阿昔洛韦壳聚糖眼用温敏性原位凝胶的研制及其体外释药研究

目的 制备阿昔洛韦（ACV）壳聚糖（CS）眼用温敏性原位凝胶（ISG）,并对其体外释药特性进行考察.方法 以CS为增黏剂及吸收促进剂,以泊洛沙姆407和188（P407,P188）为基质,制备ACV-CS-ISG,以胶凝温度为指标,筛选P407与P188的最佳配比;采用无膜溶出模型对ACV-CS-ISG的体外释药特性进行考察.结果 当P407与P188的处方用量分别为21%及6%时,ACV-CS-ISG胶凝温度为（33.6±0.4）℃,人工泪液稀释后变为（34.2±0.3）℃,与人眼表温度（34℃）相似;体外释药及凝胶溶蚀均呈现零级动力学特征,且两者相关性良好.结论 ACV-CS-ISG具有理想的胶凝温度及较好的缓释效果,值得进一步研究.

Preparation and drug release in vitro of ocular aciclovir in-situ gels

Objective To prepare ocular aeiclovir （ACV） ehitosan （CS） temperature-sensitive in-situ gels （ISG） and to investigate the drug release profile in vitro. Methods CS as the adhesive and absorption enhaneer,poloxamer 407 and 188 （P407 and P188） as the base,ACV-CS-ISG was prepared. The optimal ratio of P407 and P188 was screened according to the gelation temperature. A membraneless model was used to study the drug release in vitro. Results The optimal ratios of P407 and P188 were 21% and 6% ,respectively. The average gelation temperature before diluted by artifieiul tears was （33.6 ± 0.4）℃, and that after diluted was （34.2± 0.3）℃ ,which was nearly the eye surface temperature of 34℃. Both the drug release in vitro and the gel dissolution of ACV-CS-ISG were fitted zero order kinetics with promising correlation. Conclusion ACV-CS-ISG with promising gelation temperature and the property of sustained drug release in vitro is wluable to be studied further.