Zhang Xingwang, Wu Danni, Lai Jie, Lu Yi, Yin Zongning, Wu Wei
School of Pharmacy, Fudan University, Shanghai, China.
J Pharm Sci. 2009 Feb;98(2):665-75. doi: 10.1002/jps.21453.
This work was aimed at investigating the feasibility of fluid-bed coating as a new method to prepare cyclodextrin inclusion complex. The inclusion complex of the model drug piroxicam (PIX) and 2-hydroxypropyl-beta-cyclodextrin (HPCD) in aqueous ethanol solution was sprayed and deposited onto the surface of the pellet substrate upon removal of the solvent. The coating process was fluent with high coating efficiency. Scanning electron microscopy revealed a coarse pellet surface, and a loosely packed coating structure. Significantly enhanced dissolution, over 90% at 5 min, was observed at stoichiometric PIX/HPCD molar ratio (1/1) and at a ratio with excessive HPCD (1/2). Differential scanning calorimetry and powder X-ray diffractometry confirmed absence of crystallinity of PIX at PIX/HPCD molar ratio of 1/1 and 1/2. Fourier transform-infrared spectrometry and Raman spectrometry revealed interaction between PIX and HPCD adding evidence on inclusion of PIX moieties into HPCD cavities. Solid-state (13)C NMR spectrometry indicated possible inclusion of PIX through the pyridine ring. It is concluded that fluid-bed coating has potential to be used as a new technique to prepare cyclodextrin inclusion complex.
本研究旨在探讨流化床包衣作为制备环糊精包合物新方法的可行性。将模型药物吡罗昔康（PIX）与2-羟丙基-β-环糊精（HPCD）在乙醇水溶液中的包合物喷雾并在去除溶剂后沉积在微丸基质表面。包衣过程流畅，包衣效率高。扫描电子显微镜显示微丸表面粗糙，包衣结构疏松。在化学计量比的PIX/HPCD摩尔比（1/1）和过量HPCD的比例（1/2）下，观察到显著增强的溶出度，在5分钟时超过90%。差示扫描量热法和粉末X射线衍射法证实在PIX/HPCD摩尔比为1/1和1/2时PIX无结晶性。傅里叶变换红外光谱法和拉曼光谱法揭示了PIX与HPCD之间的相互作用，为PIX部分包合到HPCD空腔中提供了证据。固态（13）C核磁共振光谱表明PIX可能通过吡啶环被包合。结论是流化床包衣有潜力作为制备环糊精包合物的新技术。
