HPLC法测定洋川芎内酯Ⅰ的平衡溶解度和表观油水分配系数  

HPLC determination of equilibrium solubility and apparent oil/water partition coefficient of senkyunolide Ⅰ

作　　者：熊耀坤[1,2] 梁爽[1] 杜焰[1] 田凤[1] 冯怡[1] 

机构地区：[1]上海中医药大学中药现代制剂技术教育部工程研究中心,上海201203 [2]江西中医学院,南昌330004

出　　处：《药物分析杂志》2012年第9期1644-1647,共4页Chinese Journal of Pharmaceutical Analysis

基　　金：国家教育部科学技术研究重点项目(211060);上海市教委科研创新项目(11zz112);上海市教委重点学科(J50302);上海市教委创新项目(重点)(12ZZ124)

摘　　要：目的:测定洋川芎内酯Ⅰ的平衡溶解度和油水分配系数,为设计洋川芎内酯Ⅰ新剂型提供基础。方法:采用HPLC法测定洋川芎内酯Ⅰ的浓度,使用Megres-C18色谱柱(5μm,4.6 mm×100 mm),以乙腈-水(1∶3,v/v)为流动相,流速为1.0 mL.min-1,检测波长278 nm,测定洋川芎内酯Ⅰ在水和不同pH缓冲液介质中的平衡溶解度,及其在正辛醇-水/缓冲液中的表观油水分配系数。结果:37℃下洋川芎内酯Ⅰ在水中的平衡溶解度为34.31 mg.mL-1;洋川芎内酯Ⅰ在pH≥9.0的缓冲液溶剂体系中不稳定。在正辛醇-水体系中的表观油水分配系数13.43(lgPapp=1.13);pH值对洋川芎内酯Ⅰ表观油水分配系数影响不大。结论:洋川芎内酯Ⅰ水溶性好,表观油水分配系数适中,相对分子质量较小,可借此解析其快速入血入脑过程,预测洋川芎内酯Ⅰ有较好的应用价值。Objective ：To determine the equilibrium solubility of senkyunoide I and its partition coefficients for the n-octanol-water/buffer solution systems, so as to provide a basis for new formulations designing. Methods：A high performance liquid chromatography method was established to detect the concentration of senkyunolide I The Megres ODS（5 p,m,4.6 mm 100 ram）column was adopted, the mobile phase was acetonitri｜e-water（ 1：3, v/v）at a flow rate of 1.0 mL .min-1 , and the detection wavelength was 278 nm. The concentration of senkyunolide I in dif- ferent pH solutions and the partition coefficients for the n - oetanol - water and n - octanol - buffer solution systems were deteeted. Results： The equilibrium solubility reached a maximum of 34. 31 mg ~ mL-J in water at 37 ~C. Senkyunolide I was instable in solvent systems pH ≥9. 0. Partition coefficient of senkyunolideIwas 13.43 （lgPapp = 1.13 ） in the n - octanol - water system ; there was no significant effect of pH to partition coefficient of senkyunolide I. Conclusion ：The study showed that senkyunolide I is soluble, the partition coefficient of senkyunolide [ is moderate, and the relative molecular mass of senkyunolide I is small. Therefore,we can explain why senkyunolide I can quiekly reach into blood and brain. Senkyunolide [ can be predicted with a good application value.

关 键 词：高效液相色谱法 洋川芎内酯Ⅰ 平衡溶解度 表观油水分配系数 酸碱稳定性 药物体内过程预测 

分 类 号：R917[医药卫生—药物分析学]