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目的:测定盐酸苯环壬酯油水分配系数,研究不同pH值对药物脂水分配系数的影响,为盐酸苯环壬酯新剂型的处方设计提供理论参考。方法:本实验采用摇瓶-高效液相色谱法测定盐酸苯环壬酯在不同pH值条件下正辛醇-水/缓冲液体系中的表观脂水分配系数。结果:盐酸苯环壬酯的脂水分配系数lgP值为1.29±0.16;在pH为1.2,3.0,4.5,5.0,5.5,6.0,6.8,7.0,8.0,9.0的环境中,脂水分配系数lgP值分别为0.31,0.72,1.16,1.34,1.99,2.26,2.22,1.61,2.34,3.24。结论:盐酸苯环壬酯的脂水分配系数与介质的pH值有关,在pH4.5~8.0生理条件下,盐酸苯环壬酯的脂溶性较好,水溶性差。
OBJECTIVE: To determine the oil-water partition coefficient of phenylcynonate hydrochloride and to study the effect of different pH values on lipid-water partition coefficient of the drug. It provides a theoretical reference for the formulation design of new formulations of phencynonate hydrochloride. Methods: In this study, the apparent lipid-water partition coefficients of phencynonate hydrochloride in n-octanol-water / buffer system at different pH values were determined by shake flask-high performance liquid chromatography. Results: The lipid-water partition coefficient (lgP) of phencynonate hydrochloride was 1.29 ± 0.16. Under the condition of pH 1.2, 3.0,4.5,5.0,5.5,6.0,6.8,7.0,8.0,9.0, the lipid-water partition coefficient lgP The values were 0.31, 0.72, 1.16, 1.34, 1.99, 2.26, 2.22, 1.61, 2.34, 3.24, respectively. CONCLUSION: The lipid-water partition coefficient of phenylcynonate hydrochloride is related to the pH value of the medium. Under the pH of 4.5-8.0, phencynonate hydrochloride has better fat-solubility and poor water-solubility.