兔静脉注射及灌服莫昔沙星后眼内组织分布及其药动学比较研究  

Study on the Distribution of Moxifloxacin in Ocular Tissues and Its Pharmacokinetics in Rabbits with Intravenous and Perfusion Administration

作　　者：李琦[1] 张成志[2] 周远大[2] 何海霞[2] 

机构地区：[1]重庆医科大学附属第一医院眼科,重庆市400016 [2]重庆医科大学附属第一医院临床药理研究室,重庆市400016

出　　处：《中国药房》2010年第17期1575-1577,共3页China Pharmacy

摘　　要：目的:比较莫昔沙星治疗眼内感染的2种给药途径的眼内组织分布及药动学情况。方法:选取54只家兔,分为静脉注射组和灌服组各27只,每组再随机分为9个亚组、每亚组3兔6眼,各组相应给予莫昔沙星24mg·kg-1后,用高效液相色谱法测定兔眼内各组织中的药物浓度,以3p97软件计算药动学参数。结果:灌服和静脉注射给药后在角膜、房水、虹膜-睫状体、晶体和玻璃体内Cmax分别为(7.09±4.708)、(2.55±0.382),(3.84±1.217)、(3.71±0.54),(5.87±1.93)、(2.72±0.662),(1.36±0.176)、(0.74±0.396),(1.87±0.586)、(0.87±0.073)μg·g-1,AUC0～t分别为(12.24±1.112)、(9.27±0.559),(4.71±0.082)、(2.33±0.399),(13.79±0.814)、(8.04±2.045),(5.83±0.309)、(3.61±0.41),(3.45±0.064)、(3.09±0.539)μg·h·g-1,灌服组均显著高于静脉注射组(P<0.05或P<0.01)。结论:兔莫昔沙星单剂量灌服给药后在眼内各组织吸收较静脉注射给药更好,并能达到更高的药物浓度。OBJECTIVE： To compare the distribution of moxifloxacin in ocular tissue and its pharmacokinetics in rabbit with intravenous and perfusion administration. METHODS： 54 rabbits were divided into intravenous administration group and perfusion administration group （n=27 each）. Each group were randomized into 9 sub-groups （n=3）. Those groups were given 24 mg·kg-1 moxifloxacin with corresponding adminstration and HPLC was used to detect plasma concentration of moxifloxacin in ocular tissue. 3p97 software was adopted to calculate pharmacokinetic parameters. RESULTS： The Cmax of moxifloxacin by perfusion administration vs. intravenous administration in cornea,aqueous humor, iris-ciliary body,lens and vitreous were （7.09±4.708） μg·g-1 vs. （2.55±0.382） μg·g-1; （3.84±1.217） μg·g-1 vs. （3.71±0.54） μg·g-1; （5.87±1.93） μg·g-1 vs. （2.72±0.662） μg·g-1; （1.36±0.176） μg·g-1 vs. （0.74±0.396） μg·g-1; （1.87±0.586） μg·g-1 vs. （0.87±0.073） μg·g-1. The AUC0～t of two groups in above tissues were （12.24±1.112） μg·h·g-1 vs. （9.27±0.559） μg·h·g-1; （4.71±0.082） μg·h·g-1 vs. （2.33±0.399） μg·h·g-1; （13.79±0.814） μg·h·g-1 vs. （8.04±2.045） μg·h·g-1; （5.83±0.309） μg·h·g-1 vs. （3.61±0.41） μg·h·g-1; （3.45±0.064） μg·h·g-1 vs. （3.09±0.539） μg·h·g-1. The pharmacokinetic parameters in perfusion administration group were all higher than that in intravenous administration group （P0.05 or P0.01）. CONCLUSION： Perfusion administration is better than intravenous administration in absorption with high plasma concentration in ocular tisseus.

关 键 词：莫昔沙星 静脉注射 灌服 兔 组织分布 药动学 

分 类 号：R965[医药卫生—药理学] R969.1[医药卫生—药学]