Determination of the Bioavailability of 3 Intranasal Formulations of Azelastine Hydrochloride in Healthy Male Volunteers.

Abstract

The primary objective of the study was to determine the bioavailability of 2 new formulations of azelastine (AZE) hydrochloride (0.10% and 0.15% AZE) containing sorbitol and sucralose compared with the commercially available 0.10% AZE. This study was performed in healthy volunteers based on the pharmacokinetic parameters maximum plasma concentration and area under the plasma concentration-time curve from time zero to the last measurable concentration. This was a Phase 1, open-label, single-center, randomized, parallel-group study. Subjects were randomized to 1 of 3 treatment groups: (1) 0.10% AZE (treatment A), (2) 0.15% AZE (treatment B) (Groups 1 and 2 both containing sorbitol and sucralose), and (3) the commercially available 0.10% AZE (treatment C). A total of 54 subjects were randomized and received treatment A, B, or C. Maximum plasma concentration and area under the plasma concentration-time curve were similar when compared in treatments A and C (0.1%) for AZE and its metabolite, desmethylazelastine. The most frequently reported adverse events were rhinorrhea (5.6%) and sneezing (5.6%).