[Biliary excretion of apalcillin. Experimental study and evaluation in man]

Biliary excretion of apalcillin, a new derivative of the ureido-penicillin group, was investigated both experimentally and in humans. After adding 10 mg of this antibiotic to the circulating blood of an isolated rabbit liver perfusion model (n = 5), mean total apalcillin biliary recovery (0-3 h) accounted for 30.7% of the administered dose; the biliary peak averaged 686.0 +/- 135.9 micrograms/ml. In 5 healthy subjects, a mean maximum level of 1088 +/- 582 micrograms/ml was measured in the duodenal fluid collected during the 4 hours following an i.v. injection of Ig of apalcillin. In 10 cholecystectomized patients provided with T-tube drainage, after the same dosage, a mean biliary peak of 2093 +/- 859 micrograms/ml was reached at the third hour and cumulative biliary recovery of apalcillin over a period of 12 hours amounted to 12.1% of the injected dose. In 20 patients, undergoing biliary tract surgery, intra-operative assays performed 1 hour after i.v. injection of 1 g of apalcillin, showed simultaneous mean antibiotic activity of 65.5 +/- 5.0 micrograms/ml in serum, 3860 +/- 551 micrograms/ml in main duct bile and 2552 +/- 627 micrograms/ml in gallbladder bile. The results of these investigations were compared with data previously obtained under identical procedures with 13 other beta-lactam derivatives.