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研究基于淀粉的药用辅料的水蒸气吸附机制。

Investigation of water vapour sorption mechanism of starch-based pharmaceutical excipients.

机构信息

Pharmaceutics Research Laboratory, Arundel Building, School of Life Sciences, University of Sussex, BN1 9QJ, Brighton, UK.

Colorcon Inc., Global Headquarters, 275 Ruth Road, Harleysville, PA, 19438, USA.

出版信息

Carbohydr Polym. 2020 Jun 15;238:116208. doi: 10.1016/j.carbpol.2020.116208. Epub 2020 Mar 23.

Abstract

Starch-based excipients are commonly used in oral solid dosage forms. The effect of particle size and pregelatinisation level of starch-based excipients on their water absorption behaviour have been evaluated. The results showed that starch-based excipients have type ii isotherms, indicating that the principal mechanism of sorption is the formation of monolayer coverage and multilayer water molecules (10-80 RH %). It was found that the particle size of starch-based excipients did not have any influence on the rate of water sorption, whereas the level of pregelatinisation changed the kinetics of water sorption-desorption. Results showed that the higher the degree of pregelatinisation, the higher the rate of water absorption, which is irrespective of particle size. SEM images showed that a partially gelatinised starch had a firm granular structure with small pores and channels on the surface while a fully gelatinised starch had more irregular and spongy like surface with a degree of fractured particles.

摘要

淀粉类赋形剂常用于口服固体制剂。本文评价了淀粉类赋形剂的粒径和预胶化度对其吸水性的影响。结果表明,淀粉类赋形剂具有 II 型等温线,表明吸附的主要机制是形成单层覆盖和多层水分子(10-80 RH%)。研究发现,淀粉类赋形剂的粒径对吸水速率没有影响,而预胶化度改变了水的吸附-解吸动力学。结果表明,预胶化度越高,吸水率越高,这与粒径无关。SEM 图像显示,部分预胶化淀粉具有坚实的颗粒状结构,表面有小孔和通道,而完全预胶化淀粉具有更不规则和海绵状的表面,颗粒有一定程度的断裂。

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