Hasegawa J, Lin E T, Williams R L, Sörgel F, Benet L Z
J Pharmacokinet Biopharm. 1982 Oct;10(5):507-23. doi: 10.1007/BF01059034.
The pharmacokinetic profiles of triamterene and hydroxytriamterene sulfuric acid ester, the major metabolite of triamterene, were studied in six normal male volunteers using a newly developed specific HPLC analytical method. Following a 100 mg oral dose of triamterene, the plasma concentration time course of the sulfate conjugate parallels that of triamterene in all subjects, but concentrations of the metabolite were more than 10 times higher than unchanged triamterene concentrations at identical sampling times. Interestingly, the renal clearance of the sulfate conjugate was less than that of triamterene. These characteristic features of triamterene disposition were fitted to a compartment model incorporating a first-pass metabolic process. Unbound fractions of triamterene and metabolite in plasma were 0.39 and 0.10 (mean of 6 subjects), respectively. The low unbound fraction of the metabolite in plasma most probably accounts for the low renal clearance of the sulfate conjugate as compared with triamterene.
采用新开发的特异性高效液相色谱分析方法，在6名正常男性志愿者中研究了氨苯蝶啶及其主要代谢产物氨苯蝶啶硫酸酯的药代动力学特征。口服100mg氨苯蝶啶后，在所有受试者中，硫酸酯结合物的血浆浓度-时间过程与氨苯蝶啶相似，但在相同采样时间，代谢产物的浓度比未变化的氨苯蝶啶浓度高10倍以上。有趣的是，硫酸酯结合物的肾脏清除率低于氨苯蝶啶。氨苯蝶啶处置的这些特征符合包含首过代谢过程的房室模型。氨苯蝶啶及其代谢产物在血浆中的游离分数分别为0.39和0.10（6名受试者的平均值）。与氨苯蝶啶相比，代谢产物在血浆中的低游离分数很可能是硫酸酯结合物肾脏清除率低的原因。
