Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/24—Heavy metals; Compounds thereof
  • A61K33/26—Iron; Compounds thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/28—Compounds containing heavy metals
  • A61K31/295—Iron group metal compounds

Definitions

• This invention relates to a new therapeutically effective compound for providing a source of iron in the diet and more particularly relates to a new therapeutic compound in the nature of a ferrous salt of citric acid,
• ferrous compounds such as ferrous sulfate consistently causes some degree of digestive discomfort.
• a compound having the empirical formula Fe (C H O -10H O and the structural formula in which the ten molecules of water are bound by coordinate covalences may be prepared from citric acid or ferrous acid citrate by reacting either compound with the stoichiometric quantity of powdered iron required to produce triferrous dicitrate.
• the complex is a very slightly colored powder and is very stable to air oxidation, the ferrous content remaining substantially ungen is continued throughout the reaction and the mixture is stirred and heated to C. during a period of two hours and maintained at that temperature for an additional two or three hours.
• an additional 55.9 parts (1 mole) of reduced powdered iron is added and stirring is continued under nitrogen while maintaining the reaction temperature at 80 C. until the total reaction time is 24 hours.
• the mixture is suction-filtered whilehot.
• the filtered cake is washed with water until free from chloride ion and then three times with an equal volume of isopropanol.
• the product is dried at 50 C. for six hours.
• the yield is 650 parts (90% calculated as the decahydrate) of white crystalline material.
• the product so obtained is analyzed for carbon, hydrogen, and iron.
• T riferrous dicitrate decahydrate One hundred seventeen and four-tenths parts (0.445 mole) of the monoferrous acid citrate monohydrate obtained from Example 11 above is added to 500 parts of water, and air is displaced from the reaction kettle with nitrogen as described above. To this suspension is added 12.4 parts (0.223 mole) of powdered iron and the mixture is stirred and heated at 85 -90 C. for 24 hours. The product is filtered off, washed with water, then with acetone, and air dried. One hundred twenty-nine parts of a crystalline product similar to the product obtained in Example I is recovered. The product so obtained had the final analysis:
• the complex may be uniformly distributed in a suitable vehicle and formed into a tablet.
• Inert diluents or fillers are chosen which are chemically compatible with the complex. Satisfactory diluents include lactose, dextrose, sucrose, sodium chloride, glycine, kaolin and starch.
• a binder such as acacia, zein, tragacanth, gelatin, sodium carboxymethylcellulose, or methylcellulose and also, in order that a tablet may be readily prepared, that a lubricant such as magnesium stearate, zinc stearate, mineral oil, stearic acid, stearyl alcohol or monoand polyglycol esters also be intimately admixed with the filler and active agent.
• a lubricant such as magnesium stearate, zinc stearate, mineral oil, stearic acid, stearyl alcohol or monoand polyglycol esters also be intimately admixed with the filler and active agent.
• the above ingredients, including the complex may be formed into a tablet by thoroughly mixing the ingredients in a moist condition, granulating and compressing the mixture into tablets by conventional methods.
• Additives such as tricalcium citrate may be used alone or with inert diluents if it is desired to supply calcium along with the iron in
• a composition of matter in dosage unit form for oral administration effective as a source of iron in the diet which comprises a ferrous citrate complex having the formula Fe (C H O -1OH O in intimate admixture with an inert solid diluent.
• a process for the preparation of a triferrous dicitrate complex having associated therewith water of hydration comprising the steps of adding powdered iron to a suspension of monoferrous acid citrate in water and heating the mixture whereby the complex is formed and precipitated, and removing the precipitated complex.

Landscapes

• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Inorganic Chemistry (AREA)
• Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Priority Applications (2)

Applications Claiming Priority (1)

Publications (1)

Family

ID=24635617

Family Applications (1)

Country Status (2)

Cited By (10)

Citations (1)

• 1957
  • 1957-05-06 US US657042A patent/US2904573A/en not_active Expired - Lifetime
  • 1957-11-16 CH CH5274457A patent/CH367593A/de unknown

Patent Citations (1)

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