渗透促进剂对阿昔洛韦角膜透过性的影响
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张立波，刘志东，李 丁，潘卫三
(沈阳药科大学 药学院，辽宁 沈阳110016)
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。
关键词：药剂学；阿昔洛韦；渗透促进剂；角膜透过性
中图分类号：R94 文献标识码：A
contents
Different effects of penetration enhancers on corneal permeability of aciclovir
ZHANG Li-bo, LIU Zhi-dong, LI Ding, PAN Wei-san
(School of Pharmacy, Shenyang Pharmaceutical University ,Shenyang 110016,China)
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.
Key words: pharmaceutics; aciclovir; osmotic enhancer; corneal permeability
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