异长春花碱油水分配系数及pH值对其的影响

Effect of pH on Oil-water Partition Coeffi cient of Vinorelbine

目的测定异长春花碱的表观油水分配系数,研究pH值对其的影响,为异长春花碱的处方设计提供参考。方法用摇瓶法测定异长春花碱在正辛醇-水中的表观油水分配系数,建立用HPLC测定异长春花碱的方法,流动相乙腈-0.06 mol/L磷酸二氢钾（用盐酸调pH=3）（35∶65）,检测波长215 nm,加样回收率99.5%,RSD=0.8%。结果pH 5.0,5.8,6.5,7.0,8.0环境中,异长春花碱油水分配系数的平均lg P值分别为1.000 6,1.394 9,1.863 3,2.100 6和2.355 2。结论pH影响异长春花碱表观油水分配系数,在pH 5-8范围内,异长春花碱表观油水分配系数随pH增大而增大,且不受药物浓度的影响。

Objective To study the effect of pH on apparent oil-water partition coefficient of vinorelbine.Methods The apparent octanol-water partition coefficient of vinorelbine was measured by shake-flask method.The concentration of vinorelbine was measured by HPLC method.The mobile phase consisted of acetonitrile-0.06mol/L KH2PO4（35∶65） with HCL to adjust the pH to 3.The detection wavelength was 215 nm.The recovery was 99.5% with RSD of 0.8%. Results When the pH value of the solution was 5.0,5.8,6.5,7.0,8.0,respectively,the corresponding average lg P value of the partition coefficient of vinorelbine was 1.0006,1.3949,1.8633,2.1006 and 2.3552,respectively.Conclusion The effect of pH on apparent oil-water partition coefficient of vinorelbine can be described as follows： in the range of pH 5~8,the partition coefficient increases with the increasing of pH and has little relationship with the concentration of vinorelbine.