泻心汤沉淀物代谢产物的研究Ⅰ

Study on the metabolism of the precipitation of Xiexin decoction in rats Ⅰ

目的:研究泻心汤配伍沉淀物的大鼠体内过程。方法:利用液质联用技术对口服泻心汤沉淀物、单味黄芩煎液及黄芩苷后大鼠尿中黄芩苷及其代谢产物进行定性定量分析;采用原位襻技术研究各样品中的黄芩苷在小肠的吸收情况。结果:各样品中黄芩苷在大鼠体内经尿排泄各时间段内代谢的量没有显著性差异,但其排泄达峰时间存在显著性差异。大鼠对于泻心汤沉淀物中黄芩苷的吸收率明显高于黄芩煎液和黄芩苷。经液质联用分析,发现汉黄芩苷和7-O-葡萄糖醛酸-白杨素出现在口服黄芩苷后大鼠的尿中,这2个化合物作为黄芩苷的代谢产物未见相关报道。结论:泻心汤沉淀物在大鼠空肠内的吸收率明显大于黄芩和黄芩苷。其代谢产物可能与黄芩素等活性成分共存并共同构成泻心汤沉淀物的药效。

Objective： To study the process in vivo of the components in the precipitation of Xiexin decoction. Method：The components in the rats＇ urine samples after oral administration of baicalin, single herb decoction of Radix Scutellariae or the precipitation of Xiexin decoction were analyzed by LC-MS-MS method; and the absorption of baicalin in different samples were calculated by intestinal in situ loop method. Result： The urinary excretion amounts of baicalin in three samples were not obviously different, whereas the time reach eliminationpeak of baicalin in them had significant difference. The absorption of baicalin in the precipitation was obviously greater than that in the single herb decoction and single baicalin. We found that wogonoside and 7-0-glucuronide chrysin were the metabolites presenting in the rat urine samples after oral administration of baicalin by LC-MS-MS, which had never been reported. Conclusion： The resident time in the body of baicalin in the precipitation is prolonged, compared with that in the single herb decoction and single baicalin. The metabolites may be the potential biological components in vivo of baicalin in the precipitation.