Kurimoto T, Kobayashi H, Inoue A, Okachi R
Jpn J Antibiot. 1984 Jul;37(7):1263-71.
Absorption, tissue distribution and excretion of astromicin (ASTM) were studied in rats after intramuscular (i.m.), intravenous (i.v.) or drip intravenous (d.i.v.; for 15, 30 min. or 60 min.) administration at a dose of 20 mg/kg. The pharmacokinetic studies of ASTM were carried out using one-compartment open model (i.m.) or two-compartment open model (i.v. and d.i.v.). The peak values of ASTM observed in serum were 48.6 micrograms/ml (i.m.), 255.3 micrograms/ml (i.v.), 57.5 micrograms/ml (15 min. d.i.v.), 45.9 micrograms/ml (30 min. d.i.v.) and 39.1 micrograms/ml (60 min. d.i.v.). The pharmacokinetic parameters of ASTM after 15 min. d.i.v. administration were calculated as follows: Kel 0.110 min-1, T1/2 21.4 min., Vd beta 0.310 L/kg, Tmax 15.0 min., Cmax 58.6 micrograms/ml, AUC 1,991 micrograms X min/ml. ASTM was rapidly distributed into the kidneys and lungs. The peak values of ASTM in the kidneys were 156.8 micrograms/g (i.m.), 185.2 micrograms/g (i.v.), 132.9 micrograms/g (15 min. d.i.v.), 135.3 micrograms/g (30 min. d.i.v.) and 117.3 micrograms/g (60 min. d.i.v.). Urinary recovery rates of ASTM amounted to 85.5% (i.m.), 99.5% (i.v.) or 87.9% (30 min. d.i.v.). After i.m. or 30 min. d.i.v. administration of ASTM, no active metabolite was found in urine of rats.
在大鼠中，以20mg/kg的剂量进行肌内（i.m.）、静脉（i.v.）或静脉滴注（d.i.v.；持续15、30或60分钟）给药后，研究了阿司米星（ASTM）的吸收、组织分布和排泄情况。ASTM的药代动力学研究采用单室开放模型（i.m.）或双室开放模型（i.v.和d.i.v.）。血清中观察到的ASTM峰值分别为48.6微克/毫升（i.m.）、255.3微克/毫升（i.v.）、57.5微克/毫升（15分钟d.i.v.）、45.9微克/毫升（30分钟d.i.v.）和39.1微克/毫升（60分钟d.i.v.）。静脉滴注15分钟后ASTM的药代动力学参数计算如下：消除速率常数（Kel）0.110分钟-1，半衰期（T1/2）21.4分钟，β相表观分布容积（Vdβ）0.310升/千克，达峰时间（Tmax）15.0分钟，峰浓度（Cmax）58.6微克/毫升，药时曲线下面积（AUC）1991微克·分钟/毫升。ASTM迅速分布到肾脏和肺部。肾脏中ASTM的峰值分别为156.8微克/克（i.m.）、185.2微克/克（i.v.）、132.9微克/克（15分钟d.i.v.）、135.3微克/克（30分钟d.i.v.）和117.3微克/克（60分钟d.i.v.）。ASTM的尿回收率分别为85.5%（i.m.）、99.5%（i.v.）或87.9%（30分钟d.i.v.）。在ASTM进行肌内或30分钟静脉滴注给药后，大鼠尿液中未发现活性代谢物。
