胃滞留给药系统的研究进展  

Research Progress of Gastroretentive Drug Delivery Systems

作　　者：胡满钰 朱壮志[2] 王浩[2] HU Manyu;ZHU Zhuangzhi;WANG Hao(Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014;National Pharmaceutical Engineering and Research Center, China State Institute of Pharmaceutical Industry, Shanghai 201203)

机构地区：[1]浙江工业大学长三角绿色制药协同创新中心,浙江杭州310014 [2]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2019年第3期241-251,共11页Chinese Journal of Pharmaceuticals

摘　　要：药物在吸收部位的停留时间是影响治疗效果的关键因素之一。传统的口服给药系统往往由于快速的胃排空、较短的胃肠道转运时间,在药物完全释放之前就被排出体内,导致给药次数频繁、生物利用度降低。胃滞留给药系统(gastroretentive drug delivery system,GRDDS)的开发使药物在胃部长时间停留成为可能,它主要依靠增大制剂的尺寸、提高黏附性或改变密度等方式来避免快速胃排空。GRDDS能使药物在胃肠道上端的吸收程度增大、生物利用度提高,从而提高临床疗效、减少给药次数、增加患者的顺应性,目前已有多个产品上市。本文综述了GRDDS的研究进展,主要包括其影响因素、分类及体内评价方法,并展望了GRDDS的应用前景。The residence time of drugs at the absorption site is one of the key factors affecting the treatment effect. Conventional oral dosage forms are often eliminated before complete release because of rapid gastric emptying and short gastrointestinal transit time. It causes low bioavailability and frequent dosing. Based on comprehending the physiological parameters of the gastrointestinal tract, the research of gastroretentive drug delivery system (GRDDS) has been nearly 30 years. The development of GRDDS makes it possible for drugs to stay in the stomach for a longer time. It mainly depends on the size growth, the adhesion improving and the density changing of the formulation to resist gastric emptying. Various gastroretentive technologies have been developed, mainly including expandable system, high density system, bio/mucoadhesive system, floating system, superporous hydrogel, magnetic system and dual work system. GRDDS can increase the bioavailability and absorption of drugs at the upper gastrointestinal tract, thus it can reduce dosing frequency, increase patient compliance and improve clinical efficacy. Also, the emergence of multi-unit GRDDS guarantees better effectiveness and safety of drugs. Currently, GRDDS has many related marketed products. This paper reviews the recent development of GRDDS, including the impacts, the classification and in vivo evaluation methods of GRDDS, and then looks forward to the application prospects of GRDDS.

关 键 词：胃滞留 缓控释 评价方法 多单元 

分 类 号：R944.9[医药卫生—药剂学]