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目的 对含甲氨喋呤正常人体白蛋白微囊 (MTX -HAS -MC)经动物肝动脉灌注栓塞后的体内药物动力学过程及微囊在肝动脉内的栓塞方式 ,栓塞水平 ,降解时限等进行了研究 .方法 选择健康杂种狗 ,肝动脉插管 ,分别注入含 10 %MTX白蛋白微囊及单纯MTX(溶于生理盐水 ) .定时测定肝组织 ,下腔静脉血药药物浓度及行肝组织病检 ,比较二者差异 .结果 组织形态学观察发现实验组微囊大多呈单行串珠样排列栓塞肝微动脉或肝毛细动脉 (窦前水平 ) ,多数在肝小动脉内以微囊为中心形成血栓 .术后 2 0天的标本内仍可见到完整无损的微囊检塞在位 .动态检测肝组织 ,下腔静脉血药物浓度 .实验组肝、血药物浓度一时程相差 1 33～ 5 70倍 ;对照组肝、血药物浓度相差不大 .微囊组肝药浓度始终高于相应的对照组肝药浓度 ,随着时间的推延 ,由 1 3倍～ 2 8倍 .微囊组的药物消除半衰期远远长过对照组 ,两者在肝内相差 2 8倍 ,在下腔静脉血内相差 3 6倍 .结论 微囊为血管末梢栓塞剂 ,在体内其裂解时限超过2 0天 .微囊栓塞阻断末梢血供 ,大量药物浓集于肝组织中 ,并可经微囊不断裂解缓解 ,使肝内持续保持一定的药物浓度 .以上作用对肝癌治疗有积极意义 .
Objective To study the in vivo pharmacokinetics of methotrexate-containing normal human albumin microcapsules (MTX-HAS-MC) after transcatheter arterial embolization in animal hepatic arteries, and the embolization method of microcapsules in the hepatic artery, embolization level, degradation time limit, etc. A study was conducted.Methods Healthy crossbred dogs were selected and the hepatic artery was cannulated, and 10% MTX albumin microcapsules and MTX alone (in physiological saline) were injected respectively. Serum concentrations of hepatic tissue, inferior vena cava, and drug levels were determined. The histopathological examination was performed to compare the differences between the two groups. Results Morphological observation revealed that most of the microcapsules in the experimental group were embolized with hepatic arterioles or hepatic capillary arteries (pre-sinus level) mostly in a single bead-like arrangement, most of which were centered on the microcapsules in the hepatic arterioles. The formation of thrombosis. After 20 days of the specimen can still be seen in the intact microcapsules in place. Dynamic detection of liver and inferior vena cava blood drug concentration. Experimental group, liver and blood drug concentration one time difference 1 33 ~ 5 70 times; the liver and blood drug concentrations in the control group are not much different. The liver drug concentration in the microcapsule group is always higher than the corresponding liver drug concentration in the control group, and the time delay is from 1 to 3 times to 28 times. Drug elimination half-life The period is much longer than the control group. There is a difference of 28 times in the liver and 3-6 times in the blood of the inferior vena cava. Conclusion Microcapsules are vascular peripheral embolization agents and their lysis time exceeds 20 days in vivo. Microcapsule embolization Blocking peripheral blood supply, a large number of drugs concentrated in the liver tissue, and can be sustained by the micro-encapsulation of continuous relief, so that the liver continues to maintain a certain concentration of drugs. The above effect on the treatment of liver cancer has positive significance.