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目的:测定盐酸吲哚美辛2-[2-(6-甲氧基-2-萘基)吗啉基]乙酯在乙醇、乙腈、丙酮、乙酸乙酯等溶剂中的平衡溶解度以及在正辛醇-水和正辛醇-缓冲液体系中的表观油水分配系数。方法:采用HPLC法测定盐酸吲哚美辛2-[2-(6-甲氧基-2-萘基)吗啉基]乙酯的浓度,采用摇瓶法测定其表观油水分配系数。结果:25℃时盐酸吲哚美辛2-[2-(6-甲氧基-2-萘基)吗啉基]乙酯在乙醇、乙腈、丙酮、乙酸乙酯中的平衡溶解度分别为31.36,141.50,575.77,598.68 g.L-1。pH=4时此目的化合物的平衡溶解度最小,而表观油水分配系数最大。结论:盐酸吲哚美辛2-[2-(6-甲氧基-2-萘基)吗啉基]乙酯的平衡溶解度及油水分配系数与介质的pH有关。其水溶性较差,脂溶性好。
OBJECTIVE: To determine the equilibrium solubility of indomethacin 2- [2- (6-methoxy-2-naphthyl) morpholinyl] ethyl acetate in solvents such as ethanol, acetonitrile, acetone and ethyl acetate, Apparent Oil - Water Partition Coefficients in Octanol - Water and Octanol - Buffer Systems. Methods: The concentration of indomethacin 2- [2- (6-methoxy-2-naphthyl) morpholinyl] ethyl hydrochloride was determined by HPLC. The apparent oil-water partition coefficient was determined by shake flask method. Results: The equilibrium solubility of indomethacin 2- [2- (6-methoxy-2-naphthyl) morpholinyl] ethyl acetate in ethanol, acetonitrile, acetone and ethyl acetate at 25 ℃ were 31.36 , 141.50, 575.77, 598.68 gL-1. The target compound has the lowest equilibrium solubility at pH = 4 and the largest apparent water-oil partition coefficient. CONCLUSION: The equilibrium solubility, oil-water partition coefficient and solubility of indomethacin 2- [2- (6-methoxy-2-naphthyl) morpholinyl] ethyl ester are related to the pH of the medium. Its poor water solubility, fat soluble.