Kinetics of14C‐furazolidone in piglets upon oral administration during 10 days and its interaction with tissue macro‐molecules

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Abstract
After dosing piglets orally with 14C‐furazolidone (75 mg/animal/day) for 10 days, no accumulation of the drug could be detected in the blood. The half life of furazolidone in blood after the last oral administration on day 10 was 60 minutes. In blood, radioactivity reached a plateau of approximately 10 ppm equivalents of parent compound at day 6 of the medication. After a relatively fast decrease of radioactivity during the first day of the withdrawal period, a much slower decrease could be observed in the blood with a half life of approximately 6 days. 1 day after stopping the medication almost all the radioactivity in plasma appeared to be associated with plasma proteins. Furazolidone could not be detected in muscle, fat, kidney and liver of piglets two hours after the last administration. However, the level of radioactivity was 5.7–7.2μg equivalents per gram in muscle, 6.0–9.2μg equivalents per gram in fat, 30.1 μg equivalents per gram in kidney and 32.9 μg equivalents per gram in liver. After a withdrawal period of 14 days 0.9–4.3 μg equivalents per gram could be detected in the analysed tissues. It also appeared that respectively 14.0%, 9.3% and 35.0% of the residual radioactivity could not be extracted from liver, kidney and muscle of piglets sacrificed 2 hours after the last administration of 14C‐furazolidone and 27.0%. 31.2% and 55.6% of the residual radioactivity from liver, kidney and muscle respectively of piglets sacrificed after a withdrawal period of 14 days. DNA‐binding of l4C‐furazolidone in tissues of piglets varied from 87–382 pmol equivalents of parent compound per mg DNA. 61% of total dosed radioactivity had been excreted via the urine and 18.1% via the faeces. No radioactivity could be measured in the expired air.

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