Pharmacokinetics of Teicoplanin

Abstract

We investigated the pharmacokinetic properties of teicoplanin, after 200 mg i.v. and i.m. administration in 10 healthy male subjects by assuming a three-compartment open model with elimination from the central compartment. The mean peak plasma level was 7.16 μg/ml reached after 2.26 h. The half-life, the plasma and renal clearances, evaluated from i.v. data were 44.49 h, 15.31 and 9.08 ml/min, respectively. The same parameters after i.m. administration were 45.62 h, 15.31 and 9.46 ml/min. The estimates of creatinine clearance (Cl_cr > 80 ml/min), renal clearance and the low free fraction (f_B≈0.1) suggested a tubular reabsorption, FR, of the drug. The distribution volume at steady state after i.v. and i.m. administration (V_ss = 41.29 and 44.76 litres) were nearly total body water. Bioavailability of the drug (F = 92.4%) showed an almost completely absorption of teicoplanin after i.m. administration. Urinary recovery was 49.6 and 47.9% of the dose after i.v. and i.m. administration, respectively.