白芍化学成分体内吸收、分布、代谢、排泄研究进展

Research Progress on Absorption,Distribution,Metabolism and Excretion of Chemical Constituents in Baishao(Paeoniae Radix Alba)

白芍(Paeoniae Radix Alb,PRA)为毛茛科药用植物芍药的干燥根,在中医临床上应用广泛。以芍药苷(Paeoniflorin,pea)和芍药内酯苷为代表的单萜及其苷类成分是白芍中公认的药效物质。对白芍总苷及pea、芍药内酯苷等主要成分在体内吸收(Absorption)、分布(Distribution)、代谢(Metabolism)、排泄(Excretion)(即药物体内的ADME过程)的相关研究进行系统地梳理、归纳发现,白芍中主要成分为被动吸收,芍药内酯苷主要经上消化道吸收且存在吸收饱和现象,pea和白芍总苷的主要吸收肠段为空肠及十二指肠,芍药内酯苷主要分布在胃部,皮肤为pea的主要分布部位,小肠、胃、大肠为白芍总苷的主要分布部位,白芍主要通过脱羟基,脱羧,脱氢,硫酸化,葡萄糖醛酸化和甲基化进行代谢且代谢特性存在差异,并主要以胆汁和尿液的形式排出。目前对白芍ADME相关研究结果存在一定的差异,无法系统全面反映白芍中化学成分与机体的相互作用。该文可为进一步阐释白芍在体内发挥药效的机制、药效评价和新药开发以及临床应用提供参考。

Baishao(Paeoniae Radix Alba,PRA)is the dried root of Shaoyao(Paeonia lactiflora),and is widely used in clini-cal practice of traditional Chinese medicine.The monoterpenes and their glycosides represented by paeoniflorin(pea)and albi-florin are generally recognized as effective substances in PRA.In this paper,the absorption,distribution,metabolism and excretion(ADME process in drugs)of total glucosides of paeonia,pea and albiflorin in vivo were systematically combed and summarized and it has found that main ingredients in PRA are passive absorption;albiflorin is absorbed mainly through the upper digestive tract and there is absorption saturation phenomenon.The main absorption segments of pea and total glycosides of PRA are the je-junum and duodenum.Albiflorin is mainly distributed in the stomach,the skin is the main distribution site of pea,and the small intestine,stomach and large intestine are the main distribution sites of total glucosides of paeonia.PRA mainly through dehydrox-ylation,decarboxylation,dehydrogenation,sulfate,aldehyde acidification and methylation of glucose metabolism,and mainly in the form of bile and urine discharge.There are some differences in the results of studies on the ADME of PRA,which cannot system-atically and comprehensively reflect the interaction between the chemical components of PRA and the body.This paper reviewed the progress on ADME of chemical constituents in PRA to provide a reference for further explaining the mechanism of exerting ef-ficacy,efficacy evaluation,new drug research and development and clinical application of PRA.