• Archives of Pharmacal Research
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• 제19권1호
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• pp.46-51
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• 1996

The in vitro activity of LB 10517, a new catechol-substituted cephalosporin, was compared with those of E-1077, cefpirome and ceftazidime 1034 clinical isolates collected in Japan. LB10517 showed a broad-spectrum antibacterial activity against a wide range of grampositive and gram-negative bacteria including non-glucose fermenting rods, Pseudomonas aeruginosa. Against the methicillin-susceptible strains of Staphylococcus aureus (MSSA) and Strptoccus pyogenes, the $MIC_{90}$ values of LB10517 which required to inhibit 90% of the strains wre $3.13\mug/ml\; and\; 0.1\mug/ml$, respectively. It was as active as E-1077 but more active than cefpirome and ceftazidime. Methicillin-resistant strains of S.aureus (MRSA) and Enterococcus spp. were highly resistant to all the test compunds. LB10517 was highly active against most members of the family Enterobacteriaceae, 90% of which were inhibited at a concentration of less than $0.78\mug/ml$, except for Enterobacter cloacae ($1.56\mug/ml$) and Serratia marcescens ($3.13\mug/ml$)Its activity was comparable to those of E-1077 and cefpirome but it was greater than that of ceftazidime. Against Pseudomonas aeruginosa, LB10517 showed the most potent antibacterial activity among the compounds tested. Ninety percent of P. aeruginosa isolates were susceptible at the concentration of $0.39\mug/ml$. Its activity was 32-to 128 fold higher than those of E-1077, cefpirome and ceftazidime. Against imipenem- or ofloxacin-resistant P. aeruginosa, LB10517 with $MIC_{90}\; of\; 6.25 \\mug/ml\; and\; 3.13\mug/ml$, respectively, showed 16-fold more potent activity than the other test compounds. LB10517 showed a relatively high plasma level and long plasma elimination half-life in rats $(t_{1/2}(\beta,\; 52 min)\; and\; dogs\; (t_{1/2}(\beta),\; 103 min)$.