Penetrating topical pharmaceutical compositions containing corticosteroids

Claim 2

A penetration-enhancing pharmaceutical composition for topical application, comprising: (a) a safe and effective amount of a pharmaceutically-active corticosteroid; (b) 0% to about 80% by weight of a solvent selected from the group consisting of water, ethanol or 2-propanol; and (c) about 10% to about 99.9% by weight of a penetration-enhancing carrier consisting essentially of: (i) a diol selected from the group consisting of 1,2-propanediol, 1-2,-butanediol, 1,3-butanediol, 2,3-butanediol, or mixtures thereof, and (ii) a cell-envelope disordering compound selected from the group consisting of methyl laurate, oleic acid, myristyl alcohol, or mixtures thereof; wherein said diol and said cell-envelope disordering compound are present in a ratio of diol:cell-envelope disordering compound of from about 1:1 to about 500:1 by weight; and wherein said penetration-enhancing composition is substantially free from any single member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids.

Claim 3

A composition according to claim 1 wherein the cell-envelope disordering compound is methyl laurate.

Claim 4

A composition according to claim 1 wherein the cell-envelope disordering compound is oleic acid.

Claim 5

A composition according to claim 1 wherein the cell-envelope disordering compound is myristyl alcohol.

Claim 6

A composition according to claim 1 wherein the level of any specific member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids is less than about 3.5% by weight.

Claim 7

A composition according to claim 5 wherein the level of any specific member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids is less than about 1% by weight.

Claim 8

A composition according to claim 1, which is substantially free from octanoic acid, decanoic acid, cetyl alcohol and stearyl alcohol.

Claim 9

A penetration-enhancing pharmaceutical composition for topical application, comprising: (a) about 0.05% to about 5%, by weight of a corticosteroid selected from the group consisting of triamcinolone acetonide, hydrocortisone acetate, betamethasone valerate, fluocinolone acetonide, flupamesone, or mixtures thereof; (b) 0% to about 80% by weight of a solvent selected from the group consisting of water, ethanol or 2-propanol; and (c) about 10% to about 99.9% by weight of a penetration-enhancing carrier consisting essentially of: (i) a diol selected from the group consisting of 1,2-propanediol, 1,2-butanediol, or mixtures thereof, (ii) a cell-envelope disordering compound selected from the group consisting of methyl laurate, oleic acid, myristyl alcohol, or mixtures thereof; wherein said diol and said cell-envelope disordering compound are present in a ratio of diol:cell-envelope disordering compound of from about 10:1 to about 100:1 by weight; and wherein said penetration-enhancing composition is substantially free from any specific member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids.

Claim 10

A penetration-enhancing pharmaceutical composition for topical application, comprising: (a) about 0.05% to about 5%, by weight of a corticosteroid selected from the group consisting of triamcinolone acetonide, hydrocortisone acetate, betamethasone valerate, fluocinolone acetonide, flupamesone, or mixtures thereof; (b) 0% to about 80% by weight of a solvent selected from the group consisting of water, ethanol or 2-propanol; and (c) about 10% to about 99.9% by weight of a penetration-enhancing carrier consisting essentially of: (i) a diol selected from the group consisting of 1,2-propanediol, 1,2-butanediol, or mixtures thereof, (ii) a cell-envelope disordering compound selected from the group consisting of methyl laurate, oleic acid, myristyl alcohol, or mixtures thereof; wherein said diol and said cell-envelope disordering compound are present in a ratio of diol:cell-envelope disordering compound of from about 10:1 to about 100:1 by weight; and wherein said penetration-enhancing composition is substantially free from any specific member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids.

Claim 11

A composition according to claim 8 wherein the diol compound is 1,2-propanediol.

Claim 12

A composition according to claim 8 wherein the diol compound is 1,2-butanediol.

Claim 13

A composition according to claim 8 wherein the cell-envelope disordering compound is oleic acid.

Claim 14

A composition according to claim 8 wherein the cell-envelope disordering compound is myristyl alcohol.

Claim 15

A composition according to claim 8 wherein the level of any specific member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids is less than about 3.5% by weight.

Claim 16

A composition according to claim 13 wherein the level of any specific member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids is less than about 1% by weight.

Claim 17

A composition according to claim 8 which is substantially free from octanoic acid, decanoic acid, cetyl alcohol and stearyl alcohol.

Claim 18

A method of treating nonendocrine immunologic, rheumatic, hypersensitivity or inflammatory conditions in humans or lower animals comprising topically applying to a human or animal in need of such treatment a safe and effective amount of a composition according to claim 1.

Claim 19

A method according to claim 16 wherein the rheumatic or inflammatory condition is arthritis.

Claim 20

A method according to claim 16 wherein the rheumatic or inflammatory condition is rheumatic fever.

Claim 21

A method according to claim 16 wherein the hypersensitivity reaction is bronchial asthma.

Claim 22

A method according to claim 16 wherein the hypersensitivity reaction is anaphylaxsis.

Claim 23

A method according to claim 16 wherein the inflammatory condition is dermatitis.

Claim 24

A method according to claim 16 wherein the composition is applied at an application situs for systemic treatment.

Claim 25

A method according to claim 22 wherein the composition is applied from a sustained release device.

Claim 26

A method according to claim 21 wherein the composition is applied topically to the afflicted situs.

Claim 27

A method of treating nonendocrine immunologic, rheumatic, hypersensitivity or inflammatory conditions in humans or lower animals comprising topically applying a to human or animal in need of such treatment a safe and effective amount of a composition according to claim 8.

Claim 28

A method according to claim 25 wherein the rheumatic or inflammatory condition is arthritis.

Claim 29

A method according to claim 25 wherein the rheumatic or inflammatory condition is rheumatic fever.

Claim 30

A method according to claim 25 wherein the hypersensitivity reaction is bronchial asthma.

Claim 31

A method according to claim 25 wherein the hypersensitivity reaction is anaphylaxsis.

Claim 32

A method according to claim 25 wherein the inflammatory condition is dermatitis.

Claim 33

A method according to claim 25 wherein the composition is applied at an application situs for systemic treatment.

Claim 34

A method according to claim 31 wherein the composition is applied from a sustained release device.

Claim 35

A method according to claim 30 wherein the composition is applied topically to the afflicted situs.

Claim 36

A penetration-enhancing pharmaceutical composition for topical application, comprising: (a) a safe and effective amount of a pharmaceutically-active corticosteroid; (b) 0% to about 80% by weight of a solvent selected from the group consisting of water, ethanol or 2-propanol; and (c) about 10% to about 99.9% by weight of a penetration-enhancing carrier consisting essentially of: (i) 1,2-butanediol, and (ii) a cell-envelope disordering compound selected from the group consisting of methyl laurate, oleic acid, oleyl alcohol, monoolein, myristyl alcohol, or mixtures thereof; wherein said 1,2-butanediol and said cell-envelope disordering compound are present in a ratio of diol:cell-envelope disordering compound of from about 1:1 to about 500:1 by weight; and wherein said penetration-enhancing composition is substantially free from any single member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids.

Claim 37

A penetration-enhancing pharmaceutical composition for topical application, comprising: (a) a safe and effective amount of a pharmaceutically-active corticosteroid; (b) 0% to about 80% by weight of a solvent selected from the group consisting of water, ethanol or 2-propanol; and (c) about 10% to about 99.9% by weight of a penetration-enhancing carrier consisting essentially of: (i) 1,2-butanediol, and (ii) a cell-envelope disordering compound selected from the group consisting of methyl laurate, oleic acid, oleyl alcohol, monoolein, myristyl alcohol, or mixtures thereof; wherein said 1,2-butanediol and said cell-envelope disordering compound are present in a ratio of diol:cell-envelope disordering compound of from about 1:1 to about 500:1 by weight; and wherein said penetration-enhancing composition is substantially free from any single member of the C 16 -C 20 straight chain, saturated normal fatty alcohols, and C 4 -C 20 straight chain, saturated mono- or dicarboxylic acids.