国产注射用磺苄西林钠的质量评价

Quality assessment of domestic sulbenicilin sodium for injection

目的评价国内不同企业生产的注射用磺苄西林钠的质量。方法按国家标准检验与探索性研究相结合,对抽验样品进行检验,对检验结果进行统计分析。结果共抽取样品72批次,按国家标准检验合格率100%。探索性研究对磺苄西林D/L异构体的抑菌活性进行评价,结果反映D(-)磺苄西林的抑菌活性强于L(+)磺苄西林;结合有关物质检查法与稳定性研究,对主要杂质的来源与结构进行研究;通过检验项目结果间关联分析,明确水分对注射用磺苄西林钠的有关物质及聚合物均有影响;结论目前国内注射用磺苄西林钠的总体质量较好;现行标准有待进一步提高,建议现行标准增加磺苄西林对映体检查、提高水分限度要求、收录磺苄西林降解杂质结构信息;建议企业对原料工艺进行优选,以提高产品质量。

Objective To evaluate the quality status of domestic sulbenicilin sodium for injection. Methods According to the general requirements of national drug assessment programs, using statutory testing methods and combining with the exploratory research to examine sample and evaluate the quality status of sulbenicilin sodium for injection by statistical analysis of the results. Results Statutory tests showed 72 batches of samples were all qualified. The exploratory research results showed that the dextrorotatory enantiomer （D-） of sulbenicilin had more obvious antibacterial activity than the laevoisomer （L＋）, The principal impurities were characterized and the origination of the impurities were deduced by the examination of related substances and the stability study. The moisture content had an important effect on the related substances and the polymer of sulbenicilin. Conclusion At present, the quality of domestic sulbenicilin sodium for injection meets the requirements of the current statutory standard. The current statutory standard should be further improved by increasing the examination of sulbenicilin enantiomer, improving the limit of moisture content, including the information of impurity structures. An improvement was put forward to promote the quality by material optimization.