冯玉书, 朱大珠. 杜鹃素的体内代谢J. 药学学报, 1979, 14(3): 149-155.
引用本文: 冯玉书, 朱大珠. 杜鹃素的体内代谢J. 药学学报, 1979, 14(3): 149-155.
Feng Yushu, Zhu Dazhu. METABOLISM OF FARREROLJ. Acta Pharmaceutica Sinica, 1979, 14(3): 149-155.
Citation: Feng Yushu, Zhu Dazhu. METABOLISM OF FARREROLJ. Acta Pharmaceutica Sinica, 1979, 14(3): 149-155.

杜鹃素的体内代谢

METABOLISM OF FARREROL

  • 摘要: 本文报告一项从生物样品中测定杜鹃素含量的简便、灵敏的分光光度法,并利用这个方法进行了一些杜鹃素体内代谢的研究。大鼠口服杜鹃素后约有30%的药物随粪排出,其余的药物在6~12小时内被吸收。口服后,药物在胃内有少量破坏。口服杜鹃素200mg/kg后1小时,能从肝脏测得少量药物,脂肪、脑、血液仅含痕迹量。静脉注射后药物在各组织中的分布以肺最高,然后脑、肝、肾、脾、心、脂肪等依次递降,血液最少。口服后5天尿中排出的未变药物仅占剂量的1.6%,大部分药物在体内被迅速转化,肝脏是转化杜鹃素的主要器官。从给药大鼠尿中分离到结晶杜鹃素及另外4个代谢产物,其中之一可能是杜鹃素的葡萄糖醛酸结合物。

     

    Abstract: Farrerol is one of the expectorant principles isolated from the aqueous extract of the leaves of Rhododendron dauricum L. The expectorant action and some other pharmacological activities of farrerol were reported in a previous paper. In the present article, some results on the metabolism of farrerol are reported.Farrerol in biological materials was extracted with ether at pH 6 and assayed spectrophotometrically in alkaline solution at 335 nm. This method was shown to be simple, sensitive and specific for the quantitative determination of farrerol in biological materials.Seventy to eighty per cent of the dose disappeared from the gastrointestinal tract 6~12 hours after oral administration of farrerol to rats. About thirty per cent of the dose was recoyered in the feces collected for four days. Low drug level (9.2μg/gm tissue) was found in the liver and only trace amounts of the drug were detected in the brain, blood and fat one hour after an oral dose of 200 mg/kg. After intravenous administration the highest drug level was found in the lungs, and the levels decreased in the order of brain, liver, kidneys, spleen, heart and fat, with the lowest level in the blood. Only 1.6 per cent of the drug was recovered in the five-day urine sample after a single oral dose. A great part of the drug was metabolized rapidly in the body, and the liver was shown to be the chief organ for the metabolism of farrerol.In addition to unchanged drug, four metabolic products of farrerol were isolated from the urine of drug-treated rats, one of them was considered to be the glucuronic acid conjugate of farrerol.

     

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