超细头孢拉定的超重力法制备及制剂研究

在传统结晶工艺的基础上，在结晶沉淀剂中加入丙酮，利用超重力法制备超细头孢拉定，对得到的产品的形貌和晶体结构分别用扫描电镜(SEM)和X射线衍射分析(XRD)进行表征，并研究了超细头孢拉定在混悬剂和注射剂两种剂型上的应用及其抑菌性能。通过SEM可以看出超细头孢拉定的粒度明显减小，粒度分布变窄，比表面积由2.95m²/g增加至10.87m²/g；由XRD图谱可以看出晶体结构没有发生变化，但药物粉体的结晶度降低。超细头孢拉定注射剂的溶解时间缩短，当助溶剂精氨酸的用量减少了29%时，依然可以在较短的时间内完全溶解；超细头孢拉定混悬剂也显示了很好的沉降效果，说明超细头孢拉定在注射剂和混悬剂两种剂型上有很好的应用前景。此外超细头孢拉定还显示了相对稳定的较强抑菌性能。

Characteristics and application of ultrafine cephradine

The paper described a novel method of crystallization for cephradine, by which ultrafine cephradine was prepared in High Gravity Reactor (HGR) on the basis of the conventional technique with acetone used as the antisolvent. The morphology　and the crystal structure of the ultrafine cephradine were　characterized by Scanning Electron Microscopy (SEM) and X-ray diffraction (XRD). The ultrafine cephradine was investigated as injection and suspension. The application performance and the bacteriostasis ability of the ultrafine cephradine were studied individually.The study indicated that after micronization, the particle size decreased, the range of particle size distribution became narrower through SEM observations, and the specific surface area was increased from 2.95m²/g to 10.87m²/g. From the XRD spectrum, no crystal structure variation of the ultrafine cefradine could be found compared with the original one, but the crystallinity of powder was reduced. The dissolution time of the ultrafine cefradine injection was shorten, and correspondingly the amount of arginine as a solutizer was reduced by 29%. Furthermore, the sedimentation experiment showed the good effect of the ultrafine cefradine suspension. This would find wide applications in ultrafine cefradine injection and suspension in future. At the same time, the strong and stable bacteriostasis ability of the ultrafine cefradine was presented.