Pharmacokinetics of teicoplanin upon multiple dose intravenous administration to normal healthy male volunteers

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Abstract
Teicoplanin pharmacokinetics were investigated upon multiple dose intravenous administration of 6 and 12 mg kg−1 in 10 normal, healthy, male volunteers, using a two‐period, randomized, crossover design; six subjects completed both periods. On day 1, 6 or 12 mg kg−1 was administered every 12 h as a 30‐min constant rate intravenous infusion (two doses). Starting on day 2, the same dose (6 or 12 mg kg−1) was administered every 24 h for an additional 13 days. Blood and urine samples were collected over 21 days. Serum and urine were analyzed using a microbiological assay. Following a minimum of 3 weeks after completion of the first period, subjects were crossed over to the other dose. Following multiple dose intravenous administration of 6 and 12 mg kg−1, median pharmacokinetic parameters included: steady‐state volume of distribution of 1·4 and 1·21 kg−1; total clearance of 12·2 and 14·0 ml h−1 kg−1; renal clearance of 11·1 and 10·3 ml h−1 kg−1; and terminal disposition half‐life of 159 and 155 h, respectively. No statistically significant dose‐related difference was observed. In addition, a cross‐study comparison further supports dose proportionality of teicoplanin upon multiple dose intravenous administration of 3 to 12 mg kg−1.