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Details for Patent: 4,490,377

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Details for Patent: 4,490,377

Title: Acid stabilized compositions of thieno-pyridine derived compounds
Abstract:A stable pharmaceutical composition which comprises an acid salt of a thieno-pyridine derived compound, a pharmaceutically acceptable, non-volatile 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)
Filing Date:May 10, 1982
Application Number:06/376,878
Claims:1. A stable pharmaceutical composition comprising a therapeutically effective amount of an active ingredient which is a pharmaceutically acceptable acid addition salt (PAAS) 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 meaning in each (CHR.sub.1) radical and a non-toxic stabilizing amount of a pharmaceutically acceptable non-volatile acidic compound which is cinnamic acid, glycolic acid, malonic acid, or mandelic 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 2 wherein said compound is the hydrochloride salt of 5-(2-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine and said acid 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 cinnamic acid, glycolic acid, malonic acid, malic acid or mandelic 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 and said lubricant is magnesium stearate.

6. A process for preventing degradation of a pharmaceutically acceptable acid addition salt of a compound chosen from those represented by the formula ##STR3## 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 meaning in each (CHR.sub.1) radical when formulated into dry compositions which process comprises adding a pharmaceutically acceptable non-volatile organic acid which is cinnamic acid, glycolic acid, malonic acid, malic acid, or mandelic acid to said composition during the formulation thereof.

7. The process of claim 6 wherein said acidic compound is present in an amount of 0.5-5.0% (w/w) relative to the active ingredient.

8. The process of claim 7 wherein said active ingredient is the hydrochloride salt of 5-(2-chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine and said acid is present in an amount between 1-1.5% (w/w).

9. The process of claim 8 wherein there is a plurality of excipients which include a disintegrant, a lubricant, a binder and a diluent.

10. The process of claim 9 wherein the lubricant is magnesium stearate, the disintegrant is corn starch, the binder is povidone, and the diluent is lactose.
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