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

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.