1992 Volume 45 Issue 2 Pages 136-142
Ceftriaxone (CTRX) was administered in dose of 1g 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 caliculated.
Free concentration of antibiotics were following orders in each sampling time: CTRX>CTT>CPM. Mean free concentrations of CTRX at 0 hour and at 8 hours after intravenous drip infusion was more than 20μg/ml and more than 2μg/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)>CPM (5.4 hours) >CTT (4.7 hours). Mean protein binding rates were following orders: CPM (98%) >CTT (94%)> CTRX (92%).
Conclusions: Characteristic of CTRX is high free drug concentration and long half life.
