注射用米铂制剂配方与冻干工艺研究

Study on Formulation and Freeze-drying Process of Miriplatin for Injection

关键词:  米铂  冻干工艺  叔丁醇  环己烷

Key words:  miriplatin  freeze-drying process  tert-butyl alcohol  cyclohexane

摘要:

目的 研究注射用米铂的配方及冻干生产工艺。方法 通过冻干溶剂的选择、原料溶解度试验、处方筛选、预冻工艺研究等确定注射用米铂配方和冻干工艺参数的控制范围。结果 确定冻干溶剂采用叔丁醇和环己烷的混合溶剂，环己烷最佳比例范围为10%~30%，药物浓度最佳范围为5~25 mg·mL^-1，确定冻干工艺采用阶段性预冻方式。结论 选定的配方和工艺可行，自研制剂与参比制剂质量等同，节约了工艺生产成本。

Abstract:

OBJECTIVE To study the formulation and manufacturing process of Miriplatin for Injection. METHODS The control range of manufacturing process and formulation were confirmed through choosing the kinds of freeze-drying solvent, solubility study of miriplatin, formulation selection and study on pre-freezing process. RESULTS The mixed solvents of tert-butyl alcohol and cyclohexane were selected to make freeze-drying formulation, the optimum ratio of cyclohexane was in the range of 10%-30%, the optimal drug concentration was in the range of 5-25 mg·mL^-1, stage pre-freezing method was used as final freeze-drying process. CONCLUSION The formulation and manufacturing process is feasible. The self-made drug product is shown the same with and reference listed drug in pharmaceutical aspects. The production cost can be greatly saved compared with the original grinding process.