蛇床子素渗透泵控释片制备工艺的优化及其体外释药行为

Preparation optimization for osthole osmotic pump controlled release tablets and the in vitro drug release behaviors

目的优化蛇床子素渗透泵控释片制备工艺,并考察其体外释药行为。方法以Na Cl、聚氧乙烯N80、增塑剂(邻苯二甲酸二丁酯)用量及包衣增重为影响因素,累积释放度综合评分为评价指标,正交试验优化单层渗透泵控释片制备工艺;以聚氧乙烯N80、聚氧乙烯N60K、致孔剂(聚乙二醇4000)用量及包衣增重为影响因素,累积释放度综合评分为评价指标,正交试验优化双层渗透泵控释片制备工艺。然后,比较这2种渗透泵控释片的体外释药行为。结果单层渗透泵控释片最佳处方为Na Cl用量105 mg/片,聚氧乙烯N80用量95 mg/片,增塑剂用量8%,包衣增重6.5%,综合评分16.3;双层渗透泵控释片最佳处方为聚氧乙烯N80用量150 mg/片,聚氧乙烯N60K用量70 mg/片,致孔剂用量8%,包衣增重4.0%,综合评分13.5。单层、双层渗透泵控释片体外释药行为均符合零级方程,后者累积释放度高于前者。结论蛇床子素双层渗透泵控释片体外释药更完全。

AIM To optimize the preparation for osthole osmotic pump controlled release tablets and to investigate the in vitro drug release behaviors.METHODS With consumption of NaCl,polyethylene oxide N80,plasticizer(dibutyl phthalate),and coating weight gain as influencing factors,comprehensive score for accumulative release rate as an evaluation index,orthogonal test was applied to optimizing the preparation of single-layer osmotic pump controlled release tablets.With consumption of polyethylene oxide N80,polyethylene oxide N60K,poreforming agent(polyethylene glycol 4000),and coating weight gain as influencing factors,comprehensive score for accumulative release rate as an evaluation index,orthogonal test was applied to optimizing the preparation of double-layer osmotic pump controlled release tablets.Subsequently,the in vitro drug release behaviors of these two osmotic pump controlled release tablets were compared.RESULTS The optimal formulation for the single-layer osmotic pump controlled release tablets was determined to be 105 mg/tablet for NaCl consumption,95 mg/tablet for polyethylene oxide N80 consumption,8%for plasticizer consumption,and 6.5%for coating weight gain,the comprehensive score was 16.3.The optimal formulation for the double-layer osmotic pump controlled release tablets was determined to be 150 mg/tablet for polyethylene oxide N80 consumption,70 mg/tablet for polyethylene oxide N60K consumption,8%for porerelease tablets accorded with zero-order equations,and the latter demonstrated a higher accumulative release rate than the former.CONCLUSION Osthole double-layer osmotic pump controlled release tablets display more complete drug release.forming agent consumption,and 4.0%for coating weight gain,the comprehensive score was 13.5.The in vitro drug release behaviors of single-layer and double-layer osmotic pump controlled