The quantitative prediction of bitterness-suppressing effect of sweeteners on the bitterness of famotidine by sweetness-responsive sensor.

The purpose of the present study was the quantitative prediction of the bitterness-suppressing effect of sweeteners (sucrose or sugar alcohols) on the bitterness of famotidine (or quinine sulfate as control) solutions using an artificial taste sensor. Firstly, we examined the response characteristics of the sensor response to sweetness. The sensor membrane is charged negatively in the presence of sweeteners, which tend to receive protons from one of the components of the sensor membrane. The magnitude of the sensor response was shown to increase in direct proportion to the concentration of the sweetener. Secondly, we used direct or indirect methods to evaluate and predict the bitterness-suppressing effect of sweeteners on 1 mg/ml famotidine and 81.4 microM quinine sulfate solutions. In direct method, a regression between the sensor output of the sweetness-responsive sensor and the bitterness intensity obtained in human gustatory tests of famotidine solutions containing sweeteners at various concentrations, was performed. As a result, we were able to predict directly the bitterness intensity of the mixed solution. Finally, we also evaluated the bitterness intensity of the dissolution media of commercially available, orally disintegrating tablets containing famotidine by the combined usage of bitterness- and sweetness-responsive sensor. We found that the sugar alcohols in the tablet seem to be effective in the bitterness-suppression of famotidine from these tablets, especially in the initial phase (within 30 s) of the disintegration process.

[1]  H. Onishi,et al.  Development of oral acetaminophen chewable tablets with inhibited bitter taste. , 2003, International journal of pharmaceutics.

[2]  H. Onishi,et al.  Acetaminophen-containing chewable tablets with suppressed bitterness and improved oral feeling. , 2004, International journal of pharmaceutics.

[3]  T. Acree,et al.  Sweetness chemoreception theory and sweetness transduction , 2000 .

[4]  Y. Katsuragi,et al.  Lipoprotein that selectively inhibits taste nerve responses to bitter substances , 1996, Brain Research.

[5]  L. Kier A molecular theory of sweet taste. , 1972, Journal of pharmaceutical sciences.

[6]  S. Kinnamon A bitter-sweet beginning , 1996, Nature.

[7]  R. Mayr Handbook of sensory physiology, Vol.3, Part 2 , 1975 .

[8]  Hidekazu Ikezaki,et al.  Prediction of the bitterness of single, binary- and multiple-component amino acid solutions using a taste sensor. , 2002, International journal of pharmaceutics.

[9]  A. Calviño,et al.  Perception of sweetness and bitterness in different vehicles , 1993, Perception & psychophysics.

[10]  T. Indow An application of the τ scale of taste: Interaction among the four qualities of taste , 1969 .

[11]  Y. Katsuragi,et al.  Receptor mechanisms of bitter substances , 1994, Physiology & Behavior.

[12]  Y. Katsuragi,et al.  Selective Inhibition of Bitter Taste of Various Drugs by Lipoprotein , 1995, Pharmaceutical Research.

[13]  T. Acree,et al.  Molecular Theory of Sweet Taste , 1967, Nature.

[14]  A GENERAL EQUI-DISTANCE SCALE OF THE FOUR QUALITIES OF TASTE , 1966 .

[15]  K. Gannon,et al.  Transduction of bitter and sweet taste by gustducin , 1996, Nature.

[16]  David V. Smith,et al.  Neural coding of aversive and appetitive gustatory stimuli: Interactions in the hamster brain stem , 1994, Physiology & Behavior.

[17]  Kiyoshi Toko,et al.  Study of sweet taste evaluation using taste sensor with lipid/polymer membranes. , 2004, Biosensors & bioelectronics.

[18]  K. Toko,et al.  Quantification of suppression of bitterness using an electronic tongue. , 2001, Journal of pharmaceutical sciences.

[19]  Y. Katsuragi,et al.  Specific inhibitor for bitter taste: inhibition of frog taste nerve responses and human taste sensation to bitter stimuli. , 1997, Brain research. Brain research protocols.

[20]  Y. Katsuragi,et al.  Basic Studies for the Practical Use of Bitterness Inhibitors: Selective Inhibition of Bitterness by Phospholipids , 1997, Pharmaceutical Research.

[21]  P. Breslin,et al.  Bitterness Suppression with Zinc Sulfate and Na-Cyclamate: A Model of Combined Peripheral and Central Neural Approaches to Flavor Modification , 2005, Pharmaceutical Research.