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大鼠静脉注射铁-聚(山梨醇-葡萄糖酸)复合物的消除模式和组织分布

Elimination pattern and tissue distribution of intravenous iron-poly (sorbitol-gluconic acid) complex in the rat.

作者信息

Lake-Bakaar D M

出版信息

Acta Pharmacol Toxicol (Copenh). 1980 May;46(5):337-44. doi: 10.1111/j.1600-0773.1980.tb02464.x.

Abstract

The elimination pattern and tissue distribution in rats of intravenous [14C-gluconic acid]-poly(sorbitol-gluconic acid) and 59Fe-iron-poly(sorbitol-gluconic acid) complex, glusoferron (Ferastral) have been examined. Twenty-four hours after injection of 20 or 200 mg/kg of [14C-gluconic acid]-poly(sorbitol-gluconic acid), 5%-6% of the injected dose of radiolabel was eliminated as 14CO2 and about 85% in the urine and faeces. Administration of 59Fe-iron-poly(sorbitol-gluconic acid) complex (10 and 100 mg of iron/kg) resulted in a urinary and faecal excretion of about 18% and 40% of the given dose, respectively, during the first 4 days. Biliary excretion was low. The mean molecular weight of the biliary product after the iron complex was lower than that of the parent compound. Radiocarbon in tissues after 24 hours was negligible. Liver and bones accounted for most of the retained radioiron following 100 mg of iron/kg bodyweight of the 59Fe-iron complex with maximum levels of 27% and 12% of the injected dose, respectively, 4 days after dosing. Red cell incorporation of 59Fe attained a level of 16% at the end of 28 days.

摘要

已对静脉注射的[14C-葡萄糖酸]-聚(山梨醇-葡萄糖酸)和59Fe-铁-聚(山梨醇-葡萄糖酸)复合物葡糖铁(Ferastral)在大鼠体内的消除模式和组织分布进行了研究。注射20或200mg/kg的[14C-葡萄糖酸]-聚(山梨醇-葡萄糖酸)24小时后,放射性标记注射剂量的5%-6%以14CO2形式消除,约85%通过尿液和粪便排出。给予59Fe-铁-聚(山梨醇-葡萄糖酸)复合物(10和100mg铁/kg)后,在最初4天内,尿液和粪便排泄量分别约为给药剂量的18%和40%。胆汁排泄量较低。铁复合物给药后胆汁产物的平均分子量低于母体化合物。24小时后组织中的放射性碳含量可忽略不计。给予59Fe-铁复合物100mg铁/kg体重后,肝脏和骨骼在给药4天后保留了大部分放射性铁,分别占注射剂量的27%和12%,达到最高水平。28天后,红细胞中59Fe的掺入水平达到16%。

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