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目的:探讨三氧化二砷(As2O3)-碘油乳化物治疗裸鼠肝癌细胞株MHCC-97移植瘤模型的抑瘤作用及药代动力学情况。方法:将不同浓度的As2O3-碘油乳化物分别注入大白兔的腹腔内并检测外周血As2O3的浓度,绘制药物释放曲线,并将As2O3-碘油乳化物与人肝癌细胞株MHCC-97构建的肝脏型裸鼠肝细胞癌模型进行抑瘤作用。结果:3组大白兔腹腔内注入不同浓度梯度As2O3-碘油乳化物的实验组,与腹腔内单纯注入As2O3的对照组相比,30min~1h外周血中As2O3血药浓度偏低,P<0.05;2~3h外周血中的血药浓度差异无统计学意义;在4~8h血药浓度明显偏高,P<0.01;在3组实验组中,3种不同浓度梯度的As2O3-碘油乳化物在不同时间的血药浓度差异无统计学意义,P>0.05。采用As2O3-碘油乳化物对肝脏型裸鼠肝细胞癌模型的抑瘤作用与阴性对照组相比,差异有统计学意义,P<0.05;实验组与阳性对照组相比,平均瘤质量较阳性对照组有缩小,但无统计学意义,P>0.05。结论:As2O3-碘油乳化物在腹腔内释放缓慢,在外周血中能维持相对高浓度,并且维持时间长;As2O3-碘油乳化物对肝脏型裸鼠肝细胞癌模型的生长有抑制作用。
Objective: To investigate the anti-tumor effect and pharmacokinetics of arsenic trioxide (As2O3) -iodol emulsion in the treatment of human hepatocellular carcinoma cell line MHCC-97. Methods: Different concentrations of As2O3-lipiodol emulsions were injected into the peritoneal cavity of rabbits and the concentration of As2O3 in peripheral blood was measured. The drug release curve was drawn and the As2O3-lipiodol emulsion was incubated with human hepatoma cell line MHCC-97 Liver nude mouse model of hepatocellular carcinoma for tumor suppression. Results: Compared with the control group injected with As2O3 alone in the abdominal cavity, the concentration of As2O3 in peripheral blood of 30 min ~ 1 h was lower in the experimental group injected with As2O3-lipiodol emulsion with different concentration gradient ; 2 ~ 3h blood concentration in peripheral blood was no significant difference in the 4 ~ 8h plasma concentration was significantly higher, P <0.01; three experimental groups, three different concentrations of As2O3-lipiodol emulsion There was no significant difference in plasma concentration between different time points (P> 0.05). Compared with the negative control group, the inhibitory effect of As2O3-lipiodol emulsion on hepatocellular carcinoma model in nude mice was statistically significant (P <0.05). Compared with the positive control group, the average tumor mass Positive control group has reduced, but no statistical significance, P> 0.05. CONCLUSION: As2O3-lipiodol emulsion is slowly released in peritoneal cavity and can maintain a relatively high concentration in peripheral blood for a long time. As2O3-lipiodol emulsion can inhibit the growth of hepatocellular carcinoma model in nude mice.