Uchida T, Miyanaga Y, Tanaka H, Wada K, Kurosaki S, Ohki T, Yoshida M, Matsuyama K
School of Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Japan.
Chem Pharm Bull (Tokyo). 2000 Nov;48(11):1843-5. doi: 10.1248/cpb.48.1843.
The bitterness of 11 commercial medicines was evaluated both by a multichannel taste sensor and in human gustatory sensation tests with 15 volunteers. For basic drugs with amino groups in the molecule, such as quinine, there was a comparatively strong relative response electric potential (mV) of channels 1 or 2, those containing negatively charged membranes and the bitterness determined by human gustatory sensation tests. The suppression of the bitterness of quinine by sucrose and aspartame could be quantified using the artificial taste sensor and the results concurred with those from gustatory sensation tests. The usefulness of the sensor was thus confirmed for this type of compound. Anionic drugs, such as diclofenac sodium or salicylic acid gave rise in a negative response electric potential in channels 5 or 6, those containing positively charged membrane, seemed to be useful information even though their tastes are being sour rather than bitter. For drugs with both an amino (cationic) group and carboxylic acid (anionic) group in the molecule, such as theophylline, caffeine, and metronidazole, the relative response electric potential (mV) of channels containing negatively charged membranes was not increased, even though bitterness was observed in human gustatory sensation tests. Therefore, a different design of membrane component is required for more general evaluation of the bitterness of various medicines.
通过多通道味觉传感器以及在15名志愿者参与的人体味觉测试中，对11种市售药物的苦味进行了评估。对于分子中含有氨基的碱性药物，如奎宁，通道1或2（包含带负电荷膜的通道）有相对较强的相对响应电势（mV），且人体味觉测试确定其有苦味。蔗糖和阿斯巴甜对奎宁苦味的抑制作用可以使用人工味觉传感器进行量化，结果与味觉测试结果一致。因此，证实了该传感器对这类化合物的有效性。阴离子药物，如双氯芬酸钠或水杨酸，在通道5或6（包含带正电荷膜的通道）中产生负响应电势，尽管它们尝起来是酸味而非苦味，但这似乎是有用的信息。对于分子中同时含有氨基（阳离子）基团和羧酸（阴离子）基团的药物，如茶碱、咖啡因和甲硝唑，尽管人体味觉测试中观察到有苦味，但包含带负电荷膜的通道的相对响应电势（mV）并未增加。因此，需要对膜组件进行不同设计，以更全面地评估各种药物的苦味。
