Hoener B, Patterson S E
Clin Pharmacol Ther. 1981 Jun;29(6):808-16. doi: 10.1038/clpt.1981.115.
Nitrofurantoin (50 mg) was administered in a three-way random crossover design to six healthy men. After a 45-min intravenous infusion the plasma concentration data could be described by a two-compartment open-body model with a terminal t 1/2 of 58.1 +/- 15 min. Oral availability of a tablet was 0.87 +/- 0.13 on a fasting stomach and 0.94 +/- 0.13 when taken with food. Although absorption appeared to be complete, the absorption rate profile was complex and erratic. Two subjects failed to achieve the minimum effective urine concentration of 32 micrograms/ml. After the intravenous infusion 47 +/- 13% of the dose was excreted unchanged in the urine and 1.2 +/- 0.3% was recovered as the reduced metabolite aminofurantoin.
对6名健康男性采用三向随机交叉设计给予呋喃妥因(50毫克)。在45分钟静脉输注后,血浆浓度数据可用二室开放型人体模型描述,终末半衰期为58.1±15分钟。空腹时片剂的口服生物利用度为0.87±0.13,与食物同服时为0.94±0.13。虽然吸收似乎是完全的,但吸收速率曲线复杂且不稳定。两名受试者未能达到32微克/毫升的最低有效尿浓度。静脉输注后,47±13%的剂量以原形经尿液排泄,1.2±0.3%以还原代谢产物氨基呋喃妥因的形式回收。