Claims for Patent: 5,763,493

Summary for Patent: 5,763,493

Title:	Stabilized pharmaceutical
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 D. (Greenville, NC), Kalidindi; Sanvasi R. (Edison, NJ), Sutton, Jr.; Joel Elmore (Greenville, NC)
Assignee:	Glaxo Wellcome Inc. (Research Triangle Park, NC)
Application Number:	08/667,239
Patent Claims:	1. A pharmaceutical composition in solid form comprising bupropion hydrochloride and a pharmaceutically acceptable stabiliser in an effective stabilising amount, 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 the group consisting of L-cysteine hydrochloride, glycine hydrochloride, malic acid, sodium metabisulfite, citric acid, tartaric acid and L-cystine dihydrochloride. 2. A pharmaceutical composition according to claim 1, wherein the aqueous solution of the stabiliser has a pH of about 09. to 2. 3. A pharmaceutical composition according to claim 1, wherein the aqueous solution of the stabiliser has a pH of around 1. 4. A pharmaceutical composition according to claim 1, 2 or 3 which contains at least about 90% w/w of undegraded bupropion hydrochloride after storage for 6 weeks. 5. A pharmaceutical composition according to claims 1, 2 or 3 which contains at least 95% w/w of undegraded bupropion hydrochloride. 6. A pharmaceutical composition according to claims 1, 2 or 3 which contains at least 98% w/w of undegraded bupropion hydrochloride. 7. A pharmaceutical composition according to claims 1, 2 or 3, wherein the amount of stabiliser is 2.7% to 27% of the weight of bupropion hydrochloride in the composition. 8. A pharmaceutical composition according to claims 1, 2 or 3, wherein the amount of stabiliser is 5% to 16.2% of the weight of bupropion hydrochloride in the composition. 9. A tablet or capsule containing a composition according to claims 1, 2, or 3, wherein the amount of bupropion hydrochloride is 25 to 500 mg. 10. A tablet or capsule containing a composition according to claims 1, 2, or 3, wherein the amount of bupropion hydrochloride is 25 to 300 mg. 11. A tablet or capsule containing a composition according to claim 1, 2, or 3, wherein the amount of bupropion hydrochloride is 50, 75, 100 or 150 mg. 12. A method of stabilizing 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 the group consisting of L-cysteine hydrochloride, glycine hydrochloride, malic acid, sodium metabisulfite, citric acid, tartaric acid and L-cystine dihydrochloride.