酶法制备阿莫西林的工艺优化研究.pdfVIP

．44． 中国抗生素杂志2011年1月第36卷第1期 酶法制备阿莫西林的工艺优化研究 朱科王艳艳丁海平延国东王峰 (石药集团河北中润制药有限公司，石家庄050041) 摘要：目的 酶法合成阿莫西林工艺优化和稳定性研究。方法 利用对羟基苯甘氨酸甲酯为侧链在青霉素酰化酶催化 下，与底物6．氨基青霉烷酸(6．APA)合成阿莫西林；对温度、pH、侧链与底物投料比、投酶量等条件进行优化；取化学法和酶 法阿莫西林进行6个月加速实验，对比含量变化，考察成品稳定性。结果 工艺优化后阿莫西林摩尔收率达84．3％：6个月加速 实验后酶法阿莫西林含量平均下降值比化学法少0．78％。结论酶法阿莫西林工艺流程简单，方法绿色环保，杂质少，产品稳 定性优于化学法。 关键词：阿莫西林；青霉素G酰化酶；稳定性 中图分类号：R378．1文献标识码：A on ofamoxicillin method Studypreparation byenzymatic Zhu and Wang Ke，WangYan·yan，DingHai-ping，YanGuo—dong Feng PharmaceuticalHebei Pharmaceutical 050041) (Shijiazhuang GroupZhongrun Co．，LTD，Shijiazhuang Abstract To the and ofamoxicillin 0bjectivestudyprocessoptimizationstability byenzymaticsynthesis． Theamoxicillinwas withtheuseof esterasasidechain Methods synthesized P．hydroxyphenylglycinemethyl andthesubstrate6．APAin chainandsubstratefeed penicillinacylasecatalyzed；temperature，PH。sideratio， as investmentconditions．suchtheamountof was and amoxicillinwastaken enzymeoptimized；chemicalenzymatic sixmonthsaccelerated content the of Themolar test，comparingchanges，examiningstabilityproducts．Results ofamoxiciilinwas84．3％after sixmonthsacceleratedtest．thecontentof yield processoptimization；after enzymatic amoxicillin an 0．78％lessthanthechemicalmethod．Conclusionamoxiciilin droppedby average Enzymatic of Was was