Distribution of cefuroxime in ocular tissues of rabbit after intravenous administration

Authors: Gong Ruizhong, Wang Li, Wang Chen, Zhou Yingxia, Li Cuihong, Zhang Lin, Liu Zetao, Yang Liping

DOI: 10.3760/cma.j.issn.2095-0160.2019.12.006

Published 2019-12-10

Cite as Chin J Exp Ophthalmol, 2019,37(12): 967-970.

Abstract

Objective

To study the distribution and pharmacokinetics of cefuroxime in rabbit eyes after intravenous administration.

Methods

Thirty-five rabbits were randomly divided into 7 groups by random number table method, with 5 rabbits in each group.The rabbits in blank control group were feed without any treatment, the rest rabbits were injected with 40.63 mg/kg cefuroxime intravenously.The rabbits were sacrificed at 0.5 hour, 1.0 hour, 1.5, 2.0, 2.5 and 3.0 hours after injection, and the eyeballs were immediately dissected.The concentration of drug in different ocular tissues was detected by high performance liquid chromatography, and the pharmacokinetic parameters in eyes were computed by the DAS software.This study was approved by the Experimental Animal Ethics Committee of Shanxi Provincial Eye Hospital (201802b).

Results

The peak concentrations (Cmax) of cefuroxime were (11.63±0.20), (1.59±0.05), (1.51±0.08), (0.99±0.07), (1.55±0.08) and (8.57±0.17)μg/ml in aqueous humor, iris-ciliary body, vitreous body, retinal-choroid, cornea and sclera, respectively.The times to peak (Tmax) were 1.5 hours, 1.0, 1.0, 0.5, 1.0 and 0.5 hour in aqueous humor, iris-ciliary body, vitreous body, retinal-choroid, cornea and sclera, respectively.The areas under drug time curve (AUC_0-t) were (26.60±0.62), (6.22±0.84), (5.86±0.16), (3.75±0.45), (5.50±0.15) and (26.48±0.73)(μg·h)/ml in aqueous humor, iris-ciliary body, vitreous body, retinal-choroid, cornea and sclera, respectively.Cefuroxime was not detected in the lens at different time points after injection.The parameters of pharmacokinetics were fitted to two compartment model.

Conclusions

Cefuroxime shows good penetration in aqueous humor, iris-ciliary body, vitreous body, retinal-choroid, cornea and sclera when administrated by intravenous injection in rabbits and cefuroxime has no distribution in lens.Cefuroxime can reach an effective concentration in ocular tissues 0.5 to 1.5 hours after intravenous injection.