Department of Pharmaceutical and Pharmacological Sciences, KU Leuven, Leuven, Belgium; Department of Chemical and Pharmaceutical Engineering, Sofia University, Sofia, Bulgaria.
Oral Product Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Gothenburg, Sweden.
Adv Drug Deliv Rev. 2021 Apr;171:289-331. doi: 10.1016/j.addr.2021.02.001. Epub 2021 Feb 18.
Although oral drug delivery is the preferred administration route and has been used for centuries, modern drug discovery and development pipelines challenge conventional formulation approaches and highlight the insufficient mechanistic understanding of processes critical to oral drug absorption. This review presents the opinion of UNGAP scientists on four key themes across the oral absorption landscape: (1) specific patient populations, (2) regional differences in the gastrointestinal tract, (3) advanced formulations and (4) food-drug interactions. The differences of oral absorption in pediatric and geriatric populations, the specific issues in colonic absorption, the formulation approaches for poorly water-soluble (small molecules) and poorly permeable (peptides, RNA etc.) drugs, as well as the vast realm of food effects, are some of the topics discussed in detail. The identified controversies and gaps in the current understanding of gastrointestinal absorption-related processes are used to create a roadmap for the future of oral drug absorption research.
虽然口服给药是首选的给药途径,并且已经使用了几个世纪,但现代药物发现和开发管道挑战了传统的制剂方法,并突出了对口服药物吸收关键过程的机械理解不足。本文介绍了 UNGAP 科学家对口服吸收领域的四个关键主题的看法:(1)特定患者群体;(2)胃肠道的区域差异;(3)先进的制剂;(4)食物-药物相互作用。儿科和老年人群体的口服吸收差异、结肠吸收的具体问题、水溶性差(小分子)和渗透性差(肽、RNA 等)药物的制剂方法,以及广泛的食物效应,都是详细讨论的主题之一。本文还确定了当前对胃肠道吸收相关过程理解中存在的争议和差距,为未来的口服药物吸收研究制定了路线图。