Summary
The biliary excretion of Olsalazine sodium (ADS) was studied by three different methods in healthy volunteers and in patients. 1 g ADS in a 2% solution was infused during 1 h into jejunum in six healthy volunteers via a three lumen sond. The bile was collected, during 2.5–6 h, proximal of an occlusive balloon on the three lumen sond. 10 mg ADS was given i.v. to five healthy volunteers and the bile was collected during 3–4.5 h with the same type of three lumen sond as used in the first experiment. 1 g ADS was given orally to three patients, with a T-tube inserted into coleducus at surgery. The bile was collected via the T-tube for 24 h.
The mean biliary excretion of the jejunal dose was 0.41% (0.22% if one subject, who probably had a beckflow of the instillation fluid, is omitted). In patients, the mean excretion with bile of ADS was 0.35% and of ac-5-ASA 0.17%. Due to the short collection time after jejunal infusion and the probably incomplete collection of bile in both enteral studies the biliary excretion was estimated to be less than 2% as ADS and less than 1% as ac-5-ASA.
The biliary excretion of an i.v. dose showed large individual variations (0.16–12.2%) which were not correlated to the length of the collection time. The total excretion was estimated to be less than 20% as ADS. No metabolites were detected after the i.v. dose.
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Ryde, M., Gustavsson, S. Biliary excretion of Olsalazine sodium in humans. European Journal of Drug Metabolism and Pharmacokinetics 12, 17–24 (1987). https://doi.org/10.1007/BF03189857
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DOI: https://doi.org/10.1007/BF03189857