超长效胃滞留给药系统的研究进展

Research Progress of Ultra-long-acting Gastroretentive Drug Delivery Systems

传统的胃滞留给药系统(GRDDS)通过物理化学作用,延长药物在胃内的停留时间,起到减少给药频率、提高疗效的目的。然而,人体内的真实滞留效果往往受个体差异、生理及饮食等因素的影响,难以实现真正意义上超过24 h的稳定胃滞留效果。超长效GRDDS是近年来口服制剂领域为数不多的创新突破,通过机械变化(星形结构和弹簧样线圈)的颠覆性设计,大幅增强了抵抗胃生理因素破坏的能力,使胃滞留超过24 h甚至长达1个月变成了可能,若能在安全性和质量方面进一步完善,在口服制剂领域将取得更大的突破。本研究综述了近年来超长效GRDDS的发展,对其技术挑战及应用前景进行了分析和展望。

Gastroretentive drug delivery system(GRDDS) can reduce the frequency of administration and improve the efficacy by prolonging the residence time of drugs in the stomach through physical and chemical effects.However,the real retention effect in human body is often affected by individual differences,physiology,diet and other factors,so it is difficult to achieve the stable gastric retention of more than 24 h in the real sense.Ultra-long-acting GRDDS is one of the unique innovative breakthroughs in the field of oral formulations in recent years.Through the subversive design of mechanical changes(stellate structure and spring coil),ultra-long-acting GRDDS greatly enhances the ability to resist the destruction of stomach physiological factors,making it possible to realize stable gastric retention for more than 24 h or even up to 1 month.If it can be further improved in safety and quality,ultra-long-acting GRDDS will make a great breakthrough in the field of oral preparations.In this paper,the development of ultra-long-acting GRDDS in recent years is reviewed,and its technical challenges and application prospects are analyzed and prospected.