Iwasaki M, Serizawa K, Suzuki T, Morishita M, Takahashi T, Muranishi S
Jpn J Antibiot. 1987 Jan;40(1):259-66.
Placental transfer and excretion into milk of 14C-isepamicin sulfate (14C-HAPA-B) following a single intramuscular or intravenous dose of 25 mg/kg were studied in pregnant or lactating rats. Concentrations of HAPA-B in placenta, ovary and uterus reached their maxima in 10 minutes after administration then declined rapidly. The maximum concentration in the fetal membrane was similar to 10-minute levels in these other tissues, but was attained in 4 hours or later after the drug administration and some drug still remained there even at 24 hours. A small amount of radioactivity was distributed into the fetus and the maximum level in the fetus was attained in 1 approximately 4 hours after administration, much later than in maternal tissues. The concentration in the fetal kidney was the highest in the fetus, but only 1 microgram/g or lower was found. A very small amount of radioactivity was also found in the fetal bone by radioautography. The drug was excreted into milk at 2 approximately 4 micrograms/ml during the first 6 hours and decreased a little in 24 hours after administration. There was no difference in results due to administration routes.
在怀孕或泌乳大鼠中，研究了单次肌肉注射或静脉注射25mg/kg硫酸14C-异帕米星（14C-HAPA-B）后，其在胎盘的转运及向乳汁中的排泄情况。给药后10分钟，胎盘、卵巢和子宫中的HAPA-B浓度达到最大值，随后迅速下降。胎膜中的最大浓度与其他组织10分钟时的水平相似，但在给药后4小时或更晚时达到，甚至在24小时时仍有一些药物残留。少量放射性分布到胎儿体内，给药后约4小时胎儿体内达到最大水平，比母体组织晚得多。胎儿肾脏中的浓度在胎儿各组织中最高，但仅为1微克/克或更低。通过放射自显影在胎儿骨骼中也发现了极少量放射性。给药后的前6小时，药物以约2至4微克/毫升的浓度排泄到乳汁中，给药后24小时略有下降。给药途径对结果无差异。
