Solid dispersion of tacrolimus
    7.
    发明申请
    Solid dispersion of tacrolimus 审中-公开
    他克莫司的固体分散体

    公开(公告)号:US20060177500A1

    公开(公告)日:2006-08-10

    申请号:US10563972

    申请日:2004-07-09

    IPC分类号: A61K9/20

    摘要: The present invention relates to the carrier of the solid dispersion of tacrolimus, which is prepared by using the solid surfactant having a property of HLB value higher than or equal to about 7. The surfactants carry out a function of a carrier and a function of a dissolution enhancer, simultaneously. As a result, the dissolution rate of tacrolimus is improved, and the oral absorbability and the bioavailability may be increased due to rapid drug release.

    摘要翻译: 本发明涉及通过使用具有HLB值高于或等于约7的性质的固体表面活性剂制备的他克莫司的固体分散体的载体。表面活性剂具有载体的功能和作用 溶解增强剂,同时。 结果,他克莫司的溶出速度提高,口服吸收性和生物利用度可能由于快速的药物释放而增加。

    Pharmaceutical composition comprising cyclosporin solid-state microemulsion
    8.
    发明授权
    Pharmaceutical composition comprising cyclosporin solid-state microemulsion 失效
    包含环孢菌素固态微乳液的药物组合物

    公开(公告)号:US06306434B1

    公开(公告)日:2001-10-23

    申请号:US09555619

    申请日:2000-06-01

    IPC分类号: A61K966

    摘要: A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.

    摘要翻译: 公开了包含环孢菌素固态微乳液的药物组合物。 在优选的实施方案中,组合物包含分散在肠载体中的环孢菌素微乳液。 该组合物不溶于人造胃液等外部相,但在人造肠液中快速溶解,由此释放环孢菌素微乳液,提供环孢菌素的快速输送。 该组合物每天一次有效地维持环孢菌素的治疗血液浓度,提供给药的便利性,并避免通过增加与常规环孢菌素制剂相关的峰值血液环孢菌素浓度而诱发的不良反应。