Medicinal compositions retarded in the discoloration of phenolic hydroxyl compounds
AssigneeShionogi & Co., Ltd.
InventorsHidekazu Shodai, Noboru Nagafuji, Shuichi Matsuda
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Abstract
Coloring change of a pharmaceutical composition containing a compound having a phenolic hydroxyl group, such as an anti-inflammatory agent or an antioxidant having a phenolic hydroxyl group or the compound of formula (I) can be controlled by adding an acid. The present invention provides a pharmaceutical composition containing a compound having a phenolic hydroxyl group and an acid in which coloring change is controlled.
Claims11
A pharmaceutical solid composition which comprises a compound having a phenolic hydroxy group and an acid wherein coloring change is controlled, wherein said compound having a phenolic hydroxyl group is a compound of formula I:
- wherein R1 and R2 each is independently hydrogen, straight or branched C1-8 alkyl, or straight or branched C1-6 alkyloxy;
- R3 is hydrogen, straight or branched C1-8 alkyl, cycloalkyl, straight or branched C1-6 alkyloxy, arylalkyloxy, heteroarylalkyloxy, straight or branched C1-8 alkylcarbonyl, arylcarbonyl, substituted or unsubstituted carbamoyl, or a group of the formula:
- —(CH2)n—Q wherein Q is hydroxy, substituted or unsubstituted amino, aryl, heteroaryl, carboxy or straight or branched C1-6 alkyloxycarbonyl;
- and n is an integer of 0-3;
- or a pharmaceutically acceptable salt or hydrate thereof, and
- wherein the amount of said acid is 0.1 to 10% by weight relative to the compound having the phenolic hydroxyl group.
A process for manufacturing a pharmaceutical solid composition comprising a compound having a phenolic hydroxyl group with coloring change being controlled, which comprises adding an acid to said composition, wherein said compound having a phenolic hydroxyl group is a compound of formula I:
- wherein R1 and R2 each is independently hydrogen, straight or branched C1-8 alkyl, or straight or branched C1-6 alkyloxy;
- R3 is hydrogen, straight or branched C1-8 alkyl, cycloalkyl, straight or branched C1-6 alkyloxy, arylalkyloxy, heteroarylalkyloxy, straight or branched C1-8 alkylcarbonyl, arylcarbonyl, substituted or unsubstituted carbamoyl, or a group of the formula:
- —(CH2)n—Q wherein Q is hydroxy, substituted or unsubstituted amino, aryl, heteroaryl, carboxy or straight or branched C1-6 alkyloxycarbonyl;
- and n is an integer of 0-3;
- or a pharmaceutically acceptable salt or hydrate thereof, and
- wherein the amount of said acid is 0.1 to 10% by weight relative to the compound having the phenolic hydroxyl group.
A method for controlling coloring change of a pharmaceutical solid composition comprising a compound having a phenolic hydroxyl group, which comprises adding an acid to said composition, wherein the amount of said acid is 0.1 to 10% by weight relative to the compound having the phenolic hydroxyl group.
Dependencies are inferred from the claim text.