【摘要】 目的研究阿昔洛韦(ACV)的角膜透过性,为其处方设计提供理论基础。方法采用体外扩散的实验方法,在多种渗透促进剂条件下,考察阿昔洛韦在离体兔眼角膜中的透过性。结果 1%(w)的泊洛沙姆F127和2%(w)羟丙基‐β‐环糊精分别使ACV的表观渗透系数增加1.70和1.72倍,与对照组呈现显著性差异(P<0.01),而0.05%(w)月桂氮卓酮Aznoe和0.5%(w)乙二酸四乙酸二钠(EDTA)未能显著增大ACV的表观渗透系数(P>0.05);所有渗透促进剂均未显著改变ACV透过角膜的滞后时间;0.05%(w)Azone和1%(w)F127对眼组织具有刺激性。结论 2%(w)羟丙基‐β‐环糊精能够显著增加ACV的表观渗透系数,且对角膜无明显刺激性。更多还原

【Abstract】 Objective To explore the corneal permeability of aciclovir(ACV) in vitro. Methods The permeation characteristics of ACV across isolated cornea of rabbit were studied in vitro using a variety of osmotic enhancers. Results 1%(w) poloxamer (F127) and 2%(w)HP-β-CD showed a significant increment of as much as 1.70 and 1.72 times in the apparent corneal permeability of ACV, respectively,comparing with that of the control(P<0.01). However, 0.05%(w) azone and 0.5%(w) EDTA did not improve the apparent permeability of ACV significantly. The enhancers insignificantly changed the lag time pertinent to the corneal permeability. 1%(w) poloxamer (F127) and 0.05%(w) azone were irritable to eye tissues.Conclusion 2%(w) HP-β-CD servers the corneal apparent permeability of ACV better.更多还原