PDF(Pubmed)
Abstract：
Dezocine, which is well-known as an analgesic, had about 45% share of the Chinese opioid analgesic market. Since drug products containing impurities could bring serious health consequences, it was important to control the generation of impurities and degradation products in the dezocine product. In this study, two kinds of photodegradation products (i.e., degradation product 1 and degradation product 2) in the dezocine injection were isolated using high-performance liquid chromatography. The possible structures of the photodegradation products were identified using both high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy. In addition, the possible generation mechanism showed that degradation product 1 was the oxidation product of dezocine, and degradation product 2 was the coupled dimer of dezocine. Finally, we found that the degradation rate of dezocine increased with the increase in light intensity. Moreover, the degradation of dezocine easily occurred under ultraviolet light in comparison with visible light. A deeper insight into the generation of the photodegradation products in the dezocine injection would directly contribute to the safety of drug therapy based on the dezocine injection by minimizing the degradant/impurity-related adverse effects of drug preparations.
摘要：
地佐辛,这是众所周知的镇痛药，在中国阿片类镇痛药市场占有约45%的份额。由于含有杂质的药品可能会带来严重的健康后果，控制地佐辛产品中杂质和降解产物的产生非常重要。在这项研究中,两种光降解产物(即，使用高效液相色谱法分离地佐辛注射液中的降解产物1和降解产物2）。使用高分辨率质谱和核磁共振光谱鉴定了光降解产物的可能结构。此外,可能的产生机理表明，降解产物1是地佐辛的氧化产物，降解产物2为地佐辛的偶联二聚体。最后,我们发现地佐辛的降解速率随光照强度的增加而增加。此外，与可见光相比，地佐辛在紫外光下容易降解。对地佐辛注射液中光降解产物的产生的更深入的了解将通过使药物制剂的降解物/杂质相关的副作用最小化而直接有助于基于地佐辛注射液的药物治疗的安全性。
