Holder C L, Siitonen P H, Slikker W, Branscomb C J, Korfmacher W A, Thompson H C, Cerniglia C E, Gosnell A B, Lay J O
Food and Drug Administration, National Center for Toxicological Research, Jefferson, Arkansas 72079.
J Anal Toxicol. 1990 Jul-Aug;14(4):247-51. doi: 10.1093/jat/14.4.247.
Elimination and metabolic profiles of the glucuronide products of doxylamine and its N-demethylated metabolites were determined after the oral administration of (14C)-doxylamine succinate (13.3 and 133 mg/kg doses) to male and female Fischer 344 rats. The cumulative urinary and fecal eliminations of these conjugated doxylamine metabolites at the 13.3 mg/kg dose were 44.4 +/- 4.2% and 47.3 +/- 8.1% of the total recovered dose for male and female rats, respectively. The cumulative urinary and fecal eliminations of conjugated doxylamine metabolites at the 133 mg/kg dose were 55.2 +/- 2.6% and 47.9 +/- 2.5% of the total recovered dose for male and female rats, respectively. The conjugated doxylamine metabolites that were isolated, quantitated, and identified are doxylamine O-glucuronide, N-desmethyl-doxylamine O-glucuronide, and N,N-didesmethyldoxylamine O-glucuronide.
给雄性和雌性Fischer 344大鼠口服琥珀酸多西拉敏（14C）（剂量为13.3和133mg/kg）后，测定了多西拉敏及其N-去甲基代谢产物的葡萄糖醛酸苷产物的消除和代谢情况。在13.3mg/kg剂量下，这些结合的多西拉敏代谢产物在雄性和雌性大鼠中的累积尿排泄和粪便排泄分别占总回收剂量的44.4±4.2%和47.3±8.1%。在133mg/kg剂量下，结合的多西拉敏代谢产物在雄性和雌性大鼠中的累积尿排泄和粪便排泄分别占总回收剂量的55.2±2.6%和47.9±2.5%。分离、定量和鉴定的结合多西拉敏代谢产物为多西拉敏O-葡萄糖醛酸苷、N-去甲基多西拉敏O-葡萄糖醛酸苷和N，N-二去甲基多西拉敏O-葡萄糖醛酸苷。
