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7-单-0-(β-羟乙基)芦丁糖苷在犬体内的代谢与排泄

The metabolism and excretion of 7-mono-0-(beta-hydroxyethyl) rutoside in the dog.

作者信息

Hackett A M, Griffiths L A

出版信息

Eur J Drug Metab Pharmacokinet. 1979;4(4):207-12. doi: 10.1007/BF03189428.

Abstract

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.

摘要

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。

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