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头孢他美静脉注射及头孢他美酯口服在儿童体内的药代动力学

Pharmacokinetics of intravenous cefetamet and oral cefetamet pivoxil in children.

作者信息

Hayton W L, Walstad R A, Thurmann-Nielsen E, Kufaas T, Kneer J, Ambros R J, Rugstad H E, Monn E, Bodd E, Stoeckel K

机构信息

College of Pharmacy, Ohio State University, Columbus 43210-1291, USA.

出版信息

Antimicrob Agents Chemother. 1991 Apr;35(4):720-5. doi: 10.1128/AAC.35.4.720.

Abstract

The pharmacokinetics of cefetamet were determined after intravenous (i.v.) administration of cefetamet and oral administration of cefetamet pivoxil syrup to patients between the ages of 3 and 12 years. The patients were hospitalized for reconstructive urological surgery; to prevent infection, prophylactic i.v. cefetamet was administered on the day of surgery and oral cefetamet pivoxil was administered 2 days later. After i.v. administration, the mean (+/- standard deviation) half-life of cefetamet was 1.97 +/- 0.60 h (n = 18), which was different from the 2.46 +/- 0.33 h reported for nine adults (22 to 68 years old) in a previous study. The average values for the mean residence times were 2.35 +/- 0.94 and 2.83 +/- 0.34 h and the average values for the fraction of the dose eliminated unchanged in the urine were 79.9% +/- 8.99% and 80% +/- 11% in children and adults, respectively. Plots of mean systemic clearance and steady-state volume of distribution versus body weight for the children and comparative adults were linear on log-log coordinates, and the slopes of the plots were 0.661 and 0.880, respectively. These slope values suggested that mean systemic clearance values per unit of body surface area were similar in children and adults and that maintenance doses for children should be the adult maintenance dose multiplied by the child's surface area divided by 1.73 m2. The mean (+/- standard deviation) oral bioavailabilities of cefetamet pivoxil were 49.3% +/- 15.7% in 3- to 7-year-old children who received a 500-mg dose and 37.9% +/- 10.0% in 8- to 12-year-old children who received a 1,000-mg dose. These values were not different from that observed in the adult group after two 500-mg tablets. Likewise, the peak concentration of cefetamet in plasma and its time of occurrence in children were in line with the values which have been observed for adults.

摘要

在3至12岁患者静脉注射头孢他美和口服头孢他美酯糖浆后,测定了头孢他美的药代动力学。这些患者因泌尿外科重建手术住院;为预防感染,在手术当天静脉注射预防性头孢他美,并在2天后口服头孢他美酯。静脉注射后,头孢他美的平均(±标准差)半衰期为1.97±0.60小时(n = 18),这与先前一项研究中报告的9名成年人(22至68岁)的2.46±0.33小时不同。儿童和成人的平均驻留时间平均值分别为2.35±0.94和2.83±0.34小时,尿中未改变消除剂量分数的平均值分别为79.9%±8.99%和80%±11%。儿童和对照成年人的平均全身清除率和稳态分布容积与体重的对数-对数坐标图呈线性关系,图的斜率分别为0.661和0.880。这些斜率值表明,儿童和成人每单位体表面积的平均全身清除率值相似,儿童的维持剂量应为成人维持剂量乘以儿童体表面积除以1.73 m²。接受500 mg剂量的3至7岁儿童中,头孢他美酯的平均(±标准差)口服生物利用度为49.3%±15.7%,接受1000 mg剂量的8至12岁儿童中为37.9%±10.0%。这些值与服用两片500 mg片剂后的成人组中观察到的值没有差异。同样,儿童血浆中头孢他美的峰值浓度及其出现时间与成人中观察到的值一致。

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Antimicrob Agents Chemother. 1989 Jun;33(6):957-9. doi: 10.1128/AAC.33.6.957.
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