酒制大黄对大鼠体内药动学的影响

目的：建立同时测定大鼠血浆及组织中芦荟大黄素、大黄酸和大黄素的液-质联用方法，并探讨酒制大黄中游离蒽醌成分对大鼠体内的药动学的影响。方法：分别给予SD大鼠灌胃大黄生品和酒制品水煎液后，采用LC-MS测定血浆中大黄酸、芦荟大黄素、大黄素的血药浓度的含量。结果：大黄酒制品组的药动学参数（Tmax、Cmax、T1/2和AUC0-t）与生品组相比具有显著性差异，大黄酒制后，芦荟大黄素和大黄素在大鼠体内的Tmax均有不同程度的延长，Cmax均较生品组高，AUC0-t也有不同程度的增加，说明大黄酒制后有助于促进芦荟大黄素和大黄素的吸收，增加其生物利用度。但两者的半衰期T1/2均有所减少，说明两者在体内代谢较快；大黄酸的药动学参数变化不大。结论：酒制大黄中游离蒽醌成分对大鼠体内的药物代谢动力学有较大影响，该研究结果为探讨大黄炮制机理提供实验依据。

Effects of Wine Processed Rheum Palmatum on the Pharmacokinetics of Aloe-emodin, Rhein and Emodin in Rats by High Performance Liquid Chromatography/Mass Spectrometry

Objective: A sensitive and specific method was developed for the determination of aloe-emodin, rhein and emodin in rat plasma. The method was applied to explore the effects of wine processed Rheum palmatum on the pharmacokinetics of anthraquinone components. Methods: After oral administration of extracts from wine processed Rheum palmatum or Rheum palmatum, simultaneous determination of aloe-emodin, rhein and emodin in rat plasma were done by high performance liquid chromatography/mass spectrometry. Results: Compared with those of Rheum palmatum, the pharmacokinetic parameters of wine processed Rheum palmatum were quite different. Conclusion: Wine processing of Rheum palmatum can change the pharmacokinetics of anthraquinone components significantly, which provides experimental data for the study on the processing mechanism of Rheum palmatum.