Biliary excretion in foreign compounds. Sulphonamide drugs in the rat

Abstract

1. The extent of biliary excretion in the rat of 15 sulphonamide compounds was studied. 2. Most of the sulphonamides studied, with molecular weights from 172 (sulphanilamide) to 352 (N4-acetylsulphadimethoxine) are poorly excreted in the bile (0–4% of the dose), except sulphapyridine, sulphamethoxypyridazine and sulphadimethoxine. The last three are partly metabolized to glucuronides, whose molecular weights and polarities are such as to allow them to be excreted in the bile in appreciable amounts. 3. Succinylsulphathiazole and phthalylsulphathiazole are polar and have molecular weights (355 and 403) of an appropriate order, and are excreted unchanged in the bile in appreciable amounts. 4. Sulphadimethoxine N1-glucuronide (mol.wt. 487) is extensively excreted in the bile unchanged. 5. The results are examined in the light of the hypotheses put forward in the preceding paper (Millburn, Smith & Williams, 1967).