He S M, Sun Y C, Wei S L, Wu C B, Wang P U, Wang S D, Xie J X
Department of Pharmaceutics, Beijing Medical University.
Yao Xue Xue Bao. 1993;28(11):859-64.
The ion exchange adriamycin carboxymethyl-dextran-microspheres (AD-CM-DMS) was chosen as a model preparation. Pharmacokinetics, targeting and embolization effects of the microspheres were studies after hepatic arterial embolization in vivo in dogs. After hepatic arterial infusion, the concentrations of ADM in peripheral vein blood and hepatic tissue were determined by HPLC. The peak concentrations were (0.558 micrograms/ml for AD-CM-DMS and 1.013 micrograms/ml for ADM solution. T1/2 (alpha), T1/2 (beta) and MRT of AD-CM-DMS were respectively 2.82, 3.19 and 1.28 times as much as those of ADM solution. At the target site, the tissue concentrations of AD-CM-DMS were respectively 8.0 and 9.1 times those of ADM solution. The dynamic vessel angiography revealed no external and internal collaterals and no complete degradation of AD-CM-DMS after sixteen weeks was observed. These results suggest that AD-CM-DMS are useful as embolic agent for the treatment of hepatic cancer. It could facilitate intensive chemotherapy with minimum systematic side effect.
选用离子交换阿霉素羧甲基葡聚糖微球（AD-CM-DMS）作为模型制剂。在犬体内进行肝动脉栓塞后，研究了微球的药代动力学、靶向性和栓塞效果。肝动脉灌注后，采用高效液相色谱法测定外周静脉血和肝组织中阿霉素（ADM）的浓度。峰浓度分别为：AD-CM-DMS为0.558微克/毫升，ADM溶液为1.013微克/毫升。AD-CM-DMS的T1/2（α）、T1/2（β）和平均滞留时间（MRT）分别是ADM溶液的2.82倍、3.19倍和1.28倍。在靶部位，AD-CM-DMS的组织浓度分别是ADM溶液的8.0倍和9.1倍。动态血管造影显示无内外侧支循环，16周后未观察到AD-CM-DMS完全降解。这些结果表明，AD-CM-DMS可用作治疗肝癌的栓塞剂。它可以在全身副作用最小的情况下促进强化化疗。
