Masking mechanisms of bitter taste of drugs studied with ion selective electrodes

被引:30
作者
Funasaki, Noriaki [1 ]
Uratsuji, Ikumi
Okuno, Takashi
Hirota, Shun
Neya, Saburo
机构
[1] Kyoto Pharmaceut Univ, Dept Phys Chem, Yamashina Ku, Kyoto 6078414, Japan
[2] Kyoto Pharmaceut Univ, Century COE Program 21, Yamashina Ku, Kyoto 6078414, Japan
[3] Japan Sci & Technol Agcy, PRESTO, Kawaguchi, Saitama 3320012, Japan
[4] Chiba Univ, Grad Sch Pharmaceut Sci, Chiba 2638522, Japan
关键词
bitter taste; masking mechanism; ion selective electrode; cyclodextrin; polysaccharide;
D O I
10.1248/cpb.54.1155
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The masking mechanisms of the bitter taste of propantheline bromide (PB) and oxyphenonium (OB) bromide by native and modified cyclodextrins, saccharides, surfactants, organic acids, nonionic and anionic polymers, and other compounds were investigated with ion selective electrodes. The intensity of the bitter taste for a mixed solution of cyclodextrin with PB or OB was quantitatively explained from the observed electromotive force with the following assumptions: the complex and the masking agent do not have any tastes and the bitter taste is independent of other tastes. Sodium dodecyl sulfate reduced the bitter taste remarkably, and this reduction was also explicable on the basis of the same mechanism. Sodium taurodeoxycholate enhanced the bitter taste, because of its strong bitterness, although it formed 1:1 complexes with PB and OB. The masking mechanism of saccharides was ascribed to overcoming the weak bitterness of the drug by the strong sweetness. lambda-Carrageenan suppressed the bitter taste remarkably. This suppression was ascribed to the binding of PB and OB to lambda-carrageenan, the effect of the solution viscosity on the bitter taste, and the covering of the bitter taste receptor by lambda-carrageenan. It was suggested that the moderate masking by other polymers was attributable to the effect of the solution viscosity or the receptor covering. Native and modified beta-cyclodextrins, sodium dodecyl sulfate, lambda-carrageenan, Tween 20, and sodium carboxymethyl cellulose are good masking agents for the bitter tastes of PB and OB. The drug ion selective electrode is a useful tool for understanding of the masking mechanism of the bitter taste, screening of masking agents, and estimation of appropriate concentrations of the masking agents.
引用
收藏
页码:1155 / 1161
页数:7
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