[Studies on Pharmacologic Disposition of Adriamycin in Dog After Hepatic Arterial Embolization with Adriamycin Carboxymethyl-dextran-microspheres]

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.