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    • 5. 发明申请
    • CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS OF MILNACIPRAN
    • 控制释放的MILNACIPRAN的药物组合物
    • WO2011016057A2
    • 2011-02-10
    • PCT/IN2010/000520
    • 2010-08-04
    • LUPIN LIMITEDKULKARNI, Shirish, KumarKULKARNI, RajeshJADHAV, PandharinathTIWARI, Ashish
    • KULKARNI, Shirish, KumarKULKARNI, RajeshJADHAV, PandharinathTIWARI, Ashish
    • A61K9/20
    • A61K9/2027A61K9/2013A61K9/2054A61K9/2086A61K9/209A61K9/2095A61K31/165
    • A controlled release pharmaceutical composition comprising Milnacipran or pharmaceutically acceptable salts thereof and hydrophobic release controlling agent. The composition releases 90 % of the total amount of Milnacipran or pharmaceutically acceptable salts thereof between 8 to 20 hours when dissolution is carried out in 900 ml 0.1N HCl, USP apparatus Type I (Basket) at 100 rpm for 2 hrs, followed by 900 ml Phosphate buffer pH 6.8 USP apparatus Type I (Basket) at 100 rpm. A process of preparing a controlled release pharmaceutical composition comprises: a) preparing a first layer comprising i) melting hydrophobic release controlling agent and Milnacipran or pharmaceutically acceptable salts thereof in it ii) cooling followed by sieving the melted mass to obtain granules and iii) lubricating the granules; and b) preparing a second layer comprising granules which comprises hydrophobic release controlling agent and optionally Milnacipran or pharmaceutically acceptable salts thereof.
    • 包含米那普仑或其药学上可接受的盐和疏水释放控制剂的控释药物组合物。 当在900ml 0.1N HCl,USP装置I型(Basket)中以100rpm进行2小时溶解时,组合物释放出总量的90%的米那普仑或其药学上可接受的盐,其时间为8至20小时,然后900 ml磷酸盐缓冲液pH 6.8 USP装置I(Basket)以100rpm。 制备控释药物组合物的方法包括:a)制备第一层,其包括i)将疏水性释放控制剂和米那普兰或其药学上可接受的盐溶解在其中ii)冷却,然后筛分熔化的物质以获得颗粒,和iii)润滑 颗粒; 和b)制备包含颗粒的第二层,其包含疏水性释放控制剂和任选的米那普兰或其药学上可接受的盐。