US 7,320,985 B2
Method for stabilizing arylcarboxylic acid, stabilizer thereof and aqueous solution containing stabilized arylcarboxylic acid
Shirou Sawa, Kobe (Japan)
Assigned to Senju Pharmaceutical Co., Ltd., Osaka (Japan)
Filed on Jul. 23, 2003, as Appl. No. 10/624,674.
Application 09/885096 is a division of application No. 09/017626, filed on Feb. 02, 1998, granted, now 6,274,592.
Application 10/624674 is a continuation of application No. 09/885096, filed on Jun. 21, 2001, abandoned.
Claims priority of application No. 9-21805 (JP), filed on Feb. 04, 1997.
Prior Publication US 2005/0075350 A1, Apr. 07, 2005
Int. Cl. A61K 31/436 (2006.01); A61K 31/495 (2006.01); A61K 31/52 (2006.01); A61K 47/22 (2006.01)
U.S. Cl. 514—291  [514/230.5; 514/253.04; 514/253.08; 514/264; 514/300; 514/312; 514/352; 514/365; 514/420; 514/567; 514/226.2; 546/89; 546/311; 546/204; 546/500; 546/501; 544/38] 4 Claims
 
1. A method for stabilizing an arylcarboxylic acid or a pharmacologically acceptable salt thereof in an aqueous solution, which comprises adding a pyridonecarboxylic acid selected from
(a) a pyridonecarboxylic acid of the formula (IV):

OG Complex Work Unit Drawing
wherein
X is a carbon atom; and
R12, R13, R14 and R15 are the same or different and each is a hydrogen atom, a halogen, a carboxyl group, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group, an optionally substituted acyl group, an optionally substituted aryl group or an optionally substituted heterocyclic group;
wherein R12 and R13 optionally form a 4- to 6-membered heterocyclic group with the adjacent nitrogen atom and X, and R14 and R15 optionally form a 4- to 6-membered heterocyclic group with the adjacent carbon atom,
(b) cinoxacin or
(c) sparfioxacin,
or a pharmacologically acceptable salt thereof,
to an arylcarboxylic acid of the formula (I):
L1-R1COOH  (I)
wherein
L1 is an optionally substituted 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,
or a pharmacologically acceptable salt thereof.