Hackett A M, Griffiths L A
Eur J Drug Metab Pharmacokinet. 1979;4(4):207-12. doi: 10.1007/BF03189428.
Following i.v. administration of mono-HR to the beagle, plasma levels of both mono-HR and its glucuronide conjugates fell rapidly, neither being detectable 8 h after injection. Following oral administration of 14C-mono-HR, mono-HR-glucuronide was detected in plasma, confirming the absorption of mono-HR, and low levels of 14C were detectable up to 72 h after dosage. Following either oral or i.v. administration of mono-HR, the major route of excretion was fecal elimination of the compound as its aglycone form. Urinary excretion was slight being less than 15% following i.v. dosage and 4% following oral administration. Metabolism of mono-HR was confined to glucuronidation and hydrolytic cleavage of the glycoside side chain. Ring fission products of mono-HR were not detected.
将单羟基雷洛昔芬静脉注射给比格犬后，单羟基雷洛昔芬及其葡萄糖醛酸结合物的血浆水平迅速下降，注射后8小时均检测不到。口服14C标记的单羟基雷洛昔芬后，血浆中检测到单羟基雷洛昔芬-葡萄糖醛酸结合物，证实单羟基雷洛昔芬被吸收，给药后72小时内可检测到低水平的14C。口服或静脉注射单羟基雷洛昔芬后，主要排泄途径是粪便以苷元形式排出该化合物。静脉给药后尿排泄量很少，低于15%，口服给药后为4%。单羟基雷洛昔芬的代谢仅限于葡萄糖醛酸化和糖苷侧链的水解裂解。未检测到单羟基雷洛昔芬的环裂变产物。
