壳聚糖对阿昔洛韦滴眼剂兔眼房水药动学的影响  

Effects of chitosan on the pharmacokinetics of aciclovir eye drops in aqueous humor of rabbits

作　　者：宋玲[1] 胡拥军[1] 黄理[2] SONG Ling;HU Yongjun;HUANG Li(Department of Pharmacy,Maternal and Child Health Hospital,Wuhan 430070,China;Department of Pharmacy,Renmin Hospital of Wuhan University,Wuhan 430060,China)

机构地区：[1]湖北省妇幼保健院药剂科,湖北武汉430070 [2]武汉大学人民医院药学部,湖北武汉430060

出　　处：《广东药科大学学报》2020年第6期757-760,共4页Journal of Guangdong Pharmaceutical University

摘　　要：目的探讨壳聚糖(CS)对阿昔洛韦(ACV)滴眼液(ACV-CS)在兔眼房水药动学的影响。方法以健康家兔眼自身对照实验,分别滴用ACV-CS及不加CS的ACV滴眼液(ACV),在不同时间点抽取房水,用HPLC法测定ACV浓度,用DAS2.0软件计算2种滴眼液的房水药动学参数。结果用药20 min内,ACV房水内血药浓度明显高于ACV-CS;20 min后,ACV-CS房水内血药浓度均明显高于ACV,且Cmax为ACV的1.31倍,AUC0-t为ACV的1.77倍;Tmax明显滞后,MRT明显延长(P<0.05)。结论CS可显著提高ACV在房水中的药浓,延长眼部滞留时间,提高眼部生物利用度。Objective To study the effects of chitosan(CS)on the pharmacokinetics of aciclovir(ACV)eye drops(ACV-CS)in aqueous humor of rabbits.Methods Healthy rabbits were used for self-control study,and ACV-CS and ACV eye drops without CS(ACV)were respectively administrated.At the predetermined time points,aqueous humor was withdrawn,the concentration of ACV was determined by HPLC,and DAS2.0 was used to calculate the main pharmacokinetic parameters.Results Within 20 min after the administration,the aqueous drug concentrations of ACV were higher than those of ACV-CS,thereafter,the ACV concentrations of ACV-CS were significant higher than those of ACV at all time points,and the Cmax was 1.31-times of that of ACV,and the AUC0-24 was 1.77-times of that of ACV with significantly delayed Tmax and prolonged MRT(P<0.05).Conclusion CS can significantly increase the penetration of ACV into aqueous humor of rabbits,prolong the residence time and enhance the ocular bioavailability.

关 键 词：壳聚糖 阿昔洛韦 滴眼液 房水 药动学 

分 类 号：R969.1[医药卫生—药理学]