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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)
Objective To study the content and pharmacokinetic parameters of cornea in rabbits at various times after dripping with chlorhexidine gluconate eye drops. Design experimental research. Study object 24 New Zealand white rabbit corneas. Methods 0.02% chlorhexidine gluconate eye drops were injected into the eyes twice a day (50μl each time) and were observed at 5, 10, 15, 20, 30, 50, 90, Only) were taken corneal tissue, using high performance liquid chromatography analysis of the corneal drug content, the use of 3p87 software fitting pharmacokinetic parameters. The main indicators of pharmacokinetic parameters. Results The theoretical peak time (tmax) of 0.02% chlorhexidine gluconate in rabbit cornea was 13.75 min, the peak concentration (Cmax) was 0.713 μg · g-1 and the half-life of drug distribution (t1 / 2α) was 2.65 min. The half-life of drug elimination (t1 / 2β) was 48.72min, the half-life of drug absorption (t1 / 2ka) was 2.67min, the clearance rate (CL) was 1.64min- · 1μg · g-1. CONCLUSION 0.02% chlorhexidine gluconate drops first-orderly in rabbit cornea. The open-chamber two-compartment model has the highest peak value at 15min with a peak concentration of (1.218 ± 0.157) μg · g-1. These parameters have some significance for guiding clinical medication. (Ophthalmology, 2006,15: 184-186)