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Trimebutine maleate pharmacokinetics?

Time:2015/9/30 7:25:43

After oral administration in animals (rat, dog,mouse, rabbit), intestinal absorption of Trimebutine maleate is almost complete, as 94% of an oral dose of Trimebutine maleate is 

Trimebutine maleate

eliminated by the kidneys in the form of various metabolites. The peak plasma concentration is observed 1 h after ingestion.50 Fetal transfer is low: in pregnant rats given 30 


mg/kg of 14C Trimebutine maleate orally, the maximum level of radioactivity in the fetus and amniotic fluid does not exceed 0.02% of the dose. In suckling rats only 0.04% of the 


dose is excreted in milk within 8 h.50Autoradiographic studies (in rat) have shown large amounts of Trimebutine maleate concentrated in the gUt.51 In man, after a single oral 


dose of Trimebutine maleate (2 mg/kg), the peak plasma concentration is reached within 1 h and the plasma elimination half-life is about 1 h.

The main metabolite of Trimebutine maleate, norTrimebutine maleate,is formed in the liver and exerts the pharmacological properties of trirnebutine,especially in the colon.