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羟乙基芦丁的肝清除率及处置情况

Hepatic clearance and disposition of hydroxyethylrutosides.

作者信息

Griffiths L A, Hackett A M

出版信息

Arch Toxicol Suppl. 1978(1):243-6. doi: 10.1007/978-3-642-66896-8_45.

DOI:10.1007/978-3-642-66896-8_45
PMID:277108
Abstract

Although salts of rutin on i-v admin. undergo insolubilization giving rise to concretions and suppurative inflammation in the liver this was not observed in respect of the vaso-active hydroxyethylrutosides (Pfeifer et al., 1970). I-v admin. of 3',4',7-tri0-(beta-hydroxy[14C]ethyl)-rutoside (tri-HR) and 7-mono0-(beta-hydroxy[14C]ethyl)rutoside (mono-HR) to mice showed rapid biliary excretion (approx. 71% within 24 h). Approx. 2/3 of the dose was subsequently excreted in faeces and ca. 25% in urine over 72 h. Autoradiography and scintilation counting showed short term concentration in the liver over the initial 4 h period but at 72 h less than 0.22% of tri-HR and 0.59% of mono-HR was detectable in hepatic tissue. Carcasses of mice killed at 72 h contained less than 7% of the initial dose which was mainly present in intestinal contents.

摘要

尽管芦丁盐静脉注射后会发生不溶解,导致肝脏出现结石和化脓性炎症,但血管活性羟乙基芦丁糖苷(Pfeifer等人,1970年)并未观察到这种情况。给小鼠静脉注射3',4',7-三-O-(β-羟基[14C]乙基)-芦丁糖苷(三-HR)和7-单-O-(β-羟基[14C]乙基)芦丁糖苷(单-HR)后,显示出胆汁快速排泄(24小时内约71%)。随后,约2/3的剂量在72小时内通过粪便排出,约25%通过尿液排出。放射自显影和闪烁计数显示,最初4小时内在肝脏中有短期浓度,但在72小时时,肝组织中可检测到的三-HR不到0.22%,单-HR不到0.59%。在72小时处死的小鼠尸体中,所含初始剂量不到7%,主要存在于肠道内容物中。

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1
Hepatic clearance and disposition of hydroxyethylrutosides.羟乙基芦丁的肝清除率及处置情况
Arch Toxicol Suppl. 1978(1):243-6. doi: 10.1007/978-3-642-66896-8_45.
2
The disposition and metabolism of 3',4',7-tri-O-(beta-hydroxyethyl)rutoside and 7-mono-O-(beta-hydroxyethyl)rutoside in the mouse.3',4',7-三-O-(β-羟乙基)芦丁糖苷和7-单-O-(β-羟乙基)芦丁糖苷在小鼠体内的处置与代谢
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Metabolism of hydroxyethylrutosides (HR): metabolism of [14C]-HR in man.羟乙基芦丁(HR)的代谢:人体内[14C]-HR的代谢
Arzneimittelforschung. 1976;26(5):925-8.
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