Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland.
Omya International AG, R&D Minerals and Surface Chemistry, Baslerstrasse 42, 4665 Oftringen, Switzerland.
Int J Pharm. 2017 Dec 20;534(1-2):50-59. doi: 10.1016/j.ijpharm.2017.10.009. Epub 2017 Oct 4.
Orally disintegrating tablets (ODT) are comfortable and safe drug delivery methods beneficial for all age groups of patients. ODTs are characterized by fast disintegration, high physical stability, taste masking and acceptable mouthfeel. In this work, the applicability of Functionalized Calcium Carbonate (FCC) to formulate ODTs with enhanced mouthfeel was elaborated and tested for acceptability on twenty healthy volunteers, using a 10-step visual analog scale Mechanical characteristics of the ODTs were examined using Heckel analysis, modified Heckel analysis and Leuenberger equation. Disintegration time was measured with the tensiometer method and analyzed for disintegration kinetics with a system of ODE. As a result, it was shown that the tablet was well accepted in healthy volunteers, disintegrated fast in vivo and correlates well with the mathematical model. Additionally, the compactibility and the physical stability were preserved yielding high porosity to absorb liquid necessary for disintegration. In vitro disintegration time was successfully linked to in vivo disintegration time. These findings lead to the conclusion that FCC is applicable to use in ODT dosage forms and mouthfeel was successfully enhanced to a pleasant result without losing the unique characteristics of FCC.
口腔崩解片（ODT）是一种舒适且安全的药物递送方式，适用于所有年龄段的患者。ODT 的特点是快速崩解、高物理稳定性、掩味和可接受的口感。在这项工作中，详细阐述了功能化碳酸钙（FCC）在改善口感方面用于制备 ODT 的适用性，并在 20 名健康志愿者中进行了可接受性测试，使用 10 步视觉模拟量表。使用 Heckel 分析、改进的 Heckel 分析和 Leuenberger 方程来检查 ODT 的机械特性。使用张力计法测量崩解时间，并使用 ODE 系统对崩解动力学进行分析。结果表明，该片剂在健康志愿者中得到了很好的接受，在体内快速崩解，并与数学模型很好地相关。此外，还保持了可压缩性和物理稳定性，产生了高孔隙率，以吸收崩解所需的液体。体外崩解时间成功地与体内崩解时间相关联。这些发现得出的结论是，FCC 可用于 ODT 剂型，口感得到了成功改善，达到了令人愉悦的效果，而不会失去 FCC 的独特特性。
