Amar Thierry, Caillaud Thierry, Elena Pierre-Paul
Iris Pharma, La Gaude, France.
Curr Eye Res. 2008 Feb;33(2):149-58. doi: 10.1080/02713680701860499.
The aim of this study was to investigate whether the ocular pharmacokinetic parameters observed following systemic administration are also seen following topical administration.
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.
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.
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.
本研究旨在调查全身给药后观察到的眼部药代动力学参数在局部给药后是否也会出现。
采用高效液相色谱-质谱法（HPLC-MS）测定色素兔单次滴注以及连续三天每日两次滴注局部用1.50%阿奇霉素二水合物溶液后泪液、角膜、球结膜和房水中的阿奇霉素浓度。
单次给药后，滴注后泪液中阿奇霉素水平至少4小时高于敏感菌的最低抑菌浓度（MIC）4微克/克阈值，结膜中1小时，角膜中1小时。多次给药后，最后一次滴注后泪液中阿奇霉素水平至少16小时高于MIC 4微克/克，结膜中24小时，角膜中1周。
两种给药方案在结膜（相对于人类预期治疗指征（细菌性结膜炎）的眼部靶组织）、角膜和泪液中均产生了足够且持久的阿奇霉素水平。
