Determination of montelukast in human plasma by LC-ESI-MS and its application in pharmacokinetic study  

LC-ESI-MS方法测定人血浆中孟鲁司特含量及其药代动力学的研究(英文)

作　　者：黄瑶[1] 丁黎[1] 刘园园[1] 刘荷英[1] 文爱东[2] 杨林[2] 

机构地区：[1]中国药科大学药物分析教研室,江苏南京210009 [2]第四军医大学西京医院国家药品临床研究基地,陕西西安710032

出　　处：《Journal of Chinese Pharmaceutical Sciences》2009年第3期261-266,共6页中国药学（英文版）

摘　　要：A liquid chromatography-electrospray ionization-mass spectrometry （LC-ESI-MS） method was developed for the determination of montelukast in human plasma. After precipitation of plasma proteins, the plasma samples were separated on a C18 column with a mobile phase consisted of 20 mmol/L ammonium acetate buffer solution containing 0.2% formic acid-methanol （12：88, v/v）. LC-ESI-MS was performed in the selected-ion monitoring （SIM） mode using target ions [M＋H]^＋ at m/z 586.2 for montelukast and m/z 515.2 for telmisartan, the internal standard （IS）. The calibration curve was linear over the plasma concentration range of 1 ng/mL-1000 ng/mL. The lower limit of quantification （LLOQ） was 1 ng/mL for montelukast. The relative standard deviations ofintra- and inter-batches were less than 5.9% and 10.0%, respectively. The method was successfully applied to study the pharmacokinetics of montelukast sodium tablets in healthy Chinese volunteers.建立人血浆中孟鲁司特的LC-ESI-MS测定方法。孟鲁司特钠血浆样品用乙腈沉淀蛋白后,经Ci 8柱分离,流动相为20mmol/L醋酸铵缓冲盐溶液(包含0.2%甲酸)一甲醇(12:88,v/v)。LC-ESI-MS测定法采用选择性离子监测模式(SIM),检测离子为孟鲁司特的[M+H]^+m/z 586.2和内标替米沙坦的[M+H]^+离子m/z 515.2,线性范围是1ng/mL-1000ng/mL,最低定量限为1ng/mL,方法的批内和批间相对标准偏差(精密度)分别小于5.9%和10.0%。此方法已成功地用于孟鲁司特钠片剂在中国健康受试者体内的药动学研究。

关 键 词：MONTELUKAST LC-ESI-MS MS PHARMACOKINETICS 

分 类 号：R96[医药卫生—药理学]