Bitterness-Masking Effects of Different Beverages on Zopiclone and Eszopiclone Tablets

Yoshida, Miyako; Kojima, Honami; Uda, Atsushi; Haraguchi, Tamami; Ozeki, Minoru; Kawasaki, Ikuo; Yamamoto, Kazuhiro; Yano, Ikuko; Hirai, Masana; Uchida, Takahiro

doi:10.1248/cpb.c18-00502

Cited by 13 publications

(12 citation statements)

References 29 publications

(29 reference statements)

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“…BEN and AMB, basic bitter drugs, are adsorbed on the negatively charged and hydrophobic part of the taste sensor membrane and cause a change in membrane potential by altering the charge density of the taste sensor output. In previous studies, we have demonstrated a taste-masking effect when a basic bitter drug is combined with an acidic compound, for example, diphenhydramine hydrochloride as basic bitter drug with chlorogenic acid as acidic compound [11] or zopiclone as basic bitter drug with citric acid as acidic compound [37]. In this study, 1 H-NMR analysis suggested an electrostatic interaction between the amino group of the basic bitter drug and the carboxyl group of the acidic compound.…”

Section: H-nmr Spectroscopic Analysis Of the Interaction Between Fosupporting

confidence: 50%

Preparation and Evaluation of Poly-γ-Glutamic Acid Hydrogel Mixtures with Basic Drugs or Acidic Drugs: Effect on Ease of Swallowing and Taste Masking

Kojima¹,

Ikegami²,

Nakamura³

et al. 2019

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The purpose of this study was to prepare a poly-γ-glutamic acid hydrogel (PGA gel), to examine its ease of swallowing using texture profile analysis (TPA) and to evaluate its taste-masking effects on basic or acidic drugs using the artificial taste sensor. Using TPA, 0.5% and 1.0% PGA gels, 0.5% and 1.0% agar and 1.0% ι-carrageenan in the absence of drug was examined the hardness, adhesiveness and cohesiveness, ranked according to permission criteria published by the Japanese Consumers Affairs Agency. 0.5% PGA gel and 1.0% agar were classified into grade II. In the taste sensor measurement, the bitterness suppressions by 0.5% PGA gel were larger than that by 1.0% agar in all drugs and the bitterness suppressions of basic drugs in 0.5% PGA gel were more potent than those of acidic drugs in 0.5% PGA gel. 1 H-nuclear magnetic resonance spectroscopic analysis was carried out to examine the difference in mechanism of bitterness suppression between basic drugs and acidic drugs mixed with PGA gel. The signals of the proton nearest to the nitrogen atom of basic drugs shifted clearly upfield, suggesting an interaction between the amino group of basic drugs and the carboxyl group of PGA gel. In conclusion, PGA gel is expected to be a useful excipient in formulations contained various drugs, especially basic drugs; it also has advantage for not only increasing ease of swallowing but also masking the bitterness of drugs even though a small amount of a single drug dose might be preferred.

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Section: H-nmr Spectroscopic Analysis Of the Interaction Between Fosupporting

confidence: 50%

Preparation and Evaluation of Poly-γ-Glutamic Acid Hydrogel Mixtures with Basic Drugs or Acidic Drugs: Effect on Ease of Swallowing and Taste Masking

Kojima¹,

Ikegami²,

Nakamura³

et al. 2019

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“…In those articles, drug ratios were set 1:0.5, 1, 2 [15] or 1:1, 2, 8. [16] Whereas the drug ratios employed for taste sensor and human gustatory sensation test (AML:VAL; 1:7.7-30.7) were differed from those employed for 1 H-NMR spectroscopic analysis, the signal shifts of specified proton in AML would be occurred under our experimental conditions in theory because the signal shifts of specified proton in AML were expected to be occurred VAL dose dependently. In the 1 H-NMR spectrum of AML with VAL (AML:VAL = 1:1, 2 or 4), the signal of AML protons 23 and 24 was shifted downfield in a dose-dependent manner.…”

Section: Discussionmentioning

confidence: 88%

“…The experimental protocol of this study (No. [14][15][16][17][18][19][20] was approved on 20 May 2014, by the ethical committee of Mukogawa Women's University.…”

Section: Human Gustatory Sensation Testmentioning

confidence: 99%

A new strategy for taste masking on bitter drug by other combined drug in fixed-dose combination: bitterness of Amlodipine besylate could be masked efficiently by Valsartan

Kojima

Nakamura

Haraguchi

et al. 2019

Journal of Pharmacy and Pharmacology

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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 1 H-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 1 H-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 1 H-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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“…It is estimated that bitter substance establishes electrostatic interactions and hydrophobic interaction with bitter taste receptor by docking simulation of bitter taste receptor with bitter substance. 34) AML which is a basic bitter drug, has an amino group which is positively charged and hydrophobic group in the structure. Electrostatic interaction and hydrophobic interaction which are formed in AML with bitter taste receptor on the mucous membrane in the oral cavity are expected to be main mechanism of bitterness caused by AML.…”

Section: H-nmr Spectroscopic Analysis Of the Interaction Between Aml mentioning

confidence: 99%

Preparation and Evaluation of Poly-γ-glutamic Acid Hydrogel Mixtures with Amlodipine Besylate: Effect on Ease of Swallowing and Taste Masking

Kojima

Haraguchi

Ikegami

et al. 2019

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of the study was to prepare a poly-γ-glutamic acid hydrogel (PGA gel), to evaluate physicochemical properties, its ease of swallowing using texture profile analysis (TPA) and its taste-masking effects on amlodipine besylate (AML) using the artificial taste sensor and human gustatory sensation testing. Using TPA, 0.5 and 1.0% (w/v) PGA gels in the absence of drug were within the range of acceptability for use in people with difficulty swallowing according to permission criteria published by the Japanese Consumers Affairs Agency. The elution of AML from prepared PGA gels was complete within an hour and the gel did not appear to influence the bioavailability of AML. The sensor output of the basic bitterness sensor AN0 in response to AML mixed with 0.5 and 1.0% PGA gels was suppressed to a significantly greater degree than AML mixed with 0.5 and 1.0% agar. In human gustatory sensation testing, 0.5 and 1.0% PGA gels containing AML showed a potent bitterness-suppressing effect. Finally, 1 H-NMR spectroscopic analysis was carried out to examine the mechanism of bitterness suppression when AML was mixed with PGA gel. The signals of the proton nearest to the nitrogen atom of AML shifted clearly upfield, suggesting an interaction between the amino group of AML and the carboxyl group of PGA gel. In conclusion, PGA gel is expected to be a useful excipient in formulations of AML, not only increasing ease of swallowing but also masking the bitterness of the basic drug.

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Bitterness-Masking Effects of Different Beverages on Zopiclone and Eszopiclone Tablets

Cited by 13 publications

References 29 publications

Preparation and Evaluation of Poly-γ-Glutamic Acid Hydrogel Mixtures with Basic Drugs or Acidic Drugs: Effect on Ease of Swallowing and Taste Masking

Preparation and Evaluation of Poly-γ-Glutamic Acid Hydrogel Mixtures with Basic Drugs or Acidic Drugs: Effect on Ease of Swallowing and Taste Masking

A new strategy for taste masking on bitter drug by other combined drug in fixed-dose combination: bitterness of Amlodipine besylate could be masked efficiently by Valsartan

Preparation and Evaluation of Poly-γ-glutamic Acid Hydrogel Mixtures with Amlodipine Besylate: Effect on Ease of Swallowing and Taste Masking

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