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Claims for Patent: 5,356,896

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Claims for Patent: 5,356,896

Title: Stabilized pharmaceutical compositions comprising an HMG-CoA reductase inhibitor compound
Abstract:A pharmaceutical dosage form comprising an HMG-CoA reductase inhibitor compound, e.g., fluvastatin sodium, is disclosed which is stabilized against pH-related degradation by an alkaline stabilizing medium capable of imparting a pH of at least 8 to an aqueous solution or dispersion of the composition.
Inventor(s): Kabadi; Mohan B. (Marlboro, NJ), Vivilecchia; Richard V. (Rockaway, NJ)
Assignee: Sandoz Ltd. (Basel, CH)
Application Number:07/995,252
Patent Claims: 1. A pharmaceutical composition comprising an HMG-CoA reductase inhibitor compound of the formula: ##STR4## wherein R is an organic radical,

X is --CH.dbd.CH--, and

M is a physiologically acceptable cation,

and an alkaline stabilizing medium capable of imparting a pH of at least 8 to an aqueous solution or dispersion of the composition wherein the alkaline stabilizing medium comprises at least one pharmaceutically acceptable carbonate salt.

2. A pharmaceutical composition according to claim 1 wherein R is selected from the group consisting of indolyl, pyrimidinyl, indenyl, pyridinyl and quinolinyl radicals and derivatives thereof, and X is (E)--CH.dbd.CH--.

3. A pharmaceutical composition according to claims 2 wherein the pharmaceutically acceptable carbonate salt is selected from the group consisting of sodium carbonate, sodium bicarbonate, calcium carbonate and mixtures thereof.

4. A pharmaceutical composition according to claim 1 wherein the alkaline stabilizing medium comprises a mixture of a water soluble carbonate and a water insoluble or sparingly soluble carbonate.

5. A pharmaceutical composition according to claim 4 wherein the ratio of water soluble carbonate to water insoluble or sparingly soluble carbonate is from 1:40 to 2:1.

6. A pharmaceutical composition comprising the HMG-CoA reductase inhibitor fluvastatin sodium and a pharmaceutically acceptable alkaline stabilizing medium capable of imparting a pH of at least 8 to an aqueous solution or dispersion of the composition.

7. A pharmaceutical composition according to claim 6 wherein the alkaline stabilizing medium comprises at least one pharmaceutically acceptable carbonate salt.

8. A pharmaceutical composition according to claim 7 wherein the pharmaceutically acceptable carbonate salt is selected from the group consisting of sodium carbonate, sodium bicarbonate, calcium carbonate and mixtures thereof.

9. A pharmaceutical composition according to claim 8 comprising fluvastatin sodium, (i) calcium carbonate and (ii) sodium carbonate or sodium bicarbonate.

10. A pharmaceutical composition according to claims 1, 3, or 8 which comprises 0.5 to 60 wt. % HMG-CoA reductase inhibitor compound, 0.5 to 40 wt. % calcium carbonate, 0.5 to 20 wt. % sodium bicarbonate, and 10 to 65 wt. % microcrystalline cellulose.

11. A pharmaceutical composition according to claims 2 or 6 in solid unit dosage form.

12. An oral pharmaceutical composition suitable for excapsulation for delivering fluvastatin sodium which comprises 0.5 to 60 wt. % of fluvastatin sodium,

25 to 40 wt. % of calcium carbonate,

0.5 to 10 wt. % of sodium bicarbonate, and

20 to 35 wt. % of microcrystalline cellulose.

13. An oral pharmaceutical composition suitable for tableting for delivering fluvastatin sodium which comprises

0.5 to 60 wt. % of fluvastatin sodium,

5 to 20 wt. % of calcium carbonate,

5 to 20 wt. % of sodium bicarbonate, and

50 to 65 wt. % of microcrystalline cellulose.

14. A composition according to claim 12 wherein the capsule is coated with an enteric and/or film coating.

15. A composition according to claim 13 wherein the tablet is coated with an enteric and/or film coating.

16. A composition according to claim 12 wherein fluvastatin sodium is present in a dosage amount selected from the group consisting of 5, 10, 15, 20 and 40 mg. amounts.

17. A composition according to claim 13 wherein fluvastatin sodium is present in a dosage amount selected from the group consisting of 5, 10, 15, 20 and 40 mg. amounts.

18. A composition according to claims 2 or 8 wherein the HMG-CoA reductase inhibitor compound and the pharmaceutically acceptable carbonate salt are in intimate contacting association.

19. A method of preparing the composition of claims 2 or 8 which comprises bringing the HMG-CoA reductase inhibitor compound and the alkaline stabilizing medium into intimate contacting association by co-lyophilizing the HMG-CoA reductase inhibitor compound and the alkaline stabilizing medium.

20. A pharmaceutical composition according to claim 2 wherein the HMG-CoA reductase inhibitor compound is a pharmaceutically acceptable salt of erythro-3R,5S-(E)-7-[4-fluorophenyl-6-(1-methylethyl)-2-(dimethylamino-pyr imidin-5-yl)-3,5-dihydroxy-6-heptenoic acid, or its racemate.

21. A pharmaceutical composition according to claim 2 wherein the HMG-CoA reductase inhibitor compound is a pharmaceutically acceptable salt of erythro-3R,5S-(E)-dimethoxy-7-[3'-(4"-fluorophenyl)-spiro[cyclopentane-1,1 '(1H)-inden]-2'-yl]-3-hydroxyhept-6-enoic acid, or racemate.

22. A pharmaceutical composition according to claim 2 wherein the HMG-CoA reductase inhibitor compound is a pharmaceutically acceptable salt of erythro-3R,5S-(E)-7-[4-(4-fluorophenyl)-2,6-bis(1-methylethyl)-5-methoxyme thyl-pyridin-3-yl]-3,5-dihydroxy-6-heptenoic acid, or its racemate.

23. A pharmaceutical composition according to claim 2 wherein the HMG-CoA reductase inhibitor compound is a pharmaceutically acceptable salt of erythro-(.+-.)-(E)-[4-(4-fluorophenyl)-2-(1-methylethyl)-6-phenyl-pyridin- 3-yl]-3,5- dihydroxy-6-heptenoic acid, or its 3R,5S isomer.

24. A pharmaceutical composition according to claim 2 wherein the HMG-CoA reductase inhibitor compound is a pharmaceutically acceptable salt of erythro-(.+-.)-(E)-7-[4-(4-fluorophenyl)-2-(1-methylethyl)-quinolin-3-yl]- 3,5-dihydroxy-6- heptenoic acid, or its 3R,5S isomer.

25. A pharmaceutical composition according to claim 2 wherein the HMG-CoA reductase inhibitor compound is a pharmaceutically acceptable salt of erythro-(.+-.)-(E)-7-[4-(4-fluorophenyl)-2-cyclopropyl-quinolin-3-yl]-3,5- dihydroxy-6-heptenoic acid, or its 3R, 5S isomer.

26. A pharmaceutical composition according to claim 2 which comprises erythro-(E)-3R,5S-7-[3-(4-fluorophenyl)-1-(1-methylethyl)-1H-indol-2-yl]-3 ,5-dihydroxy-6-heptenoic acid, sodium salt.

27. A pharmaceutical composition according to claims 2 or 7 which comprises 0.5 to 60 wt. % HMG-CoA reductase compound, 10 to 55 wt. % pharmaceutically acceptable carbonate salts, and 10 to 65 wt. % filler.
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