Salicylate anti-inflammatory composition

Claim 2

A composition of matter for treating pain and inflammation in animal tissue, comprising from about 10 milligrams to about 500 milligrams of a salicylate-based anti-inflammatory compound selected from the group consisting of salicyclic acid, acetylsalicylic acid, aloxiprin, calcium carbaspirin, choline salicylate, methyl salicylate, salicoside, salicylamide, acetylsalicylsalicylic acid, salicylsulfuric acid, and pharmaceutically-acceptable salts and esters thereof, and from about 50 milligrams to about 250 milligrams of an organophosphonate compound selected from the group consisting of geminal organophosphonates of the formula ##STR5## or pharmaceutically-acceptable salts thereof, wherein n is an integer from 1 to about 10; R 3 is selected from the group consisting of H, C 1 -C 20 alkyl or cycloalkyl, C 2 -C 20 alkenyl, aryl, phenylethyl, benzyl, halogen, amino, substituted amino, --CH 2 COOH, --CH 2 (PO 3 H 2 ), --CH(PO 3 H 2 )(OH), or --CH 2 CH(PO 3 H 2 ) 2 ; and R 4 is selected from the group consisting of H, lower alkyl, amino, benzyl, halogen, --OH, --CH 2 COOH, --CH 2 PO 3 H 2 , or --CH 2 CH 2 PO 3 H 2 .

Claim 3

A composition according to claim 1 wherein the organophosphonate compound is a geminal diphosphonate.

Claim 4

A composition according to claim 2 wherein the organophosphonate compound is a member selected from the group consisting of ethane-1-hydroxy-1,1-diphosphonic acid, dichloromethanediphosphonic acid, methanediphosphonic acid, and the pharmaceutically-acceptable salts and esters thereof.

Claim 5

A composition according to claim 1, comprising a safe and effective amount of acetylsalicylic acid and a safe and effective amount of dichloromethanediphosphonic acid, or the pharmaceutically-acceptable salts or esters of said acids.

Claim 6

A composition according to claim 1, comprising a safe and effective amount of acetylsalicylic acid and a safe and effective amount of ethane-1-hydroxy-1,1-diphosphonic acid, or the pharmaceutically-acceptable salts or esters of said acids.

Claim 7

A composition according to claim 1, comprising a safe and effective amount of acetylsalicylic acid and a safe and effective amount of methanediphosphonic acid, or the pharmaceutically-acceptable salts or esters of said acids.

Claim 8

A composition of matter especially adapted for topical application to an afflicted situs to alleviate inflammation, comprising: (a) from about 1% to about 20% by weight of a salicylate-based anti-inflammatory compound selected from the group consisting of salicylic acid, acetylsalicylic acid, aloxiprin, calcium carbaspirin, choline salicylate, methyl salicylate, salicoside, salicylamide, acetylsalicylsalicylic acid, salicylsulfuric acid, benzyl 2-acetoxybenzoate, hexyl 2-acetoxybenzoate, and the pharmaceutically-acceptable salts and esters thereof; (b) from about 1% to about 20% by weight of a geminal organophosphonate compound having the formula ##STR6## or pharmaceutically-acceptable salts and esters thereof, wherein n is an integer from 1 to about 10; R 3 is selected from the group consisting of H, C 1 -C 20 alkyl or cycloalkyl, C 2 -C 20 alkenyl, aryl, phenylethyl, benzyl, halogen, amino, substituted amino, --CH 2 COOH, --CH 2 (PO 3 H 2 ), --CH(PO 3 H 2 )(OH), or --CH 2 CH(PO 3 H 2 ) 2 ; and R 4 is selected from the group consisting of H, lower alkyl, amino, benzyl, halogen, --OH, --CH 2 COOH, --CH 2 PO 3 H 2 , or --CH 2 CH 2 PO 3 H 2 ; and (c) the balance comprising a compatible carrier.

Claim 9

A composition of matter especially adapted for topical application to an afflicted situs to alleviate inflammation, comprising: (a) from about 1% to about 20% by weight of a salicylate-based anti-inflammatory compound selected from the group consisting of salicylic acid, acetylsalicylic acid, aloxiprin, calcium carbaspirin, choline salicylate, methyl salicylate, salicoside, salicylamide, acetylsalicylsalicylic acid, salicylsulfuric acid, benzyl 2-acetoxybenzoate, hexyl 2-acetoxybenzoate, and the pharmaceutically-acceptable salts and esters thereof; (b) from about 1% to about 20% by weight of a geminal organophosphonate compound having the formula ##STR6## or pharmaceutically-acceptable salts and esters thereof, wherein n is an integer from 1 to about 10; R 3 is selected from the group consisting of H, C 1 -C 20 alkyl or cycloalkyl, C 2 -C 20 alkenyl, aryl, phenylethyl, benzyl, halogen, amino, substituted amino, --CH 2 COOH, --CH 2 (PO 3 H 2 ), --CH(PO 3 H 2 )(OH), or --CH 2 CH(PO 3 H 2 ) 2 ; and R 4 is selected from the group consisting of H, lower alkyl, amino, benzyl, halogen, --OH, --CH 2 COOH, --CH 2 PO 3 H 2 , or --CH 2 CH 2 PO 3 H 2 ; and (c) the balance comprising a compatible carrier.

Claim 10

A composition according to claim 7 wherein the organophosphonate compound is a geminal diphosphonate.

Claim 11

A composition according to claim 8 wherein the geminal diphosphonate is a member selected from the group consisting of ethane-1-hydroxy-1,1-diphosphonic acid, dichloromethanediphosphonic acid, methanediphosphonic acid, and the pharmaceutically-acceptable salts and esters thereof.

Claim 12

A composition according to claim 7 wherein the carrier comprises a safe and effective amount of a C 10 , or higher, organic sulfoxide compound.

Claim 13

A composition according to claim 7 comprising a safe and effective amount of an anti-inflammatory compound selected from the group consisting of aspirin, benzyl 2-acetoxybenzoate and hexyl 2-acetoxybenzoate; a safe and effective amount of dichloromethanediphosphonic acid, or the pharmaceutically-acceptable salts thereof; the balance comprising a liquid, non-irritating carrier.

Claim 14

A composition according to claim 11 wherein the carrier comprises a safe and effective amount of decyl methyl sulfoxide.

Claim 15

A composition according to claim 1 or 5 wherein the salicylate-based anti-inflammatory agent is acetylsalicylic acid or a pharmaceutically-acceptable salt or ester thereof.

Claim 18

A method according to claim 14 wherein the organophosphonate compound is a geminal diphosphonate.

Claim 19

A method according to claim 15 wherein the organophosphonate compound is a member selected from the group consisting of ethane-1-hydroxy-1,1-diphosphonic acid, dichloromethanediphosphonic acid, methanediphosphonic acid, and the pharmaceutically-acceptable salts and esters thereof.

Claim 20

A method according to claim 14 wherein the animal is a human.

Claim 21

A method according to claim 17 which employs a safe and effective amount of aspirin and a safe and effective amount of dichloromethanediphosphonic acid, or the pharmaceutically-acceptable salts or esters thereof.

Claim 22

A method according to claim 17 which employs a safe and effective amount of aspirin and a safe and effective amount of ethane-1-hydroxy-1,1-diphosphonic acid, or the pharmaceutically-acceptable salts or esters thereof.

Claim 23

A method according to claim 17 which employs a safe and effective amount of aspirin and a safe and effective amount of methanediphosphonic acid, or the pharmaceutically-acceptable salts or esters thereof.

Claim 24

A method according to claim 14 or 16 wherein the salicylate-based anti-inflammatory agent is acetylsalicylic acid or a pharmaceutically-acceptable salt or ester thereof.