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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。
OBJECTIVE To determine the apparent oil-water partition coefficient of aryl morpholine derivatives of indomethacin hydrochloride and to explore the effect of pH value and structure modification on it. Methods The apparent oil-water partition coefficients of indomethacin-based aryl morpholine derivatives in n-octanol buffer were determined by shake flask method. The content of indomethacin derivatives was determined by ultraviolet spectrophotometry. Results At 25 ℃, the apparent oil-water partition coefficients of indomethacin aryl morpholine derivatives at pH 4 were the highest. Conclusion The apparent oil-water partition coefficients of aryl morpholine derivatives of indomethacin hydrochloride are related to the pH of the medium and the polarity of the introduced groups in the structural modification.