Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan, 250012, People's Republic of China.
Department of Pharmaceutical Development, Shandong Dyne Marine Biopharmaceutical Limited Corporation, 18 Fuyuan Nnalu, Rongcheng, 264300, People's Republic of China.
AAPS PharmSciTech. 2022 Feb 15;23(2):75. doi: 10.1208/s12249-022-02227-7.
Palatability is one of the most critical characteristics of oral preparations. Therefore, the exploration of new techniques to mask the aversive taste of drugs is in continuous demand. In this study, we fabricated and characterized composites based on mesoporous silica (MPS) that consisted of MPS, a bitter drug, and release regulators. We conducted a palatability evaluation to assess the taste-masking efficacy of the composites. The composites were prepared using the dry impregnation method combined with hot-melt extrusion. Morphology and components distribution in composites were characterized by scanning electron microscopy, confocal laser scanning microscopy, X-ray photoelectron spectroscopy, powder flow properties evaluation, and nitrogen-sorption measurement. The results demonstrated that drugs mainly existed in the inner pore of composites, and release regulators existed in the inner pore and covered the composites' surface. Interactions among the composite components were studied using powder X-ray diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy. The drug loaded into the composites was amorphous, and an intermolecular interaction occurred between the drug and the MPS. Taste-masked composites significantly reduced drug release levels under mouth conditions; thus, they prevented the interaction of the dissolved drug with taste receptors and improved palatability. An electronic tongue evaluation and a human taste panel assessment confirmed the better palatability of taste-masked composites. Moreover, the desired drug release behavior can be adjusted by choosing an appropriate release regulator, with stronger hydrophobicity of release regulators resulting in slower drug release. This work has provided new insights into taste-masking strategies for drugs with unpleasant tastes.
适口性是口服制剂最重要的特性之一。因此，不断需要探索新的技术来掩盖药物的不良味道。在这项研究中，我们制备并表征了基于介孔硅（MPS）的复合材料，该复合材料由 MPS、苦味药物和释放调节剂组成。我们进行了适口性评估，以评估复合材料的掩味效果。复合材料采用干浸渍法与热熔挤出法相结合制备。通过扫描电子显微镜、共聚焦激光扫描显微镜、X 射线光电子能谱、粉末流动性能评价和氮气吸附测量对复合材料的形貌和成分分布进行了表征。结果表明，药物主要存在于复合材料的内孔中，释放调节剂存在于内孔中并覆盖了复合材料的表面。通过粉末 X 射线衍射、差示扫描量热法和傅里叶变换红外光谱研究了复合材料成分之间的相互作用。负载到复合材料中的药物为无定形，药物与 MPS 之间发生了分子间相互作用。掩味复合材料在口腔条件下显著降低了药物的释放水平，从而防止了溶解药物与味觉受体的相互作用，提高了适口性。电子舌评价和人体味觉小组评估证实了掩味复合材料具有更好的适口性。此外，通过选择合适的释放调节剂可以调整所需的药物释放行为，释放调节剂的疏水性越强，药物释放越慢。这项工作为具有不良口感的药物提供了新的掩味策略。
