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Amphiphilic Block Copolymers: A Novel Substance for Bitter-Masking in Aqueous Solutions.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-03-18 , DOI: 10.1021/acs.molpharmaceut.9b01296 Pan Li 1 , Yin Tian 1 , Xiu-Mei Ke 1, 2 , Qing-Chu Tan 1 , Xue Han 3 , Hong-Yan Ma 1 , Jin Pei 1 , Jun-Zhi Lin 4 , Run-Chun Xu 1 , Li Han 1 , Ming Yang 5 , Ding-Kun Zhang 1
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-03-18 , DOI: 10.1021/acs.molpharmaceut.9b01296 Pan Li 1 , Yin Tian 1 , Xiu-Mei Ke 1, 2 , Qing-Chu Tan 1 , Xue Han 3 , Hong-Yan Ma 1 , Jin Pei 1 , Jun-Zhi Lin 4 , Run-Chun Xu 1 , Li Han 1 , Ming Yang 5 , Ding-Kun Zhang 1
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It is a challenging task to suppress the bitterness of liquid preparations, especially for children. Bitter molecules are highly dispersible in liquids, leading to a strong and instant stimulation of the bitter receptors. At present, there is no effective way to correct this issue except for adding sweeteners, resulting in an unsatisfying taste. Based on the three-point contact theory, which is a universally accepted mechanism of bitterness formation, a new idea and application of amphiphilic block copolymers (ABCs) for bitterness suppression was proposed for the first time. We found that ABCs could widely inhibit the bitterness of four typical bitter substances. The mechanism is that ABCs self-assemble to form association colloids, which attract bitter components and reduce their distribution in the molecular form in solution. The bitter components were demonstrated to automatically embed in the spiral hydrophobic cavity of the hydrophobic chain of the ABCs, and their special interaction dispersed the positive electrostatic potential of bitter groups. The combination did not affect the pharmacokinetic parameters and pharmacodynamics of bitter drugs. These findings highlight the novel application of ABCs for the inhibition of bitterness and illuminate the underlying inhibition mechanisms.
中文翻译：
两亲性嵌段共聚物：一种新型的物质，用于水溶液中的苦味掩盖。
抑制液体制剂的苦味是一项艰巨的任务，特别是对于儿童而言。苦味分子在液体中高度分散，导致强烈而即时地刺激苦味受体。目前，除了添加甜味剂以外，没有有效的方法来纠正此问题，从而导致味道不理想。基于三点接触理论，这是一种公认的苦味形成机理，首次提出了两亲性嵌段共聚物（ABCs）抑制苦味的新思路和新应用。我们发现，ABC可以广泛抑制四种典型苦味物质的苦味。其机理是ABCs自组装形成缔合胶体，该胶体吸引苦味成分并减少其在溶液中的分子形式分布。已证明苦味成分自动嵌入ABCs疏水链的螺旋疏水腔中，并且它们的特殊相互作用分散了苦味基团的正静电势。该组合不影响苦药的药代动力学参数和药效学。这些发现突出了ABC在抑制苦味方面的新应用，并阐明了其潜在的抑制机制。
更新日期：2020-03-18
中文翻译：
两亲性嵌段共聚物：一种新型的物质，用于水溶液中的苦味掩盖。
抑制液体制剂的苦味是一项艰巨的任务，特别是对于儿童而言。苦味分子在液体中高度分散，导致强烈而即时地刺激苦味受体。目前，除了添加甜味剂以外，没有有效的方法来纠正此问题，从而导致味道不理想。基于三点接触理论，这是一种公认的苦味形成机理，首次提出了两亲性嵌段共聚物（ABCs）抑制苦味的新思路和新应用。我们发现，ABC可以广泛抑制四种典型苦味物质的苦味。其机理是ABCs自组装形成缔合胶体，该胶体吸引苦味成分并减少其在溶液中的分子形式分布。已证明苦味成分自动嵌入ABCs疏水链的螺旋疏水腔中，并且它们的特殊相互作用分散了苦味基团的正静电势。该组合不影响苦药的药代动力学参数和药效学。这些发现突出了ABC在抑制苦味方面的新应用，并阐明了其潜在的抑制机制。
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