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一种用于测定大鼠血浆中灯盏花素及其药代动力学的高效液相色谱法的验证

Validation of an HPLC method for the determination of scutellarin in rat plasma and its pharmacokinetics.

作者信息

Hao Xiuhua, Cheng Gang, Sun Jin, Zou Meijuan, Yu Jie, Zhang Shuang, Cui Fude

机构信息

Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.

出版信息

J Pharm Biomed Anal. 2005 Jun 15;38(2):360-3. doi: 10.1016/j.jpba.2005.01.004.

DOI:10.1016/j.jpba.2005.01.004
PMID:15925232
Abstract

A validated HPLC method was developed for the quantification of scutellarin in rat plasma using a liquid-liquid extraction and an ultraviolet detection. Chromatographic separation of scutellarin in plasma was performed on a C18 column, with a mobile phase of acetonitrile-water (23:77, v/v), adjusted to pH 2.5 with 1M phosphoric acid, and rutin was used as an internal standard. The calibration curve was linear over the range 0.1-100 microg/ml in rat plasma. The average extraction recoveries were 85.9+/-8.9, 71.0+/-4.6, 72.7+/-1.2% (n=3) at concentrations of 0.1, 2, 100 microg/ml, respectively, and the within-day and between-day precisions were less than 15%. After intravenous administration to rats over the doses range of 10-40 mg/kg, the plasma concentration-time curve of scutellarin was best conformed to three-compartment open model. The AUC of scutellarin was proportional to dose, and the systemic clearance (Cl), elimination half-life (t1/2beta) and apparent volume of distribution (Vc) were not significantly different among the three doses, suggestive of the linear pharmacokinetics characteristic of scutellarin after intravenous administration.

摘要

建立了一种经过验证的高效液相色谱法,用于测定大鼠血浆中灯盏花素的含量,采用液-液萃取和紫外检测。血浆中灯盏花素的色谱分离在C18柱上进行,流动相为乙腈-水(23:77,v/v),用1M磷酸调节至pH 2.5,芦丁用作内标。校准曲线在大鼠血浆中0.1-100μg/ml范围内呈线性。在浓度分别为0.1、2、100μg/ml时,平均萃取回收率分别为85.9±8.9%、71.0±4.6%、72.7±1.2%(n=3),日内和日间精密度均小于15%。大鼠静脉注射剂量范围为10-40mg/kg后,灯盏花素的血浆浓度-时间曲线最符合三室开放模型。灯盏花素的AUC与剂量成正比,三种剂量下的全身清除率(Cl)、消除半衰期(t1/2β)和表观分布容积(Vc)无显著差异,提示灯盏花素静脉注射后具有线性药代动力学特征。

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