利伐沙班片溶出区分介质的筛选

Selection of dissolution medium of rivaroxaban tablets

目的获得最具有区分效应的利伐沙班片体外溶出介质。方法从药物溶解性、体外溶出度、药代特性等指标综合考量,筛选出能区分原料粒径、处方及工艺的平滑溶出曲线及溶出介质。结果利伐沙班片在0.05%十二烷基硫酸钠(pH=4.5)及0.05%十二烷基硫酸钠(pH=1.0)中,溶出曲线平滑上升,45 min释放度大于85%。结论该两种溶出介质最具有区分能力,可作为本品仿制药研发过程中处方工艺筛选的关键溶出介质。

Objective To obtain the most effective dissolution medium for rivaroxaban tablets in vitro. MethodsWe comprehensively considered the drug solubility, dissolution rate and pharmacokinetics to screen smooth dissolution curve and dissolution medium that can distinguish the size, formulation and technology of raw material. Results The dissolution curves of rivaroxaban tablets in 0.05% sodium dodecyl sulfate(pH = 4.5) and 0.05% sodium dodecyl sulfate(pH = 1.0) dissolution medium increased smoothly, and the dissolution at 45 min was greater than 85%. Conclusion The two dissolution media have the most distinguishable ability to screen the prescription and process during the research and development of generic drugs.