Pharmacokinetics and tissue distribution of 125I-Fc-G-CSF in rats / 国际药学研究杂志

ABSTRACT

Objective: To investigate the pharmacokinetics, tissue distribution and excretion characteristics of Fc- G- CSF (the fusion protein of Fc and granulocyte colony stimulating factor)in rats. Methods: Fc-G-CSF was labeled with 125I by the chloramine T method, and the content of 125I-Fc-G-CSF in each biological sample was determined by the trichloroacetic acid(TCA)precipitation method. Results: After a single subcutaneous injection of 125I-Fc-G-CSF 30 μg/kg, the AUC was(362.1±48.1)μg•h/L and the Cmax was(27.0±3.0)μg/L. Up to 36 hours of the drug administration, the drug exposure was highest in serum but lowest in brain. Up to 96 hours of the drug administration, the cumulative excretion rate through urine was about 57.5%, and the cumulative excretion rate through feces was about 23.5%. Conclusion: The blood concentration of 125I-Fc-G-CSF reached a peak after 12 h of the subcutaneous injection in rats, and the serum concentration was continuously higher than the concentrations in other tissues. The 125I-Fc-G-CSF excretion mainly adopted the urinary excretion.