青蒿素在Wistar大鼠体内的药代动力学研究  

Pharmacokinetic Study of Artemisinin in Wistar Rats

作　　者：李飞艳[1] 姚晓霞[1] 田文慧[1] 袁强[1] 

机构地区：[1]浙江中医药大学药学院,浙江杭州311402

出　　处：《时珍国医国药》2017年第10期2313-2315,共3页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(81173570)

摘　　要：目的建立检测大鼠尾静脉给药后血浆中青蒿素含量的高效液相色谱法(HPLC),来研究青蒿素在大鼠体内的药代动力学过程。方法以Wistar大鼠为模型动物,以蒿甲醚为内标,采用HPLC法测定大鼠血浆样品中青蒿素的含量,并计算药代动力学参数。结果大鼠血浆样品中青蒿素在4.67~467.2μg·ml^(-1)范围内线性关系良好,定量限为4.67μg·ml^(-1)。青蒿素的日内和日间精密度均小于10%,准确度在85%~115%范围内。用二室模型拟合大鼠尾静脉注射青蒿素的药时曲线为最佳,主要的药动学参数为:T_(max):2 min;C_(max):89.23μg·ml^(-1);t_(1/2α):3.37 min;t_(1/2β):42.87 min。结论建立了测定大鼠血浆中青蒿素含量的HPLC法,此法适用于青蒿素在大鼠体内的药代动力学研究,青蒿素在大鼠体内的动力学行为符合二室模型。Objective To study the pharmacokinetic process of artemisinin in rats by high performance liquid chromatography（ HPLC）,which was used to detect the content of artemisinin in rat tail vein. Methods Choosing Wistar rats as model animals and artemether as internal standard,the content of artemisinin in rat plasma samples was determined by HPLC,and calculating the pharmacokinetic parameters. Results Artemisinin of plasma have good linear relationship in 4. 67 ~ 467. 2 μg·ml^-1 range,the limit of quantification was 4. 67μg·ml^-1. The RSD of intra-day and inter-day are all less than 10%,and the accuracies are in the range of 85% ~ 115%. The data of plasma concentration-time after the rats were given with artemisinin by tail vein injection is analyzed and certified that the process of pharmacokinetic study in rats in vivo accorded with the 2-room. The main pharmacokinetic parameters were Tmax： 2 min; Cmax： 89. 23 μg·ml^（-1）; t1/2α： 3. 37 min; t1/2β： 42. 87 min. Conclusion Artemisinin pharmacokinetic behavior in rats accorded with the 2-room,the HPLC method can determine the content of artemisinin in rat plasma and meet the study of drug metabolism in rats.

关 键 词：青蒿素 大鼠 高效液相色谱法 药代动力学 二室模型 

分 类 号：R285.5[医药卫生—中药学]