[Evaluation of the biliary excretion of a ticarcillin-clavulanic acid combination in man].
The association of a beta-lactamase inhibitor, clavulanic acid (CA) (0.2 g) to ticarcillin (TIC) (3 g) enhances the activity of the latter on resistant strains. The aim of the present study was to assess their biliary elimination in man. Serum, urine and bile concentrations of TIC and CA were measured in biological samples collected in 10 cholecystectomized patients provided with a T-tube, during 12 hours after the IV administration of 3.2 g of claventin. Concerning TIC, a mean biliary peak of 177 +/- 49 (SEM) micrograms/ml was reached during the 2nd hour; the total biliary output (0-12 h) (AB) was 8.8 +/- 2.6 mg (0.28% of the administered dose), the hepato-biliary clearance CL HB 0.34 ml/min and the biological half-life, TB 1/2 1.2 h. The mean biliary peak of CA was 2.7 +/- 0.5 micrograms/ml and occurred during the first hour. AB amounted to 98.5 +/- 34.7 micrograms (0.04% of dose), CLHB to 0.10 ml/min and TB 1/2 1.2 h. In per-operatively sampled serum, choledochal bile, gallbladder bile and gall-bladder wall, the following concentrations were measured 1 hour after the IV administration of 3.2 g of Claventin. TIC: 105 +/- 11; 386 +/- 66; 72 +/- 20 micrograms/ml and 36 +/- 11 micrograms/g. CA: 3.6 +/- 0.7; 5.9 +/- 1.5; 0.3 +/- 0.3 micrograms/ml and 0.1 +/- 0.1 micrograms/g. The biliary pharmacokinetic profiles allow to favorably consider the prophylactic use of Claventin in the surgery of the biliary tract as well as its therapeutic administration in biliary tract infections.
D000328:Adult; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics; D001419:Bacteria / Q000187:drug effects; D001646:Bile / Q000378:metabolism*; D002763:Cholecystectomy; D002851:Chromatography, High Pressure Liquid; D019818:Clavulanic Acid; D002969:Clavulanic Acids / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology; D004338:Drug Combinations; D005260:Female; D006801:Humans; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D010406:Penicillins / Q000493:pharmacokinetics*; D013982:Ticarcillin / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D002969:Clavulanic Acids; D004338:Drug Combinations; D010406:Penicillins; D019818:Clavulanic Acid; D013982:Ticarcillin
Evaluation du passage biliaire de l'association ticarcilline-acide clavulanique chez l'homme.