钩藤碱双层渗透泵控释片的制备及处方优化

Preparation and formulation optimization for double-layer osmotic pump controlled release tablets of rhynchophylline

目的 制备钩藤碱双层渗透泵控释片,并进行处方优化.方法 以释药线性和累积释放度为评价指标,单因素试验考察PEO N750用量、PEO Coagulant用量、PEG 4000用量、包衣增重对体外释药的影响,正交试验优化处方,对体外释药过程进行模型拟合.结果 最优处方为PEO N750用量165 mg,PEO Coagulant用量55 mg,PEG 4000用量8%,包衣增重7%,12 h内累积释放度为93.36%,体外释药符合零级模型(r=0.989 5).结论 双层渗透泵控释片可有效控制钩藤碱体外缓释.

AIM To prepare the double-layer osmotic pump controlled release tablets of rhynchophylline and to perform formulation optimization. METHODS With drug release linearity and accumulative release rate as evaluation indices, single factor test was applied to investigating the effects of PEO N750 consumption, PEO Coagulant consumption, PEG 4000 consumption and coating weight gain on in vitro drug release, orthogonal test was used for formulation optimization, and model fitting was adopted in the in vitro drug release process. RESULTS The optimal formulation was determined to be 165 mg for PEO N750 consumption, 55 mg for PEO Coagulant consumption, 8% for PEG 4000 consumption and 7% for coating weight gain, the accumulative release rate was 93.36% within 12 h. The in vitro drug release accorded with zero-order model(r=0.989 5). CONCLUSION Double-layer osmotic pump controlled release tablets can effectively control the in vitro slow-release of rhynchophylline.