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|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)|
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.
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