WO2024086348A1 - Formulation de traitement de préservation de la santé cutanée - Google Patents

Formulation de traitement de préservation de la santé cutanée Download PDF

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Publication number
WO2024086348A1
WO2024086348A1 PCT/US2023/035622 US2023035622W WO2024086348A1 WO 2024086348 A1 WO2024086348 A1 WO 2024086348A1 US 2023035622 W US2023035622 W US 2023035622W WO 2024086348 A1 WO2024086348 A1 WO 2024086348A1
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Prior art keywords
composition
consisting essentially
skin
antioxidant
emollient
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PCT/US2023/035622
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English (en)
Inventor
Julie Kenner
Hanafi Tanojo
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Kenner Skin Institute, Llc
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Publication of WO2024086348A1 publication Critical patent/WO2024086348A1/fr

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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
    • A61K8/67—Vitamins
    • A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/342—Alcohols having more than seven atoms in an unbroken chain
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/345—Alcohols containing more than one hydroxy group
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/39—Derivatives containing from 2 to 10 oxyalkylene groups
    • 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
    • A61K8/494—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
    • A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • 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
    • A61K8/67—Vitamins
    • A61K8/676—Ascorbic acid, i.e. vitamin C
    • 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
    • A61K8/67—Vitamins
    • A61K8/678—Tocopherol, i.e. vitamin E
    • 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86—Polyethers
    • 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
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations

Definitions

  • aspects of the present invention relate to a skin health preservation treatment formulation. More particularly, aspects of the invention relate to treating various types of manifestations of skin damage, such as photoaging, precancerous changes, pigmentation disorders, thinning of skin with aggravation of rosacea, certain forms of acne, milia and more.
  • Topical retinoids derived from vitamin A
  • topical retinoids have been widely used in dermatology to treat a variety of skin diseases and disorders, including acne, rosacea, psoriasis, skin cancer, hyperkeratotic disorders, pigmentation, sun induced changes including acceleration of skin aging, and the like.
  • Retinoids come in many different forms. Following are merely examples, and are in no way intended to be an exhaustive list.
  • Retinoic acid is an example of an active form of retinoid.
  • Retinyl esters are an example of a storage form.
  • Retinyl propionate, retinyl acetate, and retinyl palmitate are examples of stable forms of retinoids.
  • Retinol and tretinoin are examples of unstable forms of retinoid. Ordinarily skilled artisans will appreciate that retinoids exhibit varying degrees of stability or instability depending on the degree of exposure to sunlight (visible and/or UV light), for example.
  • UV ultraviolet
  • Intrinsic factors such as stress, sleep deficiency, and nutritional deficiency also can contribute to skin aging.
  • retinoids can be used to address many of these skin issues.
  • retinoids When applied to the skin, retinoids work with skin enzymes to deliver the active ingredient to skin cells over time. It is desirable to provide retinoids in amounts that patients can tolerate, and are effective.
  • Over-the-counter (OTC) and prescription formulations of active retinoids can deliver retinoids to skin in excess of a patient's ability to tolerate them, leading to retinoid reactions.
  • active retinoids for example, retinol and tretinoin, respectively
  • Such formulations also can be highly unstable, as noted above.
  • retinoids are those that individual tolerance to retinoids can vary. Another issue is that the amount of retinoids necessary for effective treatment can be difficult for people to tolerate. Yet another relates to delivery of retinoids in sufficient quantities to be therapeutically and/or cosmeceutically effective.
  • aspects of the present invention relate to a skin care composition that provides greater retinoid tolerance for patients, thereby enhancing the effect of retinoids in the treatment of various skin conditions as discussed herein.
  • Embodiments relate to administering a therapeutically and/or cosmeceutically effective amount of compositions to be described herein.
  • compositions, kits, and methods are provided for skin care, the composition comprising: about 0.01-2.0% w/w retinoid; about 0.04-8.0% w/w antioxidant; about 0.01-2.0% w/w moisturizer; about 1.5-13.0% w/w emollient; about 4.0-36.0% w/w emulsifier; and about 0.5-3.0% w/w preservative, based on the total weight of the composition, in a physiologically acceptable medium selected from the group consisting of lotion, gel, hydrogel, and cream.
  • the active ingredient comprises vitamin A, preferably about 0.01- 2.0% w/w retinyl palmitate, more preferably 0.05-1.5%, still more preferably 0.1-1.0%.
  • the antioxidant comprises vitamin C and vitamin E, preferably further comprising rosemary leaf extract and sunflower seed oil, preferably about 0.01-2.0% w/w sodium ascorbyl phosphate, more preferably 0.05-1.5%, still more preferably 0.1-1.0%; about 0.01-2.0% w/w tocopherol acetate, more preferably 0.05-1.5%, still more preferably 0.1-1.0%; about 0.01-2.0% w/w rosmarinus officinalis leaf extract, more preferably 0.05-1.5%, still more preferably 0.1-1.0%; and about 0.01-2.0% w/w helianthus annuus seed oil, more preferably 0.05-1.5%, still more preferably 0.1-1.0%.
  • the moisturizer comprises about 0.1-2.0% allantoin, more preferably 0.2-1.8%, still more preferably 0.5-1.5%.
  • the emollient comprises glycerin and jojoba esters.
  • the emollient comprises about 1-10.0% w/w glycerin, more preferably 2.0-8.0%, still more preferably 3.0-7.0% and about 0.5-3.0% w/w jojoba esters, more preferably 0.8-2.0%, still more preferably 1.0-1.5%.
  • the emulsifier comprises a water-in-oil emulsifier or an oil-in-water emulsifier.
  • the emulsifier comprises cetyl alcohol, glycerin, and lanolin.
  • emulsifier comprises about 0.05-3.0% w/w cetyl alcohol, more preferably 0.08- 2.7%, still more preferably 1.0-2.5%; about 1-10.0% w/w glyceryl stearate, more preferably 1.8- 8.0%, still more preferably 3.0-7.0%; about 0.5-3.0% w/w lanolin alcohol, more preferably 0.8- 2.8%, still more preferably 1.0-2.5%; about 1-10.0% w/w PEG-100 stearate, more preferably 2.0- 9.0%, still more preferably 3.0-7.0%; and about 1-10.0% w/w PPG 3 benzyl ether myristate, more preferably 2.0-9.0%, still more preferably 3.0-7.0%.
  • the preservative comprises phenoxyethanol, particularly 0.5-3.0% w/w phenoxyethanol, more preferably 0.8-2.5%, still more preferably 1.0-2.0%.
  • the composition comprises: an active ingredient comprising about 0.01-2.0% retinyl palmitate; an antioxidant comprising about 0.01-2.0% w/w sodium ascorbyl phosphate; about 0.01- 2.0% w/w tocopherol acetate; about 0.01-2.0% w/w rosmarinus officinalis leaf extract; and about 0.01-2.0% w/w helianthus annuus seed oil; a moisturizer comprising about 0.01-2.0% allantoin; an emollient comprising about 1-10.0% w/w glycerin and about 0.5-3.0% w/w jojoba esters; an emulsifier comprising about 0.05-3.0% w/w cetyl alcohol; about 1-10.0% w/w glyceryl stearate; about 0.5-3.0% w/w lanolin alcohol; about 1-10.0% w/w PEG-100 stearate; and about 1-10.0% w
  • the composition consists essentially of the just-mentioned ingredients.
  • the composition consists essentially of: an active ingredient consisting essentially of about 0.01-2.0% retinyl palmitate; an antioxidant consisting essentially of about 0.01-2.0% w/w sodium ascorbyl phosphate; about 0.01-2.0% w/w tocopherol acetate; about 0.01-2.0% w/w rosmarinus officinalis leaf extract; and about 0.01-2.0% w/w helianthus annuus seed oil; a moisturizer consisting essentially of about 0.01-2.0% allantoin; an emollient consisting essentially of about 1-10.0% w/w glycerin and about 0.5-3.0% w/w jojoba esters; an emulsifier consisting essentially of about 0.05-3.0% w/w cetyl alcohol; about 1-10.0% w/w glyceryl stearate; about 0.5-3.0% w/w lanolin alcohol; about 1-10.0% w
  • the composition may address aging skin conditions as manifested in various types of skin conditions, including but not limited to deep wrinkling, coarseness, freckled/mottled pigmentation, sallowness, melasma, visible blood vessels, leathered appearance, elastotic tissue laydown, loss of volume down to bone with subsequent laxity and hanging skin, dullness, irregular dryness/oiliness, giant open or closed comedones, aggravation of rosacea, scaly pre-cancerous patches, and skin cancer.
  • skin conditions including but not limited to deep wrinkling, coarseness, freckled/mottled pigmentation, sallowness, melasma, visible blood vessels, leathered appearance, elastotic tissue laydown, loss of volume down to bone with subsequent laxity and hanging skin, dullness, irregular dryness/oiliness, giant open or closed comedones, aggravation of rosacea, scaly pre-cancerous patches, and skin cancer.
  • compositions are believed to exert their beneficial effects to the skin through improved tolerance of retinoids, leading to the ability to apply higher amounts of retinoids to the skin.
  • higher amounts may be applied in various ways, such as a higher amount at each application, or a more frequent application, or a higher amount applied more frequently.
  • the improved tolerance of retinoids is believed to result from the combination of emollient and emulsifier as a vehicle for application of the active ingredient to the skin, and more particularly from the combination of the particular moisturizer, particular emollient, and particular emulsifier as a vehicle for application of the active ingredient to the skin.
  • the composition may have an aqueous phase that is present in a content ranging from 36% to 96.4% by weight, relative to the total weight of the composition, optionally from 40% to 95%, from 45% to 90%, or from 50% to 75%.
  • compositions may be more or less fluid and may have the appearance of a white or colored cream, an ointment, a milk, a lotion, a serum, a paste, a mousse or a gel.
  • compositions according to aspects of the invention may also contain additives and adjuvants that are common in cosmetics, such as hydrophilic or lipophilic gelling agents, preservatives, antioxidants, solvents, fragrances, fillers, pigments, odor absorbers and dyestuffs.
  • additives and adjuvants that are common in cosmetics, such as hydrophilic or lipophilic gelling agents, preservatives, antioxidants, solvents, fragrances, fillers, pigments, odor absorbers and dyestuffs.
  • the amounts of these various additives and adjuvants are those conventionally employed in the field under consideration, and range, for example, from 0.01% to 10% of the total weight of the composition.
  • Exemplary hydrophilic gelling agents may include in particular, carboxyvinyl polymers (carbomer), acrylic copolymers such as acrylate/alkyl acrylate copolymers, polyacrylamides, polysaccharides, natural gums and clays.
  • Exemplary lipophilic gelling agents may include
  • antioxidant is intended a substance that helps protect the skin's surface from oxidative damage caused by free radicals and environmental aggressors like UV and pollution. Antioxidants can provide substantial anti-aging benefits. Various examples of antioxidants will be apparent to ordinarily skilled artisans, and so will not be listed or detailed here.
  • moisturizer is intended: (a) either a compound acting on the barrier function, in order to maintain the moisturization of the stratum corneum, or an occlusive compound; or (b) a compound that directly increases the water content of the stratum corneum; or (c) a compound that activates the sebaceous glands.
  • a compound acting on the barrier function in order to maintain the moisturization of the stratum corneum, or an occlusive compound
  • a compound that directly increases the water content of the stratum corneum or a compound that activates the sebaceous glands.
  • emollient is intended a preparation that softens the skin.
  • An emollient may be an ingredient that may be applied directly to the skin to soothe and hydrate it.
  • An emollient may cover the skin with a protective film to trap in moisture.
  • Various examples of emollients also will be apparent to ordinarily skilled artisans, and so will not be listed or detailed here.
  • emulsifier an ingredient that allows water and oil components in a cream or lotion to mix.
  • emulsifiers will be apparent to ordinarily skilled artisans as well, and so will not be listed or detailed here.
  • ingredients may be identified as having a particular function in the composition, for example, as an antioxidant, a moisturizer, an emollient, an emulsifier, or a preservative.
  • an ingredient identified as having a particular function also may perform another function.
  • an ingredient identified as an emollient may also function as an emulsifier or a humectant; an ingredient identified as a preservative may function as an antimicrobial agent; and so on.
  • the composition should also comprise a vehicle to enable the active ingredient to be conveyed to the skin in an appropriate dilution.
  • the composition may be in a form of a liquid, suspension, emulsion, lotion, or cream.
  • compositions of the invention presents a wide range of possibilities depending on the required product form of the composition. Suitable vehicles can be classified as described hereinafter.
  • vehicles are substances which can act as diluents, dispersants, or solvents for the active ingredients, such that the vehicles ensure that they can be applied to and distributed evenly over the skin at an appropriate concentration.
  • a vehicle may be one which aids penetration of the active ingredient into the skin, thus ensuring that the active ingredient is tolerable to subjects, at the same time ensuring the efficacy of the formulation.
  • Compositions according to aspects of the invention can include water as a vehicle, and/or at least one cosmetically acceptable vehicle other than water.
  • Vehicles other than water that can be used in compositions according to aspects of the invention can include solids or liquids such as emollients, propellants, solvents, humectants, thickeners and powders. Examples of each of these types of vehicles will be known to ordinarily skilled artisans, and so will not be listed or detailed here.
  • the amount of vehicle in the composition should preferably be sufficient to carry at least a portion of the active ingredient to the skin in an amount which is sufficient effectively to provide skin benefit.
  • the amount of the vehicle can comprise the major portion of the composition, particularly where little or no other ingredients are present in the composition.
  • composition according to aspects of the invention can contain ingredients other than those already mentioned, depending on the form of the intended product. It is, for example, possible to include antiseptics, coloring agents, and detergents, as well as other preservatives, antioxidants, emulsifiers, some of which are described in detail above.
  • composition according to aspects of the invention can also be employed as a vehicle for a wide variety of cosmetically or pharmaceutically active ingredients, particularly ingredients which have some beneficial effect when applied to the skin.
  • composition thus provides a means whereby such active ingredients can be diluted, dispersed, conveyed to, and distributed on the skin surface at an appropriate concentration.
  • kits for skin care or treatment comprising: a vessel containing the inventive composition, optionally further comprising instructions on how to use the inventive composition.
  • the kit may contain multiple vessels containing different formulations of the inventive composition.
  • Such kits may have formulations which enable, for example, progressive treatment of a patient or patients, or which may be used, for example, on younger children.
  • not all of the formulations in a kit may be suitable for younger children.
  • a kit may contain formulations with progressively larger amounts of the active ingredient that are intended for children.
  • a kit may contain formulations with progressively larger amounts of the active ingredient that are intended for adults.
  • Embodiments of the inventive composition may also be embedded in a mask for the face or the body.
  • the mask may comprise a backing sheet containing the inventive composition serving to exert a specific action on the skin.
  • the backing sheet may be in a dry or web state, preferably stretchable at least in the wet state, in order to enable the mask to be adapted to fit the shape of the face or of the portion of the body to be treated.
  • the backing sheet may be made of paper, fabric, cloth, or a polymeric material.
  • aspects of the invention also provide a process for the preparation of a cosmetic composition for topical application to skin, the process comprising mixing an active ingredient, particularly types of retinoids as described herein, with a suitable vehicle to provide a retinoid concentration of from 0.01% to 2.0%.
  • compositions according to aspects of the invention can be formulated as liquids, for example as a lotion or milk for use in conjunction with an applicator such as a roll-ball applicator, or a spray device such as an aerosol can containing propellant, or a container fitted with a pump to dispense the liquid product.
  • an applicator such as a roll-ball applicator
  • a spray device such as an aerosol can containing propellant
  • a container fitted with a pump to dispense the liquid product.
  • the compositions according to aspects of the invention can be solid or semi-solid, for example sticks, creams or gels, for use in conjunction with a suitable applicator, or simply a tube, bottle or lidded jar, or as a liquid- impregnated fabric, such as a tissue wipe.
  • the composition may be an aqueous emulsion, such as a water- in-oil emulsion, or an oil-in-water emulsion.
  • the composition for the invention may be an aqueous fat emulsion in which the aqueous phase of the emulsion acts as a carrier.
  • the invention accordingly also includes a process of topical administration of the composition of the invention to human subjects suffering from or liable to suffer from excessively dry, fissured, eroded or otherwise damaged skin and other skin disorders.
  • the dosage rate will depend on the condition to be treated as well as the route of administration. Local skin symptoms may require one or more applications of the composition.
  • aspects of the invention provide for the use of an active ingredient, as herein defined, in the topical treatment of skin disorders.
  • the active ingredient is a retinoid.
  • compositions on the promotion or restoration of the skin barrier function may be evaluated by using experimental animal models or tested on human subjects.
  • Example 1 Lotion [0051] This example describes an embodiment of the compositions according to the invention, which may be used as a skin lotion. The ingredients are listed as follows.
  • Example 2 This example is largely the same as Example 1, except that the composition is a cream rather than a lotion.
  • Example 2 This example is largely the same as Example 1, except that the composition is a gel rather than a lotion.
  • Example 2 This example is largely the same as Example 1, except that the composition is a hydrogel rather than a lotion.
  • Example 5 Effects of Inventive Lotion on Human Subjects with Known Conditions
  • This example describes effects of the lotion formulation described in Example 1 on subjects with known skin conditions. All of the subjects used the formulation to address rosacea, rough skin texture, or redness in their faces. All of these conditions showed effects of skin aging.
  • Example 1 One subject experiencing erythema had been using another retinoid formulation, and experienced a limit in relief from the condition.
  • the subject was given the Example 1 formulation which was applied to the symptomatic areas twice a day over a period of 10 months. Analysis of skin condition after 10 months showed a marked decrease in skin redness, as would be expected with an increase in collagen production, both at the surface of the skin, as well as in the collagen cuff surrounding blood vessels.
  • Example 1 The same subject also was experiencing rosacea.
  • the Example 1 formulation was applied to the symptomatic areas twice a day over a period of nine months. Analysis of skin condition after nine months showed a marked improvement in pigmentation.
  • Example 1 Another subject who had skin texture issues was given the Example 1 formulation which was applied to the symptomatic areas twice a day over a period of four months. Analysis of skin condition after four months showed a marked improvement in skin smoothness.
  • Example 1 Another subject who had facial pigmentation issues was given the Example 1 formulation which was applied to the symptomatic areas twice a day over a period of three months. Analysis of skin condition after three months showed a marked improvement in skin pigmentation consistency.
  • Example 1 Another subject who had skin texture issues was given the Example 1 formulation which was applied to the symptomatic areas twice a day over a period of three months. Analysis of skin condition after three months showed a marked improvement in skin smoothness.

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Abstract

L'invention concerne des compositions, des kits et des procédés pour préserver la santé cutanée. En général, des rétinoïdes, conjointement avec des antioxydants, des émollients, des émulsifiants, un hydratant et un conservateur sont contenus dans un milieu physiologiquement acceptable. Les compositions, les kits et les procédés peuvent être utilisés en tant que produits cosmétiques, produits cosméceutiques ou produits pharmaceutiques pour atténuer les affections cutanées telles que l'acné, la rosacée, l'hyperpigmentation cutanée, l'amincissement cutané, le plissement, le jaunissement, la sécheresse, la rugosité, ou les changements cutanés précancéreux ou d'autres changements cutanés par photodéterrioration.
PCT/US2023/035622 2022-10-21 2023-10-20 Formulation de traitement de préservation de la santé cutanée WO2024086348A1 (fr)

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US202217970649A 2022-10-21 2022-10-21
US17/970,649 2022-10-21

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WO2024086348A1 true WO2024086348A1 (fr) 2024-04-25

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Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996007396A2 (fr) * 1994-09-07 1996-03-14 Johnson & Johnson Consumer Products, Inc. Compositions a base de retinoides
DE10115840A1 (de) * 2001-03-30 2002-10-10 Basf Ag Retinylcarbonate in Kosmetika und Dermatika
US20020197285A1 (en) * 2001-04-06 2002-12-26 Bonda Craig A. Diesters or polyesters of naphthalene dicarboxylic acid as solubilizer/stabilizer for retinoids
EP1743624A1 (fr) * 2005-07-12 2007-01-17 Johnson & Johnson Consumer France SAS Emulsion silicone-dans-eau comprenant des retionoides
DE102007059703A1 (de) * 2007-02-28 2008-09-04 Henkel Ag & Co. Kgaa Wirkstoff-stabiliserte O/W-Emulsionen II
EP2376198B1 (fr) * 2008-12-22 2018-03-28 Johnson & Johnson Consumer Holdings France Composition comprenant un rétinoïde et procédé de traitement de conditions de la peau
JP2020100576A (ja) * 2018-12-20 2020-07-02 小林製薬株式会社 皮膚外用組成物

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996007396A2 (fr) * 1994-09-07 1996-03-14 Johnson & Johnson Consumer Products, Inc. Compositions a base de retinoides
DE10115840A1 (de) * 2001-03-30 2002-10-10 Basf Ag Retinylcarbonate in Kosmetika und Dermatika
US20020197285A1 (en) * 2001-04-06 2002-12-26 Bonda Craig A. Diesters or polyesters of naphthalene dicarboxylic acid as solubilizer/stabilizer for retinoids
EP1743624A1 (fr) * 2005-07-12 2007-01-17 Johnson & Johnson Consumer France SAS Emulsion silicone-dans-eau comprenant des retionoides
DE102007059703A1 (de) * 2007-02-28 2008-09-04 Henkel Ag & Co. Kgaa Wirkstoff-stabiliserte O/W-Emulsionen II
EP2376198B1 (fr) * 2008-12-22 2018-03-28 Johnson & Johnson Consumer Holdings France Composition comprenant un rétinoïde et procédé de traitement de conditions de la peau
JP2020100576A (ja) * 2018-12-20 2020-07-02 小林製薬株式会社 皮膚外用組成物

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