Biliary elimination of apalcillin: an experimental and clinical study

After adding 10 mg of apalcillin to the circulating blood of five isolated rabbit liver perfusion preparations, total apalcillin biliary recovery over a 3 h-period accounted for 30.7% of the administered dose; the biliary peak level averaged 686.0 +/- 135.9 micrograms/ml. In five healthy subjects, a maximum level of 1088 +/- 582 micrograms/ml was measured in the duodenal fluid collected during 4 h following intravenous injection of 1 g of apalcillin. In 10 cholecystectomized patients provided with T-tube drainage, after the same dosage, a biliary peak of 2093 +/- 859 micrograms/ml was attained in the 3rd hour and cumulative biliary recovery over a 12 h-period amounted to 12.1% of the injected dose. In 20 patients undergoing biliary surgery, intra-operative simultaneous sampling performed 1 h after intravenous injection of 1 g of apalcillin showed antibiotic levels of 65.5 +/- 5.0 micrograms/ml in serum, 3860 +/- 551 micrograms/ml in common bile duct bile and 2552 +/- 627 micrograms/ml in gallbladder bile. The results of these investigations were compared with data previously obtained with 13 other beta-lactam derivatives.