Non-hygroscopic, stable meldonium salts, method of...

C - Chemistry – Metallurgy – 07 – C

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C07C 243/12 (2006.01) A61K 31/205 (2006.01) C07C 53/00 (2006.01)

Patent

CA 2535150

New salts of Meldonium, the method of their preparation, and pharmaceutical formulation on their basis have been described. The general formula of these salts is X-(CH3)3N+NHCH2CH2COOH where X- is an acid anion selected from the group of pharmaceutically acceptable acids. Practically non-hygroscopic and/or increased thermal stability and/or lasting action Meldonium hydrogen salts of fumaric acid, phosphoric acid, oxalic acid, maleic acid, and pamoic acid as well as Meldonium orotate and galactarate are especially suitable. Novel pharmaceutical formulations containing non-hygroscopic and/or increased thermal stability and/or lasting action 3- (2,2,2-trimethylhydrazinium) propionate salts for oral, parenteral, rectal and transdermal introduction are concurrently described.

L'invention concerne de nouveau sels de meldonium, leur procédé de préparation ainsi qu'une formulation pharmaceutique les contenant. La formule générale de ces sels est X?-¿(CH¿3?)3N+NHCH2CH2COOH dans laquelle X?-¿ est un anion d'acide choisi dans le groupe d'acides pharmaceutiquement acceptables. Sont particulièrement adaptés des sels hydrogène propionate de meldonium pratiquement non hygroscopiques et/ou à stabilité thermique accrue et/ou à action prolongée d'acide fumarique, acide phosphorique, acide oxalique, acide maléique et d'acide pamoïque ainsi que le propionate orotate et galactarate de meldonium. L'invention concerne également de nouvelles formulations pharmaceutiques contenant les sels de meldonium non hygroscopiques et/ou à stabilité thermique accrue et/ou à action prolongée destinés à une administration par voie orale, parentérale, rectale et transdermique.

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