Penetrating topical pharmaceutical compositions containing corticosteroids
AssigneeThe Procter & Gamble Company
InventorsEugene R. Cooper, Maurice E. Loomans, Mahdi B. Fawzi
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Abstract
Topical pharmaceutical compositions containing a corticosteroid component and a penetration-enhancing vehicle are disclosed. The vehicle comprises a binary combination of a C.sub.3 -C.sub.4 diol and a "cell-envelope disordering compound". The vehicle provides marked transepidermal and percutaneous delivery of corticosteroids. A method of treating certain rheumatic and inflammatory conditions, systemically or locally, is also disclosed.
Claims34
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.sub.16 -C.sub.20 straight chain, saturated normal fatty alcohols, and C.sub.4 -C.sub.20 straight chain, saturated mono- or dicarboxylic acids.
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.sub.16 -C.sub.20 straight chain, saturated normal fatty alcohols, and C.sub.4 -C.sub.20 straight chain, saturated mono- or dicarboxylic acids.
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.sub.16 -C.sub.20 straight chain, saturated normal fatty alcohols, and C.sub.4 -C.sub.20 straight chain, saturated mono- or dicarboxylic acids.
Dependencies are inferred from the claim text.