Abstract
1. Methods were devised for the separation and quantitative determination of 1-(3,3-diphenylpropyl)amino-3-[14C]phenylthiopropane in biological fluids.
2. Urine and faeces from treated rats contained four radioactive materials, including the unmetabolized compound.
3. Concentrations of both total radioactivity and unmetabolized diphenyl-propylamino-phenylthiopropane in plasma were highest following intravenous doses, intermediate following intraperitoneal doses and lowest following oral doses; the apparent volume of distribution of diphenylpropylamino-phenylthiopropane was in excess of 1 l/kg and its half-time of disappearance from plasma, once distribution equilibrium had been reached, was approx. 14 h.
4. Unmetabolized drug and its metabolites were both present in urine and faeces; 30-35% of the dose was excreted in 72 h after administration by all routes, indicating a considerable degree of tissue retention at long time intervals after dosing.
5. The compound was bound to plasma protein; tissue distribution was uneven with highest concentrations in gastro-intestinal tissue and fat, and lowest concentrations in brain.