Yao Ke, Zhang Zheng, Yang Yao-hua, Wu Xiao-dan
Eye Center, Affiliated Second Hospital of Zhejiang University, Hangzhou 310009, China.
Zhonghua Yan Ke Za Zhi. 2003 Dec;39(12):736-9.
To compare the aqueous humor penetration of topically applied ofloxacin, ciprofloxacin and tobramycin in human eyes.
Senile cataract patients (125 eyes in 125 cases) receiving phacoemulsification were randomized into three groups: ofloxacin, 42 eyes; ciprofloxacin, 41 eyes and tobramycin, 41 eyes. Each group was randomized into five sub-groups, with 8 or 9 eyes in each sub-group. Each group received either 0.3% ofloxacin, ciprofloxacin or tobramycin topical drops preoperatively. Eyedrops were instilled one drop every 15 minutes for six times. Aqueous samples were obtained from different sub-groups during surgery, 7.5, 15.0, 30.0, 60.0 and 120.0 min after the last drop, respectively. Concentration of the antimicrobial agents was determined by the HPLC (high pressure liquid chromatography).
Aqueous humor concentration of ofloxacin was significantly higher than that of ciprofloxacin at the same period after the last drop. The bioavailability of ofloxacin was 6 times that of ciprofloxacin. Tobramycin could not be detected by HPLC, so its concentration was lower than the minimum detectable level by HPLC (0.05 micro g/ml).
Ofloxacin has the best aqueous penetration in human eyes, as compared with ciprofloxacin and tobramycin, which suggests ofloxacin could be the preferred topical medicine for the prevention and treatment of endophthalmitis.
比较局部应用氧氟沙星、环丙沙星和妥布霉素在人眼中的房水渗透情况。
将125例接受超声乳化白内障吸除术的老年性白内障患者（共125只眼）随机分为三组：氧氟沙星组42只眼；环丙沙星组41只眼；妥布霉素组41只眼。每组再随机分为五个亚组，每个亚组8或9只眼。每组患者术前分别接受0.3%氧氟沙星、环丙沙星或妥布霉素滴眼液滴眼。每隔15分钟滴一滴，共滴六次。在手术过程中，分别于最后一滴眼药水后7.5、15.0、30.0、60.0和120.0分钟从不同亚组采集房水样本。采用高效液相色谱法（HPLC）测定抗菌药物浓度。
最后一滴眼药水后同一时间段，氧氟沙星的房水浓度显著高于环丙沙星。氧氟沙星的生物利用度是环丙沙星的6倍。用HPLC法未检测到妥布霉素，因此其浓度低于HPLC的最低检测水平（0.05μg/ml）。
与环丙沙星和妥布霉素相比，氧氟沙星在人眼中具有最佳的房水渗透性，这表明氧氟沙星可能是预防和治疗眼内炎的首选局部用药。
