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目的:研究大鼠肝微粒体温孵育体系中黄芩苷和黄芩素的代谢动力学,比较半夏泻心汤全方及不同配伍组对其肝微粒体代谢的影响。方法:超高效液相色谱法(UPLC)测定大鼠肝微粒体温孵体系中黄芩苷和黄芩素含量。采用在体诱导-体外肝微粒体温孵方法,考察半夏泻心汤全方、辛温开痞配伍、苦寒降逆配伍及甘滋补益配伍对黄芩苷和黄芩素在大鼠肝微粒体系中的代谢变化影响。结果:黄芩苷温孵时间在60 min内,黄芩素在10 min内呈线性消除;黄芩苷和黄芩素质量浓度为0.5～25μg/mL内与峰面积呈良好的线性关系;肝微粒体蛋白质量浓度在0.2～1.0 g/L内,黄芩苷和黄芩素随着肝微粒体蛋白质量浓度的增大,呈线性消除。空白肝微粒体中黄芩素的代谢速率大于黄芩苷;与空白对照组比较,全方组对黄芩苷和黄芩素的代谢较其他配伍组抑制作用强,苦寒降逆配伍组次之,辛温开痞配伍组无显著性差异,甘滋补益配伍组对黄芩苷无抑制作用,对黄芩素抑制作用不显著。结论:半夏泻心汤抑制黄芩苷和黄芩素的代谢,且抑制作用较其他配伍组强,为半夏泻心汤组方合理性及临床配伍发挥相须相使的疗效提供了重要的药理学依据。
OBJECTIVE: To study the pharmacokinetics of baicalin and baicalein in rat liver microsomal temperature incubation system and compare the effect of Banxiaxiexin Decoction and different compatibility groups on liver microsome metabolism. Methods: The contents of baicalin and baicalein in rat liver microsomal incubation system were determined by ultra performance liquid chromatography (UPLC). In vivo induction - in vitro liver microsomal incubation method, to investigate the Banxiaxiexin Decoction, systolic pressure Xinmi swelling, bitter cold descending compatibility and Ganzhuo replenishing compatibility of baicalin and baicalein in rat liver microsomal metabolic changes influences. Results: The incubation time of baicalin was within 60 min and baicalein was linearly eliminated within 10 min. The linear relationship between baicalin and baicalein was 0.5-25 μg / mL and the peak area was linear. The protein content of liver microsome Concentration of 0.2 ~ 1.0 g / L, baicalin and baicalin with the increase of liver microsomal protein concentration, was linearly eliminated. Compared with the blank control group, the metabolism of baicalin and baicalein in the whole prescription group was stronger than that in the other compatibility groups, followed by the bitter, cold and descending combination group, and Xin-Wen-Kai No significant difference between the rhyme compatibility group, compatibility group Ganzhu baicalin no inhibitory effect on the inhibition of baicalein was not significant. Conclusion: Banxiaxiexin Decoction inhibits the metabolism of baicalin and baicalein, and its inhibitory effect is stronger than that of other compatibility groups, providing an important pharmacological effect for the rational use of Banxiaxiexin Decoction and the clinical compatibility. Learn from.