FUNDAMENTAL AND CLINICAL STUDIES ON LENAMPICILLIN (KBT-1585) IN THE SURGICAL FIELD
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Basic and clinical studies were conducted on a new ampicillin prodrug lenampicillin (KBT-1585) and the following results were obtained.<BR>Orally administered KBT-1585 has an activity as ampicillin in the body, and the antibacterial activity of ampicillin to clinical isolates was studied. Antibacterial activity of ABPC to coagulase positive <I>Staphylo</I>. cc. and coagulase negative <I>Staphylo</I>. cc. were examined, and proved to be equal to AMPC and more potent than CEX and CCL. ABPC showed strong activity to <I>S. faecalis</I>and moderate activity to <I>B. fragilis</I>. However, almost all strains of <I>K. pneumoniae, E. cloacae</I>and <I>P. aeruginosa</I> were resistant to it.<BR>KBT-1585 (500 mg) was administered orally without meal to three healthy adults and their mean peak serum level was 16.3 μg/ml at one hour after administration, afterward the level rapidly decreased, and mean serum level of 0.3μg/ml was at 4 hour after administration.<BR>KBT-1585 was administered to 37 cases of surgical infections mainly skin and soft tissue infections. The overall effective rate was 81.1%. No side effect or abnormal laboratory findings were observed except one case of slight nausea.
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