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安赛蜜对盐酸小檗碱的掩味效果及机制研究

Study on the taste-masking effect and mechanism of Acesulfame K on berberine hydrochloride.

作者信息

Li Haiyang, Fan Xuehua, Wu Xiangxiang, Yue Yousong, Li Chenxu, Gui Xinjing, Wang Yanli, Yao Jing, Wang Junming, Zhang Lu, Li Xuelin, Shi Junhan, Liu Ruixin

机构信息

Henan University of Chinese Medicine, Zhengzhou, China.

The First Affiliated Hospital of Henan University of Chinese Medicine, Zhengzhou, China.

出版信息

Drug Dev Ind Pharm. 2023 Jan;49(1):92-102. doi: 10.1080/03639045.2023.2183713. Epub 2023 Mar 1.

Abstract

OBJECTIVE

In our previous taste-masking study, we found that Acesulfame K (AK) had a better taste-masking effect than other high-efficiency sweeteners for several representative bitter natural drugs in aqueous decoction. Furthermore, we performed a preliminary taste-masking study of AK for representative bitter API Berberine Hydrochloride (BH) and found that it had a good taste-masking effect. We also found that flocculent precipitation was generated in the BH solution, but it was not clear whether it was related to the good taste-masking effect. This study was conducted to explore the taste-masking effect and mechanism of AK on BH.

METHODS

The taste-masking effect of AK on BH was evaluated based on the Traditional Human Taste Panel Method and the electronic tongue evaluation method. DSC, XRD, and molecular simulation techniques were used to explore the mechanism of AK on BH, from the macro level and molecular level, respectively.

RESULTS

When evaluating the taste-masking effect, we found that 0.1% AK had the best taste-masking effect on BH, while higher concentrations had a worse taste-masking effect. DSC and XRD revealed that the flocculent precipitation was a complex AK-BH. Finally, by simulating the binding of AK, BH, and TAS2R46 receptors, we found the unique taste-masking mechanism of AK.

CONCLUSION

The sweet taste stimulus of AK can mask the bitter taste stimulus of BH, and AK can generate AK-BH with BH to reduce the contact between BH and bitter taste receptors. Additionally, it could block the expression of the TAS2R46 receptors.

摘要

目的

在我们之前的掩味研究中,我们发现对于几种代表性的苦味天然药物水煎液,乙酰磺胺酸钾(AK)比其他高效甜味剂具有更好的掩味效果。此外,我们对AK针对代表性苦味原料药盐酸小檗碱(BH)进行了初步掩味研究,发现其具有良好的掩味效果。我们还发现BH溶液中产生了絮凝沉淀,但尚不清楚这是否与良好的掩味效果有关。本研究旨在探讨AK对BH的掩味效果及其机制。

方法

基于传统人体味觉小组法和电子舌评价法评估AK对BH的掩味效果。分别从宏观层面和分子层面,采用差示扫描量热法(DSC)、X射线衍射法(XRD)和分子模拟技术探讨AK对BH的作用机制。

结果

在评估掩味效果时,我们发现0.1%的AK对BH具有最佳的掩味效果,而较高浓度时掩味效果较差。DSC和XRD显示絮凝沉淀是一种AK - BH复合物。最后,通过模拟AK、BH与TAS2R46受体的结合,我们发现了AK独特的掩味机制。

结论

AK的甜味刺激可以掩盖BH的苦味刺激,并且AK可以与BH生成AK - BH,以减少BH与苦味受体的接触。此外,它还可以阻断TAS2R46受体的表达。

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