Patent EA-001731-B1 (EA)
Title: Compositions, complexes comprising a pharmaceutically acceptable salts of ziprasidone and cyclodextrin and ziprasidone salts
Inventor: JOHNSON KEVIN CHARLES
IPC: A61K47/48
Filed: 1997-04-01
Abstract: 1. A composition comprising a pharmaceutically acceptable salt of ziprasidone of the formula   and a cyclodextrin. 2. A composition as defined in Claim 1, wherein said cyclodextrin is selected from γ-cyclodextrin, hydroxypropyl β-cyclodextrin (HPBCD) and sulfobutyl ether β-cyclodextrin (SBECD). 3. A composition as defined in Claim 2, wherein said cyclodextrin is selected from HPBCD and SBECD. 4. A composition, comprising a dry mixture of the salt of ziprasidone and cyclodextrin, wherein said salt is selected from the tosylate, tartrate, napsylate, besylate, aspartate, esylate and mesylate salts; and wherein said cyclodextrin is selected from γ-cyclodextrin, sulfobutyl ether β-cyclodextrin (SBECD) and hydroxypropyl β-cyclodextrin (HPBCD). 5. An inclusion complex of a pharmaceutically acceptable salt of ziprasidone of the formula   in a cyclodextrin. 6 The complex as defined in Claim 5, wherein said cyclodextrin is selected from γ-cyclodextrin, hydroxypropyl β-cyclodextrin (HPBCD) and sulfobutyl ether β-cyclodextrin (SBECD). 7. The complex as defined in Claim 6, wherein said cyclodextrin is selected from HPBCD and SBECD. 8. 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. 9. The complex as defined in Claim 8, wherein said cyclodextrin is selected from sulfobutyl ether β-cyclodextrin (SBECD) and hydroxypropyl β-cyclodextrin (HPBCD). 10. The complex as defined in Claim 8, wherein said amount of ziprasidone is at least 10 mgA/ml. 11. The complex as defined in Claim 10, wherein said amount of ziprasidone is at least 15 mgA/ml. 12. The complex as defined in Claim 9, wherein said 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. 13. The complex as defined in Claim 12, wherein said 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. 14. The complex as defined in Claim 13, wherein said 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. 15. The complex as defined in Claim 14, wherein said complex is selected from ziprasidone mesylate and tartrate, each complexed with SBECD. 16. The complex as defined in Claim 15, wherein said complex is ziprasidone mesylate complexed with SBECD. 17. An inclusion complex comprising a pharmaceutically acceptable salt of ziprasidone and a cyclodextrin, wherein said salt is selected from the tosylate, tartrate, napsylate, besylate, aspartate, esylate and mesylate salts; and wherein said cyclodextrin is selected from γ-cyclodextrin, sulfobutyl ether β-cyclodextrin (SBECD) and hydroxypropyl β-cyclodextrin (HPBCD). 18. The complex as defined in Claim 17, wherein said 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. 19. The complex as defined in Claim 18, wherein said 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. 20. The complex as defined in Claim 19, wherein said complex is selected from ziprasidone mesylate and tartrate, each complexed with SBECD. 21. An inclusion complex of a pharmaceutically acceptable salt of ziprasidone in a cyclodextrin, wherein said complex is ziprasidone mesylate complexed with sulfobutyl ether β-cyclodextrin (SBECD). 22. A composition comprising an aqueous solution of an inclusion complex as defined in any one of Claims from 5 to 21. 23. A salt selected from ziprasidone esylate, ziprasidone mesylate, and ziprasidone tartrate. 24. A salt as defined in Claim 23, which is ziprasidone esylate. 25. A salt as defined in Claim 23, which is ziprasidone mesylate. 26. A salt as defined in Claim 23, which is ziprasidone tartrate.