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建立了液相色谱-串联质谱法测定健康志愿者全血中的阿莫地喹(1),并考察其在健康志愿者体内的药动学。以羟化氯喹为内标,使用Agilent Zorbax SB C18柱,乙腈∶20 mmol/L乙酸铵溶液(23∶77)为流动相;采用大气压力化学电离源(APCI),多反应监测(MRM)模式,正离子检测,监测离子对为m/z 356.3→m/z 283.2(1)和m/z 336.0→m/z247.1(内标)。1在0.5~100 ng/ml浓度范围内线性关系良好,日内和日间RSD均小于10.0%,提取回收率大于70.4%。18名男性健康志愿者口服青蒿琥酯1盐酸盐片,主要药动学参数为cmax(25.9±4.7)ng/ml,tmax(1.1±0.3)h,t1/2(13.9±3.9)h,AUC0→t(294.5±42.8)ng·h·ml-1,AUC0→∞(310.3±45.0)ng·h·ml-1。
A liquid chromatography-tandem mass spectrometry was developed for the determination of amodiadequine (1) in whole blood of healthy volunteers and its pharmacokinetics in healthy volunteers. Using hydroxychloroquine as an internal standard, Agilent Zorbax SB C18 column was used with acetonitrile: 20 mmol / L ammonium acetate solution (23:77) as the mobile phase. Atmospheric pressure chemical ionization (APCI), multiple reaction monitoring (MRM) , Positive ion detection, monitoring ion pairs m / z 356.3 → m / z 283.2 (1) and m / z 336.0 → m / z 247.1 (internal standard). 1 had a good linearity within the concentration range of 0.5-100 ng / ml. The RSDs were less than 10.0% during the day and the day, and the extraction recovery was more than 70.4%. Eighteen male healthy volunteers were given artesunate hydrochloride hydrochloride tablets. The main pharmacokinetic parameters were cmax (25.9 ± 4.7) ng / ml, tmax (1.1 ± 0.3) h, t1 / 2 (13.9 ± 3.9) h , AUC0 → t (294.5 ± 42.8) ng · h · ml-1, AUC0 → ∞ (310.3 ± 45.0) ng · h · ml-1.