Mouankie J B, Senczuk W, Florek E
Faculty of Pharmacy, Poznan University of Medical Sciences, Poznan, Poland.
Eur J Drug Metab Pharmacokinet. 2009 Jul-Sep;34(3-4):169-72. doi: 10.1007/BF03191169.
In this study, the kinetics of pyrimethamine elimination via the urine was investigated. The experiments were carried out on six healthy male volunteers aged 23-32 years. The drug was administered orally (p.o.) in a single dose at three different concentrations i.e.: 50, 75 and 100 mg. The concentration of the drug in the urine was determined via the modified method of Bonini et al. and Garber et al. It was found that 13.4 +/- 1.3% of the dose eliminated via the urine was in unchanged form. The process of pyrimethamine elimination may be described according to an open kinetic two-compartmental model: the formula showing the course of pyrimethamine elimination over time has been given. Several examples of the quantitative exposure test have been proposed, which allow the calculation of the drug dose absorbed and thus the degree of toxicity to be determined. This test can also be useful in a controlled clinical setting.
在本研究中，对乙胺嘧啶经尿液消除的动力学进行了研究。实验在6名年龄在23至32岁的健康男性志愿者身上进行。该药物以三种不同浓度即50、75和100毫克的单剂量口服给药。通过Bonini等人和Garber等人的改良方法测定尿液中药物的浓度。结果发现，经尿液消除的剂量中有13.4±1.3%为未变化形式。乙胺嘧啶的消除过程可根据开放动力学双室模型进行描述：给出了显示乙胺嘧啶随时间消除过程的公式。提出了几个定量暴露试验的例子，这些例子可以计算吸收的药物剂量，从而确定毒性程度。该试验在可控的临床环境中也可能有用。
