N-三甲基壳聚糖包覆司帕沙星纳米脂质体兔眼房水及角膜药动学研究  

Pharmacokinetics of N-Trimethyl Chitosan-coated Sparfloxacin Nanoliposomes in Aqueous Humor and Cornea of Rabbits

作　　者：胡拥军[1] 宋玲[1] Hu Yongjun;Song Ling(Department of Phannacy,Hubei Maternal and Children Health Care Hospital,Wuhan 430070,China)

机构地区：[1]湖北省妇幼保健院药剂科,武汉430070

出　　处：《中国药师》2021年第1期180-183,205,共5页China Pharmacist

摘　　要：目的:对N-三甲基壳聚糖(TMC60)包覆司帕沙星(SL)纳米脂质体兔眼房水及角膜的药动学进行研究。方法:采用数字法将78只健康家兔随机分为3组:SL滴眼液组、SL纳米脂质体组和TMC60包覆SL纳米脂质体组,每组26只,双眼单次各给药100μl(SL滴入量为600μg)。在预设的时间点各组处死2只家兔,取房水及角膜,检测其中SL含量,DAS 2.0软件计算药动学参数,并绘制药-时曲线。结果:兔眼单次给药后,SL在房水及角膜中的药动学均符合二室模型。与SL滴眼液组相比,SL纳米脂质体组和TMC60包覆SL纳米脂质体组在房水及角膜中的达峰时间(Tmax)滞后,血药浓度时间曲线下面积(AUC0~t)明显增加(P<0.05)。与SL纳米脂质体组相比,TMC60包覆SL纳米脂质体组AUC0~t明显增加(P<0.05)。结论:TMC60包覆纳米脂质体可显著促进SL在眼部的滞留及吸收,呈现明显的缓释性及长效性。Objective:To study the pharmacokinetics of N-trimethyl chitosan (TMC60)-coated sparfloxacin (SL) nanoliposomes in aqueous humor and cornea of rabbits.Methods:Totally 78 healthy rabbits were divided into 3 groups:SL eye drops group,SL nanoliposomes group and TMC60-coated SL nanoliposomes group with 26 ones per group treated with 100μl corresponding drug for each eye (the amount of SL was 600μg).At the predetermined time points,2 rabbits from each group were sacrificed,and aqueous humor and cornea were withdrawn to detect the SL content.The pharmacokinetic parameters were calculated by DAS2.0 software and the profiles of drug concentration-time were drawn.Results:After the determination of single dose,the changes of SL concentration in aqueous humor and cornea fitted with two-compartment models.Compare to those of SL eye drops,Tmaxof SL nanoliposomes and TMC60-coated SL nanoliposomes was delayed with increased AUC0~t(P<0.05).Compared to that of SL nanoliposomes,AUC0~t was further increased in TMC60-coated SL nanoliposomes (P<0.05).Conclusion:TMC60-coated nanoliposomes can significantly enhance the eye retention and absorption of SL with notable sustained and prolonged effects.

关 键 词：司帕沙星 N-三甲基壳聚糖 纳米脂质体 药动学 兔 

分 类 号：R945[医药卫生—微生物与生化药学]