Abstract
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 300ng ml^−1^ approximately 5h 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 24h. The accumulation factor was 1·09.