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    • 9. 发明申请
    • SOLID DISPERSIONS
    • 固体分散剂
    • WO2016145138A1
    • 2016-09-15
    • PCT/US2016/021671
    • 2016-03-10
    • SHIONOGI INC.
    • CHEN, ZhengmingCHEN, XiaomingHALLORAN, Kevin
    • A01N57/00
    • A61K9/146A61K31/085A61K47/32A61K47/38
    • An ospemifene solid dispersion for enhancing solubility and bioavailability,, and methods of preparation thereof are disclosed. The solid dispersion comprises an active pharmaceutical ingredient, such as ospemifene, and a hydfophilie carrier, such as copovidone, hypromellose acetate succinate, polyvinylpyrrolidine, a polyvinylpyrrolidine/vinyl acetate co-polymer, hydroxy! propyl methylcellulose, hypromellose acetate succinate, a Eudragit® compound, hydroxypropylcellulose, a polyvinyl caprolactam-polyvinyl acetate polyethylene glycol graft co-polymer, hydroxypropyl methylcellulose phthalate, and mixtures thereof, and optionally a surfactant The ospemifene solid, dispersions can be used in methods of treating a symptom related, to menopause, such as vaginal dryness or sexual dysfunction, or in methods of treating osteoporosis.
    • 公开了一种用于增强溶解度和生物利用度的欧司哌米芬固体分散体及其制备方法。 固体分散体包含活性药物成分,如欧司哌米芬,以及亲水载体,如共聚维酮,乙酸琥珀酸羟丙甲纤维素,聚乙烯吡咯烷酮,聚乙烯吡咯烷酮/乙酸乙烯酯共聚物, 丙基甲基纤维素,醋酸羟丙甲纤维素琥珀酸酯,化合物,羟丙基纤维素,聚乙烯基己内酰胺 - 聚乙酸乙烯酯聚乙二醇接枝共聚物,羟丙基甲基纤维素邻苯二甲酸酯及其混合物,以及任选的表面活性剂奥斯美芬固体,分散体可用于 治疗与绝经相关的症状,如阴道干燥或性功能障碍,或治疗骨质疏松症的方法。