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Fate of the analgesic and anti-inflammatory drug K 4277 after oral administration to man

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Summary

The fate of the new analgesic and anti-inflammatory agent α-[4-(1-oxo-2-iso-indolinyl)-phenyl]-propionic acid (compound K 4277) in healthy volunteers has been investigated by a radio-isotope method and gas-liquid chromatography. After oral administration, the drug was absorbed rapidly and completely and occurred in plasma mainly as unchanged compound bound extensively to plasma proteins. Its disappearance from plasma followed at least a bi-exponential function and was almost complete in 24 to 48 h. Most of the drug is excreted in urine as a glucuronide and a lesser amount as the unchanged compound. There were only negligible amounts of other metabolites.

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Authors and Affiliations

  1. Carlo Erba Research Institute, Milan, Italy

    L. M. Fuccella, G. C. Goldaniga, E. Moro, V. Tamassia, G. P. Tosolini & G. Valzelli

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  1. L. M. Fuccella
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  2. G. C. Goldaniga
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  3. E. Moro
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  4. V. Tamassia
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  5. G. P. Tosolini
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  6. G. Valzelli
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Fuccella, L.M., Goldaniga, G.C., Moro, E. et al. Fate of the analgesic and anti-inflammatory drug K 4277 after oral administration to man. Eur J Clin Pharmacol 6, 256–260 (1973). https://doi.org/10.1007/BF00644742

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  • DOI: https://doi.org/10.1007/BF00644742

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