熊去氧胆酸的杂质控制研究进展

Research progress in impurity control of ursodeoxycholic acid

熊去氧胆酸(UDCA)是由胆固醇衍生而来的天然亲水性胆汁酸,在人体中含量较低,可用于治疗胆结石、胆汁淤积性肝病、脂肪肝等。由于国内外UDCA的合成工艺、原料药来源及杂质控制标准存在差异,因此,笔者通过查询相关文献总结UDCA在国内外的合成工艺,分析其原料药杂质来源及杂质控制标准。结果发现,美国、英国和欧洲的药典对UDCA的合成路线和杂质控制提出了明确的要求,并且制定了相应杂质控制标准;但是国内关于UDCA的合成工艺和杂质控制标准均较为简单。建议国内研究机构不断完善UDCA杂质谱,改进其合成工艺,提高其质量标准,为其进一步的药学研究和临床合理应用提供参考。

Ursodeoxycholic acid(UDCA)is a natural hydrophilic bile acid derived from cholesterol,which has a low content in human body,and can be used for the treatment of gallstones,cholestatic liver disease,fatty liver and so on.Due to the differences in the synthesis process,source of active pharmaceutical ingredients(API)and impurity control standards of UDCA at home and abroad,the author summarized the synthesis process of UDCA at home and abroad by searching relevant literature,and analyzed the impurity sources and impurity control standards of API.The results showed that the pharmacopoeia of the United States,the United Kingdom and Europe put forward clear requirements on the synthesis route and impurity control of UDCA,and formulated corresponding impurity control standards.However,synthesis process and impurity detection standards of UDCA were relatively simple in China.It is suggested that domestic research institutions constantly improve impurity spectrum,promote the synthesis process,and improve the quality detection standards of UDCA,so as to provide a reference for pharmaceutical study and reasonable clinical application of UDCA.