【摘要】 研究０．３％左氧氟沙星局部应用给兔眼后，在泪液和房水中的药动学行为。方法 采用新西兰大白兔，双侧眼准确滴入０．３％左氧氟沙星滴眼液后，分别于不同时间取出房水和滤纸片并对其定量（定容及称重）。组织中的药物浓度采用反相高效液相色谱荧光检测法定量测定。药动学参数采用非线性最小二乘法进行计算机拟合求得。结果 采用反相高效液相色谱荧光检测法可以将左氧氟沙星同其他杂质很好分离，最低定量浓度为０．００５μｇ／ｍｌ，测定不同时间组织中药物浓度结果表明左氧氟沙星滴眼后，５ ｍｉｎ时泪液左氧氟沙星浓度最高（１１０８．８６ μｇ／ｇ±７１２．０８μｇ／ｇ；），３０ ｍｉｎ时房水浓度最高（１．２１ μｇ／ｍｌ± ０．４３μｇ／ｍｌ）。测得泪液中的药物浓度半衰期为２７．０５ ｍｉｎ，房水中为５４．６５ｍｉｎ。结论 左氧氟沙星能在眼内达到较高的抗菌浓度，可治疗眼内常见感染性疾病。更多还原

【Abstract】 Objective To observe the penetration of Levofloxacin into the tears and aqueous humors of New Zealand white rabbits following topical application of 0. 3% Levofloxacin to the rabbit eyes. Methods The rabbit tears and aqueous humors were obtained and the drug quantified at different times after topically applying 0. 3% Levofloxacin to the rabbit eyes. The drug levels were assayed by reversed phase high performance liquid chromatography fluorescence detection (RP-HPLC). The pharmacokinetic parameters were calculated with nonlinear least square method using the computer. Results The peak levels of levofloxacin occurred immediately (5 min) in the tears(1108. 86 μg/g ± 712. 08 μg/g) and at 30 min in the aqueous(1. 21 μg/ ml ± 0. 43 μg/ml) which was achieved against a majority of pathogens after administration. The half-life(t1/2 ) of levofloxacin was 27. 05 min in tears and 54. 65 min in aqueous humor,respectively. Conclusion 0. 3% Levofloxacin eye drops can be used as a topical antibacterial agent for treatment of conjunctivitis, keratitis and endophthalmitis.更多还原