Invention Grant
US09073857B2 Aripiprazole type I microcrystal, aripiprazole solid preparations, and preparation method
有权
阿立哌唑I型微晶,阿立哌唑固体制剂及其制备方法
- Patent Title: Aripiprazole type I microcrystal, aripiprazole solid preparations, and preparation method
- Patent Title (中): 阿立哌唑I型微晶,阿立哌唑固体制剂及其制备方法
-
Application No.: US14129838Application Date: 2012-06-26
-
Publication No.: US09073857B2Publication Date: 2015-07-07
- Inventor: Siji Zheng , Bo Tan , Linyong Fu , Xiaoyi Liu , Shaoqing Yuan , Zhihui Cao
- Applicant: Siji Zheng , Bo Tan , Linyong Fu , Xiaoyi Liu , Shaoqing Yuan , Zhihui Cao
- Applicant Address: CN Shanghai CN Shanghai
- Assignee: SHANGHAI ZHONGXI PHARMACEUTICAL CORPORATION,SHANGHAI ZHONGXI SUNVE PHARMACEUTICAL CO., LTD.
- Current Assignee: SHANGHAI ZHONGXI PHARMACEUTICAL CORPORATION,SHANGHAI ZHONGXI SUNVE PHARMACEUTICAL CO., LTD.
- Current Assignee Address: CN Shanghai CN Shanghai
- Agency: Oliff PLC
- Priority: CN201110180032 20110627
- International Application: PCT/CN2012/077515 WO 20120626
- International Announcement: WO2013/000392 WO 20130103
- Main IPC: C07D215/227
- IPC: C07D215/227 ; A61K9/00 ; A61K9/20 ; A61K9/48 ; A61K31/496

Abstract:
A method for preparing an aripiprazole type I microcrystal, including the following steps: dissolving aripiprazole in an acidifier, acquiring a medicament-having acid solution; adding an alkalizer while stirring, then adding water or aqueous ethanol 10 to 60 wt % while stirring, and separating by precipitation the aripiprazole type I microcrystal. Furthermore, a method for preparing a solid preparation having the aripiprazole type I microcrystal, an aripiprazole microcrystal having an average particle size of less than 20 μm, and a solid preparation having the microcrystal. The method for preparing the aripiprazole type I microcrystal allows reduced pollution and loss, great safety, easy and convenient, reduced use of organic solvents, obviated need for demanding process conditions (such as cooling condition) and apparatus, low cost, and facilitated applicability in industrialized manufacturing. This solid preparation provides great stability, solubility, and bioavailability, reduced individual differences, and reduced content of related substances.
Public/Granted literature
- US20140135344A1 ARIPIPRAZOLE TYPE I MICROCRYSTAL, ARIPIPRAZOLE SOLID PREPARATIONS, AND PREPARATION METHOD Public/Granted day:2014-05-15
Information query