【摘要】 目的:制备盐酸小檗碱眼用温敏凝胶并考察其在家兔眼房水内的药动学特征。方法:以泊洛沙姆为温敏材料,盐酸小檗碱为模型药物制备眼用温敏原位凝胶,高效液相色谱法测定给药后不同时间兔眼房水中的盐酸小檗碱浓度,绘制药-时曲线,计算相关药动学参数。结果:盐酸小檗碱眼用温敏原位凝胶在兔眼内的吸收和消除过程呈线性二室模型动力学特征,其t1/2β、t1/2α,MRT、Tmax、Cmax、AUC0-τ和AUC0-∞分别为4.585 h,0.911 h,1.966 h,1 h,1.4 mg.L-1,2.561 mg.h.L-1,2.581 mg.h.L-1。结论:此方法可用于测定房水中盐酸小檗碱的浓度,对于盐酸小檗碱眼部局部给药药动学研究提供评价方法。更多还原

【Abstract】 Objective:To prepare in-situ thermosensitive gel containing berberine hydrochloride for ophthalmic use and study its pharmacokinetic parameters in aqueous humors of rabbit eyes.Methods:The in-situ thermosensitive gel of berberine hydrochloride was prepared using poloxamer 407 and poloxamer 188 as thermosensitive material,drug concentration in aqueous humors of rabbit eyes at different time was determined by HPLC.Aqueous humors concentration-time curve of berberine hydrochloride was plotted and pharmacokinetic parameters were calculated by the DAS(Drug and Statistics)soft.Results:The absorption and elimination of berberine hydrochloride were fitted to a two-compartment model with the main pharmacokinetic parameters as follows: t1/2 β,t1/2α,MRT,Tmax,Cmax,AUC0-τ and AUC0-∞ were 4.585 h,0.911 h,1.966 h,1 h,1.4 mg·L-1,2.561 mg·h·L-1 and 2.581 mg·h·L-1,respectively.Conclusion:This method can be used to determine the concentration of berberine hydrochloride in aqueous humors of rabbit eyes,and be suitable for the pharmacokinetic study of berberine hydrochloride in local ophthalmic system.更多还原