Method for stabilizing arylcarboxylic acid, stabilizer thereof and aqueous solution containing stabilized arylcarboxylic acid
AssigneeSenju Pharmaceutical Co., Ltd.
InventorShirou Sawa
Life of this patent
Estimating the term…
Abstract
A method for stabilizing an arylcarboxylic acid, which comprises adding a heterocyclic base to the arylcarboxylic acid or a pharmacologically acceptable salt thereof, a stabilizer thereof and an aqueous solution containing a stabilized arylcarboxylic acid. According to the stabilization method of the present invention, arylcarboxylic acid and pharmacologically acceptable salts thereof, particularly pranoprofen, can be stabilized at every temperature range, particularly at lower temperatures, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.
Claims7
A method for stabilizing an carboxylic acid or a pharmacologically acceptable salt thereof, which comprises adding a heterocyclic base of the formula (II):
- wherein
- A and A′ are each a carbon atom or a nitrogen atom;
- X is a carbon atom or a nitrogen atom;
- Y and Z are each a carbon atom or Y and Z taken together optionally form CH;
- R2, R3, R4, R5, R6, R7 and R8 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 R4 and R5 optionally form a 4- to 6-membered heterocyclic group with the adjacent nitrogen atom and X, and R6 and R7 optionally form a 4- to 6-membered heterocyclic group with the adjacent Y and Z, provided that when X is a nitrogen atom, R5 is void;
- and
- is a single bond or a double bond, provided that when A is a carbon atom, Y and Z are each CH and is a double bond, and when A is a nitrogen atom, Y and Z combinedly form CH and is a single bond,
- to an carboxylic acid of the formula (I):
- L1—R1COOH (I)
- wherein
- L1 is an optionally substituted heterocyclic 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.
Dependencies are inferred from the claim text.