Tamami Haraguchi

Bitterness prediction of H1-antihistamines and prediction of masking effects of artificial sweeteners using an electronic tongue

The study objective was to quantitatively predict a drugs bitterness and estimate bitterness masking efficiency using an electronic tongue (e-Tongue). To verify the predicted bitterness by e-Tongue, actual bitterness scores were determined by human sensory testing. In the first study, bitterness intensities of eight H(1)-antihistamines were assessed by comparing the Euclidean distances between the drug and water. The distances seemed not to represent the drugs bitterness, but to be greatly affected by acidic taste. Two sensors were ultimately selected as best suited to bitterness evaluation, and the data obtained from the two sensors depicted the actual taste map of the eight drugs. A bitterness prediction model was established with actual bitterness scores from human sensory testing. Concerning basic bitter substances, such as H(1)-antihistamines, the predictability of bitterness intensity using e-Tongue was considered to be sufficiently promising. In another study, the bitterness masking efficiency when adding an artificial sweetener was estimated using e-Tongue. Epinastine hydrochloride aqueous solutions containing different levels of acesulfame potassium and aspartame were well discriminated by e-Tongue. The bitterness masking efficiency of epinastine hydrochloride with acesulfame potassium was successfully predicted using e-Tongue by several prediction models employed in the study.

Evaluation of palatability of 10 commercial amlodipine orally disintegrating tablets by gustatory sensation testing, OD‐mate as a new disintegration apparatus and the artificial taste sensor

The purpose of this study was to evaluate and compare the palatability of 10 formulations (the original manufacturers formulation and nine generics) of amlodipine orally disintegrating tablets (ODTs) by means of human gustatory sensation testing, disintegration/dissolution testing and the evaluation of bitterness intensity using a taste sensor.

Single injection of ONO-1301-loaded PLGA microspheres directly after ischaemia reduces ischaemic damage in rats subjected to middle cerebral artery occlusion

Objectives  ONO‐1301 was developed as a novel long‐acting prostacyclin agonist with thromboxane synthase inhibitory activity. In this study, we investigated the therapeutic time window of oral ONO‐1301 and the effect of a single subcutaneous injection of ONO‐1301‐loaded poly(lactide‐co‐glycolide) (PLGA) microspheres (ONO‐1301 PLGA MS) on infarction volume, functional deficits and plasma ONO‐1301 levels following a 1 h middle cerebral artery occlusion (MCAO) in rats.

Bitterness evaluation of intact and crushed Vesicare orally disintegrating tablets using taste sensors.

Vesicare tablets, whose main component is solifenacin succinate, are known to be extremely bitter. The purpose of this study was to evaluate the effect of crushing on the bitterness of the Vesicare orally disintegrating tablets (ODTs).

Preparation of ONO-1301-loaded poly(lactide-co-glycolide) microspheres and their effect on nerve conduction velocity

Objectives  The aim of this study was to prepare poly(lactide‐co‐glycolide) (PLGA) microspheres containing ONO‐1301, a novel long‐acting prostacyclin agonist with thromboxane synthase inhibitory activity, with 10% of drug released in the initial burst and a sustained‐release period of about 3 weeks after administration. The effect of PLGA type (molecular weight and the lactide/glycolide (L/G) ratio in PLGA), the preparative conditions and the particle size on the in‐vitro release profile were examined. The effect of optimized ONO‐1301‐loaded PLGA microspheres on delayed nerve condition velocity (NCV) was investigated in streptozotocin (STZ) induced diabetic rats.

The effect of treatment with a sustained-release prostacyclin analogue (ONO-1301-loaded PLGA microsphere) on short-term memory impairment in rats with transient global cerebral ischemia

The purpose of this study was to prepare the ONO-1301 loaded poly(lactide-co-glycolide) microsphere (ONO-1301 PLGA MS) and to evaluate neuroprotective effects for short-term memory by a single subcutaneous injection of ONO-1301 PLGA MS on repeated induction of cerebral ischemia (2 × 10-min with a 1-min interval) in rat. Drug release profiles from ONO-1301 PLGA MS in vitro and in vivo were evaluated. The extent of ischemic injury was assessed behaviourally using the passive avoidance test and histopathologically by evaluating hippocampal CA1 pyramidal damage on day 42 after ischemia. Experiments in vitro showed that the release of ONO-1301 from ONO-1301 PLGA MS was sustained for approximately 3 weeks with maintenance of steady plasma levels. The neuroprotective effect was shown by treatment with ONO-1301 PLGA MS from 2 days after induction of ischemia behaviourally and histopathologically. These results suggest that ONO-1301 PLGA MS can limit short-term learning injury following global cerebral ischemia.

Ability of Food/Drink to Reduce the Bitterness Intensity of Topiramate as Determined by Taste Sensor Analysis

The purpose of this study was to determine which foods and/or drinks are capable of reducing the bitterness of topiramate when consumed together with the medicine. The inhibitory effects of foods/drinks (yoghurt and nine other foods/drinks) on the bitterness of topiramate (5 mg/mL) were evaluated with a taste sensor using a bitterness-responsive membrane (C00). The effect of topiramate on the taste characteristics of the foods/drinks themselves was also evaluated by taste sensor outputs. The viscosities of the foods/drinks and the influence of the lactic acid and orotic acid components of yoghurt, the most successful of the tested substances in taste masking, on the bitterness of topiramate were also measured. Yoghurt was predicted to be the most effective of the foods/drinks tested in reducing the acidic bitterness-responsive sensor output of topiramate. The outputs of the astringency sensor, sourness sensor, and saltiness sensor to yoghurt were not reduced by the addition of topiramate. The viscosity and lactic acid and orotic acid components of yoghurt seemed to be the keys in reducing the bitterness of topiramate. Yoghurt is predicted to be the food/drink most capable of reducing the bitterness of topiramate without losing the taste of the food/drink itself.

Evaluation of the palatabilities in 10 different famotidine orally disintegrating tablets by combination of disintegration device and taste sensor

Abstract The purpose of this study was to evaluate the palatabilities of the original and nine generic versions of famotidine orally disintegrating tablets (FODTs) by means of disintegration times and bitterness intensities determined using in combination disintegration device and taste sensor comparison of human gustatory sensation tests. The disintegration times were determined using a new disintegration testing equipment for ODTs, the OD-mate and bitterness intensities were determined using the SA501C taste-sensing system. The disintegration time and bitterness of each FODT was evaluated in gustatory sensation tests. There was a good correlation between the disintegration times of 10 FODTs estimated in human gustatory testing and those found using the OD-mate. The bitterness intensities of FODTs at 10, 20 and 30 s after starting the disintegration using the OD-mate and the values determined by the taste sensor were highly correlated with the bitterness intensities determined in gustatory sensation testing. A combination of the OD-mate and the SA501C was capable of predicting the palatabilities, disintegration properties and bitterness intensity of FODTs.

Evaluation of ebastine-loaded orally disintegrating tablets using new apparatus of detecting disintegration time and e-tongue system

The aim of this study was to predict the palatability of ebastine-loaded orally disintegrating tablets (ODTs). The disintegration time of the ODTs was measured using the OD-mate while their bitterness was measured using electronic tongue (e-tongue). Principal component analysis was carried out on the e-tongue data of the ODT solutions, and the Euclidean distances between a solution of quinine hydrochloride and each sample solution were calculated. The disintegration times determined by the OD-mate correlated well with those obtained in human sensation tests, while the Euclidean distances calculated from e-tongue analysis correlated with the bitterness scores obtained in human sensation tests. The OD-mate and the e-tongue were able to predict accurately the disintegration times and bitterness expression of ODTs, both of which are important in determining their palatability. The ability of the OD-mate and the e-tongue to predict palatability will be useful in evaluating ODTs without using human sensation tests.

Evaluation of the odour of Aminoleban® EN, taste-masked with flavoured powders, by human and electronic noses.

Aminoleban® EN is a bitter total enteral nutrient product with an unpleasant odour. The purpose of this study was to evaluate the odour of Aminoleban® EN, taste‐masked with various flavoured powders, by human testing and by using an electronic nose system (Alpha M.O.S.).