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

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.

Keywords: Bitter-blocker; Excipient; Palatability; Taste-modifier.

Publication types

  • Systematic Review

MeSH terms

  • Administration, Oral
  • Drug Compounding / methods
  • Excipients / chemistry
  • Excipients / pharmacology*
  • Humans
  • Medication Adherence
  • Taste / drug effects*

Substances

  • Excipients