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[吗啡向吗啡 -3- 葡糖苷酸和吗啡 -5- 葡糖苷酸葡糖醛酸化的剂量依赖性初步研究]

[Pilot study of dose dependence in glucuronidation of morphine to morphine-3- and morphine-5-glucuronide].

作者信息

Friedrich G, Krieger A, Stritt W, Vach W

机构信息

Institut für Rechtsmedizin, Universität Freiburg.

出版信息

Beitr Gerichtl Med. 1992;50:215-20.

PMID:1489328
Abstract

In the capacity of an initial study both, the half-lives of morphine and its metabolites morphine-3-glucuronide and morphine-6-glucuronide as well as the ratio of concentrations in the development of time using two different dosages were determined and shown by comparison. A bolus of 10 mg (10 micrograms) tritium-marked morphine was administered intravenously. Subsequently the half-lives of morphine, morphine-3-glucuronide and morphine-6-glucuronide in serum, saliva and urine were determined. To achieve this, morphine and its glucuronides were separated via HPLC and then quantified by measuring the radioactivity. In addition to the short half-lives of morphine and morphine-glucuronides long half-lives were found in the range of 12.6 to 20 hours in serum and urine. There was no positive evidence for glucuronides in saliva. In urine the morphine/glucuronide ratio showed a linear resp. exponential development dependent of dose.

摘要

作为一项初步研究,测定并比较了吗啡及其代谢产物吗啡 - 3 - 葡萄糖醛酸苷和吗啡 - 6 - 葡萄糖醛酸苷的半衰期,以及两种不同剂量下随时间变化的浓度比。静脉注射10毫克(10微克)氚标记的吗啡。随后测定血清、唾液和尿液中吗啡、吗啡 - 3 - 葡萄糖醛酸苷和吗啡 - 6 - 葡萄糖醛酸苷的半衰期。为此,通过高效液相色谱法分离吗啡及其葡萄糖醛酸苷,然后通过测量放射性进行定量。除了吗啡和吗啡 - 葡萄糖醛酸苷的半衰期较短外,在血清和尿液中还发现了12.6至20小时范围内的长半衰期。唾液中未发现葡萄糖醛酸苷的阳性证据。尿液中吗啡/葡萄糖醛酸苷的比例呈线性或指数增长,取决于剂量。

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