Tanji S, Akima K, Horiba M, Amemiya K, Aimoto T
Central Research Laboratory, Kaken Pharmaceutical Co., Ltd., Shizuoka, Japan.
Yakugaku Zasshi. 1990 Nov;110(11):869-75. doi: 10.1248/yakushi1947.110.11_869.
Degradation and excretion of Sizofiran (SPG), an anti-tumor polysaccharide, were studied in rats after a single or multiple administration. After a single intravenous injection of [14C]SPG (3 mg/kg), SPG distributed in the liver was degraded at very slow rate to SPG-like substances (SPGLS) having lower molecular weight than that of SPG, while SPG in the spleen and mesenteric lymph node was metabolized at much slower rate than that in the liver. In the experiment with multiple subcutaneous administration, SPG was also found to be present mainly as SPGLS in the liver, but almost as an unchanged SPG in the spleen. SPG was excreted in the urine mainly as metabolites with a molecular weight of less than 10000. These results indicate that degradation of SPG to lower molecular weight-SPGLS is a prerequisite for efficient urinary excretion and the degradation occurs mainly in the liver.
对一种抗肿瘤多糖裂褶菌多糖（SPG）在大鼠单次或多次给药后的降解和排泄情况进行了研究。单次静脉注射[14C]SPG（3毫克/千克）后，肝脏中分布的SPG以非常缓慢的速率降解为分子量低于SPG的类似裂褶菌多糖的物质（SPGLS），而脾脏和肠系膜淋巴结中的SPG代谢速率比肝脏中的要慢得多。在多次皮下给药实验中，还发现肝脏中的SPG主要以SPGLS形式存在，但在脾脏中几乎以未变化的SPG形式存在。SPG主要作为分子量小于10000的代谢产物经尿液排泄。这些结果表明，SPG降解为低分子量的SPGLS是其有效经尿液排泄的前提条件，且降解主要发生在肝脏中。
