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    • 3. 发明申请
    • TACROLIMUS COMPOSITIONS FOR AEROSOL ADMINISTRATION
    • 用于气溶胶管理的TACROLIMUS组合物
    • US20110318277A1
    • 2011-12-29
    • US13168856
    • 2011-06-24
    • Richard N. DalbyRalph Niven
    • Richard N. DalbyRalph Niven
    • A61K9/12A61P37/06
    • A61K31/436A61K9/008
    • The present disclosure relates generally to highly concentrated macrolide solutions for aerosol administration, and related methods of producing and administering the same. In one aspect, provided herein is a receptacle containing a highly concentrated solution of a macrolide compound such as tacrolimus, where the solution exhibits long-term stability in a pMDI canister and achieves high respirable fractions when actuated, among, other features. In yet another aspect, provided is a composition suitable for aerosol administration comprising tacrolimus dissolved in an ethanol-liquified propellant mixture, characterized by a tacrolimus concentration of greater than 0.15 weight percent (w/w) and comprising no more than about 10 weight percent (w/w) ethanol.
    • 本公开一般涉及用于气雾剂给药的高度浓缩的大环内酯溶液及其相关的生产和施用方法。 在一个方面,本文提供的是含有大环内酯类化合物如他克莫司的高度浓缩溶液的容器,其中溶液在pMDI罐中表现出长期稳定性,并且在致动时实现高呼吸成分,以及其它特征。 在另一方面,提供了适用于气溶胶施用的组合物,其包含溶解在乙醇液化的推进剂混合物中的他克莫司,其特征在于他克莫司浓度大于0.15重量%(w / w),并且包含不超过约10重量% w / w)乙醇。