Thompson H C, Holder C L, Siitonen P H, Rowland K L, Gosnell A B, Cmarik J L
Food and Drug Administration, National Center for Toxicological Research, Jefferson, Arkansas 72079.
J Anal Toxicol. 1987 Nov-Dec;11(6):252-6. doi: 10.1093/jat/11.6.252.
Male and female Fisher 344 rats (12 per group) were dosed by gavage with either 2 or 10 mg (based on the free amine) pyrilamine maleate containing about 12 and 6 muCi 14C-pyrilamine maleate, respectively, to determine excretion of the activity as a function of dose and sex with time. Urine and feces were collected at timed intervals through 144 h. Most of the dose (about 70%) was eliminated within 48 h through the urine and feces, but only about 80% of the total dose was recovered during the experiment. Less than 1% of the total dose remained in the rats at the end of the test period. In an additional experiment to determine the location of the remainder of the dose (about 20%), male rats were dosed with 2 mg pyrilamine maleate containing 14C-pyrilamine maleate. After 144 h, exhaustive washing of the cages resulted in recovery of approximately 20% of the dose, thus identifying its location. There were no significant sex or dose related differences observed in the total amount of 14C that was eliminated through the urine or feces and recovered. Urine and feces are the major routes of elimination of pyrilamine maleate in the Fischer 344 rat. The urinary route of elimination was more predominant than the fecal route in both sexes at either dose.
选用雄性和雌性Fisher 344大鼠（每组12只），分别经口灌胃给予2毫克或10毫克（以游离胺计）马来酸氯苯那敏，其中分别含有约12微居里和6微居里的14C-马来酸氯苯那敏，以确定其活性排泄量随剂量、性别和时间的变化情况。在144小时内定时收集尿液和粪便。大部分剂量（约70%）在48小时内通过尿液和粪便排出，但实验期间仅回收了约80%的总剂量。试验期结束时，大鼠体内残留的总剂量不到1%。在另一项确定剩余剂量（约20%）位置的实验中，给雄性大鼠灌胃2毫克含14C-马来酸氯苯那敏的马来酸氯苯那敏。144小时后，对笼子进行彻底冲洗，回收了约20%的剂量，从而确定了其位置。通过尿液或粪便排出并回收的14C总量未观察到显著的性别或剂量相关差异。尿液和粪便是Fischer 344大鼠体内马来酸氯苯那敏的主要排泄途径。在两种剂量下，两性中尿液排泄途径均比粪便途径更为主要。
