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天钩降压胶囊中天麻素在大鼠体内的药代动力学

[Pharmacokinetics of gastrodin from Tiangou Jiangya capsule in rats].

作者信息

Li Ling-Jun, Yan Rui

出版信息

Zhongguo Zhong Yao Za Zhi. 2014 Aug;39(15):2964-7.

Abstract

The paper aims to study the pharmacokinetic parameters of gastrodin in rats effected by compound compatibilitiy and different doses of Tiangou Jiangya capsule. The extracts from Gastrodiae Rhizoma( equivalent to gastrodin 16.82 mg x kg(-1) and Tiangou jiangya capsule (equivalent to gastrodin 8.410, 16.82, 33.64 mg x kg(-1)) were oral administrated to rats respectively. The plasma were taken at various time points and treated with acetonitrile to measure the contents of gastrodin by HPLC method. The mean plasma concentration-time data were analyzed by 3P97 pharmacokinetic software and the pharmacokinetic parameters between groups were treated by SPSS 16.0. The results showed that gastrodin in rat was fitted to one-compartment model, Cmax and AUC of Tiangou Jiangya capsule were in direct proportion to oral administration, and t1/2Ka had nothing to do with doses, which indicated that gastrodin was fitted first-order rate transfter process in vivo. Morever, comparison with the Gastrodiae Rhizoma extract, isodose gastrodin in Tiangou Jiangya capsule showed a significant decrease for Cmax, Ke and increase for t1/2Ke, V/Fc, this indicated that compound compatibility can delay the absorbtion of gastrodin, prolong the resident time and promote the distribution in vivo, but its bioavailability is not significantly effected.

摘要

本文旨在研究复方配伍及不同剂量天麻钩藤降压胶囊对大鼠体内天麻素药代动力学参数的影响。分别将天麻提取物(相当于天麻素16.82mg·kg⁻¹)和天麻钩藤降压胶囊(相当于天麻素8.410、16.82、33.64mg·kg⁻¹)灌胃给予大鼠。于不同时间点取血,用乙腈处理后,采用高效液相色谱法测定天麻素含量。用3P97药代动力学软件分析血浆浓度-时间均值数据,用SPSS 16.0处理组间药代动力学参数。结果表明,大鼠体内天麻素符合一室模型,天麻钩藤降压胶囊的Cmax和AUC与灌胃剂量成正比,t1/2Ka与剂量无关,提示天麻素在体内符合一级速率转运过程。此外,与天麻提取物相比,等剂量天麻钩藤降压胶囊中天麻素的Cmax、Ke显著降低,t1/2Ke、V/Fc升高,表明复方配伍可延缓天麻素吸收,延长其在体内的停留时间,促进其分布,但对其生物利用度影响不显著。

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