Adam D, Timmler R
Arzneimittelforschung. 1982;32(4):416-9.
Serum concentrations and urinary recovery of ceftizoxime were investigated in 18 healthy volunteers. The substance was given as a bolus (2 min) i.v. injection. In volunteers the injection was preceded by orally administered probenecid, 500 mg, 7 and 1 h before (Group II); the remaining 12 volunteers received medication. 5 min after the injection, the serum concentration in Group I was 107 +/- 22 micrograms/ml and in II 93 +/- 18 micrograms/ml in the mean; 30 min after the injection in I 45 +/- 8 micrograms/ml and 44 +/- 10 micrograms/ml in II. The further of the serum concentration was slower in II than in I: serum concentration 6 h after the injection was 2.6 +/- 0.9 micrograms/ml in I and 4.4 +/- 2 micrograms/ml in II. During the first 8-h period 81% of the administered cephalosporin was recovered in the urine of I and 58% in the urine of II. t/2 beta was calculated for I with 1.76 h and 2.13 h for II. The distribution volume was equal, so that the differences in serum concentrations could be explained by the reduced renal clearance: from 2.1 to 1.4 ml/s. Because the comparison was done with two independent groups and furthermore only 6 volunteers participated in the probenecid group, only the difference in the urine in the first 2 h was statistically significant.
在18名健康志愿者中研究了头孢唑肟的血清浓度和尿回收率。该药物通过静脉推注(2分钟)给药。在志愿者中,在注射前7小时和1小时口服丙磺舒500毫克(第二组);其余12名志愿者接受药物治疗。注射后5分钟,第一组血清浓度平均为107±22微克/毫升,第二组为93±18微克/毫升;注射后30分钟,第一组为45±8微克/毫升,第二组为44±10微克/毫升。第二组血清浓度下降比第一组慢:注射后6小时血清浓度第一组为2.6±0.9微克/毫升,第二组为4.4±2微克/毫升。在最初8小时内,第一组尿液中回收了81%的头孢菌素,第二组尿液中回收了58%。第一组计算的t/2β为1.76小时,第二组为2.13小时。分布容积相等,因此血清浓度差异可由肾清除率降低来解释:从2.1降至1.4毫升/秒。由于是在两个独立组之间进行比较,而且丙磺舒组只有6名志愿者参与,因此只有前2小时尿液中的差异具有统计学意义。