Pharmacokinetics of dibenzylamine administered in a sustained drug delivery system with cefazolin.
The pharmacokinetics of dibenzylamine administered in a sustained drug delivery system with cefazolin was studied after i.m. administration of a dose of 1250 mg to healthy volunteers. The serum and urine levels of dibenzylamine were determined by a GLC technique using a specific nitrogen-phosphorus detector. Characterization of the kinetic parameters was performed by applying compartmental and non-compartmental analysis. Dibenzylamine was found to reach concentrations close to 300 ng ml-1 approximately 5 h after administration. The elimination constant had a value of 0.832 +/- 0.821 h-1 (mean +/- S.D.), which is higher than the release constant of the derivative (0.109 +/- 0.072 h-1) (mean +/- S.D.). These results show that release of dibenzylamine may be considered the limiting kinetic process, which governs the elimination of the product from the organism. Only a small amount of dibenzylamine is excreted in urine unchanged 3.43 +/- 3.28 per cent (mean +/- S.D.). Using the pharmacokinetic parameters calculated for dibenzylamine, a prediction has been made of the concentrations reached in a multiple dosage regimen after administration of a dose of 1250 mg every 24 h. The accumulation factor was 1.09.
Calvo
M B
MB
Department of Pharmacy, University of Salamanca, Spain.
Pedraz
J L
JL
Domínguez-Gil
A
A
D000328:Adult; D001596:Benzylamines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002437:Cefazolin / Q000008:administration & dosage; D003692:Delayed-Action Preparations; D004338:Drug Combinations; D006801:Humans; D007273:Injections, Intramuscular; D011292:Premedication
D001596:Benzylamines; D003692:Delayed-Action Preparations; D004338:Drug Combinations; C005051:dibenzylamine; D002437:Cefazolin