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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 intraocular tissue distribution and pharmacokinetics of two routes of administration of moxifloxacin for the treatment of intraocular infections. Methods: Fifty-four rabbits were selected and divided into intravenous injection group and fed-fed group of 27 rats, each group was randomly divided into 9 subgroups, 3 rabbits in each subgroup with 6 eyes. Each group received 24 mg · of moxifloxacin kg-1, the concentration of the drug in each tissue of the rabbit eye was measured by high performance liquid chromatography, and the pharmacokinetic parameters were calculated by 3p97 software. Results: The Cmax in cornea, aqueous humor, iris - ciliary body, lens and vitreous were (7.09 ± 4.708), (2.55 ± 0.382), (3.84 ± 1.217) and (3.71 ± (0.87 ± 0.073) μg · g-1, (5.87 ± 1.93), (2.72 ± 0.662), (1.36 ± 0.176), (0.74 ± 0.396), (1.87 ± 0.586) 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) and (3.09 ± 0.539) μg · h-g-1, respectively. CONCLUSION: Rabbit moxifloxacin is better than single intravenous injection in all intraocular tissues after single-dose oral administration, and can achieve higher drug concentration.