Development of Palatable Amorphous Trazodone Hydrochloride Formulations via Ion Exchange

Objectives: The oral route is the most widely used method of administration. However, the bitter taste of drugs is a prevalent issue compromising patient acceptance. This study aimed to develop a palatable amorphous trazodone hydrochloride (TRA) formulation via ion exchange with Amberlite IRP88 resin as the carrier. Methods: TRA-Amberlite IRP88 complexes (TRCs) were prepared using the static exchange method and their physical properties were then characterized. Molecular docking was carried out to elucidate the molecular interaction. Finally, the dissolution profiles and taste of TRCs were evaluated. Results: The Physical characterizations confirmed that TRA was amorphously dispersed in Amberlite IRP88. Importantly, the in vivo taste masking study suggested that the bitterness of TRA was effectively masked. The reason was that the dissociation of TRCs was suppressed in the saliva, resulting in reduced dissolution in the oral cavity. Conclusion: this study suggests that amorphization is effective in masking the bitterness of drugs and provides guidance for the development of palatable oral formulations.