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目的:建立基于脂质体毛细管电泳(LCE)的一种快速测定脂水分配系数(P)的方法,将其测定结果与摇瓶法测得值进行比较,验证方法的可靠性和适用性。方法:根据已知P值的标准化合物在脂质体中的迁移时间tm,以其logP的非线性关系,再通过待测药物的tlip,求得药物的脂水分配系数。结果:不同批次的脂质体测得的药物的logP值的重现性较好,RSD为5.7%,用LCE法测得的6种药物的logP值与文献值吻合,平均差值为0.30。结论:LCE法简单、快速,重现性较好,从已测定的6种药物的logP值来看,准确度较高,为药物脂水分配系数的测定提供了一种新的方法。
OBJECTIVE: To establish a rapid liposome partition coefficient (P) method based on liposome capillary electrophoresis (LCE) and compare the results with those measured by shake flask method to verify the reliability and applicability of the method. Methods: According to the migration time tm of standard compounds with known P value in liposomes and its non-linear relationship with logP, and then through the tlip of the test drug, the lipid-water partition coefficient of the drug was calculated. Results: The reproducibility of the logP values of different batches of liposomes was better, with a RSD of 5.7%. The logP values of the six drugs measured by LCE method were consistent with the literature values, with an average difference of 0.30. Conclusion: The LCE method is simple, rapid and reproducible. From the logP values of the six drugs tested, the LAC method has higher accuracy and provides a new method for the determination of lipid-water partition coefficients.