Combination effect of physical and gustatory taste masking for propiverine hydrochloride orally disintegrating tablets on palatability

Biological & Pharmaceutical Bulletin
Rakan MatsuiNoriyuki Namiki

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 t...Continue Reading

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Citations

Jul 29, 2015·International Journal of Pharmaceutics·Hideshi NakamuraNoriyuki Namiki
Feb 24, 2017·Acta Pharmaceutica : a Quarterly Journal of Croatian Pharmaceutical Society and Slovenian Pharmaceutical Society, Dealing with All Branches of Pharmacy and Allied Sciences·Aleksandra AmelianKatarzyna Winnicka
Jan 25, 2018·Journal of the Science of Food and Agriculture·Anne S BertelsenUlla Kidmose
Jun 4, 2019·Chemical & Pharmaceutical Bulletin·Mai SotoyamaNoriyuki Namiki
Apr 7, 2017·Biological & Pharmaceutical Bulletin·Mai SotoyamaNoriyuki Namiki
Dec 4, 2020·Biological & Pharmaceutical Bulletin·Shimako TanakaNoriyuki Namiki
Nov 26, 2021·Expert Opinion on Drug Delivery·Raphael WiedeyJörg Breitkreutz

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