目的：合成肝靶向药联糖米托蒽醌（ＮＧＡＤＨＡＱ）的趋肝性研究。方法：以合成配体半乳糖基拟糖白蛋白（ｎｅｏｇｌｙｃｏａｌｂｕｍｉｎ，ＮＧＡ）为载体，与抗癌药物米托蒽醌（ｍｉｔｏｘａｎｔｒｏｎｅ，ＤＨＡＱ）偶联得肝靶向抗癌药物ＮＧＡＤＨＡＱ。采用紫外光谱和ＨＰＬＣ确证其偶联的形式及在血液中的稳定性。用９９ｍＴｃ标记后进行家兔放射性显像及小鼠体内的分布实验。结果：ＮＧＡＤＨＡＱ为化学偶联物且在血中很稳定，家兔及小鼠肝中药物的量均在５ｍｉｎ时达最大，分别占全身放射量的６５．１％和６５．４％±４．３％（ｎ＝３）。结论：说明ＮＧＡＤＨＡＱ具肝靶向分布性。 OBJECTIVE: To synthesize liver-targeting chemotherapeutic drugs, mitoxantrone (NGADHAQ). Methods: NGADHAQ, a liver-targeted anticancer drug, was conjugated with the anticancer drug mitoxantrone (DHAQ) using a synthetic ligand, galactosyl bromide (NGA) as a carrier. The coupled forms and their stability in the blood were confirmed by UV spectroscopy and HPLC. 99mTc labeled rabbits after radioactive imaging and distribution in vivo experiments in mice. Results: NGADHAQ was a chemical conjugate and was stable in blood. The amounts of drugs in rabbit and mouse liver reached the maximum at 5 min, accounting for 65.1% and 65.4% of the total body radiation 4.3% (n = 3). Conclusion: NGA DHAQ liver targeting distribution.