Bitterness evaluation of acidic pharmaceutical substances (NSAIDs) using a taste sensor.
Bitterness evaluation of acidic pharmaceutical substances (NSAIDs) using a taste sensor.
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使用味觉传感器评估酸性药物 (NSAID) 的苦味。
DOI：
10.1248/cpb.c14-00577
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发表时间：
2014
影响因子：
1.7
通讯作者：
T. Uchida
中科院分区：
文献类型：
--
作者：
Miyako Yoshida;T. Haraguchi;T. Uchida
本研究的目的是评估一种改进的苦味传感器，该传感器已被开发为允许精确和灵敏地预测酸性苦味药物活性成分的苦味，使用9种非甾体抗炎药（NSAID）作为示例。使用多通道味觉传感系统测量九种NSAID的苦味，所述味觉传感系统结合苦味传感器C 00，其具有高疏水性的膜表面，并且被开发以允许与酸性苦味物质的增强的疏水相互作用。9种NSAID的酸味强度也在味觉测试中和通过使用酸味敏感膜的味觉传感器CA 0确定。还使用膜C 00在酒石酸浓度增加的情况下测定了双氯芬酸钠和依托度酸的“吸附引起的膜电位变化”（CPA）。对使用味觉传感器和味觉测试获得的苦味强度数据进行的多元回归分析表明，C 00的CPA值可用于预测NSAID的苦味。推导出的方程为y = -0.0413 × CPA + 0.3164，其中y表示预测的苦味强度。双氯芬酸钠和依托度酸的苦味强度存在浓度依赖性变化，而酸味强度没有任何变化。对于双氯芬酸钠和依托度酸，在酒石酸浓度增加的情况下，预测和实际苦味强度之间存在良好的相关性。味觉传感器可用于预测酸性苦味药物活性成分如NSAID的苦味强度。
The objective of this study was to evaluate an improved bitterness sensor which has been developed to allow the precise and sensitive prediction of the bitterness of acidic bitter pharmaceutical active ingredients, using as examples nine non-steroidal anti-inflammatory drugs (NSAIDs). The bitterness of the nine NSAIDs was measured using a multichannel taste-sensing system incorporating a bitterness sensor, C00, which has a membrane surface with high hydrophobicity, and was developed to allow an enhanced hydrophobic interaction with acidic bitter substances. The sourness intensities of the nine NSAIDs were also determined in gustatory sensation testing and by a taste sensor using a sourness-sensitive membrane, CA0. The 'Change in membrane Potential caused by Adsorption' (CPA) of sodium diclofenac and etodolac were also determined in the presence of increasing concentrations of tartaric acid using membrane C00. Multiple regression analysis performed on the data on bitterness intensity obtained using the taste sensor and in gustatory sensation testing showed that CPA values from C00 could be used to predict the bitterness of the NSAIDs. The derived equation was y = -0.0413 × CPA + 0.3164, where y represents the predicted bitterness intensity. There were concentration-dependent changes in the bitterness intensities of diclofenac sodium and etodolac without any change in their sourness intensities. For diclofenac sodium and etodolac, there was a good correlation between predicted and actual bitterness intensities in the presence of increasing concentrations of tartaric acid. The taste sensor may be useful for predicting the bitterness intensity of acidic bitter pharmaceutical active ingredients such as NSAIDs.