PMID: 18203079Jan 19, 2008Paper

Tear concentrations of azithromycin following topical administration of a single dose of azithromycin 0.5%, 1.0%, and 1.5% eyedrops (T1225) in healthy volunteers

European Journal of Ophthalmology
F ChiambarettaI Cochereau

Abstract

To evaluate azithromycin tear concentrations after one drop of T1225 0.5%, 1.0%, and 1.5% eyedrops. In this randomized, double-masked study, 91 healthy volunteers received one drop into each eye of T1225 0.5% (n=23), T1225 1.0% (n=38), or T1225 1.5% (n=38). Azithromycin tear concentrations were measured by HPLC-MS at seven time points for 24 hours. Tolerability was evaluated. T1225 1.0% and 1.5% had similar pharmacokinetic profiles. After a post-instillation peak (167 to 178 mg/L after 10 minutes), mean concentrations remained above 7 mg/L for 24 hours (except for T1225 1% at H24). A delayed increase of the azithromycin mean tear concentration might be explained by the known late azithromycin release from tissues after storage in cells. Areas under inhibitory curve (AUICs) of T1225 1.0% and 1.5% were higher than AUICs of T1225 0.5% and ranged between 47 and 90. The three T1225 concentrations were safe for the ocular surface. Once daily instillation of T1225 1.0% and 1.5% was shown to reach an AUIC markedly above the required threshold for an antibacterial activity against Gram-positive bacteria (25-35). These results suggest that a BID instillation is more likely to ensure antimicrobial activity against Gram-negative bacteria (...Continue Reading

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Citations

Mar 3, 2009·Journal of the European Academy of Dermatology and Venereology : JEADV·O BakarS Cakir
Jun 6, 2009·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Joel W ProkschKeith W Ward
Jan 1, 2012·Ophthalmology and Eye Diseases·Dominick L Opitz, Jennifer S Harthan
Feb 24, 2017·Graefe's Archive for Clinical and Experimental Ophthalmology = Albrecht Von Graefes Archiv Für Klinische Und Experimentelle Ophthalmologie·Andrzej GrzybowskiStephen Jae Kim
Jul 6, 2017·Clinical & Experimental Optometry : Journal of the Australian Optometrical Association·Ozlem Balci, Gokhan Gulkilik
Feb 15, 2014·The British Journal of Ophthalmology·Dominique Bremond-GignacUNKNOWN AZI Study Group
Sep 6, 2008·Current Opinion in Ophthalmology

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