药物代谢物在生物等效性评价中的意义

Role of drug metabolites in bioequivalence evaluation

关于药物代谢物在生物等效性评价中的地位已经争论数十年,目前对于达到最后统一的意见还有相当的距离。一部分人认为检测母体药物就足以反映药物制剂间的性能差异,而另一部分人则认为建立一个能反映所有药物制剂有效性和安全性的生物等效性标准是保证药物间相互替代的可靠方法,而且在实际应用中也存在着很多需要探讨的问题。通过相关情况的综述使我们意识到,对于在生物等效性评价中是否使用代谢物资料没有简单的规则,而众多争议问题的解决必须更多地依赖于以后对于影响药物和代谢物浓度因素的全面了解,药物代谢相关模拟试验的完善和药物基因组学的研究必将大大推动这一问题的解决。

The role of metabolites in bioequivalence studies has been a contentious issue for decades, and there is a long way to get a clear consensus on it. One opinion argues that the parent drug alone is sensitive to pick up formulation differences, while another believes that establishing criteria on all species that contribute to safety and efficacy is a reliable way to ensure the switchability of two drugs, and there are many problems to be solved when metabolites data were used in bioequivalence test. All of these make us to realize that there are no simple rules about the potential use of metabolites data in bioequivalence studies, and additional work is needed to understand all the facts that might influence the concentrations of both the parent drug and the metabolites to answer the related questions, so better of the simulations and the developing of pharmacogenetics will inevitable to give much strength to solve the problems.