Comparative pharmacokinetics of sulbactam/ampicillin and clavulanic acid/amoxycillin in human volunteers.
In this study, the pharmacokinetic parameters of 2 different beta-lactamase inhibitors (sulbactam and clavulanic acid) in combination with 2 different aminobenzylpenicillins (ampicillin and amoxycillin) were compared. The study involved 10 healthy volunteers who received sulbactam 250 mg plus ampicillin 500 mg intravenously, clavulanic acid 100 mg plus amoxycillin 500 mg intravenously, sultamicillin equivalent to sulbactam 294 mg plus ampicillin 440 mg orally, and clavulanic acid 125 mg plus amoxycillin 500 mg orally in a crossover, randomised trial. Serum and urine concentrations of ampicillin, amoxycillin and clavulanic acid were assayed by agar diffusion test, and the concentrations of sulbactam by gas chromatography with mass spectrometry. Pharmacokinetic parameters were calculated according to open 1- and 2-compartment models. Test results showed that the addition of sulbactam significantly increases the bioavailability of oral ampicillin when the 2 drugs are administered in the form of the prodrug sultamicillin. Also, sulbactam does not interfere with the kinetics of intravenous ampicillin but increases the absorption of oral ampicillin.
Hampel
B
B
Klinikum Steglitz, Free University of Berlin, West Berlin.
Lode
H
H
Bruckner
G
G
Koeppe
P
P
D000284:Administration, Oral; D000328:Adult; D000658:Amoxicillin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000667:Ampicillin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D002969:Clavulanic Acids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D013407:Sulbactam / Q000008:administration & dosage / Q000493:pharmacokinetics*
D002969:Clavulanic Acids; D000667:Ampicillin; D000658:Amoxicillin; D013407:Sulbactam