头孢氨苄酶法合成影响因素概述  

Research on influencing factors of enzymatic preparation of cephalexin

作　　者：吕娜 牛昆 LüNa;Niu Kun(NCPC New Drug Research and Development Co.,Ltd,Shijiazhuang 050015)

机构地区：[1]华北制药集团新药研究开发有限责任公司,石家庄050015

出　　处：《中国抗生素杂志》2018年第12期1469-1473,共5页Chinese Journal of Antibiotics

摘　　要：头孢氨苄作为第一代口服的头孢菌素类抗生素,对多种革兰阳性菌和革兰阴性菌均有很强的抗菌活性。目前我国制药工业中生产头孢氨苄主要是化学合成法,合成过程步骤繁琐,对环境污染严重。与传统化学合成法相比,生物酶法合成头孢氨苄具有反应条件温和、工艺简便、绿色环保、洁净安全等优点。本文概述了酶法合成头孢氨苄固定化酶的制备,合成过程中各个反应物浓度、温度、pH、投酶量、非水介质对反应转化率的影响以及酶法合成头孢氨苄存在的问题。Cephalexin is a first-generation semi-synthetic oral cephalosporin antibiotic.It has strong antimicrobial activity against a variety of Gram-positive and Gram-negative bacteria.The main methods of industrial preparation of cephalexin are established by chemical synthesis in our country.These synthesis processes are complicated and lead to environmental pollution.Compared with the traditional chemical method,the enzymatic synthesis of cephalexin has the advantages of mild reaction condition,simple process,environmental protection, cleanness,and safety.This review briefly summarized the research progresses of the preparation of immobilized penicillin acylase,the influence of concentrations of reactants,temperature,pH,the amount of enzyme,and the nonaqueous medium on the reaction conversion rate,and problems in enzymatic synthesis.

关 键 词：头孢氨苄 青霉素G酰化酶 酶法合成 

分 类 号：R978.11[医药卫生—药品] TQ460.6[医药卫生—药学]