Kwong E C, Chen F C, Young L M
CanTest Ltd., Vancouver, British Columbia.
Can J Vet Res. 1989 Apr;53(2):147-53.
The urinary excretion of a sustained-release formulation of pentoxifylline was studied in the horse after the oral administration of 4.0 grams of Trental tablets. Urine samples were collected for 24 hours after dosing and analyzed for pentoxifylline and its metabolites using high-performance liquid chromatography coupled with an ultraviolet detector. Six metabolites of pentoxifylline were identified in horse urine in addition to less than 0.2% of unchanged drug. Concomitant use of gas chromatography/mass spectrometry allowed for the elucidation of the chemical structures of the metabolites. Metabolism of pentoxifylline yields one demethylated derivative, four hydroxylated metabolites and a conjugate of one of the hydroxymetabolites as urine products. The demethylated derivative, 3-methyl-1-(5-oxohexyl)-xanthine, was found to be the predominant metabolite in the urine.
在给马口服4.0克己酮可可碱片（Trental片）后，对己酮可可碱缓释制剂的尿排泄情况进行了研究。给药后收集24小时尿液样本，采用高效液相色谱-紫外检测器分析其中的己酮可可碱及其代谢产物。除了不到0.2%的未变化药物外，在马尿中还鉴定出了六种己酮可可碱代谢产物。同时使用气相色谱/质谱联用技术有助于阐明代谢产物的化学结构。己酮可可碱的代谢产生一种去甲基化衍生物、四种羟基化代谢产物以及其中一种羟基化代谢产物的共轭物作为尿液产物。去甲基化衍生物3-甲基-1-(5-氧代己基)-黄嘌呤被发现是尿液中的主要代谢产物。
