Single-dose pharmacokinetics of sodium ferric gluconate complex in iron-deficient subjects.
OBJECTIVE
To determine the single-dose pharmacokinetics of intravenous sodium ferric gluconate complex in sucrose injection (SFGC) in iron-deficient human volunteers, and to assess iron transport.


METHODS
Open-label, randomized study.


METHODS
Clinical research facility.


METHODS
Fourteen iron-deficient men and women.


METHODS
Subjects were randomized to receive a single intravenous dose of either SFGC 62.5 mg administered over 30 minutes or SFGC 125 mg over 60 minutes. Five days later, the same subjects were rerandomized to receive a second intravenous dose of SFGC, either 62.5 mg administered over 4 minutes or 125 mg over 7 minutes.


RESULTS
Blood samples were collected at predefined times before, during, and up to 72 hours after the infusion to determine the single-dose pharmacokinetics of SFGC. Assays were performed for both total iron and transferrin-bound iron, from which drug-bound iron could be calculated. Urine was collected over 24 hours before dosing and for 24 hours after the start of infusion to determine the renal elimination of iron. Clearance of SFGC from serum was rapid and far exceeded rates reported for iron dextran. Pharmacokinetic parameters were unaffected by dose or infusion rate. Serum iron derived from SFGC did not exceed the binding capacity of transferrin. Serum iron from SFGC became rapidly available (< 24 hrs) as transferrin-bound iron, but only after passage through another compartment, presumably the reticuloendothelial system (RES). At least 80% of the administered iron was transported to bone marrow within 24 hours after infusion.


CONCLUSIONS
Iron derived from SFGC appears to be rapidly transferred to a bioavailable iron compartment as transferrin-bound iron after digestion in the RES. At the doses administered in this study, liberation of potentially toxic, free iron was not detectable.
Seligman
Paul A
PA
Department of Medicine, University of Colorado Health Sciences Center, Denver 80262, USA.
Dahl
Naomi V
NV
Strobos
Jur
J
Kimko
Hui C
HC
Schleicher
Rhoda B
RB
Jones
Michael
M
Ducharme
Murray P
MP
D000328:Adult; D001682:Biological Availability; D005260:Female; D005290:Ferric Compounds / Q000493:pharmacokinetics* / Q000627:therapeutic use; D005293:Ferritins / Q000097:blood; D006207:Half-Life; D006801:Humans; D007501:Iron / Q000097:blood / Q000378:metabolism; D000090463:Iron Deficiencies; D008297:Male
D005290:Ferric Compounds; D005293:Ferritins; D007501:Iron; C035552:ferric gluconate