盐酸奥昔布宁微孔渗透泵控释片的制备及其处方优化

Preparation and optimization of oxybutynin hydrochloride microporous membrane osmotic pump tablets

目的:制备盐酸奥昔布宁微孔渗透泵控释片,考察其体外释放度,并筛选出最佳处方。方法:以体外累积释放度为评价指标,分别考察渗透泵片的促渗剂含量,致孔剂含量以及包衣增重的改变对其体外释放的影响,采用响应面法优化处方,从而确定出最佳处方。结果:该控释片的体外释药由渗透压驱动的,片芯促渗剂的含量,致孔剂的用量,包衣增重对于释药行为有显著影响。结论:中心复合设计法优化的处方制备的控释片释放度符合要求,药物释药行为符合零级释放。

Objective： To develop a microporous-controlled delivery system for oxybutynin hydrochloride, to investigate the drug release in vitro, and to determine the best formulation eventually. Methods： The cumulative release was used as an evaluating index, the amount of penetration enhancer and pore-forming agents as well as thickness of coating were assessed to study the impacts on the drug release in vitro. The response surface methodology was employed to optimize formulations in terms of three variables. Results： The drug release was driven by the osmotic pressure, and the three variables mentioned above had a significant effect on the release rate. Conclusion ： The release rate of controlled-release tablets prepared by the optimized formulations fulfilled the requirements; furthermore, the release profile matched the zero-order release characteristics well.