[Biliary excretion of cefotaxime and desacetylcefotaxime]

The biliary excretion of cefotaxime (CTX) and its metabolite desacetylcefotaxime (DSCTX) was measured by HPLC in 9 recently cholecystectomized-patients following the IV injection of 15 mg/kg body weight of CTX. The totality of bile was collected by an original procedure: the inflated balloon of a Fogarty catheter was introduced into the distal branch of a Kehr drain T-tube. Biliary clearance of CTX and DSCTX was measured for 8 h. Cefotaxime peaked at 90 min. after injection at 34.5 +/- 15.3 micrograms/ml; in the 7-8 h sample it was 2.7 +/- 1.7 micrograms/ml. DSCTX peaked at the same time at 49.3 +/- 17.0 micrograms/ml, and was 4.6 +/- 3.2 micrograms/ml at 8 h. The bile/serum ratio of CTX and DSCTX concentration was 1 from the 1st to the 8th hours (range: 1.35 +/- 1.08 to 11.0 +/- 3.1). The biliary clearance of CTX was 0.190 ml/min. The total amounts of CTX and DSCTX eliminated in bile were respectively 1050 +/- 472.8 micrograms and 1902.7 +/- 804.1 micrograms (0.093 +/- 0.041 p. 100 of the dose and 0.186 +/- 0.077 p. 100 of the dose). Considering the minimum inhibitory concentration of the pathogens currently encountered in the biliary sepsis, CTX should be a suitable antimicrobial agent for the treatment of biliary infections.