State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, 27th Taiping Road, Haidian District, Beijing, 100850, China.
School of Pharmacy, Xuzhou Medical University, Xuzhou, 221000, China.
Pharm Res. 2021 May;38(5):831-842. doi: 10.1007/s11095-021-03041-9. Epub 2021 May 11.
PURPOSE: Proper taste-masking formulation design is a critical issue for instant-dissolving tablets (IDTs). The purpose of this study is to use the electronic tongue to design the additives of the 3D printed IDTs to improve palatability. METHODS: A binder jet 3D printer was used to prepare IDTs of levetiracetam. A texture analyzer and dissolution apparatus were used to predict the oral dispersion time and in vitro drug release of IDTs, respectively. The palatability of different formulations was investigated using the ASTREE electronic tongue in combination with the design of experiment and a model for masking bitter taste. Human gustatory sensation tests were conducted to further evaluate the credibility of the results. RESULTS: The 3D printed tablets exhibited rapid dispersion (<30 s) and drug release (2.5 min > 90%). The electronic tongue had an excellent ability of taste discrimination, and levetiracetam had a good linear sensing performance based on a partial least square regression analysis. The principal component analysis was used to analyze the signal intensities of different formulations and showed that 2% sucralose and 0.5% spearmint flavoring masked the bitterness well and resembled the taste of corresponding placebo. The results of human gustatory sensation test were consistent with the trend of the electronic tongue evaluation. CONCLUSIONS: Owing to its objectivity and reproducibility, this technique is suitable for the design and evaluation of palatability in 3D printed IDT development.
目的:对于即释片(IDTs)而言,正确的掩味配方设计是一个关键问题。本研究旨在使用电子舌来设计 3D 打印 IDTs 的添加剂,以改善口感。
方法:使用粘合剂喷射 3D 打印机制备左乙拉西坦的 IDTs。使用质构分析仪和溶解仪分别预测 IDTs 的口腔分散时间和体外药物释放。使用 ASTREE 电子舌结合实验设计和掩蔽苦味模型来研究不同配方的口感。进行人体味觉测试以进一步评估结果的可信度。
结果:3D 打印片剂表现出快速分散(<30s)和药物释放(2.5min>90%)。电子舌具有出色的味觉区分能力,左乙拉西坦基于偏最小二乘回归分析具有良好的线性感应性能。主成分分析用于分析不同配方的信号强度,结果表明 2%蔗糖素和 0.5%薄荷香精能够很好地掩蔽苦味,并且与相应的安慰剂的味道相似。人体味觉测试的结果与电子舌评估的趋势一致。
结论:由于其客观性和可重复性,该技术适用于 3D 打印 IDT 开发中口感的设计和评估。
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