Baker J K, McChesney J D, Hufford C D, Clark A M
J Chromatogr. 1982 Jun 11;230(1):69-77. doi: 10.1016/s0378-4347(00)81431-0.
Using rats that had been dosed with 20 mg/kg of primaquine diphosphate (11.4 mg/kg free base), it was found that the drug underwent a metabolic oxidative deamination to give 8-(3-carboxy-1-methylpropylamino)-6-methoxyquinoline. The presence of this new mammalian metabolite was verified using high-performance liquid chromatographic, gas chromatographic, and mass spectral methods. A quantitative high-performance liquid chromatographic method for the determination of primaquine and the carboxylic acid metabolite in plasma using only 50 microliters of whole blood from the rat was developed and the method could be used to detect levels as low as 0.05 microgram/ml of the metabolite. Following intravenous administration of the drug, it was found that the plasma levels of primaquine fell very rapidly and after 30 min, the levels of the metabolite were much higher than those of primaquine.
使用已给予20毫克/千克磷酸伯氨喹（11.4毫克/千克游离碱）的大鼠，发现该药物发生代谢性氧化脱氨反应，生成8-(3-羧基-1-甲基丙基氨基)-6-甲氧基喹啉。使用高效液相色谱、气相色谱和质谱方法验证了这种新的哺乳动物代谢产物的存在。开发了一种仅使用大鼠50微升全血测定血浆中伯氨喹和羧酸代谢产物的定量高效液相色谱方法，该方法可用于检测低至0.05微克/毫升代谢产物的水平。静脉注射该药物后，发现伯氨喹的血浆水平下降非常迅速，30分钟后，代谢产物的水平远高于伯氨喹。
