黄芩素药代动力学研究进展

黄芩为中国药典收载的常用中药材,具有悠久的用药历史,含有多种黄酮类化合物,其中黄芩素为常用中药黄芩中的主要活性成分之一。笔者通过对黄芩素在体内的药动学研究进行总结,发现:黄芩素胃肠道吸收较好,主要分布在肝、肾、肺等组织器官中;黄芩素在大鼠体内代谢物主要是葡萄糖醛酸结合物,后者又可经胆汁和肠黏膜转运至肠腔,形成再吸收;黄芩素口服后血浆原型药物浓度极低。目前针对黄芩素的药动学行为研究主要是通过其代谢物黄芩苷的测定来间接实现,由此使得黄芩素替代黄芩苷进行口服制剂研究也成为可能。

Progress in Pharmacokinetic Researches of Baicalein

Scutellaria baicalensis Georgi, included in Chinese Pharmacopoeia, has been long used as a traditional Chinese medicinal material, which contains many kinds of flavonoids compounds, and baicalein is one of the main active components. Here, we present the recent reviews of pharmacokinetics of baicalein in vivo, and find out that:it has good absorption in gastrointestinal tract and distributes mainly in liver, kidney, lung and other vital organs and tissues; the main metabolites of baicalein in rat are the compounds of baicalein with glucuronic acid, which can be transported to gut lumen by bile and intestine mucous membrane, and can be reabsorbed. The concentration of the unchanged drug in plasma is very low after oral administration of baicalein. At present, the research on pharmacokinetics of baicalein is mainly achieved indirectly by determining baicalin, which suggests that baicalein may substitute for baicalin in oral preparation.