Iwasaki M, Serizawa K, Suzuki T, Morishita M, Takahashi T, Muranishi S
Jpn J Antibiot. 1987 Jan;40(1):253-8.
Tissue concentrations of 14C-isepamicin (14C-HAPA-B) and its excretion were studied in male rats after 8- and 15-successive intramuscular administrations of 25 mg/kg/day. Plasma levels were hardly affected by the successive administration, and plasma concentrations as time patterns with 8- and 15-successive administrations were very similar to that with a single administration. Kidney levels of the drug increased remarkably by successive administrations. In all the organs tested except kidney, the elimination of the drug from the tissues tended to become somewhat slower with successive administrations but maximum concentrations were hardly affected by successive administrations. There was little difference between the excretion rates (urinary and fecal) after the successive doses and that after a single dose.
在雄性大鼠中,连续8次和15次以25mg/kg/天的剂量进行肌肉注射后,研究了14C-异帕米星(14C-HAPA-B)的组织浓度及其排泄情况。连续给药对血浆水平几乎没有影响,8次和15次连续给药时的血浆浓度随时间变化模式与单次给药时非常相似。连续给药后肾脏中的药物水平显著升高。在除肾脏外的所有测试器官中,随着连续给药,药物从组织中的消除往往会稍微变慢,但最大浓度几乎不受连续给药的影响。连续给药后的排泄率(尿液和粪便)与单次给药后的排泄率之间几乎没有差异。