脂质体毛细管电泳方法评价有机化合物在体内的吸收

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

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(logPlw)(由保留因子k的对数值(logk)转化而来)及其在正辛醇/水体系中的疏水参数(logPow)与其渗透系数的对数值(logPm)的相关性,logPlw与logPm的相关系数为0.94,logPow与logPm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。

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.