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中国临床药理学与治疗学 ›› 2006, Vol. 11 ›› Issue (10): 1148-1153.

• 研究原著 • 上一篇    下一篇

高效液相色谱-质谱-质谱联用法测定人血浆中艾司西酞普兰浓度及其药代动力学研究

杨倩, 刘文英, 郑枫, 徐继华, 饶金华, 孙棣, 高暑1   

  1. 中国药科大学药分教研室, 南京 210009, 江苏;
    1合肥合源医药科技有限公司, 合肥 230088, 安徽
  • 收稿日期:2006-07-12 接受日期:2006-09-18 出版日期:2006-10-26 发布日期:2020-11-05

A rapid and sensitive method for determination of escitalopram in human plasma and its application in pharmacokinetic study by liquid chromatography-tandem mass spectrometry

YANG Qian, LIU Wen-ying, ZHENG Feng, XU Ji-hua, RAO Jin-hua, SUN Di, GAO Shu1   

  1. Department of Pharmaceutical Analysis, China Pharmaceutical University , Nanjing 210009 , Jiangsu, China;
    1Hefei Con-Source Medicine Technology Coop, Hefei 230088 , Anhui , China
  • Received:2006-07-12 Accepted:2006-09-18 Online:2006-10-26 Published:2020-11-05
  • About author:YANG Qi an, female, master student, specialized in pharmaceutical anulysis.Tel:13814007636 E-mail:yangqian0111@163.com

摘要: 目的 建立测定人血浆中艾司西酞普兰浓度的高效液相色谱-质谱-质谱联用法。方法 血浆样品经甲醇沉淀后进行分析。色谱柱:Lichrospher CN柱150 mm×4.6 mm I.D.5 μm, 流动相:甲醇∶水(含15 mmol·L-1乙酸铵) ∶甲酸(72∶28∶0.1, v/v/v) , 流速:1.0 ml·min-1 , 电喷雾离子化三重四极杆串联质谱检测, 以选择离子反应监测(SRM) 扫描方式进行检测, 采用选择离子反应监测(SRM) 方式进行定量分析, 用于监测的离子为m/z325.0 ※234.0(西酞普兰) 和m/z 409.1 ※238.1(氨氯地平, 内标) 。结果 线性范围为0.20 ~ 50.00 ng·ml-1 , 最低定量浓度为0.20 ng·ml-1 , 应用此法测试了10 名健康受试者口服草酸艾司西酞普兰片(10 mg) 后不同时间的血药浓度, 得到艾司西酞普兰药动学参数, Cmax 为9.21 ±2.10 ng·ml-1 , Tmax 为3.75 ±1.04 h , AUC0 -t 为514.6 ±152.3 ng·h·ml-1 , AUC0 -∞ 为540.5 ±162.3 ng·h·ml-1 , t1/2 为34.06 ±7.71 h 及K e 为0.021 ±0.004 h-1结论 该法专属、灵敏、简便、快速, 适用于人血浆中艾司西酞普兰浓度的测定。

关键词: 艾司西酞普兰, 高效液相色谱-质谱-质谱联用法, 血药浓度, 药代动力学

Abstract: AIM: To determine the concentration of escitalopram in human plasma by HPLC-MS MS and investigate the pharmacokinetics of escitalopram.METHODS: The method involved protein precipitation with methanol.The chromatographic separation was achieved within 6.0 min by using methanol-water with 15 mmol·L-1ammonium acetate-formic acid (72 ∶28 ∶0.1, v/v/v) as mobile phase and a Lichrospher CN 150 mm ×4.6 mm analytical column.The analytes were detected using an electrospray ionization tandem mass spectrometry in SRM mode.Detection of the ions was performed by monitoring the transitions of m/z 325.0 to 234.0 for escitalopram and m/z 409.1 to 238.1 for amlodipine(internal standard) , respectively.RESULTS: The standard curve was linear (r =0.999) over the concentration range of 0.20 -50.00 ng·ml-1.Accuracy and precision were below the acceptance limits of 15%.The recoveries of escitalopram ranged from 96.0% to 103.6%.The lower limit of quantification for escitalopram was 0.20 ng·ml-1 using 200 μl plasma sample.The pharmacokinetic parameters of escitalopram after a single oral dosing of escitalopram oxalate tablet (10 mg)to ten healthy male volunteers were achieved.The Cmax ,Tmax , AUC0 -t , AUC0 -∞, t1 2and K e of escitalopram were 9.21 ±2.10 ng·ml-1 , 3.75 ±1.04 h, 514.6 ±152.3 ng·h·ml-1 , 540.5 ±162.3 ng·h·ml-1 , 34.06 ±7.71 h and 0.021 ±0.004 h-1 , respectively.CONCLUSION: The determination of concentration of escitalopram in human plasma by HPLC-MS MS method was rapid, sensitive and reliable.It can be used for clinical pharmacokinetic study of escitalopram.

Key words: escitalopram, HPLC-MS/MS, human plasma, pharmacokinetics

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