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目的:考察知母配伍黄柏对知母有效成分芒果苷在大鼠体内药物动力学的影响。方法:SD大鼠随机分为4组,分别单次灌胃(ig)芒果苷单体、知母单煎液、知母-黄柏1∶3和1∶1合煎液(剂量按芒果苷计算为35 mg·kg-1),采用液相色谱-串联质谱法测定血浆中芒果苷浓度,用DAS软件根据非房室模型法计算药物动力学参数。结果:知母单煎液组芒果苷血药浓度比单体组明显升高,配伍黄柏后有所下降。大鼠单次ig芒果苷单体、知母单煎液、知母-黄柏1∶3和1∶1合煎液后的主要药动学参数:药时曲线下面积(AUC0～t)分别为0.626,122.4,94.36,53.97 mg·L-1·h-1,峰浓度(Cmax)分别为0.149,21.52,16.26,8.27 mg·L-1,达峰时间(Tmax)分别为1.0,3.0,4.0,6.0 h,半衰期t1/2分别为3.41,1.46,1.65,1.77 h。结论:知母配伍黄柏后,芒果苷在大鼠体内的吸收随黄柏配伍比例的增加而减少,吸收速度减慢,t1/2未发生明显变化。
OBJECTIVE: To investigate the effects of Anemarrhena asphodeloides Rhizome on the pharmacokinetics of the active ingredient mangiferin in rats. Methods: The SD rats were randomly divided into 4 groups. The rats were given a single intragastric (ig) mangiferin monomer solution, Zhimu Decoction, Anemarrhena to Treats 1: 3 and 1: 1 decoction (35 mg · kg-1). The plasma concentrations of mangiferin were determined by liquid chromatography-tandem mass spectrometry. The pharmacokinetic parameters were calculated by DAS software based on the non-compartmental model. Results: The blood concentration of mangiferin in Zhimu Decoction group was significantly higher than that in the monomer group, but decreased after compatibility with the cork. The main pharmacokinetic parameters of rats single ig mangiferin monomer, Zhimu Dan decoction, Anemarrhena to Treats 1: 3 and 1: 1 decoction: the area under the curve (AUC0 ~ t) 0.626,122.4,94.36,53.97 mg · L-1 · h-1, the peak concentrations (Cmax) were 0.149,21.52,16.26,8.27 mg · L-1, the peak time (Tmax) were 1.0,3.0,4.0 , 6.0 h, half-life t1 / 2 were 3.41,1.46,1.65,1.77 h. Conclusion: The results showed that the absorption of mangiferin decreased with the increase of the proportion of cortex phellodendri in Rhizoma et Rhizoma. However, the absorption rate of mangiferin slowed down and t1 / 2 did not change obviously.