鸡肝散药效成分木犀草素在大鼠体内的药代动力学  

Pharmacokinetics of luteolin from Elsholtzia blanda extracts in rats

作　　者：应景艳[1] 麻佳蕾[1] 夏宗玲[1] 姚彤炜[1] 

机构地区：[1]浙江大学药学院,浙江杭州310058

出　　处：《药学学报》2008年第5期523-527,共5页Acta Pharmaceutica Sinica

基　　金：浙江省科技厅重大科技攻关项目(2005C13026);浙江省科技厅基金资助项目(2004C33009).

摘　　要：建立RP-HPLC法测定大鼠灌胃鸡肝散提取物后血浆中木犀草素的含量,并研究木犀草素在大鼠体内的药代动力学行为。大鼠灌胃鸡肝散提取物后,血浆样品经三氯乙酸沉淀蛋白,用RP-HPLC法测定。血浆中木犀草素的线性范围为0.37~47.27μg.mL-1;定量限为0.37μg.mL-1;方法回收率93%~99%,提取回收率75%~85%,日内及日间精密度均小于5%。鸡肝散提取物在大鼠体内的药代动力学行为符合开放二室模型。经大鼠性别和测定时间两因素方差分析,提示不同性别的大鼠的血药浓度具有显著性差异。通过质谱法鉴定了血浆中代谢物为葡糖醛酸结合物。建立的大鼠血浆中木犀草素的含量测定方法具有灵敏、准确,专属性强等特点,可用于鸡肝散药效成分木犀草素的体内药代动力学研究。An RP-HPLC method for determination of luteolin from Elsholtzia blanda Benth. extracts in rats＇ plasma was established and the pharmacokinetics of luteolin in rats was studied. Drug blood samples from caudal vein were gotten after oral administration of luteolin. Plasma samples were determined by RP-HPLC after being deproteinized with trichloroacetic acid and extracted with ethyl acetate. The calibration curve was linear in the range of 0. 37 -47.27 μg · mL^-1 The limit of quantification was 0.37 μg · mL^-1 The method recovery of luteolin was 93% -99%. The extract recovery was 75% - 85%. RSDs of intra-and inter-day precisions were less than 5%. The concentration-time curve of luteolin after oral administration of Elsholtzia blanda Benth. extracts was fitted to two compartment open model. Two factors analysis of variance were adopted in the evaluation of gender and time spots for collection of blood. The result suggested that the gender-based difference in blood-drug concentrations had statistical significance. The metabolite in blood was identified as galcuronide. The method is sensitive, specific, accurate, and is appropriate for determination of luteolin in vivo.

关 键 词：高效液相色谱 鸡肝散提取物 木犀草素 药代动力学 

分 类 号：R969[医药卫生—药理学]