Shiraishi Sayuko, Haraguchi Tamami, Nakamura Saki, Li Dahong, Kojima Honami, Yoshida Miyako, Uchida Takahiro
Faculty of Pharmaceutical Science, Mukogawa Women's University.
Chem Pharm Bull (Tokyo). 2017;65(2):127-133. doi: 10.1248/cpb.c16-00621.
The purpose of this study was to evaluate the taste-masking effects of chlorogenic acid (CGA) on bitter drugs using taste sensor measurements and surface plasmon resonance (SPR) analysis of CGA-drug interactions. Six different bitter drugs were used: amlodipine besylate (AMD), diphenhydramine hydrochloride (DPH), donepezil hydrochloride (DNP), rebamipide (RBM), diclofenac sodium (DCF) and etodolac (ETD). Taste sensor outputs were significantly inhibited by the addition of CGA to all drugs. The inhibition ratio of the taste sensor output decreased in the following order DPH>DNP>AMD≈DCF≈RBM≈ETD. The association rate constant (k) for the interaction between drugs and CGA as evaluated by SPR measurement also decreased in the following order DPH>DNP>AMD>DCF≈ETD≈RBM. It was suggested that basic drugs (AMD, DNP, DPH) associate more easily with CGA than acidic drugs (DCF, RBM, ETD). The inhibition ratios (%) of the taste sensor output of bitter drugs caused by CGA and the association rate constants (k) between the drugs and CGA were significantly correlated (r=0.886, p<0.05, Spearman's correlation test). Our findings suggest that the taste-masking effects of CGA are due to its direct association with the drugs. CGA may therefore be a useful taste-masking agent for basic drugs.
本研究的目的是利用味觉传感器测量以及绿原酸（CGA）与药物相互作用的表面等离子体共振（SPR）分析，评估绿原酸对苦味药物的掩味效果。使用了六种不同的苦味药物：苯磺酸氨氯地平（AMD）、盐酸苯海拉明（DPH）、盐酸多奈哌齐（DNP）、瑞巴派特（RBM）、双氯芬酸钠（DCF）和依托度酸（ETD）。向所有药物中添加CGA后，味觉传感器输出均受到显著抑制。味觉传感器输出的抑制率按以下顺序降低：DPH>DNP>AMD≈DCF≈RBM≈ETD。通过SPR测量评估的药物与CGA之间相互作用的缔合速率常数（k）也按以下顺序降低：DPH>DNP>AMD>DCF≈ETD≈RBM。结果表明，碱性药物（AMD、DNP、DPH）比酸性药物（DCF、RBM、ETD）更容易与CGA缔合。CGA引起的苦味药物味觉传感器输出抑制率（%）与药物和CGA之间的缔合速率常数（k）显著相关（r = 0.886，p<0.05，Spearman相关检验）。我们的研究结果表明，CGA的掩味效果归因于其与药物的直接缔合。因此，CGA可能是一种用于碱性药物的有用掩味剂。
