论文部分内容阅读
目的制备大剂量难溶性药物尼美舒利双层渗透泵片,并考察其处方因素和体外释放行为,优化尼美舒利双层渗透泵的处方。方法以12 h药物累积释放量、释放曲线的线性为考察指标,以含药层聚氧乙烯量、包衣膜中致孔剂量、包衣增质量,为考察的主要因素,采用星点设计-效应面法对尼美舒利渗透泵片处方进行优化,并对优化处方进行验证。结果成功找到了最优释药区域,优化处方为:含药层聚氧乙烯220.27 mg,致孔剂用量质量分数为19.27%,包衣增质量6.81%。自制渗透泵与预测值基本一致,2~12 h内药物呈零级释放特征。结论星点设计-效应面法成功建立了处方优化模型,实现了尼美舒利双层渗透泵的处方筛选。
Objective To prepare a large dose of poorly soluble drug nimesulide double osmotic pump tablets and investigate the prescription factors and in vitro release behavior and optimize the prescription of nimesulide double-layer osmotic pump. Methods The cumulative release amount of 12 h and the linearity of the release curve were taken as the indexes. Taking the amount of polyoxyethylene in the coating layer, the amount of porogen in the coating film and the quality of the coating as the main factors, The response surface method was used to optimize the prescription of nimesulide osmotic pump tablets and validate the optimized prescription. Results The optimal drug release region was successfully found. The optimal formulation was as follows: 220.27 mg of polyoxyethylene containing drug layer, 19.27% of porogen and 6.81% of coating weight. Self-made osmotic pump and the predicted value is basically the same, 2 ~ 12 h within a zero-order release characteristics of the drug. Conclusions The star design-response surface method has successfully established a prescription optimization model and achieved the prescription screening of nimesulide dual-layer osmotic pump.