Kállay Z, Soltés L, Trnovec T
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, Czechoslovakia.
Biopharm Drug Dispos. 1991 Apr;12(3):201-5. doi: 10.1002/bdd.2510120304.
Stobadin dihydrochloride was administered p.o. to rats at a dose of 1 mg kg-1 once daily for 25 consecutive days. The peak and trough concentrations of the sum of stobadin metabolites, determined from Days 6-16 of treatment, demonstrated a steady-state. The mean daily excretion of 3H-radioactivity during this period was 43 per cent and 52 per cent of the administered dose into urine and faeces, respectively. The terminal half-life of stobadin in plasma following a 25-day chronic treatment was 78.3 min, which was shorter than the value of 95.3 min, determined in a single dose experiment. The data indicate that no accumulation of stobadin and of its labelled metabolites occurs in the course of repeated administration of 3H-stobadin.
将盐酸司巴丁以1毫克/千克的剂量口服给予大鼠，每日一次，连续给药25天。在治疗的第6至16天测定的司巴丁代谢物总和的峰浓度和谷浓度显示达到了稳态。在此期间，3H放射性的平均日排泄量分别为给药剂量的43%和52%，进入尿液和粪便中。经过25天慢性治疗后，司巴丁在血浆中的终末半衰期为78.3分钟，这比单次给药实验中测定的95.3分钟的值要短。数据表明，在重复给予3H-司巴丁的过程中，司巴丁及其标记代谢物不会发生蓄积。
