STABLE 5, 10-METHYLENE-TETRAHYDROFOLATE PHARMACEUTICAL COMPOUNDS
Patent Number: WO2004112761
Publication date: 2004-12-29
Inventor(s): MOSER RUDOLF (CH); AMMANN THOMAS (CH)
Applicant(s): MERCK EPROVA AG (CH); MOSER RUDOLF (CH); AMMANN THOMAS (CH)
Requested Patent: WO2004112761
Application Number: WO2004EP06944 20040628
Priority Number(s): CH20030001123 20030626
IPC Classification: A61K31/00
EC Classification: A61K31/00, A61K31/191, A61K31/519
Equivalents:
Cited Documents: WO9727764; WO9526963; US4931441; US5434087
Abstract
The invention relates to 5,10-methylene-(6R)-,-(6S)-or (6R,S)-tetrahydrofolate (MTHF) pharmaceutical compounds whose stability is due to the adjustment thereof to a basic pH value and to a simultaneous citrate use. Said stabilisation is self-producible in the absence of a reducing agent. Said invention is particularly suitable for preparing lyophilization solution or lyophilisates or dry powders and dry mixtures since the stable MTHF solutions can be filled at the high concentration thereof into corresponding recipients like, for example vials, ampoules etc. Said lyophilisates are surpassingly storable and stable. They are easily reconstituted by adding water or aqueous solutions, thereby providing diluted injection solutions ready for use with an excellent stability. Said invention also makes it possible to produce highly concentrated calcium or acid MTHF salts, even difficult-to-dissolve, in the form of isotonic physiologically compatible solutions.
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