Pabst J, Leopold G, Ungethüm W, Dingeldein E
Arzneimittelforschung. 1979;29(2a):437-43.
In two consecutive cross-over studies, each involving 10 healthy volunteers, the pharmacokinetics of (6R,7R)-7-(2-[3,5-dichloro-4-oxo-1(4H)-pyridyl]-acetamindo)-3-([(5-methyl-1,3,4-thiadiazol-2-yl)-thio]methyl)-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid (cefazedone, Refosporen) in comparison with cefazolin were investigated after single i.v. and i.m. administration. The doses were: i.v. cefazedone 500 mg and 1000 mg; cefazolin 1000 mg; i.m. cefazedone 500 mg, cefazolin 500 mg. The pharmacokinetic parameters were analysed by applying an open two-compartment model. The pharmacokinetics of cefazedone are nearly identical with those of cefazolin. In particular, it must be noted that cefazedone has a relatively long serum elimination half-life (1.64 +/- 0.23 h after i.v. and 1.85 +/- 0.51 h after i.m. administration) and that cefazedone exhibits, in comparison with cefazolin, a more favourable concentration ratio of central vs. peripheral (= tissue) compartment (1:2).
在两项连续的交叉研究中，每项研究涉及10名健康志愿者，在单次静脉注射和肌肉注射后，对(6R,7R)-7-(2-[3,5-二氯-4-氧代-1(4H)-吡啶基]-乙酰氨基)-3-([(5-甲基-1,3,4-噻二唑-2-基)-硫代]甲基)-8-氧代-5-硫杂-1-氮杂双环[4,2,0]辛-2-烯-2-羧酸（头孢地嗪，瑞呋新）与头孢唑林的药代动力学进行了研究。剂量分别为：静脉注射头孢地嗪500毫克和1000毫克；头孢唑林1000毫克；肌肉注射头孢地嗪500毫克，头孢唑林500毫克。应用开放二室模型分析药代动力学参数。头孢地嗪的药代动力学与头孢唑林几乎相同。特别需要注意的是，头孢地嗪具有相对较长的血清消除半衰期（静脉注射后为1.64±0.23小时，肌肉注射后为1.85±0.51小时），并且与头孢唑林相比，头孢地嗪在中央室与外周（=组织）室的浓度比方面表现更优（1:2）。
