阿托伐他汀钙片的处方工艺优化及质量考察

Preparation and quality control of atorvastatin calcium tablets

目的优化阿托伐他汀钙片的处方工艺。方法处方工艺优化中进行稳定剂、填充剂、黏合剂、崩解剂、润滑剂、增溶剂、初混制粒、干燥工艺、总混工艺、包衣工艺等考察,考察项目为外观性状、溶出度、有关物质、异构体及主药含量等。结果最终选择碳酸钙36 mg/片作为稳定剂,微晶纤维素30.0 mg/片和乳糖60.0 mg/片作为填充剂,10%聚维酮K30水溶液作为黏合剂,交联羧甲基纤维素9.0 mg/片作为崩解剂,硬脂酸镁1.16 mg/片作为润滑剂,聚山梨酯800.5 mg/片作为增溶剂。按优化工艺所制备的中试样品质量稳定可控,关键性能指标均在合格范围内,与原研制剂关键性能指标无显著差异。结论优化的阿托伐他汀钙片处方工艺合理、可行、稳定。

Objective To optimize the formula and preparation of atorvastatin calcium tablets.Methods The stabilizer,filler,binder,disintegrating agent,lubricant,solubilizer,preliminary mixing granulation,drying process,total mixing process,and coating process were tested.The appearance,dissolution,related substances,isomers and main drug content were determined.Results Calcium carbonate(36 mg/tablet)was used as the stabilizer,microcrystalline cellulose(30.0 mg/tablet)and lactose(60.0 mg/tablet)were used as the filler,10%povidone K30 aqueous solution was used as the binder,cross-linked carboxymethyl cellulose(9.0 mg/tablet)was used as the disintegrating agent,magnesium stearate(1.16 mg/tablet)was used as the lubricant,and polysorbate 80(0.5 mg/tablet)was used as the solvent.According to the optimized formula and preparation techniques,the pilot test sample was stable and controllable.The key performance indexes were all within an acceptable range.Compared with the original preparation,there was no significant difference.Conclusion The formula is stable and the preparation of atorvastatin calcium tablets is feasible and reasonable.