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药物-乳糖结合方面的研究:通过改变乳糖载体表面来控制干粉吸入剂配方中的性能。

Drug-lactose binding aspects in adhesive mixtures: controlling performance in dry powder inhaler formulations by altering lactose carrier surfaces.

机构信息

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia.

出版信息

Adv Drug Deliv Rev. 2012 Mar 15;64(3):275-84. doi: 10.1016/j.addr.2011.07.002. Epub 2011 Jul 18.

Abstract

For dry powder inhaler formulations, micronized drug powders are commonly mixed with coarse lactose carriers to facilitate powder handling during the manufacturing and powder aerosol delivery during patient use. The performance of such dry powder inhaler formulations strongly depends on the balance of cohesive and adhesive forces experienced by the drug particles under stresses induced in the flow environment during aerosolization. Surface modification with appropriate additives has been proposed as a practical and efficient way to alter the inter-particulate forces, thus potentially controlling the formulation performance, and this strategy has been employed in a number of different ways with varying degrees of success. This paper reviews the main strategies and methodologies published on surface coating of lactose carriers, and considers their effectiveness and impact on the performance of dry powder inhaler formulations.

摘要

对于干粉吸入制剂,通常将微粉化药物粉末与粗乳糖载体混合,以在制造过程中便于粉末处理,并在患者使用期间促进粉末气溶胶传递。此类干粉吸入制剂的性能强烈取决于药物颗粒在气溶胶化过程中流场中所受应力诱导下所经历的内聚和粘附力之间的平衡。用适当的添加剂进行表面改性已被提议作为改变颗粒间力的实用且有效的方法,从而有可能控制制剂性能,并且已经以不同程度的成功采用了多种不同的策略。本文综述了有关乳糖载体表面涂层的主要策略和方法,并考虑了它们对干粉吸入制剂性能的有效性和影响。

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