顺铂壳聚糖微球犬肝动脉栓塞的研究  

STUDIES ONHE PATICARTERIALEMBOLIZATI ONWITH CISPLATIN- CHITOSAN- MICROSPHE RESINDOGS

作　　者：王亚敏[1] 石庭森[1] 蒲永林[1] 朱建纲[1] 赵延乐[1] 

机构地区：[1]北京军事医学科学院毒物药物研究所,北京医科大学人民医院放射科

出　　处：《药学学报》1995年第12期891-895,共5页Acta Pharmaceutica Sinica

摘　　要：研究了顺铂壳聚糖微球经犬肝动脉栓塞后体内药动学过程、靶向特征及栓塞效果，并初步应用于临床。经肝动脉给药材２４ｈ，栓塞组肝组织顺铂浓度为顺铂溶液组的２．９２倍，而其血浓峰值及药时曲线下面积（ＡＵＣ）均低于溶液组。血管造影显示，微球栓塞后肝脏外周血管明显减少，病理切片可见栓塞部位组织坏死。微球栓塞后ＧＰＴ，ＧＯＴ及ＡＬＰ有一过性升高，３周后基本恢复正常；微球临床初步应用效果较好。结果表明，以壳聚糖为载体材料制备的微球是一种良好的癌症化疗栓塞剂。Cisplatin- chitosan- microspheres( CDDP-DAC-MS )was chosen as a model prepara-tion.Pharmacokinetics,targeting and embolization effects and alteration of liver function were studied after hepatic arterial embolization in dogs with CDDp-DAC- MS, and the platinum content in plasma and liver was determined by flameless atomic absorption spectrophotometry (FAAS).The result of clinical trial was also reported. After the CDDP-DAC- MS and CDDP sol ution were respectively in fused into hepatic artery of dogs through a 5F catheter, the plasma concentration of platinum and AUC of CDDP-DAC- MS group was lower than that of CDDP solution group , but the platin um content in hepatic tissue was 2.92 times as much as that when CDDP solution was given after 24 h;Angiograms revealed a remarkable decrease in the number of arterioles in liver ,and histopathalogogic specimens showed nodular necrosis and hepatic cell degeneration in embolized region. The levels of Ger, GOT and ALP rose transiently after embolization and recovered to normal within 3 weeks. The clin ical therapy in six liver cancer Patients was successful.It would appear that CDDP- DAC- MS may be a good chemoembolization agent.

关 键 词：肝动脉栓塞 药代动力学 顺铂壳聚糖微球 

分 类 号：R969.1[医药卫生—药理学] R944.9[医药卫生—药学]