环孢素A眼用pH敏感型乳剂凝胶的角膜滞留性及药效学  

Corneal retention and pharmacodynamics in vivo of pH sensitive ophthalmic gel of cyclosporine A emulsion

作　　者：刘玉生[1] 薛晓[2] 李实[2] 杨磊[2] 王东凯[2] 

机构地区：[1]北京红太阳药业有限公司,北京100020 [2]沈阳药科大学,沈阳110016

出　　处：《中国新药杂志》2015年第2期199-203,共5页Chinese Journal of New Drugs

摘　　要：目的:制备环孢素A眼用pH敏感型乳剂凝胶并研究其角膜滞留性及药效学。方法:以家兔为模型动物,环孢素A眼用乳剂为对照组,利用γ-闪烁扫描技术考察环孢素A眼用pH敏感型乳剂凝胶的眼部滞留性;并建立干眼症模型,以泪液分泌实验(schirmer I test,SIT)和角膜荧光素染色(fluorescence integral,FI)值为指标,结合外观评价,考察环孢素A眼用pH敏感型乳剂凝胶治疗干眼症的效果。结果:环孢素A眼用pH敏感型乳剂凝胶与对照组相比,显著延长在角膜的滞留时间;利用SPSS 19.0统计分析软件显示:实验组与阳性对照组在增加SIT值方面有极显著性差异(P<0.01),在降低FI值方面有显著性差异(P<0.05)。结论:环孢素A眼用p H敏感型乳剂凝胶显著延长在角膜的滞留时间,对干眼病的治疗起效更快,治疗效果更好。Objective： To prepare pH sensitive ophthalmic gel of cyclosporine A（ CsA） emulsion and study its corneal retention and pharmacodynamics in vivo. Methods： Rabbits were used as model animals. Gamma scintigraphic images was used to study the corneal retention capability of the gel. Dry eye syndrome model was established by dropping atropine sulfate ophthalmic gel to evaluate the pharmacodynamics by using Schirmer I test（ SIT）and fluorescence integral（ FI） value as indexes. Results： The pH-sensitive ophthalmic gel of CsA emulsion prolonged the corneal retention remarkably. Statistical analysis with SPSS 19. 0 software indicated that there were significant differences in SIT increase and FI decrease between pH-sensitive ophthalmic gel of CsA emulsion and Cs A ophthalmic emulsion. Conclusion： pH-sensitive ophthalmic gel of Cs A emulsion had better corneal retention ability and therapeutic effect for dry eyes with more rapid onset.

关 键 词：环孢素A pH敏感型乳剂凝胶 角膜滞留性 药效学 

分 类 号：R988.1[医药卫生—药品]