The aim of this investigation was to assess the bioavailability and pharmacokinetics of oxytocin in six male subjects after a sublingual dose of 400 int. units (684 /xg) and after an intravenous dose of 1 int. unit (1*71 /¿g).After intravenous administration, the pharmacokinetic profile could be described with a two-compart ment model. The distribution half-life was 0-049 ± 0*016 h, the elimination half-life was 0-33 db 0*23 h, the total body clearance was 67*1 ± 13-4Lh' 1 and the volume of distribution was 33-2 ± 28-1 L. After sublingual administration, a poor bioavailability with a 10-fold variation between 0-007 and 0-07% was observed. The pharmacokinetic profile could be described with a one-compartment model. The lag time was subject-dependent and ranged between 0-12 and 0*30 h (40% CV). The absorption half-life was 0*45 ± 0'29 h, and the apparent elimination half-life 0-69 ± 0-26h.This study showed a very poor and interindividual variability in bioavailability. The sublingual route of administration with its 'long' lag time and 'long' absorption half-life would not seem a reliable route for accurate high dosing for immediate prevention of post-partum haemorrhage.
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