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

Abstract

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.

• Authors: William E Berger
• Journal: Expert opinion on drug metabolism & toxicology (Expert Opin Drug Metab Toxicol) Vol. 5 Issue 1 Pg. 91-102 (Jan 2009) ISSN: 1744-7607 [Electronic] England
• PMID: 19220164 (Publication Type: Journal Article, Review)

Chemical References

• Aerosols
• Histamine Antagonists
• Phthalazines
• azelastine

Topics

• Administration, Intranasal
• Aerosols
• Biological Availability
• Clinical Trials as Topic
• Histamine Antagonists (administration & dosage, adverse effects, pharmacokinetics, therapeutic use)
• Humans
• Phthalazines (administration & dosage, adverse effects, pharmacokinetics, therapeutic use)
• Rhinitis, Allergic, Seasonal (drug therapy)
• Rhinitis, Vasomotor (drug therapy)
• Treatment Outcome