基于低共熔溶剂增溶作用的灯盏乙素体内药动学研究

陈丽蓉; 黄冬霆; 游慧鑫; 刘永静; 王晓颖

doi:10.13748/j.cnki.issn1007-7693.20243451

基于低共熔溶剂增溶作用的灯盏乙素体内药动学研究

Study on Pharmacokinetic Behavior of Scutellarin Base on Solubilization Effect of Deep Eutectic Solvents

摘要

摘要:
目的研究不同低共熔溶剂(deep eutectic solvents，DESs)对灯盏乙素的增溶作用，以及口服后对其在大鼠体内的药动学影响。
方法建立灯盏乙素的HPLC含量测定方法，测定灯盏乙素在不同DESs中的溶解度；以大鼠为实验动物，分别灌胃给予不同DESs溶解的灯盏乙素溶液，绘制血药浓度-时间曲线，计算药动学参数，比较各组灯盏乙素的药动学行为。
结果 DESs对灯盏乙素的溶解能力远远大于传统溶剂，在氯化胆碱/乙二醇中的溶解度最大；药动学研究表明，与灯盏乙素水混悬液组相比，DESs组的血药浓度-时间曲线下面积显著增加，并延长了灯盏乙素在血液中的滞留时间。
结论 DESs对灯盏乙素有很强的增溶效果，并能显著提高灯盏乙素口服生物利用度。

Abstract:
OBJECTIVE To study the solubilization effect of different types of deep eutectic solvents(DESs) on scutellarin and its pharmacokinetic behavior after oral administration in rats.
METHODS An HPLC method was established to determine the solubility of scutellarin in different DESs. Scutellarin solutions were prepared with water and different DESs, and rats were given different scutellarin solutions by gavage. The pharmacokinetics of scutellarin solutions were studied by plasma drug concentration-time curve and pharmacokinetic parameters.
RESULTS The solubility of DESs to scutellarin was much higher than that of traditional solvents, and the solubility was the highest in choline chloride/ethylene glycol. The pharmacokinetic study showed that the area under the drug concentration-time curve of the DESs group was significantly increased compared with the water suspension group, and prolonged the residence time of scutellarin in the blood.
CONCLUSION DESs have a strong solubilization effect on scutellarin, and the oral bioavailability of scutellarin is significantly enhanced by DESs.

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