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机构地区:[1]广州军区武汉总医院药剂科,湖北武汉430070 [2]湖北中医药大学药学院,湖北武汉430065 [3]南方医科大学武汉临床医学院,湖北武汉430070
出 处:《中国医院药学杂志》2017年第5期409-412,共4页Chinese Journal of Hospital Pharmacy
基 金:国家"十二五"重大新药创制科技重大专项经费资助课题(编号:2013ZX09J13109-05C)
摘 要: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 apparent oil/water partition coefficients of phencynonate hydrochloride in n-octanol-water/buffer solution system and study its effect of pH value,and privide a reference for new dosage forms of benzene ring nonyl ester hydrochloride.METHODS The apparent oil-water partition coefficient of phencynonate hydrochloride was measured by shake-flask method and determined by HPLC.The effects of different pH values on apparent octanol-water partition coefficient of phencynonate hydrochloride were determined.RESULTS The apparent oil-water partition coefficient of phencynonate hydrochloride was 1.29±0.16.When the pH values of the solution were 1.2,3.0,4.5,5.0,5.5,6.0,6.8,7.0,8.0,9.0,the corresponding average lgP values of the partition coefficient of phencynonate hydrochloride were 0.31,0.72,1.16,1.34,1.99,2.26,2.22,1.61,2.34 and 3.24,respectively.CONCLUSION The apparent oil/water partition coeficients of phencynonate hydrochloride is correlated to pH value of the medium.The drug is more soluble in oil than in water at physiological pH values.
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