Terahertz-based analysis of immediate-release tablet hydration and disintegration: Effects of croscarmellose sodium and magnesium stearate.

IF 5.3 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics Pub Date : 2025-03-22 DOI:10.1016/j.ijpharm.2025.125478
Jongmin Lee, Daniel J Goodwin, Ranjit M Dhenge, Joelle Nassar, J Axel Zeitler
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Abstract

This study investigated the influence of croscarmellose sodium (CCS) and magnesium stearate (MgSt) on tablet hardness, hydration time, and disintegration time to understand their roles and interactions at different stages of the disintegration process using terahertz pulsed imaging technique. Six powder blends were formulated by combining three CCS concentrations (3%, 4%, and 5%w/w) and two MgSt concentrations (0.5% and 1%w/w) and were direct-compressed. A high-power terahertz time-domain spectrometer with an open-immersion cell was used to track the advancing liquid front in the tablet matrix during disintegration. The obtained liquid transport profiles were analysed alongside tensile strength and disintegration time to explore how CCS and MgSt affect the tablet matrix. The results highlighted (1) the critical role of the liquid penetration process in understanding the disintegration mechanisms, and (2) the contradictory effects of CCS and MgSt, as both excipients exhibited factors that accelerated and retarded disintegration at different stages. These findings lay the groundwork for optimising immediate-release tablet formulations and developing predictive disintegration models.

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本研究利用太赫兹脉冲成像技术研究了氨甲蝶呤钠(CCS)和硬脂酸镁(MgSt)对片剂硬度、水合时间和崩解时间的影响,以了解它们在崩解过程不同阶段的作用和相互作用。将三种浓度的 CCS(3%、4% 和 5%w/w)和两种浓度的 MgSt(0.5% 和 1%w/w)混合配制成六种粉末混合物,并进行直接压缩。在崩解过程中,使用带有开放浸入池的高功率太赫兹时域光谱仪跟踪片剂基质中前进的液体前沿。获得的液体传输曲线与拉伸强度和崩解时间一起进行分析,以探索 CCS 和 MgSt 如何影响片剂基质。结果凸显了:(1)液体渗透过程在理解崩解机制中的关键作用;(2)CCS 和 MgSt 的作用相互矛盾,因为这两种辅料在不同阶段都表现出加速和延缓崩解的因素。这些发现为优化速释片剂配方和开发预测性崩解模型奠定了基础。
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来源期刊
CiteScore
10.70
自引率
8.60%
发文量
951
审稿时长
72 days
期刊介绍: The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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