THE DETOXICATION AND EXCRETION OF BETA PHENYLISOPROPYLAMINE (BENZEDRINE)
THE DETOXICATION AND EXCRETION OF BETA PHENYLISOPROPYLAMINE (BENZEDRINE)
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β-苯基异丙胺（苯丙胺）的解毒和排泄
DOI：
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发表时间：
1940
期刊：
影响因子：
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通讯作者：
J. Skinner
中科院分区：
文献类型：
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作者：
K. Beyer;J. Skinner
描述了一种检测和测定苯扎碱的新方法。显色反应的原理是β-苯基异丙胺与氯化对硝基苯重氮盐偶合，当偶合化合物的溶液呈碱性时，产生颜色。该方法已适用于研究身体消除苯基异丙胺的方式。结果发现，摄入后 48 小时内排出的化合物量略低于一半。在人类中，给定剂量的排泄百分比通常与尿量输出平行。较小剂量的排泄百分比通常较高。个体排泄光学活性形式药物的能力各不相同。为了解释药物的剩余部分，进行了多项实验。通过这些结果表明：1）不仅仅是一半而是可能全部药物都从胃肠道吸收，2）尿液样品的水解不会导致胺产量增加，3）胺氧化酶显然不会激活苯扎碱的氧化脱氨作用。由于药物的排泄明显超过了其生理作用，并且四氯化碳对某些器官的功能损害增加到每 24 小时排泄药物量的 100%，因此进行了以下扣除。苯扎汀显然通过与体内通常含有的某些药剂的松散组合而在体内缓慢且部分失活。目前研究的问题是药物是否被部分破坏，或者在几天的时间内缓慢排出，无论是游离的还是松散地结合到没有明显结合的程度。
A new method is described for the detection and determination of benzedrine. The principle of the color reaction is the coupling of betaphenylisopropylamine with para nitrobenzenediazonium chloride with resulting color formation when the solution of the coupled compound is made alkaline. The method has been adapted to a study of the manner in which the body eliminates phenylisopropylamine. It was found that somewhat less than half the amount of the compound was excreted within 48 hours following ingestion. In man the per cent excreted of a given dose generally paralleled the volume output of urine. The per cent excreted was usually greater for the smaller doses. Individuals varied in their ability to excrete optically active forms of the drug. In an attempt to account for the remainder of the drug several experiments were conducted. By means of these it was shown: 1) that not just half but probably all the drug is absorbed from the gastrointestinal tract, 2) hydrolysis of urine samples does not result in a greater yield of the amine, and 3) amine oxidase apparently does not activate oxidative deamination of benzedrine. From the fact that the excretion of the drug so markedly outlasts its physiological effect, and that impairing the function of certain organs by carbon tetrachloride increased to 100 per cent the amount of the drug excreted per 24 hours the following deduction was made. Benzedrine is apparently slowly and partially inactivated in the body by a loose combination with some agent normally contained therein. Whether the drug is then partially destroyed, or excreted slowly over a period of several days either free or so loosely combined as to be not apparently conjugated is the problem of a present investigation.