Toxicokinetics of 14C‐endosulfan in male Sprague–Dawley rats following oral administration of single or repeated doses

Abstract Endosulfan (ES), an organochlorine (OC) insecticide that belongs to the cyclodiene group, is one of the most commonly used pesticides to control pests in vegetables, cotton, and fruits. The toxicokinetics of 14 C‐endosulfan following oral administration of a single dose of 5 mg/kg body weight was investigated in male Sprague–Dawley rats. Three rats were sacrificed 30 min, 1 h, 2 h, 4 h, and 8 h after dosing. 14 C‐endosulfan radioactivity was detected in all tissues at each time point. In a separate experiment urine and feces were collected for 96 h. The total radioactivity recovered in the excreta for 4 days was 106.8% ± 26.2%, with fecal elimination the major route of elimination route (94.4% ± 21.4%). The cumulative excretion in the urine for 4 days was 12.4% ± 4.8%. Radioactivity 8 h after administration was highest in gastrointestinal (GI) tract tissue (20.28 ± 16.35 mg ES eq./L) and lowest in muscle (0.18 ± 0.06 mg ES eq./L). The toxicokinetic parameters obtained from 14 C‐endosulfan‐derived radioactivity in blood were distribution half‐life ( T 1/2 x ) = 31 min and terminal elimination half‐life ( T 1/2 y ) = 193 h. Blood concentration reached its maximum ( C max ) of 0.36 ± 0.08 mg ES eq./L 2 h after the oral dose. Endosulfan was rapidly absorbed into the GI tract in rats, with an absorption rate constant ( k a ) of 3.07 h −1 . © 2005 Wiley Periodicals, Inc. Environ Toxicol 20: 533–541, 2005.