High biliary elimination of ceftriaxone in man.

Biliary elimination of ceftriaxone was studied in man using chromatography (HPLC). After a single i.v. administration of 2 g of ceftriaxone to 6 normal subjects, a peak concentration of 565 +/- s.e.m. 347 micrograms/ml was reached during the 1st h in the collected duodenal fluid, and 1.4 +/- 0.5% of the given dose was recovered within 4 h. In 10 cholecystectomized patients provided with a T-drain, a maximal biliary concentration of 1,078 +/- 158 micrograms/ml was measured during the 2nd h after i.v. injection of 2 g of ceftriaxone and the 24-h recovery was 9.5 +/- 2.9%. Intraoperative samples obtained in 12 patients undergoing cholecystectomy 1 h after i.v. administration of 2 g of the antibiotic, gave the following results: serum concentration 199 +/- 10 micrograms/ml, choledochal bile = 5,259 +/- 1,085 micrograms/ml, gallbladder bile 4,533 +/- 809 micrograms/ml. These data indicate an excellent biliary elimination of ceftriaxone in comparison with other beta-lactams previously studied under the same conditions and point to be a promising therapeutic potential in biliary tract infections.