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中国临床药理学与治疗学 ›› 2005, Vol. 10 ›› Issue (3): 310-313.

• 研究原著 • 上一篇    下一篇

灯盏花素在小鼠体内药物动力学研究

刘奕明, 林爱华, 陈汇1, 曾繁典1   

  1. 广东省中医院中心实验室, 广州510120, 广东;
    1华中科技大学同济医学院临床药理研究所, 武汉430030, 湖北
  • 收稿日期:2004-12-28 修回日期:2005-02-06 出版日期:2005-03-26 发布日期:2020-11-18
  • 通讯作者: 曾繁典, 男, 教授, 博士生导师, 研究方向:心血管药理与临床药理。Tel:027-83630652 E-mail:fdzeng@mails.tjmu.edu.cn
  • 作者简介:刘奕明, 女, 博士, 助理研究员, 研究方向:临床药理学。Tel:020-81887233-30904 E-mail:Lyming2000@163.com

Pharmacokinetics of breviscapine in mice

LIU Yi-ming, LIN Ai-hua, CHEN Hui1, ZENG Fan-dian1   

  1. Central Laboratory, Guangdong Provincial Hospital of TCM, Guangzhou 510120, Guangdong, China;
    1Institute of Clinical Pharmacology, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, Hubei, China
  • Received:2004-12-28 Revised:2005-02-06 Online:2005-03-26 Published:2020-11-18

摘要: 目的:研究灯盏花素在小鼠体内的药物动力学和绝对生物利用度。方法:采用固相萃取-高效液相色谱(SPE-HPLC)法, 测定小鼠静脉注射灯盏花素50 mg°kg-1和灌胃150 mg°kg-1后血浆灯盏乙素浓度, 3p97 程序处理数据。结果:小鼠静注灯盏花素后灯盏乙素的血浓-时间变化符合三房室模型,AUC、C0 和T1/2β 分别为12.97±3.55 mg°L-1 °h、132.23±39.90 mg°L-1 和4.04±1.29 h。灌胃后药物吸收很快, 但血浓低。采用非房室模型法计算AUC 为1.97±0.53 mg°L-1°h, T1/2Ke 为3.41±1.23 h。绝对生物利用度为5.05%。结论:灯盏花素经静注在小鼠体内的药代动力学符合三室模型。灌胃给药吸收快, 但吸收差, 绝对生物利用度低, 且药时曲线变化不规则。

关键词: 灯盏花素, 灯盏乙素, 小鼠, 药物动力学, 生物利用度

Abstract: AIM: To study the pharmacokinetics and absolute bioavailability of breviscapine in mice.METHODS: After iv injection (50 mg°kg-1)and ig administration (150 mg°kg-1)of breviscapine in mice, the plasma scutellarin concentration were detected by SPE-HPLC method.The pharmacokinetic parameters were calculated by 3p97 program.RESULTS: The plasma scutellarin concentration-time curve after iv injection of breviscapine was fitted with a three compartment model.AUC, C0 and T1/2β were 12.97 mg°h°L-1, 132.23 mg°L-1 and 4.04 h, respectively.After ig administration of breviscapine, the drug absorption was rapid, but the plasma concentration was very low.The parameters of AUC and T1/2Ke calculated with non-compartment model were 1.966 mg°h°L-1 and 3.4 h, respectively.The absolute bioavailability was 5.05%.CONCLUSSION:The pharmacokinetics of breviscapine in mice after iv injection fitted with three-compartment model.After ig administration, the drug is absorbed rapidly but the absolute bioavailability is very low, and the changes of plasma concentration of scutellarin is not regulation.

Key words: breviscapine, scutellarin, mice, pharmacokinetics, bioavailability

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