Davis Stanley S
Institute of Pharmaceutical Sciences, University of Nottingham, University Park, Nottingham, NG7 2RD, UK.
Drug Discov Today. 2005 Feb 15;10(4):249-57. doi: 10.1016/S1359-6446(04)03351-3.
Absorption windows in the proximal gut can limit the bioavailability of orally administered compounds and can be a major obstacle to the development of controlled release formulations for important drugs. Methods to increase the residence of drug formulations at or above the absorption window are discussed in this review. Two main approaches are presently being explored: (i) bioadhesive microspheres that have a slow intestinal transit; and (ii) the gastroretentive dosage system, which is based on multiparticulates or large single unit systems. A good understanding of gastrointestinal transit in humans and the effect of factors such as food can be helpful in the design of rational systems that will have clinical benefit.
近端肠道的吸收窗会限制口服化合物的生物利用度,并且可能成为重要药物控释制剂开发的主要障碍。本综述讨论了增加药物制剂在吸收窗或其上方停留时间的方法。目前正在探索两种主要方法:(i)具有缓慢肠道转运的生物粘附微球;以及(ii)基于多颗粒或大的单一单元系统的胃滞留给药系统。深入了解人类胃肠道转运以及食物等因素的影响,有助于设计出具有临床益处的合理系统。