罗沙司他胶囊的制备及其初步质量评价

Preparation and preliminary quality evaluation of roxadustat capsules

目的优化罗沙司他胶囊的处方和制备工艺并进行批量放大生产。方法采用高剪切湿法制粒工艺,与参比制剂进行体外溶出曲线对比,以相似因子(f 2)为考察指标,筛选原料粒径、崩解剂和粘合剂用量及加入方式,得到优选的处方和制备工艺,并进行批量放大生产。结果罗沙司他胶囊优选的处方为:罗沙司他50 mg,乳糖289.8 mg,微晶纤维素9.36 mg,交联羧甲纤维素钠1.8 mg(内加),聚维酮5.4 mg(外加),硬脂酸镁3.6 mg,以纯化水为粘合剂溶剂。结论本品处方和制备工艺简单,放大生产显示工艺稳定,重现性好,同时体外多介质溶出曲线与原研制剂相似。

Objective To optimize the formulation and preparation process of roxadustat and conduct scale-up production.Methods The dissolution profile in vitro was compared with that of the reference product,using the high shear wet granulation process.With the similarity factor(f 2)as the evaluation index,the particle size of active pharmaceutical ingredient,the amount of disintegrant and binder and the way of addition were screened to obtain the optimal formulation and preparation process,and the batch scale-up production was carried out.Results The optimized formulation of roxadustat capsules was as follows:roxadustat 50 mg,lactose 289.8 mg,microcrystalline cellulose 9.36 mg,croscarmellose sodium 1.8 mg(internal),povidone 5.4 mg(external),magnesium stearate 3.6 mg and purified water as binder solvent.Conclusion The formulation and preparation process is simple and the scale-up production shows that the process is stable and the reproducible,and the dissolution curve in vitro is similar to that of the reference product.