Intoccia A P, Walkenstein S S, Joseph G, Wittendorf R, Girman C, Walz D T, Actor P, Weisbach J
J Antibiot (Tokyo). 1978 Nov;31(11):1188-94. doi: 10.7164/antibiotics.31.1188.
SK&F 75073 is a new cephalosporin with broad spectrum antibacterial activity. SK&F 75073-14C and cefazolin-35S were administered separately to groups of rats as a single intramuscular dose of 20 mg/kg. Tissues with highest drug levels 15 minutes following dose were as follows: (SK&F 75073/cefazolin levels), kidney - 86/70 microgram/g, liver - 33/22 microgram/g, lung - 29/17 microgram/g, heart - 23/10 microgram/g, adrenal - 13/7 microgram/g. Plasma levels at peak were 134 microgram SK&F 75073/ml (half-life, 1.9 hours) and 72 microgram cefazolin/ml (half-life, 0.75 hours). Dose excreted in 24 hours was: SK&F 75073, urine 66% and feces 27%; cefazolin, urine 96% and feces 2%. Both antibiotics were also administered, at 20 mg/kg, to rats with the carrageenan-induced inflammatory pouches. Exudate from these pouches contained from 2 to 10 times more SK&F 75073 than cefazolin. Radioassay and bioassay of these substances in the exudate gave similar results. Serum protein binding ranged from 96 approximately 98% for SK&F 75073 and 34 approximately 69% for cefazolin. Data indicated that highly protein bound SK&F 75073 enters tissues and tissue fluid to a greater extent than the lesser bound but therapeutically proven antibiotic agent cefazolin.
SK&F 75073是一种具有广谱抗菌活性的新型头孢菌素。将SK&F 75073-14C和头孢唑林-35S分别以20mg/kg的单一肌肉注射剂量给予几组大鼠。给药后15分钟药物水平最高的组织如下：（SK&F 75073/头孢唑林水平），肾脏 - 86/70微克/克，肝脏 - 33/22微克/克，肺 - 29/17微克/克，心脏 - 23/10微克/克，肾上腺 - 13/7微克/克。峰值时的血浆水平为134微克SK&F 75073/毫升（半衰期，1.9小时）和72微克头孢唑林/毫升（半衰期，0.75小时）。24小时内排出的剂量为：SK&F 75073，尿液66%，粪便27%；头孢唑林，尿液96%，粪便2%。两种抗生素也都以20mg/kg的剂量给予角叉菜胶诱导的炎症袋大鼠。这些袋子的渗出液中SK&F 75073的含量比头孢唑林多2至10倍。对渗出液中这些物质的放射测定和生物测定给出了相似的结果。血清蛋白结合率对于SK&F 75073为96%至98%，对于头孢唑林为34%至69%。数据表明，与结合程度较低但已被证明具有治疗作用的抗生素头孢唑林相比，与蛋白高度结合的SK&F 75073能更大程度地进入组织和组织液。
