Quistad G B, Mulholland K M, Skinner W S
Toxicol Appl Pharmacol. 1986 Sep 15;85(2):215-20. doi: 10.1016/0041-008x(86)90115-8.
Within four days of receiving a single oral dose (1 mg/kg) of [U-ring-14C]dienochlor [bis(pentachloro-2,4-cyclopentadien-1-yl)] female rats excreted 2 and 88% of the applied 14C in urine and feces, respectively. Metabolites could not be identified and the preponderance of the fecal radioactivity consisted of unextractable 14C-labeled residues. Within 1 day virtually all of the dienochlor had been degraded by rats, with only traces of parent dienochlor in excreta and tissues. After four days only 2% of the applied dose remained in tissues (mainly kidney, liver, and gastrointestinal tract). Pharmacokinetic studies with blood plasma and bile showed dienochlor (and/or its metabolites) to be poorly absorbed. Rats were exposed dermally for 24 hr to [14C]dienochlor formulated as Pentac WP miticide both as an aqueous suspension and as an undiluted wettable powder. Half of the dose adhered to the skin and the other half was found in gauze patches used to protect the treated skin. After a 24-hr exposure over 60% of the radiolabel that adhered to skin was removed by washing with an aqueous soap solution and 86% of this rinsing solution was unmetabolized dienochlor. The dienochlor and its metabolites were transported inefficiently from the application site; only 1% of the applied dose was detected in urine plus feces and less than or equal to 0.2% in tissues. With application rates that simulate field exposure by humans, the actual residue of dienochlor and metabolites in skin (i.e., not removable by washing) is about thirteen times higher following exposure to dienochlor as undiluted wettable powder than as an aqueous suspension.
雌性大鼠单次口服剂量为1毫克/千克的[U-环-14C]地诺氯(双(五氯-2,4-环戊二烯-1-基))后,在四天内分别从尿液和粪便中排出了所施用14C的2%和88%。无法鉴定出代谢产物,粪便中的放射性物质主要是不可提取的14C标记残留物。在1天内,几乎所有的地诺氯都被大鼠降解,排泄物和组织中仅残留微量的母体地诺氯。四天后,仅2%的施用剂量残留在组织中(主要是肾脏、肝脏和胃肠道)。血浆和胆汁的药代动力学研究表明,地诺氯(和/或其代谢产物)的吸收较差。大鼠经皮暴露于以戊杀威WP杀螨剂配制的[14C]地诺氯24小时,该杀螨剂以水悬浮液和未稀释的可湿性粉剂两种形式存在。一半的剂量附着在皮肤上,另一半则在用于保护处理过皮肤的纱布贴片中被发现。暴露24小时后,用肥皂水溶液冲洗可去除60%以上附着在皮肤上的放射性标记物,且该冲洗液的86%是未代谢的地诺氯。地诺氯及其代谢产物从施药部位的转运效率较低;尿液和粪便中仅检测到1%的施用剂量,组织中的含量小于或等于0.2%。在模拟人类田间暴露的施用量下,暴露于未稀释可湿性粉剂形式的地诺氯后,皮肤中地诺氯及其代谢产物的实际残留量(即不可通过冲洗去除的残留量)比暴露于水悬浮液形式的地诺氯高出约13倍。