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Pharmacokinetics and biotransformation, in rats and dogs, of trithiozine, a new antisecretory drug

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Summary

Trithiozine (T) is a new antisecretory drug submitted to a pharmacokinetic study after having developed a specific gaschromatographic method for its determination in biological fluids and tissues.

(T) shows an apparent plasma half-life of about 2.5 hr in rats and 1 hr in dogs. It is excreted as such in rat bile and in rat and dog urine only to a very limited extent. (T) is rapidly metabolized yielding two metabolites and two conjugates. One of this metabolite has been identified as 4-(3, 4, 5-trimethoxybenzoyl)tetrahydro-l, 4-oxazine (TBO) in the plasma and urine of rats and dogs. This metabolite is provided with tranquillizing activity.

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Correspondence to G. Pifferi.

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Pacifici, G.M., Bianchetti, G., Frigerio, A. et al. Pharmacokinetics and biotransformation, in rats and dogs, of trithiozine, a new antisecretory drug. European Journal of Drug Metabolism and Pharmacokinetics 1, 141–147 (1976). https://doi.org/10.1007/BF03189268

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Key-words

  • Trithiozine
  • pharmacokinetics
  • metabolism
  • chromatography
  • antisecretory drug ISF 2001
  • mass spectrometry