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目的:观察阿霉素以不同剂型肝动脉给药后的药代动力学和生物学分布.方法:23例肝癌经肝动脉分别注入单纯阿霉素(A组,n=5),阿霉素与碘油混合液(B组,n=5),阿霉素与碘油混合并制成乳剂(C组,n=7),或C组之乳剂加用明胶海绵栓塞(D组,n=6).用高效液相色谱仪测定阿霉素外周血药浓度,对其中12例(A,B,C和D组各3例),用ECT测定肝脏的放射性强度.结果:肝动脉单纯注入阿霉素,仅形成一过性血浆高浓度,无器官优势分布特点.阿霉素碘油简单混合,未能发挥碘油的载体特点,出现的只是阿霉素和碘油各自的单一作用,与单纯注入阿霉素的疗效无显著差别.阿霉素碘油乳剂,能明显降低血药峰值浓度,延缓药物释放,并能选择性分布于肝肿瘤内,达到了靶向治疗肝癌的目的.加用明胶海绵栓塞,使上述作用更加明显.结论:从药代动力学和生物学分布角度分析,抗癌药碘油乳剂并用明胶海绵是最好的肝动脉化疗栓塞治疗肝癌的方法
Objective: To observe the pharmacokinetics and biodistribution of doxorubicin after different doses of hepatic artery administration. METHODS: Twenty-three cases of hepatocellular carcinoma were injected with adriamycin alone (group A, n=5), doxorubicin and lipiodol (group B, n=5), adriamycin and lipiodol were mixed and prepared. Emulsion (group C, n=7), or emulsion in group C plus gelatin sponge embolism (group D, n=6). The peripheral blood drug concentration of doxorubicin was measured by high performance liquid chromatography. Of these, 12 cases (3 cases each in group A, B, C, and D) were examined for the radioactivity of liver by ECT. RESULTS: The hepatic artery was injected with adriamycin alone. Only a transient high plasma concentration was formed. No organ predominance was found. Doxorubicin and lipiodol were simply mixed and failed to exert the carrier characteristics of lipiodol. What appeared was only the single action of doxorubicin and lipiodol, and there was no significant difference from the efficacy of doxorubicin alone. Doxorubicin lipiodol emulsion can significantly reduce the peak plasma concentration, delay drug release, and can be selectively distributed in liver tumors, achieving the purpose of targeted treatment of liver cancer. Add gelatin sponge embolism to make the above effect more obvious. Conclusion: From the perspective of pharmacokinetics and biological distribution, anti-cancer drug lipiodol emulsion combined with gelatin sponge is the best method of hepatic arterial chemoembolization for liver cancer.