Rautio A, Kraul H, Kojo A, Salmela E, Pelkonen O
Department of Pharmacology and Toxicology, University of Oulu, Finland.
Pharmacogenetics. 1992 Oct;2(5):227-33. doi: 10.1097/00008571-199210000-00005.
A test designed to estimate the extent and rate of formation of 7-hydroxycoumarin by measuring the urinary excretion of the metabolite in humans after administering 5 mg coumarin was developed. Coumarin was rapidly metabolized after oral administration and more than 95% of the 7OHC formed was excreted in 4 h. The total amount of 7OHC formed was 64 +/- 15% (mean +/- SD, variation 20-100%) of the dose given. The percentage of 7OHC excreted in 2 h, as compared with the 7OHC excretion in 4 h, was found to be a constant and stable individual characteristic for the rate of the formation of 7OHC ('2 h coumarin test'). In 110 volunteers, there was a great interindividual variability in the extent and rate of 7OHC formation. Four individuals had relatively 'slow' coumarin test values (50-60%), but much larger populations would be needed for the demonstration of polymorphism.
开发了一种通过测量5毫克香豆素给药后人体尿液中代谢物的排泄情况来估计7-羟基香豆素形成程度和速率的测试。香豆素口服后迅速代谢，形成的7OHC中超过95%在4小时内排出。形成的7OHC总量为给药剂量的64±15%（平均值±标准差，变异范围20 - 100%）。与4小时内7OHC排泄量相比，2小时内排泄的7OHC百分比被发现是7OHC形成速率的一个恒定且稳定的个体特征（“2小时香豆素测试”）。在110名志愿者中，7OHC形成的程度和速率存在很大的个体间差异。有4个人的香豆素测试值相对“较慢”（50 - 60%），但需要更大的样本量来证明多态性。
