Matsumoto H, Ochiai K, Nakajima A, Matsuzaki M
Jpn J Antibiot. 1982 Aug;35(8):2034-46.
Absorption, excretion and distribution of amikacin sulfate (AMK) obtained following administration by drip intravenous infusion (d.i.v.) were studied in dogs, rabbits and rats, and were compared with those obtained after one shot intravenous infusion (i.v.) and intramuscular injection (i.m.). 1. The plasma concentration and urinary excretion of AMK following d.i.v. were compared with those after i.v. and i.m. in dogs and rabbits. The peaks of plasma concentration following d.i.v. were obtained at the end of d.i.v. and it was clearly observed a linear dependence between the peak values and the doses both in dogs and in rabbits. There were no significant differences in the peak plasma concentrations between 1 hour d.i.v. and i.m. at the doses of 25 mg/kg and 50 mg/kg in dogs and at each dose in rabbits. At the higher dose (100 mg/kg) in dogs, the peak plasma concentration following 1 hour d.i.v. was slightly higher than that after i.m. The plasma concentrations at 10 minutes after i.v. were elevated about twice as high as the peak plasma concentrations following 1 hour d.i.v. both in dogs and in rabbits. The urinary recoveries following d.i.v. and i.v. were more than 90% and those after i.m. were about 85%. 2. The tissue and organ concentrations of AMK following 1 hour d.i.v. were studies in rats and rabbits. The peak concentrations were obtained at the end of d.i.v. in any tissue and organ. Kidney was the highest and plasma, lungs, heart, stomach and so on were followed. The concentration in kidney was remained but those in other tissues and organs were decreased soon. 3. The plasma concentrations following d.i.v. in dogs were well agreed with the pharmacokinetic analysis in the two-compartment model, as the means of relative errors (1Xm - Xc1 divided by Xc) between the measured plasma concentration (Xm) and the calculated one (Xc) were less than 10% and the deviations of the pharmacokinetic parameters were in little ranges. The plasma concentrations during and just after d.i.v. were also agreed enough with the pharmacokinetic analysis in the one-compartment model.
研究了硫酸阿米卡星(AMK)通过静脉滴注(d.i.v.)给药后在犬、兔和大鼠体内的吸收、排泄和分布情况,并与单次静脉注射(i.v.)和肌肉注射(i.m.)后的情况进行了比较。1. 在犬和兔中,比较了静脉滴注后AMK的血浆浓度和尿排泄与静脉注射和肌肉注射后的情况。静脉滴注后血浆浓度峰值在滴注结束时出现,并且在犬和兔中均清楚地观察到峰值与剂量之间呈线性关系。在犬中25mg/kg和50mg/kg剂量以及兔中的各剂量下,静脉滴注1小时后的血浆峰值浓度与肌肉注射1小时后的血浆峰值浓度之间无显著差异。在犬中较高剂量(100mg/kg)时,静脉滴注1小时后的血浆峰值浓度略高于肌肉注射后的。静脉注射后10分钟时的血浆浓度在犬和兔中均比静脉滴注1小时后的血浆峰值浓度高出约两倍。静脉滴注和静脉注射后的尿回收率超过90%,肌肉注射后的约为85%。2. 研究了大鼠和兔静脉滴注1小时后AMK在组织和器官中的浓度。在任何组织和器官中,峰值浓度在滴注结束时出现。肾脏中浓度最高,其次是血浆、肺、心脏、胃等。肾脏中的浓度保持不变,但其他组织和器官中的浓度很快下降。3. 犬静脉滴注后的血浆浓度与二室模型的药代动力学分析结果吻合良好,因为实测血浆浓度(Xm)与计算浓度(Xc)之间的相对误差平均值((1Xm - Xc1)除以Xc)小于10%,药代动力学参数的偏差范围很小。静脉滴注期间及刚结束后的血浆浓度也与一室模型的药代动力学分析结果吻合得足够好。