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Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size
专利权人:
DR. FALK PHARMA GMBH
发明人:
WILHELM RUDOLF,PRÖLS MARKUS,FISCHER ERIK,WAENERLUND POULSEN HEIDI
申请号:
NZ70898811
公开号:
NZ708988A
申请日:
2011.11.30
申请国别(地区):
NZ
年份:
2016
代理人:
摘要:
Disclosed is a method for the preparation of a pure polymorph of Nor-UDCA (norursodeoxycholic) or Bis-nor-UDCA (bis-nor-ursodeoxycholic acid), or of a pharmaceutically acceptable salt thereof, comprising the following steps: crystallizing the potassium salt of Nor-UDCA or Bis-nor-UDCA; and dissolving the potassium salt in a solvent (e.g., water and acetone) and acidifying the solution (e.g., to a pH of 1-2) to obtain pure Nor-UDCA or Bis-nor-UDCA. The method does not require a milling step and/or a micronization step. The pure polymorphs of Nor-UDCA (norursodeoxycholic) and Bis-nor-UDCA (bis-nor-ursodeoxycholic acid) are suitable for the treatment of bile- and liver diseases.
来源网站:
中国工程科技知识中心
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