《生命科学》 2013, 25(8): 794-802

同步辐射显微CT研究药物制剂结构的进展

杨　硕^1，2，殷宪振¹，李海燕¹，何　珺²，张继稳^1*

(1 中国科学院上海药物研究所，上海 201203；2 贵州省生化工程中心，贵阳 550025)

摘　要：摘　要：固体药物制剂的结构研究是实现优化给药的基础，也是给药系统创新的重要内容。同步辐射显微CT (synchrotron radiation X-ray microtomography，SR-μCT) 技术，不仅能够在微米、亚微米级分辨率上展示药剂粉体、微粒给药系统、片剂类固体剂型等三维静态形貌特征，而且能够连续观察缓控释制剂释药过程中的动态变化，揭示释药速率的关键结构因素，为新型给药系统的设计、质量控制提供依据和新方法。综述了同步辐射显微CT 在药物制剂结构研究方面的国内外进展。我国新近应用该技术开展了药剂粉体颗粒的表征、制剂微观结构及基于结构的释放动力学研究，在药物的晶型研究、颗粒混合及分层的评价、制剂复杂结构的分形特征、难溶性药物凝胶骨架片的水化动力学和渗透泵三维立体释放动力学研究方面取得了一系列进展。

Research progress on architecture of dosage forms using    synchrotron radiation X-ray microtomography

YANG Shuo^1，2， YIN Xian-Zhen¹， LI Hai-Yan¹， HE Jun²， ZHANG Ji-Wen^1*

(1 Shanghai Institute of Materia Medica， Chinese Academy of Sciences， Shanghai 201203， China; 2 Guizhou Province Biochemistry Engineering Centre， Guiyang 550025， China)

Abstract: Abstract: As the element of innovation for the drug delivery system， the architecture of the solid pharmaceutical dosage forms is the ground work to have an optimized drug delivery. With the high resolution of micron and submicron， the synchrotron radiation X-ray microtomography (SR-μCT) technique can show the static threedimensional morphology and the structural characteristics of the solid dosage forms， such as powders， particulate drug delivery systems and tablets. Furthermore， the SR-μCT can correlate the dynamic structure transformation of the pharmaceutical dosage forms during the drug release phase with the drug release kinetics. Therefore， it’s possible to identify the significant structural factors governing the drug release rate of the controlled/sustained release systems， which can provide new measure and novel methodologies for the design and quality control of drug delivery systems. This article reviews the advances and applications in characterization of pharmaceutical preparations. China has commenced the SR-μCT researches in structural characterization of powders， internal and microstructure of pharmaceutical preparations and structure based drug release kinetics， e.g.， the identification of crystal polymorphs， quantitative profiling of mixing and segregation of granules， fractal analysis of complicated structure， the hydration dynamic characteristics of poorly water-soluble drugs in gel forming matrix tablets and the three dimensional release kinetics of monolith osmotic pump tablets.