Phamacokinetics of 14C-teicoplanin in healthy volunteers

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Abstract
Five healthy male volunteers received over 60 sec a single intravenous injection of 400 mg of teicoplanin labelled with 41 μ Ci of 14 C. Plasma and urine total radioactivity was measured up to 10 and 16 days, respectively. Teicoplanin was assayed in plasma and urine also by a microbiological method, with similar results. Pharmacokinetic parameters were estimated by model-independent analysis and the following mean values were obtained: elimination half-life 77 h; total body clearance 9·8 ml/h/kg; renal clearance 7·81 ml/h/kg; volume of distribution at steady-state 0·759 l/kg. Similar estimates were obtained by a compartmental analysis. A total of 80% of the administered dose was recovered in urine in 16 days; 2·7% of the dose was recovered in faeces collected for eight days after administration. The mean total recovery of the drug was 83±0·6±. The plasma and urine concentrations of teicoplanin observed after a single 400 mg iv dose exceeded the MIC for most pathogens for at least one day, and this suggests that a daily dosage regimen would be satisfactory for patients with normal renal function.

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