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Ocular pharmacokinetic study following single and multiple azithromycin administrations in pigmented rabbits.

Author(s): Amar T, Caillaud T, Elena PP

Affiliation(s): Iris Pharma, La Gaude, France.

Publication date & source: 2008-02, Curr Eye Res., 33(2):149-58.

PURPOSE: The aim of this study was to investigate whether the ocular pharmacokinetic parameters observed following systemic administration are also seen following topical administration. METHODS: Azithromycin concentrations were measured by HPLC-MS in pigmented rabbits' tears, cornea, bulbar conjunctiva, and aqueous humor following single instillation and twice-daily instillations for three consecutive days of topical 1.50% azithromycin dihydrate solution. RESULTS: Following a single administration, azithromycin levels were higher than the MIC 4 microg/g breakpoint for susceptible germs for at least 4 hr in tears, 1 hr in conjunctiva, and 1 hr in cornea after instillation. Following multiple administrations, azithromycin levels were higher than the MIC 4 microg/g for at least 16 hr in tears, 24 hr in conjunctivae, and 1 week in cornea after the last instillation. CONCLUSIONS: Both dosage regimens resulted in adequate and long-lasting azithromycin levels in the conjunctiva, the ocular target tissue relative to the expected therapeutic indication in man (bacterial conjunctivitis), and also in the cornea and tears.

Page last updated: 2008-06-22

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