天然产物研究与开发 ›› 2016, Vol. 28 ›› Issue (1): 30-35.doi: 10.16333/j.1001-6880.2016.1.006

• 研究论文 • 上一篇    下一篇

平衡透析法考察豆腐果苷血浆蛋白结合率:种属差异研究

贾元威,沈杰*,谢海棠,李相鸿,梁大虎,汪旻晖,胡骅   

  1. 安徽省药物临床评价中心 皖南医学院弋矶山医院,芜湖 241001
  • 出版日期:2016-01-29 发布日期:2016-02-01

Analysis of Plasma Protein Binding of Helicid Using Equilibrium Dialysis Method:An Investigation on Species Differences

JIA Yuan-wei,SHEN Jie*,XIE Hai-tang,LI Xiang-hong,LIANG Da-hu,WANG Min-hui,HU Hua   

  1. Anhui provincial Center for Drug Clinical Evaluation,Yijishan Hospital of Wannan Medical College,Anhui Wuhu 241001,China
  • Online:2016-01-29 Published:2016-02-01

摘要: 糖苷类化合物豆腐果苷在人与大鼠体内处置过程存在种属差异。药物血浆蛋白结合率是决定药物整体分布、排泄、活性及毒性的重要决定过程。本文旨在应用平衡透析法评价蛋白结合率差异在豆腐果苷种属差异中的作用。研究采用HPLC-ESI-MS方法进行检测,并对试验中的一些影响因素进行了优化。在试验中的四个浓度下,大鼠血浆蛋白结合率在10.33%~11.03%,人血浆蛋白结合率在10.60%~10.98%。结果表明人与大鼠药代动力学参数的差异不是由蛋白结合率的差异所导致。这是有关豆腐果苷蛋白结合率相关研究的首次报道。

关键词: 血浆蛋白结合率, 豆腐果苷, HPLC-ESI-MS, 种属差异

Abstract: Previous studies showed species difference of helicid metabolic process between human and rat. Plasma protein binding rate of drugs is an important process for determining their overall distribution,excretion,activity and toxicity. The aim of this study was to assess the effects of helicid plasma protein binding rates in species difference using equilibrium dialysis. Liquid chromatography-mass spectrometry analysis was carried out and was optimized against some influencing factors during experimental procedures. The method developed in this research was validated to be specific,sensitive and accurate. The binding fractions were about 10.33%-11.03% for rats and 10.60%-10.98% for human within four concentration levels. According to our results,it was concluded that the PK parameters differences between human and rat were not due to plasma protein binding. This was the study of helicid plasma protein binding reported for the first time.

Key words: plasma protein binding, helicid, LC-ESI-MS, species differences

中图分类号: 

R969.1