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Claims for Patent: 6,617,328

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Claims for Patent: 6,617,328

Title: Sustained release ranolazine formulations
Abstract:A sustained release ranolazine formulation contains an intimate mixture of ranolazine and a partially neutralized pH-dependent binder to form a film that is mostly insoluble in aqueous media below pH 4.5 and soluble in aqueous media above pH 4.5. The formulation is suitable for twice daily administration of ranolazine and is useful for controlling the rate of dissolution of ranolazine, and to maintain human plasma ranolazine levels at between 550 and 7500 ng base/mL.
Inventor(s): Wolff; Andrew A. (San Francisco, CA), Baker; Fiona (Dunfermline, GB), Langridge; John (Wrexham, GB)
Assignee: CV Therapeutics, Inc (Palo Alto, CA) Syntex (USA), LLC (Palo Alto, CA)
Application Number:10/259,143
Patent Claims: 1. A pharmaceutical dosage form comprising at least about 50 wt % ranolazine and at least one pH dependent binder that inhibits the release of ranolazine from the sustained release dosage form when the sustained release dosage form is subjected to an aqueous environment having a pH of the stomach and that promotes the release of a therapeutic amount of ranolazine in an aqueous solution having a pH above about 4.5.

2. The pharmaceutical dosage form of claim 1 including no more than two tablets per dose.

3. The pharmaceutical dosage form of claim 2 wherein the pharmaceutical dosage form includes from about 50% to about 95% by weight ranolazine.

4. The pharmaceutical dosage form of claim 2 wherein the pharmaceutical dosage form includes from about 70% to about 80% by weight ranolazine.

5. The pharmaceutical dosage form of claim 1 wherein the pH dependent binder is selected from methacrylic acid copolymers, hydroxypropyl cellulose phthalate, hydroxpropyl methycellulose phthalate, cellulose acetate phthalate, polyvinyl acetate, phthalate, polyvinylpyrrolidine phthalate, and mixtures thereof.

6. The pharmaceutical dosage form of claim 1 wherein the pH dependent binder is a methacrylic acid copolyer.

7. The pharmaceutical dosage form of claim 6 wherein the methacrylic acid copolymer is methacrylic acid copolymer Type C USP.

8. The pharmaceutical dosage form of claim 6 wherein pharmaceutical dosage form includes from about 5 to about 12 wt % methacrylic acid copolymer Type C USP.

9. The pharmaceutical dosage form of claim 6 wherein the pharmaceutical dosage form includes about 10 wt % methacrylic acid copolymer.

10. The pharmaceutical dosage form of claim 1 wherein the pharmaceutical dosage form includes a pH-independent binder.

11. The pharmaceutical dosage form of claim 10, wherein the pH-independent binder is selected from hydroxypropyl methylcellulose, hydroxypropyl cellulose, poly(meth)acrylate esters, poly-vinylpyrrolidone, and mixtures thereof.

12. The pharmaceutical dosage form of claim 10 wherein the pH-independent binder is hydroxypropyl methylcellulose.

13. The pharmaceutical dosage form of claim 12 wherein the pharmaceutical dosage form includes from about 1 to about 3 wt % hydroxypropyl methylcellulose.

14. The pharmaceutical dosage form of claim 12 wherein the pharmaceutical dosage form includes about 2 wt % hydroxypropyl methylcellulose.

15. The pharmaceutical dosage form of claim 1 wherein the dosage form includes from about 650 to about 850 mg ranolazine.

16. The pharmaceutical dosage form of claim 1 wherein the dosage form includes from about 900 to about 1100 mg ranolazine.

17. The pharmaceutical dosage form of claim 1 wherein the dosage form includes from about 400 to about 600 mg ranolazine.

18. The pharmaceutical dosage form of claim 1 wherein the dosage form includes from about 300 to about 1000 mg ranolazine.

19. The pharmaceutical dosage form of claim 2 wherein the pharmaceutical dosage form is a compressed tablet.

20. A compressed tablet comprising from about 70 to about 80 wt % ranolazine, at least one pH dependent binder selected from methacrylic acid copolymers, hydroxypropyl cellulose phthalate, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, polyvinyl acetate, phthalate, polyvinylpyrrolidine phthalate, and mixtures thereof, and at least one pH independent binder wherein the compressed tablet includes from about 350 to about 800 mg ranolazine.

21. A dosage form for delivering ranolazine to a human, wherein the dosage form comprises at least 50% by weight ranolazine and at least one pharmaceutically acceptable excipient, said dosage form when administered at least once over a 24 hour period provides a peak to trough ranolazine level ratio in plasma that does not exceed 4:1 over the 24 hour period.

22. The dosage form of claim 21 wherein the dosage form when administered at least once over a 24 hour period provides a peak to trough ranolazine level ratio in plasma that does not exceed 3:1 over the 24 hour period.

23. The dosage form of claim 21 wherein the dosage form when administered at least once over a 24 hour period provides a peak to trough ranolazine level ratio in plasma that does not exceed 2:1 over the 24 hour period.

24. The dosage form of claim 21 wherein said at least one pharmaceutically acceptable excipient inhibits the release of ranolazine from the dosage form when the dosage form is subjected to an aqueous environment having a pH of the stomach and that promotes the release of a therapeutic amount of ranolazine in an aqueous solution having a pH above about 4.5.

25. A dosage form for delivering ranolazine to a human, wherein the dosage form comprises at least 50% by weight ranolazine and the admixture of at least one pharmaceutically acceptable excipient, said dosage form when administered at least once during a 24 hour period maintains a trough plasma ranolazine level that is not less than about 550 ng base/mL over the 24 hour period.

26. The dosage form of claim 25 wherein said admixture inhibits the release of ranolazine from the dosage form when the dosage form is subjected to an aqueous environment having a pH of the stomach and that promotes the release of a therapeutic amount of ranolazine in an aqueous environment having a pH above about 4.5.

27. A dosage form for delivering ranolazine to a patient, wherein the dosage form comprises at least 50% by weight ranolazine and the admixture of at least one pharmaceutically acceptable excipient, said dosage form when administered periodically over a 24 hour period maintains plasma ranolazine levels close to minimal effective levels without peak fluctuations.

28. A method for preparing a sustained release ranolazine dosage form comprising the steps of (a) intimately admixing ranolazine with at least one pharmaceutically acceptable excipient; (b) granulating the result of step (a) with an aqueous solution of a strong base; (c) drying and screening the granules from step (b); (d) blending the granules from step (c) with lubricants or tabletting aids; (e) compressing the granules from step (d) into a tablet; and optionally (f) coating the tablets from step (e).

29. A dosage form for delivering ranolazine to a human, wherein the dosage form comprises at least 50% by weight ranolazine and the admixture of at least one pharmaceutically acceptable excipient, said dosage form when administered at least once during a 24 hour period maintains a trough plasma ranolazine level that is not less than about 850 ng base/mL over the 24 hour period.

30. The dosage form of claim 29 wherein said admixture inhibits the release of ranolazine from the dosage form when the dosage form is subjected to an aqueous environment having a pH of the stomach and that promotes the release of a therapeutic amount of ranolazine in an aqueous environment having a pH above about 4.5.

31. A dosage form for delivering ranolazine to a patient, wherein the dosage form comprises at least 50% by weight ranolazine and the admixture of at least one pharmaceutically acceptable excipient, said dosage form when administered at least once during a 24 hour period maintains a peak plasma ranolazine level that is not more than about 7500 ng base/mL over the 24 hour period.

32. A dosage form for delivering ranolazine to a patient, wherein the dosage form comprises at least 50% by weight ranolazine and the admixture of at least one pharmaceutically acceptable excipient, said dosage form when administered at least once during a 24 hour period maintains a peak plasma ranolazine level that is not more than about 4000 ng base/mL over the 24 hour period.

33. A dosage form for delivering ranolazine to a patient, wherein the dosage form provides a therapeutic advantage of minimizing variations in ranolazine plasma concentration over a 24 hour period.
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