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[使用超临界二氧化碳制备布地奈德-聚环氧乙烷固体分散体及体外评价]

[Preparation of budesonide-poly (ethylene oxide) solid dispersions using supercritical carbon dioxide and in vitro evaluation].

作者信息

Liu Hui, Pan Wei-san, Zhou Li-li, Zhang Zhi-hong

机构信息

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.

出版信息

Yao Xue Xue Bao. 2007 Feb;42(2):206-10.

Abstract

An application of supercritical fluids technology for processing of budesonide-poly (ethylene oxide) solid dispersions was presented. The correlations of the operation parameters in the preparation process were studied. Solid dispersions of budesonide in poly (ethylene oxide) were prepared using a static method for supercritical carbon dioxide and characterized by powder X-ray diffractometry, differential scanning calorimetry, intrinsic dissolution, and in vitro dissolution. It was found that the optimum condition of solid dispersions formation was as follows: temperature, 40 degrees C ; pressure, 20 MPa; the ratio of budesonide and poly (ethylene oxide) , 1: 10. Drug existed in amorphous state in hydrophilic poly (ethylene oxide) carriers and intrinsic solubility and dissolution rates were significantly enhanced. The mechanism of the enhanced dissolution may be attributed to the amorphous character of the budesonide, improvement of the wettability of the hydrophobic budesonide, together with the formation of hydrogen bond of budesonide and hydrophilic poly (ethylene oxide). The supercritical fluids process can be used as an alternative method for preparation of solid dispersions.

摘要

介绍了超临界流体技术在布地奈德-聚环氧乙烷固体分散体加工中的应用。研究了制备过程中操作参数的相关性。采用超临界二氧化碳静态法制备了布地奈德在聚环氧乙烷中的固体分散体,并通过粉末X射线衍射、差示扫描量热法、固有溶出度和体外溶出度进行了表征。结果发现,固体分散体形成的最佳条件如下:温度40℃;压力20MPa;布地奈德与聚环氧乙烷的比例为1:10。药物以无定形状态存在于亲水性聚环氧乙烷载体中,固有溶解度和溶出速率显著提高。溶出增强的机制可能归因于布地奈德的无定形特性、疏水性布地奈德润湿性的改善以及布地奈德与亲水性聚环氧乙烷形成的氢键。超临界流体工艺可作为制备固体分散体的替代方法。

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