公开(公告)号：EP2726461A1

公开(公告)日：2014-05-07

申请号：EP12748263.6

申请日：2012-06-29

申请人： Otsuka Pharmaceutical Co., Ltd.

发明人： BANDO, Takuji ,  YANO, Katsuhiko ,  FUKANA, Makoto ,  AOKI, Satoshi

IPC分类号： C07D215/22 ,  A61K31/4704 ,  A61P25/18

CPC分类号： C07D215/22

摘要： The present invention provides a novel method for producing fine particles of aripiprazole anhydride crystals B. The method for producing fine particles of aripiprazole anhydride crystals B comprises the steps of: (1) heating and dissolving crude aripiprazole in a lower alcohol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (2) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (3) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals.

摘要翻译： 本发明提供了制备阿立哌唑无水物晶体B微粒的新方法。制备阿立哌唑无水物晶体B微粒的方法包括以下步骤：（1）将粗阿立哌唑加热溶解在低级醇中，随后冷却 得到的混合物沉淀结晶，得到阿立哌唑低级醇溶剂化物晶体; （2）使阿立哌唑低级醇溶剂合物的晶体以含有低级醇的浆料的形式进行湿磨; （3）将湿磨晶体的分散体进行固液分离以获得晶体，并加热晶体。