摘要
目的:建立大鼠血浆中雷公藤内酯醇的HPLC测定法,测定大鼠尾静脉注射雷公藤内酯醇后的血药浓度,并对其药代动力学进行评价。方法:血浆样品加入适量HCl后用乙酸乙酯提取进行HPLC分析,流动相为乙腈-水(23:77),流速为1.0ml/min,检测波长为217nm。大鼠尾静脉注射100μg/kg、200μg/kg、300μg/kg的三个剂量雷公藤内酯醇后,测定血浆中不同时间点雷公藤内酯醇的浓度,并计算主要药动学参数。结果:血浆中雷公藤内酯醇在0.02~10.0μg/ml浓度范围内线性关系良好,血浆中雷公藤内酯醇的最低检测线为0.02μg/ml,平均回收率为88.03%,日内和日间差异RSD均小于5%,峰面积与血药浓度呈良好的线性关系(r2=0.9993)。大鼠尾静脉分别注射三个剂量雷公藤内酯醇后,各剂量纽相对应的分布相(t1/2α)半衰期分别为:0.033,0.021,0.026h。消除相半衰期(t1/2β)分别为:0.753,0.630,0.574h。结论:本实验方法简便,可靠,可用于雷公藤内酯醇血药浓度分析及其药代动力学研究,测定结果可为该药的临床用药提供依据。
Objectives: To develop a high performance liquid chromatographic ( HPLC ) assay for determination of triptolide in rats plasma and to study the pharmacokinetics of triptolide in rats. Method: The plasma samples were extracted by ethyl acetate and seperated by a C18 reversed-phase column. The acetonitrile and the purified water composed mobile phase. The flow rate was 1.0 ml/min, ultraviolet detection wavelength was at 217 nm. Result: The calibration curve was linear over the range from 0. 02 - 10.0 μg/ml with a correlation coefficiency of 0. 9993. The lower limit of quantitation (LLOQ) was 0. 02 μg/ml. The mean recovery was 88.03%. The relative standard deviation (RSD) of intra-day and inter-day were all less than 15%. After intravenous administration of triptolide with 3 dosages of 100, 200, 300 μg/kg to rats, the corresponding distribution half-lives (t1/2α) were 0. 033, 0. 021, 0. 026 h, and the elimination half-lives (tl/213) were 0. 753, 0. 630, 0. 574 h, respectively. Conclution: This method is convenient, accurate and reliable. It can be used for determination of triptolide in rats plasma and pharmacokinetic studies.
出处
《中药药理与临床》
CAS
CSCD
北大核心
2007年第2期15-17,共3页
Pharmacology and Clinics of Chinese Materia Medica
基金
福建省重点建设高校项目(NoXZ04001)
福建省重大专项前期研究课题(NoYZ20051008)