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利用基于重力的高速压缩分析方法研究各种药用辅料的力学性能。

Examining mechanical properties of various pharmaceutical excipients with the gravitation-based high-velocity compaction analysis method.

机构信息

Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, P.O. Box 56 (Viikinkaari 5E), FIN-00014, Finland.

Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, P.O. Box 56 (Viikinkaari 5E), FIN-00014, Finland.

出版信息

Int J Pharm. 2018 Mar 25;539(1-2):131-138. doi: 10.1016/j.ijpharm.2018.01.048. Epub 2018 Feb 27.

Abstract

The compression physics of powders must be considered when developing a suitable tablet formulation. In the present study, the gravitation-based high-velocity method was utilized to analyze mechanical properties of eight common pharmaceutical excipients: two grades of lactose, anhydrous glucose, anhydrous calcium hydrogen phosphate, three grades of microcrystalline cellulose and starch. Samples were compressed five times consecutively with varying pressure and speed so that Setup A produced higher pressure and longer contact time than Setup B. The important parameters obtained from samples were porosity profiles, compaction pressure, contact time, internal energy change and the amount of elastic recovery. All acquired data was only based on distance-time profile of the compression event. Lactose and glucose fragmented effectively while calcium hydrogen phosphate remained in rearrangement phase, due to its hardness and insufficient pressure applied. Microcrystalline cellulose samples showed plastic behaviour and starch was most elastic of all the samples. By utilizing the method, examined excipients could be categorized according to their compression behaviour in an accurate and cost-efficient manner.

摘要

在开发合适的片剂配方时,必须考虑粉末的压缩物理性质。在本研究中,利用基于重力的高速方法分析了八种常见药物赋形剂的机械性能:两种乳糖、无水葡萄糖、无水磷酸氢钙、三种微晶纤维素和淀粉。样品以不同的压力和速度连续压缩五次,使得设置 A 产生的压力高于设置 B,接触时间更长。从样品中获得的重要参数包括孔隙率分布、压缩压力、接触时间、内能变化和弹性恢复量。所有获得的数据仅基于压缩事件的距离-时间分布。由于硬度和施加的压力不足,乳糖和葡萄糖有效地碎裂,而磷酸氢钙仍处于重排阶段。微晶纤维素样品表现出塑性行为,而淀粉是所有样品中最有弹性的。通过利用该方法,可以以准确和经济高效的方式根据赋形剂的压缩行为对其进行分类。

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