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药物形态对干粉吸入剂制剂雾化效率的影响。

The influence of drug morphology on aerosolisation efficiency of dry powder inhaler formulations.

作者信息

Adi Handoko, Traini Daniela, Chan Hak-Kim, Young Paul M

机构信息

Advanced Drug Delivery Group, University of Sydney, Sydney, NSW 2006, Australia.

出版信息

J Pharm Sci. 2008 Jul;97(7):2780-8. doi: 10.1002/jps.21195.

Abstract

The physicochemical properties of two forms of spray dried bovine serum albumin (BSA) have been investigated using particle sizing, surface energy measurement, atomic force microscopy (AFM) and colloid probe microscopy. The BSA powder had similar particle size distributions and surface energy but significantly different morphologies and roughness, classified as smooth and corrugated BSA. Adhesion forces between the corrugated BSA and alpha-lactose monohydrate indicated median adhesion forces were significantly less than for smooth/carrier interaction forces. These observations correlated well with aerosolisation from BSA/carrier blends, where the corrugated BSA particles gave a higher fine particle fraction than the smooth BSA, suggesting reduced BSA/carrier adhesion and increased drug liberation. The use of corrugated drug particle morphology in drug carrier DPI systems may lead to improved aerosol performance through reduced drug carrier contact area.

摘要

使用粒度分析、表面能测量、原子力显微镜(AFM)和胶体探针显微镜对两种喷雾干燥牛血清白蛋白(BSA)的物理化学性质进行了研究。BSA粉末具有相似的粒度分布和表面能,但形态和粗糙度显著不同,分为光滑型和波纹型BSA。波纹型BSA与α-乳糖一水合物之间的粘附力表明,中位粘附力明显小于光滑型/载体相互作用力。这些观察结果与BSA/载体混合物的雾化情况密切相关,其中波纹型BSA颗粒比光滑型BSA产生更高的细颗粒分数,这表明BSA/载体粘附力降低,药物释放增加。在药物载体干粉吸入剂(DPI)系统中使用波纹状药物颗粒形态可能会通过减少药物与载体的接触面积而改善雾化性能。

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