差溶性药物通过胃肠道膜的体内外渗透性研究：受体区介质成分。

IF 6.5 2区医学 Q1 PHARMACOLOGY & PHARMACY

Drug Discovery Today Pub Date : 2024-10-18 DOI:10.1016/j.drudis.2024.104214

Andrejs Sitovs , Valentyn Mohylyuk

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引用次数: 0

摘要

跨胃肠道（GI）膜的体内外药物渗透性测试对于药物发现和口服给药至关重要。对于溶解度高的药物来说，这是一种可靠的方法，但对于溶解度低的药物来说，则是一种挑战。虽然使能配方能提高药物在消化道腔室（溶解容器或渗透室的供体腔室）中的表观溶解度，但在体内外测试过程中，保持药物在受体腔室中的溶解度在很大程度上仍是一个悬而未决的问题。本综述汇编并批判性地评估了用于低溶解性药物体内外渗透性研究的受体介质的各种成分，强调了制药科学中这一重要但尚未充分探索的方面。本文提出了一种算法，用于在体内外低溶性药物渗透性研究中为受体介质选择溶解性增强添加剂。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Ex vivo permeability study of poorly soluble drugs across gastrointestinal membranes: acceptor compartment media composition

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Ex vivo permeability study of poorly soluble drugs across gastrointestinal membranes: acceptor compartment media composition

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.

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来源期刊

Drug Discovery Today 医学-药学

CiteScore

14.80

自引率

2.70%

发文量

293

审稿时长

6 months

期刊介绍： Drug Discovery Today delivers informed and highly current reviews for the discovery community. The magazine addresses not only the rapid scientific developments in drug discovery associated technologies but also the management, commercial and regulatory issues that increasingly play a part in how R&D is planned, structured and executed. Features include comment by international experts, news and analysis of important developments, reviews of key scientific and strategic issues, overviews of recent progress in specific therapeutic areas and conference reports.