Tabbara K F, al-Kharashi S A, al-Mansouri S M, al-Omar O M, Cooper H, el-Asrar A M, Foulds G
Department of Ophthalmology, College of Medicine, King Saud University, Riyadh, Saudi Arabia.
Arch Ophthalmol. 1998 Dec;116(12):1625-8. doi: 10.1001/archopht.116.12.1625.
To assess azithromycin levels in human serum, aqueous humor, tear fluid, and conjunctival tissue specimens after administration of a single 1-g oral dose of azithromycin.
Sixty patients undergoing cataract surgery were included in this analysis. Serum, aqueous, and tear specimens were collected 3, 6, and 12 hours and 1, 2, 3, and 4 days after azithromycin administration. Conjunctival tissue biopsy specimens were collected 1, 2, 3, 4, 6, 8, 10, 12, and 14 days after azithromycin administration. All specimens were subjected to analysis by high-performance liquid chromatography-mass spectrometry.
Azithromycin concentration ranges during the specified sampling times were as follows: serum, 21 to 974 ng/mL; tear, 82 to 2892 ng/mL; aqueous, 10 to 69 ng/mL; and conjunctival, 0.7 to 32 micrograms/g. Levels above the 90% minimal inhibitory concentration (MIC90) for Chlamydia trachomatis were detected after 4 days in all tear samples and after 14 days in all conjunctival tissue specimens following oral azithromycin administration.
We demonstrated prolonged high levels of azithromycin in drug-targeted ocular tissue. Prolonged high concentrations of azithromycin in conjunctival tissue make this drug suitable for treatment of conjunctivitis caused by chlamydiae and other susceptible organisms.
评估单次口服1克阿奇霉素后人体血清、房水、泪液和结膜组织标本中的阿奇霉素水平。
本分析纳入了60例接受白内障手术的患者。在给予阿奇霉素后3、6和12小时以及1、2、3和4天收集血清、房水和泪液标本。在给予阿奇霉素后1、2、3、4、6、8、10、12和14天收集结膜组织活检标本。所有标本均采用高效液相色谱-质谱分析法进行分析。
在指定采样时间内阿奇霉素的浓度范围如下：血清，21至974纳克/毫升；泪液，82至2892纳克/毫升；房水，10至69纳克/毫升；结膜，0.7至32微克/克。口服阿奇霉素后，所有泪液样本在4天后以及所有结膜组织标本在14天后均检测到高于沙眼衣原体90%最小抑菌浓度（MIC90）的水平。
我们证明了阿奇霉素在药物靶向眼组织中的高水平持续存在。结膜组织中阿奇霉素的高浓度持续存在使得该药物适用于治疗由衣原体和其他易感微生物引起的结膜炎。
