Kleinberg J, Dea F J, Anderson J A, Leopold I H
Arch Ophthalmol. 1979 May;97(5):933-6. doi: 10.1001/archopht.1979.01020010491024.
Ocular penetration of lincomycin hydrochloride in albino rabbits was determined by bioassay. On topical application, the frequency of multiple instillation of drops played an important role in producing therapeutic levels in the anterior chambers. Therapeutic levels were attained in the cornea, aqueous humor, and iris-ciliary body, with peak values occurring at 30 to 45 minutes. Varying the pH of the dosing solution did not change ocular absorption and distribution substantially. Removal of corneal epithelium, however, greatly enhanced absorption. Relative to clindamycin, lincomycin hydrochloride had longer onset of peak values and lower overall concentration in ocular tissues. Intravitreous injection of lincomycin hydrochloride produced therapeutic and steady levels of antibiotic in anterior chambers. Injection produced a concentration in aqueous humor twice that achievable topically. The major route of elimination from the posterior chamber was through retina-choroid.
通过生物测定法测定了盐酸林可霉素在白化兔眼中的穿透力。局部应用时,多次滴眼的频率在房水中产生治疗水平方面起着重要作用。在角膜、房水和虹膜睫状体中达到了治疗水平,峰值出现在30至45分钟。改变给药溶液的pH值并没有显著改变眼部的吸收和分布。然而,去除角膜上皮会大大增强吸收。相对于克林霉素,盐酸林可霉素在眼部组织中达到峰值的时间更长,总体浓度更低。玻璃体内注射盐酸林可霉素在前房中产生了治疗性且稳定的抗生素水平。注射产生的房水浓度是局部应用所能达到浓度的两倍。后房的主要消除途径是通过视网膜脉络膜。