【摘要】 目的 探究益气活血固肾颗粒中巴马汀、药根碱、小檗碱、表小檗碱、芒柄花素在大鼠体内的药动学特征及组织分布规律，为进一步阐明该方的药效物质基础提供依据。方法 建立HPLC-MS/MS法测定大鼠口服给药4.75 g/kg益气活血固肾颗粒后血浆及各组织中的药物浓度，色谱柱选择Kromasil C₁₈柱（3.5μm, 2.1 mm×100 mm）,流动相为乙腈-0.1%甲酸水溶液，流速为0.3 mL/min,进样量5μL,采用电喷雾电离源（ESI）分别在正、负离子多反应监测模式（MRM）下进行扫描，选择WinNonlin 3.3软件计算主要药动学参数。结果 所建立的分析方法符合生物样品的检测要求，给予复方灌胃药液后，5种成分均可快速吸收入血，在30 min内血药浓度达到高峰，且药物在体内半衰期较短，消除速率快。各成分的达峰浓度Cmax、药时曲线下面积AUC_0-t分别为4.87～233.12μg/L、16.11～493.13 h/（μg·L）。组织分布结果显示，5种成分在体内分布迅速且广泛，具有不均衡的特征，在胃和小肠中分布较多，其次是肝、肾、肺等组织，而在脾脏、心脏中分布较少。结论 该方法稳定、可靠，为复方益气活血固肾颗粒临床应用提供了参考。更多还原

【Abstract】 Objective To investigate the pharmacokinetics and tissue distribution of palmatine, jatrorrhizine, berberine, epiberberine and formononetin of Yiqi Huoxue Gushen Granules(YHGG) in rats. To provide evidence for further clarifing the pharmacodynamic material basis of this prescription. Methods The HPLC-MS/MS method was established to detect the drug concentration in rat plasma and tissues after oral administration of 4.75 g/kg YHGG. A Kromasil C18 column(3.5 μm, 2.1 mm×100 mm) as the stationary phase and the mobile phase consisted of acetonitrile-0.1% formic acid in water at the flow rate of 0.3 mL/min, the injection volume was 5 μL. The electrospray ionization source(ESI) was set in positive and negative ion mode respectively by multiple reaction monitoring(MRM) scanning. The main pharmacokinetic parameters were calculated by WinNonlin 3.3 software. Results The method met the detection requirements of biological samples. After intragastric administration of compound YHGG, the five components absorbed into the blood rapidly and the plasma concentrations can reached the peak within 30 min. Furthermore, all components owned short half-life and quick elimination rate in vivo. The Cmax and AUC0-t of each component were 4.87～233.12 μg/L, 16.11～493.13 h/(μg·L), respectively. The results of tissue distribution showed that 5 components distributed rapidly, widely but unevenly in vivo. They were more distributed in the stomach and small intestine, followed by liver, kidney and lung, and less in the spleen and heart. Conclusion The method was stable and reliable which will provide reference for the clinical application of YHGG.更多还原