Distribution and pharmacokinetics of five Rhubarb anthraquinones in rabbits and rats  

五种大黄蒽醌类化合物在家兔和大鼠体内的分布和药代动力学(英文)

作　　者：Ting Cui Qixin Zhou Dan Zhang Xinhui Jiang 崔婷;周岐新;张丹;蒋心惠(重庆医科大学药学院,重庆400016;四川大学华西药学院,成都610041)

机构地区：[1]School of Pharmacy, Chongqing Medical University, Chongqing 400016, China [2]West China School of Pharmacy, Sichuan University, Chengdu 610041, China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2017年第2期115-123,共9页中国药学（英文版）

基　　金：The Research Fund of Chongqing Science&Technology Commission(Grant No.cstc2013jcyj A10040);Research Start-up Fund of Pharmacy School of Chongqing Medical University

摘　　要：The main active components of Rhubarb are anthraquinones（AQs）, most of which are glycosides and others are free. The concentrations of AQs derivatives（rhein, aloe-emodin, emodin, chrysophanol and physcion） in plasma and homogenate were assayed with a high performance liquid chromatography（HPLC） method. The pharmacokinetic parameters and distribution of Rhubarb AQs in rabbits or rats were studied after administration of different formulas. Elimination of AQs was fit to a two-compartment model in rats and rabbits. There were no significant difference in the main pharmacokinetic parameters between rhein and AQs in rats. AQs were distributed progressively in the kidney, liver, blood, and heart. The AQs were mainly composed of rhein in vivo and was excreted by the kidney. For formulas that contained Rhubarb, rhein could be used as a probe for in vivo pharmacokinetic studies.大黄的主要有效成分是大多以苷形式存在的蒽醌类化合物。我们采用高效液相色谱法来测定组织和血浆中蒽醌类化合物(芦荟大黄素、大黄素、大黄酸、大黄酚和大黄素甲醚)的浓度。对家兔和大鼠灌胃给予不同制剂后大黄蒽醌类化合物的药代动力学参数和分布特征进行了研究,结果发现其在家兔和大鼠体内的消除过程满足二室模型,在大鼠体内的过程用大黄酸以及总蒽醌的量来计算出的主要药代动力学参数无统计学差异。大黄蒽醌类化合物主要分布于肾、肝、心和血中,并依次减少,蒽醌类化合物在体内主要以大黄酸的形式存在并由肾排出体外。可以以大黄酸作为指标成分来进行含大黄类成分的复方制剂在体内的药代动力学研究。

关 键 词：RHUBARB ANTHRAQUINONES PHARMACOKINETICS DISTRIBUTION 

分 类 号：R285.5[医药卫生—中药学]