Abstract
BRL 25000 is a formulation consisting of 2 parts of amoxicillin (AMPC) and 1 part of clavulanic acid (CVA). The antibacterial activity of BRL 25000 was investigated against clinical isolates of S. aureus, E. coli, K. pneumoniae, Proteus sp. and Bacteroides sp. using amoxicillin as a control drug, and the activity of BRL 25000 was superior to that of amoxicillin.
A cross over study with 187.5 and 375 mg BRL 25000 was carried out in 6 healthy volunteers and the serum concentrations and urinary excretion of AMPC and CVA were studied, respectively. The peak serum concentration of AMPC was 2.5 and 5.6μg/ml, and that of CVA was 1.4 and 3.1μg/ml.
The urinary excretion rate of AMPC was 64.6 and 67.0%, and that of CVA was 46.9 and 46.0% within 8 hours after administration. The serum and urine concentration ratio between AMPC and CVA was similar to that of the administration ratio.
Forty five patients with various infections were treated with 3 or 4 tablets daily of BRL 25000 (375 mg). The clinical response was excellent in 21 cases, good in 18 cases, fair in 3 cases and poor in 3 cases. Overall the efficacy rate was 87.0%.
Gastro intestinal side effects were observed in 3 cases. Two cases of elevated GPT and 1 eosinophilia were noted in the laboratory findings.
