[Bone and blood levels of azlocillin after intra-arterial injection in the dog].
Pharmacokinetic values of azlocillin--a semisynthetic penicillin of the ureidopenicillin family--were determined in dogs after injection of the drug into the right femoral artery by measuring plasma concentrations in the right femoral artery and left femoral vein and tissue concentrations in ipsi- and contralateral bones. Two different doses of azlocillin were administered, one group of dogs receiving 100 mg X kg-1 by fast (1 min) bolus injection and the other group receiving 250 mg X kg-1. The drug was assayed by high performance liquid chromatography in reverse phase, which proved to be the simplest, most rapid and most sensitive method. Changes in plasma and bone tissue concentrations after intra-arterial injection were interpreted as order one kinetics with a two-compartment open model. Following the 100 mg/kg dose, concentrations versus time corresponded to the following equations: --Arterial blood (mg/l) = 7570 e-0.15 t (min) + 240 e-0.017 t --Venous blood (mg/l) = 553 e-0.13 t + 222 e-0.016 t --Bone tissue (micrograms/g) = 15 e-0.0115 t (elimination phase). Distribution and elimination constants were identical in arterial and venous blood. Distribution half-life was 5 +/- 1 min in arterial blood and biological half-life was 42 +/- 11 min. However, bioavailability was comparatively lower in veins due to higher levels in arteries during the distribution phase. Bone tissue concentrations were much lower than plasma concentrations and were identical on both sides despite high arterial levels on the ipsilateral side during the distribution phase. Bone concentrations diminished rapidly and elimination kinetic values were the same in bone and in plasma. It is concluded that bone tissue concentrations of azlocillin after intra-arterial injection are highest during the distribution phase.
D000818:Animals; D001390:Azlocillin; D001842:Bone and Bones / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D004285:Dogs; D005260:Female; D005263:Femoral Artery; D005268:Femoral Vein; D007269:Injections, Intra-Arterial; D007700:Kinetics; D008297:Male; D010406:Penicillins / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D014018:Tissue Distribution
D010406:Penicillins; D001390:Azlocillin
Taux osseux et sanguins de l'azlocilline après injection intra-artérielle chez le chien.