首页> 外国专利> COMPOSITIONS, COMPLEXES COMPRISING A PHARMACEUTICALLY ACCEPTABLE SALTS OF ZIPRASIDONE AND CYCLODEXTRIN AND ZIPRASIDONE SALTS

COMPOSITIONS, COMPLEXES COMPRISING A PHARMACEUTICALLY ACCEPTABLE SALTS OF ZIPRASIDONE AND CYCLODEXTRIN AND ZIPRASIDONE SALTS

机译:组成包括齐拉西酮和环糊精和齐拉西酮盐的药学上可接受的盐的组合物

摘要

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 -cyclodextrin, hydroxypropyl -cyclodextrin (HPBCD) and sulfobutyl ether -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 -cyclodextrin, sulfobutyl ether -cyclodextrin (SBECD) and hydroxypropyl -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 -cyclodextrin, hydroxypropyl -cyclodextrin (HPBCD) and sulfobutyl ether -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 -cyclodextrin (SBECD) and hydroxypropyl -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 -cyclodextrin, sulfobutyl ether -cyclodextrin (SBECD) and hydroxypropyl -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 -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.
机译:1.一种组合物,其包含下式的齐拉西酮的药学上可接受的盐和环糊精。 2.根据权利要求1的组合物,其中所述环糊精选自-环糊精,羟丙基-环糊精(HPBCD)和磺丁基醚-环糊精(SBECD)。 3.权利要求2的组合物,其中所述环糊精选自HPBCD和SBECD。 4.一种组合物,其包含齐拉西酮的盐和环糊精的盐的干燥混合物,其中所述盐选自甲苯磺酸盐,酒石酸盐,萘酚盐,苯磺酸盐,天冬氨酸盐,乙磺酸盐和甲磺酸盐;其中所述环糊精选自-环糊精,磺丁基醚-环糊精(SBECD)和羟丙基-环糊精(HPBCD)。 5.下式的齐拉西酮的药学上可接受的盐在环糊精中的包合物。 6.如权利要求5所述的复合物,其中所述环糊精选自-环糊精,羟丙基-环糊精(HPBCD)和磺丁基醚-环糊精(SBECD)。 7.权利要求6的复合物,其中所述环糊精选自HPBCD和SBECD。 8.环糊精中齐拉西酮的药学上可接受的盐的包合物,所述包合物在环糊精浓度为40%w的情况下提供至少2.5mgA / ml的齐拉西酮量。 / v在水中。 9.权利要求8的复合物,其中所述环糊精选自磺基丁基醚-环糊精(SBECD)和羟丙基-环糊精(HPBCD)。 10.权利要求8的复合物,其中所述齐拉西酮的量为至少10mgA / ml。 11.如权利要求10所述的复合物,其中所述齐拉西酮的量为至少15mgA / ml。 12.如权利要求9所述的复合物,其中,所述复合物选自(1)齐拉西酮的甲苯磺酸盐,萘磺酸盐,苯磺酸盐,天冬氨酸盐,酒石酸盐,乙磺酸盐和甲磺酸盐,各自与SBECD复合。 (2)齐拉西酮的酒石酸盐,乙磺酸盐和甲磺酸盐,均与HPBCD络合。 13.如权利要求12所述的复合物,其中所述复合物选自(1)各自与SBECD复合的齐拉西酮的甲苯磺酸盐,萘磺酸盐,苯磺酸盐,酒石酸盐,乙磺酸盐和甲磺酸盐; (2)齐拉西酮的酒石酸盐,乙磺酸盐和甲磺酸盐,均与HPBCD络合。 14.权利要求13的复合物,其中所述复合物选自(1)均与SBECD复合的齐拉西酮的酒石酸盐,乙磺酸盐和甲磺酸盐。 (2)齐拉西酮的酒石酸盐,乙磺酸盐和甲磺酸盐,均与HPBCD络合。 15.如权利要求14所述的复合物,其中所述复合物选自甲磺酸齐拉西酮和酒石酸盐,各自与SBECD复合。 16.权利要求15的复合物,其中所述复合物是与SBECD复合的甲磺酸齐拉西酮。 17.一种包含齐拉西酮的药学上可接受的盐和环糊精的包合物,其中所述盐选自甲苯磺酸盐,酒石酸盐,萘酚盐,苯磺酸盐,天冬氨酸盐,乙磺酸盐和甲磺酸盐;其中所述环糊精选自-环糊精,磺丁基醚-环糊精(SBECD)和羟丙基-环糊精(HPBCD)。 18.权利要求17的复合物,其中所述复合物选自(1)齐拉西酮的甲苯磺酸盐,萘磺酸盐,苯磺酸盐,酒石酸盐,乙磺酸盐和甲磺酸盐,每个均与SBECD复合。 (2)齐拉西酮的酒石酸盐,乙磺酸盐和甲磺酸盐,均与HPBCD络合。 19.权利要求18的复合物,其中所述复合物选自(1)均与SBECD复合的齐拉西酮的酒石酸盐,乙磺酸盐和甲磺酸盐。 (2)齐拉西酮的酒石酸盐,乙磺酸盐和甲磺酸盐,均与HPBCD络合。 20.根据权利要求19所述的复合物,其中所述复合物选自甲磺酸齐拉西酮和酒石酸盐,各自与SBECD复合。 21.环糊精中齐拉西酮的药学上可接受的盐的包合物,其中所述络合物是与磺基丁基醚-环糊精复合的甲磺酸齐拉西酮(SBECD)。 22.一种组合物,其包含权利要求5至21中任一项所定义的内含物复合物的水溶液。23.一种盐,其选自齐拉西酮乙磺酸盐,齐拉西酮甲磺酸盐和齐拉西酮酒石酸盐。 24.如权利要求23所述的盐,其为齐拉西酮乙磺酸盐。 25.根据权利要求23所述的盐,其是甲磺酸齐拉西酮。 26.如权利要求23所述的盐,其是酒石酸齐拉西酮。

著录项

  • 公开/公告号EA001731B1

    专利类型

  • 公开/公告日2001-08-27

    原文格式PDF

  • 申请/专利权人 PFIZER INC.;

    申请/专利号EA19980000910

  • 申请日1997-04-01

  • 分类号C07D417/14;C08L5/16;C08B37/16;A61K47/48;A61P25/18;

  • 国家 EA

  • 入库时间 2022-08-22 01:25:36

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号