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肝癌是全世界最常见的恶性肿瘤之一,而经导管肝动脉化疗栓塞(TACE)是治疗不能手术的中晚期肝癌的标准手段。从给药方式上而言,相对于静脉系统化疗及单纯的肝动脉灌注,肝动脉化疗栓塞术,尤其是进行明胶海绵补充栓塞,可明显改善物代谢动力学参数,既减少外周药物浓度和非靶器官毒性,又能增加局部药物浓度从而增强药物的治疗效果。从剂型上而言,阿霉素碘化油乳剂能明显降低血药峰值浓度,并能选择性分布于肝脏肿瘤内,达到靶向治疗肝癌的目的。加用明胶海绵补充栓塞,上述作用会更加明显。肝动脉化疗药微囊栓塞也能取得较明显的物代谢动力学优势,缓释、增加局部浓度、延长作用时间和减轻药物不良反应。无论外周血药峰值浓度(Cmax)还是曲线下面积(AUC),载药洗脱微球(DEB)栓塞均显著低于阿霉素碘化油乳剂栓塞,从而取得比传统的化疗栓塞更好的肝癌治疗效果。对不同给药方式及载药剂型的物代谢动力学研究,将对不断提高TACE的疗效和安全性有重要意义。
Liver cancer is one of the most common malignancies in the world, and transcatheter hepatic arterial chemoembolization (TACE) is the standard procedure for the treatment of inoperable advanced liver cancer. From the mode of administration, compared with intravenous chemotherapy and simple hepatic artery perfusion, hepatic artery chemoembolization, especially for gelatin sponge replacement embolization, can significantly improve the metabolite parameters, both to reduce peripheral drug concentration and non Target organ toxicity, but also increase the local drug concentration and thus enhance the therapeutic effect of the drug. In terms of dosage form, doxorubicin iodized oil emulsion can significantly reduce peak plasma concentration, and can selectively distributed in liver tumors, to achieve the goal of liver cancer treatment. Add gelatin sponge embolization, the above effect will be more obvious. Hepatic arterial chemotherapeutic drug microencapsulated embolization can also obtain more obvious advantages of metabolites, sustained release, increase the local concentration, prolong the action time and reduce the adverse drug reactions. Embolism of drug-eluting microspheres (DEB) was significantly lower than that of doxorubicin-iodinated oil emulsion, which was better than traditional chemoembolization, regardless of the peak plasma concentration (Cmax) or area under the curve (AUC) Liver cancer treatment effect. The study on the pharmacokinetics of different modes of administration and drug-loaded dosage forms will be of great significance to continuously improve the efficacy and safety of TACE.