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Using milk fat to reduce the irritation and bitter taste of ibuprofen.
Chemosensory Perception ( IF 1 ) Pub Date : 2012-05-01 , DOI: 10.1007/s12078-012-9128-6
Samantha M Bennett 1 , Lisa Zhou , John E Hayes
Affiliation  

Bitterness and irritation elicited by pharmaceutically active molecules remain problematic for pediatric medications, fortified foods, and dietary supplements. Few effective methods exist for reducing these unpalatable sensations, negatively impacting medication compliance and intake of beneficial phytonutrients. A physicochemical approach to masking these sensations may be the most successful approach for generalizability to a wide range of structurally and functionally unique compounds. Here, solutions of the nonsteroidal anti-inflammatory drug, ibuprofen, were prepared in milk products with varying fat content. Our hypothesis, based on other reports of similar phenomena, was that increasing the fat content would cause ibuprofen to selectively partition into the fat phase, thereby reducing interaction with sensory receptors and decreasing adversive sensations. Quantification of the aqueous concentration of ibuprofen was performed using an isocratic high-performance liquid chromatography (HPLC) method coupled with an external standard curve. Sensory testing showed a modest but significant decrease (~20 %) in irritation ratings between the skim milk (0 % fat) and the half-and-half (11 % fat) samples, indicating that increased fat may contribute to a reduced sensory response. Bitterness was not reduced, remaining constant over all fat levels. The HPLC results indicate a constant amount of ibuprofen remained in the aqueous phase regardless of fat level, so a simple partitioning hypothesis cannot explain the reduced irritancy ratings. Association of ionized ibuprofen with continuous phase solutes, such as unabsorbed protein, should be explored in future work.

中文翻译:

使用乳脂肪减少布洛芬的刺激性和苦味。

药物活性分子引起的苦味和刺激对于儿科药物、强化食品和膳食补充剂来说仍然是个问题。几乎没有有效的方法可以减少这些令人不快的感觉,从而对药物依从性和有益植物营养素的摄入产生负面影响。掩饰这些感觉的物理化学方法可能是对广泛的结构和功能独特的化合物进行泛化的最成功的方法。在这里,非甾体抗炎药布洛芬的溶液在不同脂肪含量的奶制品中制备。我们的假设是基于其他类似现象的报告,增加脂肪含量会导致布洛芬选择性地进入脂肪相,从而减少与感觉受体的相互作用并减少不良感觉。使用等度高效液相色谱 (HPLC) 方法结合外部标准曲线对布洛芬的水溶液浓度进行定量。感官测试表明,脱脂牛奶(0% 脂肪)和半个半(11% 脂肪)样品的刺激等级适度但显着降低(~20%),表明增加的脂肪可能导致感官反应降低. 苦味没有减少,在所有脂肪水平上保持不变。HPLC 结果表明,无论脂肪含量如何,水相中都会保留恒定量的布洛芬,因此简单的分配假设无法解释刺激性等级的降低。离子化布洛芬与连续相溶质的结合,
更新日期:2012-05-01
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