【作者】 刘辉； 潘卫三； 汤韧； 张志宏；

【Author】 LIU Hui1,PAN Wei-san2,TANG Ren1,Zhang Zhi-hong2 (1. Department of Pharmacy, Wuhan General Hospital of Guangzhou Military Command, Wuhan 430070, China; 2. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China)

【机构】 广州军区武汉总医院药剂科； 沈阳药科大学药学院；

【摘要】 目的以水难溶性药物布地奈德为模型药物,研究超临界流体技术制备布地奈德-聚氧乙烯固体分散体的方法及其影响因素。方法采用超临界流体二氧化碳(SCCO2)静态法制备布地奈德-聚氧乙烯固体分散体,用粉末X射线衍射法(PXRD)、差示扫描量热法(DSC)、溶解度法和体外溶出实验进行固体分散体的物相鉴别。结果在40℃,20MPa条件下,布地奈德-聚氧乙烯N750(1∶10)是形成固体分散体的最佳条件,布地奈德在其中主要以无定形状态存在,溶解度和累积溶出率显著提高。结论超临界流体技术是制备固体分散体的一种可行方法。更多还原

【Abstract】 Aim An application of supercritical fluids (SCF) for processing of budesonide-poly (ethylene oxide) solid dispersions was presented. The correlations of the operation parameters on the process were studied. Methods Solid dispersions of budesonide in poly (ethylene oxide) (PEO) were prepared using a static method for supercritical carbon dioxide (SC CO2) and characterized by powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), intrinsic dissolution, and in vitro dissolution. Results It was found that the optimum condition of solid dispersions formation was as follows: temperature, 40 ℃; pressure, 20 MPa; the ratio of budesonide and PEO, 1∶10. Drug existed in amorphous state in hydrophilic PEO carriers and intrinsic solubility and dissolution rates were significantly enhanced. Conclusion The SCF process can be used as an alternative method for preparation of solid dispersions.更多还原