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Claims for Patent: 6,232,304

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Claims for Patent: 6,232,304

Title: Inclusion complexes of aryl-heterocyclic salts
Abstract:Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex or an aqueous solution. The salt/cyclodextrin inclusion complex preferably provides an amount of ziprasidone of at least 2.5 mgA/ml when the complex is dissolved in water at 40% w/v. A variety of ziprasidone salts are preferred, including the mesylate, esylate, besylate, tartrate, napsylate, and tosylate.
Inventor(s): Kim; Yesook (Branford, CT), Johnson; Kevin C. (Niantic, CT), Shanker; Ravi M. (Groton, CT)
Assignee: Pfizer Inc. (New York, NY)
Application Number:09/147,239
Patent Claims: 1. A composition of matter comprising a pharmaceutically acceptable salt of a compound of the formula ##STR3##

and a cyclodextrin, wherein

Ar is benzoisothiazolyl or an oxide or dioxide thereof each optionally substituted by one fluoro, chloro, trifluoromethyl, methoxy, cyano, or nitro;

n is 1 or 2; and

X and Y together with the phenyl to which they are attached form benzothiazolyl; 2-aminobenzothiazolyl; benzoisothiazolyl; indazolyl; 3-hydroxyindazolyl; indolyl; oxindolyl optionally substituted by one to three of (C.sub.1 -C.sub.3)alkyl, or one of chloro, fluoro or phenyl, said phenyl optionally substituted by one chloro or fluoro; benzoxazolyl; 2-aminobenzoxazolyl; benzoxazolonyl; 2-aminobenzoxazolinyl; benzothiazolonyl; benzoimidazolonyl; or benzotriazolyl.

2. A composition as defined in claim 1, comprising a dry mixture of said compound and said cyclodextrin.

3. A composition as defined in claim 1, comprising a dry inclusion complex of said compound complexed with said cyclodextrin.

4. A composition as defined in claim 1, comprising an aqueous solution of an inclusion complex of said drug complexed with said cyclodextrin.

5. A compositon as defined in claim 1, wherein X and Y together with the phenyl to which they are attached form oxindole.

6. A composition as defined in claim 1, wherein Ar is benzoisothiazolyl.

7. A composition as defined in claim 1, wherein n is 1.

8. A composition as defined in claim 1, wherein said compound is ziprasidone.

9. A composition as defined in claim 1, wherein said cyclodextrin is selected from .gamma.-cyclodextrin, HPBCD and SBECD.

10. A composition as defined in claim 9, wherein said cyclodextrin is selected from HPBCD and SBECD.

11. A composition of matter comprising an inclusion complex of a pharmaceutically acceptable salt of a compound of the formula ##STR4##

in a cyclodextrin, wherein

Ar is benzoisothiazolyl or an oxide or dioxide thereof each optionally substituted by one fluoro, chloro, trifluoromethyl, methoxy, cyano, or nitro;

n is 1 or 2; and

X and Y together with the phenyl to which they are attached form benzothiazolyl; 2-aminobenzothiazolyl; benzoisothiazolyl; indazolyl; 3-hydroxyindazolyl; indolyl; oxindolyl optionally substituted by one to three of (C.sub.1 -C.sub.3)alkyl, or one of chloro, fluoro or phenyl, said phenyl optionally substituted by one chloro or fluoro; benzoxazolyl; 2-aminobenzoxazolyl; benzoxazolonyl; 2-aminobenzoxazolinyl; benzothiazolonyl; benzoimidazolonyl; or benzotriazolyl.

12. A compositon as defined in claim 11, wherein X and Y together with the phenyl to which they are attached form oxindole.

13. A composition as defined in claim 11, wherein Ar is benzoisothiazolyl.

14. A composition as defined in claim 11, wherein n is 1.

15. A composition as defined in claim 11, wherein said compound is ziprasidone.

16. A composition as defined in claim 11, wherein said cyclodextrin is selected from .gamma.-cyclodextrin, HPBCD, and SBECD.

17. A composition as defined in claim 16, wherein said cyclodextrin is selected from HPBCD and SBECD.

18. A composition of matter comprising an inclusion complex of a pharmaceutically acceptable salt of ziprasidone in a cyclodextrin.

19. A composition as defined in claim 18, wherein said cyclodextrin is selected from HPBCD and SBECD.

20. A composition of matter comprising an inclusion complex of a pharmaceutically acceptable salt of ziprasidone in a cyclodextrin, said inclusion complex providing an amount of ziprasidone of at least 2.5 mgA/ml when the amount of ziprasidone provided by said complex is measured at a cyclodextrin concentration of 40% w/v in water.

21. A composition as defined in claim 20, wherein said cyclodextrin is selected from SBECD and HPBCD.

22. A composition as defined in claim 20, wherein said amount of ziprasidone is at least 10 mgA/ml.

23. A composition as defined in claim 22, wherein said amount of ziprasidone is at least 15 mgA/ml.

24. A composition as defined in claim 21, wherein said inclusion complex is selected from

(1) the tosylate, napsylate, besylate, aspartate, tartrate, esylate and mesylate salts of ziprasidone, each complexed with SBECD; and

(2) the tartrate, esylate, and mesylate salts of ziprasidone, each complexed with HPBCD.

25. A composition as defined in claim 24, wherein said inclusion complex is selected from

(1) the tosylate, napsylate, besylate, tartrate, esylate and mesylate salts of ziprasidone, each complexed with SBECD; and

(2) the tartrate, esylate, and mesylate salts of ziprasidone, each complexed with HPBCD.

26. A composition as defined in claim 25, wherein said inclusion complex is selected from

(1) the tartrate, esylate, and mesylate salts of ziprasidone, each complexed with SBECD; and

(2) the tartrate, esylate and mesylate salts of ziprasidone, each complexed with HPBCD.

27. A composition as defined in claim 26, wherein said inclusion complex is selected from ziprasidone mesylate and tartrate, each complexed with SBECD.

28. A composition as defined in claim 27, wherein said inclusion complex is ziprasidone mesylate complexed with SBECD.

29. A composition of matter comprising a pharmaceutically acceptable salt of ziprasidone and a cyclodextrin,

wherein said salt is selected from the tosylate, tartrate, napsylate, besylate, aspartate, tartrate, esylate and mesylate salt;

and wherein said cyclodextrin is selected from .gamma.-cyclodextrin, SBECD and HPBCD.

30. A composition of matter as defined in claim 29, wherein said composition is an inclusion complex of said salt in said cyclodextrin.

31. A composition as defined in claim 30, wherein said inclusion complex is selected from

(1) the tosylate, napsylate, besylate, tartrate, esylate and mesylate salts of ziprasidone, each complexed with SBECD; and

(2) the tartrate, esylate, and mesylate salts of ziprasidone, each complexed with HPBCD.

32. A composition as defined in claim 31, wherein said inclusion complex is selected from

(1) the tartrate, esylate, and mesylate salts of ziprasidone, each complexed with SBECD; and

(2) the tartrate, esylate and mesylate salts of ziprasidone, each complexed with HPBCD.

33. A composition as defined in claim 32, wherein said inclusion complex is selected from ziprasidone mesylate and tartrate, each complexed with SBECD.

34. A composition as defined in claim 33, wherein said inclusion complex is ziprasidone mesylate complexed with SBECD.

35. A composition as defined in claim 29, comprising dry mixture of said salt and said cyclodextrin.

36. A composition of matter which is an inclusion complex of a pharmaceutically acceptable salt of ziprasidone in a cyclodextrin, wherein said inclusion complex is ziprasidone mesylate complexed with SBECD.
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