Relative systemic availability of sulfapyridine from commercial enteric-coated and uncoated sulfasalazine tablets

Journal of Clinical Pharmacology
H J PieniaszekT R Bates

Abstract

The absorption of sulfapyridine after a single 2.0-Gm oral dose of sulfasalazine, the drug of choice in the treatment of inflammatory bowel disease, as commercial uncoated and enteric-coated and uncoated tablets was evaluated in four healthy male adults. The peak plasma concentration of sulfapyridine after the enteric-coated tablets occurred at 20 hours on the average (compared to 14 hours for the uncoated tablets) and was only 50% of that attained from the uncoated tablets (P less than 0.05). The low relative extent of systemic availability of sulfapyridine from the enteric-coated tablets (65.5 +/- 6.3 per cent, mean +/- S.E.) compared to uncoated tablets may be due to absorption rate-dependent presystemic metabolism, since the relative extent of sulfapyridine absorption was 92.7 +/- 6.2 per cent compared to uncoated tablets. These findings suggest that enteric-coated and uncoated tablets of sulfasalazine are not bioequivalent. It remains to be determined whether the clinical efficacy of sulfasalazine from enteric-coated tablets is affected.

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Citations

Jan 1, 1990·Pharmacology & Therapeutics·K F IlettR F Minchin
Jun 7, 2000·Journal of Molecular Graphics & Modelling·T I Oprea, J Gottfries
Mar 5, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Margot FonteyneThomas De Beer
Jun 14, 2019·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Daniela Amaral SilvaRaimar Löbenberg
Jul 11, 2020·Journal of Controlled Release : Official Journal of the Controlled Release Society·Daniela Amaral SilvaRaimar Löbenberg
Jan 24, 2007·Journal of Chemical Information and Modeling·Tingjun HouXiaojie Xu

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