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 measure lipid-water partition coefficients(P)of pharmaceuticals by LCE method.And its logarithm(logP)values of six pharmaceuticals determined by this LCE method were compared with literature values.Method:The migration time of liposome phase(tlip)was obtained by non-linearity fitting with logP values from literature and measured migration time(tm)of a series of standard compounds,a calibration curve for estimating logP of pharmaceuticals was thus obtained.Results:The logP values of 3 pharmaceuticals measured by LCE method using the different liposome were close to the literatures,and the average RSD was 5.7%.The logP values of 6 pharmaceuticals measured by LCE method were close to those determined by shake-flask method,and the average error between values from two methods was 0.30.Conclusions:This method is simple,rapid,reproducible and reliable,which can be useful to estimate lipid-water partition coefficients of pharmaceuticals.