脂质体电动色谱与磷脂膜色谱及正辛醇/水系统亲脂性测量尺度的比较研究

Comparative study of lipophilicity from liposome electrokinetic chromatography and phospholipid membrane chromatography and n-octanol/water systems

目的:对脂质体电动色谱、磷脂膜色谱、正辛醇/水系统的亲脂性测量尺度进行比较研究。方法:采用脂质体电动色谱法测定了20种荷电药物的色谱保留因子,并与磷脂膜色谱保留因子和正辛醇/水系统分配系数(logP)进行线性相关比较。结果:脂质体电动色谱保留因子与磷脂膜保留因子的相关程度(R2=0.55)比其与logP的相关程度(R2=0.25)要高;对于碱性药物,其与脂质体相互作用时,疏水作用力占据主要地位;对于酸性药物,其与脂质体相互作用时,静电排斥力占据了主导作用。结论:脂质体电动色谱、磷脂膜色谱、正辛醇/水系统三者的亲脂性测量尺度明显不同。

Objective：To compare the lipophilicity from liposome electrokinetic chromatography and phospholipid membrane chromatography and n-octanol/water systems.Method：The retention factors of twenty drugs were determined with liposome electrokinetic chromatography,and were correlated with the retention factors of phospholipid membrane chromatography and n-octanol/water partition coefficients（logP）.Result：The degree of correlation between the retention factors of liposome electrokinetic chromatography and the retention factors of phospholipid membrane chromatography was higher than that between liposome electrokinetic chromatography and logP.Hydrophobic interaction was dominating when basic drugs interacted with liposome,electrostatic force was primary as acidic drugs interacted with liposome.Conclusion：Lipophilicity from liposome electrokinetic chromatography and phospholipid membrane chromatography and n-octanol/water systems was remarkable different.