Laboratory of Pharmaceutical Process Analytical Technology (LPPAT), Department of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium.
Laboratory of Pharmaceutical Process Analytical Technology (LPPAT), Department of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium.
Int J Pharm. 2020 Apr 15;579:119153. doi: 10.1016/j.ijpharm.2020.119153. Epub 2020 Feb 19.
Orally disintegrating tablets (ODTs) produced by lyophilisation have a unique porous structure which leads to a favorable orodispersable functionality. They possess ultra-fast disintegration kinetics, have acceptable mechanical strength and give a smooth mouth texture. Only limited literature is available on the characterization of ODTs and even fewer on lyophilised tablets. The suitability of a broad range of characterization methods for lyophilised tablets was evaluated since they possess other mechanical properties compared to compressed tablets. Four ODTs with diverse properties were carefully selected and thoroughly analysed using various characterization techniques leading to a multitude of descriptors. The functionality of these four lyophilised tablets was examined and the relation between the different descriptors was evaluated using a Principal Component Analysis (PCA). Furthermore, μCT images of two ODTs were acquired to study the internal structure and active pharmaceutical ingredient (API) distribution inside the tablets. The important descriptors, disintegration and mechanical strength, interacted inversely indicating the importance of a well-balanced ODT formulation to achieve favorable properties. μCT data can improve the process knowledge as it yields very diverse descriptors. Ultimately, the different tablets were ranked at their performance.
冻干口腔崩解片（ODT）具有独特的多孔结构，这使其具有良好的口腔速崩性能。它们具有超快的崩解动力学特性、可接受的机械强度，并能提供光滑的口感。目前，仅有有限的文献涉及 ODT 的特性描述，而涉及冻干片剂的则更少。由于冻干片剂具有与压片不同的其他机械性能，因此需要评估广泛的特性描述方法的适用性。本研究精心选择了 4 种具有不同特性的 ODT，并使用各种特性描述方法对其进行了全面分析，得出了大量的描述符。此外，还使用 μCT 图像对其中 2 种 ODT 进行了研究，以研究片剂内部的微观结构和活性药物成分（API）分布。结果表明，重要的描述符（崩解和机械强度）呈负相关，这表明需要一个平衡良好的 ODT 配方才能实现有利的性能。μCT 数据可以提高工艺知识，因为它提供了非常多样化的描述符。最终，根据不同的片剂性能对其进行了排序。
