title: The quantitative prediction of bitterness-suppressing effect of sweeteners on the bitterness of famotidine by sweetness-responsive sensor.
abstract: 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.
authors.affiliation: Astellas Pharma Inc., Information System Management Department, 3-17-1 Hasune, Tokyo 174-8612, Japan.
authors.forename: Yoshimi
authors.initials: Y
authors.lastname: Hashimoto
authors.forename: Chiharu
authors.initials: C
authors.lastname: Matsunaga
authors.forename: Emi
authors.initials: E
authors.lastname: Tokuyama
authors.forename: Eriko
authors.initials: E
authors.lastname: Tsuji
authors.forename: Takahiro
authors.initials: T
authors.lastname: Uchida
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Okada
mesh_terms: D000328:Adult; D015374:Biosensing Techniques; D002851:Chromatography, High Pressure Liquid; D015738:Famotidine / Q000494:pharmacology*; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D006801:Humans; D011237:Predictive Value of Tests; D011803:Quinine / Q000494:pharmacology; D013395:Sucrose / Q000494:pharmacology; D013402:Sugar Alcohols / Q000494:pharmacology; D013549:Sweetening Agents / Q000737:chemistry / Q000494:pharmacology*; D013607:Tablets; D013649:Taste / Q000187:drug effects*
chemical_list: D006635:Histamine H2 Antagonists; D013402:Sugar Alcohols; D013549:Sweetening Agents; D013607:Tablets; D013395:Sucrose; D015738:Famotidine; D011803:Quinine