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目的研究合成表阿霉素与Vk3的偶联物(EVk)的组织分布情况。方法经同位素示踪法和HPLC法观察EVk在动物组织中的分布。结果同位素示踪法中,肝脏有一过性浓集现像,但未见特异性高药物浓度分布。结合HPLC检测到保留时间1.9、5.1 min处有两个较高的未知吸收峰,推测未知吸收峰应为EVk的肝代谢产物,肝组织较其他组织有较高的代谢物浓度。结论 EVk原药在肝脏及其他组织中的分布浓度低,但其代谢产物浓度较高,可能通过快速肝代谢进而通过代谢物在肝脏发挥靶向治疗作用。
Objective To study the tissue distribution of synthetic conjugate of epirubicin and Vk3 (EVk). Methods The distribution of EVk in animal tissues was observed by isotope tracer method and HPLC method. Results In the isotope tracer method, the liver had a transient concentration phenomenon, but no specific high drug concentration distribution was found. The retention time of 1.9 was detected by HPLC. There were two higher unknown peaks at 5 min and 5 min. The unknown peak was supposed to be the hepatic metabolites of EVk. The liver tissue had higher metabolite concentration than other tissues. Conclusion The original drug of EVk is low in the liver and other tissues, but its metabolite concentration is high. It may play a role in the liver by metabolizing rapidly through liver metabolism.