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Claims for Patent: 4,743,450

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Claims for Patent: 4,743,450

Title: Stabilized compositions
Abstract:The cyclization, hydrolysis, and coloration of certain ACE inhibitors is minimized when they are formulated with a metal-containing stabilizer and a saccharide.
Inventor(s): Harris; Michael (Hackettstown, NJ), Hokanson; Gerard (Long Valley, NJ), Murthy; Kuchi (Morris Plains, NJ), Reisch; Robert (Haledon, NJ), Waldman; Frank (Wayne, NJ)
Assignee: Warner-Lambert Company (Morris Plains, NJ)
Application Number:07/017,962
Patent Claims: 1. A pharmaceutical composition which contains:

(a) a drug component which comprises a suitable amount of an ACE inhibitor which is susceptible to cyclization, hydrolysis, and discoloration,

(b) a suitable amount of an alkali or alkaline earth metal carbonate to inhibit cyclization and discoloration, and

(c) a suitable amount of a saccharide to inhibit hydrolysis.

2. The composition of claim 1 wherein (a) is enalapril or a pharmaceutically acceptable acid addition salt thereof.

3. The composition of claim 1 wherein (a) contains at least one additional drug.

4. The composition of claim 1 wherein (b) contains magnesium carbonate.

5. The composition of claim 1 wherein (c) contains at least one of mannitol and lactose.

6. The composition of claim 1 wherein the composition also contains at least one material selected from the group consisting of: binders, disintegrants, and lubricants.

7. The composition of claim 1 wherein (a) is a compound of the formula ##STR2## wherein A is absent, a fused five, six, or seven-membered cycloaliphatic ring or a fused benzene ring which is unsubstituted or substituted by one or two alkoxy groups having one to four carbon atoms; n is zero or one, and R is hydrogen or alkyl having one to five carbon atoms, or a pharmaceutically acceptable acid addition salt thereof.

8. The composition of claim 7 wherein A is absent, a fused five or six-membered cycloaliphatic ring or a fused benzene ring which is unsubstituted or substituted by two methoxy groups; n is zero or one, and R is hydrogen or ethyl, or a pharmaceutically acceptable acid addition salt thereof.

9. The composition of claim 1 wherein (a) is quinapril, or a pharmaceutically acceptable acid addition salt thereof.

10. The composition of claim 1 wherein (a) is quinapril hydrochloride.

11. The composition of claim 1 wherein (a) is indolapril or a pharmaceutically acceptable acid addition salt thereof.

12. A tablet containing the composition of claim 1.

13. A tablet containing the composition of claim 3.

14. A candy formulation containing the composition of claim 1.

15. A candy formulation containing the composition of claim 3.

16. A process for stabilizing an ACE inhibitor drug against cyclization which comprises the step of contacting the drug with:

(a) a suitable amount of an alkali or alkaline earth-metal carbonate and,

(b) one or more saccharides.

17. The process of claim 16 wherein the drug is selected from the group consisting of quinapril, enalapril, and indolapril, or a pharmaceutically acceptable acid addition salt thereof.
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