Yonemochi E, Kitahara S, Maeda S, Yamamura S, Oguchi T, Yamamoto K
Faculty of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho Inage-ku, Chiba 263-8522, Japan.
Eur J Pharm Sci. 1999 Mar;7(4):331-8. doi: 10.1016/s0928-0987(98)00040-2.
In order to characterize the amorphous clarithromycin (CAM) obtained by grinding and spray drying, physicochemical properties (crystallinity, thermal behavior, stability and solubility parameters) were evaluated. From powder X-ray diffraction, it was estimated that the crystalline state of CAM was changed into an amorphous state by grinding and spray drying. In differential scanning calorimetry measurements, both broad and sharp peaks for crystallization were observed in ground samples, whereas spray dried samples showed one broad peak due to crystallization. As to the stability test under high humidity, structural difference was confirmed between ground CAMs and spray dried CAM. The heat of dissolution of ground CAMs was greater than that of intact CAM. In the solubility parameter measurement, the increase of the special term, deltas, indicated that the energy change was due to the polarity of the surface energy of the powder particles by grinding.
为了表征通过研磨和喷雾干燥获得的无定形克拉霉素（CAM），对其物理化学性质（结晶度、热行为、稳定性和溶解度参数）进行了评估。通过粉末X射线衍射估计，CAM的结晶态通过研磨和喷雾干燥转变为无定形态。在差示扫描量热法测量中，研磨样品中观察到了结晶的宽峰和尖峰，而喷雾干燥样品由于结晶显示出一个宽峰。至于在高湿度下的稳定性测试，研磨的CAM和喷雾干燥的CAM之间证实了结构差异。研磨的CAM的溶解热大于完整CAM的溶解热。在溶解度参数测量中，特殊项δs的增加表明能量变化是由于研磨导致粉末颗粒表面能的极性变化。
