Pharmacokinetic characteristics and safety and tolerability of a reformulated azelastine hydrochloride nasal spray in patients with chronic rhinitis.

BACKGROUND

Intranasal azelastine hydrochloride (Astelin, Meda Pharmaceuticals, Somerset, NJ, USA) is a first-line treatment for allergic and non-allergic vasomotor rhinitis with well-established therapeutic efficacy and safety. A new formulation of azelastine nasal spray (Astepro, Meda Pharmaceuticals, Somerset, NJ, USA), with a sorbitol-based vehicle and sucralose as a taste-masking agent, was developed to reduce the bitter taste of azelastine experienced by some patients.

OBJECTIVE

Two studies were conducted to evaluate the safety, tolerability and pharmacokinetic parameters of this new formulation compared with the original azelastine nasal spray.

METHODS

In a pharmacokinetic study, 18 healthy volunteers received either a single dose of the new formulation or the original formulation and pharmacokinetic parameters were determined. In a 1-year safety study, patients with chronic rhinitis were randomized to the new formulation (n = 430) or the original formulation (n = 432) to assess tolerability and the potential for adverse effects on the nasal mucosa.

RESULTS/

CONCLUSIONS

The new formulation was safe and well tolerated with long-term use and had a comparable pharmacokinetic profile to the original formulation. The overall incidence of treatment-emergent adverse events with the new formulation (48.4%) and the original formulation (49.1%) was similar, with no evidence of increased nasal irritation, nasal septal perforation, severe epistaxis or ulceration with either formulation during the 1-year study.