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片剂崩解性能:压缩压力和储存条件对表面液体吸收和溶胀动力学的影响。

Tablet disintegration performance: Effect of compression pressure and storage conditions on surface liquid absorption and swelling kinetics.

机构信息

Strathclyde Institute of Pharmacy & Biomedical Sciences, University of Strathclyde, Glasgow, UK; EPSRC Centre for Continuous Manufacturing & Advanced Crystallisation, University of Strathclyde, Glasgow, UK.

Strathclyde Institute of Pharmacy & Biomedical Sciences, University of Strathclyde, Glasgow, UK.

出版信息

Int J Pharm. 2021 May 15;601:120382. doi: 10.1016/j.ijpharm.2021.120382. Epub 2021 Apr 1.

Abstract

The disintegration process of pharmaceutical tablets is a crucial step in the oral delivery of a drug. Tablet disintegration does not only refer to the break up of the interparticle bonds, but also relates to the liquid absorption and swelling behaviour of the tablet. This study demonstrates the use of the sessile drop method coupled with image processing and models to analyse the surface liquid absorption and swelling kinetics of four filler combinations (microcrystalline cellulose (MCC)/mannitol, MCC/lactose, MCC/dibasic calcium phosphate anhydrous (DCPA) and DCPA/lactose) with croscarmellose sodium as a disintegrant. Changes in the disintegration performance of these formulations were analysed by quantifying the effect of compression pressure and storage condition on characteristic liquid absorption and swelling parameters. The results indicate that the disintegration performance of the MCC/mannitol and MCC/lactose formulations are driven by the liquid absorption behaviour. For the MCC/DCPA formulation, both liquid absorption and swelling characteristics affect the disintegration time, whereas DCPA/lactose tablets is primarily controlled by swelling characteristics of the various excipients. The approach discussed in this study enables a rapid (<1 min) assessment of characteristic properties that are related to tablet disintegration to inform the design of the formulation, process settings and storage conditions.

摘要

药物片剂的崩解过程是口服给药的关键步骤。片剂崩解不仅指的是颗粒间键的断裂,还与片剂的液体吸收和溶胀行为有关。本研究采用固着液滴法结合图像处理和模型分析了四种填充剂组合(微晶纤维素(MCC)/甘露醇、MCC/乳糖、MCC/无水磷酸二钙(DCPA)和 DCPA/乳糖)与交联羧甲基纤维素钠作为崩解剂的表面液体吸收和溶胀动力学。通过定量分析压缩压力和储存条件对特征液体吸收和溶胀参数的影响,分析了这些配方的崩解性能变化。结果表明,MCC/甘露醇和 MCC/乳糖配方的崩解性能由液体吸收行为驱动。对于 MCC/DCPA 配方,液体吸收和溶胀特性都影响崩解时间,而 DCPA/乳糖片剂主要受各种赋形剂的溶胀特性控制。本研究中讨论的方法可以快速(<1 分钟)评估与片剂崩解相关的特征性质,为配方设计、工艺参数和储存条件提供信息。

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