Mylan School of Pharmacy, Graduate School of Pharmaceutical Sciences, Duquesne University, Pittsburgh, PA, USA.
Crit Rev Ther Drug Carrier Syst. 2011;28(1):47-99. doi: 10.1615/critrevtherdrugcarriersyst.v28.i1.20.
The oral delivery of drugs with a narrow absorption window in the gastrointestinal tract (GIT) is often limited by poor bioavailability with conventional dosage forms due to incomplete drug release and short residence time at the site of absorption. To overcome this drawback and to maximize the oral absorption of these drugs, gastroretentive systems such as mucoadhesive, high-density, expandable, and floating systems have been developed. These systems provide controlled delivery of drugs with prolonged gastric residence time. However, in humans, differences in various physiological and biological factors can affect the gastric residence time and drug-delivery behavior from gastroretentive systems. Some floating drug-delivery systems (FDDS) have shown the capability to accommodate these variations without affecting drug release. This review mainly focuses on various physiological considerations for development of FDDS, and highlights recent technological developments including new dosage forms and their production techniques (e.g., holt-melt extrusion, melt pelletization, and pulsed plasma-irradiation processes). Alternatives to the existing in vitro compendial methods for evaluating floating dosage forms will be discussed, and a critical analysis of the existing literature on FDDS, identifying the potential areas for future research, is provided.
口服在胃肠道(GIT)中吸收窗口狭窄的药物,由于药物释放不完全和吸收部位的停留时间短,常受到常规剂型生物利用度差的限制。为了克服这一缺点,并使这些药物的口服吸收最大化,已经开发了胃滞留系统,如粘膜粘附、高密度、可膨胀和漂浮系统。这些系统提供了具有延长胃滞留时间的药物控释。然而,在人体中,各种生理和生物学因素的差异会影响胃滞留时间和胃滞留系统的药物传递行为。一些漂浮药物递送系统(FDDS)已显示出适应这些变化而不影响药物释放的能力。本综述主要侧重于开发 FDDS 的各种生理考虑因素,并强调了最近的技术发展,包括新的剂型及其生产技术(例如,热熔挤出、熔融造粒和脉冲等离子体照射工艺)。还将讨论替代现有评价漂浮剂型的体外统编方法,并对 FDDS 的现有文献进行批判性分析,确定未来研究的潜在领域。