槲皮素平衡溶解度的测定及热力学计算

目的: 测定槲皮素在不同溶剂中的平衡溶解度和表观油水分配系数,为槲皮素的提取纯化及剂型设计提供依据。方法: 采用高效液相色谱法测定槲皮素在9种溶剂中的平衡溶解度及表观油水分配系数,并计算槲皮素在水和正辛醇中达到溶解平衡的热力学参数。结果: 槲皮素在水和正辛醇中的平衡溶解度随温度的升高而升高,在水和正辛醇中的溶解过程是吸热的(Δ_solH⁰>0),并且是熵增加过程;槲皮素在丙酮中溶解度最大,为16.91 mg·mL^-1,水中最小,为0.09 μg·mL^-1;常温下槲皮素的表观油水分配系数为29 813.46(lgP=4.47)。结论: 槲皮素为水溶性较差的中等极性化合物,可考虑应用增溶辅料或通过制剂技术增大溶解度,以提高生物利用度。

Objective: To determine the equilibrium solubility of quercetin in different solvents,so as to provide a basis for extraction and dosage form design. Methods: A high performance liquid chromatography(HPLC)was established to detect the equilibrium solubility of quercetin in nine solvents and the apparent coefficient;and to calculate the thermodynamic parameters for quercetin reaching equilibrium solubility in the 1-octanol and water system. Results: The solubility of quercetin in water and 1-octanol increased with the increase of temperature.The process of dissolving in water and 1-octano was endothermic(Δ_solH⁰>0),meanwhile the entropy was increasing.The maximum solubility of quercetin was in acetone,being 16.91 mg·mL^-1 and the minimum in water,being 0.09 μg·mL^-1.The apparent oil-water partition coefficient of quercetin at room temperature was 29 813.46(lgP=4.47). Conclusion: Quercetin is a moderate-polar compound which has a poor water solubility and a good permeability.Therefore solubilizers and drug preparation technology can be considered to increase its equilibrium solubility in order to improve its bioavailability.

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