目的 通过多酚-唾液蛋白络合作用的涩味形成关键机制，建立pH调控两者结合能力的三果汤含片涩味掩蔽新方法。方法 采用荧光淬灭光谱法测定不同pH条件（2.5、3.5、4.5、5.5、6.5）下三果汤提取物与β-酪蛋白的相互作用。调节三果汤提取物pH至最佳条件，制备三果汤掩味含片。以电子舌涩味量化方法和志愿者视觉模拟量表法（visual analogue scale，VAS）评价掩味效果。采用DPPH自由基清除能力、纸片扩散法评价含片的抗氧化活性和抑菌活性。结果 荧光淬灭光谱测得三果汤提取物在pH 4.5时与β-酪蛋白的结合能力最弱，调节提取物pH至4.5制备三果汤掩味含片。掩味含片的涩度明显弱于原片；没食子酸的溶出度与原片基本一致；掩味含片的抗氧化活性和抑菌活性仅受到轻微影响。结论 基于pH调控的多酚涩味掩蔽方法可行，解决了三果汤含片涩味突出的品质缺陷，对于多酚类中药口含片的涩味掩蔽提供了可行的技术方案。

Objective To establish a new astringency masking method of Triphala Buccal Tablets (TBT, 三果汤含片) by regulating the polyphenol-salivary protein interaction through pH, which is the key mechanism of astringency. Methods Fluorescence quenching spectroscopy was used to determine the binding ability between triphala extract under different pH of 2.5, 3.5, 4.5, 5.5, 6.5 and β-casein. The pH of triphala extract was adjusted to the optimum conditions to prepare taste-masking buccal tablets. The astringent quantification methods based on electronic tongue and human visual analogue scale were used to evaluate the taste masking effect. Antioxidant activity and antibacterial activity were respectively evaluated by DPPH radical scavenging ability and kirby bauer test. Results The binding ability with β-casein was the weakest, when the pH of Triphala extract was at 4.5. The pH of Triphala extract was adjusted to 4.5 to prepare taste-masking TBT. And the astringency of the taste-masking tablets was significantly weaker than the original tablets. The dissolution of gallic acid in masked buccal tablets was basically the same as that of the original tablets. The antioxidant activity and antibacterial activity of taste-masking tablets were only slightly affected. Conclusion The above results demonstrate that the polyphenol astringency masking method based on pH regulation is feasible, and solves the quality defect of astringency of TBT. And it provides a feasible technology solution for astringency masking of polyphenol traditional Chinese medicine buccal tablets.

R283.6

国家自然科学基金资助项目(81403115);国家自然科学基金资助项目(82003955);成都医学院校基金(CYZ19-05);四川省大学生创新创业训练计划(S202013705018);成都医学院学科建设创新团队项目(CMC-XK-2104);三勒浆药业-成中医联合实验室项目(2019-YF04-00086-JH)