处方设计及冻干工艺对注射用盐酸吡柔比星稳定性的影响  

Effects of Formulation Design and Freeze-drying Process on Stability of Pirarubicin Hydrochloride for Injection

作　　者：杜加秋 董福霞 蔡邱华 易芬芬 邵婷婷 DU Jiaqiu;DONG Fuxia;CAI Qiuhua;YI Fenfen;SHAO Tingting(Hanhui Pharmaceutical Co.,Ltd.,Hangzhou 311400,China)

机构地区：[1]瀚晖制药有限公司,杭州311400

出　　处：《中国现代应用药学》2022年第15期1979-1983,共5页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的 制备盐酸吡柔比星冻干制剂,考察处方设计及冻干工艺对产品质量的影响。方法 采用冻干工艺制备注射用吡柔比星,分别考察赋形剂种类和用量、中间体配液pH值控制及冻干曲线设计对吡柔比星稳定性的影响。结果 通过处方和工艺筛选,选择乳糖作为赋形剂,最优处方赋形剂用量为每瓶90 mg,最优成盐pH值为3.7~3.9,中间体pH控制范围在5.0~6.0内无显著性差异,预冻工艺选择先迅速降温至–50℃后再升温至–20℃,继续降温至–50℃的退火程序,2次干燥时间为600 min时产品水分为0.3%,继续延长时间水分不再下降。结论 通过处方和工艺筛选,确定了最优处方工艺。OBJECTIVE To prepare pirarubicin hydrochloride freeze-dried preparation and investigate the effects of prescription design and freeze-drying process on product quality.METHODS Pirarubicin hydrochloride was prepared by freeze-drying process.The effects of the type and dosage of excipients,pH control of intermediate solution and freeze-drying curve design on related substances or moisture content were investigated.RESULTS The optimal dosage of lactose was 90 mg per bottle,the optimal pH value of salt formation was 3.7-3.9.There was no significant difference in the pH control range of 5.0-6.0 for intermediate.The pre-freezing process was to rapidly reduce the temperature to –50 ℃,then increase the temperature to –20 ℃ and continue to cool down to –50 ℃.When the second drying time was 600 min,the moisture content was 0.3%,and the moisture content would not drop again with longer time of second drying.CONCLUSION The optimal prescription process is determined by screening the prescription and process.

关 键 词：盐酸吡柔比星 注射剂 冻干曲线 配液工艺 处方设计 

分 类 号：R943[医药卫生—药剂学]