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Ro23-9424是Roche公司新近研制的一个具有双重作用的新型头孢菌素(见图)。它是喹诺酮型衍生物氟罗沙星(Fleroxacin)的羧酸基与头孢噻肟(Cefotaxime)的代谢产物去乙酰头孢噻肟C_3位形成酯键而成。本文研究和探讨了它的体内抗菌活性及其药动学,以阐明Ro23-9424是以整体起作用还是以其酯键断裂产物起作用的。一、微生物试验 1.体外抗菌活性对1000株菌株测试Ro23-9424的抗菌活性,表明它与氟罗沙星非常接近。Ro23-9424以≤16μg/ml的浓度(MIC_(50)在≤0.006μg/ml～1μg/ml之间)即能抑制全部肠杆菌属细菌。葡萄球菌、链球菌、卡他球
Ro23-9424 is a new double-acting cephalosporin recently developed by Roche (see photo). It is the quinolone derivative of fleroxacin (Fleroxacin) carboxylic acid group with cefotaxime (Cefotaxime) metabolites cefotaxime C_3 form ester bond formed. This article studies and explores its in vivo antibacterial activity and its pharmacokinetics to elucidate whether Ro23-9424 functions either as a whole or as a product of its ester bond cleavage. First, the microbial test 1. In vitro antibacterial activity of 1000 strains tested Ro23-9424 antibacterial activity, indicating that it is very close to fleroxacin. Ro23-9424 inhibited all Enterobacter bacteria at a concentration of ≤16μg / ml (MIC_ (50) ≤0.006μg / ml ~ 1μg / ml). Staphylococcus, Streptococcus, Carte ball