【摘要】 目的:测定0.1%双氯芬酸钠壳聚糖滴眼液单次滴眼后,不同时间兔眼房水的浓度,计算其药动学参数,研究药动学特点。方法:取24只大白兔分为8组,各组于用药后0.25,0.5,0.75,1,2,4,8,12h,抽取房水,所有检测均采用高效液相色谱法。结果:经DAS2.0药动学软件拟合符合一室开放模型,tmax:(0.79±0.12)h,Cmax:(1.490±0.018)mg·mL-1,t1/2:(3.02±0.13)h,AUC0-12:(4.810±0.020)mg.h.L-1,MRT:(3.44±0.06)h。结论:壳聚糖可促进双氯芬酸钠的吸收,提高双氯芬酸钠在眼房水内的浓度,是一种很有前景的眼用增黏剂和增效剂。更多还原

【Abstract】 OBJECTIVE To determine the rabbit ocular concentration of diclofenac sodium chitosan eye drops after topical application and calculate the pharmacokinetic parameters.METHODS 24 rabbits for the experiment were divided into 8 groups.The rabbit eyeballs of these groups were enucleated 0.25,0.5,0.75,1,2,4,8,12 h after instilled.All measurements were performed with HPLC.RESULTS Ocular pharmacokinetic parameters of diclofenac sodium were calculated by DAS 2.0 software.The concentration-time data of this drug in aqueous humor was subjected to 1 st order absorption.The observed pharmacokinetic parameters were found to be as follows:Cmax=(1.490±0.018)mg·L-1,tmax=(0.79±0.12)h,t1/2=(3.02±0.13)h,AUC0-12=(4.810±0.020)mg·h·L-1,MRT=(3.44±0.06)h.CONCLUSION Chitosan could able to improve the absorption of diclofenac sodium.It is valuable to be further studied as clinical preparation using chitosan as an adhesive of ocular administration.更多还原