Sugiyama H, Hatano T, Takayanagi K, Aoyama H, Kikuchi Y
Jpn J Antibiot. 1986 May;39(5):1297-301.
Transfer of cefotetan (CTT) into exudates from excoriated skin wounds was studied in 9 adult patients. Each subject was given an intravenous bolus injection of 50 mg/kg of body weight. Concentrations of CTT in serum and in exudate fluid were determined by bioassay using Escherichia coli NIHJ as the test organism. The mean (+/- S.D.) CTT concentration in serum reached 274.3 +/- 78.3 micrograms/ml at 30 minutes after the injection and decreased to 30.0 +/- 12.0 micrograms/ml at 8 hours after the injection. The peak value of CTT in exudate fluid was 143.1 +/- 22.3 micrograms/ml at 1 hour. Eight hours after the injection, the mean concentration in the exudate was 25.7 +/- 21.1 micrograms/ml. The data obtained were analysed pharmacokinetically: CTT concentrations in serum were analysed by two-compartment model, and those in exudate fluid from excoriated skin wounds were analysed by the model in which skin was considered as a small part of the peripheral compartment. Thus T1/2(beta) of CTT levels in serum was calculated as 2.38 hours, AUC0----infinity was 1,000.2 micrograms X hr/ml and Vd was 164.5 ml/kg. Tmax and Cmax of CTT levels in exudates were calculated as 1.05 hours and 131.2 micrograms/ml, respectively.
在9名成年患者中研究了头孢替坦（CTT）向擦伤皮肤伤口渗出液中的转移情况。每位受试者静脉推注50mg/kg体重的药物。使用大肠杆菌NIHJ作为测试生物体，通过生物测定法测定血清和渗出液中CTT的浓度。注射后30分钟时血清中CTT的平均（±标准差）浓度达到274.3±78.3μg/ml，注射后8小时降至30.0±12.0μg/ml。渗出液中CTT的峰值在1小时时为143.1±22.3μg/ml。注射后8小时，渗出液中的平均浓度为25.7±21.1μg/ml。对获得的数据进行药代动力学分析：血清中CTT浓度采用二室模型分析，擦伤皮肤伤口渗出液中的浓度采用将皮肤视为外周室一小部分的模型进行分析。因此，血清中CTT水平的T1/2（β）计算为2.38小时，AUC0----无穷大为1,000.2μg×hr/ml，Vd为164.5ml/kg。渗出液中CTT水平的Tmax和Cmax分别计算为1.05小时和131.2μg/ml。
