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Abstract
1. The peak plasma concn. of total radioactivity occurred 6 h after a single oral dose of [carboxyl-14C; methyl-2H3] propantheline bromide was administered to a healthy man. At this time 10% of the dose was present in the total plasma volume.
2. A total of 71% dose of radioactivity was excreted in urine in 96 h afrer dosage, 59% dose being excreted in the first 24 h. About 5·3% of the orally administered propantheline bromide was excreted unchanged.
3. T.l.c. analysis and g.l.c.-mass spectrometry showed xanthanoic acid, hydroxyxanthanoic acid(s) and propantheline as urinary metabolites of the drug.
4. A glucuronide of xanthanoic acid, a hydroxylated propantheline and the (2-hydroxyethyl)diisopropylammonium ion were tentatively identified as urinasy metabolites. Hydrolysis of propantheline and conjugation of the resulting xanthanoic acid appear to be the major routes of metabolism of this compound.
5. A mean elimination half-life of 9·2 h was obtained for the total radioactivity by pharmacokinetic analysis of plasma and urine levels of 14C.