阿魏酸在辐照处理的微晶纤维素中的稳定性及降解产物分析  

Stability and Degradation Products of Ferulic Acid in Irradiated Microcrystalline Cellulose

作　　者：寿纪纲 霍志鹏 王玉 乔敏莎[1] 刘吉华 何毅[1] Shou Jigang;Huo Zhipeng;Wang Yu;Qiao Minsha;Liu Jihua;He Yi(Research Institute of Tasly Pharmaceutical Group Co.,Ltd.,State Key Laboratory of Critical Technology of Innovative Chinese Medicine,Tianjin 300410,China;School of Traditional Chinese Pharmacy,China Pharmaceutical University,Nanjing,Jiangsu 211198,China;School of Chinese Materia Medica,Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;School of Pharmaceutical Science and Technology,Tianjin University,Tianjin 300072,China)

机构地区：[1]天士力医药集团股份有限公司研究院,创新中药关键技术国家重点实验室,天津300410 [2]中国药科大学中药学院,江苏南京211198 [3]天津中医药大学中药学院,天津301617 [4]天津大学药物科学与技术学院,天津300072

出　　处：《化工与医药工程》2023年第1期44-50,共7页Chemical and Pharmaceutical Engineering

基　　金：国家“重大新药创制”科技重大专项(2017ZX09301005)。

摘　　要：辐照灭菌工艺可能使药物辅料降解从而间接影响活性成分的稳定性。考察了微晶纤维素经过60Co辐照后对阿魏酸稳定性的影响,通过超高效液相色谱法(UPLC)检测样品中阿魏酸的含量变化;通过超高效液相色谱-质谱联用技术(UPLC-Q-TOF-MS)对阿魏酸的降解产物进行分析。结果发现辐照处理后的微晶纤维素与阿魏酸混合后可使阿魏酸在一个月内持续降解并产生了一系列降解产物,分别为:3, 4-二羟基苯乙酮、咖啡酸、香草酸、二氢阿魏酸、香草醛、松柏醛。推测微晶纤维素在辐照降解的过程中产生了自由基,这些自由基通过不同的作用机制使阿魏酸产生降解,此研究结果可为有关药物灭菌工艺的选择以及辐照降解杂质的产生机制提供参考。Irradiation sterilization process may degrade pharmaceutical excipients and indirectly affect the stability of active ingredients.The effect of microcrystalline cellulose irradiated by 60Co on the stability of ferulic acid was investigated.The content of ferulic acid was detected by ultra high performance liquid chromatography(UPLC).The degradation products of ferulic acid were analyzed by ultra performance liquid chromatography-mass spectrometry(UPLC-Q-TOF-MS).The results showed that the mixture of irradiated microcrystalline cellulose and ferulic acid could degrade ferulic acid continuously within a month and produce a series of degradation products,including 3,4-dihydroxyacetophenone,caffeic acid,vanillin,dihydroferulic acid.It is speculated that free radicals were produced in the process of irradiation degradation of microcrystalline cellulose,and these free radicals degraded ferulic acid through different mechanisms of action.The results of this study can provide references for the selection of drug sterilization technology and the generation mechanism of impurity degradation by irradiation.

关 键 词：辐照 微晶纤维素 自由基 阿魏酸 降解产物 

分 类 号：R28[医药卫生—中药学]