【摘要】 目的研究滴用葡萄糖酸氯己定滴眼液后不同时间兔角膜中药物的含量及其药代动力学参数。设计实验性研究。研究对象24只新西兰白兔眼角膜。方法0.02%葡萄糖酸氯己定滴眼液兔双眼点药2次(每次50μl),于点眼后5、10、15、20、30、50、90、120min(随机分8组,每组3只)分别取角膜组织,采用高效液相色谱法分析测定角膜中的药物含量,利用3p87软件拟合药代动力学参数。主要指标药代动力学参数。结果0.02%葡萄糖酸氯己定在兔角膜中的理论达峰时间(tmax)为13.75min、达峰浓度(Cmax)为0.713μg·g-1、药物分布半衰期(t1/2α)为2.65min、药物消除半衰期(t1/2β)为48.72min、药物吸收半衰期(t1/2ka)为2.67min,清除率(CL)为1.64min-·1μg·g-1。结论0.02%葡萄糖酸氯己定滴眼后在兔角膜中呈一级吸收,开放式二室模型,实测值在15min时达高峰,其达峰浓度为(1.218±0.157)μg·g-1。这些参数对于指导临床用药具有一定意义。(眼科,2006,15:184-186)更多还原

【Abstract】 Objective To study the chlorhexidine gluconate concentration and dynamic changes in rabbit cornea with high-performance liquid chromatographic assay(HPLC). Design Experimental study. Participants The corneas of 24 healthy New Zealand white rabbits. Methods Twenty-four white rabbits were randomly divided into 8 groups. The cornea tissue was collected at 5,10,15,20,30,50,90,120 min for analysis after 0.02% chlorhexidine gluconate was applied to the rabbit eyes. The concentration of chlorhexidine was detected with HPLC method,and pharmacokinetic parameters were estimated with 3p87 program according to the results of HPLC. Main Outcome Measures Pharmacokinetic parameters. Results The pharmacokinetic parameters were as following: tmax =13.75 minutes,Cmax =0.713 μg·g-1,t1/2α=2.65 minutes,t1/2β=48.72 minutes,t1/2ka=2.67 minutes,CL=1.64 min-1·μg·g-1. Conclusion The concentration-time data of chlorhexidine gluconate in rabbits’ cornea were fitted to a two-compartment open model with first-order absorption. The observed maximum concentration of chlorhexidine reached 1.218±0.157 μg·g-1 at 15 min. This result may be helpful for the treatment of acanthamoeba keratitis on clinic.(Ophthalmol CHN,2006,15:184-186)更多还原