Pharmacokinetics of oxiracetam following intravenous and oral administration in healthy volunteers

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Abstract
The kinetics of oxiracetam after single intravenous and oral doses (2000 mg) were investigated in four healthy volunteers. Following intravenous administration, the decline in serum levels showed a prolonged, rapid phase followed by a delayed terminal phase. Mean residence times ranged from 3.9 to 6.5 h. Volumes of distribution ranged from 0.9 to 1.81 · kg−1, whereas clearance values ranged from 100 to 119 ml·.h−1· kg -1 More than 90% of the intravenous dose was recovered unchanged in the urine within 48 h. Oral administration resulted in peak levels within 1–2 h; thereafter, the decline in serum levels showed a pattern similar to that observed after the intravenous dose — almost 50% of the oral dose was excreted in the urine within 6 h. The absolute availability of oral oxiracetam was 75 ± 7%.