中国中药杂志

2014, v.39(09) 1593-1596

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HPLC测定白头翁皂苷D的油水分配系数及平衡溶解度
Determination of equilibrium solubility and n-octanol /water partition coefficient of pulchinenosiden D by HPLC

饶小勇;尹姗;张国松;罗晓健;简晖;冯育林;杨世林;
RAO Xiao-yong;YIN Shan;ZHANG Guo-song;LUO Xiao-jian;JIAN Hui;FENG Yu-lin;YANG Shi-lin;Beijing University of Traditional Chinese Medicine;National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine;Jiangxi University of Traditional Chinese Medicine;

摘要(Abstract):

目的:测定白头翁皂苷D的油水分配系数及其在不同溶剂中的平衡溶解度。方法:采用摇瓶法与高效液相色谱法相结合测定白头翁皂苷D的油水分配系数,采用高效液相色谱法测定白头翁皂苷D在6种有机溶剂及不同pH缓冲液中的平衡溶解度。结果:白头翁皂苷D在不同pH条件下油水分配系数大于零,随着pH升高白头翁皂苷D的平衡溶解度逐渐增加,在不同溶剂中白头翁皂苷D的平衡溶解度以甲醇最大(达到255.89 g·L-1),乙腈中最小(0.20 g·L-1)。结论:在胃肠生理条件下,白头翁皂苷D以分子状态形式存在,由lgPapp可知其吸收性较好,但水溶性较差,提示增加白头翁皂苷D的溶解度可能有利于提高其生物利用度。
Objective: To determine the equilibrium solubility of pulchinenosiden D in different solvents and its n-octanol/water partition coefficients. Method: Combining shaking flask method and high performance liquid chromatography( HPLC) to detect the n-octanol / water partition coefficients of pulchinenosiden D,the equilibrium solubility of pulchinenosiden D in six organic solvents and different pH buffer solution were determined by HPLC analysis. Result: n-Octanol / water partition coefficients of pulchinenosiden D in different pH were greater than zero,the equilibrium solubility of pulchinenosiden D was increased with increase the pH of the buffer solution. The maximum equilibrium solubility of pulchinenosiden D was 255. 89 g·L-1in methanol,and minimum equilibrium solubility of pulchinenosiden D was 0. 20 g·L-1in acetonitrile. Conclusion: Under gastrointestinal physiological conditions,pulchinenosiden D exists in molecular state and it has good absorption but poor water-solubility,so increasing the dissolution rate of pulchinenosiden D may enhance its bioavailability.

关键词(KeyWords): HPLC;白头翁皂苷D;油水分配系数;平衡溶解度
HPLC;pulchinenosiden D;equilibrium solubility;n-octanol/water partition coefficien

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基金项目(Foundation): 国家“重大新药创制”科技重大专项(2011ZX11102-001-19);; 江西省自然科学基金项目(20114BAB215045);; 江西省优势科技创新团队计划项目(2010DQB01700);; 江西省教育厅产学研合作项目(GJJ11006)

作者(Author): 饶小勇;尹姗;张国松;罗晓健;简晖;冯育林;杨世林;
RAO Xiao-yong;YIN Shan;ZHANG Guo-song;LUO Xiao-jian;JIAN Hui;FENG Yu-lin;YANG Shi-lin;Beijing University of Traditional Chinese Medicine;National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine;Jiangxi University of Traditional Chinese Medicine;

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