辛苯聚醇温敏凝胶的制备及其体外释放研究

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（T_GEL），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。

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

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 T_GEL and 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 T_GEL of 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.