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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。

Effect of diammonium glycyrrhizinate on entecavir pharmacokinetics in rats.

机构信息

State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China.

出版信息

Chin J Nat Med. 2013 May;11(3):309-13. doi: 10.1016/S1875-5364(13)60034-5.

Abstract

AIM

This study was designed to explore the effects of short-term and long-term pretreatment of diammonium glycyrrhizinate (GLN) on the pharmacokinetics 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(-1)/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(-1); all administration was continued for 15 days. On the 16(th) day, 0.09 mg·kg(-1) ETV was administrated to all groups. Blood samples were obtained at different time points after ETV administration 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.

CONCLUSION

Diammonium glycyrrhizinate has no effect on ETV pharmacokinetics in rats.

摘要

目的

本研究旨在探讨短期和长期预处理甘草酸二铵(GLN)对大鼠恩替卡韦(ETV)药代动力学的影响。

方法

雄性 SD 大鼠随机分为短期实验组和长期实验组。在短期实验中,对照组给予生理盐水,低剂量组给予 GLN 13.5mg·kg(-1),高剂量组给予 GLN 40.5mg·kg(-1)。GLN 给药 0.5 小时后,大鼠经口给予 ETV(0.09mg·kg(-1))。对于长期实验,大鼠分为两种实验设计。对照组给予生理盐水/ETV(0.09mg·kg(-1)),低剂量组给予 GLN 13.5mg·kg(-1)/ETV 0.09mg·kg(-1)+GLN 13.5mg·kg(-1),高剂量组给予 GLN 40.5mg·kg(-1)/ETV 0.09mg·kg(-1)+GLN 40.5mg·kg(-1);所有给药均持续 15 天。第 16 天,所有组均给予 0.09mg·kg(-1)ETV。ETV 给药后不同时间点采集血样,测定血浆 ETV 浓度。

结果

GLN 预处理对短期和长期给药实验中 ETV 的主要药代动力学参数无显著影响。

结论

在大鼠中,甘草酸二铵对 ETV 的药代动力学无影响。

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