An Electronic Tongue: Evaluation of the Masking Efficacy of Sweetening and/or Flavoring Agents on the Bitter Taste of Epinephrine

• Published in: AAPS PharmSciTech 2010-06, Vol.11 (2), p.550-557
• Main Authors: Rachid, Ousama, Simons, F. Estelle R., Rawas-Qalaji, Mutasem, Simons, Keith J.
• Format: Article
• Language: English
• Subjects: Anaphylaxis; Animals; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biomimetic Materials; Biotechnology; Conductometry - instrumentation; Drug Evaluation, Preclinical - instrumentation; Electronics - instrumentation; Epinephrine - analysis; Epinephrine - chemistry; Equipment Design; Equipment Failure Analysis; Flavoring Agents - chemistry; Humans; Pharmacology/Toxicology; Pharmacy; Reproducibility of Results; Research Article; Sensitivity and Specificity; Taste; Technology, Pharmaceutical - instrumentation; Tongue
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-010-9402-3

An epinephrine (E) tablet is under development for sublingual (SL) administration for the first-aid treatment of anaphylaxis; however, the inherent bitterness of E may hinder acceptability by patients, especially children. To assess the degree of E bitterness and to predict the masking effects of sweetening and/or flavoring non-medicinal ingredients (NMIs), the potential usefulness of an electronic tongue (e-Tongue) was evaluated. The e-Tongue sensors were conditioned, calibrated, and tested for taste discrimination. Six standard active pharmaceutical ingredients were used to build and validate a bitterness model which was then used to assess E bitartrate (EB) solutions from 0.3–9 mM. Taste-masking efficiency of aspartame (ASP), acesulfame potassium (ASK), and citric acid (CA) each at 0.5 mM was evaluated. Using EB 9 mM, the bitterness score was 20 on a scale of 20 (unacceptable) down to 1 (not detected). When NMIs 0.5 mM were added, neither ASK (17.2, unacceptable) nor was ASP (14.0, limit acceptable) effective in masking the bitter taste. When the combination of ASK and ASP was used, the bitterness score was reduced to 9.2 (acceptable). However, the addition of CA alone resulted in the best reduction of the bitterness score to 3.3 (not detected). Using the e-Tongue, the incorporation of a variety of sweetening and/or flavoring NMIs into a SL tablet of E could be shown to mask its bitter taste by up to 80%. These results should be confirmed by in vivo studies.