Suppression in Bitterness Intensity of Bitter Basic Drug by Chlorogenic Acid.
The purpose of the study was to evaluate suppression of the bitterness intensity of bitter basic drugs by chlorogenic acid (CGA) using the artificial taste sensor and human gustatory sensation testing and to investigate the mechanism underlying bitterness suppression using1H-NMR. Diphenhydramine hydrocholoride (DPH) was the bitter basic drug used in the study. Quinic acid (QNA) and caffeic acid (CFA) together form CGA. Although all three acids suppressed the bitterness intensity of DPH in a dose-dependent manner as determined by the taste sensor and in gustatory sensation tests, CFA was less effective than either CGA or QNA. Data from1H-NMR spectroscopic analysis of mixtures of the three acids with DPH suggest that the carboxyl group, which is present in both QNA and CGA but not CFA, interact with the amine group of DPH. This study showed that the bitterness intensity of DPH was suppressed by QNA and CGA through a direct electrostatic interaction with DPH as confirmed in1H-NMR spectroscopic analysis. CGA and QNA may therefore be useful bitterness-masking agents for the basic drug DPH.
School of Pharmaceutical Sciences, Mukogawa Women's University.
Sayuko
S
Shiraishi
Tamami
T
Haraguchi
Saki
S
Nakamura
Honami
H
Kojima
Ikuo
I
Kawasaki
Miyako
M
Yoshida
Takahiro
T
Uchida
D000328:Adult; D002109:Caffeic Acids / Q000494:pharmacology; D002726:Chlorogenic Acid / Q000737:chemistry / Q000494:pharmacology*; D004155:Diphenhydramine / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D005260:Female; D006801:Humans; D066244:Proton Magnetic Resonance Spectroscopy; D011801:Quinic Acid / Q000494:pharmacology; D013649:Taste / Q000187:drug effects*; D055697:Taste Perception / Q000187:drug effects*; D055815:Young Adult
D002109:Caffeic Acids; D011801:Quinic Acid; D002726:Chlorogenic Acid; D004155:Diphenhydramine; C040048:caffeic acid