Sidon E W, Moody R P, Franklin C A
Health and Welfare, Canada, Ottawa, Ontario.
J Toxicol Environ Health. 1988;23(2):207-16. doi: 10.1080/15287398809531107.
Dermal absorption of cis- and trans-permethrin isomers was determined in rhesus monkeys and Sprague-Dawley rats. Four 14C radiolabels were used (cis alcohol, cis cyclopropyl, trans alcohol, and trans cyclopropyl). One microcurie of each radiolabel was applied to either the forehead or forearm of rhesus monkeys or to the midlumbosacral region of the rat. Urine was collected for 7 or 14 d. Correction factors for incomplete urine excretion were derived from measurements of radiolabel in the urine following im injection of an equivalent dose. It was noted that the total im dose recovered in the urine of both species was lower for the cis isomer than for the trans isomer. There was no significant difference between the dermal absorption of the cis isomer and that of the trans isomer in monkeys. The forehead, however, was more permeable for both isomers than the forearm (alcohol- and cyclopropyl-labeled cis and trans isomers, respectively, showed permeation in forehead, cis 28 +/- 6%, 24 +/- 6%, trans 21 +/- 3%, 14 +/- 4%, forearm, cis 9 +/- 3%, 9 +/- 3%, trans 12 +/- 3%, and 5 +/- 2%). There was no difference between absorption of the isomers (cis 46 +/- 4%, trans 43 +/- 5%) in rats, but absorption was significantly greater than in monkeys. The IM urinary t1/2 values in monkeys and rats were similar for both isomers (0.8-1.1 d).
在恒河猴和斯普拉格-道利大鼠中测定了顺式和反式氯菊酯异构体的皮肤吸收情况。使用了四种14C放射性标记物（顺式醇、顺式环丙基、反式醇和反式环丙基）。将每种放射性标记物的1微居里分别涂抹于恒河猴的前额或前臂或大鼠的腰骶中部区域。收集尿液7天或14天。不完全尿液排泄的校正因子来自于肌肉注射等效剂量后尿液中放射性标记物的测量值。注意到两种动物尿液中回收的肌肉注射总剂量，顺式异构体低于反式异构体。恒河猴中顺式异构体和反式异构体的皮肤吸收之间没有显著差异。然而，对于两种异构体，前额的渗透性均高于前臂（分别用醇和环丙基标记的顺式和反式异构体，在前额的渗透率分别为顺式28±6%、24±6%，反式21±3%、14±4%；在前臂的渗透率分别为顺式9±3%、9±3%，反式12±3%和5±2%）。大鼠中异构体的吸收情况没有差异（顺式46±4%，反式43±5%），但吸收明显高于恒河猴。两种异构体在恒河猴和大鼠中的肌肉注射尿半衰期值相似（0.8 - 1.1天）。
