Kunst M W, Mattie H
Infection. 1978;6(4):166-70. doi: 10.1007/BF01641906.
The relationship between serum concentrations and tissue levels of various doses of cefazolin and cephradine was determined in experimentally infected mice. An infection was induced by injection of 5 X 10(6) Escherichia coli into the right hind leg, antibiotics were administered 1 h later. At 15-minute intervals mice were killed by exsanguination after a blood sample was taken, and the infected thigh was taken out and homogenized. The total amount of antibiotic per gram thigh muscle tissue was calculated on the basis of the concentration in the supernatant of the homogenate. From the parallel course between blood concentrations and total tissue contents it may be concluded that the thigh was easily accessible for both cephalosporins. The ratio between the total tissue content and the free serum concentrations was the same for both antibiotics despite the difference in protein binding between cefazolin and cephradine in mouse serum. This implies that the discrepancy between the relative antibacterial activity of the cephalosporins in vitro and in vivo found in earlier experiments cannot be explained by differences in accessibility of the tissue.
在实验感染的小鼠中测定了不同剂量头孢唑林和头孢拉定的血清浓度与组织水平之间的关系。通过向右侧后腿注射5×10⁶ 大肠杆菌诱导感染，1小时后给予抗生素。每隔15分钟采集血样后放血处死小鼠，取出感染的大腿并匀浆。根据匀浆上清液中的浓度计算每克大腿肌肉组织中抗生素的总量。从血药浓度和组织总含量的平行变化过程可以得出结论，两种头孢菌素都很容易进入大腿。尽管头孢唑林和头孢拉定在小鼠血清中的蛋白结合率不同，但两种抗生素的组织总含量与游离血清浓度之比相同。这意味着早期实验中发现的头孢菌素在体外和体内相对抗菌活性的差异不能用组织可达性的差异来解释。
