依度沙班片的处方工艺筛选与优化

Study on the Prescription and Technology of Edaxaban Tablets

目的:立足工业化生产,开发依度沙班片的处方工艺。方法:以原研药依度沙班片溶出曲线作为指标,对处方组成、制备工艺进行筛选,同时对其中关键的因素粘合剂进行优化。结果:最终确定的处方为依度沙班30 mg,甘露醇105 mg,预胶化淀粉45 mg,交联聚维酮8.0 mg,羟丙基纤维素(HPC-SSL)4.0%水溶液适量,欧巴代胃溶型包衣粉增重2%~3%;工艺中关键参数优化结果为湿法制粒时间10 min;依照此法制备得到的依度沙班片与原研品的溶出行为相似。结论:本品处方工艺设计合理,具有可操作性,可以进行大规模的工业化生产。

Objective:Based on industrial production,develop the prescription technology of Edoxaban tablets.Methods:Using the original edoxaban tablet dissolution profile as an indicator,the formulation composition and formulation process were screened,and the key factors of the binder were optimized.Results:The final formulation was edoxaban 30 mg,mannitol 105 mg,pregelatinized starch 45 mg,crospovidone 8.0 mg,hydroxypropyl cellulose(HPC-SSL)4.0%aqueous solution,Coating powder 2%~3%.The optimization result of the key parameters in the process is that the wet granulation time is 10 minutes.The dissolution behavior of edoxaban tablets prepared according to this method is similar to the original research product.Conclusion:The formulation of this product has reasonable design and can be used for large-scale industrial production.