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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 measurement of liposome electrokinetic chromatography, phospholipid membrane chromatography and n-octanol / water system. Methods: Chromatographic retention factors of 20 charged drugs were determined by liposome electrokinetic chromatography and linearly correlated with the partition coefficient of phospholipid membrane chromatographic retention factor and n-octanol / water system (logP). Results: The degree of correlation between electrokinetic chromatographic retention factor of liposome and phospholipid membrane retention factor (R2 = 0.55) was higher than that of logP (R2 = 0.25). For basic drug, when it interacted with liposome , Hydrophobic force occupies a major position; for acidic drugs, which interact with the liposomes, electrostatic repulsion force plays a dominant role. CONCLUSION: The lipophilicity measurements of liposome electrokinetic chromatography, phospholipid membrane chromatography and n-octanol / water system are obviously different.