Absorption, distribution and excretion of sultopride in man and several animal species

Abstract

Single oral and intramuscular doses of ¹⁴C-sultopride to rat, rabbit and dog and single oral doses of sultopride to human volunteers were well absorbed.

2. Mean blood levels of total ¹⁴C peaked at 0·4–1·1 h and declined with half-lives of 2, 1·5 and 3 h in rat, rabbit and dog, respectively. In man mean serum levels of unchanged drug attained a peak at 1·5 h and were eliminated with a half-life of 3·6 h.

3. Highest concn. of radioactivity were found in rat liver, kidney, hypophysis, submaxillary gland and gastrointestinal tract. The concn. in the cerebrum and cerebellum were low. ¹⁴C-Sultopride passed through the placental barrier.

4. ¹⁴C-Suttopride was poorly bound to plasma proteins (<25% bound) in all species.

5. Repeated doses of the drug slightly increased the blood and tissue levels of ¹⁴C in the rat.

6. Most of the dose was eliminated via the kidneys in all species. Male rats excreted larger amounts of ¹⁴C into bile and faeces.

7. A high ratio of A.U.C. (milk)/(blood) (c. 3·5) was found in the lactating rat.