Desai Neel, Redfearn Andrew, MacLeod Graeme, Tuleu Catherine, Hanson Ben, Orlu Mine
Department of Pharmaceutics, School of Pharmacy, University College London, London WC1N 1AX, UK.
SPI Pharma Inc., 503 Carr Road, Wilmington, DE 19809, USA.
Pharmaceutics. 2020 Jul 9;12(7):651. doi: 10.3390/pharmaceutics12070651.
Orodispersible tablets (ODTs) offer rapid disintegration of the dosage form when placed on the tongue, which leads to fast release of the active pharmaceutical ingredient. Despite increased use in diverse patient populations, there have been numerous challenges associated with ODTs. One such concern is the lack of standardised assessment of disintegration behaviour. In the European Pharmacopoeia, 'orodispersibles' are defined as such if disintegration time is faster than 3 min. Common in vitro measurement methods only provide single time point data and have limited physiological accuracy. To determine more bio-predictive disintegration kinetics, a bench-top in vitro oral cavity model (OCM) was modified and piloted to assess disintegration of three ODTs of differing hardness. All ODTs disintegrated similarly within the OCM-surface breakdown/swelling, initial 'wash away' and final 'wash away'. The distinct advantage presented within this pilot study using the OCM is the opportunity to ascertain disintegration behaviour profiles of ODTs by evaluating changes in the observable area during simulated oral processing. The model could be implemented as a decision-support tool during the early stages of the drug design process to improve acceptability and further understand ODT disintegration behaviour.
口腔崩解片（ODTs）置于舌上时剂型能迅速崩解，从而使活性药物成分快速释放。尽管在不同患者群体中的使用日益增加，但口腔崩解片仍存在诸多挑战。其中一个问题是缺乏对崩解行为的标准化评估。在欧洲药典中，如果崩解时间快于3分钟，“口腔崩解片”即如此定义。常见的体外测量方法仅提供单个时间点的数据，且生理准确性有限。为了确定更具生物预测性的崩解动力学，对台式体外口腔模型（OCM）进行了改进和试点，以评估三种硬度不同的口腔崩解片的崩解情况。所有口腔崩解片在口腔模型表面的分解/膨胀、初始“冲蚀”和最终“冲蚀”过程中的崩解情况相似。在这项使用口腔模型的试点研究中呈现的明显优势是，有机会通过评估模拟口腔处理过程中可观察区域的变化来确定口腔崩解片的崩解行为特征。该模型可在药物设计过程的早期阶段作为决策支持工具实施，以提高可接受性并进一步了解口腔崩解片的崩解行为。
