贝前列素钠缓释片制备及体外释放研究

Preparation and in vitro dissolution study on beraprost sodium sustained release tablets

目的制备非pH依赖性的贝前列素钠缓释片。方法筛选处方中pH调节剂种类、pH调节剂用量、缓释材料用量,与参比制剂对比研究pH 1.2盐酸溶液和pH 6.8磷酸盐缓冲液中的释放曲线,采用f2相似因子比较体外释放行为,利用星点设计试验优化得到最佳处方。结果采用7.07%的枸橼酸作为pH调节剂、54.47%的聚醋酸乙烯/聚乙烯吡咯烷酮共聚物作为缓释材料,可获得非pH依赖性的释放曲线,且释放曲线与参比制剂相似(f_(2)>50)。结论pH调节剂在缓释制剂中可调控微环境pH值,使贝前列素钠实现非pH依赖性的释放行为。

s:Objective To prepare pH independent sustained-release tablets of beraprost sodium.Method The types and the contents of pH regulators,and the content of sustained-release materials in the formulation were screened.The dissolution curves in pH 1.2 hydrochloric acid solution and pH 6.8 phosphate buffer solution were compared with the reference preparation.In vitro dissolution behavior was compared using the f2 similarity factor,and the optimal formulation was optimized using central composite design.Results Using 7.07%citric acid as pH regulator and 54.47%polyvinyl acetate-polyvinylpyrrolidone mixture as sustained-release material,pH independent dissolution curve can be obtained,and the dissolution curve was similar to the reference preparation(f_(2)>50).Conclusion The pH regulators can control the pH value of the microenvironment in sustained-release formulations,thus enabling the pH dependent release behavior of beraprost sodium with pH independent.