Phase i studies on BRL 28500 (clavulanic acid-ticarcillin) —Dose response following single intravenous infusion and multiple intravenous infusion studies—

Abstract

As part of a Phase I programme on BRL 28500, a formulation of ticarcillin and clavulanic acid, serum levels and urinary excretion of the components of the drug were determined following intravenous drip infusion in healthy volunteers. 1. BRL 28500 at doses of 1. 6 g, 3. 2 g and 6. 4 g was administered to 11 healthy male volunteers by intravenous drip infusion in cross over fashion and a dose response was found for serum and urinary concentrations. 2. BRL 28500 3.2 g was administered to 4 healthy male volunteers by multiple intravenous drip infusion twice a day for 6 consecutive days. No variation in the serum levels or urinary excretion was observed during administration and there was no significant accumulative tendency. 3. One case of fever and rash following administration of 1.6 g BRL 28500 was observed but disappeared without treatment. From the above results, BRL 28500 was considered to be a safe drug for administration in these doses. © 1986, Japanese Society of Chemotherapy. All rights reserved.