特比萘芬滴眼液在家兔房水及角膜中的药代动力学研究  

Pharmarcokinetics of terbinafine eye drops in rabbits aqueous and cornea

作　　者：刘宏伟[1] 王香兰[1] 周毅[1] 彭淑玲[1] 

机构地区：[1]首都医科大学北京同仁医院北京市眼科研究所药理室,100005

出　　处：《眼科研究》2006年第1期15-17,共3页Chinese Ophthalmic Research

基　　金：北京市科委基金资助(9555101700)

摘　　要：目的以高效液相色谱法测定家兔房水和角膜的盐酸特比萘芬含量。方法18只家兔分为6组,每组3只(6只眼),盐酸特比萘芬滴眼液50μl滴入家兔眼中,点眼后的0.08、0.25、0.5、1、2和4h,分别取3只家兔(6只眼)房水和角膜,经甲醇提取后在C18柱上分析。结果房水药物质量浓度在0.08、0.25、0.5、1、2和4h分别为0.08、0.13、0.03、0.04、0.05和0.03μg/ml,角膜药物质量分数在0.08、0.25、0.5、1、2和4h分别为2.47、0.80、0.41、1.22、0.60和0.25μg/g。结论单次滴眼在兔眼角膜及房水中的含量均高于多数真菌的最低抑菌浓度(MIC),盐酸特比萘芬滴眼液可用于真菌性角膜炎的治疗。Objective To measure the concentration of terbinafine in rabbit aqueous and cornea by high pressure liquid chromatography （HPLC） after the topieal administration of terbinafine. Methods Eighteen rabbits were divided 6 groups and 3 rabbits（6 eyes） for each. Terbinafine drops was topically administrated in rabbit eye. The aqueous and cornea spaceman from 6 eyes of 3 rabbits were obtained in 0. 08,0. 25,0. 5,1,2 and 4 hours and analyzed by C18 PHLC after terbinafine was used separately. Results The regression analysis showed a good linearity relation between peak area to concentration over the range of 0. 01 to 2. 00μg/ml（ r =0. 999 9 ,P =0. 000 0）. The terbinafine concentrations in aqueous were 0. 08,0. 13,0. 03,0. 04,0. 05 and 0. 03μg/ml in 0. 08,0.25,0.5,1,2 and 4 hours. The terbinafine concentrations in cornea were 2.47,0. 80,0.41 , 1.22,0.60 and 0.25μg/g in 0. 08,0. 25,0. 5,1,2 and 4 hours. Conclusion The terbinafine concentration in aqueous and cornea is higher than minimum inhibitory concentration （MIC） of most fungus. The terbinafine eye drops could be used to treatment of fungus keratitis.

关 键 词：高效液相色谱法 盐酸特比萘芬滴眼液 房水 角膜 

分 类 号：R96[医药卫生—药理学]