摘要
本文报道头孢唑肟在9名健康志愿者单次和多次给药后的药代动力学研究。药物浓度以微生物法测定。 单次给药受试对象6人。按交叉设计每次肌注或静注头孢唑肟1g。肌注与静注后的药时数据分别符合一级动力学一室和二室开模型。静注后即刻浓度为159.32±14.24μg/ml,肌注后 1小时达峰浓度为38.87±5.57μg/ml。肌注和静注后血浆半衰期分别为1.72±0.15和1.73±0.06h,生物利用度为95.95±4.23％。肌注与静注后24小时尿药回收率分别为83.7％和93.6％。头孢唑肟的人血清蛋白结合率为23％。 多次给药受试对象3人,每12小时肌注头孢唑肟1g,连续6天。第1天与第6天平均峰浓度为31.36±6.43和30.98±9.91μg/ml。第2～5天首次给药后1小时平均血药浓度波动于36.64～38.60μg/ml,12小时平均血药浓度为1.02～1.1μg/ml。第1天与第 6天的消除速率常数及药物的肾清除率无显著统计学差异。本品间隔12小时多次重复给药无明显蓄积现象。
The pharmacokinetics of ceftizoxime (CZX) was studied in single and multi-pledose studies in nine healthy volunteers. The drug concentration was measured by the bioassay method.
In single-dose studies,each of the six volunteers was given 1g of CZX intramuscularly and intravenously by a crossover design . The pharmacokinetics after iv bolus injection conformed to a two-compartment open model, and those after im injection were fitted to the one-compartment open model. Meanpeak serum level after iv bolus injection was 159.32±14.24 μg/ml and was 38.87 ± 5.57μg/ml after im injection at 1 hr.Serum half-lives were 1.72 ± 0.15 hrs after im injection and were 1.73 ±0.06 hrs after iv injection, and the bioavailability was approximately complete. The majority of the drug was excreted in the urine(about 83.7~93.6%within 24 hr).Protein binding of CZX was 23%. In multiple-dose studies, CZX was administered to 3 volunteers intramuscularly in a dose of 1g 12-hourly for 6 days. Multiple im injection produced serum levels of 36.64~38.60 μg/ml at 1 hr.Mean serum levels at 12hr ranged from 1.02~1.14μg/ml.The elimination rate constants and T1/2 ke on day 1 and 6 showed no statistical differences, and no significant dif-fernces in the renal clearance of the drug on day 1 and day 6 were noted. No obvious
accumulation of the drug was noted in multiple-dose administration.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
1989年第6期425-432,共8页
Chinese Journal of Antibiotics
