Thompson H C, Gosnell A B, Holder C L, Siitonen P H, Rowland K L, Cmarik J L
J Anal Toxicol. 1986 Jan-Feb;10(1):18-23. doi: 10.1093/jat/10.1.18.
Experiments were conducted with male and female rats (12 per group) dosed by gavage with 2 or 20 mg (based on the free amine) doxylamine succinate containing about 10 microCi 14C-doxylamine succinate to determine distribution and excretion of the activity as a function of dose and sex with time. Urine and feces were collected at intervals up to 72 hr. Most of the dose (approximately equal to 70%) was eliminated in the first 24 hr after dosing and 95 to 100% of the dose was recovered during the 72-hr course of the experiments with both sexes and dose levels. Less than 1% of the total dose remained in the rats at the end of the test period. The urinary route of elimination was more predominant than the fecal route in both sexes given the 20-mg dose. The fecal route predominates in low-dose males whereas there is no significant difference between urinary and fecal routes of elimination in low-dose females. Preliminary characterization of urinary metabolite form using extraction techniques shows 99% of the metabolites to be in the polar conjugated form.
对雄性和雌性大鼠（每组12只）进行实验，通过灌胃给予含约10微居里14C - 琥珀酸多西拉敏的2毫克或20毫克（基于游离胺）琥珀酸多西拉敏，以确定活性物质随剂量、性别和时间的分布及排泄情况。每隔一段时间收集尿液和粪便，直至72小时。给药后的头24小时内，大部分剂量（约70%）被消除，在72小时的实验过程中，无论性别和剂量水平，95%至100%的剂量被回收。在试验期结束时，大鼠体内残留的总剂量不到1%。给予20毫克剂量时，两性中通过尿液排泄的途径比通过粪便排泄的途径更占主导。低剂量雄性大鼠中粪便排泄途径占主导，而低剂量雌性大鼠中尿液和粪便排泄途径之间没有显著差异。使用提取技术对尿液代谢物形式进行的初步表征显示，99%的代谢物为极性共轭形式。
