Vrettos Napoleon-Nikolaos, Roberts Clive J, Zhu Zheying
School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, UK.
Pharmaceutics. 2021 Sep 30;13(10):1591. doi: 10.3390/pharmaceutics13101591.
There have been many efforts to improve oral drug bioavailability and therapeutic efficacy and patient compliance. A variety of controlled-release oral delivery systems have been developed to meet these needs. Gastroretentive drug delivery technologies have the potential to achieve retention of the dosage form in the upper gastrointestinal tract (GIT) that can be sufficient to ensure complete solubilisation of the drugs in the stomach fluids, followed by subsequent absorption in the stomach or proximal small intestine. This can be beneficial for drugs that have an "absorption window" or are absorbed to a different extent in various segments of the GIT. Therefore, gastroretentive technologies in tandem with controlled-release strategies could enhance both the therapeutic efficacy of many drugs and improve patient compliance through a reduction in dosing frequency. The paper reviews different gastroretentive drug delivery technologies and controlled-release strategies that can be combined and summarises examples of formulations currently in clinical development and commercially available gastroretentive controlled-release products. The different parameters that need to be considered and monitored during formulation development for these pharmaceutical applications are highlighted.
为提高口服药物的生物利用度、治疗效果以及患者的依从性,人们进行了诸多努力。已开发出多种控释口服给药系统以满足这些需求。胃滞留型给药技术有潜力使剂型在上消化道(GIT)中滞留,这足以确保药物在胃液中完全溶解,随后在胃或近端小肠中被吸收。这对于具有“吸收窗”或在胃肠道不同部位吸收程度不同的药物可能有益。因此,胃滞留型技术与控释策略相结合,可以提高许多药物的治疗效果,并通过减少给药频率来提高患者的依从性。本文综述了可结合使用的不同胃滞留型给药技术和控释策略,并总结了目前处于临床开发阶段的制剂实例以及市售的胃滞留型控释产品。文中强调了在这些药物应用的制剂开发过程中需要考虑和监测的不同参数。