熊果酸平衡溶解度和油水分配系数的测定.pdf

·药 剂· 熊果酸平衡溶解度和油水分配系数的测定 1,2 1,3 1* 林杭娟 , 钦富华 , 高建青 (1.浙江大学药学院，杭州 310058 ；2.宁波市中医院，浙江 宁波 315010 ；3.浙江医药高等专科学校， 浙江 宁波 315100) 摘要：目的 测定熊果酸的平衡溶解度及其在正辛醇-水中的表观油水分配系数，为设计熊果酸新剂型提供基础。方法 采 用HPLC 测定熊果酸在不同pH 介质、不同溶剂中的溶解度及熊果酸在正辛醇-水中的表观油水分配系数。结果 25 ℃下 熊果酸在水中的平衡溶解度为5.64 mg·L1 ，在pH 2.0~7.4 的缓冲体系中，熊果酸的溶解度不受pH 的影响。熊果酸在油 中溶解度不佳，在表面活性剂及半极性溶剂中溶解度相对较好，在正辛醇-水体系中的油水分配系数1gP=2.17。结论 熊 果酸为溶解度小的亲脂性药物。 关键词：熊果酸；平衡溶解度；表观油水分配系数 中图分类号：R943.3 文献标志码：A 文章编号：1007-7693(2012)07-0635-03 Determination of Equilibrium Solubility and Apparent Oil/Water Partition Coefficient of Ursolic Acid LIN Hangjuan1,2, QIN Fuhua1,3, GAO Jianqing1*(1.College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China; 2.Ningbo Municipal Hospital of TCM, Ningbo 315010, China; 3.Zhejiang Pharmaceutical College, Ningbo 315100, China) ABSTRACT: OBJECTIVE To determine the equilibrium solubility of ursolic acid and its partition coefficients in the n-octanol-water system for designing new formulations．METHODS High performance liquid chromatography (HPLC) was established to determine the contents of ursolic acid in different pH solutions, differernt solvents and the partition coefficients for the n-octanol- water systems. RESULTS The equilibrium solubility of ursolic acid was 5.64 mg·L1 in water at 25 ℃and was not influenced by the pH of the buffer solution. The solubility of ursolic acid in oils was poor, but was relatively good in surfactants and Semi polar solvents. Partition coefficient of ursolic acid was 2.17 in n-octanol-water system. CONCLUSION Ursolic acid is a lipophilic drug with little solubility property. KEY WORDS: ursolic acid; equilibrium solubility; apparent oil/water partition coefficient 熊果酸(ursolic acid，UA)又名乌索酸、乌苏酸， 油水分配系数的文献报道。本实验对UA 的平衡溶 属三萜类化合物，在自然界分布很广，以游离形 解度、油水分配