灯盏乙素脂质体的制备及其在大鼠体内药动学

摘要

目的 研究卡波姆包衣灯盏乙素脂质体的制备,并考察其在大鼠体内的药动学特性.方法 采用薄膜分散法制备灯盏乙素脂质体,通过孵育法用卡波姆对灯盏乙素脂质体包衣,用微柱离心法测定其包衣前后包封率的变化;将SD大鼠随机分成3组,分别灌胃给予灯盏乙素混悬液、灯盏乙素脂质体及灯盏乙素包衣脂质体,比较药动学特征.结果 灯盏乙素包衣脂质体大鼠灌胃给药后药动学呈双室模型特征,灯盏乙素混悬剂、脂质体及包衣脂质体经大鼠灌胃给药后,AUC0-∞ 分别为(50.03±13.45),(78.99±20.28)和(107.97±27.26)μg?h?mL-1,与灯盏乙素混悬液及脂质体相比,其包衣脂质体的口服AUC0-∞ 显著提高(P<0.01).结论 包衣脂质体可明显提高灯盏乙素的生物利用度,药物峰浓度显著增加.%Objective To prepare scutellarin liposomes and to investigate the pharmacokinetics in rats. Methods The liposomes of scutellarin coated with carbopol were prepared with the film dispersion method.Minicolumn centrifugation method was applied to measure the encapsulation efficiency (EE) before and after coating. SD rats were randomly divided into three groups, which were given intragastric administration of scutellarin suspension, scutellarin liposomes, and carbopol-coated scutellarin liposomes, respectively. And then the pharmacokinetic parameters were compared. Results Carbopol-coated scutellarin liposomes after intragastric administration in rats showed pharmacokinetic characteristics of two-compartment model. The main pharmacokinetic parameters of scutellarin suspension,scutellarin liposomes,and carbopol-coated scutellarin liposomes were as follows:AUC0-∞(50.03±13.45) μg?h?mL-1 ,(78.99±20.28) μg?h?mL-1 ,and (107.97±27.26) μg?h?mL-1 , respectively. Conclusion After coated liposomes, the oral bioavailability of scutellarin 1iposomes can be significantly improved,and the maximum drug concentration also increased.