辛苯聚醇温敏凝胶的制备及其体外释放研究  

Preparation and in vitro release of octoxynol-9 thermosensitive in situ gel

作　　者：袁萍[1,2] 陈鹰[1] 刘丽娜[1,2] 

机构地区：[1]广州军区武汉总医院药剂科,湖北武汉430070 [2]湖北中医药大学药学院,湖北武汉430065

出　　处：《中国医院药学杂志》2017年第14期1352-1356,共5页Chinese Journal of Hospital Pharmacy

基　　金：湖北省卫生和计划生育委员会科研项目(编号:WJ2015MB115)

摘　　要：目的:制备辛苯聚醇阴道用温敏凝胶[(O-9)-VTG],并对其释放机制进行探讨。方法:采用冷溶法以泊洛沙姆407(P407)和泊洛沙姆188(P188)为温敏凝胶材料制备凝胶,倒置法测定其胶凝温度(TGEL),再应用星点设计-效应面法优化处方,并采用无膜溶出模型考察其体外溶蚀及释药情况。结果:优化的处方基质配比为P407∶P188∶甘油∶壳聚糖=16.3∶5.7∶5∶0.6,胶凝温度为33℃,胶凝时间约1.6 min;辛苯聚醇体外释放符合零级动力学方程。结论:效应面法筛选辛苯聚醇温敏凝胶处方合理,(O-9)-VTG作为新型阴道用避孕制剂前景良好。OBJECTIVE To prepare octoxynol-9 vaginal thermosensitive in situ gel（（O-9）-VTG）and research its in vitro release.METHODS（O-9）-VTG was prepared with P407 and P188 in cold dissolving method.Tube inversion method was used to measure the TGELand RSM plus CCD was used to design formulation.Membraneless dissolution model was selected to determine gel erosion and in vitro release of（O-9）-VTG.RESULTS Optimized formulation was confirmed as 16.3% P407,5.7% P188,5% glycerin and 0.6%chitosan.The observed TGELof optimized formulation was 33 ℃and the gelation time was about 1.6 min.The in vitro release study indicated that drug release of octoxynol-9 was best fitted to zero order kinetics.CONCLUSION RSM plus CCD method is reasonable to design formulation and（O-9）-VTG may be a promising vaginal contraceptive preparation.

关 键 词：辛苯聚醇 温敏凝胶 含量测定 体外释放 

分 类 号：R943[医药卫生—药剂学]