精胺普鲁兰糖对氧氟沙星角膜透过性影响的实验研究  

Effect of sperminated pullulans on the transcorneal permeability of ofloxacin

作　　者：于楠楠[1] 寻延滨[2,3] 金迪[1] 刘洁[1] 崔浩[1] 

机构地区：[1]哈尔滨医科大学第一临床医学院眼科医院,黑龙江哈尔滨150001 [2]中国药科大学,江苏南京210009 [3]黑龙江省药品检验所,黑龙江哈尔滨150001

出　　处：《哈尔滨医科大学学报》2010年第6期545-548,共4页Journal of Harbin Medical University

摘　　要：目的研究不同氨基含量的精胺普鲁兰糖(SP)对氧氟沙星角膜渗透量的影响,并评估其体内外眼部刺激性。方法采用离体角膜扩散实验的方法,实验分为对照组、低氨基含量精胺普鲁兰糖(SP-L)组和高氨基含量精胺普鲁兰糖(SP-H)组,每组6只角膜。用高效液相色谱-质谱仪测定分别加入0%SP、0.2%SP-L或0.2%SP-H后各时间点样品中的氧氟沙星的浓度,并测量角膜水化值,进行Draize试验评分。结果 0.2%的SP-L和SP-H使氧氟沙星的表观渗透系数分别增加了1.39倍(P<0.05)和2.01倍(P<0.01),SP-H促渗效力明显强于SP-L(P<0.01)。各组角膜水化值均小于83%,Draize试验评分均小于4。结论精胺普鲁兰糖是一种安全、有效的渗透促进剂,能够提高水溶性药物的角膜透过性,且随氨基含量的增多促渗作用增强。Objective To investigate the effect of sperminated pullulans（SP） with different numbers of amino groups on transcorneal permeation of ofloxacin and on in vitro and in vivo ocular irritation.Methods The excised corneas were randomly divided into control group,SP-L group and SP-H group,with 6 corneas in each group.Ofloxacin in sample solution was determinated by high pressure liquid chromatography-mass spectrum at appropriate time intervals after co-administrated with 0% SP,0.2% SP-L or 0.2% SP-H.Corneal hydration level was calculated and modified Draize test was also performed.Results The apparent permeability coefficient（Papp） for ofloxacin was increased 1.39 fold（P0.05） by SP-L and 2.01 fold（P0.01） by SP-H,respectively.SP-H was the more effective enhancer than SP-L（P0.01）.The corneal hydration level of each group was less than 83% and the scores of Draize test were all lower than 4.Conclusion SP as a safe and effective permeability enhancer can increase the corneal permeation of hydrophilic drug.The effect is enhanced with the increase of amino content of SP.

关 键 词：精胺普鲁兰糖 氧氟沙星 阳离子聚合物 角膜 

分 类 号：R-332[医药卫生] R77