冻干注射剂中辅料选择的考虑

目的通过阐述冻干注射剂辅料选择的基本考虑,为药学开发提供借鉴和思考。方法汇总了近年来FDA已上市化药冻干注射剂的辅料使用情况,包括辅料组成、FDA收载的最大辅料用量等,论述冻干注射剂辅料选择需重点考虑的问题。结果已上市冻干注射剂中有四分之一不使用辅料,而使用最多的辅料类别分别是冻干赋形剂、缓冲盐和pH调节剂,其他辅料包括增加溶解的辅料、抗氧剂等。结论冻干注射剂辅料的选择要重点考虑安全性、处方合理性、功能性指标及辅料控制方面的问题。

Consideration of Excipient Selection in Freeze-dried Injections

OBJECTIVE To provide reference and consideration for pharmaceutical development by expounding the basic considerations for the selection of freeze-dried injection excipients.METHODS The excipients in freeze-dried injections approved by FDA in recent years have been listed,and the composition of excipients in the preparations and the maximum amount of excipients contained were summarized.The issues to be considered in the selection of freeze-dried injections were discussed.RESULTS One quarter of the freeze-dried injections that have been marketed do not use excipients,while the most commonly used excipients are bulking agents,buffering agents and pH adjusters.Other excipients include solubilizing agent,antioxidants,etc..CONCLUSION The selection of freeze-dried injection excipients should focus on safety,formulation rationality,functionality-related characteristics and control of excipients.