复方天麻颗粒中天麻素在大鼠体内的药动学研究

为了研究麦冬、五味子与天麻配伍对大鼠体内天麻素药动学的影响, 分别给Wistar大鼠灌胃低、中、高剂量复方天麻颗粒提取物 (剂量分别相当于天麻素50、100和200 mg·kg^?1) 及天麻提取物 (剂量相当于天麻素100 mg·kg^?1), 于不同时间点采集大鼠血浆。血浆样品经甲醇-乙腈沉淀蛋白后, 用液相色谱法测定血浆中天麻素含量。各给药组天麻素平均血药浓度-时间数据用WinNonlin 5.2.1药动学软件进行动力学分析, 组间药动学参数用SPSS 17.0软件进行统计分析。结果表明, 低、中剂量复方组天麻素在大鼠体内符合一级吸收非房室模型, 高剂量复方组天麻素在大鼠体内符合零级吸收非房室模型。对比分析大鼠灌胃100 mg·kg^?1天麻素的复方天麻颗粒提取物和天麻提取物时的药动学参数, 复方组C_max显著变小 (P < 0.01)、MRT_0?∞显著延长 (P < 0.01), 表明麦冬、五味子与天麻配伍, 可延缓天麻素的吸收, 降低消除速率, 增加体内作用时间。

Pharmacokinetics of gastrodin from compound Tianma granule in rats

To study the influence of the compatibility of ophiopogonis tuber and Chinese magnoliavine fruit with gastrodia rhizome on the pharmacokinetics of gastrodin in rat, three dosages of compound Tianma granule extract (equivalent to gastrodin 50, 100, 200 mg·kg⁻¹) and one dosage of Tianma extract (equivalent to gastrodin 100 mg·kg⁻¹) were administered to rats by intragastric administration separately.  Plasma samples were collected at different times and treated with methanol and acetonitrile to precipitate protein.  The contents of gastrodin in plasma were determined by HPLC method.  The mean plasma concentration-time curves of different medication administration teams were processed with WinNonlin 5.2.1 pharmacokinetic software.  The pharmacokinetic parameters of different medication administration teams were analyzed with SPSS statistics 17.0 software.  The results indicated that the in vivo kinetic process of gastrodin was fitted to first-order absorption un-compartment model at low, middle dosages and zero-order absorption un-compartment model at high dosage of compound Tianma granule extract.  By comparison with the pharmacokinetic parameters of gastrodin (100 mg·kg⁻¹) in Tianma extract, the significant decrease for C_max and significant increase for MRT_0−∞ in compound Tianma granule extract indicated that the compatibility of ophiopogonis tuber and Chinese magnoliavine fruit with Gastrodia rhizome can delay the absorption, reduce the elimination rate and prolong the action time of gastrodin in vivo.