Sun Yu, Østergaard Jesper
Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen Ø, Denmark.
Pharm Res. 2017 May;34(5):929-940. doi: 10.1007/s11095-016-2047-5. Epub 2016 Oct 20.
Efficient drug delivery is dependent on the drug substance dissolving in the body fluids, being released from dosage forms and transported to the site of action. A fundamental understanding of the interplay between the physicochemical properties of the active compound and pharmaceutical excipients defining formulation behavior after exposure to the aqueous environments and pharmaceutical performance is critical in pharmaceutical development, manufacturing and quality control of drugs. UV imaging has been explored as a tool for qualitative and quantitative characterization of drug dissolution and release with the characteristic feature of providing real-time visualization of the solution phase drug transport in the vicinity of the formulation. Events occurring during drug dissolution and release, such as polymer swelling, drug precipitation/recrystallization, or solvent-mediated phase transitions related to the structural properties of the drug substance or formulation can be monitored. UV imaging is a non-intrusive and simple-to-operate analytical technique which holds potential for providing a mechanistic foundation for formulation development. This review aims to cover applications of UV imaging in the early and late phase pharmaceutical development with a special focus on the relation between structural properties and performance. Potential areas of future advancement and application are also discussed.
高效的药物递送取决于药物溶解于体液、从剂型中释放并转运至作用部位。深入了解活性化合物的物理化学性质与药物辅料之间的相互作用（这种相互作用决定了剂型在暴露于水性环境后的行为及药物性能）对于药物研发、生产和质量控制至关重要。紫外成像已被探索作为一种用于定性和定量表征药物溶解和释放的工具，其特点是能够实时可视化制剂附近溶液相药物的转运。药物溶解和释放过程中发生的事件，如聚合物溶胀、药物沉淀/重结晶，或与药物物质或制剂结构性质相关的溶剂介导的相变等均可被监测。紫外成像技术是一种非侵入性且操作简便的分析技术，具有为制剂研发提供机理基础的潜力。本综述旨在涵盖紫外成像在药物研发早期和后期阶段的应用，特别关注结构性质与性能之间的关系。还讨论了未来潜在的发展和应用领域。
