Van der Meer M J, Hundt H K, Müller F O
J Pharm Pharmacol. 1986 Oct;38(10):781-4. doi: 10.1111/j.2042-7158.1986.tb04494.x.
A metabolic pattern of atropine in man, based on the detection of radiolabelled products in urine by high performance liquid chromatography after administration of [3H]atropine sulphate to a normal volunteer is proposed. Noratropine (24%), atropine-N-oxide (equatorial isomer) (15%), tropine (2%) and tropic acid (3%) appear to be the major metabolites, while 50% of the administered dose is excreted as apparently unchanged atropine. No conjugates were detectable. Evidence that atropine is present as (+)-hyoscyamine was found, suggesting that stereoselective metabolism of atropine probably occurs.
提出了一种人体中阿托品的代谢模式,该模式基于对一名正常志愿者静脉注射[3H]硫酸阿托品后,通过高效液相色谱法检测尿液中放射性标记产物得出。去甲阿托品(24%)、阿托品 - N - 氧化物(赤道异构体)(15%)、托品(2%)和托品酸(3%)似乎是主要代谢产物,而给药剂量的50%以明显未变化的阿托品形式排泄。未检测到结合物。发现有证据表明阿托品以(+)- 莨菪碱形式存在,这表明阿托品可能发生立体选择性代谢。