Ceftriaxone (CTRX) was administered in dose of 1 g 30 minutes intravenous drip infusion to 5 healthy volunteers. Cefpiramide (CPM) and cefotetan (CTT) were administered as control antibiotics. The serum concentrations of total and free drugs, using ultrafiltration, were assayed by bioassay and HPLC. Protein binding rates and pharmacokinetic parameters were calculated. Free concentration of antibiotics were following orders in each sampling time: CTRX greater than CTT greater than CPM. Mean free concentrations of CTRX at 0 hour and at 8 hours after intravenous drip infusion was more than 20 micrograms/ml and more than 2 micrograms/ml. Even at 24 hours after intravenous drip infusion free concentrations of CTRX were detectable. Mean half life in beta phase by HPLC was following orders: CTRX (7.5 hours) greater than CPM (5.4 hours) greater than CTT (4.7 hours). Mean protein binding rates were following orders: CPM (98%) greater than CTT (94%) greater than CTRX (92%).
Conclusions: Characteristic of CTRX is high free drug concentration and long half life.