西他沙星片制备与工艺放大研究

Study on preparation and process pcale-up of Sitafloxacin Tablets

目的 优选西他沙星片处方工艺,通过数学模型确定放大工艺参数。方法 以体外溶出相似性(相似因子f2≥50)为评价指标筛选处方工艺,通过数学模型确定放大工艺参数。结果 制剂配方为西他沙星片50 mg,甘露醇50 mg,玉米淀粉36 mg,低取代羟丙纤维素18 mg,硬脂酸镁1 mg,3%的羟丙基纤维素水溶液适量,薄膜包衣预混剂(欧巴代),包衣增重3%;关键工艺参数为制粒转速80 r/min,制粒时间2 min。结论 所开发的西他沙星片与原研药体外溶出曲线相似,处方、工艺参数合理,可用于指导西他沙星片商业化生产。

Objective To optimize the formula process of Sitafloxacin Tablets, and determine its scale-up of process parameters through mathematical models. Methods The in vitro dissolution similarity(similarity factor f2≥50) was used as the evaluation index to screen the prescription process, and the scale-up process parameters were determined by mathematical model. Results The preparation formula was Sitafloxacin 50 mg, mannitol 50 mg, corn starch 36 mg, lowsubstituted hydroxypropylcellulose 18 mg, appropriate amount of 3% hydroxypropyl cellulose aqueous solution, magnesium stearate 1 mg, film coating premix(Opadry), the coating weight gain was 3%;the key processing parameters were the granulation speed of 80 r/min, the granulation time of 2 min. Conclusion The developed sitafloxacin tablets are similar in vitro dissolution curve of the original drug, and the prescription and process parameters are reasonable, which can be used to guide the commercial production of sitafloxacin tablets.