诺氟沙星滴入兔眼与注入球结膜下其组织分布及药动学比较  

A comparative study on the distribution and pharmacokinetics of norfloxacin between topical instillation and subbulbar conjunctival injection in the rabbits

作　　者：周远大[1] 何海霞[1] 雷自强[1] 李远宗[1] 朱治本[1] 杨淑群[1] 

机构地区：[1]重庆医科大学第一附属医院,重庆医科大学第二附属医院

出　　处：《中国抗生素杂志》1995年第5期379-383,共5页Chinese Journal of Antibiotics

摘　　要：用高效液相色谱法对诺氟沙星点眼与球结膜下注射后眼各组织药物浓度进行测定，比较两种给药途径的眼各组织浓度及其药物动力学参数。结果表明，诺氟沙星点眼与球结膜下注射后４ｈ，泪液诺氟沙星浓度分别为２．０８±０．１９与１６．０７±３．１４μｇ／ｍｌ（Ｐ＜０．０１）；角膜分别为０．７１±０．０７与１．６５±０．２４μｇ／ｇ（Ｐ＜０．０１）。泪液ＡＵＣ分别为９８．３３±７．３１与２７９．８２±３１．７ｈ·μｇ／ｍｌ；角膜ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ、Ｔ１／２Ｋｃ分别为１７．４２±１．２１ｈ·μｇ／ｇ、８．９４±０．８μｇ／ｇ、０．５７±０．０６ｈ、０．９１７±０．１６ｈ与２０．０１±１．０１ｈ·μｇ／ｇ、１０．０５±０．０７μｇ／ｇ、０．４５±０．０５ｈ、１．１５±０．２０ｈ；房水ＡＵＣ、Ｃｍａｘ、Ｔｍａｘ分别为１．１３±０．２１ｈ·μｇ／ｍｌ、０．３９±０．０５μｇ／ｍｌ、０．６２±０．０９ｈ与１．７９±０．０７ｈ·μｇ／ｍｌ、１．００±０．１５μｇ／ｍｌ、０．４７±０．１０ｈ。诺氟沙星点眼与球结膜下注射两种给药途径的上述药动学参数有明显差异（Ｐ＜０．０５或０．０１）。The intraocular concentrations of norfloxacin were measured by highperformance liquid chromatography (HPLC)after topical instillation(TI)and subbulbularconjuntival injection(CI)with 0.3%norfloxacin soltition to rabbit eyes,The pharmacokine-tic parameters were calculated with pharmacokinetic program 3P87.Results showed thatconcentractions of norfloxacin in various ocular tisues were 2.08 ± 0. 19 and 16.07 ± 3.14μg/g(P<0.01)in lacrimal fluid,0.71±0.07 and 1.65±0.24μg/(P<0.01) in cornea 4hafter topically applying and injecting, respectively.The pharmacokinetic parameters inlacrimal fluid were AUC:98.33±7. 31 and 297. 82±31.70h·μg/g(P<0. 01,TI vs CI);incornea AUC:17.42±1. 21 and 20.01±1.01h·μg/g(P<0.05,TI vs CI),Cmax:8.94±0. 88and 10.05±0. 77μg/g(P<0.05,TI vs CI),Tmax:0.57±0.06 and 0.45±0. 05h(P<0.01,TIvs CI),T1/2Ke:0.91±0.16 and 1. 15±0.20h(P<0.05,TI vs CI),in aqueous humotir AUC:1.13±0. 21and 1. 79±0. 07h·μg/ml(P<0.05,TI vs CI),Cmax:0.39±0. 05and 1.00±0. 15μg/ml(P<0.01,TI vs CI),Tmax:0.62±0.09 and 0.47±0. 10h(P<0.05,TI vs CI),T1/2Ke:1. 50±0.32 and 1.06±0.07h(P<0.01,TI vs CI), From these results,we concludedthat concentration of norfloxacin by subbulbular conjunctival injecting would be higher inlacrimal fluid and cornea than that by topical instillation.

关 键 词：诺氟沙星 眼 组织分布 药物动力学 球结膜下 

分 类 号：R978.69[医药卫生—药品]