Determination of Equilibrium Solubility and Apparent Oil-water Partition Coefficient of -Hederin

HE Ming-zhen; LIANG Qi-dong; RAO Xiao-yong; OUYANG Hui; SU Dan; SUN Yong-bing; MENG Tuo; FENG Yu-lin; YANG Shi-lin

doi:10.13422/j.cnki.syfjx.2014130052

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Determination of Equilibrium Solubility and Apparent Oil-water Partition Coefficient of -Hederin

更新时间：2024-01-04

- Determination of Equilibrium Solubility and Apparent Oil-water Partition Coefficient of -Hederin
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 20, Issue 13, Pages: 52-54(2014)
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2014130052
  CLC： R284.1
- Published：2014
- 稿件说明：
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HE Ming-zhen, LIANG Qi-dong, RAO Xiao-yong, et al. Determination of Equilibrium Solubility and Apparent Oil-water Partition Coefficient of -Hederin[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(13): 52-54.
DOI：

HE Ming-zhen, LIANG Qi-dong, RAO Xiao-yong, et al. Determination of Equilibrium Solubility and Apparent Oil-water Partition Coefficient of -Hederin[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(13): 52-54. DOI： 10.13422/j.cnki.syfjx.2014130052.

摘要

目的：测定α-常春藤皂苷的平衡溶解度及表观油水分配系数（Papp）。方法：采用HPLC测定α-常春藤皂苷在水、有机溶剂及缓冲液中平衡溶解度，在正辛醇-水及缓冲盐溶液中表观油水分配系数，流动相乙腈-0.2%磷酸水溶液（45：55），检测波长203 nm。结果： 25 ℃时，α-常春藤皂苷在水中平衡溶解度0.011 g·L-1，Papp=24.73（logPapp=1.39），在正丁醇和乙醇中平衡溶解度分别为86.10，28.18 g·L-1。结论： α-常春藤皂苷的水溶性较差，改善其口服制剂的溶出度有利于提高体内生物利用度。

Abstract

Objective: To determine equilibrium solubility and apparent oil-water partition coefficient(Papp) of α-hederin. Method: HPLC was adopted to determine equilibrium solubilities of α-hederin in water

organic solvents and buffer solutions

then determine partition coefficients in n-octanol/water and buffer salt solutions

mobile phase of acetonitrile-0.2% phosphoric acid(45:55)

detection wavelength was set at 203 nm. Result: At 25 ℃

equilibrium solubility of α-hederin was 0.011 g·L-1 in water and Papp was 24.37(logPapp=1.39);Equilibrium solubilities of α-hederin were 86.10 and 28.18 g·L-1 in n-butyl alcohol and ethanol

respectively. Conclusion: α-Hederin was a hydrophobic drug

increasing dissolution of α-hederin from its oral drug delivery system had possibility to enhance its bioavailability.

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