摘要
目的探讨替格瑞洛仿制片的制备方法及其工艺稳定性,为实现工业化生产提供科学依据。方法以原研制剂(倍林达?)为参比制剂,以溶出曲线为评价指标,通过对溶出相似因子f2的比较,对片剂原料药的粒径、辅料稀释剂、崩解剂和黏合剂的用量进行了筛选,确定处方组成。放大制备3批替格瑞洛仿制片,考察3批自制替格瑞洛片剂样品和原研片在4种不同溶出介质中的溶出一致性,以评估其工艺质量稳定性。结果替格瑞洛仿制片处方为:替格瑞洛90 g、甘露醇120 g、磷酸氢钙60 g、羧甲基淀粉钠10 g、羟丙基纤维素8 g、硬脂酸镁3 g,包衣增重3%。3批自制片与原研片在不同溶出介质中f2均大于50,稳定性较好。结论替格瑞洛片制备工艺稳定且自制制剂与参比制剂在不同溶出介质中的体外溶出行为一致。
Objective To explore the preparation technology and process stability of generic Ticagrelor Tablets. Methods Using the original preparation (Brilinta?) as the reference drug, taking the dissolution curve as the evaluating indicator, the dissolution similarity factors (f2) were compared, and the formulation was determined by systematic optimization of the factors including the particle size of raw materials and the amount of excipient diluent, disintegrating agent and adhesive. Afterwards, 3 batches of Ticagrelor Tablets were prepared for investigation of the dissolution consistency of the selfmade preparation and original preparation in 4 different dissolution media. Results The formulation of generic Ticagrelor Tablets was as follows: ticagrelor 90 g, mannitol 120 g, calcium hydrogen phosphate 60 g, sodium carboxymethyl starch 10 g, hydroxypropyl cellulose 8 g, magnesium stearate 3 g, and the coating weight was 3 %. Moreover, all the f2 values between the original preparation and the generic preparation were all greater than 50 in different dissolution media. Conclusion The preparation process of generic Ticagrelor Tablets is stable. Moreover, the dissolution behavior of the generic preparation is similar with that of original preparation.
作者
赵文聪
ZHAO Wen-cong(Pharmacy Department, Women & Infants Hospital of Zhenzhou, Zhengzhou 450053, China)
出处
《食品与药品》
CAS
2019年第1期65-70,共6页
Food and Drug
关键词
替格瑞洛
溶出曲线
相似因子
稳定性
ticagrelor
dissolution profile
similar factor (f2)
stability
