中文摘要：

前药研究是提高生物药剂学分类系统中第Ⅲ和Ⅳ类药物口服吸收的有效途径之一。本文综述了近年来口服前药研究的进展，主要包括经典前药设计和靶向前药设计。经典前药设计重在改善母体药物的油水分配系数或减少药物的代谢。靶向前药设计重在主动利用胃肠道的生理特性靶向组织、酶及肠内流转运器，其中靶向小肠内流转运器一肽类转运器的口服前药成为目前研究的热点。前药研究还面临选题，设计和体内研究等方面的挑战。

英文摘要：

Prodrug is an effective way to improve the oral absorption of the drugs which belong to Biopharmaceuticals Classification System （BCS） class Ⅲ and Ⅳ. This review addresses the progress of the oral prodrugs in recent years, mainly including classical prodrug design and targeted prodrug design. Classical prodrug design is focused on modification of oil-water partition coefficient or decrease the metabolism of parent drugs. Targeted prodrug design is actively concerned with the physiological characteristics of the gastrointestinal tract to target tissues, enzymes and influx transporters. Intestinal influx transporter, the peptide transporter-targeted prodrug design is a growing field of the research of oral prodrugs recently. Challenges of prodrug strategy, design and investigation in vivo are also discussed.