利巴韦林眼用在体凝胶剂在兔眼前房内的药动学研究

Study on aqueous humor pharmacokinetics for ribavirin ophthalmic in-situ gel in the conscious rabbits by microdialysis

目的:研究利巴韦林眼用在体凝胶剂在兔眼前房内的药动学。方法:在清醒家兔结膜囊内滴入40μL利巴韦林在体凝胶剂或利巴韦林滴眼液,采用微渗析技术取样,高效液相色谱法测定渗析液中利巴韦林的浓度。数据经非隔室模型处理,以方差分析和双单侧t检验评价各参数。结果:眼用在体凝胶剂在兔房水内的药动学参数为:AUC=(2.110±0.726)mg.L-1.h,Cmax=(1.548±0.822)mg.L-1,Tmax=(0.92±0.12)h,Ke=(0.225±0.093);滴眼液的药动学参数为:AUC=(0.615±0.126)mg.L-1.h,Cmax=(0.491±0.101)mg.L-1,Tmax=(0.25±0.11)h,Ke=(0.853±0.052)。结论:眼用在体凝胶剂明显提高了药物眼内的生物利用度,并且延长了作用时间,达到了处方的设计要求。

Objective： To study the ocular pharmacokinetics of ribavirin ophthalmic in-situ gel. Methods： The ocular pharmacokinetics of ribavirin gels was conducted by microdialysis using eye drops as control. The concentrations of ribavirin in aqueous humor were determined by HPLC method. Results： The pharmaceutical parameters of ribavirin gels were as follows： AUC = （2. 110 ±0. 726） mg.L^-1 .h, C ： （1. 548 ±0. 822） mg.L^-1, T = （0.92 ± 0.12） h, K = （0. 225 ± 0. 093）. The pharmaceutical parameters of ribavirin eye drops were as follows： AUC=（0.615±0.126） mg.L^-1.h, Cmax =（0.491 ±0.101） mg.L^-1, Tmax =（0.25±0.11） h, Ke = （0. 853 ± 0. 052）. Conclusion： The ocular bioavailability for ribavirin in-situ gel has been significantly improved.