Beermann B, Groschinsky-Grind M, Rosén A
Clin Pharmacol Ther. 1976 May;19(5 Pt 1):531-7. doi: 10.1002/cpt1976195part1531.
14C-hydrochlorothiazide (hct) was administered orally (n=4) and iv (n = 2 to healthy subjects. The gastrointestinal absorption ranged between 60% and 80%, most of it took place in the duodenum and the upper jejunum. The radioactivity was eliminated mainly in the urine, while no sigificant biliary excretion was observed. Chromatographic analysis of the urinary radioactivity demonstrated that greater than 95% of the absorbed or injected 14C-hct was excreted unchanged. The radioactivity in plasma during the first 10 hr after oral administration declined with a fast phase but the levels of label thereafter suggested a slow phase. The existence of such a phase was verified in 1 subject given 75 mg hct orally. His plasma levels of hct (determined with gas-liquid chromatography) declined according to a 2-compartment model, the half-lives of the alpha-and beta-phases being 1.7 and 13.1 hr, respectively. Hct accumulated in the blood cells and the ratio between the radioactivity in cells and that in plasma averaged 3.5. The fate of a single dose of 14C-hct in 2 hypertensive patients treated with the drug chronically was similar to that in the healthy subjects. A third patient, who had slightly elevated serum creatinine, eliminated hct more slowly than the others. Like the healthy subjects, the patients eliminated hct to greater than 95% in unchanged form.
给4名健康受试者口服14C - 氢氯噻嗪（hct），给2名健康受试者静脉注射14C - 氢氯噻嗪。胃肠道吸收范围在60%至80%之间，大部分吸收发生在十二指肠和空肠上段。放射性主要经尿液排出，未观察到明显的胆汁排泄。对尿液放射性的色谱分析表明，吸收或注射的14C - hct中超过95%以原形排泄。口服给药后最初10小时内血浆中的放射性以快速相下降，但此后的标记物水平显示为缓慢相。在1名口服75mg hct的受试者中证实了该相的存在。他的血浆hct水平（用气液色谱法测定）根据二室模型下降，α相和β相的半衰期分别为1.7小时和13.1小时。hct在血细胞中蓄积，细胞与血浆中的放射性之比平均为3.5。2名长期接受该药物治疗的高血压患者单次服用14C - hct后的情况与健康受试者相似。第三名患者血清肌酐略有升高，其hct清除比其他患者慢。与健康受试者一样，患者以大于95%的原形清除hct。
