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

Abstract

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.

The prediction of the palatability of orally disintegrating tablets by an electronic gustatory system

“…We previously showedthat we were able to quantitatively evaluate the palatability of several ODTs using the VAS in human gustatory sensation tests (Matsui et al, 2015;Nakano et 345 al., 2013;Sugiura et al, 2012).VAS is widely used for assessing the levels of pain or palatability in human subjects and is regarded as a reproducible approach that provides a good representation of subjective measurements (Carlsson, 1983;Hames et al, 2008;Wewers and Lowe, 1990). In the current study, the palatability of ODTs wasevaluated using the VAS.…”

“…The use of the human gustatory sensation test is a commonly applied method for taste assessment of pharmaceutical formulations.Previously, we have shown to beableto quantitatively evaluatepalatability of ODTsusing the visual analogue scale (VAS) (Matsui et al, 2015;Nakano et al, 2013;Sugiura 80 et al, 2012).However, it is difficult to test and evaluate the palatability of candidate ODTformulations using clinical trials, because of the high number of candidate formulations thatneeds to be investigated during the development process.Other drawbacks of the humangustatory sensation test are ethical and safety concerns due to the potential toxicity of the active pharmaceutical ingredients, especially for new chemical entities. Furthermore, 85 children have difficulties making valid statements of differences in taste perception (Sjovall et al, 1984).…”

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

“…We previously showed that the palatability of several ODTs could be quantitatively evaluated using the VAS in human gustatory sensation tests. [3][4][5]13) VAS is widely used to assess the levels of . Paired t-test with Bonferroni correction was used to detect significant differences among the orally disintegrating tablets for each test compared with C2.5-ODT.…”

“…Some studies reported that flavorings and sweeteners suppressed the bitterness and improved the palatability of ODTs. [3][4][5] Acids are widely used in many food products, beverages, and drugs to improve their taste, adjust pH, and maintain their stability. 6) Adding acids to ODTs may mask their bitterness and improve palatability because sourness has been reported to be liked by patients, particularly pediatric patients.…”

Preparation of Cocoa Powder-Containing Orally Disintegrating Tablets of Rebamipide (Rebamipide Chocolet) and Evaluation of Their Clinical Palatability

“…One of the taste-masking method involves suppressing the bitterness of a drug by modifying its organoleptic properties by adding a flavoring substance or a bitter blocker to the preparation. [11][12][13] The abovementioned method is the most convenient taste-masking method. Cocoa has been used as a flavoring agent in a variety of food and confectionery items.…”