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Biomedical subjects

Eriko Tsuji

Publications and source records attributed to Eriko Tsuji.

11 recordsLinked to original sources

Evaluation of bitterness suppression of macrolide dry syrups by jellies.

The purpose of this study was to evaluate the bitterness-suppressing effect of three jellies, all commercially available on the Japanese market as swallowing aids, on two dry syrups containing the macrolides clarithromycin (CAM) or azithromycin (AZM). The bitterness intensities of mixtures of the dry syrups and acidic jellies were significantly greater than those of water suspensions of the dry syrups in human gustatory sensation tests. On the other hand, the mixture with a chocolate jelly, which has a neutral pH, was less bitter than water suspensions of the dry syrups. The bitterness intensities predicted by the taste sensor output values correlated well with the observed bitterness intensities in human gustatory sensation tests. When the concentrations of CAM and AZM in solutions extracted from physical mixtures of dry syrup and jelly were determined by HPLC, concentrations in the solutions extracted from mixtures with acidic jellies were higher than those from mixtures with a neutral jelly (almost 90 times higher for CAM, and almost 7-10 times higher for AZM). Thus, bitterness suppression is correlated with the pH of the jelly. Finally, a drug dissolution test for dry syrup with and without jelly was performed using the paddle method. There was no significance difference in dissolution profile. It was concluded the appropriate choice of jelly with the right pH is essential for taste masking. Suitable jellies might be used to improve patient compliance, especially in children. The taste sensor may be used to predict the bitterness-suppressing effect of the jelly.

Adult↗

Evaluation of the taste and smell of bottled nutritive drinks.

The purpose of this study was to evaluate the palatability of 15 bottled nutritive drinks, all commercially available in the Japanese market, using data from artificial taste and odor sensors. In gustatory sensation tests, well-trained healthy volunteers were asked to score the drinks in terms of palatability and of the four basic tastes. The results suggest that overall palatability is positively correlated with sourness intensity and fruitiness (R=0.82 and 0.86, respectively) and negatively correlated with bitterness intensity and the tasting of medicinal plants (R=-0.85 and -0.80, respectively). The sourness and bitterness intensity could be predicted by taste sensor and fruitiness could be predicted by odor sensor, respectively. By performing principal component analysis of the taste sensor data, the 15 drinks could be classified into four groups. The group classified as being predominantly sour had the highest palatability score, 3.8. By principal component analysis of odor sensor data, the drinks could also be classified into four groups and this time the group with a fruity flavor (smell) showed the highest palatability score, 3.4. In the combined analysis of both taste and odor data, products containing medicinal plants showed the lowest palatability. Finally, the combined usage of the taste and odor sensors gave rise to a three-group classification. Thus, not only the taste sensor but also the odor sensor may be useful in evaluating the palatability of bottled nutritive drinks.

Beverages↗

Synthesis of 2-, 4- and 5-(2-alkylcarbamoyl-1-methylvinyl)-7-alkyloxybenzo[b]furans and their leukotriene B4 receptor antagonistic activity.

Variable benzo[b]furan derivatives having (E)- and (Z)-2-alkylcarbamoyl-1-methylvinyl groups at the 2-, 4- and 5-positions and a carboxylpropoxy or (1-phenyl)ethoxy group at the 7-position were prepared to find novel and selective leukotriene B4(LTB4) receptor antagonists. (E)-2-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (4v) showed selective inhibition to the human BLT2 receptor (hBLT2). On the other hand, (E)-2-acetyl-4-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (7v) inhibited both human BLT(1) receptor (hBLT1) and hBLT2. The (E)-2-(2-diethylcarbamoyl-1-methylvinyl) group lay on approximately the same plane as the benzo[b]furan ring, whereas the (E)-4-(2-diethylcarbamoyl-1-methylvinyl) group had the torsion angle (45.7 degree) from the benzo[b]furan ring plane. However, the (Z)-(2-alkylcarbamoyl-1-methylvinyl)benzo[b]furans were inactive. The inhibitory activity depended on the conformation of the 2-diethylcarbamoyl-1-methylvinyl group.

Benzofurans↗

Preparation of 2- and 4-(2-alkylcarbamoyl-1-methylvinyl)-7-alkyloxybenzo[b]furans having potent antagonistic activity against human leukotriene B4 BLT1 and/or BLT2 receptors.

(E)-2-Acetyl-4-(2-diethylcarbamoyl-1-methylvinyl)-7-(1-phenylethoxy)benzo[b]furan (4b) with a characteristic conformation and (E)-2-(2-morpholinocarbo-1-methylvinyl)-7-ethoxycarbopropoxybenzo[b]furan ((E)-3b) were prepared and evaluated for their leukotriene B4(LTB4) antagonistic activity. Compound 4b showed potent antagonistic activity against human BLT1 and BLT2 receptors. Compound (E)-3b displayed selective BLT2 receptor antagonistic activity. Both compounds were inactive to cysteinyl LT receptors.

Animals↗

Evaluation of bottled nutritive drinks using a taste sensor.

The purpose of this study was to evaluate the taste of 20 bottled nutritive drinks, all commercially available on the Japanese market, both in human gustatory sensation tests and using a multi-channel taste sensor. In the gustatory sensation tests, seven trained healthy volunteers were asked to score the drinks in terms of the intensities of four basic tastes (sweetness, saltiness, sourness, and bitterness), for overall palatability (ease of drinking), and for nine components of palatability (astringency, pungency, fruitiness, tasting of a medicinal plant, refreshing, irritating to the throat, seeming beneficial, good aftertaste, and the desire to drink again). The data were analysed to determine the critical factors for overall palatability. There was a positive linear correlation between overall palatability and 'sourness', 'fruitiness', 'refreshing', and 'good aftertaste' scores (r = 0.79, 0.85, 0.74, and 0.70, respectively). There was a negative correlation between overall palatability and 'bitterness intensity', 'tasting of a medicinal plant', 'seeming beneficial', and 'pungency' scores (r = -0.76, -0.64, -0.62, and -0.50, respectively). When evaluated using a multi-channel taste sensor, there was a positive linear correlation between the intensities of sourness and bitterness determined by the human volunteers and those predicted by the taste sensor (r = 0.85 and 0.71, respectively). The pungency intensity, as evidenced in gustatory sensation tests, could be also predicted by sensor output (r = 0.84). The taste sensor seems therefore to be a potentially useful tool in evaluating the palatability of bottled nutritive drinks.

Beverages↗

Syntheses of 3-acetoacetylaminobenzo[b]furan derivatives having cysteinyl leukotriene 2 receptor antagonistic activity.

Novel 3-acetoacetylaminobenzo[b]furan derivatives having a modified triene system at the 3-position were synthesized starting with 3-aminobenzo[b]furans. The enol isomers, 3-[(3-hydroxybut-2-enonyl)amino]benzo[b]furans (), of the 3-acetoacetylaminobenzo[b]furans were obtained as stable isomers owing to formation of a hydrogen bonding between the enol hydroxyl group and the amidocarbonyl group. The planarity of the C-2 substituent through the C-3 side chain suggested the existence of a modified conjugational triene system in the enol compound. Cysteinyl leukotriene 1 and 2 receptor antagonistic activities for these compounds were evaluated. 2-(4-Cyanobenzoyl or ethoxycarbonyl)-3-[(2-cyano-3-hydroxybut-2-enonyl)amino]benzo[b]furans (, ) were moderately active.

Animals↗

Quantitative taste evaluation of total enteral nutrients.

The purpose of this study was to evaluate quantitatively the taste of the various total enteral nutrients marketed in Japan using human gustatory sensation tests and an artificial taste sensor. In the human gustatory sensation test, four basic taste intensities (sweetness, saltiness, sourness, and bitterness), as well as 15 kinds of palatability scales, were evaluated according to the semantic differential (SD) method. Among 15 palatability items, the item; difficult to drink/easy to drink, was adopted as an overall palatability since it shows the highest factor loading by factor analysis. The overall palatability was found to be highly positively correlated with sweetness and sourness, but negatively correlated with bitterness and saltiness. Addition of a flavour to the amino acid-based enteral nutrient AminolebanEN significantly improved its palatability. This effect is presumably due to sour components of the flavour, such as citric acid, which reduce the bitterness intensity of branched-chain amino acids in the product. The sweetness and sourness intensities predicted by the taste sensor showed a high correlation with the results obtained in the human gustatory sensation tests. The taste sensor was able to predict the overall palatability of the total enteral nutrients with high accuracy. The products could be classified into three groups (peptide-based, amino-acid-based, and protein-based) by principal component analysis using sensor output of 8 channels. The products could be also classified into four groups; peptide-based, amino-acid-based, and protein-based and flavor addition group by principal component analysis using sensor output of channels 1, 3, 4 and 7, which are specific to basic tastes. The taste sensor could therefore be useful in predicting the taste or palatability of total enteral nutrients, and could contribute to attempts to improve compliance for such products and for enteral nutrients.

Biosensing Techniques↗

The combination effect of L-arginine and NaCl on bitterness suppression of amino acid solutions.

The purpose of the present study was to quantify the degree of suppression of the bitterness of two amino acids (L-isoleucine (L-Ile), and L-phenylalanine (L-Phe)) which could be achieved by the addition of various test chemicals, and to examine the mechanism of this bitterness suppression. The test chemicals used were two sweeteners (sucrose, aspartame), NaCl, various acidic (L-aspartic acid, L-glutamic acid), or basic (L-histidine, L-lysine and L-arginine) amino acids, tannic acid and phosphatidic acid. The combination of L-arginine (L-Arg) and NaCl together was the most effective in reducing the bitterness of 100 mM L-Ile and L-Phe solutions in human gustatory sensation tests. Even in bitterness of 0.1 mM quinine solution, L-Arg was also successful in reducing the bitterness. This bitterness-suppression effect was specific to L-Arg and not to the other basic amino acids. No comparable taste-masking effect was observed for the acidic amino acids. The artificial taste sensor failed to predict completely the bitterness-suppressing effect of L-Arg. It seems likely that the bitterness-suppressing effect of L-Arg is mediated not only by binding at the receptor site, but also elsewhere in the process of bitterness perception, such as a direct effect on the sodium channel. It is conjectured that the guanidinium group of L-Arg may interact with sodium channels in taste bud membranes.

Arginine↗

Bitterness evaluation of medicines for pediatric use by a taste sensor.

The purpose of this study was to evaluate the bitterness of 18 different antibiotic and antiviral drug formulations, widely used to treat infectious diseases in children and infants, in human gustatory sensation tests and using an artificial taste sensor. Seven of the formulations were found to have a bitterness intensity exceeding 1.0 in gustatory sensation tests (evaluated against quinine as a standard) and were therefore assumed to have an unpleasant taste to children. The bitterness intensity scores of the medicines were examined using suspensions in water or an acidic sports drink. In the case of three macrolide antibiotic formulations containing erythromycin (ERYTHROCIN dry syrup), clarithromycin (CLARITH dry syrup for pediatric), and azithromycin (ZITHROMAC fine granules for pediatric use), the bitterness intensities of suspensions in acidic sports drinks were dramatically enhanced compared with the corresponding scores of suspensions in water. This enhancement could be predicted using the taste sensor. On the other hand, a reduction of bitterness intensity was observed for an acidic sports drink suspension of an amantadine product (SYMMETREL fine granules) compared with an aqueous suspension. This reduction in bitterness could also be predicted using the taste sensor output value. Thus, the taste sensor could predict whether or not suspension in an acidic sports drink would enhance or reduce the bitterness intensity of pediatric drug formulations, compared with suspensions in water.

Amantadine↗

The bitterness intensity of clarithromycin evaluated by a taste sensor.

The purpose of this study was to evaluate the ability of a quantitative prediction method using a taste sensor to determine the bitterness of clarithromycin powder suspensions of various concentrations and of a commercial clarithromycin dry syrup product (Clarith dry syrup, Taisho Pharmaceutical Co., Ltd., Tokyo) containing aminoalkyl methacrylate polymer as a taste-masker. The bitterness of the clarithromycin dry syrup product dissolved in various beverages was also evaluated in gustatory sensation tests and using the taste sensor. In the sensor measurements, three variables were used to predict bitterness in single and multiple regression analysis: relative sensor output (R), the change of membrane potential caused by adsorption (CPA), and CPA/R ratio. The CPA values for channel 3 of the sensor predicted well the bitterness of clarithromycin powder suspensions and their filtered solutions. For Clarith dry syrup, the sensor output was small, suggesting that aminoalkyl methacrylate polymer was successful in almost complete masking of the bitter taste of the dry syrup product. When the bitterness intensities of mixtures of 1 g of Clarith dry syrup with 25 ml of water, coffee, tea, green tea, cocoa, milk, and a sports drink were examined, a good correlation was obtained between the results from human taste tests and the predicted values calculated on the basis of multiple regression analysis using CPA data from channel 4, and the CPA/R ratio from channel 3 of the taste sensor (r(2)=0.963, p<0.005). Co-administration of 1 g of Clarith dry syrup with an acidic sports drink was found to be the most bitter using either method.

Adsorption↗