肌注苯环壬酯在大鼠体内的药物动力学研究

首都医科大学学报 ›› 2006, Vol. 27 ›› Issue (2): 203-205.

肌注苯环壬酯在大鼠体内的药物动力学研究

寇于营¹, 徐艳霞¹, 李晓蓉¹, 阮金秀², 张振清², 刘克良², 薛明¹

1. 首都医科大学化学生物学与药学院药理学系;2. 军事医学科学院毒物药物研究所

收稿日期:2005-08-26 修回日期:1900-01-01 出版日期:2006-04-24 发布日期:2006-04-24
通讯作者: 薛明

Determination and Pharmacokinetics of Phencynonate in Rat

Kou Yuying¹, Xu Yanxia¹, Li Xiaorong¹, Ruan Jinxiu², Zhang Zhenqing², Liu Keliang², Xue Ming¹

1. Department of Pharmacology, School of Chemical Biology & Pharmaceutical Sciences, Capital University of Medical Sciences;2. Institute of Pharmacology and Toxicology Academy of Military Medical Science

Received:2005-08-26 Revised:1900-01-01 Online:2006-04-24 Published:2006-04-24

摘要/Abstract

摘要： 目的研究苯环壬酯在大鼠血液中的高效液相色谱-电喷雾离子阱质谱测定方法及其药物动力学.方法以BetaBasic-18色谱柱分离苯环壬酯,正离子电喷雾离子阱质谱法检测,内标法定量.结果苯环壬酯在大鼠血中的线性范围为1～100 μg/L,萃取回收率为69.6%～79.1%,日内与日间精密度均小于10%,最低定量限为1μg/L.单剂量肌肉注射(im)给药后,苯环壬酯在大鼠体内的血药时程符合一级吸收二室模型,其主要药物动力学参数为:t_1/2α0.679 h,t_1/2β3.98 h,t_1/2Ka0.013h,t_max 0.076 h,C_max 54.1μg/L,血药浓度-时间曲线下面积(AUC)77.7(ng·h)/mL.结论该检测方法省时,重现性好,具有较高的灵敏度.药物动力学结果为开发新药与临床应用提供理论依据.

关键词: 苯环壬酯, 高效液相色谱-电喷雾离子阱质谱法, 体内定量, 药物动力学

Abstract: Objective Quantification and pharmacokinetics of phencynonate were investigated in rat by the method of high-performance liquid chromatographic assay with electro spray ionization mass spectrometry detection(LC-ESI-MS).Methods The chromatography was on BetaBasic-18 column(150mm×2.1mm id,3μm).Mass spectrometric measurements were performed on ion-trap mass spectrometer equipped with ESI source working in positive ion mode.Results The linearity was obtained over the concentration range of 1～100μg/L in rat blood.The lower limit of quantification was at 1μg/L in blood.Extraction recoveries were in the range of 69.6%～79.1%.The concentration-time curves in rats were all best fitted to first order Absorption two-compartments open model after a single dose phencynonate(0.35mg/kg) intramuscularly.The main pharmacokinetic parameters of phencynonate were as follows:t_1/2α 0.679h,t_1/2β 3.98h,t_1/2Ka 0.013h,t_max 0.076h,C_max 54.1μg/L,AUC 77.7(ng·h)/mL.Conclusion The method is simple,sensitive and specific.It is successfully applied for quantification of phencynonate and for the clinic drug monitoring and the pharmacokinetic studies.

Key words: phencynonate, liquid chromatography assay with electro spray ionization mass spectrometry detection, quantifi-cation, pharmacokinetics

中图分类号:

R969.1

寇于营;徐艳霞;李晓蓉;阮金秀;张振清;刘克良;薛明. 肌注苯环壬酯在大鼠体内的药物动力学研究[J]. 首都医科大学学报, 2006, 27(2): 203-205.

Kou Yuying;Xu Yanxia;Li Xiaorong;Ruan Jinxiu;Zhang Zhenqing;Liu Keliang;Xue Ming. Determination and Pharmacokinetics of Phencynonate in Rat[J]. Journal of Capital Medical University, 2006, 27(2): 203-205.