Ocular Pharmacokinetics of AzaSite Xtra—2% Azithromycin Formulated in a DuraSite Delivery System

Abstract

The PK/PD profile of 2% azithromycin suggests efficacy against common causative bacteria with just one dose per day for three days.

New method for ophthalmic delivery of azithromycin by poloxamer/carbopol-based in situ gelling system

“…Comparing our rabbit tear concentrations at 0.5-12 h with those of Amar et al (2008) and Si et al (2009), we believe, with twice-daily administrations of 1% (w/v) ATM in situ gel in the eyes, significant antibacterial ATM levels remain for a long period of time in the tears and in the conjunctiva.…”

“…However, others have demonstrated that dosing of 1.5 or 2% ATM achieved adequate conjunctiva concentrations to eradicate ATM-susceptible bacteria in a rabbit model of experimental keratitis (Amar et al, 2008;Si et al, 2009). Comparing our rabbit tear concentrations at 0.5-12 h with those of Amar et al (2008) and Si et al (2009), we believe, with twice-daily administrations of 1% (w/v) ATM in situ gel in the eyes, significant antibacterial ATM levels remain for a long period of time in the tears and in the conjunctiva.…”

Update and critical appraisal of the use of topical azithromycin ophthalmic 1% (AzaSite®) solution in the treatment of ocular infections

“…Recently, the pharmacokinetics of a 2% ocular solution of azithromycin in DuraSite (AzaSite Xtra™) was analysed in forty-two male pigmented rabbits 30. Twenty-four hours after administration of a single drop, corneal and conjunctival concentrations exceeded the minimum inhibitory concentration breakpoint for the most common causative pathogens of bacterial conjunctivitis by 3.5- and 5.8-fold, respectively; whereas the plasma levels were four to five orders of magnitude lower than ocular tissue levels.…”

Effectiveness, tolerability and safety of azithromycin 1% in DuraSite® for acute bacterial conjunctivitis

“…The studies on formulations give insight into how this new preparation is thought to work. 29,30 Azithromycin is hydrophobic and is sparingly soluble in water at neutral pH. Aqueous preparations of azithromycin for topical administration to the eye are therefore labile at room temperature and can degrade.…”