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

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 158; pp. 35 - 51
• Main Authors: Andrews, Danielle, Salunke, Smita, Cram, Anne, Bennett, Joanne, Ives, Robert S., Basit, Abdul W., Tuleu, Catherine
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.01.2021
• Subjects: Bitter-blocker; Excipient; Palatability; Taste-modifier; Excipient; Palatability; Bitter-blocker; Taste-modifier
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2020.10.017

[Display omitted] 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.