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使用阳离子和阴离子系列盐类改善特定口服药物的苦味。

Modifying the bitterness of selected oral pharmaceuticals with cation and anion series of salts.

作者信息

Keast Russell S J, Breslin Paul A S

机构信息

Monell Chemical Senses Center, Philadelphia, Pennsylvania 19104, USA.

出版信息

Pharm Res. 2002 Jul;19(7):1019-26. doi: 10.1023/a:1016474607993.

Abstract

PURPOSE

NaCl has proven to be an effective bitterness inhibitor, but the reason remains unclear. The purpose of this study was to examine the influence of a variety of cations and anions on the bitterness of selected oral pharmaceuticals and bitter taste stimuli: pseudoephedrine, ranitidine, acetaminophen, quinine, and urea.

METHOD

Human psychophysical taste evaluation using a whole mouth exposure procedure was used.

RESULTS

The cations (all associated with the acetate anion) inhibited bitterness when mixed with pharmaceutical solutions to varying degrees. The sodium cation significantly (P < 0.003) inhibited bitterness of the pharmaceuticals more than the other cations. The anions (all associated with the sodium cation) also inhibited bitterness to varying degrees. With the exception of salicylate, the glutamate and adenosine monophosphate anions significantly (P < 0.001) inhibited bitterness of the pharmaceuticals more than the other anions. Also, there were several specific inhibitory interactions between ammonium, sodium and salicylate and certain pharmaceuticals.

CONCLUSIONS

We conclude that sodium was the most successful cation and glutamate and AMP were the most successful anions at inhibiting bitterness. Structure forming and breaking properties of ions, as predicted by the Hofmeister series. and other physical-chemical ion properties failed to significantly predict bitterness inhibition.

摘要

目的

氯化钠已被证明是一种有效的苦味抑制剂,但其原因尚不清楚。本研究的目的是考察多种阳离子和阴离子对所选口服药物及苦味刺激物(伪麻黄碱、雷尼替丁、对乙酰氨基酚、奎宁和尿素)苦味的影响。

方法

采用全口暴露程序进行人体心理物理味觉评估。

结果

阳离子(均与醋酸根阴离子结合)与药物溶液混合时,能不同程度地抑制苦味。钠离子对药物苦味的抑制作用显著强于其他阳离子(P < 0.003)。阴离子(均与钠离子结合)也能不同程度地抑制苦味。除水杨酸盐外,谷氨酸根和磷酸腺苷阴离子对药物苦味的抑制作用显著强于其他阴离子(P < 0.001)。此外,铵离子、钠离子和水杨酸盐与某些药物之间存在几种特定的抑制相互作用。

结论

我们得出结论,在抑制苦味方面,钠离子是最有效的阳离子,谷氨酸根和磷酸腺苷是最有效的阴离子。正如霍夫迈斯特序列所预测的,离子的结构形成和破坏特性以及其他物理化学离子特性未能显著预测苦味抑制情况。

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