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茶叶科学 ›› 2004, Vol. 24 ›› Issue (1): 44-48.doi: 10.13305/j.cnki.jts.2004.01.009

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脂质体儿茶素在家兔体内的生物利用度与药物动力学

孙志良1,刘湘新1,林亲录2,刘自逵1,刘进辉1,何湘蓉1   

  1. 1. 湖南农业大学动物科技学院,湖南 长沙 410128;
    2. 湖南农业大学食品科技学院,湖南 长沙 410128.
  • 收稿日期:2003-03-06 修回日期:2004-02-11 出版日期:2004-03-25 发布日期:2019-09-11
  • 作者简介:孙志良(1967— ),男,副教授,主要从事药理学和毒理学教学与科研工作。
  • 基金资助:
    湖南省自然科学基金(01JJY2096)资助

Pharmacokinetics and Bioavailability of Catechin Liposome in Rabbits

SUN Zhi-liang1, Liu Xiang-xin1, Ling Qin-lu2, Liu Zi-kui1, Liu jin-fei1, He Xiang rong1   

  1. 1. College of Animal Science and Technology;
    2. College of Food Science and Technology, HNAU, Changsha 410128, China
  • Received:2003-03-06 Revised:2004-02-11 Online:2004-03-25 Published:2019-09-11

摘要: 取健康家兔10只,随机分为2组,单剂量静注和灌服脂质体儿茶素(Catechin Liposome)25mg/kg。用高效液相色谱法测定血浆中儿茶素原药质量浓度。房室模型分析表明:健康家兔静注儿茶素脂质体的药时数据符合无吸收二室开放模型,主要药物动力学参数为:t1/2α0.18±0.01βh,t1/2β1.52±0.08βh,Vd4.48±0.24L,ClB2.05±0.07L/h,AUC29.20±1.00βmg/(L.h),K101.64±0.19h–1,K211.08±0.06h–1,K121.61±0.19h–1。健康家兔灌服脂质体儿茶素的药时数据符合一级吸收一室开放模型,主要药物动力学参数为:t1/2ka 0.27±0.03βh,t1/2ke 1.72±0.04βh,tmax0.87±0.05βh,Cmax6.53±0.62βmg/L,AUC 25.90±1.34βmg/(L.h),F 88.60±5.73%。脂质体儿茶素在健康家兔体内的药动学特征是:吸收迅速,达峰时间较短,消除慢,半衰期延长,表现分布容积大,口服生物利用度高。结果表明:儿茶素经脂质体包封后,药物动力学及组织分布均发生了明显改变。

关键词: 儿茶素, 药物动力学, 脂质体, 家兔

Abstract: Pharmacokinetics and bioavailability of Catechin Liposome were studied in 10 healthy rabbits following single intravenous (25mg/kg) and oral administration (25mg/kg)of the drug. Plasma concentrations of. Catechin Liposome were determined by high-performance liquid chromatography. The concentration-time data were fitted to a two-compartment model following a single intravenous injection in rabbits. The main pharmacokinetic parameters were as follows: distribution half-life (t1/2α) (0.18±0.01)h,elimination half-life (t1/2β) (1.52±0.08)h,apparent distribution volume (Vd) (4.48±0.24)L total body clearance (ClB) (2.05±0.07)L/h,the area under curve (AUC) (29.20±1.00)mg/(L.h). The drug concentration-time data also were fitted to a one-compartment open model with first order absorption after a single oral administration Catechin Liposome. The pharmacokinetic parameters were as follows: t1/2kα (0.27±0.03)h, t1/2ke(1.72±0.04)h, tmax (0.87±0.05) h, Cmax 6.53±0.62βmg/L, AUC 25.90±1.34βmg/(L.h), bioavailability F 88.60±5.73%. Pharmacokinetic characteristics of Catechin Liposome in healthy rabbits showed a rapid absorption, the time to reach Cmax is short, slow elimination, long half-life, large apparent distribution volume, and high bioavailability of oral administration. The results showed:after Catechin was prepared in liposome form, the tissue distribution and pharmacokinetics were changed significantly.

Key words: Catechin, Liposome, Pharmacokinetics, Bioavailability, Rabbits

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