Ogrodowczyk Magdalena, Dettlaff Katarzyna, Kachlicki Piotr, Marciniec Barbara
Poznan University of Medical Sciences, Department of Pharmaceutical Chemistry, Grunwaldzka 6, 60-780 Poznań, Poland.
J AOAC Int. 2015 Jan-Feb;98(1):46-50. doi: 10.5740/jaoacint.14-096.
Two therapeutically active compounds from the group of β-blockers, acebutolol (AC) and alprenolol (AL), in solid form were subjected to ionizing radiation emitted by a beam of high energy electrons from an accelerator with a standard sterilization dose of 25 kGy and in higher doses of 50-400 kGy. The effects of irradiation were detected by chromatographic methods (TLC, HPLC) and a hyphenated method (HPLC/MS/MS). No significant changes in the physicochemical properties of both compounds studied irradiated with 25 kGy were noted, but upon irradiation with the highest dose (400 kGy) the loss of AC and AL content determined by HPLC was 2.79 and 9.12%, respectively. The product of AC decomposition and the two products of AL decomposition were separated and identified by HPLC/MS/MS. It has been established that radiodegradation of AC and AL takes place by oxidation, leading to formation of the products of radiolysis, most probably alcohol derivatives of the β-blockers studied. The additional product that appears on radiodegradation of AL is probably formed as a result of two simultaneous reactions: oxidation and CH2 group elimination.
两种β受体阻滞剂类的治疗活性化合物醋丁洛尔（AC）和阿普洛尔（AL）的固体形式，接受了来自加速器的高能电子束发射的电离辐射，标准灭菌剂量为25 kGy，以及更高剂量的50 - 400 kGy。通过色谱方法（薄层色谱法、高效液相色谱法）和联用方法（高效液相色谱/质谱/质谱法）检测辐照效果。用25 kGy辐照所研究的两种化合物，未观察到其物理化学性质有显著变化，但用最高剂量（400 kGy）辐照时，通过高效液相色谱法测定的AC和AL含量损失分别为2.79%和9.12%。AC分解产物和AL的两种分解产物通过高效液相色谱/质谱/质谱法进行了分离和鉴定。已经确定AC和AL的辐射降解是通过氧化发生的，导致形成辐射分解产物，很可能是所研究的β受体阻滞剂的醇衍生物。AL辐射降解时出现的额外产物可能是由两个同时发生的反应形成的：氧化和CH₂基团消除。
