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小儿口服抗生素的药代动力学研究。III. 头孢丙烯在小儿中的药代动力学研究

[Pharmacokinetic study on oral antibiotics in pediatrics. III. A pharmacokinetic study on cefprozil in pediatrics].

作者信息

Nakamura H, Iwai N

机构信息

Department of Pediatrics, Meitetsu Hospital.

出版信息

Jpn J Antibiot. 1992 Nov;45(11):1489-504.

PMID:1494232
Abstract

The absorption and excretion were studied in the field of pediatrics, and pharmacokinetic analyses were performed. 1. Influence of food: Cefprozil (CFPZ, BMY-28100) was given to 6 school children in a before and after meal cross over design. With before meal administration, Tmax was 1.11 +/- 0.08 hours, Cmax was 5.08 +/- 0.27 micrograms/ml, T 1/2 was 0.77 +/- 0.09 hour, and urinary recovery rate (0-8 hours) was 55.2 +/- 4.7%. With after meal administration, these values were 1.31 +/- 0.04 hours, 3.98 +/- 0.38 micrograms/ml, 0.72 +/- 0.03 hour and 46.3 +/- 9.0%, respectively. A shorter Tmax value was, obtained higher Cmax and more or less higher urinary recovery rate when the drug was administered before meal, hence the food was considered to influence the absorption of the drug. 2. Dose effect: CFPZ was given on empty stomach to 6 school children in doses of 7.5 mg/kg and 15.0 mg/kg in the cross over design. With the lower dose Cmax was 6.19 +/- 0.36 micrograms/ml and AUC was 14.90 +/- 1.02 micrograms.hr/ml, and with the higher dose they were 12.38 +/- 1.29 micrograms/ml and 28.56 +/- 1.79 micrograms.hr/ml. Dose effects appeared to exist for CFPZ. A higher urinary recovery rate was obtained at the dosage of 7.5 mg/kg (82.1 +/- 6.4%) compared to the dosage of 15.0 mg/kg (51.1 +/- 7.1%). 3. Influence of age: CFPZ was given on empty stomach to 17 school children, 19 younger children and 5 infants. Tmax were 1.07 +/- 0.09, 1.06 +/- 0.07, and 1.40 +/- 0.09 hours, respectively for the 3 groups, hence significantly longer Tmax was observed in infants. Cmax were higher in older children and they were 5.62 +/- 0.38, 4.72 +/- 0.53 and 4.05 +/- 0.33 micrograms/ml, in the 3 age groups, respectively. T 1/2 were 0.73 +/- 0.04, 0.78 +/- 0.09 and 0.98 +/- 0.12 hour, respectively, it was longer in infants. The AUCs were not different among the 3 groups, but different urinary recovery rates were obtained with higher recovery in school children, with values of 64.1 +/- 4.3, 44.3 +/- 3.8 and 51.6 +/- 3.3%, respectively.

摘要

在儿科学领域研究了头孢丙烯(CFPZ,BMY - 28100)的吸收和排泄情况,并进行了药代动力学分析。1. 食物的影响:采用饭前饭后交叉设计,给6名学龄儿童服用头孢丙烯。饭前给药时,达峰时间(Tmax)为1.11±0.08小时,血药峰浓度(Cmax)为5.08±0.27微克/毫升,半衰期(T 1/2)为0.77±0.09小时,尿回收率(0 - 8小时)为55.2±4.7%。饭后给药时,这些值分别为1.31±0.04小时、3.98±0.38微克/毫升、0.72±0.03小时和46.3±9.0%。饭前给药时Tmax值较短,Cmax较高,尿回收率或多或少也较高,因此认为食物会影响药物的吸收。2. 剂量效应:采用交叉设计,空腹给6名学龄儿童分别服用7.5毫克/千克和15.0毫克/千克剂量的头孢丙烯。较低剂量时,Cmax为6.19±0.36微克/毫升,曲线下面积(AUC)为14.90±1.02微克·小时/毫升;较高剂量时,它们分别为12.38±1.29微克/毫升和28.56±1.79微克·小时/毫升。头孢丙烯似乎存在剂量效应。7.5毫克/千克剂量时的尿回收率(82.1±6.4%)高于15.0毫克/千克剂量时的尿回收率(51.1±7.1%)。3. 年龄的影响:空腹给17名学龄儿童、19名低龄儿童和5名婴儿服用头孢丙烯。三组的Tmax分别为1.07±0.09、1.06±0.07和1.40±0.09小时,因此婴儿的Tmax明显更长。大龄儿童的Cmax较高,三个年龄组的Cmax分别为5.62±0.38、4.72±0.53和4.05±0.33微克/毫升。T 1/2分别为0.73±0.04、0.78±0.09和0.98±0.12小时,婴儿的T 1/2更长。三组的AUC没有差异,但尿回收率不同,学龄儿童的回收率较高,分别为64.1±4.3%、44.3±3.8%和51.6±3.3%。

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