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  • 标题:Combination Effect of Physical and Gustatory Taste Masking for Propiverine Hydrochloride Orally Disintegrating Tablets on Palatability
  • 本地全文:下载
  • 作者:Rakan Matsui ; Shinya Uchida ; Noriyuki Namiki
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2015
  • 卷号:38
  • 期号:1
  • 页码:17-22
  • DOI:10.1248/bpb.b14-00467
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:

    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.

  • 关键词:orally disintegrating tablet (ODT); propiverine; organoleptic masking; gustatory sensation study
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