Green K, Bowman K, Luxenberg M N, Friberg T R
Arch Ophthalmol. 1983 Feb;101(2):284-8. doi: 10.1001/archopht.1983.01040010286021.
The penetration of indomethacin labeled with radioactive carbon (14C) into all ocular tissues and fluids was determined at various intervals in both phakic and aphakic rabbit eyes after either single or multiple (every 12 hours for three days) topical application (50 microL) regimens. More indomethacin was found in the vitreous of aphakic eyes compared with phakic eyes after single- or multiple-drop administration. Retinal and choroidal indomethacin concentrations were equal in both phakic and aphakic eyes after either drug regimen and are much greater than those of the vitreous. A pathway other than diffusion through the vitreous exists for the drug to reach these tissues. The concentration of indomethacin reaching the retina and choroid is not sufficient to inhibit prostaglandin formation locally. The concentrations of indomethacin are high enough to inhibit the biotransformation of prostaglandin precursor only in the anterior segment.
在有晶状体和无晶状体兔眼中,分别采用单次或多次(每12小时一次,共三天)局部应用(50微升)的给药方案,在不同时间间隔测定放射性碳(14C)标记的吲哚美辛在所有眼组织和眼液中的渗透情况。单次或多次滴眼给药后,与有晶状体眼相比,无晶状体眼玻璃体中的吲哚美辛含量更高。两种给药方案后,有晶状体和无晶状体眼中视网膜和脉络膜的吲哚美辛浓度相等,且远高于玻璃体中的浓度。药物到达这些组织存在除通过玻璃体扩散之外的其他途径。到达视网膜和脉络膜的吲哚美辛浓度不足以局部抑制前列腺素的形成。吲哚美辛浓度仅在前房足够高,足以抑制前列腺素前体的生物转化。