败酱皂苷H_1平衡溶解度和表观油水分配系数的测定  

Determination of Solubility and Apparent Oil and Water Partition Coefficient of Saponin H_1

作　　者：房启龙[1] 刘宏尉 刘江云[1] 郝丽莉[1] 杨世林[1] 

机构地区：[1]苏州大学医学部药学院,江苏苏州215123

出　　处：《中国药房》2016年第3期364-366,共3页China Pharmacy

基　　金：国家自然科学基金资助项目(No.81274190);江苏省重大科技支撑与资助创新专项项目(No.BE2012649)

摘　　要：目的：测定败酱皂苷H1平衡溶解度和表观油水分配系数（1g P）,为败酱皂苷后续的剂型设计和成药性研究提供参考。方法：采用高效液相色谱-蒸发光散射检测（HPLC-ELSD）法测定败酱皂苷H1在不同有机溶剂和不同pH缓冲液中的平衡溶解度;采用摇瓶法测定败酱皂苷H1的1g P。结果：25℃下败酱皂苷H1在水、甲醇和乙醇中的平衡溶解度依次为0.091 75、96.51、46.89 g/L,在磷酸盐缓冲液pH 7.6-10.0范围内平衡溶解度随着pH升高而明显增大;败酱皂苷H1在pH 6.0-8.0缓冲液中其1g P范围为0.695-0.773。结论：败酱皂苷H1及该类齐墩果酸型皂苷属于低溶解度、低透过性的成分,因而不适宜作为常规口服制剂开发使用。OBJECTIVE： To determine the solubility and apparent oil and water partition coefficient （lg P） of saponin H1, and provide reference for dosage form design and druggability research of saponin. METHODS： HPLC-ELSD was conducted to determine the equilibrium solubility of saponin H1 in different organic solvents and pH buffer solutions ; shaking flask was applied to determine lg P value of saponin H1. RESULTS：The equilibrium solubility of saponin H1 in water, methanol and ethanol at 25 μ was 0.09175 g/L, 96.51 g/L and 46.89 g/L, respectively. The solubility increased apparently at high pH within pH range at 7.6-10.0; the lg P value was between 0.695-0.773 in buffers within pH range at 6.0-8.0. CONCLUSIONS： Saponin H1 and the oleanolic acid type saponins belong to low solubility, low transmission components, so it is not suitable for use as a conventional oral formulation is developed.

关 键 词：败酱皂苷H1 高效液相色谱-蒸发光散射检测法 平衡溶解度 表观油水分配系数 

分 类 号：R917[医药卫生—药物分析学]