WO2005123103A1 - Topical compositions and methods for epithelial-related conditions - Google Patents
Topical compositions and methods for epithelial-related conditions Download PDFInfo
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- WO2005123103A1 WO2005123103A1 PCT/US2005/020555 US2005020555W WO2005123103A1 WO 2005123103 A1 WO2005123103 A1 WO 2005123103A1 US 2005020555 W US2005020555 W US 2005020555W WO 2005123103 A1 WO2005123103 A1 WO 2005123103A1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
- A61K8/447—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof containing sulfur
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/496—Triazoles or their condensed derivatives, e.g. benzotriazoles
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- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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Definitions
- FIG 10. AFC reduces TPA-induced erythema
- a "penetration enhancer” is an agent known to accelerate the delivery of a substance through the skin.
- Suitable penetration enhancers usable in the present invention include, but are not limited to, dimethylsulfoxide (DMSO), dimethyl formamide (DMF), allantoin, urazole, N,N-dimethylacetamide (DMA), decylmethylsulfoxide (CioMSO), polyethylene glycol monolaurate (PEGML), propylene glycol (PG), propylene glycol monolaurate (PGML), glycerol monolaurate (GML), lecithin, the 1 -substituted azacycloheptan-2-ones, particularly l-n-dodecylcyclazacycloheptan-2-one (available under the trademark Azone R TM from Whitby Research Inco ⁇ orated, Richmond, Va.), alcohols, and the like.
- the permeation enhancer may also be a vegetable oil. Such oils include, for example,
- the water-ethanol mixtures are generally employed in a weight ratio from about 1:1 to about 20:1, preferably from about 3:1 to about 20:1, and most preferably from about 3:1 to about 10:1, respectively.
- the pH value of the oral vehicle is generally from about 4 to about 7, and preferably from about 5 to about 6.5.
- An oral topical vehicle having a pH value below about 4 is generally irritating to the oral cavity and an oral vehicle having a pH value greater than about 7 generally results in an unpleasant mouth feel.
- anti-fungal agent means any of a group of chemical substances having the capacity to inhibit the growth of or to destroy fungi.
- Anti-fungal agents include but are not limited to Amphotericin B, Candicidin, Dermostatin, Filipin, Fungichromin, Hachimycin, Hamycin, Lucensomycin, Mepartricin, Natamycin, Nystatin, Pecilocin, Perimycin, Azaserine, Griseofulvin, Oligomycins, Neomycin, Pyrrolnitrin, Siccanin, Tubercidin, Viridin, Butenafine, Naftifine, Terbinafine, Bifonazole, Butoconazole, Chlordantoin, Chlormidazole, Cloconazole, Clotrimazole, Econazole, Enilconazole, Fenticonazole, Flutrimazole, Isoconazole, Ketoconazole, Lanoconazole, Miconazole,
- antioxidants that are usable in the context of the present invention include ascorbic acid (vitamin C) and its salts, ascorbyl esters of fatty acids, ascorbic acid derivatives (e.g., magnesium ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl sorbate), tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other esters of tocopherol, butylated hydroxy benzoic acids and their salts, 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (commercially available under the tradename Trolox R ), gallic acid and its alkyl esters, especially propyl gallate, uric acid and its salts and alkyl esters, sorbic acid and its salts, lipoic acid, amines (e.g., N,N-diethylhydroxylamine, amino-guanidine), sulfhydryl compounds (e.g., glutaminol
- Hormone refers to natural substances produced by organs of the body that travel by blood to trigger activity in other locations or their synthetic analogs. Suitable hormones for use in the context of the present invention include, but are not limited to, calciferol (Vitamin D ) and its products, androgens, estrogens and progesterones.
- Anti-dandruff agents refer to agents that reduce, eliminate or prevent a scurf from forming on skin, especially of the scalp, that comes off in small white or grayish scales.
- a method of treating a medical, cosmetic and/or cosmeceutical condition associated with epithelial tissues is effected by topically applying, a pharmaceutically, cosmetically or cosmeceutically effective amount of the composition of the present invention as described above onto a surface.
- Non limiting examples of epithelial surfaces onto which the compositions of the present invention can be applied topically include the lateral aspect of forearms, the lateral aspect of legs, elbows, feet, backhands, back, scalp, face, buttocks, the ear canal and any other skin surfaces, and any mucosal membrane described herein.
- Topical application also includes applying the inventive compositions orally to the gingiva.
- the surface is a wound surface.
- topical application may include applying the inventive compositions to a non-epithelial surface such as the dermis.
- the wound surface is an open wound surface.
- an "open wound" is a physical trauma where the skin is lacerated, cut or punctured.
- compositions of the invention also are administered to treat a skin disorder that is already present, such as dry cracked skin.
- inventive compositions are administered to treat irritated skin, such as occurs with diaper rash.
- Inflammation can result from a wide variety of non-limiting conditions. These conditions include, but are not limited to, a) dermatitis, including, but not limited to, atopic dermatitis, medicamentosa, contact dermatitis, sebonheic, nummular dermatitis, chronic dermatitis of hands and feet, generalized exfoliative stasis, and localized scratches; b) acne, including, but not limited to, acne vulgaris, nodulocystic acne, acne fulminans, steroid acne, acne keloidalis nuchae, chloracne, pyoderma faciale, and cysts; c) folliculitis, including, but limited to, scalp folliculitis, spa pool folliculitis, oil folliculitis, pityrosporum folliculitis, and gram negative folliculitis; d) pseudofolliculitis barbae; e) chilblains; f) miliaria (prickly
- Dermal inflammation results in edema, erythema and tenderness.
- Dermal inflammation has the advantage of being rapidly induced, easily observed and rapidly measured.
- Epidermal keratinocytes which respond directly to a irritant because of their superficial location, also, release inflammatory mediators. These mediators can act directly (1) to attract inflammatory cells to the endothehum of the dermal venules or (2) to guide inflammatory cells through the dermis to the site of inflammation after they have passed through the vascular endothehum.
- mice Increasing concentrations of TPA dissolved in acetone were applied with the aid of a micropipetter onto the right ear of each of the five 6-8 week old, male Swiss Webster mice used in this analysis. Ten microliters were spread evenly onto the inner and outer surfaces using the pipette tip. The mice were then returned to their cages. The contralateral ear was treated only with acetone. After 5.5 hours, the mice were sacrificed and 6 mm punches were taken from each ear and weighed. Edema response was expressed as a percent increase in the treated ear's weight over the untreated ear.
- the increase in ear weight depends on TPA dose from 0.25 to 1.75 ⁇ g / 20 ⁇ l, reaching a maximum increase of approximately 150%) of the acetone-treated ear.
- This experiment identified doses between 1.5 - 2.0 ⁇ g / 20 ⁇ l as suitable to use in eliciting edema in future tests of anti-inflammatory agents.
- Each concentration was applied with the aid of a micropipetter onto the right ear of each of six mice so that 10 ⁇ l of each of the concentrations of the AFC inventive compositions were applied to an inner ear surface and 10 ⁇ l was applied to an outer ear surface of the right ear.
- the AFC inventive compositions were spread evenly with a pipette tip. Each contralateral ear was treated with only acetone in the same manner. The mice then were returned to their cages. After 5.5 hours, mice were sacrificed and 6 mm punches were taken from each ear and weighed. Edema response was expressed as the percent increase in the treated ear's weight over the untreated (acetone, vehicle only) ear.
- the ED 50 of the inventive AFC composition was approximately 0.44 mg/20 ⁇ l for TPA-induced edema inhibition.
- Example 2. AFC inhibits TPA-induced neutrophil infiltration in mice.
- TPA induces neutrophil infiltration in mice.
- Acute contact irritants such as TPA can also induce dermal infiltration of neutrophils. This may or may not be independent of the reduction of edema, as: 1) the maximum neutrophil response is delayed relative the maximal edema response; 2) some initants will induce edema independent of neutrophil infiltration; and 3) some of the known anti-inflammatory agents reduce one, but not the other.
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Priority Applications (10)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2005800274693A CN101039689B (zh) | 2004-06-12 | 2005-06-13 | 用于上皮相关病症的局部组合物和方法 |
| CA2579605A CA2579605C (en) | 2004-06-12 | 2005-06-13 | Topical compositions and methods for epithelial-related conditions |
| ES05757465T ES2420516T3 (es) | 2004-06-12 | 2005-06-13 | Composiciones tópicas y uso de las mismas para el tratamiento de afecciones relacionadas con el epitelio |
| DK05757465.9T DK1765376T3 (da) | 2004-06-12 | 2005-06-13 | Topiske sammensætninger og anvendelse deraf til behandling af epitel-relaterede tilstande |
| BRPI0512021-7A BRPI0512021A (pt) | 2004-06-12 | 2005-06-13 | composições tópicas e métodos para tratar condições epiteliais correlatas |
| MXPA06014514A MXPA06014514A (es) | 2004-06-12 | 2005-06-13 | Composiciones topicas y metodos para condiciones relacionada con epitelio. |
| AU2005254035A AU2005254035B2 (en) | 2004-06-12 | 2005-06-13 | Topical compositions and methods for epithelial-related conditions |
| RU2007101243/15A RU2007101243A (ru) | 2004-06-12 | 2005-06-13 | Композиции и способы для местного применения для состояний, связанных с эпителием |
| EP05757465.9A EP1765376B1 (en) | 2004-06-12 | 2005-06-13 | Topical compositions and use thereof for the treatment of epithelial-related conditions |
| JP2007527776A JP4987715B2 (ja) | 2004-06-12 | 2005-06-13 | 上皮関連状態のための局所用組成物及び方法 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57909304P | 2004-06-12 | 2004-06-12 | |
| US60/579,093 | 2004-06-12 | ||
| US65292105P | 2005-02-14 | 2005-02-14 | |
| US60/652,921 | 2005-02-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2005123103A1 true WO2005123103A1 (en) | 2005-12-29 |
Family
ID=35509456
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US2005/020555 Ceased WO2005123103A1 (en) | 2004-06-12 | 2005-06-13 | Topical compositions and methods for epithelial-related conditions |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1765376B1 (https=) |
| JP (1) | JP4987715B2 (https=) |
| KR (1) | KR20070061516A (https=) |
| CN (1) | CN101039689B (https=) |
| AU (1) | AU2005254035B2 (https=) |
| BR (1) | BRPI0512021A (https=) |
| CA (1) | CA2579605C (https=) |
| DK (1) | DK1765376T3 (https=) |
| ES (1) | ES2420516T3 (https=) |
| MX (1) | MXPA06014514A (https=) |
| PT (1) | PT1765376E (https=) |
| RU (1) | RU2007101243A (https=) |
| WO (1) | WO2005123103A1 (https=) |
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1899480A4 (en) * | 2005-06-13 | 2009-04-22 | Signum Biosciences Inc | COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATORY CONDITIONS |
| EP2389357A4 (en) * | 2009-01-20 | 2013-01-23 | Signum Biosciences Inc | INFLAMMATORY COMPLEXES |
| CN104739758A (zh) * | 2013-12-30 | 2015-07-01 | 天津高科生产力促进有限公司 | N-乙酰-l-半胱氨酸含漱液 |
| US9301988B2 (en) | 2007-03-30 | 2016-04-05 | Hi-Tech Pharmacal Co., Inc. | Method of treatment using a therapeutic agent for intranasal administration |
| US9669001B2 (en) | 2008-12-20 | 2017-06-06 | Convatec Technologies Inc. | Antimicrobial composition |
| US10117904B2 (en) | 2009-11-12 | 2018-11-06 | Signum Biosciences, Inc. | Use of anti-bacterial agents for the treatment of epithelial-related conditions |
| US10232047B2 (en) | 2011-12-20 | 2019-03-19 | Vyome Biosciences Private Limited | Topical oil composition for the treatment of fungal infections |
| US10493101B2 (en) | 2005-12-14 | 2019-12-03 | Convatec Technologies Inc. | Antimicrobial composition |
| EP3497080A4 (en) * | 2016-08-08 | 2020-07-29 | Signum Biosciences, Inc. | PHARMACEUTICAL FORMULATIONS AND THEIR USE |
| FR3104943A1 (fr) * | 2019-12-19 | 2021-06-25 | L'oreal | Lipoaminoacides et leurs utilisations comme actif antipelliculaire |
| US11135315B2 (en) | 2010-11-30 | 2021-10-05 | Convatec Technologies Inc. | Composition for detecting biofilms on viable tissues |
| US11286601B2 (en) | 2012-12-20 | 2022-03-29 | Convatec Technologies, Inc. | Processing of chemically modified cellulosic fibres |
| US12502454B2 (en) | 2013-05-15 | 2025-12-23 | Convatec Technologies Inc. | Wound dressing comprising an antimicrobial composition |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2683258C (en) * | 2009-10-20 | 2011-08-09 | Asa Bullion Investment Limited | Lotion for cleaning human anorectal area |
| US20160243011A1 (en) * | 2012-09-14 | 2016-08-25 | Elizabeth Arden, Inc. | Formulations Comprising Idebenone, N-Acetyl-S-Farnesyl-L-Cysteine and Ergothioneine and Uses Thereof |
| TWI687405B (zh) * | 2016-03-16 | 2020-03-11 | 慧穎應用生物科技有限公司 | 一種沉香樹籽萃取物、製備方法及其應用於抗過敏之用途 |
| CN111773212A (zh) * | 2020-08-14 | 2020-10-16 | 云南中医药大学 | 一种瑞香素的应用 |
| CN111909069B (zh) * | 2020-08-25 | 2022-04-19 | 安徽启威生物科技有限公司 | 一种可降解的季铵盐化合物及其制备方法和应用 |
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| US6372793B1 (en) * | 1999-08-20 | 2002-04-16 | Florida Agricultural & Mechanical University | Method for treatment of a neurological disease characterized by impaired neuromodulator function |
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- 2005-06-13 WO PCT/US2005/020555 patent/WO2005123103A1/en not_active Ceased
- 2005-06-13 CN CN2005800274693A patent/CN101039689B/zh not_active Expired - Fee Related
- 2005-06-13 CA CA2579605A patent/CA2579605C/en not_active Expired - Fee Related
- 2005-06-13 AU AU2005254035A patent/AU2005254035B2/en not_active Ceased
- 2005-06-13 PT PT57574659T patent/PT1765376E/pt unknown
- 2005-06-13 KR KR1020077000738A patent/KR20070061516A/ko not_active Withdrawn
- 2005-06-13 BR BRPI0512021-7A patent/BRPI0512021A/pt not_active IP Right Cessation
- 2005-06-13 EP EP05757465.9A patent/EP1765376B1/en not_active Expired - Lifetime
- 2005-06-13 DK DK05757465.9T patent/DK1765376T3/da active
- 2005-06-13 RU RU2007101243/15A patent/RU2007101243A/ru not_active Application Discontinuation
- 2005-06-13 MX MXPA06014514A patent/MXPA06014514A/es not_active Application Discontinuation
- 2005-06-13 ES ES05757465T patent/ES2420516T3/es not_active Expired - Lifetime
- 2005-06-13 JP JP2007527776A patent/JP4987715B2/ja not_active Expired - Fee Related
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| US5043268A (en) | 1990-05-04 | 1991-08-27 | The Trustees Of Princeton University | Substrates and inhibitors for prenyl cysteine methyltransferase enzymes |
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Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1899480A4 (en) * | 2005-06-13 | 2009-04-22 | Signum Biosciences Inc | COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATORY CONDITIONS |
| US10493101B2 (en) | 2005-12-14 | 2019-12-03 | Convatec Technologies Inc. | Antimicrobial composition |
| US9301988B2 (en) | 2007-03-30 | 2016-04-05 | Hi-Tech Pharmacal Co., Inc. | Method of treatment using a therapeutic agent for intranasal administration |
| US9669001B2 (en) | 2008-12-20 | 2017-06-06 | Convatec Technologies Inc. | Antimicrobial composition |
| EP2389357A4 (en) * | 2009-01-20 | 2013-01-23 | Signum Biosciences Inc | INFLAMMATORY COMPLEXES |
| US10117904B2 (en) | 2009-11-12 | 2018-11-06 | Signum Biosciences, Inc. | Use of anti-bacterial agents for the treatment of epithelial-related conditions |
| US11135315B2 (en) | 2010-11-30 | 2021-10-05 | Convatec Technologies Inc. | Composition for detecting biofilms on viable tissues |
| US10232047B2 (en) | 2011-12-20 | 2019-03-19 | Vyome Biosciences Private Limited | Topical oil composition for the treatment of fungal infections |
| US11286601B2 (en) | 2012-12-20 | 2022-03-29 | Convatec Technologies, Inc. | Processing of chemically modified cellulosic fibres |
| US12502454B2 (en) | 2013-05-15 | 2025-12-23 | Convatec Technologies Inc. | Wound dressing comprising an antimicrobial composition |
| CN104739758A (zh) * | 2013-12-30 | 2015-07-01 | 天津高科生产力促进有限公司 | N-乙酰-l-半胱氨酸含漱液 |
| EP3497080A4 (en) * | 2016-08-08 | 2020-07-29 | Signum Biosciences, Inc. | PHARMACEUTICAL FORMULATIONS AND THEIR USE |
| FR3104943A1 (fr) * | 2019-12-19 | 2021-06-25 | L'oreal | Lipoaminoacides et leurs utilisations comme actif antipelliculaire |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1765376B1 (en) | 2013-04-10 |
| JP4987715B2 (ja) | 2012-07-25 |
| MXPA06014514A (es) | 2007-08-07 |
| AU2005254035A1 (en) | 2005-12-29 |
| EP1765376A4 (en) | 2009-04-22 |
| JP2008502735A (ja) | 2008-01-31 |
| PT1765376E (pt) | 2013-06-27 |
| CA2579605A1 (en) | 2005-12-29 |
| CA2579605C (en) | 2013-10-01 |
| EP1765376A1 (en) | 2007-03-28 |
| DK1765376T3 (da) | 2013-07-01 |
| CN101039689B (zh) | 2013-01-30 |
| KR20070061516A (ko) | 2007-06-13 |
| AU2005254035B2 (en) | 2011-03-24 |
| ES2420516T3 (es) | 2013-08-23 |
| RU2007101243A (ru) | 2008-07-20 |
| BRPI0512021A (pt) | 2008-02-06 |
| CN101039689A (zh) | 2007-09-19 |
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