Paradelis A G, Stathopoulos G, Trianthaphyllidis C, Logaras G
Arzneimittelforschung. 1977;27(11):2167-70.
This paper deals with data on the pharmacokinetics of cephazolin, cephalothin, cephapirin, cephaloridine and cephradine after i.m. injection of a single dose of 0.5 g in healthy male volunteers. Peak serum concentrations occurred 45 min after the administration and were 31.52 microgram/ml for cephazolin, 17.32 microgram/ml for cephaloridine, 13.98 microgram/ml for cephapirin, 9.51 microgram/ml for cephradine and 8.60 microgram/ml for cephalothin. The average half-lives were found to be 2.07, 1.80, 0.98, 1.24 and 0.97 h, respectively. The percentage of protein binding was found to be 82 for cephazolin, 59 for cephalothin, 51 for cephapirin, 31 for cephaloridine and only 10 for cephradine, half an hour after drug administration. The total urine recovery of the above cephalosporins, within 24 h, was 91.9% for cephradine, 81.9% for cephaloridine, 73.3% for cephazolin, 69.5% for cephapirin and 51.2% for cephalothin.
本文研究了健康男性志愿者肌肉注射单剂量0.5g头孢唑林、头孢噻吩、头孢匹林、头孢噻啶和头孢拉定后的药代动力学数据。给药后45分钟出现血清峰值浓度，头孢唑林为31.52微克/毫升，头孢噻啶为17.32微克/毫升，头孢匹林为13.98微克/毫升，头孢拉定为9.51微克/毫升，头孢噻吩为8.60微克/毫升。发现平均半衰期分别为2.07、1.80、0.98、1.24和0.97小时。给药半小时后，发现蛋白结合率头孢唑林为82%，头孢噻吩为59%，头孢匹林为51%，头孢噻啶为31%，头孢拉定仅为10%。上述头孢菌素在24小时内的总尿回收率，头孢拉定为91.9%，头孢噻啶为81.9%，头孢唑林为73.3%，头孢匹林为69.5%，头孢噻吩为51.2%。
