Pharmacokinetic and biopharmaceutic parameters of gitoformate
Lesne, M.; Cremers, S.; Carlier, J.
Therapie 33(6): 723-734
1978
ISSN/ISBN: 0040-5957 PMID: 746519 Document Number: 4443
The pharmacokinetic properties and the bioavailability of gitoformate have been studied in 8 healthy volunteers who were given a single dose of gitoformate intravenously (1 mg) as well as orally as a drinkable solution (1 mg) and under tablet form (0.8 mg; the effects of a chronic treatment for 6 weeks at a daily dose of 0.1 mg of gitoformate have also been studied in 8 healthy volunteers who were given a single dose of gitoformate intravenously In the experiments with the single dose, gitoformate has a half-life of 65.9 + 4.6 h. (s.e.m.) (n -=20) and an apparent distribution volume of 51.7 + 3.8 1. (n=20). At the end of the chronic treatment, the half-life drops to 16.7±1.9 h. (n=8). The plateau is reached after 20.7±1.6 days (n=8), the plasma levels being at that moment 10.7±1.2 ng/ml (n=8). The absolute bioavailability of gitoformate given as a drinkable solution is 89.6 p. 100, i.e. a loss of 10.4 p. 100, probably due to pre- or intrahepatic biodegradation. The bioavailability of the tablets with respect to drinkable solution is estimated to be 72.7 p. 100.
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