Patent US4246261A successfully refreshed from Google Patents.
US4246261A
Expired / Lapsed
US
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Additives enhancing topical corticosteroid action
Assignee: Individual
•
Filing: 1979-08-09
•
Granted: 1981-01-20
•
Expires: 1999-08-09
Abstract
Abstract Composition and method for enhancing therapeutic effects of corticosteroids to alleviate the symptoms of inflammation and exfoliation such as psoriasis, eczema, seborrheic dermatitis and other inflammatory skin conditions consisting of a solution, cream, lotion, ointment or gel containing as two active ingredients a corticosteroid and an additive are disclosed. The therapeutic composition may include one or more of corticosteroids typically present in a total amount of from 0.01 to 2 percent and one or more of hydroxy acids or related compounds present in a total amount from 0.01 to 2 percent by weight of the total composition. Topical application of the therapeutic composition in a solution, cream, lotion, gel or ointment has been found to achieve a substantial increase in antiinflammatory action of corticosteroids.
Inventors
- 👤 Eugene J. Van Scott
- 👤 Ruey J. Yu
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 14:43
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/12; A61K31/00; A61K31/56; A61K31/57; A61K9/00; A61K9/0012; A61K9/0014
Claims Analysis
Total Claims: 48
Claim 1
Independent Claim
100 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerate, hydrocortisone-17-butyrate and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Glycolic Acid, α-Hydroxyisocaproic Acid,
Glucuronic Acid, α-Hydroxyisovaleric Acid,
Galacturonic Acid,
β-Hydroxybutyric Acid,
Gluconic Acid, Lactic Acid,
Glucoheptonic Acid,
β-Phenyllactic Acid,
α-Hydroxybutyric Acid,
Atrolactic Acid,
α-Hydroxyisobutyric Acid,
Mandelic Acid,
Galactonic Acid,
Pantoic Acid, and
Glyceric Acid.
______________________________________
Claim 2
Independent Claim
100 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerate, hydrocortisone-17-butyrate and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Glycolic Acid, α-Hydroxyisocaproic Acid,
Glucuronic Acid, α-Hydroxyisovaleric Acid,
Galacturonic Acid,
β-Hydroxybutyric Acid,
Gluconic Acid, Lactic Acid,
Glucoheptonic Acid,
β-Phenyllactic Acid,
α-Hydroxybutyric Acid,
Atrolactic Acid,
α-Hydroxyisobutyric Acid,
Mandelic Acid,
Galactonic Acid,
Pantoic Acid, and
Glyceric Acid.
______________________________________
Claim 3
Dependent Claim
23 words
The method of claim 1 wherein said member is present in a concentration of 0.01 to 2 percent by weight of said composition.
Claim 4
Dependent Claim
27 words
The method of claim 1 wherein a plurality of said members are present in a total concentration of 0.01 to 2 percent by weight of said composition.
Claim 5
Independent Claim
85 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerate, hydrocortisone-17-butyrate and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Malic Acid, Isocitric Acid,
Mucic Acid, Dihydroxymaleic Acid,
Citric Acid, Dihydroxtartaric Acid,
Saccharic Acid, [Dihydroxyfumaric Acid].
Tartaric Acid,
Tartronic Acid.
______________________________________
Claim 6
Independent Claim
85 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerate, hydrocortisone-17-butyrate and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Malic Acid, Isocitric Acid,
Mucic Acid, Dihydroxymaleic Acid,
Citric Acid, Dihydroxtartaric Acid,
Saccharic Acid, [Dihydroxyfumaric Acid].
Tartaric Acid,
Tartronic Acid.
______________________________________
Claim 7
Dependent Claim
23 words
The method of claim 4 wherein said member is present in a concentration of 0.01 to 2 percent by weight of said composition.
Claim 8
Dependent Claim
27 words
The method of claim 3 wherein a plurality of said members are present in a total concentration of 0.01 to 2 percent by weight of said composition.
Claim 9
Independent Claim
87 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerate, hydrocortisone-17-butyrate, and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflame areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Pyruvic Acid, Methyl Benzoylformate,
Methyl Pyruvate,
Ethyl Benzoylformate,
Ethyl Pyruvate,
β-Phenylpyruvic Acid,
Isopropyl Pyruvate,
β-Hydroxypyruvic Acid,
Benzoylformic Acid, and
β-Hydroxypyruvic Acid Phosphate.
______________________________________
Claim 10
Independent Claim
87 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerate, hydrocortisone-17-butyrate, and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflame areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Pyruvic Acid, Methyl Benzoylformate,
Methyl Pyruvate,
Ethyl Benzoylformate,
Ethyl Pyruvate,
β-Phenylpyruvic Acid,
Isopropyl Pyruvate,
β-Hydroxypyruvic Acid,
Benzoylformic Acid, and
β-Hydroxypyruvic Acid Phosphate.
______________________________________
Claim 11
Dependent Claim
23 words
The method of claim 7 wherein said member is present in a concentration of 0.01 to 2 percent by weight of said composition.
Claim 12
Dependent Claim
27 words
The method of claim 7 wherein a plurality of said members are present in a total concentration of 0.01 to 2 percent by weight of said composition.
Claim 13
Independent Claim
77 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone-17-valerate, hydrocortisone-17-butyrate, and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Gluconolactone, Saccharic acid Lactone
Glucuronolactone, Mucic acid lactone,
Glucoheptono Lactone,
Pantoyllactone, and
Galactonolactone.
______________________________________
Claim 14
Independent Claim
77 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone-17-valerate, hydrocortisone-17-butyrate, and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Gluconolactone, Saccharic acid Lactone
Glucuronolactone, Mucic acid lactone,
Glucoheptono Lactone,
Pantoyllactone, and
Galactonolactone.
______________________________________
Claim 15
Dependent Claim
23 words
The method of claim 10 wherein said member is present in a concentration of 0.01 to 2 percent by weight of said composition.
Claim 16
Dependent Claim
27 words
The method of claim 10 wherein a plurality of said members are present in a total concentration of 0.01 to 2 percent by weight of said composition.
Claim 17
Independent Claim
76 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerat hydrocortisone-17-butyrate and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Maleic Acid, Diethylacetylene dicarboxylate,
Diethylmaleate,
Dimethylacetylene dicarboxylate,
Acetylenedicarboxylic
Acid, and Dimethylmaleate.
______________________________________
Claim 18
Independent Claim
76 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerat hydrocortisone-17-butyrate and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Maleic Acid, Diethylacetylene dicarboxylate,
Diethylmaleate,
Dimethylacetylene dicarboxylate,
Acetylenedicarboxylic
Acid, and Dimethylmaleate.
______________________________________
Claim 19
Dependent Claim
23 words
The method of claim 13 wherein said member is present in a concentration of 0.01 to 2 percent by weight of said composition.
Claim 20
Dependent Claim
27 words
The method of claim 13 wherein a plurality of said members are present in a total concentration of 0.01 to 2 percent by weight of said composition.
Claim 21
Independent Claim
72 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerat hydrocortisone-17-butyrate and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Cysteic Acid, Homocysteic Acid, and
Cysteinesulfinic Acid.
______________________________________
Claim 22
Independent Claim
72 words
A method for enhancing the antiinflammatory activity of a therapeutic composition including a corticosteroid compound selected from the group consisting of hydrocortisone, hydrocortisone-21-acetate, hydrocortisone 17-valerat hydrocortisone-17-butyrate and triamcinolone acetonide in a pharmaceutically acceptable vehicle for topical application to inflamed areas of the human body comprising: admixing in said composition an effective amount of at least one member selected from the group consisting of: ______________________________________
Cysteic Acid, Homocysteic Acid, and
Cysteinesulfinic Acid.
______________________________________
Claim 23
Dependent Claim
23 words
The method of claim 16 wherein said member is present in a concentration of 0.01 to 2 percent by weight of said composition.
Claim 24
Dependent Claim
27 words
The method of claim 16 wherein a plurality of said members are present in a total concentration of 0.01 to 2 percent by weight of said composition.
Claim 25
Dependent Claim
93 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Glycolic Acid, α-Hydroxybutyric Acid,
Glucuronic Acid, α-Hydroxyisobutyric Acid,
Galacturonic Acid,
α-Hydroxyisocaproic Acid,
Gluconic Acid, α-Hydroxyisovaleric Acid,
Glucoheptonic Acid,
β-Hydroxybutyric Acid,
Lactic Acid, β-Phenyllactic Acid,
Atrolactic Acid, Mandelic Acid,
Galactonic Acid, Pantoic Acid, and
Glyceric Acid
______________________________________ Present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 26
Dependent Claim
93 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Glycolic Acid, α-Hydroxybutyric Acid,
Glucuronic Acid, α-Hydroxyisobutyric Acid,
Galacturonic Acid,
α-Hydroxyisocaproic Acid,
Gluconic Acid, α-Hydroxyisovaleric Acid,
Glucoheptonic Acid,
β-Hydroxybutyric Acid,
Lactic Acid, β-Phenyllactic Acid,
Atrolactic Acid, Mandelic Acid,
Galactonic Acid, Pantoic Acid, and
Glyceric Acid
______________________________________ Present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 27
Dependent Claim
24 words
The composition of claim 19 wherein said member is present in said composition in a concentration of from 0.01 to 2 percent by weight.
Claim 28
Dependent Claim
27 words
The composition of claim 19 wherein a plurality of said members are present in said composition in a total concentration of 0.01 to 2 percent by weight.
Claim 29
Dependent Claim
79 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Malic Acid, Isocitric Acid,
Mucic Acid, Dihydroxymaleic Acid
Citric Acid, Dihydroxytartaric Acid
Saccharic Acid, [Dihydroxyfumaric Acid,]
Tartaric Acid, and
Tartronic Acid
______________________________________
present in said composition to enhance the antiinflammatory activity of
said corticosteroid.
Claim 30
Dependent Claim
79 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Malic Acid, Isocitric Acid,
Mucic Acid, Dihydroxymaleic Acid
Citric Acid, Dihydroxytartaric Acid
Saccharic Acid, [Dihydroxyfumaric Acid,]
Tartaric Acid, and
Tartronic Acid
______________________________________
present in said composition to enhance the antiinflammatory activity of
said corticosteroid.
Claim 31
Dependent Claim
24 words
The composition of claim 22 wherein said member is present in said composition in a concentration of from 0.01 to 2 percent by weight.
Claim 32
Dependent Claim
27 words
A composition of claim 22 wherein a plurality of said members are present in said composition in a total concentration of 0.01 to 2 percent by weight.
Claim 33
Dependent Claim
80 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Pyruvic Acid, Methyl Benzoylformate,
Methyl Pyruvate,
Ethyl Benzoylformate,
Ethyl Pyruvate,
β-Phenylpyruvic Acid,
Isopropyl Pyruvate,
β-Hydroxypyruvic Acid,
Benzoylformic Acid, and
β-Hydroxypyruvic Acid Phosphate
______________________________________ present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 34
Dependent Claim
80 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Pyruvic Acid, Methyl Benzoylformate,
Methyl Pyruvate,
Ethyl Benzoylformate,
Ethyl Pyruvate,
β-Phenylpyruvic Acid,
Isopropyl Pyruvate,
β-Hydroxypyruvic Acid,
Benzoylformic Acid, and
β-Hydroxypyruvic Acid Phosphate
______________________________________ present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 35
Dependent Claim
24 words
The composition of claim 25 wherein said member is present in said composition in a concentration of from 0.01 to 2 percent by weight.
Claim 36
Dependent Claim
27 words
The composition of claim 25 wherein a plurality of said members are present in said composition in a total concentration of 0.01 to 2 percent by weight.
Claim 37
Dependent Claim
71 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Gluconolactone, Saccharic Acid, Lactone,
Glucuronolactone, Mucic Acid Lactone,
Glucoheptono Lactone,
Pantoyllactone, and
Galactonolactone
______________________________________ present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 38
Dependent Claim
71 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Gluconolactone, Saccharic Acid, Lactone,
Glucuronolactone, Mucic Acid Lactone,
Glucoheptono Lactone,
Pantoyllactone, and
Galactonolactone
______________________________________ present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 39
Dependent Claim
24 words
The composition of claim 28 wherein said member is present in said composition in a concentration of from 0.01 to 2 percent by weight.
Claim 40
Dependent Claim
27 words
The composition of claim 28 wherein a plurality of said members are present in said composition in a total concentration of 0.01 to 2 percent by weight.
Claim 41
Dependent Claim
69 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Maleic Acid, Diethylacetylene dicarboxylate,
Diethylmaleate, Dimethylacetylene dicarboxylate,
Dimethylmaleate, and
Acetylenedicarboxylic Acid
______________________________________ present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 42
Dependent Claim
69 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Maleic Acid, Diethylacetylene dicarboxylate,
Diethylmaleate, Dimethylacetylene dicarboxylate,
Dimethylmaleate, and
Acetylenedicarboxylic Acid
______________________________________ present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 43
Dependent Claim
24 words
The composition of claim 31 wherein said member is present in said composition in a concentration of from 0.01 to 2 percent by weight.
Claim 44
Dependent Claim
27 words
The composition of claim 31 wherein a plurality of said members are present in said composition in a total concentration of 0.01 to 2 percent by weight.
Claim 45
Dependent Claim
65 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Cysteic Acid Homocysteic Acid, and
Cysteinesulfinic Acid
______________________________________ present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 46
Dependent Claim
65 words
In an antiinflammatory composition for topical application to involved areas of the human body comprising an antiinflammatory effective amount of a corticosteroid in a pharmaceutically acceptable vehicle, the improvement comprising: an effective amount of at least one member selected from the group consisting of ______________________________________
Cysteic Acid Homocysteic Acid, and
Cysteinesulfinic Acid
______________________________________ present in said composition to enhance the antiinflammatory activity of said corticosteroid.
Claim 47
Dependent Claim
24 words
The composition of claim 34 wherein said member is present in said composition in a concentration of from 0.01 to 2 percent by weight.
Claim 48
Dependent Claim
27 words
The composition of claim 34 wherein a plurality of said members are present in said composition in a total concentration of 0.01 to 2 percent by weight.
References Cited (Backward Citations)
US3966924A
Cited
US4144332A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-01-20 | 1984-07-21 | 1985-01-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-01-20 | 1988-07-21 | 1989-01-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-01-20 | 1992-07-21 | 1993-01-20 | $7700.00 | Window Closed / Lapsed |