Dettlaff Katarzyna, Ogrodowczyk Magdalena, Kycler Witold, Dołhań Agnieszka, Cwiertnia Barbara, Garbacki Piotr, Jelińska Anna
Department of Pharmaceutical Chemistry, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznań, Poland.
Department of Oncological Surgery II, Greater Poland Cancer Centre, Garbary 15, 61-866 Poznań, Poland.
Biomed Res Int. 2014;2014:571376. doi: 10.1155/2014/571376. Epub 2014 Aug 4.
Eplerenone was subjected to the influence of ionizing radiation in the form of a high-energy electron beam (25-400 kGy), high temperature (90°C RH 0% and 60°C RH 76.4%), and light (6 mln lux h). An HPLC method was used to determine the content of eplerenone and to establish the impurity profile of all samples. As eplerenone was found to be a compound of great resistance to the above stress factors with the exception of high doses of ionizing radiation (≥ 200 kGy) when its degradation was above 1%, it is possible to sterilize eplerenone by radiation method with the standard dose of 25 kGy. Based on the analysis of impurities and degradation products, the mechanism of radiodegradation was demonstrated to differ from the mechanisms of photo- and thermodegradation. The observation that the DSC curves for the nondegraded and degraded samples of eplerenone were significantly different only under exposure to the electron beam confirmed the applicability of DSC for studies of radiolytic degradation of eplerenone.
依普利酮受到高能电子束（25 - 400千戈瑞）形式的电离辐射、高温（90°C，相对湿度0%和60°C，相对湿度76.4%）以及光照（600万勒克斯·小时）的影响。采用高效液相色谱法测定依普利酮的含量并确定所有样品的杂质谱。由于发现依普利酮是一种对上述应激因素具有很强耐受性的化合物，但高剂量电离辐射（≥200千戈瑞）除外，此时其降解率超过1%，所以可以采用25千戈瑞的标准剂量通过辐射法对依普利酮进行灭菌。基于对杂质和降解产物的分析，证明辐射降解机制与光降解和热降解机制不同。依普利酮未降解和降解样品的差示扫描量热曲线仅在电子束照射下有显著差异，这一观察结果证实了差示扫描量热法适用于依普利酮辐射降解的研究。
