注射用米铂制剂配方与冻干工艺研究

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。

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

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.