Pharmacokinetics, renal clearance, tissue distribution, and residue aspects of sulphadimidine and its N4‐acetyl metabolite in pigs
作者:
J. F. M. Nouws,
T. B. Vree,
M. Baakman,
F. Driessens,
L. Vellenga,
D. J. Mevius,
期刊:
Veterinary Quarterly
(Taylor Available online 1986)
卷期:
Volume 8,
issue 2
页码: 123-135
ISSN:0165-2176
年代: 1986
DOI:10.1080/01652176.1986.9694031
出版商: Taylor & Francis Group
数据来源: Taylor
摘要:
Pharmacokinetics and tissue distribution experiments were conducted in pigs to which sulphadimidine (SDM) was administered intravenously, orally, and intramuscularly at a dosage of 20 mg SDM/kg. SDM was acetylated extensively, but neither hydroxy metabolites nor their derivatives could be detected in plasma, edible tissues or urine. Following i.v. and two oral routes of administration, the N4‐acetylsulphadimidine (N4‐SDM) concentration‐time curve runs parallel to that of SDM. The percentage of N4‐SDM in plasma was in the range between 7 and 13.5% of the total sulphonamide concentration. The bioavailability of SDM administered in a drench was 88.9 ± 5.4 % and administered mixed with pelleted feed for 3 consecutive days it was 48.0 ± 11.5 %. The renal clearance of unbound SDM, which was urine flow related, was 1/7 of that of creatinine, indicating reabsorption of the parent drug. The unbound N4SDM was eliminated three times faster than creatinine, indicating that tubular secretion was the predominant mechanism of excretion.
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