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目的：研究肝靶向抗癌药物半乳糖基拟糖白蛋白米托蒽醌（ＮＧＡＤＨＡＱ）的小鼠体内分布，及对ＮＧＡＤＨＡＱ和米托蒽醌（ＤＨＡＱ）在小鼠体内的药代动力学进行比较。方法：利用放射性核索示踪法及ＨＰＬＣ进行测定。结果：体内分布结果表明ＮＧＡＤＨＡＱ具有良好的趋肝性，５ｍｉｎ时肝摄取率为６５％左右，ＨＰＬＣ实验结果表明ＮＧＡＤＨＡＱ在血中有较好的稳定性，不易解离出ＤＨＡＱ。ＮＧＡＤＨＡＱ和ＤＨＡＱ在肝中的达峰时间分别为０．２和１０ｍｉｎ，两者在血中消除均较快，ＮＧＡＤＨＡＱ的峰浓度是ＤＨＡＱ的１．９倍，不同时间点ＮＧＡＤＨＡＱ的肝药浓度／血药浓度均比ＤＨＡＱ的大。结论：ＮＧＡＤＨＡＱ浓集肝脏速度快，具肝靶向分布特征。
Objective: To study the in vivo distribution of the liver-targeted anticancer drug galactosyl-mimetic albumin-mitoxantrone (NGA-DHAQ) in mice and the effects of NGADHAQ and mitoxantrone (DHAQ) in mice. Pharmacokinetic comparisons. Methods: The radionuclide tracer method and HPLC were used for the determination. Results: The results of in vivo distribution showed that NGADHAQ had good hepatotropism. The liver uptake rate was about 65% at 5 min. HPLC results showed that NGADHAQ had good stability in blood and it was not easy to dissociate DHAQ. The peak time of NGADHAQ and DHAQ in the liver was 0.2 and 10 min, respectively, both of which were rapidly eliminated in blood. The peak concentration of NGADHAQ was 1.9 times that of DHAQ, and NGADHAQ at different time points. The liver drug concentration/blood concentration is greater than that of DHAQ. Conclusion: NGADHAQ condenses liver rapidly and has liver targeting characteristics.