人眼滴用氧氟沙星和环丙沙星及妥布霉素的前房穿透性研究

目的 比较人眼滴用氧氟沙星、环丙沙星及妥布霉素的前房穿透性差异。方法 2003年4～8月在我院门诊预行白内障超声乳化术的老年白内障患者125例(125只单侧眼),使用随机数字表分为3个大组：氧氟沙星组(42只眼),环丙沙星组(41只眼),妥布霉素组(42只眼),每个大组再使用随机排列表分为5个小组,每个小组8或9只眼。按不同大组,术前局部给予0．3％氧氟沙星、0．3％环丙沙星或0．3％妥布霉素,滴眼6次,每次间隔15min。手术时按不同小组,于最后1次给药后7．5、15．0、30．0、60．0、120．0min时抽取前房水约100μl。使用高效液相色谱仪分析前房水中药物浓度。结果 各时间点前房内氧氟沙星浓度均明显高于环丙沙星,氧氟沙星生物利用度是环丙沙星的6倍。高效液相色谱仪未能检测到妥布霉素,故其浓度低于最低检测限0．05μg／ml。结论 人眼滴用氧氟沙星、环丙沙星和妥布霉素的结果表明氧氟沙星前房穿透性最好,提示可作为预防和治疗眼内炎的首选局部用药。

Aqueous humor penetration of topically applied ofloxacin, ciprofloxacin and tobramycin

OBJECTIVE: To compare the aqueous humor penetration of topically applied ofloxacin, ciprofloxacin and tobramycin in human eyes. METHODS: 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). RESULTS: 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). CONCLUSION: 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.