目的:采用液相色谱-质谱联用(LC-MS/MS)法测定大鼠血浆及组织样品中毛蕊花糖苷的浓度,并探讨其在大鼠体内吸收、分布及排泄研究。方法:SD大鼠灌胃给予毛蕊花糖苷20,40,80,160 mg·kg~(-1)后,于不同时间点采血,给予40 mg·kg~(-1)剂量进行分布和排泄试验,测定血浆、组织和排泄物中的毛蕊花糖苷浓度,并用DAS 2.0软件拟合并计算药动学参数。结果:大鼠给药20,40,80,160 mg·kg-1的毛蕊花糖苷后,药时曲线呈二室开放模型,主要药动学参数tmax,Cmax,t1/2α,AUC0-t,AUC0-∞,CL/F,V/F分别为(17.50±10.37)min、(0.313±0.04)mg·L-1、(6.79±12.10)min、(21.39±4.03)mg·L~(-1)·min~(-1)、(22.39±3.89)mg·L~(-1)·min~(-1)、(1.83±0.30)L·min~(-1)·kg-1、(179.10±52.77)L·kg~(-1)。大鼠给予40 mg·kg-1的毛蕊花糖苷后,毛蕊花糖苷在尿液和粪便中36 h内的累积排泄百分数分别为(0.037±0.005)%、(0.004 2±0.000 8)%,胆汁中12 h内的累积排泄率基本为零。结论:毛蕊花糖苷在大鼠体内吸收符合一级动力学,分布在小肠和肺浓度最高,其次为胃和肌肉,其他组织都有少量的分布;且通过尿液、粪便和胆汁排泄量较少,其可能主要通过代谢过程进行消除。 OBJECTIVE: To determine the concentrations of verbascoside in rat plasma and tissue samples by liquid chromatography-mass spectrometry (LC-MS / MS) and investigate their absorption, distribution and excretion in rats. Methods: SD rats were given gavagenoside 20, 40, 80 and 160 mg · kg ~ (-1) orally, and the blood samples were taken at different time points. The distribution and excretion of 40 mg · kg ~ (-1) , Verbascoside concentrations in tissues and excretions, and fitted with the DAS 2.0 software and calculated pharmacokinetic parameters. RESULTS: After administration of 20, 40, 80 and 160 mg · kg-1 of verbascoside, the pharmacokinetic parameters of rats were two-compartment open model. The main pharmacokinetic parameters tmax, Cmax, t1 / 2α, AUC0-t and AUC0-∞ , And the values ​​of CL / F and V / F were (17.50 ± 10.37) min, (0.313 ± 0.04) mg · L -1, (6.79 ± 12.10) min and (21.39 ± 4.03) mg · L -1 · min (-1), (22.39 ± 3.89) mg · L -1 · min -1, 1.83 ± 0.30 L · min -1 · kg -1, and (179.10 ± 52.77) L · kg ~ (-1). After excretion of 40 mg · kg -1 of verbascoside, the cumulative excretion percentages of verbascoside in urine and feces within 36 h were (0.037 ± 0.005)%, (0.0042 ± 0.000 8)%, 12 The cumulative excretion rate within h is essentially zero. Conclusions: Abacus glycosides uptake in rats is consistent with the first order kinetics, with the highest concentration in the small intestine and lung, followed by the stomach and muscle, and the other tissues have a small amount of distribution; and excretion of urine, feces and bile is less, It may be eliminated primarily through metabolic processes.