Journal
JOURNAL OF PHARMACY AND PHARMACOLOGY
Volume 71, Issue 9, Pages 1384-1392Publisher
OXFORD UNIV PRESS
DOI: 10.1111/jphp.13134
Keywords
amlodipine besylate; bitterness; fixed-dose combination; taste sensor; valsartan
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Funding
- Japan Society for Promotion of Science [24590226]
- Grants-in-Aid for Scientific Research [24590226] Funding Source: KAKEN
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Objectives The aim of this study was to evaluate the bitterness of amlodipine besylate (AML) combined with other five antihypertensive drugs: alacepril, benazepril, hydrochlorothiazide, telmisartan (TEL) and valsartan (VAL), which have possibility of usage as a fixed-dose combination (FDC) drugs. Methods The bitterness of individual six drugs and AML combined with each of the five drugs was evaluated using taste sensor SA402B (Intelligent Sensor Technology Inc.). AML combined with TEL or VAL was evaluated by taste sensor and human gustatory sensation tests. The interaction between AML with TEL or VAL was evaluated by H-1-NMR. Key findings The bitterness of AML was significantly decreased by addition of VAL, whereas it remained unchanged by the addition of TEL in taste sensor and human gustatory sensation test. In the H-1-NMR spectrum of AML with VAL, signal shifts of protons in AML were observed compared to that in AML alone. On the other hand, in the H-1-NMR spectrum of AML with TEL, signal shifts of protons in AML were not observed. Conclusions It was suggested that when VAL was mixed with AML, the electrostatic interactions between positive charged amino group of AML and negative charged tetrazole group of VAL were caused, and thereby led the suppression the bitterness of AML.
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