Department of Chemical Engineering, Imperial College London, London SW7 2AZ, United Kingdom.
J Pharm Sci. 2011 Nov;100(11):4745-55. doi: 10.1002/jps.22667. Epub 2011 Jun 10.
This work presents the novel application of attenuated total reflection-Fourier transform infrared spectroscopic (ATR-FTIR) imaging to study the dissolution of ibuprofen form tablets in which the internal pH of the matrix has been modified by addition of acidic and basic powders to the formulations. Acidic additives to the matrix retarded the dissolution of crystalline ibuprofen domains. Basic additives formed both soluble and insoluble salts with the ibuprofen depending on the pH modifier added. Tablets consisting of hydroxypropyl methylcellulose, ibuprofen, and an acidic or basic additive were studied. FTIR imaging in ATR mode was used for analysis of water ingress into the tablet and the presence, distribution, and chemical state of the drug. The FTIR imaging data showed distinct changes in the dissolution of crystalline ibuprofen between the formulations with different pH modifiers. In the basic formulations, FTIR imaging identified the formation of salts. The sodium salt formed was highly soluble and enhanced dissolution, whereas the calcium salt was highly insoluble and slowed the dissolution. FTIR imaging has produced important data concerning the internal matrix dissolution performance.
这项工作提出了衰减全反射-傅里叶变换红外光谱（ATR-FTIR）成像的新应用，用于研究布洛芬片剂在基质内部 pH 值通过向配方中添加酸性和碱性粉末而被改变的情况下的溶解情况。基质中的酸性添加剂会延迟结晶布洛芬区域的溶解。碱性添加剂会根据添加的 pH 值调节剂与布洛芬形成可溶性和不溶性盐。研究了由羟丙基甲基纤维素、布洛芬和酸性或碱性添加剂组成的片剂。ATR 模式下的 FTIR 成像用于分析水进入片剂以及药物的存在、分布和化学状态。FTIR 成像数据显示，具有不同 pH 值调节剂的配方中结晶布洛芬的溶解有明显差异。在碱性配方中，FTIR 成像确定了盐的形成。形成的钠盐高度可溶，增强了溶解，而钙盐则高度不溶，减缓了溶解。FTIR 成像提供了有关内部基质溶解性能的重要数据。
