Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
J Pharm Sci. 2011 Aug;100(8):3405-3410. doi: 10.1002/jps.22532. Epub 2011 Mar 8.
Dissolution critically affects the bioavailability of Biopharmaceutics Classification System class 2 compounds. When unexpected dissolution behaviour occurs, detailed studies using high information content technologies are warranted. In the present study, an evaluation of real-time ultraviolet (UV) imaging for conducting single-crystal dissolution studies was performed. Using lidocaine as a model compound, the aim was to develop a setup capable of monitoring and quantifying the dissolution of lidocaine into a phosphate buffer, pH 7.4, under stagnant conditions. A single crystal of lidocaine was placed in the quartz dissolution cell and UV imaging was performed at 254 nm. Spatially and temporally resolved mapping of lidocaine concentration during the dissolution process was achieved from the recorded images. UV imaging facilitated the monitoring of lidocaine concentrations in the dissolution media adjacent to the single crystals. The concentration maps revealed the effects of natural convection due to density gradients on the dissolution process of lidocaine. UV imaging has great potential for in vitro drug dissolution testing.
溶出度会显著影响生物药剂分类系统（BCS）Ⅱ类化合物的生物利用度。当出现意料之外的溶出行为时，有必要使用具有丰富信息含量的技术进行详细研究。在本研究中，我们评估了实时紫外（UV）成像技术在单晶溶出研究中的应用。以利多卡因作为模型化合物，旨在开发一种能够监测和定量测定利多卡因在磷酸盐缓冲液（pH7.4）中在静止条件下溶出的装置。将一片利多卡因单晶置于石英溶出池中，并在 254nm 处进行 UV 成像。通过记录的图像实现了溶解过程中利多卡因浓度的空间和时间分辨映射。UV 成像有助于监测单晶附近溶出介质中的利多卡因浓度。浓度图揭示了由于密度梯度引起的自然对流对利多卡因溶出过程的影响。UV 成像在体外药物溶出测试中具有巨大的潜力。
