摘要
目的优化磷酸特地唑胺片的制备工艺,并进行工业化生产。方法制备工艺采用流化床制粒,随后压片、包衣的工艺流程。对关键性辅料粘合剂、崩解剂及原料药粒度、素片硬度和包衣增重等进行优化,并对优化后处方进行放大生产。结果最终确定处方为磷酸特地唑胺200 mg、微晶纤维素78 mg、甘露醇78 mg、聚维酮K3016 mg、交联聚维酮12 mg(内加)、交联聚维酮12 mg(外加)、硬脂酸镁4 mg、薄膜包衣预混剂16 mg,制粒工艺为流化床制粒,润湿剂为纯化水。结论本品制备工艺简单,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 preparation process of tedizolid phosphate tablets and to carry out industrial production.Methods The preparation process was fluidized bed granulation followed by tableting and tablet coating.The key excipients such as binder,disintegrant,particle size of API,tablet hardness and coating weight gain were optimized,and the optimized formulation was scaled-up for production.Results The composition of final formulation was as follows:tedizolid phosphate 200 mg,microcrystalline cellulose 78 mg,mannitol 78 mg,povidone K3016 mg,crospovidone 12 mg(internal),crospovidone 12 mg(external),magnesium stearate 4 mg,and coating materials 16 mg.The granulation process was fluid-bed granulation with purified water as the wetting agent.Conclusion The 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.
作者
陈中亚
王群
拥青她姆
CHEN Zhongya;WANG Qun;YONGQING Tamu(Jiangsu Hansoh Pharmaceutical Group Co.,Ltd.,Lianyungang 222000,China)
出处
《中国药剂学杂志（网络版）》
2022年第6期213-223,共11页
Chinese Journal of Pharmaceutics：Online Edition
基金
江苏省科协青年科技人才托举工程项目(2019年度)。
关键词
磷酸特地唑胺片
质量评价
流化床制粒
溶出曲线
tedizolid phosphate tablets
quality evaluation
fluid-bed granulation
dissolution curve
