Kau S T, Sastry B V
J Pharm Sci. 1977 Jan;66(1):53-6. doi: 10.1002/jps.2600660112.
The tissue distribution of 14C-triamterene was examined in the fact. After intravenous administration of 14C-triamterene, high concentration ratios between tissues and blood were found in most tissues except the brain, fat, and testes. The maximal concentration of the drug was in the kidneys, liver, heart, lungs, and skeletal muscle within the first 20 min, when the maximal natriuresis was observed. No metabolite of triamterene was detected in these tissues. The pharmacokinetics of 14C-triamterene also were investigated. The volume of distribution of the drug was greater in the central compartment (60% of the dose) than in the peripheral compartment (40%). The binding of the drug to skeletal muscle is responsible for the fraction of the dose in the peripheral compartment. Rate constants indicate that slow elimination of triamterene is related to its binding to tissue in the central compartment.
在实验中检测了14C-氨苯蝶啶的组织分布。静脉注射14C-氨苯蝶啶后，除脑、脂肪和睾丸外，大多数组织中组织与血液之间的浓度比很高。给药后最初20分钟内，药物在肾脏、肝脏、心脏、肺和骨骼肌中的浓度最高，此时观察到最大利钠作用。在这些组织中未检测到氨苯蝶啶的代谢产物。还研究了14C-氨苯蝶啶的药代动力学。药物在中央室的分布容积（占剂量的60%）大于外周室（占剂量的40%）。药物与骨骼肌的结合导致了外周室中药物剂量的一部分。速率常数表明，氨苯蝶啶的缓慢消除与其在中央室中与组织的结合有关。
