基于肠道微生物的口服药物生物利用度研究进展

Research Progress of Bioavailability of Oral Drugs Based on the Gut Microbiota

口服给药是目前较普遍的给药方式之一,具有安全性高、经济便捷等特点。然而,许多药物的强大功效与其口服后较低的生物利用度之间有巨大差异,限制了应用。近年来的研究显示,这种差异与肠道中作为有效生物反应器的肠道微生物密切相关。肠道微生物除了可通过生物转化直接参与药物代谢外,还可通过调节宿主肝脏代谢酶以及转运蛋白的表达间接影响药物的口服生物利用度。本研究简要介绍了影响药物生物利用度的因素,主要探讨了肠道微生物及益生菌对药物生物利用度的影响,为进一步了解肠道微生物与药物口服生物利用度的关系,以及如何提高药物口服生物利用度提供文献参考。

Oral administration,with the characteristics of high safety and economic convenience,is one of the most common ways of drug delivery.However,the substantial discrepancy between potent therapeutic properties of various medicines and their low oral bioavailability limits their application.In recent years,researches have revealed that gut microbiota,which act as a practical bioreactor in the human intestinal tract,have an essential effect on the discrepancy.In addition to directly participating in drug metabolism through biotransformation,gut microbiota can also indirectly affect bioavailability of oral drugs by regulating the expression levels of host liver metabolic enzymes and the transporters.This review briefly introduces the factors affecting drug bioavailability,and mainly discusses the effects of gut microbiota and probiotics on drug oral bioavailability to provide a reference for understanding the relationship between gut microbiota and drug oral bioavailability,and developing novel strategies for improving drug oral bioavailability.