Iscan M, Rostami H, Iscan M, Güray T, Pelkonen O, Rautio A
Department of Toxicology, Faculty of Pharmacy, Ankara University, Turkey.
Eur J Clin Pharmacol. 1994;47(4):315-8. doi: 10.1007/BF00191161.
One hundred healthy Turkish volunteers (70 male, 30 female) aged from 19 to 56 years were given 5 mg coumarin p.o. after an overnight fast. Urine samples were collected before and 2, 4 and 8 h after drug administration. The extent and rate of formation of 7-OH-coumarin (7OHC) was determined by the urinary excretion of the metabolite as measured with the fluorometric method. On average, 80% of 7OHC formed was excreted in 2 h. The total amount of 7OHC formed was 59.8% (21.5%) (mean and SD, n = 100, range 17-100%) of the given dose. The percentage of 7OHC excreted during the first 2 h compared with the 7OHC excretion at 8 h was a constant and stable individual characteristic for the rate of the formation of 7OHC ('2 h coumarin test'). Although four individuals had relatively slow coumarin test values (34-40%), no clear-cut polymorphism in the rate of 7OHC formation was found. However, 7OHC formation was lower in males and in cigarette smokers.
一百名年龄在19至56岁之间的健康土耳其志愿者（70名男性，30名女性）在禁食过夜后口服5毫克香豆素。在给药前以及给药后2、4和8小时收集尿液样本。通过荧光法测量代谢物的尿排泄量来确定7-羟基香豆素（7OHC）的生成程度和速率。平均而言，生成的7OHC中有80%在2小时内排出。生成的7OHC总量为给予剂量的59.8%（21.5%）（均值和标准差，n = 100，范围17 - 100%）。与8小时时7OHC排泄量相比，前2小时内排泄的7OHC百分比是7OHC生成速率的一个恒定且稳定的个体特征（“2小时香豆素试验”）。尽管有四名个体的香豆素试验值相对较低（34 - 40%），但未发现7OHC生成速率有明显的多态性。然而，男性和吸烟者的7OHC生成量较低。
