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脂质体毛细管电泳方法评价有机化合物在体内的吸收

邹小兵1,2,蒋宏贵1,董志强1,夏之宁1,2,蒋雪梅2   

  1. 1.Department of Pharmaceutics, Institute of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, China; 2.College of Bioengineering, Chongqing University, Chongqing 400030, Chin
  • 收稿日期:2008-04-23 修回日期:2008-07-01 出版日期:2008-11-30 发布日期:1983-06-25
  • 通讯作者: 夏之宁
  • 基金资助:
    国家自然科学基金项目(批准号:20775096)和科技部国际合作项目(2006DFA43520)

Evaluation of absorption of organic compounds in human body using liposome capillary electrophoresis

ZOU Xiaobing1,2, JIANG Honggui1, DONG Zhiqiang1, XIA Zhining1,2, JIANG Xuemei2   

  1. 1.Department of Pharmaceutics, Institute of Chemistry and Chemical Engineering, Chongqing University, Chongqing 400030, China; 2.College of Bioengineering, Chongqing University, Chongqing 400030, Chin
  • Received:2008-04-23 Revised:2008-07-01 Online:2008-11-30 Published:1983-06-25
  • Contact: XIA Zhining

摘要: 有机化合物在脂质体毛细管电泳中的保留值大小可以体现化合物的亲脂性大小。比较了9种有机化合物在脂质体毛细管电泳中脂质体/水的疏水参数(log Plw)(由保留因子k的对数值(log k)转化而来)及其在正辛醇/水体系中的疏水参数(log Pow)与其渗透系数的对数值(log Pm)的相关性,log Plw与log Pm的相关系数为0.94,log Pow与log Pm的相关系数仅为0.78,说明脂质体/水模型较正辛醇/水模型更加接近于生物膜模型。脂质体毛细管电泳可以快速、准确地测定化合物的疏水参数,通过化合物在脂质体毛细管中的保留可以快速、初步地预测化合物在体内的吸收情况。

关键词: 渗透系数, 疏水参数, 体内吸收, 有机化合物, 预测 , 脂质体毛细管电泳

Abstract: Liposome capillary electrophoresis (LCE) was used as a model for the in vitro evaluation of the degree of membrane penetration of organic compounds. The hydrophobic parameters of 9 compounds were determined by LCE. In comparison of the correlation coefficient of log Plw ( the logarithm of the partition coefficient of liposome/water system, calculated from retention factor) vs. log Pm (the logarithm of osmotic coefficient) with that of log Pow (the logarithm of the partition coefficient of octanol/water system) vs. log Pm, the former was 0.94, much greater than the latter 0.78. It means that as the biomembrane model, liposome is more similar than the octanol/water system. The LCE method has the potential to be an in vitro screening model.

Key words: absorption in human body, hydrophobic parameter, organic compounds, permeability coefficient, prediction , liposome capillary electrophoresis