1984 Volume 32 Issue Supplement4 Pages 142-154
Sulbactam (SBT)/Cefoperazone (CPZ) is a formulation consisting of one part of SBT, a new β-lactamase inhibitor, and one part of CPZ. The antibacterial activity of SBT/CPZ was investigated against 139 strains of clinical isolates of E.coli, Klebsiella sp., Rmirabilis, P.morganii and S. marcescens using CPZ as a control drug. The activity of SBT/CPZ was superior to that of CPZ slightly. A cross over pharmacokinetic study CPZ with and without SBT were carried out in 6 healthy volunteers. The peak serum concentration of CPZ without SBT was 252μ/ml after 5 minute 2g dose administration. The levels was 113.8μ/ml after 1 hour and 9.9μg/ml after 6 hours. The half-life of the drug was calculated to be 1.7 hour. The blood level curve of CPZ with SBT was as same as that of CPZ without SBT. On the other hand, the peak serum concentration of SBT administered lg dose was 128.7μg/ml after 5 minutes and 23.5μg/ml after 1 hour (T/2: 1.2 hour). The urinary excretion rate of CPZ was ca 25% and that of SBT was 85.2% within 8 hours after administration.
Twenty three patients with various infections were treated with lg twice a daily of SBT/CPZ for 7-26 days. The clinical response was excellent in 14 cases, good in 5, fair in one and failure in 3. Overall the efficacy rate was 82.6%. As to the side effect, chest in-comfortability in intravenous injection was occured one patient, and no abnormal laboratory findings were observed.
