Pharmacokinetics of sulfadimethoxine and sulfamethoxazole in combination with trimethoprim after oral single- and multiple-dose administration to healthy pigs.
作者： M.J.B. Mengelers , E.R. van Gogh , M.B.M. Huveneers , P.E. Hougee , H.A. Kuiper
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摘要: The pharmacokinetics were studied of sulfadimethoxine (SDM) or sulfamethoxazole (SMX) in combination with trimethoprim (TMP) administered as a single oral dose (25 mg + 5 per kg body weight) to two groups 6 healthy pigs. elimination half-lives SMX and TMP quite similar (2-3 h); SDM had relatively long half-life 13 h. Both sulfonamides (S) exclusively metabolized N4-acetyl derivatives but different extents. main metabolic pathway for was O-demethylation subsequent conjugation. In addition, the plasma concentrations these drugs their metabolites after medication in-feed determined. drug (S:TMP) feed 250:50, 500:100, 1000:200 kg. Steady-state achieved within 48 h medication, twice daily (SDM+TMP) three times day (SMX+TMP). Protein binding its metabolite high (>93%), whereas SMX, showed moderate (48-75%). Feed 500 ppm sulfonamide combined 100 provided minimum steady-state (C(ss,min)) higher than concentration required inhibition growth 90% Actinobacillus pleuropneumoniae strains (n = 20).
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