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Pharmacokinetic study of 2,3-dichloro 4-[2-thienyl keto14C] phenoxyacetic acid (Tienilic acid) in animals I. Localisation, distribution and elimination of14C Tienilic acid in animals

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Summary

The localization, distribution and elimination of14C-Tienilic acid, a new diuretic and hypouricemic drug has been described.

This study was carried out using14C labelled compound on four different animal species: mice, rats, pigs and dogs. The blood level is expressed as /gmg/ml equivalents of the administered product. After oral administration, the absorption rate of this product in doses of 5 mg/kg for rats, pigs and dogs was between 50 and 80 %, depending on the species. Tienilic acid was rapidly distributed in most of the essential organs and tissues with the exception of the brain. In the blood the product was found only at the plasmatic level with high plasmatic protein binding, around 72–95 %.

Biliary and particularly urinary elimination was fast and practically complete in 48 hours.

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Reference

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    Levron, J. C, Dormard, Y., Le Fur, J. M., Adnot, P., Pharmacokinetic Study of 2,3-dichloro 4-/2-thienyl keto-14C/phenoxyacetic acid (Tienilic acid) in animals II. Study and identification of the metabolites of14C-Tienilic acid in animals, which will appear later in this journal.

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Correspondence to Y. Dormard.

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Dormard, Y., Levron, J.-., Adnot, P. et al. Pharmacokinetic study of 2,3-dichloro 4-[2-thienyl keto14C] phenoxyacetic acid (Tienilic acid) in animals I. Localisation, distribution and elimination of14C Tienilic acid in animals. European Journal of Drug Metabolism and Pharmacokinetics 1, 41–49 (1976). https://doi.org/10.1007/BF03192278

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Key-words

  • 14C-Tienilic acid
  • diuretic
  • pharmacokinetic
  • animals