Distribution of endosulfan in plasma and brain after repeated oral administration to rats.

Rats were fed endosulfan (5 or 10 mg/kg) containing alpha- and beta-isomers in the ratio of 2:1, daily for 15 days. The distribution pattern of endosulfan, its isomers and metabolite, endosulfan sulfate, was estimated in the plasma and brain of the rats. On day 16, the alpha-isomer in rats receiving 5 mg/kg was highest in the cerebrum (3.76 microgram/g) followed by the remaining part of the brain (2.66 microgram/g), and the cerebellum (2.04 microgram/g). The concentration of the beta-isomer was 0.06 microgram/g in the cerebrum and 0.02 microgram/g in the cerebellum; no beta-isomer was detected in the remaining part of the brain. The plasma concentration of alpha- and beta-isomers was 2.26 and 0.46 microgram/ml, respectively. No metabolite other than endosulfan sulfate was detected in plasma. No significant changes in brain tissue were observed in any of the groups under treatment. On day 30 (15 days after the last treatment), the concentration in plasma declined more rapidly than that in the brain tissue. At a higher dose (10 mg/kg), the distribution pattern of isomers and its metabolite, endosulfan sulfate, followed almost the same trend except that the concentration was higher than in rats receiving lower doses.