甘草香豆素平衡溶解度和油水分配系数的测定  

Determination of equilibrium solubility and oil-water partition coefficient of glycycoumarin

作　　者：汤玉梅 欧水平 叶林虎 黄玉普 王森 TANG Yu-mei;OU Shui-ping;YE Lin-hu;HUANG Yu-pu;WANG Sen(College of Pharmacy,Zunyi Medical University,Zunyi Guizhou 563000;Affiliated Hospital of Zunyi Medical University,Zunyi Guizhou 563099)

机构地区：[1]遵义医科大学药学院,贵州遵义563000 [2]遵义医科大学附属医院,贵州遵义563099

出　　处：《中南药学》2023年第4期959-962,共4页Central South Pharmacy

基　　金：贵州省科技计划项目(黔科合基础-ZK[2023]一般561);贵州省科技计划项目(No.黔科合支撑[2020]4Y118号)。

摘　　要：目的测定甘草香豆素的平衡溶解度及其油水分配系数,为甘草香豆素的剂型设计提供依据。方法用烧瓶法测定其在不同pH缓冲液中的溶解度,用高效液相色谱法和摇瓶法测定甘草香豆素的油水分配系数。结果37℃时甘草香豆素在pH为1.2、2.0、5.0、6.8、7.4的缓冲液以及水中的平衡溶解度分别为39.17、38.26、24.00、23.83、25.44、28.00μg·L^(-1),高效液相色谱法测得油水分配系数为(3.06±0.0002),摇瓶法中pH 2.0缓冲液中油水分配系数最小。结论本文建立的甘草香豆素的含量测定方法可行,37℃时甘草香豆素不溶或几乎不溶于水,在pH 1.2~7.4随着pH的增大平衡溶解度逐渐减小,属于水难溶性、高渗透性、亲脂性药物,可考虑通过提高溶解度改善其药物溶出和吸收。Objective To determine the equilibrium solubility and oil-water partition coefficient of glycycoumarin,and to provide a basis for the dosage form design of glycycoumarin.Methods The Flask method was used to determine its solubility in water and HPLC method and the shakflask method were used to determine the oil-water partition coefficient collection of glycycoumarin.Results The equilibrium solubilities of glycycoumarin in buffers with pH 1.2,2.0,5.0,6.8 and 7.4,and water at 37℃were 39.17,38.26,24.00,23.83,25.44,and 28.00μg·L^(-1),respectively.The oilwater partition coefficient was(3.06±0.0002)by HPLC,and the oil-water partition coefficient was the smallest in pH 2.0 buffer by.Conclusion The content determination of glycycoumarin is feasible.It is almost insoluble in water at 37℃.The equilibrium solubility decreases gradually with the increase of pH between 1.2 and 7.4,which is a water-insoluble,highly permeable,and lipophilic drug.The dissolution and absorption can be improved by increasing the solubility.

关 键 词：甘草香豆素 溶解度 油水分配系数 烧瓶法 高效液相色谱法 

分 类 号：R932[医药卫生—生药学]