去氢吴茱萸碱的药动学研究进展

Research progress on pharmacokinetics of dehydroevodiamine

去氢吴茱萸碱是吴茱萸的主要活性成分之一,作为吲哚喹唑酮类生物碱,其药理作用包括抗肿瘤、抗心律失常、抗炎、抗病毒等,尤其抗阿尔茨海默病作用显著。去氢吴茱萸碱易透过血脑屏障发挥中枢神经作用,其药时曲线呈现双峰,在体内发生羟基化、去甲基化、与葡萄糖醛酸结合等代谢反应。对去氢吴茱萸碱单体及其在吴茱萸和制剂中的吸收、分布、代谢与排泄过程等药动学研究进展进行综述,总结其药动学特征,以期为临床应用及新药研发提供参考。

Dehydroevodiamine is a main active ingredient from Euodia rutaecarpa.As an indoline-quinazolone alkaloid,its pharmacological effects include anti-tumor,anti-arrhythmia,anti-inflammatory,antiviral,especially in anti-Alzheimer's disease.Dehydroevodiamine could easily cross the blood-brain barrier and act on central nervous system.Its drug time curve showed a bimodal phenomenon,and metabolic pathways are summarized such as hydroxylation,demethylation and conjugation with glucuronic acid.The pharmacokinetics research progress on absorption,distribution,metabolism and excretion of dehydroevodiamine,and dehydroevodiamine in Euodia rutaecarpa and its preparations,were reviewed,and the pharmacokinetic characteristics were summarized,so as to provide reference for the clinical application,further development and application of dehydroevodiamine.