高效液相色谱-串联质谱法测定健康人体血浆中青蒿素浓度及其药代动力学研究  

Determination the concentration of artemisinin in healthy human plasma and study on its pharmacokinetics by LC-MS-MS

作　　者：高洪志[1] 李海燕[1] 徐树光[2] 刘泽源[1] 王京燕[3] 

机构地区：[1]军事医学科学院附属307医院药剂室临床药理室,北京100071 [2]昆明制药集团股份有限公司药物研究院,昆明650100 [3]军事医学科学院微生物流行病研究所病原微生物生物安全国家重点实验室,北京100071

出　　处：《中国临床药理学杂志》2009年第2期138-140,共3页The Chinese Journal of Clinical Pharmacology

基　　金：全军“十一五”指令性课题基金资助项目(06Z071)

摘　　要：目的建立测定血浆中青蒿素（抗疟药）的高效液相色谱-串联质谱法,研究青蒿素在健康人体内的药代动力学。方法10名健康男性志愿者,单剂口服青蒿素片1000 mg;用高效液相色谱-串联质谱法测定血药浓度。结果本方法检测青蒿素的线性范围为4-1 000μg.L^-1,最低定量限为4μg.L^-1;口服青蒿素1 000 mg后,Cm ax为（466.50±120.15）μg.L^-1,AUC0-24h为（2.78±0.85）mg.h.L^-1,AUC0-∞为（2.82±0.87）mg.h.L-1,t1/2为（3.58±0.86）h,tm ax为（2.15±0.91）h。结论该方法操作简便、快速、灵敏度高,适于青蒿素类药物的药代动力学研究。Objective To establish a rapid and sensitive LC -MS -MS method for the analysis of artemisinin in the plasma and study the pharmacokinetics of artemisinin tablets in healthy volunteers. Methods Ten healthy male volunteers were received oral single dose artemisinin tablets （1 000 rag）. The plasma samples were determined by L-MS-MS method. Results The limits of quantitation of method for artemisinin was 4 μg · L^-1, the calibration curves in plasma was linear in the range of 4 to 1 000 μg · L^-1. The pharmacokinetic parameters were as follows ： C was （466.50 ± 120. 15） μg · L^-1; AUC0-24h was （2. 78 ±0. 85） mg· h · L^- 1 ; AUC0-∞ was （2.82 ± 0.87） mg· h · L^- 1 ; t1/2 was （3.58 ± 0. 86） h; tm., was （2. 15 ± 0. 91 ） h . Conclusion The method is shown to be accurate and convenient, and suitable for pharmaeokinetie study of artemisinin .

关 键 词：青蒿素 药代动力学 高效液相色谱-串联质谱 

分 类 号：R969.1[医药卫生—药理学] R978.6[医药卫生—药学]