Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heavy metal containing doai
Patent
1992-03-23
1993-04-27
Dees, Jose G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heavy metal containing doai
514814, 556147, A61K 31295, C07F 1502
Patent
active
052062651
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a novel iron citrate complex, process for its production, and its pharmaceutical use.
Iron compounds with di- and trivalent iron, as well as iron chelates of a low or relatively high molecular weight have been utilized for a long time for the therapy of iron deficiency anemia. Most of these iron preparations, when used on a long-term scale, lead to gastrointestinal complications or exhibit a certain toxicity. In contrast thereto, ferritin proved to be an agent of local as well as general compatibility. However, ferritin has the drawback that it is available only in limited amounts because, besides horse spleen, there are no raw material sources for ferritin worth mentioning.
Therefore, it is an object of the invention to provide an iron compound, the micellar structure of which is very similar to the structure of the micelles of the ferritin nucleus, without concomitantly losing the favorable pharmaceutical and toxicological properties of ferritin.
Japanese Laid-Open Application JP 18 798/61 discloses a process for the production of a water-soluble iron complex from alkali citrate and iron carbonate. The iron carbonate, formed from 1 mole of FeCl.sub.3.6H.sub.2 O and 1.5 moles of sodium bicarbonate at temperatures of below 13.degree. C. is reacted with sodium citrate to form an iron complex salt consisting of about 60% iron.
It has now been discovered surprisingly that a brown-colored iron citrate micellar complex is produced from FeCl.sub.3.6H.sub.2 O, NaHCO.sub.3 and trisodium citrate exhibiting the following properties: sodium; Na.sub.7).sub.n wherein n=9-10; conventional organic solvents; =23-26.5;
This novel iron citrate complex is stable even in low pH ranges, thus having the advantage of passing through the stomach as an active agent without decomposition. The composition of the novel complex varies within the range customary for elementary analyses. Consequently, the indicated composition merely represents an average value, and the novel complex is not to be restricted to this value.
The iron citrate complex according to the invention is distinguished by extraordinary stability. Thus, solutions of the novel complex in a water/glycerol mixture (40:60) stored at room temperature proved to be stable even after 3 years. They showed no signs of decomposition whatever, i.e. there was no separation of flocculent precipitate, for example.
The novel complex is found to be an extensively unitary polymeric compound in all investigations. Thus, the electropherogram of a solution of this complex in a buffer on cellulose acetate film showed in all cases only one uniform band.
Further analyses yielded a content of bound citrate of about 28% for the complex.
The invention likewise relates to a process for the production of the iron citrate micellar complex having the above-disclosed properties, characterized by adding solid NaHCO.sub.3 to an aqueous solution of FeCl.sub.3.6H.sub.2 O, removing the thus-released CO.sub.2 from the solution with an inert gas or by vacuum degasification, adding solid trisodium citrate, and precipitating from the thus-obtained solution, after a relatively long period of equilibrating at room temperature, the product of the process with methanol.
Instead of using methanol precipitation, the product of the process can also be obtained by dialysis or gel filtration and subsequent freeze-drying. However, methanol precipitation is preferred.
The invention furthermore concerns medicinal agents containing the iron citrate micellar complex of this invention and nontoxic, pharmaceutically harmless extenders and auxiliary agents. Among these extenders and auxiliary agents are all substances and compounds known to a person skilled in this field of art. The novel complex can also be administered in combination with folic acid. The novel agent is likewise suited for the treatment of diseases involving iron deficits. The iron citrate complex utilized for the treatment of iron deficiencies in children, women, reconvalescent persons, high-performance athletes can be adm
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patent: 2904573 (1959-09-01), Orosnik et al.
patent: 2955981 (1960-10-01), Linkenheimer
patent: 2957806 (1960-10-01), Rummel
patent: 3873588 (1975-03-01), Osawa et al.
patent: 4400535 (1983-08-01), Madaus et al.
Antonini, deceased Eraldo
Vidic Hans-Jorg
Dees Jos,e G.
Nazario Porfirio
Schering Aktiengesellschaft
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