Claims for Patent: 4,591,592
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Summary for Patent: 4,591,592
| Title: | Acid stabilized compositions of thieno-pyridine derived compounds |
| Abstract: | A novel pharmaceutical composition which comprises an acid salt of a thieno-pyridine derived compound, a pharmaceutically acceptable, non-volatile organic acid (particularly citric acid) and optionally other suitable pharmaceutical excipients. |
| Inventor(s): | Chowhan; Zaka-ud-Din T. (Sunnyvale, CA) |
| Assignee: | Syntex (U.S.A.) Inc. (Palo Alto, CA) |
| Application Number: | 06/665,675 |
| Patent Claims: |
1. A stable pharmaceutical composition comprising a therapeutically effective amount of an active ingredient which is a pharmaceutically acceptable acid addition salt (PASS) of a
compound having the formula ##STR2## wherein: R is phenyl or benzyl, each optionally substituted on the phenyl ring with 1 to 3 halogen atoms, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy or nitro;
R.sub.1 is hydrogen, halogen, hydroxy or alkyl having 1-6 carbon atoms; R.sub.2 is hydrogen or halogen; and n is 1 or 2, and when n is 2, R.sub.1 may have different meanings in each (CHR.sub.1) radical and a non-toxic stabilizing amount of a pharmaceutically, non-volatile acidic compound which is ascorbic acid, benzoic acid, citric acid, fumaric acid, or tartaric acid and at least one pharmaceutically acceptable excipient. 2. The composition of claim 1 wherein said acidic compound is present in an amount of 0.5-5.0% (w/w) relative to the active ingredient. 3. The composition of claim 3 wherein said compound is the hydrochloride salt of 5-(2-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine said acid is citric acid and is present in an amount of 1-1.5% (w/w). 4. A pharmaceutical composition which comprises 40-90% by weight of a pharmaceutically acceptable acid addition salt of a thieno-pyridine derived compound; 0.5-5% by weight of a pharmaceutically acceptable, non-volatile organic acid which is ascorbic acid, benzoic acid, citric acid, fumaric acid, or tartaric acid; 0.2-5% by weight of a pharmaceutically acceptable lubricant; 5-15% by weight of a pharmaceutically acceptable disintegrant; 1-5% by weight of a pharmaceutically acceptable binder and the remainder a pharmaceutically acceptable diluent. 5. The composition of claim 4 wherein the compound is the hydrochloride salt of 5-(2-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine, said acid is citric acid, and said lubricant is magnesium stearate. |
