Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Int J Pharm. 2012 May 10;427(2):270-5. doi: 10.1016/j.ijpharm.2012.02.017. Epub 2012 Feb 16.
Tomographic imaging techniques are attractive tools for the visualization of the internal structural characteristics of pharmaceutical solid dosage forms. In this paper, the internal structure of the tablet core for a monolith osmotic drug delivery system, felodipine sustained-release tablet, was visualized via synchrotron radiation X-ray computed microtomography during the drug release process. The surface areas and three dimensional parameters of the tablet core were calculated based on the three dimensional reconstruction of the images. At different stages of the drug release process, the surface morphology, the hydration, the swelling, and the structure changing of the tablet, were visualized from the two dimensional monochrome X-ray images. The three dimensional volumes of the remaining tablet core correlated well with the percentages of felodipine (R=0.9988). Also, the three dimensional surface area almost unchanged during the drug release process, which clearly demonstrated the intrinsic drug release mechanism of the osmotic drug delivery system. In conclusion, the synchrotron radiation X-ray computed microtomography, with rapid acquisition, high intensity and micro-scale spatial resolution, was found to be a useful tool for the quantitative elucidation of the intrinsic drug release kinetics and the three dimensional parameters such as surface areas of the remained core obtained by the synchrotron radiation. Thus, X-ray computed microtomography can be considered as a new and complimentary analytical tool to standard compendial pharmaceutical tests for quality control of osmotic drug delivery systems.
断层成像技术是可视化药物固体制剂内部结构特征的一种很有吸引力的工具。在本文中,通过药物释放过程中的同步辐射 X 射线计算机微断层扫描,对单室渗透药物传递系统(非洛地平缓释片)的片剂核心的内部结构进行了可视化。基于图像的三维重建,计算了片剂核心的表面积和三维参数。在药物释放过程的不同阶段,从二维单色 X 射线图像中可视化了片剂的表面形态、水化、溶胀和结构变化。剩余片剂核心的三维体积与非洛地平的百分比(R=0.9988)密切相关。此外,在药物释放过程中,三维表面积几乎保持不变,这清楚地表明了渗透药物传递系统的内在药物释放机制。总之,同步辐射 X 射线计算机微断层扫描具有快速采集、高强度和微尺度空间分辨率的特点,是定量阐明内在药物释放动力学和通过同步辐射获得的剩余核心的表面积等三维参数的有用工具。因此,X 射线计算机微断层扫描可以被认为是一种新的、互补的分析工具,可用于渗透药物传递系统的质量控制的标准药典药物测试。