PHARMACOKINETICS OF ARTENIBENZOATE IN RATS

Artenibenzoate is a new schistosomacide.This paper reports the pharmacokineticsof artenibenzoate in rats after oral administration.The concentrations in biological samples weredetected by spectrophotometry.The concentration—time curve of the drug in plasma showed a double-peak after 150,300 and 600 mg·kg^-1 ig.Artenibenzoate absorption was fast and peak plasma levelwas found 1h after administration.Then,the drug level declined to the lowest in 8 h.A secondabsorption peak appcared in 12 h.Two hours after oral administration to normal rats,the highest levelof artenibenzoate was present in the stomach wall,while appreciable level was found in testicle,liver,spleen,heart,kidney and lung.Artenibenzoate in fat and intestine was lower,almost no drug wasdetected in brain and muscle.Six hours after oral administration,the drug concentration in varioustissues decreased rapidly,but that in testicle,heart,kidney and fat decreased slowly.Urinaryexcretion was an important route of excretion.Artenibenzoate excreted in urine was about 45.6%ofthe administered dosage and that in feces 24.8%within a 48 hours period.The excreted amount inbile was 0.54%within 36 hours.Plasma protein binding of artenibenzoate was about 70%.Majorunchanged artenibenzoate was detected in the extract from plasma,major reduced-arteannuin fromfeces,and both unchanged artenibenzoate and reduced -arteannuin from urine after oral administrationin ratsa.