目的研究头孢呋辛静脉注射后在兔眼内各组织的分布及药代动力学参数。
方法选取6月龄健康家兔35只，按照随机数字表法随机分为7个组，每组5只。空白对照组不做处理，其余实验兔耳缘静脉注射40.63 mg/kg头孢呋辛，分别于注射后0.5、1.0、1.5、2.0、2.5和3.0 h空气栓塞法各处死1组家兔，剖取各时间点实验兔眼球，分离眼部各组织，利用高效液相色谱法测定药物质量浓度，采用DAS软件进行头孢呋辛在眼部的药代动力学模型拟合。
结果给药后房水、虹膜睫状体、玻璃体、视网膜脉络膜、角膜、巩膜组织中头孢呋辛的峰质量浓度(Cmax)分别为(11.63±0.20)、(1.59±0.05)、(1.51±0.08)、(0.99±0.07)、(1.55±0.08)和(8.57±0.17)μg/ml，达峰时间(Tmax)分别为1.5、1.0、1.0、0.5、1.0和0.5 h，药时曲线下面积(AUC 0－t)分别为(26.60±0.62)、(6.22±0.84)、(5.86±0.16)、(3.75±0.45)、(5.50±0.15)和(26.48±0.73)(μg·h)/ml。给药后不同时间点晶状体中均未测得头孢呋辛。头孢呋辛药物在眼部代谢动力学均符合二室模型。
结论家兔静脉注射头孢呋辛后，头孢呋辛在房水、虹膜睫状体、玻璃体、视网膜脉络膜、角膜、巩膜等组织中均有良好的通透性，在晶状体内无头孢呋辛分布。静脉注射后0.5～1.5 h头孢呋辛在眼部各组织中能达到有效浓度。
ObjectiveTo study the distribution and pharmacokinetics of cefuroxime in rabbit eyes after intravenous administration.
MethodsThirty-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).
ResultsThe 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.
ConclusionsCefuroxime 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.
宫瑞中,王丽,王琛,等. 头孢呋辛静脉注射后在兔眼内组织的分布[J]. 中华实验眼科杂志,2019,37(12)：967-970.
DOI:10.3760/cma.j.issn.2095-0160.2019.12.006版权归中华医学会所有。
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