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苦味阻滞剂作为一种掩味策略:对其在药物制剂中效用的系统评价

Bitter-blockers as a taste masking strategy: A systematic review towards their utility in pharmaceuticals.

作者信息

Andrews Danielle, Salunke Smita, Cram Anne, Bennett Joanne, Ives Robert S, Basit Abdul W, Tuleu Catherine

机构信息

School of Pharmacy, UCL, 29 - 39 Brunswick Square, London WC1N 1AX, United Kingdom.

Pfizer Ltd., Discovery Park, Ramsgate Road, Sandwich CT13 9ND, United Kingdom.

出版信息

Eur J Pharm Biopharm. 2021 Jan;158:35-51. doi: 10.1016/j.ejpb.2020.10.017. Epub 2020 Oct 30.

Abstract

Acceptable palatability of an oral dosage form is crucial to patient compliance. Excipients can be utilised within a formulation to mask the bitterness of a drug. One such category is the bitter-blockers. This term is used inconsistently within the literature and has historically been used to describe any additive which alters the taste of an unpleasant compound. This review defines a bitter-blocker as a compound which interacts with the molecular pathway of bitterness at a taste-cell level and compiles data obtained from publication screening of such compounds. Here, a novel scoring system is created to assess their potential utility in a medicinal product using factors such as usability, safety, efficacy and quality of evidence to understand their taste-masking ability. Sodium acetate, sodium gluconate and adenosine 5'monophophate each have a good usability and safety profile and are generally regarded as safe and have shown evidence of bitter-blocking in human sensory panels. These compounds could offer a much needed option to taste-mask particularly aversive medicines where traditional methods alone are insufficient.

摘要

口服剂型可接受的适口性对患者的依从性至关重要。辅料可用于制剂中以掩盖药物的苦味。其中一类是苦味阻滞剂。该术语在文献中的使用并不一致,并且历史上一直用于描述任何改变不愉快化合物味道的添加剂。本综述将苦味阻滞剂定义为在味觉细胞水平与苦味分子途径相互作用的化合物,并汇编了从这类化合物的文献筛选中获得的数据。在此,创建了一种新颖的评分系统,以使用可用性、安全性、有效性和证据质量等因素来评估它们在药品中的潜在效用,从而了解它们的掩味能力。醋酸钠、葡萄糖酸钠和5'-单磷酸腺苷各自具有良好的可用性和安全性概况,通常被认为是安全的,并且在人体感官小组中已显示出苦味阻断的证据。这些化合物可为掩味提供急需的选择,特别是对于传统方法单独使用不足的厌恶药物。

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