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对雄性和雌性大鼠口服给予14C-芦荟大黄素后的药代动力学-代谢研究。

Pharmacokinetic-metabolic studies with 14C-aloe emodin after oral administration to male and female rats.

作者信息

Lang W

机构信息

Department of Radiobiochemistry, Madaus AG, Köln, FRG.

出版信息

Pharmacology. 1993 Oct;47 Suppl 1:110-9. doi: 10.1159/000139849.

DOI:10.1159/000139849
PMID:8234417
Abstract

After oral administration of 4.5 mg/kg 14C-aloe emodin (AE) to rats 20-30% of the dose was excreted in urine and the rest in feces. AE was quickly metabolized to rhein, to an unknown metabolite and to conjugates of all three. In the plasma about 10% of 14C-activity was identified as free AE. Maximum plasma values were reached 1.5-3 h p.a. with 248 (male) and 441 (female) ng equivalents AE/ml. Maximum concentrations in plasma were about 3 times higher than those in ovaries and 10 times higher than those in testes. Only liver, kidney and intestinal tract showed higher concentrations than plasma. Terminal half-life (for radioactivity) in blood was about 50 h.

摘要

给大鼠口服4.5mg/kg的14C-芦荟大黄素(AE)后,20%-30%的剂量经尿液排出,其余经粪便排出。AE迅速代谢为大黄酸、一种未知代谢物以及这三种物质的结合物。血浆中约10%的14C活性被鉴定为游离AE。给药后1.5-3小时达到血浆最大值,雄性为248 ng当量AE/ml,雌性为441 ng当量AE/ml。血浆中的最大浓度约为卵巢中的3倍,睾丸中的10倍。只有肝脏、肾脏和肠道的浓度高于血浆。血液中放射性的终末半衰期约为50小时。

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