去甲斑蝥酸钠脂质微球在大鼠体内的组织分布

目的比较去甲斑蝥酸钠脂质微球注射液与溶液型注射液在大鼠体内组织中的分布特征。方法大鼠股静脉注射去甲斑蝥酸钠脂质微球注射液,采用HPLC-MS法测定不同时间点大鼠组织脏器中的药物浓度。结果与去甲斑蝥素注射液相比,脂质微球注射液在肝脏组织中具有较高的浓度,肝脏相对分布率由16.3%增加至32%,AUC值为218.72 mg.L-1.h-1。而在心脏、肾脏、血液中的药物分布均无明显的变化。结论将去甲斑蝥酸钠制备成以脂质微球载药,使其在体内分布具有肝脏靶向性,从而在一定程度上提高了药物对肝癌及肝硬化的治疗效果。

The tissue distribution of sodium-NCTD lipid microsphere in the rats

Objective To compare the distribution patterns in tissues of sodium-norcantharidin(sodium-NCTD) lipid microsphere and injection in rat.Methods The sodium-NCTD lipid microsphere and injection were administered to the rats through thigh vein.The HPLC-MS method was used to determine the drug concentration in various tissues.Results Compared with the sodium-NCTD injection,the lipid microsphere could increase the concentration of the drug in the liver.The rate of relative distribution of the liver was increased from 16.3% to 32%.AUC was 218.72 mg·L-1·h-1.No obvious differences were found for the distribution of NCTD in heart,kidney,plasma between lipid microsphere and reference solution.Conclusion The sodium-NCTD lipid microsphere is proved to have targeting efficacy,it can improve the efficacy for the treatment of liver cancer and hepatic cirrhosis.