Cefixime is a new oral cephalosporin antibiotic with improved activity against Gram-negative pathogens comparable to the parenteral third generation cephalosporins, high beta-lactamase stability and a long elimination half-life of about 3 h. 15 patients undergoing cholecystectomy received 2 x 200 mg/day cefixime for two days before surgery. The last application was administered 13-17 h preoperatively. Intraoperatively, the mean biliary level of cefexime was 199.3 micrograms/ml (8.8 micrograms/ml-1163.8 micrograms/ml). The mean level in gallbladder wall was 25.02 micrograms/g (0.68 micrograms/g-61.20 micrograms/g). Serum samples were taken simultaneously. Despite relevant concentrations in bile and gallbladder wall, no cefixime could be detected in the serum samples of two patients. The other 13 patients, however, showed relevant serum levels between 0.28 micrograms/ml and 2.98 micrograms/ml (mean 1.01 micrograms/ml). Side effects as well as an influence on laboratory parameters were not seen. After administration of cefixime in bile and gallbladder tissue high antibiotic levels were achieved, even 13-17 hours after the last application.