Clinical Disintegration Time of Orally Disintegrating Tablets Clinically Available in Japan in Healthy Volunteers

Yoshita, Tomohiro; Uchida, Shinya; Namiki, Noriyuki

doi:10.1248/bpb.b13-00353

Cited by 17 publications

(12 citation statements)

References 15 publications

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“…Generally, most ODTs are formulated to disintegrate within 30 s. 21) In this study, the difference regarding dissolution ratio between the in vivo and in vitro tests seemed to be minimized with the 30-s period, indicating the reasonableness of that amount of time. For statistical analysis, we calculated %MPE, %MAE, and %RMSE values.…”

Section: Discussionmentioning

confidence: 58%

“…In a previous study that conducted human gustatory sensation tests using amlodipine ODTs, differences between the presence and absence of ethyl cellulose coating used for bitterness masking were noted. 20) In that study, ODTs were manufactured with the same ingredients and method as in the present investigation, then a visual analog scale (VAS) was utilized for evaluation, with a larger VAS value considered to indicate better palatability. Their results confirmed that ODTs with coated amlodipine besylate had a higher level of palatability as compared to non-coated ODTs.…”

Section: Discussionmentioning

confidence: 99%

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In Vivo Drug Dissolution in Human Oral Cavity from Orally Disintegrating Tablet and Comparability with in Vitro Testing

Katayama

Uchida

Kamiya

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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We examined the amlodipine dissolution from orally disintegrating tablets (ODTs) in vivo in the human oral cavity. Additionally, 5 different in vitro short dissolution test methods (Tricorptester, magnetic stirrer, rotating injection syringe, paddle apparatus, shaking) were used to evaluate dissolution and the results were compared to those obtained with the human volunteers. Various amlodipine ODTs with different levels of physical masking effectiveness were manufactured using the RACTAB ® technique. Quantitative findings showed that amlodipine dissolution from ODT was dependent on time in the oral cavity and the amount of coating applied for physical masking. We also found that dissolution in the oral cavity was best correlated to that in in vitro short dissolution tests with a time period of 30 s. For more detailed evaluations, mean prediction error, mean absolute error, and root mean square error values were calculated, each of which was lowest with the Tricorptester method among all of the investigated test methods. Our results indicate that mimicking of the inside of the human oral cavity is accurate with a testing time of 30 s, while the Tricorptester method was the most preferable of all in vitro tests investigated in this study.

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Section: Discussionmentioning

confidence: 58%

Section: Discussionmentioning

confidence: 99%

In Vivo Drug Dissolution in Human Oral Cavity from Orally Disintegrating Tablet and Comparability with in Vitro Testing

Katayama

Uchida

Kamiya

et al. 2018

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…12) Artificial saliva (NaCl, 1.44 g/L; KCl, 1.47 g/L; Tween 80, 0.3%) warmed to 37°C was used as the test solution, and was dripped from a height of 80 mm at a flow rate of 6.0 mL/min. Five tablets of each type of ODTs were evaluated and the mean disintegration time was calculated.…”

Section: Methodsmentioning

confidence: 99%

Citric Acid Suppresses the Bitter Taste of Olopatadine Hydrochloride Orally Disintegrating Tablets

Sotoyama

Uchida

Tanaka

et al. 2017

Biological & Pharmaceutical Bulletin

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Orally disintegrating tablets (ODTs) are formulated to disintegrate upon contact with saliva, allowing administration without water. Olopatadine hydrochloride, a second-generation antihistamine, is widely used for treating allergic rhinitis. However, it has a bitter taste; therefore, the development of taste-masked olopatadine ODTs is essential. Some studies have suggested that citric acid could suppress the bitterness of drugs. However, these experiments were performed using solutions, and the taste-masking effect of citric acid on ODTs has not been evaluated using human gustatory sensation tests. Thus, this study evaluated citric acid's taste-masking effect on olopatadine ODTs. Six types of olopatadine ODTs containing 0-10% citric acid were prepared and subjected to gustatory sensation tests that were scored using the visual analog scale. The bitterness and overall palatability of olopatadine ODTs during disintegration in the mouth and after spitting out were evaluated in 11 healthy volunteers (age: 22.8 2.2 years). The hardness of the ODTs was >50 N. Disintegration time and dissolution did not differ among the different ODTs. The results of the gustatory sensation tests suggest that citric acid could suppress the bitterness of olopatadine ODTs in a dose-dependent manner. Olopatadine ODTs with a high content of citric acid (5-10%) showed poorer overall palatability than that of those without citric acid despite the bitterness suppression. ODTs containing 2.5% citric acid, yogurt flavoring, and aspartame were the most suitable formulations since they showed low bitterness and good overall palatability. Thus, citric acid is an effective bitterness-masking option for ODTs.

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“…18) Artificial saliva (NaCl, 1.44 g/L; KCl, 1.47 g/L; Tween 80, 0.3%) warmed to 37°C was used as the test solution, and dripped from a height of 80 mm at a flow rate of 6.0 mL/min. This measurement was conducted on 10 tablets of each type of ODT and the mean disintegration time was measured.…”

Section: S-od(−) M-od(−) and L-od(−)) Odts With Organoleptic Maskimentioning

confidence: 99%

Combination Effect of Physical and Gustatory Taste Masking for Propiverine Hydrochloride Orally Disintegrating Tablets on Palatability

2015

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Orally disintegrating tablets (ODTs) containing propiverine hydrochloride (which is extremely bitter and leaves a feeling of numbness in the mouth) were prepared with a combined use of physical and organoleptic taste masking. Propiverine-loaded masking particles (PLMPs) were prepared with different amounts of gastric-soluble coatings as physical masking. ODTs without organoleptic masking were prepared by mixing each group of PLMPs with Ludiflash ® , crospovidone, and magnesium stearate. ODTs with organoleptic masking were also prepared by addition of L-menthol, aspartame, thaumatin, and cinnamon. Fifteen-minute dissolution of propiverine in solutions with pH 1.2 was ≥85% for all ODTs, whereas that in pH 6.8 solutions was ≤85% and increased with physical masking. A single blind randomized crossover trial was conducted. Ten healthy volunteers were asked to quantify the bitterness, numbness, and overall palatability using a 100-mm visual analog scale (VAS) at the period of disintegration as well as 1 and 5 min later. VAS scores of bitterness, numbness, and overall palatability improved along with increasing amounts of physical masking, and the effects persisted for 5 min. VAS scores for numbness increased over time regardless of the amount of physical masking. Bitterness, numbness, and overall palatability were significantly improved by organoleptic masking if the amount of physical masking was small. Combined use of physical and organoleptic masking is useful for improving palatability of ODTs containing propiverine.

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Clinical Disintegration Time of Orally Disintegrating Tablets Clinically Available in Japan in Healthy Volunteers

Cited by 17 publications

References 15 publications

<i>In Vivo</i> Drug Dissolution in Human Oral Cavity from Orally Disintegrating Tablet and Comparability with <i>in Vitro</i> Testing

<i>In Vivo</i> Drug Dissolution in Human Oral Cavity from Orally Disintegrating Tablet and Comparability with <i>in Vitro</i> Testing

Citric Acid Suppresses the Bitter Taste of Olopatadine Hydrochloride Orally Disintegrating Tablets

Combination Effect of Physical and Gustatory Taste Masking for Propiverine Hydrochloride Orally Disintegrating Tablets on Palatability

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