Sitovs Andrejs, Mohylyuk Valentyn
Leading Research Group, Faculty of Pharmacy, Rīga Stradiņš University, Riga, Latvia; Department of Pharmacology, Faculty of Pharmacy, Rīga Stradiņš University, Riga, Latvia.
Leading Research Group, Faculty of Pharmacy, Rīga Stradiņš University, Riga, Latvia.
Drug Discov Today. 2024 Dec;29(12):104214. doi: 10.1016/j.drudis.2024.104214. Epub 2024 Oct 18.
Ex vivo drug permeability testing across gastrointestinal (GI) membranes is crucial in drug discovery and oral drug delivery. It is a reliable method for drugs with good solubility, but it poses challenges for poorly soluble drugs, which are common in development pipelines today. Although enabling formulations increase the apparent solubility in the GI compartment (dissolution vessel or permeation chamber's donor compartment), maintaining solubilized drug in the acceptor compartment during ex vivo testing remains largely unresolved. This review compiles and critically evaluates the diverse compositions of acceptor media used in ex vivo permeability studies for poorly soluble drugs, highlighting this significant yet underexplored aspect of pharmaceutical science. An algorithm is proposed for selecting solubility-enhancing additives for the acceptor media in ex vivo permeability studies of poorly soluble drugs.
跨胃肠道（GI）膜的体外药物渗透性测试在药物研发和口服药物递送中至关重要。对于具有良好溶解性的药物来说，这是一种可靠的方法，但对于难溶性药物则构成挑战，而难溶性药物在当今的研发流程中很常见。尽管促溶制剂可增加药物在胃肠道隔室（溶解容器或渗透室的供体隔室）中的表观溶解度，但在体外测试期间如何在受体隔室中维持溶解状态的药物在很大程度上仍未得到解决。本综述汇编并批判性地评估了用于难溶性药物体外渗透性研究的受体介质的不同组成，突出了药物科学这一重要但尚未充分探索的方面。本文提出了一种算法，用于在难溶性药物的体外渗透性研究中选择受体介质的增溶添加剂。
