Design of iron (III) chelates in oral treatment of anemia: solution properties and absorption of iron (III) acetohydroxamate in anemic rats.
The design and use of iron(III) chelates in the oral treatment of iron-deficiency anemia is discussed in terms of the following criteria: (1) the ability of a chelate to exist as a monomeric species even at physiological pH values, (2) the rate of transfer of iron from the chelate to the iron-transporting protein-apotransferrin, (3) the rate of depolymerization of ferric citrate polymer by the free ligand, and (4) its nontoxicity and ability to regenerate hemoglobin levels in anemic rats. Detailed species distribution studies, stability constants, and kinetic data for iron(III) acetohydroxamate (criteria 1-3 above) show that it remains monomeric at physiological pH values and undergoes very rapid iron transfer with apotransferrin. Detailed animal studies show a significant increase in regeneration of hemoglobin in rats fed 2 ml of 4 mM Fe(III) acetohydroxamate daily when compared to rats fed similarly with Fe(III) citrate. A strong potential is thus indicated for Fe(III) acetohydroxamate as a source of iron in the anemic animal.
D000284:Administration, Oral; D000747:Anemia, Hypochromic / Q000188:drug therapy* / Q000378:metabolism; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D006877:Hydroxamic Acids / Q000008:administration & dosage / Q000378:metabolism / Q000627:therapeutic use; D007408:Intestinal Absorption; D007501:Iron / Q000378:metabolism; D007502:Iron Chelating Agents / Q000008:administration & dosage / Q000378:metabolism / Q000627:therapeutic use*; D007700:Kinetics; D008297:Male; D011199:Potentiometry; D051381:Rats; D012996:Solutions; D014168:Transferrin / Q000378:metabolism
D006877:Hydroxamic Acids; D007502:Iron Chelating Agents; D012996:Solutions; D014168:Transferrin; D007501:Iron