Miyazaki T, Kaneko T, Yoshimura T, Crucq A S, Tilquin B
Department of Applied Chemistry, Faculty of Engineering, Nagoya University, Japan.
J Pharm Sci. 1994 Jan;83(1):68-71. doi: 10.1002/jps.2600830116.
Fundamental information on radiosterilization of ceftazidime was obtained by electron spin resonance (ESR) measurement of free radicals produced in gamma-ray-irradiated ceftazidime at 4.2-295 K. Three types of free radicals are produced by gamma-irradiation. The first one shows septet lines in an ESR spectrum and decays at 230 K: it is assigned as a .C(CH3)2COOH radical. The second one shows triplet lines and decays at 293 K: it is assigned as iminoxyl radicals (> C = N-O.). The third one shows a broad singlet line and survives even at 295 K. The plausible assignment of this spectrum is discussed. It is concluded that an O-C bond of the gamma-irradiated ceftazidime is ruptured, producing the iminoxyl radicals and .C(CH3)2COOH radicals. The yields of free radicals increase linearly with the increasing dose of gamma-irradiation up to 10 kGy at 295 K as well as 77 K. Half of the radicals that show a broad singlet line survive at 295 K upon storage of the irradiated ceftazidime for 159 days. It is concluded that the ESR measurement of free radicals gives a good method for discrimination of irradiated antibiotics from non-irradiated ones and an estimation of an irradiation dose.
通过在4.2 - 295K温度下对γ射线辐照的头孢他啶产生的自由基进行电子自旋共振(ESR)测量,获得了头孢他啶辐射灭菌的基本信息。γ射线辐照产生三种类型的自由基。第一种在ESR谱中显示七重线,并在230K时衰减:它被确定为.C(CH3)2COOH自由基。第二种显示三重线,并在293K时衰减:它被确定为亚胺氧基自由基(> C = N - O.)。第三种显示宽单重线,甚至在295K时仍存在。讨论了该谱的合理归属。得出的结论是,γ射线辐照的头孢他啶的O - C键断裂,产生亚胺氧基自由基和.C(CH3)2COOH自由基。在295K以及77K时,自由基产率随γ射线辐照剂量增加至10kGy呈线性增加。辐照后的头孢他啶储存159天后,在295K时,显示宽单重线的自由基中有一半存活下来。得出的结论是,自由基的ESR测量为区分辐照抗生素和未辐照抗生素以及估计辐照剂量提供了一种很好的方法。