Pharmacokinetic studies with dibekacin, a new aminoglycoside, after intravenous and intramuscular administration to human volunteers

Abstract

The pharmacokinetics of dibekacin, a new aminoglycoside antibiotic, was studied in volunteers given the same dose (100 mg) intramuscularly on two separate occasions and intravenously at two different rates of infusion. The kinetic parameters (t 1/2, 2.24 h, and Vd, 0.136 liter/kg, as the overall mean) observed after intramuscular administration appear to be compatible with those of other aminoglycosides and fairly reproducible within the same individuals. Dibekacin was rapidly absorbed (tmax, 0.84 h), yielding a peak level of 10.4 microgram/ml after the 100-mg intramuscular dose. After the 30- or 60-min infusion, the concentrations of dibekacin in serum fell bi-exponentially, giving an elimination half-life (t 1/2 beta) of 2.50 to 2.88 h. The highest serum levels after th 30- and 60-min infusions were 15.2 +/- 0.9 and 12.1 +/- 1.8 microgram/ml, respectively. Serum levels at 6 h after completion of infusions were 1.9 +/- 0.3 and 1.7 +/- 0.4 microgram/ml, respectively.