大黄化学成分的药动学及其代谢的研究进展

Research Progress of Pharmacokinetics and Metabolism of Chemical Compositions in Rhei Radix et Rhizoma

大黄是临床常用中药之一,当前关于其药动学和代谢研究主要关注游离蒽醌类成分。本文综述近年来关于大黄药动学与代谢的文献,梳理大黄化学成分的药动学研究(应用的分析技术、药味配伍对大黄蒽醌药动学影响、在不同机体状态下对大黄蒽醌药动学影响、大黄复方中蒽醌药动学研究),大黄化学成分在体内的代谢研究(应用的分析手段、借助的信息技术、体内的代谢途径)和大黄化学成分在体外的代谢研究。总结其吸收和代谢的特征,为该药物的后期研究奠定基础和提供参考。研究发现大黄蒽醌吸收快而消除慢,而药味配伍和机体状态都会影响其吸收和代谢。大黄化学成分的体内和体外代谢途径主要是葡萄糖醛酸化、硫酸酯化、甲基化等,其代谢物主要来源于蒽醌类成分。

Rhei Radix et Rhizoma is a widely used crude herb. Currently,pharmacokinetic and metabolism studies of chemical components in Rhei Radix et Rhizoma was focused on free anthraquinones. This paper focused on current reports of pharmacokinetic and metabolism studies of Rhei Radix et Rhizoma, and illuminated its characteristics of pharmacokinetic and metabolism. Based on related references, anthraquinones were absorbed rapidly, but eliminated slowly. However, its absorption and elimination was easily affected by formula compatibility and body status. According to reports on in vivo and in vitro metabolism of Rhei Radix et Rhizoma,its major metabolic pathway was glucuronidation,sulfation,methylation,etc. Besides,its metabolites was mainly derived from anthraquinones.