小分子苦味淬灭剂应用于口服液体制剂的研究概况

张婷,张定堃,林俊芝,韩雪,姜红,许润春,马鸿雁, 谭庆刍, 杨明, 韩丽

中国药学杂志 ›› 2017, Vol. 52 ›› Issue (18) : 1569-1575.

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中国药学杂志
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中国药学杂志 ›› 2017, Vol. 52 ›› Issue (18) : 1569-1575. DOI: 10.11669/cpj.2017.18.001
综述

小分子苦味淬灭剂应用于口服液体制剂的研究概况

  • 张婷1,张定堃1*,林俊芝2,韩雪1,姜红1,许润春1,马鸿雁1, 谭庆刍1, 杨明3, 韩丽1*
作者信息 +

Summary of Small Molecular Bitter Quenchers are Applied to Oral Liquid Preparations

  • ZHANG Ting1, ZHANG Ding-kun1*, LIN Jun-zhi2, HAN Xue1, JIANG Hong1, XU Run-chun1, MA Hong-yan1, TAN Qing-chu1, YANG Ming3, HAN Li1*
Author information +
文章历史 +

摘要

口服液体制剂中苦味药物多以分子态或胶体形式存在,分散度大,能瞬时形成广泛而强烈的刺激,使得传统掩味与矫味方法难以完全掩蔽苦味,严重制约患者服用的顺应性。近年来,小分子苦味淬灭剂的发现,为改善口服液体制剂的口感提供了新的选择,逐渐成为掩味技术研究的热点。基于此,笔者阐释了小分子苦味淬灭剂的概念与特点,归纳了苦味淬灭的作用机制与影响因素,介绍了常用的小分子苦味淬灭剂及其特点和应用,以期推动小分子苦味淬灭剂在口服液体制剂中的开发应用,为口服液体制剂的苦味掩蔽提供科学的理论指导与技术支持,对于推动口服液体制剂现实问题的解决、处方设计优化与产品品质提升具有重要理论价值与实践意义。

Abstract

Bitter drugs in oral liquid preparations are mostly in the form of molecule or colloid, which can instantly form a broad and strong stimulation with the large dispersion. Therefore, it makes the traditional bitter-masking method difficult to completely mask the bitterness, and greatly restrict the compliance of patients. In recent years, the discovery of small molecular bitter quenchers (SMBQ)has provided a new choice for improving the taste of oral liquid and has gradually become a hotspot in the research of bitter-masking technology. Based on these reasons, the paper explained the concept and characteristics of SMBQ, summarized the mechanism and influencing factors of bitterness quenching, and introduced the commonly-used small bitter quench quencher and its characteristics and applications. This study was aimed to promote the development and application of SMBQ in oral liquid preparations, and provide scientific theoretical guidance and technical support for bitter masking of oral liquid preparations. It may be of great theoretical and practical significance to promote the solution of the practical problems of oral liquid, the optimization of prescription design, and the improvement of product quality.

关键词

口服液 / 抑苦 / 结构特点 / 小分子 / 苦味淬灭剂

Key words

oral liquid / bitter-masking / structural characteristic / small molecule / bitter quencher

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张婷,张定堃,林俊芝,韩雪,姜红,许润春,马鸿雁, 谭庆刍, 杨明, 韩丽. 小分子苦味淬灭剂应用于口服液体制剂的研究概况[J]. 中国药学杂志, 2017, 52(18): 1569-1575 https://doi.org/10.11669/cpj.2017.18.001
ZHANG Ting, ZHANG Ding-kun, LIN Jun-zhi, HAN Xue, JIANG Hong, XU Run-chun, MA Hong-yan, TAN Qing-chu, YANG Ming, HAN Li. Summary of Small Molecular Bitter Quenchers are Applied to Oral Liquid Preparations[J]. Chinese Pharmaceutical Journal, 2017, 52(18): 1569-1575 https://doi.org/10.11669/cpj.2017.18.001
中图分类号： R944   

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基金

国家自然科学基金资助项目(81403115);国家基础科学人才培养基金资助项目(J13100340-19)
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