humidity and in which an aqueous solution of the stabiliser in a concentration of about 6% w/w has a pH of about 0.9 to about 4, the stabiliser being selected from an organic acid, a carboxylic acid other than ascorbic acid and isoascorbic acid, an acid salt of an amino acid and sodium metabisulphite.

3. A pharmaceutical composition according to claim 1, wherein the aqueous solution of the stabiliser has a pH of about 0.9 to 2.

4. A pharmaceutical composition according to claim 1, wherein the aqueous solution of the stabiliser has a pH of around 1.

5. A pharmaceutical composition according to claim 1 which contains at least 95% w/w of undegraded bupropion hydrochloride.

6. A pharmaceutical composition according to claim 1, wherein the amount of stabiliser is 2.7% to 27% of the weight of bupropion hydrochloride in the composition.

7. A pharmaceutical composition according to claim 2, wherein the amount of stabiliser is 5% to 16.2% of the weight of bupropion hydrochloride in the composition.

8. A pharmaceutical composition according to claim 1, wherein the acid salt of the amino acid is cysteine hydrochloride, glycine hydrochloride or cystine dihydrochloride.

9. A pharmaceutical composition according to claim 1, wherein the organic acid is tartaric acid, citric acid or malic acid.

10. A pharmaceutical composition according to claim 1 wherein the carboxylic acid is ascorbic acid or isoascorbic acid.

11. A tablet or capsule according to claim 1, wherein the mount of bupropion hydrochloride is 50, 75, 100 or 150 mg.

12. A method of stabilising bupropion hydrochloride in a solid pharmaceutical composition so that at least about 80% w/w of bupropion hydrochloride is present in the undegraded form after storage for 6 weeks at about 40.degree. C. and 75% relative humidity, wherein said method comprises mixing bupropion hydrochloride with a stabiliser of which an aqueous solution in a concentration of about 6% w/w has a pH of about 0.9 to about 4, the stabiliser being selected from an organic acid, a carboxylic acid, an acid salt of an amino acid and sodium metabisulfite.

13. A method of stabilising bupropion hydrochloride in a solid pharmaceutical composition so that at least about 80% w/w of bupropion hydrochloride is present in the undegraded from after storage for 6 weeks at about 50.degree. C. and 27% relative humidity, wherein said method comprises mixing bupropion hydrochloride with a stabiliser of which an aqueous solution in a concentration of about 6% w/w has a pH of about 0.9 to about 4, the stabiliser being selected from an organic acid, a carboxylic acid other than ascrobic acid or isoascrobic acid, an acid salt of an amino acid and sodium metabisulfite.

14. A pharmaceutical composition according to claim 2, wherein the aqueous solution of the stabiliser has a pH of about 0.9 to 2.

15. A pharmaceutical composition according to claim 2, wherein the aqueous solution of the stabiliser has a pH of around 1.

16. A pharmaceutical composition according to claim 2 which contains at least 95% w/w of undegraded bupropion hydrochloride.

17. A pharmaceutical composition according to claim 2, wherein the acid salt of the acid is cysteine hydrochloride, glycine hydrochloride or cystine dihydrochloride.

18. A pharmaceutical composition according to claim 2, wherein the organic acid is tartaric acid, citric acid or malic acid.

19. A pharmaceutical composition according to claim 2 wherein the carboxylic acid is ascorbic acid or isoascorbic acid.

20. A tablet or capsule according to claim 2, wherein the amount of bupropion hydrochloride is 50, 75, 100 or 150 mg.

21. A pharmaceutical composition according to claim 1, wherein

the aqueous solution of the stabiliser has a pH of about 0.9 to 2;

the composition contains at least 95% w/w of undegraded bupropion hydrochloride;

the amount of stabiliser is 2.7% to 27% of the weight of bupropion hydrochloride in the composition;

the acid salt of the amino acid is cysteine hydrochloride, glycine hydrochloride or cystine dihydrochloride;

the organic acid is tartaric acid, citric acid or malic acid;

the carboxylic acid is ascorbic acid or isoascorbic acid; and wherein

the amount of bupropion hydrochloride is 50, 75, 100 or 150 mg.

22. A pharmaceutical composition according to claim 2, wherein the aqueous solution of the stabiliser has a pH of about 0.9 to 2;

the composition contains at least 95% w/w of undegraded bupropion hydrochloride;

the amount of stabiliser is 2.7% to 27% of the weight of bupropion hydrochloride in the composition;

the acid salt of the amino acid is cysteine hydrochloride, glycine hydrochloride or cystine dihydrochloride;

the organic acid is tartaric acid, citric acid or malic acid;

the carboxylic acid is ascorbic acid or isoascorbic acid; and wherein

the amount of bupropion hydrochloride is 50, 75, 100 or 150 mg.
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