Tsuji Eriko, Uchida Takahiro, Fukui Atsuko, Fujii Ryuta, Sunada Hisakazu
School of Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Hyogo, Japan.
Chem Pharm Bull (Tokyo). 2006 Mar;54(3):310-4. doi: 10.1248/cpb.54.310.
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.
本研究的目的是评估三种果冻对两种含大环内酯类药物克拉霉素(CAM)或阿奇霉素(AZM)的干糖浆的苦味抑制效果,这三种果冻在日本市场上均作为吞咽辅助剂销售。在人体味觉测试中,干糖浆与酸性果冻混合物的苦味强度明显高于干糖浆的水悬浮液。另一方面,与具有中性pH值的巧克力果冻混合的产品苦味低于干糖浆的水悬浮液。味觉传感器输出值预测的苦味强度与人体味觉测试中观察到的苦味强度高度相关。当通过高效液相色谱法测定从干糖浆和果冻的物理混合物中提取的溶液中CAM和AZM的浓度时,从与酸性果冻混合的产品中提取的溶液中的浓度高于与中性果冻混合的产品(CAM几乎高90倍,AZM几乎高7 - 10倍)。因此,苦味抑制与果冻的pH值相关。最后,使用桨法对有无果冻的干糖浆进行了药物溶出度试验。溶出曲线无显著差异。得出结论,选择合适pH值的果冻对于掩盖味道至关重要。合适的果冻可用于提高患者的依从性,尤其是儿童。味觉传感器可用于预测果冻的苦味抑制效果。