左氧氟沙星白芨多糖滴眼液的眼部药物代谢动力学研究  

Pharmacokinetics and bioavailability of levofloxacin-bletilla striata polysaccharides eye drops applied in eyes

作　　者：杨丽娜[1] 辛萌[2] 吴祥根[2] 

机构地区：[1]青岛大学医学院,山东省青岛市266071 [2]山东省眼科研究所 山东省眼科学重点实验室一省部共建国家重点实验室培育基地,山东省青岛市266071

出　　处：《眼科新进展》2010年第5期422-426,共5页Recent Advances in Ophthalmology

摘　　要：目的评价5g.L-1左氧氟沙星白芨多糖滴眼液(左氧白芨滴眼液)滴兔眼后,药物在眼部的药物代谢动力学,以及与5g.L-1左氧氟沙星滴眼液(可乐必妥)比较其相对生物利用度。方法新西兰大白兔64只(128眼),平均分为2组,实验组给予左氧白芨滴眼液50μL滴眼,对照组给予可乐必妥50μL滴眼。分别于不同时间点取房水和角膜,应用高效液相色谱法测定左氧氟沙星浓度。采用DASver2.0药物代谢动力学程序计算各药物代谢动力学参数。结果所建立的高效液相色谱法能将左氧氟沙星与其他杂质很好地分离,其最低定量浓度为53.95μg.L-1,组织中回收率稳定。左氧白芨滴眼液与可乐必妥在房水中的半衰期(t1/2)分别为90.512min和106.480min,达峰时间(tmax)分别为45.000min和60.000min,达峰浓度(Cmax)分别为2318.973μg.L-1和1111.457μg.L-1(P<0.05);角膜中t1/2分别为109.400min和64.956min,tmax分别为10.000min和15.000min,Cmax分别为23.012μg.g-1和16.389μg.g-1。左氧白芨滴眼液组房水和角膜中药物质量浓度曲线下面积(AUC0-240)分别是可乐必妥组的1.79倍和1.37倍。结论左氧白芨滴眼液较可乐必妥生物利用度显著提高。Objective To evaluate the pharmacokinetics of 5 g·L-1 levofloxacin-bletilla striata polysaccharides eye drops applied in rabbit eye,and to compare its relative bioavailability with normal 5 g·L-1 levofloxacin eye drops.Methods Six-four New-Zealand white rabbits（128 eyes）were divided into two groups,32 cases（64 eyes）in each group.The experimental group was topically given 50 μL levofloxacin-bletilla striata polysaccharides eye drops,and the control group was given 50 μL levofloxacin eye drops.The aqueous humor and corneas were collected at different time points,the concentration of levofloxacin was detected by reverse phase high performance liquid chromatography.The pharmacokinetic parameters of each drug were calculated by DAS ver2.0 processing program.Results The levofloxacin could be separated well from other foreign matter by reverse phase high performance liquid chromatography,the lowest quantitative concentration of levofloxacin was 53.95 μg·L-1,the recovery rate from the tissue was stable.In aqueous humor,the half-life（t1/2）of levofloxacin-bletilla striata polysaccharides eye drops and levofloxacin eye drops was 90.512 minutes and 106.480 minutes,the tmax was 45.000 minutes and 60.000 minutes,and the Cmax were 2 318.973 μg·L-1 and 1 111.457 μg·L-1 respectively,there were statistical differences（All P0.05）.In cornea,the t1/2 of the two eye drops was 109.400 minutes and 64.956 minutes,the tmax was10.000 minutes and 15.000 minutes,and the Cmax were 23.012 μg·g-1 and 16.389 μg·g-1.The areas under curve（AUC0-240）of levofloxacin-bletilla striata polysaccharides eye drops in aqueous humor and cornea were 1.78 times and 1.37 times higher than those of levofloxacin eye drops.Conclusion The ocular bioavailability of levofloxacin-bletilla striata polysaccharides eye drops is higher than that of levofloxacin eye drops.

关 键 词：左氧氟沙星 白芨多糖 药物代谢动力学 生物利用度 

分 类 号：R772.2[医药卫生—眼科]