国产头孢他美酯、头孢他美体内外抗菌作用研究

The in vitro and in vivo antibacterial activity of cefetamet and cefetamet pivoxil

采用琼脂二倍稀释法评价国产头孢他美酯 (cefetamet pivoxil)、头孢他美对临床分离的 5 5 8株致病菌的体外抗菌作用及其对小鼠感染细菌的体内疗效 ,并与进口头孢他美酯、头孢克洛、头孢噻啶、头孢唑林、司帕沙星、环丙沙星进行比较。结果表明 :头孢他美酯体外抗菌活性弱 ,对所试多数革兰氏阳性、阴性细菌的MIC为 4～ >12 8mg/ L,而其母体化合物头孢他美体外呈现出较强的抗菌活性 ,对所试表葡球菌、肺炎链球菌、溶血性链球菌的 MIC5 0 在 0 .0 6～ 8mg/ L(其中包括产 β-内酰胺酶菌株 ) ,对金葡球菌非产酶株和产酶株的MIC5 0 各是 32和 6 4mg/ L;对革兰氏阴性菌中的大肠埃希氏菌 (包括产 β-内酰胺酶菌株 ) ,肺炎克雷伯氏菌、伤寒杆菌、痢疾杆菌、变形杆菌、硝酸盐阴性不动杆菌、普鲁威登斯菌、阴沟肠杆菌、粘质沙雷氏菌及鲍氏不动杆菌等均敏感 ,MIC5 0 在 0 .5～ 8mg/ L;本品对铜绿假单胞菌无效。头孢他美对金葡球菌、表葡球菌的抗菌活力不如第一、二代头孢菌素 ,如头孢噻啶、头孢唑林、头孢克洛 ,但对肺炎链球菌、溶血性链球菌的活力比头孢克洛、头孢噻啶和头孢唑林强 4～ 8倍 ,与司帕沙星、环丙沙星相近。头孢他美对革兰氏阴性杆菌的抗菌活力强于头孢克洛、头孢噻啶 ,头孢唑林 2～ 6 4倍 ,比不上司帕?

The prodrug of cefetamet (CETM), were examined as compared to those of cefaclor (CCL), cefaloridine (CFD), cefazolin (CEZ), sparfloxacin (SPLX), and ciprofloxacin (CPLX). CETM had a broad spectrum of activity against Gram positive and Gram negative bacteria and retained good antibacterial activity against S.epideronidis, S.pneumoniae and S.pysogenes . Its MIC 50 was 0.06~8mg/L (including β lactamase strains), but had poor activity against S.aureus . CETM displayed much better activity against Gram negative bacteria than CCL, CED, CEZ, and similar to those of SPLX and CPLX. The MICs 50 were 0.5~8mg/L against E.coli, Klebsiella, S.typhi, Shigella, Proteus, E.cloacae, S.marcescens and Acinetobacter . Intrapertioneal infection against S.aureus, S.pneumoniae, K.pneumoniae and E.coli in mice,the therapeutic efficacy of cefetamet pivoxil (CETM Pi) was superior to CCL 2~20 times. Results showed that: the in vitro and in vivo antibacterial activity of domestic CETM was similar to that of CETM made in Japan.