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中国临床药理学与治疗学 ›› 2004, Vol. 9 ›› Issue (7): 751-754.

• 研究原著 • 上一篇    下一篇

HPLC-MS法测定Beagle犬血浆中氧化苦参碱及其药代动力学

王素军, 王广基, 李晓天, 马仁玲1, 盛龙生1, 孙建国, 谢海棠   

  1. 中国药科大学药物代谢研究中心, 1分析测试中心, 南京210009, 江苏
  • 收稿日期:2004-04-10 修回日期:2004-05-20 出版日期:2004-07-26 发布日期:2020-11-20
  • 通讯作者: 王广基,男,教授,博士生导师,研究方向:药代动力学。Tel:025-83271544 E-mail:gjwang@cpu.edu.cn
  • 作者简介:王素军,男,博士生,研究方向:药代动力学。Tel:025-85391035 E-mail:wsj7272@sina.com
  • 基金资助:
    国家863计划资助项目(№2003AA2Z347A);江苏省药物代谢动力学重点实验室资助项目(№BM2001201)

Pharmacokinetics of oxymatrine in Beagle dogs by LC-MS

WANG Su-Jun, WANG Guang-Ji, LI Xiao-Tian, MA Ren-Ling1, SHENG Long-Sheng1, SUN Jian-Guo   

  1. Center of Drug Metabolism and Pharmacokinetics, 1Center for Instrumental Analysis, China Pharmaceutical University,Nanjing 210009, Jiangsu, China
  • Received:2004-04-10 Revised:2004-05-20 Online:2004-07-26 Published:2020-11-20

摘要: 目的: 建立Beagle犬血浆中氧化苦参碱的LC-MS测定法,测定它的绝对生物利用度。方法: Beagle犬6只,随机分为2组,采用单剂量双周期自身交叉设计,分别给犬单剂量静脉注射或灌胃氧化苦参碱,用LC-MS法测定给药后的血浆中药物浓度。结果: 氧化苦参碱在2~5000μg·L-1的范围内呈良好的线性关系(r=0.9990),最低检出限达0.6μg·L-1,日内和日间误差均小于4.2 %,方法回收率大于96.7 %;氧化苦参碱的药-时数据符合二室模型,Cmax为2.42±0.97μg·L-1,Tmax为1.0±0.3 h,T1/2β为5.54±1.58h,AUC0→∝为6.12±1.08μg·L-1·h-1,绝对生物利用度为(19.4±9.01)%。结论: 该法灵敏、简单,专属性强;氧化苦参碱在Beagle犬体内绝对生物利用度较低。

关键词: 氧化苦参碱, 液相色谱质谱联用, 药代动力学, Beagle犬, 绝对生物利用度

Abstract: AIM: To establish LC-MS method in determination of oxymatrine in plasma of Beagle dogs and to investigate its absolute bioavailability.METHODS: According to a randomized two-period crossover design, the Beagle dogs were iv 6 mg·kg-1 and ig 30 mg·kg-1 of oxymatrine, respectively.Drug concentration in plasma was assayed by HPLC ESI MS. RESULTS: The linearity of oxymatrine ranged from 2 to 5 000 μg·L-1(r=0.9990).The detection limits of oxymatrine was 0.6μg·L-1 .The values of RSD of within day and between day were less than 4.2 %.The recovery of this method was more than 96.7 %.The disposition was conformed to a two-compartment model .The Cmax, Tmax, T1/2β, AUC0→∝ and absolute bioavailability of oxymatrine were 2.42±0.97μg·L-1,1.0±0.3h,5.54±1.58h,6.12±1.08μg·L-1·h-1 and (19.4±9.0)%, respectively.CONCLUSION: This study provides a simple, reliable and special method for determining concentrations of oxymatrine in plasma of Beagle dog.Oxymatrine shows low absolute bioavailability in Beagle dogs.

Key words: oxymatrine, liquid chromatography mass determination, pharmacokinetics, Beagle dogs, absolute bioavailability

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