人血浆中氟康唑的LC-MS/MS法测定及药动学  

Pharmacokinetics and Determination of Fluconazole in Human Plasma by LC-MS/MS

作　　者：任进民[1] 孙倩[1] 张国旗[1] 赵曦 刘焕龙[1] 

机构地区：[1]河北医科大学第二医院,河北石家庄050000 [2]中奇制药技术有限公司,河北石家庄050051

出　　处：《中国医药工业杂志》2010年第12期929-931,共3页Chinese Journal of Pharmaceuticals

摘　　要：建立了LC-MS/MS法测定人血浆中的氟康唑(1)。采用C_(18)色谱柱,以甲磺酸酚妥拉明(2)为内标,2 mmol/L乙酸铵溶液(含0.05%甲酸)-甲醇(40∶60)为流动相,电喷雾离子化源,选择性正离子多反应监测,检测离子分别为m/z 307.2→238.2(1)和m/z 282.2→212.2(2)。1在0.03～10μg/ml浓度范围内线性关系良好,方法回收率大于94%,提取回收率大于90%,日内和日间RSD均小于5.4%。20名男性健康志愿者单剂量口服1片150 mg,主要药动学参数为c_(max)(3.26±0.54)μg/ml,t_(max)(1.42±0.65)h,t_(1/2)(29.75±4.89)h,AUC_(-120h)(131.4±23.4)μg·ml^1·h和AUC_(0→∞)(140.5±26.3)μg·ml^1·h。A LC-MS/MS method was established for the determination of fluconazole（1） in human plasma.A C_（18） column was used with phentolamine mesylate（2） as the internal standard and 2 mmol/L ammonium acetate solution （containing 0.05%formic acid）-methanol（40：60） as the mobile phase.ESI was applied and operated in positive ion multiple-reaction monitoring mode.The detected ions were m/z 307.2→238.2（1） and m/z 282.2→212.2（2）.The calibration curve was linear in the concentration range of 0.03 - 10μg/ml.The recovery was over 94%and the extraction recovery was above 90%.The inter- and intra-day RSDs were less than 5.4%.A single oral dose of 150 mg 1 tablets were given to 20 male healthy volunteers.The main pharmacokinetic parameters were as follows：c_（max）（3.26±0.54）μg/ml, t_（max）（1.42±0.65） h,t_（1/2）（29.75±4.89） h,AUC_（0→120h）（131.4±23.4）μg·ml^（-1）·h and AUC_（0→∞）（140.5±26.3）μg·ml^（-1）·h.

关 键 词：氟康唑 液相色谱-串联质谱 测定 药动学 

分 类 号：R917[医药卫生—药物分析学] O657.72[医药卫生—药学]