摘要
目的测定盐酸雷洛昔芬的平衡溶解度以及表观油水分配系数,为药物新剂型设计与研究提供基础。方法采用饱和溶液法和摇瓶法测定盐酸雷洛昔芬在蒸馏水和pH 2.0-9.0磷酸盐缓冲液的平衡溶解度及其在正辛醇-水/磷酸盐缓冲液体系中的表观油水分配系数。结果 37℃时,盐酸雷洛昔芬在水中溶解度为（3.941±0.06）μg/mL,在pH 2.0-9.0缓冲液中,平衡溶解度随pH值升高而减小;盐酸雷洛昔芬在正辛醇-水体系中表观油水分配系数（P）为（17.261±2.84）,lgP=1.24;在正辛醇-缓冲液体系中,P值随pH值升高而增大。结论本文建立的测定方法简单可行,盐酸雷洛昔芬不溶于水,且pH值影响平衡溶解度和表观油水分配系数。
Objective To determine the equilibrium solubility and the apparent oil/water partition coefficient of raloxifene hydrochloride. Methods A saturated solution and shake flask method was applied to determine the equilibrium solubility and the apparent partition coefficient of raloxifene hydrochloride in water and phosphate buffer solution with pH 2. 0 - 9.0 value. Results The equilibrium solubility of raloxifene hydrochloride in water was （3.941 ±0.06）μg/mL, and the equilibrium solubility decreased as the increase of pH value. The apparent oil/water partition coefficient （P） of raloxifene hydrochloride in water was （ 17.261 ± 2.84）, lgP = 1.24, and the partition coefficient increased as the increase of pH value. Conclusion The shake flask method was simple and feasible in this study. Raloxifene hydrochloride was not soluble in water, and the equilibrium solubility, as well as the apparent oil/water partition coefficient were influenced by the pH value.
出处
《广东药学院学报》
CAS
2014年第3期269-273,共5页
Academic Journal of Guangdong College of Pharmacy
基金
广东药学院大学生创新创业训练计划项目(1057313034)
广东省科技计划项目(粤科规划字[2013]137号)
关键词
盐酸雷洛昔芬
平衡溶解度
表观油水分配系数
PH值
raloxifene hydrochloride
equilibrium solubility
apparent oil/water partition coefficient
pH value
