Di Carlo F J, Crew M C, Brusco L S, Davidson I W
Clin Pharmacol Ther. 1977 Sep;22(3):309-15. doi: 10.1002/cpt1977223309.
The absorption, excretion, and biotransformation of 14C-labeled pentaerythritol (PE) trinitrate was studied in man. The administration of a single sublingual dose was followed by rapid absorption and extensive biotransformation. Six drug metabolites were identified. Final excretion of the drug and its metabolites was almost totally through the kidney. Low levels of unchanged drug were present in plasma and urine. PE mononitrate was the major drug metabolite in plasma and urine. Glucuronides of PE trinitrate, dinitrate, and mononitrate were identified for the first time in man. PE trinitrate glucuronide appeared in plasma rapidly and about 8% of the dose was excreted in urine. Reversible and irreversible pathways are proposed for the formation of the metabolites. The reconversion of PE trinitrate glucuronide to PE trinitrate is postulated to explain the duration of drug activity and excretion.
对14C标记的季戊四醇三硝酸酯（PE）在人体中的吸收、排泄及生物转化进行了研究。单次舌下给药后，药物迅速吸收并发生广泛的生物转化。鉴定出六种药物代谢产物。药物及其代谢产物的最终排泄几乎完全通过肾脏。血浆和尿液中存在少量未变化的药物。单硝酸PE是血浆和尿液中的主要药物代谢产物。首次在人体中鉴定出三硝酸PE、二硝酸PE和单硝酸PE的葡糖醛酸苷。三硝酸PE葡糖醛酸苷迅速出现在血浆中，约8%的剂量经尿液排泄。提出了代谢产物形成的可逆和不可逆途径。推测三硝酸PE葡糖醛酸苷向三硝酸PE的再转化可解释药物活性和排泄的持续时间。
