Equilibrium Solubility and Dissolution Thermodynamic Analysis of Isorhamnetin

ZHANG Hui-jie; CHEN Lin; WANG Meng; CHEN Li-na; LIU Ya-nan; REN Xiao-liang; DENG Yan-ru; QI Ai-di

doi:10.13422/j.cnki.syfjx.2016170015

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Equilibrium Solubility and Dissolution Thermodynamic Analysis of Isorhamnetin

更新时间：2024-01-04

- Equilibrium Solubility and Dissolution Thermodynamic Analysis of Isorhamnetin
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 22, Issue 17, Pages: 15-18(2016)
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2016170015
  CLC： TQ460.1
- Published：2016
- 稿件说明：
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ZHANG Hui-jie, CHEN Lin, WANG Meng, et al. Equilibrium Solubility and Dissolution Thermodynamic Analysis of Isorhamnetin[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(17): 15-18.
DOI：

ZHANG Hui-jie, CHEN Lin, WANG Meng, et al. Equilibrium Solubility and Dissolution Thermodynamic Analysis of Isorhamnetin[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(17): 15-18. DOI： 10.13422/j.cnki.syfjx.2016170015.

摘要

目的：测定异鼠李素在水及正辛醇中的溶解度，计算热力学参数，为异鼠李素剂型设计与体内过程预测提供依据。方法：采用HPLC测定不同温度下异鼠李素在水、正辛醇中的平衡溶解度，测定常温下该成分在正辛醇-水中的表观油水分配系数，流动相甲醇-0.1%甲酸水溶液（70：30），检测波长370 nm。结果：异鼠李素水溶性差，易溶于正辛醇中，采用Apelblat经典模型对异鼠李素溶解度数据进行拟合，在水、正辛醇中的溶解度拟合方程为lnxcal=879.18-53895.05/T-126.30lnT（r=0.9997），lnxcal=-1.32-2699.36/T+0.35lnT（r=0.9998），表明该模型拟合结果与实验数据吻合良好。异鼠李素在水和正辛醇中的溶解过程均为吸热和熵增加的过程，常温下异鼠李素的表观油水分配系数P为5163（lgP=3.71）。结论：异鼠李素为脂易溶性化合物，水溶性较差，通过优化制剂工艺等方法增加其水溶解度可能会提高其口服吸收效率及生物利用度。

Abstract

Objective: To determine equilibrium solubility of isorhamnetin in water and 1-octanol

then calculate thermodynamic parameters

which might be important for its further studies on formulation development and in vivo absorption. Method: HPLC was established to determine equilibrium solubility of isorhamnetin in water and 1-octanol at different temperatures and its apparent partition coefficient in 1-octanol-water solution system. Result: Solubility of isorhamnetin in water and 1-octanol increased with increasing of temperature.Isorhamnetin was more soluble in 1-octanol than in water.Solubility data of isorhamnetin were fitted with Apelblat classic model

its regression equations in water and 1-octanol were lnxcal=879.18-53895.05/T-126.30lnT (r=0.9997)

lnxcal=-1.32-2699.36/T+0.35lnT (r=0.9998).The dissolution processes in water and 1-octanol over the experimental temperature range were endothermic with increasing of entropy.The apparent oil-water partition coefficient of isorhamnetin at room temperature was 5163(lgP=3.71). Conclusion: Isorhamnetin is a fat soluble compound

its water-solubility is poor.By optimizing preparation process and other methods can improve its oral absorption efficiency and bioavailability.

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