顺铂明胶微球体内释药特性的实验研究

目的 对比顺铂不同给药方法的效果，以了解顺铂明胶微球在体内的释药特点。方法在X线监视下，将顺铂明胶微球超选择栓塞在犬颈外动脉及其分支，以顺铂溶液灌注颈外动脉或在股静脉点滴作为对照，不同时间点取血样测试血药浓度。取栓塞组织石蜡切片，常规苏木精一伊红染色，光镜观察。结果 动脉灌注法可以产生局部较高的血药浓度，但维持时间较短；静脉滴注法血药浓度维持时间较长，但局部与全身血药浓度无显著差异；使用顺铂明胶微球进行栓塞可以在较小的用药剂量上在局部维持相对较长时间较高的血药浓度。结论 顺铂明胶微球进行动脉栓塞可以显著降低全身血药浓度及用药剂量，达到肿瘤靶向治疗的目的。

Experimental study on drug release characters of cisplatin gelatin microsphere

Objective To evaluate the release characteristics of cisplatin gelatin microsphere (CGM) in experimental dogs by the analysis of different administration methods of cisplatin.Methods CGM was injected into the external carotid artery of dogs by selective artery catherization for embolization under the supervision of X ray. Cisplatin solution was perfused into the external carotid artery or infused into femoral vein as control. Blood samples were tested at different times and analyzed statistically. The embolized tissue was investigated histologically. Results A transient higher blood drug concentration (BDC) was produced by artery perfusion but a longer time of BDC maintainance was achieved through venous infusion. There was no significant difference shown between the concentrations in systemic and local circulations. Small dosage of CGM through artery embolization could produce a high BDC level for a longer period in the local region.Conclusions External carotid artery embolization with CGM could signifcantly reduce the circulatory drug level and application dosage achieving the purpose of targeted tumor therapy.