アセトアミノフェン小児用ドライシロップ剤の味覚評価(苦味マスキングに関する評価 第1報)  [in Japanese] Effective Taste Evaluation of the Dry Syrup Formulations of Acetaminophen for Pediatric Use  [in Japanese]

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Abstract

アセトアミノフェン(N-(4-Hydroxyphenyl)acetamide;APAP)は, 解熱鎮痛薬として広く臨床現場に於いて使用されている. APAPはアセトアニリド及びフェナセチンの主要代謝物で, それらの解熱鎮痛効果の活性本体と考えられている. 解熱・鎮痛作用は中枢性で, その作用機序は体水分の移動と末梢血管の拡張とが相まって起こる発汗を伴う解熱及び視床と大脳皮質の痛覚閾値の上昇効果によるとされる. 解熱鎮痛作用はアスピリンと同程度であるが, 平熱時にはほとんど体温に影響を及ぼさないことが特徴である1). 近年, APAPの同効薬であるジクロフェナクナトリウム, メフェナム酸及びサリチル酸系薬剤の投与とインフルエンザ脳症・脳炎との関連性が問題視されており, 小児のインフルエンザ発熱時にこれら薬剤の投与を禁止する旨の通知が厚生労働省から発出されている2). また, 日本小児科学会より「インフルエンザに伴う発熱に対して使用するのであればAPAPが適切であり, 非ステロイド性消炎剤の使用は慎重にすべきである」という見解も公表された3).

<p>The purpose of this study was to evaluate the degrees of bitterness and sweetness of five commercially available preparations (1 granule (B) and 4 dry syrups (DS-1-DS-4)) of acetaminophen (APAP) when suspended in water by human gustatory sensation testing and drug release test. The drug release experiment was performed in distilled water as the release medium at 4, 25 and 37°. The amount of APAP released from each preparation increased with an increase in medium temperature. In the human gustatory sensation test, we evaluated the bitterness and sweetness, respectively, at two time points. First, we evaluated the tastes immediately after the suspension had been kept in the mouth for 5 seconds, which we termed "immediately taste". The second time point was 15 seconds after the suspension was ejected from the mouth but the mouth was not rinsed with water, which we referred as "residual taste".</p><p>In the gustatory sensation test, all preparations were found to be significantly masked against the bitterness, but DS-2 was not sufficiently masked against the immediate bitterness, as compared with other DS preparations. In addition, the rank order of continued sweetness tended to be DS-1≥DS-4≥DS-3>B=DS-2 in descending order. These results suggest that the masking of bitterness was probably due to the sweetness enhancement and the decreased dissolution of APAP.</p>

Journal

  • Journal of Pharmaceutical Science and Technology, Japan

    Journal of Pharmaceutical Science and Technology, Japan 68(4), 281-289, 2008-07-01

    The Academy of Pharmaceutical Science and Technology, Japan

References:  16

Cited by:  1

Codes

  • NII Article ID (NAID)
    10024592660
  • NII NACSIS-CAT ID (NCID)
    AN00266708
  • Text Lang
    JPN
  • Article Type
    Journal Article
  • ISSN
    03727629
  • Data Source
    CJP  CJPref  IR  J-STAGE 
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