Evaluation of bitterness suppression of macrolide dry syrups by jellies
Evaluation of bitterness suppression of macrolide dry syrups by jellies
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DOI：
10.1248/cpb.54.310
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发表时间：
2006-03-01
影响因子：
1.7
通讯作者：
Sunada, H
中科院分区：
文献类型：
--
作者：
Tsuji, E;Uchida, T;Sunada, H
本研究的目的是评估三种果冻对两种含有大环内酯类克拉霉素（CAM）或阿奇霉素（AZM）的干糖浆的苦味抑制作用，这三种果冻均在日本市场上作为吞咽辅助剂出售。在人体味觉测试中，干糖浆与酸性果冻混合后的苦味强度明显大于干糖浆的水悬浮液。另一方面，巧克力果冻的混合物pH值为中性，比干糖浆的水悬浮液的苦味要小。味觉传感器输出值预测的苦味强度与人类味觉测试中观察到的苦味强度具有良好的相关性。用高效液相色谱法测定干糖浆和果冻物理混合物中CAM和AZM的浓度时，酸性果冻混合物中CAM和AZM的浓度高于中性果冻混合物（CAM高约90倍，AZM高约7-10倍）。因此，苦味抑制与果冻的pH值有关。最后，用桨片法测定了含果冻和不含果冻的干糖浆的药物溶出度。溶出谱差异无统计学意义。因此，选择合适pH值的果冻是掩盖味道的关键。适当的果冻可用于提高患者的依从性，特别是儿童。味觉传感器可用于预测果冻的抑苦效果。
The purpose of this study was to evaluate the bitterness-suppressing effect of three jellies, all commercially available on the Japanese market as swallowing aids, on two dry syrups containing the macrolides clarithromycin (CAM) or azithromycin (AZM). The bitterness intensities of mixtures of the dry syrups and acidic jellies were significantly greater than those of water suspensions of the dry syrups in human gustatory sensation tests. On the other hand, the mixture with a chocolate jelly, which has a neutral pH, was less bitter than water suspensions of the dry syrups. The bitterness intensities predicted by the taste sensor output values correlated well with the observed bitterness intensities in human gustatory sensation tests. When the concentrations of CAM and AZM in solutions extracted from physical mixtures of dry syrup and jelly were determined by HPLC, concentrations in the solutions extracted from mixtures with acidic jellies were higher than those from mixtures with a neutral jelly (almost 90 times higher for CAM, and almost 7-10 times higher for AZM). Thus, bitterness suppression is correlated with the pH of the jelly. Finally, a drug dissolution test for dry syrup with and without jelly was performed using the paddle method. There was no significance difference in dissolution profile. It was concluded the appropriate choice of jelly with the right pH is essential for taste masking. Suitable jellies might be used to improve patient compliance, especially in children. The taste sensor may be used to predict the bitterness-suppressing effect of the jelly.