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甘草酸二铵对恩替卡韦在大鼠体内药代动力学的影响(英文)
引用本文:李飞燕,郝海平,郝琨,颜婷婷,王广基.甘草酸二铵对恩替卡韦在大鼠体内药代动力学的影响(英文)[J].中国天然药物,2013(3):309-313.
作者姓名:李飞燕  郝海平  郝琨  颜婷婷  王广基
作者单位:[1]中国药科大学“天然药物活性组分与药效”国家重点实验室,210009 [2]中国药科大学药物代谢动力学重点实验室,南京210009
基金项目:supported by the Key Laboratory of Drug Metabolism and Pharmacokinetics of Jiangsu Province(No.BM2012012)~~
摘    要:目的:探讨短期和长期给予甘草酸二铵(GLN)对恩替卡韦(ETV)在大鼠体内药代动力学的影响。方法:雄性SD大鼠分为短期给药组和长期给药组,短期给药实验中,对组给予生理盐水,低剂量组给予GLN13.5mg·kg–1,高剂量组给予GLN40.5mg·kg–1,半小时后灌胃给药ETV0.09mg·kg–1。长期给药实验分为两种给药方案,方案一中,连续15d,对照组给予生理盐水,低剂量组给予GLN13.5mg·kg–1,高剂量组给予GLN40.5mg·kg–1;方案二中,连续15d,对照组给予ETV0.09mg·kg–1,低剂量组给予ETV0.09mg·kg–1+GLN13.5mg·kg–1,高剂量组给予ETV0.09mg·kg–1+GLNmg·kg–1,第16天所有大鼠灌胃给ETV0.09mg·kg–1。于不同时间点采集大鼠血浆,血浆样品经处理后,采用HPLC-MS/MS法测定各时间点血浆中ETV的含量。结果:短期或长期与甘草酸二铵均不影响恩替卡韦在大鼠体内的药代动力学参数。结论:甘草酸二铵不影响恩替卡韦药代动力学过程。

关 键 词:药代动力学  恩替卡韦  甘草酸二铵  大鼠

Effect of diammonium glycyrrhizinate on entecavir pharmacokinetics in rats
LI Fei-Yan,HAO Hai-Ping,HAO Kun,YAN Ting-Ting,WANG Guang-Ji.Effect of diammonium glycyrrhizinate on entecavir pharmacokinetics in rats[J].Chinese JOurnal of Natural Medicines,2013(3):309-313.
Authors:LI Fei-Yan  HAO Hai-Ping  HAO Kun  YAN Ting-Ting  WANG Guang-Ji
Institution:1 State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China 2. Key Laboratory of Drug Metabohsm and Pharmacokmetlcs, China Pharmaceutical University, Nanjing 210009, China
Abstract:AIM: This study was designed to explore the effects of short-term and long-term pretreatment of diammonium glycyrrhizinate (GLN) on the pharrnacokinetics of entecavir (ETV) in rats. METHODS: Male SD rats were randomized into short-term and long-term experimental groups, respectively. In the short-term experiment, the control group received saline, the low dose group received GLN 13.5 mg.kg-1 and the high dose group received GLN 40.5 mg·kg-1. ETV (0.09 mg.kg-1) was given i.g. 0.5 h after saline/GLN administration. For the long-term experiment, rats were allocated into two experimental designs. The control group received saline/ETV (0.09 mg.kg-1), the low dose group received GLN 13.5 mg.kg-l/ETV 0.09 mg.kg-1 + GLN 13.5 mg.kg-1, while the high dose group received GLN 40.5 mg.kg-1/ETV 0.09 mg.kg-1 + GLN 40.5 mg-kg-l; all administration was continued for 15 days. On the 16th day, 0.09 mg-kg-1 ETV was administrated to all groups. Blood samples were obtained at different time points after ETV ad- ministration to determine plasma ETV concentrations. RESULTS: Pretreatment with glycyrrhizin resulted in no significant alterations in the main pharmacokinetic parameters of ETV in the short-term and long-term administration experiments. CONCLUSIONS: Diammonium glycyrrhizinate has no effect on ETV pharrnacokinetics in rats.
Keywords:Pharmacokinetics  Entecavir  Diammonium Glycyrrhizinate  Rat
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