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  • Urinary excretion and metabolism of salts of 2-pyridinethiol-1-oxide following intravenous administration to female Yorkshire pigs☆
  • Add time:09/27/2019         Source:sciencedirect.com

    A single dose of zinc pyridine-2-thiol-1-oxide (ZPT; 5 mg/kg; oil-in-water emulsion), sodium pyridine-2-thiol-1-oxide (SPT; 50 mg/kg; aqueous solution), or the magnesium sulfate adduct of 2,2′-dithio-bis-pyridine-1-oxide (MDS; 4 mg/kg; aqueous solution), which included 5 μCi/kg of 2,6-14C-labeled material, was injected via a jugular vein cannula into female Yorkshire pigs in order to study the plasma half-life, the urinary excretion rate, and the metabolism of these antimicrobial and antifungal agents during a 96-hr period. At the doses employed, all of these agents produced cholinergic effects (parasympathetic and somatomotor) which lasted for 30–60 min. Plasma decline in radioactivity was a biphasic exponential function for each compound. Half-lives for the initial phase of plasma disappearance (0.25 to 8 hr after injection) ranged from 2.0 to 2.9 hr and the slower, secondary phase was characterized by half-lives of 26.6 to 36.3 hr. The urinary excretion in terms of the percentage of total dose excreted within 96 hr, was 95 for SPT, 56 for ZPT, and 54 for MDS. The majority of total radioactivity was recovered in the urine within the first 24 hr postinjection. Thin-layer radiochromatographic analysis indicated that 2,2′-(pyridyl-N-oxide) disulfide was the primary metabolite of SPT whereas the primary metabolite for both ZPT and MDS appeared to be 2-(pyridyl-N-oxide) sulfonic acid.

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