Abstract
Regulations in the US and EU require and incentivize the development of palatable, age-appropriate medicines for children. However, the taste masking challenge of new drug actives is generally unknown, making development of palatable drug products extremely difficult. To develop palatable drug products, formulation scientists first need to determine if the drug active is bitter, has an offensive aroma (malodor) or is burning as each perception requires a different formulation approach. This retrospective compilation of results of 155 taste assessment studies reveals diversity in aversive flavor attributes of active ingredients. Bitterness was the primary taste masking challenge for 65% of the drug actives. Aversive aromas (e.g., solvent, fishy, oxidized oil) were the second most common challenge, impacting 8% of drug actives. Approximately 5% had trigeminal irritation, and a smaller subset were sour or salty (4%). None were found to be sweet. Of note, 14% of drug actives were “bland” in flavor, with no measured aversive attributes. Complicating development, most actives (>90%) were found to have multiple aversive flavor attributes. These findings highlight the need to determine the aversive attributes early in clinical development (Phase 1) to guide dosage form selection and formulation design.