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Claims for Patent: 6,150,366

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Claims for Patent: 6,150,366

Title: Ziprasidone formulations
Abstract:Compositions comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size less than 85 .mu.m, and a pharmaceutically acceptable carrier, are substantially bioequivalent and can be used to treat psychoses such as schizophrenia.
Inventor(s): Arenson; Daniel R. (East Lyme, CT), Busch; Frank Robert (Gales Ferry, CT), Hausberger; Angela G. (East Lyme, CT), Rasadi; Bijan (Groton, CT)
Assignee: Pfizer Inc. (New York, NY)
Application Number:09/320,985
Patent Claims: 1. A composition comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size equal to or less than about 85 .mu.m and a pharmaceutically acceptable diluent or carrier.

2. A composition as defined in claim 1, wherein said composition comprises ziprasidone hydrochloride monohydrate.

3. A composition as defined in claim 1, wherein said mean particle size is equal to or less than 50 .mu.m.

4. A composition as defined in claim 3, wherein said mean particle size is from 5 to 50 .mu.m.

5. A composition as defined in claim 4, wherein said mean particle size is from 5 to 40 .mu.m.

6. A composition as defined in claim 5, wherein said mean particle size is from 5 to 30 .mu.m.

7. A composition as defined in claim 1 which exhibits an AUC and/or C.sub.max that is at least 80% of the mean AUC and/or C.sub.max observed for an equivalent formulation differing only in that the ziprasidone hydrochloride mean particle size is 20 .mu.m.

8. A composition as defined in claim 1, wherein, when an amount of said dosage form equivalent to 100 mgA or less of ziprasidone is placed in a USP-2 apparatus containing 900 ml of aqueous NaH.sub.2 PO.sub.4 buffer, pH 7.5, containing 2% (w/v) sodium dodecyl sulfate, and equipped with paddles stirring at 75 rpm, at least 70% of the ziprasidone therein dissolves within 45 minutes.

9. A method of treating a psychosis, comprising administering to a patient in need of such treatment an effective amount of a composition as defined in claim 1.

10. A method as defined in claim 9, wherein said composition comprises ziprasidone hydrochloride monohydrate.

11. A method as defined in claim 9, wherein said mean particle size is equal to or less than 50 .mu.m.

12. A method as defined in claim 11, wherein said mean particle size is from 5 to 50 .mu.m.

13. A method as defined in claim 12, wherein said mean particle size is from 5 to 40 .mu.m.

14. A method as defined in claim 13, wherein said mean particle size is from 5 to 30 .mu.m.

15. A method as defined in claim 9 wherein said composition exhibits an AUC and/or C.sub.max that is at least 80% of the mean AUC and/or C.sub.max observed for an equivalent composition differing only in that the ziprasidone hydrochloride particle size is 20 .mu.m.

16. A method as defined in claim 9 wherein, when an amount of said composition equivalent to 100 mgA or less of ziprasidone is placed in a USP-2 apparatus containing 900 ml of aqueous NaH.sub.2 PO.sub.4 buffer, pH 7.5, containing 2% (w/v) sodium dodecyl sulfate, and equipped with paddles stirring at 75 rpm, at least 70% of the ziprasidone therein dissolves within 45 minutes.

17. A composition comprising crystalline ziprasidone free base or crystalline ziprasidone hydrochloride particles having a mean particle size equal to or less than about 85 .mu.m, as measured by Malvern light scattering, and a pharmaceutically acceptable carrier, said composition exhibiting a mean AUC and/or C.sub.max which is at least 80% of the mean AUC exhibited by a composition equivalent thereto but differing only in that it has a crystalline ziprasidone hydrochloride mean particle size of 20 .mu.m.

18. A composition as defined in clam 17, which comprises crystalline ziprasidone hydrochloride monohydrate.

19. A composition as defined in claim 17, wherein said mean particle size is equal to or less than 50 .mu.m.

20. A composition as defined in claim 19, wherein said mean particle size is from 5 to 50 .mu.m.

21. A composition as defined in claim 20, wherein said mean particle size is from 5 to 40 .mu.m.

22. A composition as defined in claim 21, wherein said mean particle size is from 5 to 30 .mu.m.

23. A composition as defined in claim 17, wherein, when an amount of said composition equivalent to 100 mgA or less of ziprasidone is placed in a USP-2 apparatus containing 900 ml of aqueous NaH.sub.2 PO.sub.4 buffer, pH 7.5, containing 2% (w/v) sodium dodecyl sulfate, and equipped with paddles stirring at 75 rpm, at least 70% of the ziprasidone hydrochloride therein dissolves within 45 minutes.

24. A method of treating a psychosis, comprising administering to a patient in need of such treatment an effective amount of a composition as defined in claim 17.

25. A method as defined in claim 24, which comprises ziprasidone hydrochloride monohydrate.

26. A method as defined in claim 24, wherein said mean particle size is equal to or less than 50 .mu.m.

27. A method as defined in claim 26, wherein said mean particle size is from 5 to 50 .mu.m.

28. A method as defined in claim 27, wherein said mean particle size is from 5 to 40 .mu.m.

29. A method as defined in claim 28, wherein said mean particle size is from 5 to 30 .mu.m.

30. A method as defined in claim 24, wherein, when an amount of said composition equivalent to 100 mgA or less of ziprasidone is placed in a USP-2 apparatus containing 900 ml of aqueous NaH.sub.2 PO.sub.4, pH 7.5, containing 2% (w/v) sodium dodecyl sulfate, and equipped with paddles stirring at 75 rpm, at least 70% of the ziprasidone therein dissolves within 45 minutes.

31. A process of preparing large crystals of ziprasidone hydrochloride monohydrate, comprising the steps of:

1) dissolving ziprasidone free base in a solvent comprising THF and water, in a volume ratio of about 22-35 unit volumes of THF to about 1.5-8 volumes of water;

2) heating the solution resulting from step (1);

3) adding HCl to the solution resulting from step (2); and

4) cooling the solution resulting from step (3).

32. A process as defined in claim 31, wherein the volume ratio of THF to water in said solvent is 24-30 to 2-6.

33. A process as defined in claim 31, wherein, in said step (3), the temperature of said solution is maintained below reflux.

34. A process as defined in claim 33, wherein said temperature is 60-64.degree. C.
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