公开(公告)号：US20100240711A1

公开(公告)日：2010-09-23

申请号：US12678714

申请日：2008-09-18

申请人： Masatoshi Takada ,  Yuki Murakami ,  Shunji Ichio ,  Minako Fujii ,  Asako Takakura ,  Takeshi Funaki

发明人： Masatoshi Takada ,  Yuki Murakami ,  Shunji Ichio ,  Minako Fujii ,  Asako Takakura ,  Takeshi Funaki

IPC分类号： A61K31/44 ,  A61P3/04

CPC分类号： C07D213/76 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1652 ,  A61K9/1694

摘要： A preparation which can improve solubility of a NPYY5 receptor antagonist in water, even when the NPYY5 receptor antagonist is contained in the preparation at a high content is provided. A solid preparation containing a NPYY5 receptor antagonist, an amorphous stabilizer, and optionally an amorphousization inducing agent. Particularly, when the amorphous stabilizer is hydroxypropylmethylcellulose phthalate and/or hydroxypropylmethylcellulose acetate succinate, and the amorphousization inducing agent is urea and/or saccharine sodium at an addition amount of less than 8% by weight, dissolution out property of a water-hardly soluble NPYY5 receptor antagonist could be improved.

摘要翻译： 提供了即使NPYY5受体拮抗剂以高含量包含在制剂中，也能够提高NPYY5受体拮抗剂在水中的溶解性的制剂。 含有NPYY5受体拮抗剂，无定形稳定剂和任选的非晶化诱导剂的固体制剂。 特别是当无定形稳定剂为羟丙基甲基纤维素邻苯二甲酸酯和/或羟丙基甲基纤维素乙酸酯琥珀酸酯时，无定形诱导剂为加入量小于8重量％的尿素和/或糖精钠，水难溶性NPYY5的溶出性 受体拮抗剂可以改善。