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[儿童磷霉素钠吸收与排泄的研究]

[A study of the absorption and excretion of fosfomycin sodium in children].

作者信息

Iwai N, Nakamura H, Miyazu M, Watanabe Y

机构信息

Pediatric Department, Meitetsu Hospital.

出版信息

Jpn J Antibiot. 1991 Mar;44(3):345-56.

PMID:1880916
Abstract

Fosfomycin sodium (FOM-Na, Forocyle-S) was administered at 25 mg/kg or 50 mg/kg to 15 children between the ages of 3 and 15 through intravenous injection or through 1 hour intravenous drip infusion, and concentrations in blood serum and excretion through urine were examined and a pharmacokinetic analysis was carried out using the one-compartment model. 1. Average concentrations in the blood serum after injections with 25 mg/kg and 50 mg/kg were 55.3 +/- 6.3 micrograms/ml and 118.8 +/- 31.1 micrograms/kg 30 minutes after injection, respectively, and their half-lives were 1.04 +/- 0.15 hours and 0.98 +/- 0.17 hours, respectively. Six hours after injection, the levels were 2.7 +/- 1.6 micrograms/kg and 6.2 +/- 5.5 micrograms/kg, respectively. With 1 hour intravenous drip infusion of 25 mg/kg and 50 mg/kg, average concentrations the blood serum were 34.2 +/- 14.9 micrograms/ml and 89.7 +/- 6.7 micrograms/ml, respectively, and their half-lives were 0.87 +/- 0.24 hour and 0.69 +/- 0.10 hour, respectively. Six hours after the administration, the levels were 2.7 +/- 1.8 micrograms/ml and 6.7 +/- 0.8 micrograms/ml. There was a clear dose response in the concentration levels in the blood in those given the drug at 25 mg/kg and 50 mg/kg in either method of administration. 2. Average levels in urine after injection of 25 mg/kg and 50 mg/kg were 5,778 +/- 2,257 micrograms/ml and 6,268 +/- 3,329 micrograms/ml 0-2 hours after administration, respectively, and average levels at 4-6 hours were 701 +/- 765 micrograms/ml and 1,588 +/- 1,324 micrograms/ml, respectively. Average excretion, rates into the urine were 72.8 +/- 11.0 and 73.9 +/- 11.1%, respectively. In case of 1 hour drips infusion of 25 mg/kg and 50 mg/kg, average concentrations in the urine 0-2 hours after administration were 3,570 +/- 1,540 micrograms/ml and 11,800 micrograms/ml, respectively, and averages for 4-6 hours were 211 +/- 124 micrograms/ml and 1,300 micrograms/ml. Average rates of excretion into the urine for the first group was 57.9 +/- 16.3% and the second group was 78.4%. Clear dose response was observed in changes of drug concentration levels in the urine with 25 mg/kg and 50 mg/kg doses through either administration method, and in terms of excretion into the urine, no noticeable differences were observed between the different amounts administered or different administration methods.(ABSTRACT TRUNCATED AT 400 WORDS)

摘要

将磷霉素钠(FOM-Na,复美欣)以25mg/kg或50mg/kg的剂量通过静脉注射或1小时静脉滴注的方式给予15名3至15岁的儿童,检测血清浓度和尿排泄情况,并采用一室模型进行药代动力学分析。1. 以25mg/kg和50mg/kg注射后30分钟,血清平均浓度分别为55.3±6.3微克/毫升和118.8±31.1微克/千克,半衰期分别为1.04±0.15小时和0.98±0.17小时。注射后6小时,浓度分别为2.7±1.6微克/千克和6.2±5.5微克/千克。以25mg/kg和50mg/kg进行1小时静脉滴注时,血清平均浓度分别为34.2±14.9微克/毫升和89.7±6.7微克/毫升,半衰期分别为0.87±0.24小时和0.69±0.10小时。给药后6小时,浓度分别为2.7±1.8微克/毫升和6.7±0.8微克/毫升。两种给药方法中,给予25mg/kg和50mg/kg药物的受试者血液中的浓度水平均有明显的剂量反应。2. 以25mg/kg和50mg/kg注射后,给药后0至2小时尿平均水平分别为5778±2257微克/毫升和6268±3329微克/毫升,4至6小时平均水平分别为701±765微克/毫升和1588±1324微克/毫升。尿平均排泄率分别为72.8±11.0%和73.9±11.1%。以25mg/kg和50mg/kg进行1小时滴注时,给药后0至2小时尿平均浓度分别为3570±1540微克/毫升和11800微克/毫升,4至6小时平均值分别为211±124微克/毫升和1300微克/毫升。第一组尿平均排泄率为57.9±16.3%,第二组为78.4%。两种给药方法中,25mg/kg和50mg/kg剂量的药物在尿中浓度水平变化均呈现明显的剂量反应,且在尿排泄方面,不同给药量和不同给药方法之间未观察到明显差异。(摘要截选至400字)

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