Scheurlen M, Bittiger H, Ammann B
J Pharm Sci. 1984 Apr;73(4):561-3. doi: 10.1002/jps.2600730432.
A sensitive radioligand binding assay is described for the determination of scopolamine in human urine. As a measure for the drug concentration, the quantitative displacement of scopolamine of tritiated quinuclidinyl benzylate from rat brain receptors was used. The assay is sensitive to concentrations as low as 1.2 ng/mL, surpassed only by GC-MS techniques. It can be performed easily and quickly and does not include extraction procedures. Scopoline and scopine , possible metabolites of scopolamine, do not interfere with the assay. After transdermal administration of scopolamine, 34% of the drug is found in the urine. Of the total scopolamine excreted, 79% is conjugated to glucuronic and/or sulfuric acid and 21% is excreted in the unbound form.
本文描述了一种用于测定人尿液中东莨菪碱的灵敏放射性配体结合分析方法。作为药物浓度的一种测量方法，使用了氚标记的奎宁环基苯甲酸酯从大鼠脑受体上被东莨菪碱定量取代的情况。该分析方法对低至1.2 ng/mL的浓度敏感，仅被气相色谱-质谱联用技术超越。它操作简便、快速，且不包括提取步骤。东莨菪碱可能的代谢产物东莨菪醇和东莨菪碱对该分析无干扰。经皮给予东莨菪碱后，34%的药物可在尿液中被发现。在排泄出的总东莨菪碱中，79%与葡萄糖醛酸和/或硫酸结合，21%以未结合形式排泄。
