pH值对吲哚美辛芳基吗啉酯衍生物表观油水分配系数的影响

Effect of pH on Apparent Oil/Water Partition Coefficient of Prodrugs of Indomethacin

摘要: 目的测定盐酸吲哚美辛芳基吗啉酯衍生物的表观油水分配系数并探讨pH值和结构改造对其的影响。方法用摇瓶法测定盐酸吲哚美辛芳基吗啉酯衍生物在正辛醇缓冲液体系中的表观油水分配系数，建立紫外分光光度法测定其含量。结果 25 ℃时盐酸吲哚美辛芳基吗啉酯衍生物在pH为4时其表观油水分配系数最大。结论盐酸吲哚美辛芳基吗啉酯衍生物的表观油水分配系数与介质的pH和结构改造中引入基团的极性等因素有关。

Abstract: OBJECTIVE To study the effect of pH on apparent oil/water partition coefficient of prodrugs of indomethacin. METHODS The apparent oil/water partition coefficient of prodrugs of indomethacin was measured by shaking flask method. The concentration of prodrugs of indomethacin was determined by UV. RESULTS When the temperature was 25 ℃, the prodrugs of indomethacin have the highest partition coefficients in n-octanol/pH 4 buffer solution system. CONCLUSION The apparent oil/water partition coefficients of prodrugs of indomethacin are correlated to pH of the medium and the polarity of group which is added.