国产氨苄西林胶囊质量评价

摘要

目的 对国产氨苄西林胶囊的质量现状进行评价.方法 按照国家评价性抽验计划的总体要求,采用现行质量标准检验结合探索性研究,对31家企业的203批次氨苄西林胶囊样品进行统计分析.结果 按现行标准检验,203批次样品全部符合规定;建立了氨苄西林聚合物的测定方法,按USP39规定限值判定样品合格率为99.5％;本品制剂以氨苄西林噻唑酸和氨苄西林聚合物为主要杂质,杂质主要由原料引入,样品中杂质的种类基本一致,但杂质含量及分布有较大变化;不同生产厂家胶囊的溶出行为差异显著,PBPK模型初步预测表明氨苄西林胶囊样品的体外溶出曲线差异对体内吸收未见明显影响,溶出度可能不是影响该药在体内吸收的限速因素.结论 国内氨苄西林胶囊质量总体良好,现行质控标准需进一步完善.建议对原料工艺进行优选,以提高产品质量.%Objective To evaluate the quality status of domestic ampicillin.Methods According to the general requirements of national drug assessment programs,the statutory standard methods and the exploratory research methods were used to analyze 203 batches of ampicillin capsules from thirty-one enterprises.Results The statutory tests showed that 203 bathes of drugs were all qualified.The determination of polymers of ampicillin was established in the exploratory researches.According to the USP39 limits,the qualified rate of the test products was 99.5％.Exploratory research showed that all impurities were mainly from impurities in raw materials,including penicilloic acids of ampicillin and polymers of ampicillin.The kinds of impurities from different batches of different manufacturers were roughly the same,but the distribution and the contents of them had a greater difference;the dissolution behavior in capsules from different manufactures were significant different.The preliminary prediction of PBPK model showed that the dissolution curves of ampicillin capsules in vitro had no significant influence on the in vivo absorption,and the dissolution might not be the speed limiting factor affecting it.Conclusion The quality of domestic ampicillin was generally under good control.However,the quality control specification needs to be further improved.An improvement was put forward to promote the quality by material optimization.