Abstract
Serum and urinary concentrations of BRL 28500, a formulation of clavulanic acid (CVA, 1 part) with ticarcillin (TIPC, 15 parts), were determined in normal volunteers and in patients with renal dysfunction (Creatine clearance rate: 23.3-44.9 ml/min). Clinical studies were conducted on BRL 28500 in patients with chronic complicated urinary tract infections.
The fllowoing results were obtained:
(1) Pharmacokinetic studies
1.6 g of BRL 28500 was administered by i. v. infusion. In serum, the peak level and the elimination half life of TIPC were 173.9μg/ml and 0.95 hr. in normal volunteers, and 136.4-185.3μg/ml, 0.96-2.83 hr in renally impaired patients. Corresponding values for CVA were 6.9μg/ml, 0.95 hr. in normal volunteers and 4.3-6.3μg/ml, 1.35-2.08 hr. in patients. In urine, the peak level and the 24 hours recovery rate for TIPC were 9, 395μg/ml, 82.9% in normal volunteers and 1, 971-3, 964μg/ml, 30.8-70.2% in patients, and those of CVA were 501 pernl, 54.0% and 98-206μg/ml, 21.5-42.6% respectively.
(2) Clinical studies
BRL 28500 was administered to 11 patients suffering from chronic complicated urinary tract infections.
The clinical effect was evaluated as excellent in 4 cases, moderate in 3 cases and poor in 4 cases, the overall rate of effectiveness being 63.6%. No side effects was observed, whilst the laboratory findings, three cases of transient elevation of BUN, Cr, GPT and slight leucopenia were observed.
