Method for solubilizing pyridonecarboxylic acid, solubilizer...

A - Human Necessities – 61 – K

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A61K 31/495 (2006.01) A61K 9/00 (2006.01) A61K 9/08 (2006.01) A61K 31/435 (2006.01) A61K 31/4375 (2006.01) A61K 31/44 (2006.01) A61K 31/496 (2006.01) A61K 31/50 (2006.01) A61K 31/5025 (2006.01) A61K 31/535 (2006.01) A61K 31/5383 (2006.01) A61K 47/12 (2006.01)

Patent

CA 2228535

A method for solubilizing a pyridonecarboxylic acid or a pharmacologically acceptable salt thereof, which comprises adding an arylcarboxylic acid of the formula (I): L1 - R1 COOH (I) wherein L' is an optionally substituted heterocyclic group or aryl group having not more than 14 carbon atoms, and R1 is an optionally substituted alkyl group having not more than 4 carbon atoms or a single bond, to the pyridonecarboxylic acid or the pharmacologically acceptable salt thereof, a solubilizer thereof and an aqueous solution containing a solubilized pyridonecarboxylic acid. According to the solubilization method of the present invention, the solubility of pyridonecarboxylic acid compounds and salts thereof at near physiological pH can be increased, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.

Une méthode pour solubiliser un acide pyridonecarboxylique ou un sel pharmacologiquement acceptable de ce dernier, qui comprend l'addition d'un acide arylcarboxylique de formule (I) : L1 - R1 COOH (I) où L' est un groupe hétérocyclique ou un groupe aryle facultativement substitué ne comptant pas plus de 14 atomes de carbone, et R1 est un groupe alkyle facultativement substitué ne comptant pas plus de 4 atomes de carbone ou une liaison simple, à l'acide pyridonecarboxylique ou au sel pharmacologiquement acceptable de ce dernier, un solubilisant de ce dernier et une solution aqueuse contenant un acide pyridonecarboxylique solubilisé. Conformément à la méthode de solubilisation de la présente invention, la solubilité des composés à base d'acide pyridonecarboxylique et des sels de ce dernier peut être augmentée au voisinage du pH physiologique, ce qui rend possible la production d'une solution aqueuse qui peut être utilisée comme gouttes oculaires, nasales ou auriculaires ou autre produit semblable.

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