The biliary elimination of cefotaxime (CTX) and its metabolite desacetylcefotaxime (DSCTX) were measured by HPLC in nine recently cholecystectomised patients following the i. v. injection of 15 mg/kg body weight of CTX. All of the 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 mg/l; in the 7-8 h sample it was 2.7 +/- 1.7 mg/l. DSCTX peaked at the same time at 49.3 +/- 17.0 mg/l, and was 4.6 +/- 3.2 mg/l at 8 h. The bile/serum ratio of CTX and DSCTX concentrations was above 1 from the first to the eighth 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% of the dose and 0.186 +/- 0.077% of the dose). Considering the minimum inhibitory concentration of the pathogens currently encountered in biliary sepsis, CTX should be a suitable antimicrobial agent for the treatment of biliary infections.

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