Toxicokinetics of 14C‐endosulfan in male Sprague–Dawley rats following oral administration of single or repeated doses
Toxicokinetics of 14C‐endosulfan in male Sprague–Dawley rats following oral administration of single or repeated doses
复制标题
口服单次或重复剂量后 14C-硫丹在雄性 Sprague-Dawley 大鼠中的毒代动力学
DOI：
10.1002/tox.20142
复制
发表时间：
2005
影响因子：
4.5
通讯作者：
M. Yoneda
中科院分区：
文献类型：
--
作者：
M. Chan;S. Morisawa;Aki Nakayama;Y. Kawamoto;M. Sugimoto;M. Yoneda
硫丹（ES）是一种有机氯（OC）杀虫剂，属于环二烯类，是控制蔬菜、棉花和水果害虫最常用的杀虫剂之一。研究了雄性Sprague-Dawley大鼠口服单剂量（5mg /kg体重）14C硫丹的毒代动力学。分别于给药后30 min、1 h、2 h、4 h、8 h处死3只大鼠。在每个时间点的所有组织中检测到14C‐硫丹放射性。单独收集尿液和粪便96 h， 4 d排泄物中总放射性回收率为106.8%±26.2%，其中粪便消除是主要的消除途径（94.4%±21.4%）。4 d尿中累积排泄量为12.4%±4.8%。给药后8 h，胃肠道组织放射性最高（20.28±16.35 mg ES当量/L），肌肉最低（0.18±0.06 mg ES当量/L）。血中14C硫丹衍生放射性毒性动力学参数为分布半衰期(T1/2 x) = 31 min，终末消除半衰期(T1/2 y) = 193 h，血药浓度在口服2h后达到最大值（Cmax） 0.36±0.08 mg ES当量/L。硫丹在大鼠消化道吸收迅速，吸收速率常数（ka）为3.07 h−1。©2005 Wiley期刊公司环境科学与技术，2009(5):533-541。
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 14C‐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. 14C‐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 14C‐endosulfan‐derived radioactivity in blood were distribution half‐life (T1/2 x) = 31 min and terminal elimination half‐life (T1/2 y) = 193 h. Blood concentration reached its maximum (Cmax) 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 (ka) of 3.07 h−1. © 2005 Wiley Periodicals, Inc. Environ Toxicol 20: 533–541, 2005.