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本文报告了丝裂霉素葡聚糖微球的制备与性质,也研究了丝裂霉素葡聚糖微球(简称(MMC-DMS)在狗体内的药物动力学特征和栓塞效果。微球的平均粒径为75±19μm,MMC含量为5%。在体外实验中,药物释放速度证明微球有缓释的性质。丝裂霉素葡聚糖微球与常规丝裂霉素通过导管分别输入狗的肝动脉内进行栓塞。用高效液相色谱(HPLC)法测定血药浓度,结果表明常规丝裂霉素峰浓度比MMC-DMS大1.6倍。血管造影显示肝的外周血管显著减少。组织病理学检查表明微球嵌入肝动脉内并在栓塞部分显示结节性坏死。MMC-DMS 在临床上试用于100例患肝癌的病人,肝动脉栓塞后病人瘤块缩小,症状改善,存活期延长。这些结果提示丝裂霉素葡聚糖微球是治疗肝癌很有用的栓塞剂,将有利于增强癌症化疗效果减少全身毒副反应。
In this paper, the preparation and properties of mitomycin-dextran microspheres were reported, and the pharmacokinetics and embolization effects of mitomycin-dextran microspheres (MMC-DMS) in dogs were also studied. The average particle size of 75 ± 19μm, MMC content of 5% .In vitro experiments, the release rate of drug proved that the microspheres sustained release properties of mitomycin-loaded dextran microspheres with conventional mitomycin by catheter Enter the hepatic artery in dogs for embolization.High performance liquid chromatography (HPLC) method for the determination of plasma concentration, the results showed that conventional mitomycin peak concentration than MMC-DMS 1.6 times .Anchorography showed that the liver peripheral vessels significantly reduced. Histopathological examination showed that the microspheres were embedded in the hepatic artery and showed nodular necrosis in the embolization section.MMC-DMS was clinically tested in 100 patients with liver cancer, the tumor mass was reduced, the symptoms were improved, and the survival time was decreased after hepatic artery embolization These results suggest that mitomycin-dextran microspheres is a useful embolic agent for the treatment of liver cancer, which will help enhance the efficacy of cancer chemotherapy to reduce systemic toxicity.