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给兔子肠胃外注射精氨酸血红素后血红素的去向

Fate of haem after parenteral administration of haem arginate to rabbits.

作者信息

Lindén I B, Tokola O, Karlsson M, Tenhunen R

出版信息

J Pharm Pharmacol. 1987 Feb;39(2):96-102. doi: 10.1111/j.2042-7158.1987.tb06952.x.

Abstract

Rabbits were injected either intravenously or intramuscularly with [14C]haem arginate and [59Fe]haem arginate (haem 5 mg kg-1). The main part (80%) of AUCINF of labelled haem was associated with the beta-phase, T1/2 being about 6 h. Only 1% of the haem dose had been taken up by the red blood cells. In contrast, the iron moiety from the haem molecule was effectively utilized. Thirty days post-injection of [59Fe]haem arginate, 40% of the dose after intravenous injection and 60% after intramuscular injection was circulating with the red cells. Radioactivity was shown to concentrate in the liver, where haem is mainly metabolized and eliminated. An accumulation of haem in the adrenals was also evident. Haem itself did not concentrate in the bone marrow, and a negligible amount of radioactivity was recovered from brain, implying a poor penetration of the blood brain barrier.

摘要

给兔子静脉注射或肌肉注射[14C]血红素精氨酸盐和[59Fe]血红素精氨酸盐(血红素5毫克/千克)。标记血红素的AUCINF的主要部分(80%)与β期相关,半衰期约为6小时。只有1%的血红素剂量被红细胞摄取。相比之下,血红素分子中的铁部分得到了有效利用。注射[59Fe]血红素精氨酸盐30天后,静脉注射后40%的剂量和肌肉注射后60%的剂量与红细胞一起循环。放射性显示集中在肝脏,血红素主要在肝脏中代谢和消除。肾上腺中也明显有血红素积累。血红素本身并不集中在骨髓中,从大脑中回收的放射性极少,这意味着血脑屏障的穿透性较差。

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