Hou Sui Yuen Eddie, Cowles Verne E, Berner Bret
Depomed, Inc., Menlo Park, California, USA.
Crit Rev Ther Drug Carrier Syst. 2003;20(6):459-97. doi: 10.1615/critrevtherdrugcarriersyst.v20.i6.30.
Gastric retentive dosage forms have been investigated to provide controlled release therapy for drugs with reduced absorption in the lower gastrointestinal (GI) tract or for local treatment of diseases of the stomach or upper GI tract. Gastric retentive dosage forms rely on either natural GI physiology, such as floating or large tablets that depend on delayed emptying from the fed stomach, or those dosage forms that are designed to fight the physiology and avoid emptying in the fasted state through dosage forms of even larger sizes with or without flotation or bioadhesion. To understand the behavior of the dosage forms, an introduction to GI motility and its measurement is provided. Because the fed mode underlies the successful development of dosage forms that rely on size or flotation, the emptying of these dosage forms in the fed mode and identification of the key factors influencing the variability of gastric retention are discussed. The design and limitations of size or density-based fed mode, and mucoadhesive and expandable fasting-state gastric retentive systems are presented.
胃滞留剂型已被研究用于为在下消化道(GI)吸收减少的药物提供控释治疗,或用于胃部或上消化道疾病的局部治疗。胃滞留剂型依赖于自然的胃肠道生理机制,例如依靠进食后胃排空延迟的漂浮剂型或大片剂,或者是那些旨在对抗生理机制并通过具有或不具有漂浮或生物粘附性的更大尺寸剂型避免在禁食状态下排空的剂型。为了理解这些剂型的行为,本文介绍了胃肠动力及其测量方法。由于进食模式是依赖尺寸或漂浮的剂型成功开发的基础,因此讨论了这些剂型在进食模式下的排空以及影响胃滞留变异性的关键因素的识别。还介绍了基于尺寸或密度的进食模式、粘膜粘附和可膨胀的禁食状态胃滞留系统的设计和局限性。