Biliary excretion of olsalazine sodium in humans.

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.