刘志东,郭宏,李佳玮,丁平田,潘卫三
LIU Zhi-dong1; GUO Hong2; LI Jia-wei3; DING Ping-tian1; PAN Wei-san1 (1.School of Pharmacy;

• 1:沈阳药科大学药学院
• 2:佳木斯大学化学与药学院
• 3:沈阳药科大学制药工程学院
• 4:沈阳药科大学药学院

摘要(Abstract)：

目的研究羟丙 β 环糊精 (HP β CD)对依诺沙星 (enoxacin ,ENX)角膜透过性的影响。 方法采用体外扩散实验考察在不同浓度HP β CD条件下ENX的离体兔眼角膜透过性。 结果 13、2 6和39mmol·L-1HP β CD组的表观渗透系数与对照组相比显著性增加 (P <0 0 1) ,2 6mmol·L-1HP β CD使得ENX的表观渗透系数达到最大 ,是对照组的 3 5 8倍 ;5 2和78mmol·L-1HP β CD组表观渗透系数与对照组相比没有显著性差异 (P >0 0 5 )。结论HP β CD浓度与ENX的表观渗透系数之间没有线性关系。
Objective To study the effect of HP-β-CD on the transcorneal permeability of enoxacin(ENX).Methods The permeability of a ENX across isolated rabbit′s cornea was measured using the in vitro method under HP-β-CD with different concentrations.Results 13,26 and 39 mmol·L -1 HP-β-CD showed more significantly promoting activity than the control.The largest value of the apparent permeation coefficient could be obtained at 26 mmol·L -1 HP-β-CD level which was 3.58 times more than that of the control.However,52 and 78 mmol·L -1 HP-β-CD showed no significant influence on the permeation coefficient.Conclusion There was lack of linearity between HP-β-CD and the apparent permeation coefficient of ENX.

关键词(KeyWords)： 依诺沙星;羟丙基-β-环糊精;角膜透过性
enoxacin; HP-β-CD; transcorneal permeability

Abstract:

Keywords:

基金项目(Foundation):

作者(Authors): 刘志东,郭宏,李佳玮,丁平田,潘卫三
LIU Zhi-dong1; GUO Hong2; LI Jia-wei3; DING Ping-tian1; PAN Wei-san1 (1.School of Pharmacy;

参考文献(References)：

• [1]LoftssonI,Stef劋nssonE.Effectofcyclodextrinsontopi caldrugdeliverytotheeye[J].DrugDevelIndPharmSci,1997,23:473-481.
• [2]JavittJC ,JavittNB ,McDonnellP .Topicalcompositionsfortheeyecomprsingabeta cyclodextrinderivativeandacarconicanhydlicaraseinhibitor[P].WO :94/15582,1994-06-12.
• [3]ThorsteinnLoftsson,Stef劋nssonE,KristinssonJK ,etal.Topicallyeffectiveacetazolamideeye solutioninman[J].PharmSci,1996,6:277-279.
• [4]LoftssonaT ,J仭rvinenT.Cyclodextrinsinophthalmicdrugdelivery[J].AdvDrugDelRev,1999,36:59-79.
• [5]RojanasakulY ,RobinsonJR .Transportmechanismsofthecornea:characterizationofbarrier permselectivity[J].IntJPharm,1989,55:237-246.
• [6]曾玲,刘宁,傅建.HPLC法测定依诺沙星软膏的含量[J].中国抗生素杂志,1997(4):153-154.
• [7]SaettoneMF ,ChetoniR .Evaluationofocularperme ationenhancers:invitroeffectsoncornealtransportoffourβ blockers,andinvitro/invivotoxicactivity[J].IntJPharm,1996,142:103-113.