Journal
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
Volume 158, Issue -, Pages 35-51Publisher
ELSEVIER
DOI: 10.1016/j.ejpb.2020.10.017
Keywords
Bitter-blocker; Taste-modifier; Excipient; Palatability
Categories
Funding
- CDT in Advanced Therapeutics and Nanomedicines - Engineering and Physical Sciences Research Council (EPSRC) [EP/L01646X]
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The palatability of an oral dosage form is crucial for patient compliance, and excipients can be used to mask the bitterness of a drug. Bitter-blockers are compounds that interact with the molecular pathway of bitterness at a taste-cell level. Some compounds, such as sodium acetate and adenosine 5 ' monophophate, have shown evidence of bitter-blocking and could provide an option for taste-masking aversive medicines.
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.
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