Franklin R A, Robson P, Stevenson D
Eur J Clin Pharmacol. 1983;24(5):629-34. doi: 10.1007/BF00542212.
The absorption, metabolism and excretion of the new antihypertensive agent indoramin (Baratol) have been studied in male volunteers following oral administration of the drug labelled either with 14C or with tritium. Absorption of the drug proceeded at moderate rate, peak plasma radioactivity levels being seen by 3 h after dosing. Metabolism was extensive as shown by very little unchanged compound appearing in urine. Two major urinary metabolites accounting for some 35-40% of the renally excreted material were identified as acid labile conjugates of indoramin itself and indole 6-hydroxylated indoramin. The pattern of biotransformation appeared to be similar to that in the patas monkey, the species used in the long term safety evaluation of the drug. Excretion of the drug and metabolites occurred primarily via the faeces which accounted for 49.7 +/- 4.9% of the dose. A further 31.7 +/- 2.4% was recovered in the urine. Renal elimination of total radioactivity occurred in an apparently monoexponential manner with a half-life of 11.9 +/- 1.2 h.
在男性志愿者口服用¹⁴C或氚标记的新型抗高血压药物吲哚拉明（Baratol）后，对其吸收、代谢和排泄情况进行了研究。药物吸收速度适中，给药后3小时可见血浆放射性水平达到峰值。由于尿液中几乎没有未变化的化合物，表明代谢广泛。两种主要的尿液代谢物约占经肾脏排泄物质的35 - 40%，被鉴定为吲哚拉明本身和吲哚6 - 羟基化吲哚拉明的酸不稳定共轭物。生物转化模式似乎与用于该药物长期安全性评估的白脸猴相似。药物和代谢物主要通过粪便排泄，占剂量的49.7±4.9%。另外31.7±2.4%在尿液中回收。肾脏对总放射性的消除呈明显的单指数方式，半衰期为11.9±1.2小时。
