酒制大黄对大鼠体内药动学的影响  

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

作　　者：吴育[1] 张永鑫 蒋晟昰 陈刚[1] 姜晓燕[1] WU Yu ZHANG Yong-xin JIANG Sheng-shil CHEN Gang JIANG Xiao-yan(Department of Pharmacy, Nantong Chinese Medicine Hospital, Nantong 226001, China Simcere Pharma- ceutical Group, Nanjing 210042, China)

机构地区：[1]南通市中医院药剂科,南通226001 [2]南京先声药业集团,南京210042

出　　处：《药学与临床研究》2017年第5期392-396,共5页Pharmaceutical and Clinical Research

基　　金：江苏省南通市青年基金(WQ2016056)

摘　　要：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。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 aloeemodin, 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.

关 键 词：大黄酸 芦荟大黄素 大黄素 药物代谢动力学 液-质联用 

分 类 号：R965.1[医药卫生—药理学]