Classifications

• • 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
  • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
  • A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
• • 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
• • 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
  • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
• • 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
  • A61P17/04—Antipruritics
• • 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
  • A61P17/16—Emollients or protectives, e.g. against radiation
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P37/00—Drugs for immunological or allergic disorders
  • A61P37/08—Antiallergic agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P39/00—General protective or antinoxious agents
  • A61P39/06—Free radical scavengers or antioxidants
• • 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
  • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
• • 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

• the present invention relates to methods for improving the aesthetic appearance of skin.
• the present invention further relates to methods of treating sensitive skin, methods of treating rosacea and/or telangiectasia, and methods of treating dermatological signs of aging.
• the present invention further relates the topical application of an effective amount of mangostin or an analog thereof.
• Cosmetic products which enhance the appearance of skin, are increasingly in demand. Consumers are interested in mitigating or delaying the signs of chronologically or hormonally aged or photo-aged skin, such as fine lines, wrinkles, drying, and sagging skin.
• the complexion of the skin i.e., the color and appearance of the skin, deteriorates slowly from aging and/or exposure to sunlight.
• Telangiectasia typically presents as superficial cutaneous capillaries near the surface of the skin having a bright red center portion and branching radiations. Such a skin condition is often called “spider veins.” When telangiectasia includes capillaries that are burst, leak blood or other fluids and/or become highly branched, the skin condition is commonly referred to as “broken capillaries.” Telangiectasia may be spurred by UV exposure, stress, environmental conditions, injury and/or general skin aging.
• U.S. Pat. No. 5,268,176 provides for treatment via repeated applications of a composition having inositol phosphoric acid or derivatives thereof.
• U.S. Pat. No. 5,698,206 provides for treatment via topical application of natural herbs in a carrier oil and concurrent ingestion of vitamin C.
• Mangostin has been employed in the prior art for a variety of purposes, but heretofore has not been employed to treat rosacea, telangiectasia, or aging skin.
• French Patent No. 2,754,447 relates to sunscreen compositions having mangostin.
• Japanese Patent Publication No. 10072357 relates to antiallergenic agents and foods having mangostin.
• the publication, Antimicrobial Activities of Chemical Constituents from Garcinia mangostana , J. Sci. Soc. Thailand (1986), 12(4), pages 239-43 relates to the use of mangostin and mangostin derivatives as antimicrobials.
• treating or “treat” as used in the present invention mean reduce, diminish, ameliorate, or prevent.
• To improve skin appearance means to partially or fully restore the normal appearance of the skin.
• Mangostin and its analogs are compounds that can be derived from natural sources (e.g., Garcinia mangostana L. , Guttiferae as described in Schmid, Ann. 93, 83 (1855)) and/or synthesized.
• R 1 , R 2 , R 3 and R 4 may, independently, be any of the following: a hydrogen atom; a carbohydrate; an acyl group, substituted or unsubstituted, straight-chain or branched, fully saturated or having one or more unsaturated bonds, that has from 1 to 22, preferably 1 to 18, and most preferably from 1 to 12, carbon atoms; an alkyl group, substituted or unsubstituted, straight-chain or branched, fully saturated or having one or more unsaturated bonds, that has from 1 to 22, preferably 1 to 18, and most preferably from 1 to 12, carbon atoms; an alkenyl group, substituted or unsubstituted, straight-chain or branched, fully saturated or having one or more unsaturated bonds, that has from 1 to 22, preferably from 1 to 18, and most preferably from 1 to 12 carbon atoms; an alkynyl group, substituted or unsubstituted, straight-chain or branched, fully saturated or having one or
• Suitable carbohydrates include but are not limited to glucose, lactose, fructose, rhamnose, trehalose, or fucose. Glucose and fucose are preferred carbohydrates.
• at least two of R 1 , R 2 , R 3 and R 4 are hydrogen atoms.
• R 1 is an alkyl group or acyl group having from 1 to 12 carbon atoms and R 2 , R 3 and R 4 are each hydrogen atoms.
• Mangostin has the chemical name of 1,3,6-trihydroxy-7-methoxy-2,8-di(3-methyl-2-butenyl)xanthone or, alternately, 1,3,6-trihydroxy-7-methoxy-2,9-bis(3-methyl-2-butenyl)-9H-xanthen-9-one.
• the physical properties of mangostin are set forth in The Merck Index, 10 th Edition (1983), page 818, which is incorporated herein by reference.
• Analogs of mangostin can be derived from plant or natural sources or be prepared via conventional organic synthesis is procedures such catalytic esterification, ethoxylation, and etherification.
• Such analogs include the following: alpha mangostin, beta mangostin, bicyclomangostin, gamma mangostin, 3-O-methylmangostin, mangostin triacetate, and mangostin-3,6-di-O-glucoside.
• mangostin and/or its analogs can be topically applied without a vehicle, i.e. in an amount 100 percent by weight (wt %). More preferably, mangostin and/or its analogs are admixed with a vehicle suitable to form a composition for topical application.
• the composition preferably has about 0.0001 wt % to less than 100 wt %, more preferably about 0.0001 wt % to about 90 wt %, still more preferably about 0.01 wt % to about 50 wt %, and most preferably about 0.5 wt % to about 20 wt %, of mangostin and/or its analogs based on the total weight of the composition.
• mangostin and/or its analogs can be used to improve the overall appearance of the skin and treat sensitive skin.
• Treatable skin conditions include itch, irritation, inflammation, loss of tone (e.g., sagging and/or uneven color), redness, allergic responses, combination (oil/dry/unbalanced) skin, blemishes, flushing and blushing.
• mangostin and/or its analogs can be used to treat dermatological signs of aging due to, for example, chronological aging, hormonal aging and/or photoaging.
• signs of aging include, but are not limited to, skin fragility; loss of collagen and/or elastin; skin atrophy; appearance and/or depth of lines and/or wrinkles including fine lines; skin discoloration including dark eye circles; skin sagging; skin fatigue and/or stress, e.g., skin breakout due to environmental stress, such as pollution and/or temperature changes; loss of skin tone, clarity or luster; loss of skin firmness; poor skin texture; loss of skin elasticity and/or resiliency; and thin skin.
• compositions of the present invention can be effectively applied daily for about 1, 2 or 4 weeks, or more. Preferably, the compositions are applied daily for about 2 weeks.
• compositions useful in the present method can be formulated in any suitable product form.
• product forms include, but are not limited to, aerosol spray, cream, dispersion, foam, gel, lotion, mask, mousse, ointment, powder, patch, pomade, solution, pump spray, stick, tape and towelette.
• compositions useful in the present method can include a vehicle that is pharmaceutically or cosmetically acceptable.
• vehicles include, but are not limited to, one or more C 1-4 alcohols, fatty alcohols, fatty ethers, fatty esters, polyols, glycols, vegetable oils, mineral oils, liposomes, laminar lipid materials, silicone oils, water, or any combinations thereof.
• compositions useful in the present method can include one or more of the following additional ingredients: amino acids, anesthetics, anti-acne agents, anti-allergenics, antifungals, antimicrobials, anti-inflammatory agents, anti-irritants, antineoplastics, antioxidants, antiseptics, antivirals, chelating agents, colorants, depigmenting agents, emollients, emulsifiers, exfollients such as oxa acids and alpha and beta hydroxy acids, film formers, fragrances, humectants, hypopigmenting agents, immune system boosting agents, immune system suppressing agents, insect repellents, lubricants, moisturizers, pharmaceutical agents, photostabilizing agents, preservatives, retinoids, skin protectants, skin penetration enhancers, staining agents, sunscreens, stabilizers, surfactants, thickeners, viscosity and/or rheology modifiers, vitamins, or any combinations thereof.
• additional ingredients amino acids, anesthetic
• Oil-in-Water Emulsion wt % Humectant e.g. Glycols, Glycerols
• Thickeners e.g. Gums, Starches, Polymers
• Chelants e.g. Disodium EDTA, Tetrasodium EDTA
• Sunscreen e.g.
• Parsol 1789 TM 0.1-50 ethylhexylmethoxycinnamate, benzophenone-3) Silicone 0.1-15 Silica 0.01-10 Extracts (e.g., one or more of 0.0001-50 Pomegranate extract, Neem Seed Cell Broth, Grape Seed Extract, Salvia Miltiorrhiza Extract, Iris Florentina Root Extract, Carrot Extract, Cucumber Extract, White Birch (Betula Alba) Bark Extract, Rosemary Extract, Algae Extract, or any combination) Fatty alcohol/Emulsifers/Wax/Fatty acid 0.5-15 (e.g.
• Emulsion Stabilizers/Viscosity Modifiers 0.1-20 e.g. acrylates/C 10-30 alkyl acrylate crosspolymer, acrylate/aminoacrylates/ C 10-30 alkyl PEG-20 itaconate, sodium acrylate/ acryloyldimethyl taurate copolymer, acrylates/C 10-30 alkyl acrylate crosspolymer Film Formers (e.g.
• decene/butene copolymer 0.001-2 acrylates/octylacrylamide copolymer, adipic acid/diethylene glycol/ glycerin crosspolymer)
• Emollients 0.1-20 Mangostin 0.5-20 Demineralized Water Q.S.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Dermatology (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Organic Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Gerontology & Geriatric Medicine (AREA)
• Epidemiology (AREA)
• Toxicology (AREA)
• Birds (AREA)
• Immunology (AREA)
• Pulmonology (AREA)
• Rheumatology (AREA)
• Pain & Pain Management (AREA)
• Biochemistry (AREA)
• Cosmetics (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Tires In General (AREA)
• Medicines Containing Material From Animals Or Micro-Organisms (AREA)
• Medicinal Preparation (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicines Containing Plant Substances (AREA)

Priority Applications (14)

Applications Claiming Priority (1)

Related Child Applications (1)

Publications (1)

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Cited By (7)

Families Citing this family (9)

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• 2001
  • 2001-12-27 US US10/033,169 patent/US20030138467A1/en not_active Abandoned
• 2002
  • 2002-12-12 AT AT02795837T patent/ATE473729T1/de not_active IP Right Cessation
  • 2002-12-12 CA CA2471657A patent/CA2471657C/fr not_active Expired - Fee Related
  • 2002-12-12 WO PCT/US2002/039734 patent/WO2003057141A2/fr active IP Right Grant
  • 2002-12-12 PL PL02369453A patent/PL369453A1/xx not_active Application Discontinuation
  • 2002-12-12 JP JP2003557500A patent/JP2005518399A/ja active Pending
  • 2002-12-12 CN CNA028261690A patent/CN1607932A/zh active Pending
  • 2002-12-12 DE DE60237039T patent/DE60237039D1/de not_active Expired - Lifetime
  • 2002-12-12 EP EP02795837A patent/EP1465577B1/fr not_active Expired - Lifetime
  • 2002-12-12 BR BRPI0215362-9A patent/BR0215362A/pt not_active Application Discontinuation
  • 2002-12-12 AU AU2002360571A patent/AU2002360571B2/en not_active Ceased
• 2004
  • 2004-06-23 MX MXPA04006229A patent/MXPA04006229A/es active IP Right Grant
  • 2004-12-30 US US11/026,198 patent/US7825157B2/en not_active Expired - Fee Related
• 2005
  • 2005-04-06 HK HK05102866.2A patent/HK1070004A1/xx not_active IP Right Cessation

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