Determination of fexofenadine in human plasma by LC-MS/MS and its application in pharmacokinetic study  

液相色谱串联质谱法测定人体血浆中非索非那定含量及其药代动力学研究（英文）

作　　者：陈彦安[1,2] 周心怡 张文魁 许光阳[1] 

机构地区：[1]台北医学大学药学院 [2]佳生科技顾问股份有限公司 [3]马偕纪念医院淡水分院内科部

出　　处：《Journal of Chinese Pharmaceutical Sciences》2013年第5期409-414,共6页中国药学（英文版）

摘　　要：This study presented a simple, rapid, and sensitive liquid chromatography analytical method employing tandem mass spectrometry （LC-MS/MS） to determine fexofenadine in human plasma. After the de-proteination procedure with acetonitrile, chromatographic separation of fexofenadine was performed using a reversed-phase Eclipse XDB-C8 column with a mobile phase consisted of 1 mmol/L ammonium acetate buffer solution containing 0.2% formic acid-methanol （45：55, v/v）. Fexofenadine was quantified using tandem mass detection in the electrospray ionization （ESI） positive ion mode. The flow rate of the mobile phase was 1 mL/min, and the retention times of fexofenadine and the internal standard （IS, losartan） were 1.76 min and 2.65 min, respectively. The calibration curve was linear over the plasma concentration range of 1-1000 ng/mL. The relative standard deviations of intra- and inter-batches were less than 10.4% and 15.4%, respectively. The LC-MS/MS method reported in this study showed higher sensitivity for the quantification of fexofenadine in human plasma than that shown by previously described analytical methods. Lastly, the method was successfully applied to the pharmacokinetic of fexofenadine in healthy Taiwan volunteers.本研究建立了高敏感度、具选择性且快速的LC-MS/MS测定方法,用以定量测定人血浆中非索非那定的浓度。含非索非那定血浆样品在用乙腈沉淀蛋白质处理后,经Eclipse XDB-C8层析管柱分离,流动相为1 mmol/L醋酸铵缓冲盐溶液(包含0.2%甲酸)–甲醇(45:55,v/v),以电喷雾串联质谱法定量。流动相流速设定在1 mL/min,并选用氯沙坦为内标,非索非那定与内标的保留时间分别为1.76 min与2.65 min。线性范围是1–1000 ng/mL,方法的批内和批间相对标准偏差精密度分别小于10.4%和15.4%。此液相色谱串联质谱仪法相较于过去已发表的分析方法,提供了更灵敏的定量能力。分析方法亦已成功应用于非索非那定在台湾健康受试者体内的药代动力学研究。

关 键 词：FEXOFENADINE LC-MSfMS MS PHARMACOKINETICS 

分 类 号：R969.1[医药卫生—药理学]