摘要
目的采用冷冻干燥法制备注射用醋酸地加瑞克,并对制备工艺进行优化。方法以配液温度、pH值(醋酸水平)、药液残氧量和光照强度为考察因素,以光密度为评价指标,正交实验优化工艺,并对优化后的工艺进行验证。结果注射用醋酸地加瑞克的最佳工艺为:配液温度为(10±2)℃,药液pH值为3.5,配制过程充氮保护,配制及灌装过程应避光。优化后的工艺所得冻干制剂光密度为0.020 AU。本品于40℃、RH 75%(加速试验)条件下放置3个月,光密度、醋酸含量、黏度和含量均无明显变化,且与原研制剂一致。结论优化后的注射用醋酸地加瑞克工艺具有很好的耐用性、可行性及可控性,为冻干制剂的生产工艺的研究提供了实验参考。
OBJECTIVE Degarelix acetate for injection was prepared by freeze-drying method and the process of preparation was optimized.METHODS The solution temperature,pH value(acetic acid level),residual oxygen in solution and the optical density were used as the evaluation indicators.The orthogonal test was used to optimize process.And the optimized process was verified.RESULTS The optimized process of degarelix acetate for injection was determined.The solution temperature was(10±2)℃,the pH value was 3.5,the preparation process was protected by nitrogen,and the preparation and filling process should avoid light.The optical density of formulation obtained from the optimized process was 0.020 AU.There were no significant change in optical density,acetic acid content,viscosity and content after 3 months under the conditions of 40℃/RH 75%(accelerated test).It was consistent with the listed reference drug.CONCLUSION The optimized process of degarelix acetate for injection is very durable,feasible and controllable,which provides experimental reference for the research of lyophilized preparation technology.
作者
黄继玫
刘留成
张金连
HUANG Ji-mei;LIU Liu-cheng;ZHANG Jin-lian(Nanjing University of Chinese Medicine Hanlin College,Taizhou 214500,China;Jiangsu Aosaikang Pharmaceutical Co.,Ltd,Nanjing 211112,China;Hangzhou Haishan Pharmaceutical Equipment Co.,Ltd,Hangzhou 311400,China)
出处
《海峡药学》
2022年第12期18-22,共5页
Strait Pharmaceutical Journal
关键词
注射用醋酸地加瑞克
工艺优化
正交实验
醋酸含量
光密度
Degarelix acetate for injection
Process optimization
Orthogonal test
Acetic acid assay
Optical density
