Wang Y M, Shi T S, Pu Y L, Zhu J G, Zhao Y L
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing.
Yao Xue Xue Bao. 1995 Dec;30(12):891-5.
Cisplatin-chitosan-microspheres (CDDP-DAC-MS) was chosen as a model preparation. 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 solution were respectively infused 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 platinum 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 histopathologic specimens showed nodular necrosis and hepatic cell degeneration in embolized region. The levels of GPT, GOT and ALP rose transiently after embolization and recovered to normal within 3 weeks. The clinical therapy in six liver cancer patients was successful. It would appear that CDDP-DAC-MS may be a good chemoembolization agent.
选用顺铂-壳聚糖微球（CDDP-DAC-MS）作为模型制剂。对犬经肝动脉栓塞CDDP-DAC-MS后进行了药代动力学、靶向及栓塞效果以及肝功能变化的研究，并采用无火焰原子吸收分光光度法（FAAS）测定血浆和肝脏中的铂含量。还报道了临床试验结果。将CDDP-DAC-MS和CDDP溶液分别通过5F导管注入犬肝动脉后，CDDP-DAC-MS组的血浆铂浓度和AUC低于CDDP溶液组，但24小时后肝组织中的铂含量是给予CDDP溶液时的2.92倍。血管造影显示肝脏小动脉数量显著减少，组织病理学标本显示栓塞区域有结节性坏死和肝细胞变性。栓塞后GPT、GOT和ALP水平短暂升高，并在3周内恢复正常。对6例肝癌患者的临床治疗取得成功。看来CDDP-DAC-MS可能是一种良好的化疗栓塞剂。
