Aqueous iron carbohydrate complexes, their production and medicaments containing them

Abstract

A water soluble iron carbohydrate complex obtainable from an aqueous solution of iron(III) salt and an aqueous solution of the oxidation product of one or more maltrodextrins using an aqueous hypochlorite solution at a pH-value within the alkaline range, where, when one maltodextrin is applied, its dextrose equivalent lies between 5 and 20, and when a mixture of several maltodextrins is applied, the dextrose equivalent of the mixture lies between 5 and 20 and the dextrose equivalent of each individual maltodextrin contained in the mixture lies between 2 and 40, a process for its production and a medicament for the treatment and prophylaxis of iron deficiency conditions.

1 . An iron carboxypolymaltose complex of formula:
   [Fe0x(OH)y(H20)zin[{(c6H1005).(c6H1207)}ilk   
       wherein the values for variables x, y, z, n, m, 1 and k are such that said iron carboxypolymaltose complex has an average molecular weight in the range of from about
 80 kDa to about 400 kDa and an iron content in the range of from about 24 to about 32% 
 
       by weight. 
     
     
         2 . The iron carboxypolymaltose complex of claim  39 : 
       wherein
 n is about 103; 
 m is about 8; 
 1 is about 11; and 
 k is about 4. 
 
     
     
         3 . A medicament comprising the iron carboxypolymaltose complex of  claim 1  and a pharmaceutically acceptable carrier, excipient, or additive. 
     
     
         4 . The medicament of  claim 3  wherein said medicament is an aqueous solution of said iron carboxypolymaltose complex. 
     
     
         5 . The medicament of  claim 4 , wherein said aqueous solution is a brine solution. 
     
     
         6 . The medicament of  claim 3 , wherein said iron carboxypolymaltose complex is present in said aqueous solution in an amount of from about 1% to about 20% by weight,
 based on the total weight of the aqueous solution.   
     
     
         7 . The medicament of  claim 3 , wherein said iron carboxypolymaltose complex is present in said aqueous solution in an amount of about 5% by weight, based on the total weight of the aqueous solution. 
     
     
         8 . A method for treating an iron deficiency condition comprising the step of administering to a subject in need thereof a pharmaceutically effective amount of the medicament of  claim 3 . 
     
     
         9 . The method of  claim 8 , wherein said iron deficiency condition is iron deficiency anaemia. 
     
     
         10 . The method of  claim 8 , wherein said medicament is administered parenterally or orally. 
     
     
         11 . The method of  claim 8 , wherein said medicament is administered intravenously or intramuscularly. 
     
     
         12 . The method of  claim 8 , wherein said medicament is administered via injection. 
     
     
         13 . The method of  claim 8 , wherein said medicament is administered via infusion. 
     
     
         14 . The method of  claim 8 , wherein said medicament is administered in the form of a single dose. 
     
     
         15 . The method of  claim 14 , wherein said single dose comprises from 500 to 1000 mg of iron. 
     
     
         16 . The method of  claim 15 , wherein said single dose is applied over the course of less than one hour. 
     
     
         17 . A water-soluble iron carboxypolymaltose complex comprising from about 24% to about 32% weight to weight of iron, from about 25% to about 50% weight to weight of at least one oxidation product of maltodextrin, and which has a weight average molecular weight in the range of from 80 kDa to 400 kDa. 
     
     
         18 . The water-soluble iron carboxypolymaltose complex of  claim 17 , having a weight average molecular weight in the range of from 100 kDa to 350 kDa. 
     
     
         19 . A medicament comprising the water-soluble iron carboxypolymaltose complex of  claim 17  and a pharmaceutically acceptable carrier, excipient, or additive. 
     
     
         20 . The medicament of  claim 19 , wherein said medicament is an aqueous solution of said iron carboxypolymaltose complex. 
     
     
         21 . The medicament of  claim 20 , wherein said aqueous solution is a brine solution. 
     
     
         22 . The medicament of  claim 20 , wherein said iron carboxypolymaltose complex is present in said aqueous solution in an amount of from about 1% to about 20% by weight,
 based on the total weight of the aqueous solution.   
     
     
         23 . The medicament of  claim 20 , wherein said iron carboxypolymaltose complex is present in said aqueous solution in an amount of about 5% by weight, based on the total weight of the aqueous solution. 
     
     
         24 . A method for treating an iron deficiency condition comprising the step of administering to a subject in need thereof a pharmaceutically effective amount of the medicament of  claim 19 . 
     
     
         25 . The method of  claim 24 , wherein said iron deficiency condition is iron deficiency anaemia. 
     
     
         26 . The method of  claim 24 , wherein said medicament is administered parenterally or orally. 
     
     
         27 . The method of  claim 24 , wherein said medicament is administered intravenously or intramuscularly. 
     
     
         28 . The method of  claim 24 , wherein said medicament is administered via injection. 
     
     
         29 . The method of  claim 24 , wherein said medicament is administered via infusion. 
     
     
         30 . The method of  claim 24 , wherein said medicament is administered in the form of a single dose. 
     
     
         31 . The method of  claim 30 , wherein said single dose comprises from 500 to 1000 mg of iron. 
     
     
         32 . The method of  claim 31 , wherein said single dose is applied over the course of less than one hour.