Anti-inflammatory combination having reduced ulcerogenicity
AssigneeMerck & Co., Inc.
InventorTsung-Ying Shen
Life of this patent
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Abstract
A novel drug combination for more effective treatment of pain, fever, and inflammation with reduced ulcerogenicity comprising (a) 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid (indomethacin), and (b) a member selected from phenyl benzoic acid compounds, especially 2-hydroxy-5-(2',4'-difluorophenyl)benzoic acid (diflunisal), wherein the molar ratio of (b) to (a) is from 0.5 to 1.0 to 15.0 to 1.0.
Claims8
In combination:
- (a) 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid;
- and
- (b) a member selected from phenyl benzoic acid compounds of the formula:
- ##STR7## wherein X.sub.1-5) is halo;
- X being on one or more of the phenyl carbon atoms;
- R.sub.1 is selected from the group consisting of hydroxy, phenoxy, diloweralkylamino, and diloweralkylamino loweralkoxy;
- R.sub.2 is selected from the group consisting of hydrogen;
- lower alkanoyl;
- and lower alkoxycarbonyl;
- and
- R.sub.3 is selected from the group consisting of hydrogen and methyl;
- and pharmaceutically acceptable, non-toxic salt thereof;
- wherein the molar ration of (b) to (a) is from 0.5 to 1.0 to 15.0 to 1.0.
A method of treating pain, fever, and inflammation which comprises orally administering to a patient in need of such treatment, daily doses of from 1 mg. to mg./kg. of body weight of the combination of
- (a) 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid;
- and
- (b) a member selected from phenyl benzoic acid compounds of the formula:
- ##STR8## wherein X.sub.(1-5) is halo;
- X being on one or more of the phenyl carbon atoms;
- R.sub.1 is selected from the group consisting of hydroxy, phenoxy, diloweralkylamino, and diloweralkylamino loweralkoxy;
- R.sub.2 is selected from the group consisting of hydrogen;
- lower alkanoyl;
- and lower alkoxycarbonyl;
- and
- R.sub.3 is selected from the group consisting of hydrogen and methyl;
- and pharmaceutically acceptable, non-toxic salt thereof;
- wherein the molar ratio of (b) to (a) is from 0.5 to 1.0 to 15.0 to 1.0.
A pharmaceutical composition for treating pain, fever, and inflammation consisting of a non-toxic pharmaceutical carrier and an effective amount of the combination of
- (a) 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid;
- and
- (b) a member selected from phenyl benzoic acid compounds of the formula:
- ##STR9## wherein X.sub.(1-5) is halo;
- X being on one or more of the phenyl carbon atoms;
- R.sub.1 is selected from the group consisting of hydroxy, phenoxy, diloweralkylamino, and diloweralkylamino loweralkoxy;
- R.sub.2 is selected from the group consisting of hydrogen;
- lower alkanoyl;
- and lower alkoxycarbonyl;
- and
- R.sub.3 is selected from the group consisting of hydrogen and methyl;
- and pharmaceutically acceptable, non-toxic salt thereof;
- wherein the molar ratio of (b) to (a) is from 0.5 to 1.0 to 15.0 to 1.0.
A method of reducing the ulcerogenicity of 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid when given perorally to a host to treat pain, fever, and inflammation, comprising co-administering to said host an amount sufficient to reduce the ulcerogenicity of said 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid, of a member selected from phenyl benzoic acid compounds of the formula:
- ##STR10## wherein X.sub.(1-5) is halo;
- X being on one or more of the phenyl carbon atoms;
- R.sub.1 is selected from the group consisting of hydroxy, phenoxy, diloweralkylamino, and diloweralkylamino loweralkoxy;
- R.sub.2 is selected from the group consisting of hydrogen;
- lower alkanoyl;
- and lower alkoxycarbonyl;
- and
- R.sub.3 is selected from the group consisting of hydrogen and methyl;
- and pharmaceutically acceptable, non-toxic salt thereof.
Dependencies are inferred from the claim text.