Abstract A pharmacokinetic comparison was made to evaluate the influence from other components in the Radix Puerariae Extract on pharmacokinetic behavior of Puerarin. Samples of blood and brain were collected by microdialysis and determined by high-performance liquid chromatography–mass spectrometry (MS)/MS. Pharmacokinetic parameters were estimated from the concentration versus time data using non-compartmental methods. In addition, a comparative pharmacokinetic study of Puerarin in stroke rats was studied after administration of the Radix Puerariae Extract via different routes to find an effective way to deliver drug into brain. Obvious pharmacokinetic differences were also observed in comparison between the Puerarin group and the Radix Puerariae Extract group based on middle cerebral artery occlusion (MCAO) rats. The C max and area under the curve (AUC) of Puerarin in olfactory bulb of the Extract group significantly reduced when it was intravenously administered. However, the AUCs of Puerarin in plasma are 134.72 and 1707.02 mg/L min, via intranasal and intravenous administration of the Radix Puerariae Extract, respectively. The AUC of the intranasal group in brain is seven times higher than that of intravenous administration. Other ingredients in the Extract may affect the disposition of Puerarin and its transportation through the blood–brain barrier via intravenous administration. But intranasal administration is an effective route to deliver isoflavone-C-glycoside with poor hydrophilicity into brain.

中文翻译：

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黄酮类共存及给药途径对葛根素在MCAO大鼠体内药代动力学的影响

摘要 通过药代动力学比较研究葛根提取物中其他成分对葛根素药代动力学行为的影响。通过微透析收集血液和大脑样本，并通过高效液相色谱-质谱 (MS)/MS 进行测定。使用非房室方法从浓度对时间的数据估计药代动力学参数。此外，通过不同途径给予葛根提取物后，研究了葛根素在中风大鼠中的比较药代动力学研究，以寻找将药物输送到大脑的有效方法。基于大脑中动脉闭塞（MCAO）大鼠，葛根素组与葛根提取物组之间的比较也观察到明显的药代动力学差异。静脉给药时，提取物组嗅球中葛根素的C max 和曲线下面积（AUC）显着降低。然而，通过鼻内和静脉内给予葛根提取物，血浆中葛根素的 AUC 分别为 134.72 和 1707.02 mg/L min。鼻内组脑内AUC比静脉给药高7倍。提取物中的其他成分可能会影响葛根素的分布及其通过静脉给药通过血脑屏障的运输。但鼻内给药是将亲水性差的异黄酮-C-糖苷输送到大脑中的有效途径。通过鼻内和静脉内给予葛根提取物，血浆中葛根素的 AUC 分别为 134.72 和 1707.02 mg/L min。鼻内组脑内AUC比静脉给药高7倍。提取物中的其他成分可能会影响葛根素的分布及其通过静脉给药通过血脑屏障的运输。但鼻内给药是将亲水性差的异黄酮-C-糖苷输送到大脑中的有效途径。通过鼻内和静脉内给予葛根提取物，血浆中葛根素的 AUC 分别为 134.72 和 1707.02 mg/L min。鼻内组脑内AUC比静脉给药高7倍。提取物中的其他成分可能会影响葛根素的分布及其通过静脉给药通过血脑屏障的运输。但鼻内给药是将亲水性差的异黄酮-C-糖苷输送到大脑中的有效途径。提取物中的其他成分可能会影响葛根素的分布及其通过静脉给药通过血脑屏障的运输。但鼻内给药是将亲水性差的异黄酮-C-糖苷输送到大脑中的有效途径。提取物中的其他成分可能会影响葛根素的分布及其通过静脉给药通过血脑屏障的运输。但鼻内给药是将亲水性差的异黄酮-C-糖苷输送到大脑中的有效途径。