EP3709955A1 - Topische zusammensetzungen - Google Patents

Topische zusammensetzungen

Info

Publication number
EP3709955A1
EP3709955A1 EP18800091.3A EP18800091A EP3709955A1 EP 3709955 A1 EP3709955 A1 EP 3709955A1 EP 18800091 A EP18800091 A EP 18800091A EP 3709955 A1 EP3709955 A1 EP 3709955A1
Authority
EP
European Patent Office
Prior art keywords
range
phytantriol
topical composition
glyceryl caprylate
skin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP18800091.3A
Other languages
English (en)
French (fr)
Inventor
Christine Mendrok-Edinger
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
DSM IP Assets BV
Original Assignee
DSM IP Assets BV
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by DSM IP Assets BV filed Critical DSM IP Assets BV
Publication of EP3709955A1 publication Critical patent/EP3709955A1/de
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37Esters of carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/30Characterized by the absence of a particular group of ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52Stabilizers
    • A61K2800/524Preservatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59Mixtures
    • A61K2800/592Mixtures of compounds complementing their respective functions
    • A61K2800/5922At least two compounds being classified in the same subclass of A61K8/18

Definitions

  • the present invention relates to topical compositions comprising phytantriol and glyceryl caprylate, characterized in that the composition is free of phenoxyethanol as well as to the use of phytantriol in combination with glyceryl caprylate for the prevention and/or treatment of ailments associated with Propionibacterium acnes and to prevent microbial decay of cosmetic products.
  • preservatives To protect cosmetic compositions, household products, plastics, paper and / or paints against mold and bacteria, most products currently on the market contain preservatives. While these preservatives protect against bacteria and fungi, studies have linked daily exposure to many of these substances to an increased risk of skin irritation, cancer and / or endocrine problems. Thus, many manufactures are searching for alternative antimicrobial actives which allow reducing the amount of preservatives and don’t appear to pose any health risks.
  • Antimicrobial active compounds furthermore play a key role for many cosmetic applications:
  • Acne is taken to mean a skin disorder which is evident in inflamed papules, pustules or nodules, caused by increased talc production and impaired keratinization of the skin.
  • the inflammation may be associated with reddening, swelling and pressure pain.
  • possible causes of acne formation can be androgens, comedogenic substances (for example in cosmetics), smoking, stress or excessive colonization of the skin by bacteria.
  • Acne is in particular triggered by the microorganism Propionibacterium acnes (P. acnes), which is a bacterium which usually colonizes the skin and lives on sebum. Acne may arise, for example, if the number of these bacteria is increased.
  • Topical antibiotics which have been utilized to attempt to inhibit the overgrowth of P. acnes are clindamycin, erythromycin, tetracycline, and metronidazole. Each of these topical antibiotics reportedly cause side effects and widespread use also contributes to the risk of bacterial resistance.
  • Phenoxyethanol is used as an anti-bacterial in cosmetics but can have significant adverse effects. Thus, there is an ongoing need to replace phenoxyethanol for the treatment of acne with other well accepted cosmetic ingredients.
  • the combination of phytantriol and glyceryl caprylate shows a synergistic antimicrobial effect against P. acnes.
  • the combination can effectively be used in cosmetic compositions which are free of any phenoxyethanol to control the P. acnes on the skin and / or the scalp and thus overcome the adverse effects resulting from a P. acnes overpopulation on the skin and / or scalp such the treatment of inflammation triggered by P. acnes, red nodules or pustules.
  • the present invention relates to topical compositions comprising phytantriol and glyceryl caprylate with the proviso that the composition does not contain any phenoxyethanol.
  • the invention relates to a combination of phytantriol and glyceryl caprylate as antimicrobial agent against P. acnes.
  • the invention relates to a method for killing and / or inhibiting P. acnes, said method comprising contacting P. acnes with a combination of phytantriol and glyceryl caprylate.
  • the combination of phytantriol and glyceryl caprylate is further suitable for the treatment of any adverse skin condition associated with an overpopulation of P. acnes by maintaining a healthy skin homeostasis and / or improving the health of the skin microbiome.
  • the invention also relates to a method of treating the skin and / or the scalp, said method comprising the steps of contacting the skin and / or scalp with a topical composition according to the present invention for the treatment, prevention and/or prophylaxis of acne as well as for maintaining a healthy skin homeostasis and / or skin microbiome balance.
  • the present invention relates to the use of a topical composition according to the present invention for the treatment, prevention and/or prophylaxis of acne as well as for maintaining skin homeostasis and / or skin microbiome balance.
  • Phytantriol [CAS: 74563-64-7] is a colourless to light yellow, viscous liquid with the chemical name 3,7,1 1 ,15-tetramethyl-hexadecane-1 ,2,3-triol. Phytantriol is e.g. commercially available at DSM Nutritional Products Ltd, Kaiseraugst.
  • Glyceryl caprylate [26402-26-6] is e.g. commercially available as Dermosoft GMCY at Dr. Straetmann.
  • antimicrobial activity means a capability of killing and/or inhibiting the growth of microbial cells such as in particular P. acnes.
  • the topical compositions preferably comprise phytantriol in an amount selected in the range of about 0.005 to 5 wt.-%, more preferably in the range of about 0.01 to 3 wt.-% and most preferably in the range of 0.025 to 2 wt.-%, such as in an amount of 0.04 to 1.5 wt.-% and particularly advantageous in an amount of 0.04 to 1 wt.-%, based on the total weight of the composition.
  • the topical compositions preferably comprise the glyceryl caprylate in an amount selected in the range of about 0.01 to about 2 wt.-%, preferably in the range of 0.05 to 1.5 wt.-%, most preferably in the range of 0.1 to 1 wt.-%, based on the total weight of the composition.
  • the ratio (w/w) of phytantriol to glyceryl caprylate in all embodiments of the present invention is preferably selected in the range of 5: 1 to 1 :5, such as in the range of 2.5:1 to 1 :2.5, such as most preferable in the range of about 1 :1.
  • the anti-microbial activity of the combination of phytantriol and glyceryl caprylate can be used in a multiplicity of formulations or applications, such as, for example, topical compositions, medicinal products or household products, also for preservation purposes.
  • the invention relates to a method of preventing microbial decay and breakdown of topical compositions according to the present invention, wherein said method comprises adding to the compositions phytantriol in combination with glyceryl caprylate, even more preferably further in combination with propanediol as an antimicrobial agent.
  • the method also encompasses the step of appreciating the result.
  • the invention also relates to a method of preserving the topical composition according to the present invention against microbiological contamination or growth, wherein said method comprises adding to the compositions, phytantriol in combination with glyceryl caprylate, even more preferably further in combination with propanediol.
  • the method also encompasses the step of appreciating the result.
  • the compositions next to being isopropylparabene and / or phenoxyethanol free, the compositions also advantageously do not contain isobutylparaben, phenylparaben, benzylparaben and / or pentylparaben. Most preferably in all embodiments of the present invention, the compositions contain no parabenes at all, i.e. no methylparaben, ethylparaben, isopropylparabene, isobutylparaben, phenylparaben, benzylparaben and pentylparaben.
  • the present invention relates to method for preserving a topical composition according to the present invention, wherein the formulation is free of isopropylparabene, preferably of any parabenes, said method comprising incorporating into the composition phytantriol and glyceryl caprylate, even more preferably in combination with propanediol.
  • the method also encompasses the step of appreciating the result.
  • the invention relates to a method of preventing microbial decay and breakdown of topical compositions as outlined herein which compositions furthermore comprise water and at least one further agent selected from the group consisting of surfactants, emulsifiers, thickeners, and oils as such compositions are particular sensitive to microbial growth.
  • the compositions do not exhibit a microbial contamination exceeding the initial contamination rate with at least one microorganism in a period of at least 7 days, more preferably of at least 14 days, most preferably of at least 28 days, (assessed according ISO 1 1930). Even more preferably, the number (i.e. Colony Forming Unit, CFU) of at least one bacteria or mold, such as in particular Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and / or Candida albicans is significantly reduced.
  • CFU Colony Forming Unit
  • Propanediol [CAS: 504-63-2] is e.g. commercially available as ZEMEA from DuPont Tate & Lyle Bio Products Company, LLC.
  • the topical compositions preferably comprise the propanediol in an amount selected in the range of about 0.01 to about 10 wt.-%, preferably in the range of 0.5 to 7.5 wt.-%, most preferably in the range of 1 to 5 wt.-%, based on the total weight of the composition.
  • the amount of propanediol used in the compositions is higher than the sum of the amounts of phytantriol and glyceryl caprylate, preferably at least two times higher, more preferably at least 3 times higher.
  • the use according to the invention of the combination of phytantriol and glyceryl caprylate and optionally propanediol can take place both in the cosmetic sense as well as in the pharmaceutical sense.
  • a pharmaceutical application is conceivable, for example, in the case of specific anti-acne compositions.
  • the use is however preferably cosmetic (non-therapeutic) such as for maintenance of skin homeostasis and/ or balancing the skin microbiome.
  • compositions according to the present invention are preferably cosmetic or pharmaceutical compositions which are topically applied to mammalian keratinous tissue such as in particular to human skin or the human scalp and hair.
  • cosmetic composition refers to cosmetic compositions as defined under the heading "Kosmetika” in Rompp Lexikon Chemie, 10th edition 1997, Georg Thieme Verlag Stuttgart, New York as well as to cosmetic compositions as disclosed in A. Domsch, "Cosmetic Compositions", Verlag fOr chemische Industrie (ed. H. Ziolkowsky), 4 th edition, 1992.
  • the cosmetic or pharmaceutical compositions according to the present invention preferably further comprise a physiologically acceptable medium, that is to say a medium compatible with keratinous substances, such as the skin, mucosa, and keratinous fibers.
  • a physiologically acceptable medium is a cosmetically or pharmaceutically acceptable carrier.
  • cosmetically or pharmaceutically acceptable carrier refers to all carriers and/or excipients and/ or diluents conventionally used in cosmetic compositions.
  • the topical compositions according to the present invention are generally prepared by admixing phytantriol and glyceryl caprylate in the amounts indicated herein with a suitable carrier.
  • carrier e.g., other active ingredients
  • the cosmetic or pharmaceutical compositions according to the present invention comprise from about 50% to about 99%, preferably from about 60% to about 98%, more preferably from about 70% to about 98%, such as in particular from about 80% to about 95% of a carrier, based on the total weight of the cosmetic composition.
  • the carrier consists furthermore of at least 40 wt.-%, more preferably of at least 50 wt.-%, most preferably of at least 55 wt.-% of water, such as in particular of about 55 to about 90 wt.-% of water.
  • compositions of the invention may comprise conventional adjuvants and additives, such as preservatives/antioxidants, fatty substances/oils, organic solvents, silicones, thickeners, softeners, emulsifiers, antifoaming agents, aesthetic components such as fragrances, surfactants, fillers, anionic, cationic, nonionic or amphoteric polymers or mixtures thereof, propellants, acidifying or basifying agents, dyes, colorings/colorants, abrasives, absorbents, chelating agents and / or sequestering agents, essential oils, skin sensates, astringents, pigments or any other ingredients usually formulated into such compositions.
  • adjuvants and additives such as preservatives/antioxidants, fatty substances/oils, organic solvents, silicones, thickeners, softeners, emulsifiers, antifoaming agents, aesthetic components such as fragrances, surfactants, fillers, anionic, cationic, nonionic or amphoter
  • compositions according to the invention may also comprise further cosmetically active ingredients conventionally used in cosmetic or pharmaceutical compositions.
  • active ingredients encompass skin lightening agents; UV-filters, agents for the treatment of hyperpigmentation; agents for the prevention or reduction of inflammation; firming, moisturizing, soothing, and / or energizing agents as well as agents to improve elasticity and skin barrier.
  • cosmetic excipients examples include cosmetic excipients, diluents, adjuvants, additives as well as active ingredients commonly used in the skin care industry which are suitable for use in the cosmetic compositions of the present invention are for example described in the International Cosmetic Ingredient Dictionary & Handbook by Personal Care Product Council (http://www.personalcarecouncil.org/), accessible by the online INFO BASE (http://online.personalcarecouncil.org/jsp/Home.jsp), without being limited thereto.
  • the necessary amounts of the active ingredients as well as the excipients, diluents, adjuvants, additives etc. can, based on the desired product form and application, easily be determined by the skilled person.
  • the additional ingredients can either be added to the oily phase, the aqueous phase or separately as deemed appropriate.
  • the cosmetically active ingredients useful herein can in some instances provide more than one benefit or operate via more than one mode of action.
  • the cosmetic or pharmaceutical compositions according to the invention are in the form of a suspension or dispersion in solvents or fatty substances, or alternatively in the form of an emulsion or micro emulsion (in particular of 0/W- or W/O-type), PIT-emulsion, nano emulsion, multiple emulsion (e. g. O/W/O- or W/O/W- type), pickering emulsion, hydrogel, lipogel, one- or multiphase solution or vesicular dispersion.
  • an emulsion or micro emulsion in particular of 0/W- or W/O-type
  • PIT-emulsion nano emulsion
  • multiple emulsion e. g. O/W/O- or W/O/W- type
  • pickering emulsion hydrogel, lipogel, one- or multiphase solution or vesicular dispersion.
  • the cosmetic or pharmaceutical compositions in accordance with the invention can be in the form of a liquid, lotion, a thickened lotion, a gel, a cream, a milk, an ointment or a paste.
  • the cosmetic or pharmaceutical compositions according to the invention have a pH in the range of 3-10, preferably in the range of pH of 3-8, most preferred in the range of pH 3-7.5.
  • the pH is adjusted by methods known to a person skilled in the art, e.g. by using an acid such as a hydroxy acid including glycolic acid, lactic acid, malic acid, citric acid and tartaric acid or a base such as e.g. sodium or potassium hydroxide or ammonium hydroxide as well as mixtures thereof.
  • the acid if present, is used in an amount of at least 0.0001 wt.-%, such as e.g. in an amount of 0.01 -1 wt.-%, in particular in an amount of 0.01 to 0.5 wt.-%.
  • the cosmetic compositions according to the present invention advantageously comprise an additional preservative.
  • suitable preservatives in all embodiments of the present invention are benzoic acid, sodium benzoate, sorbic acid, potasssium sorbate, dehydroacetic acid, alcohol, alcohol denat.; as well as mixtures thereof.
  • the preservative is preferably used in an amount of 0.01 to 2 wt.-%, more preferably in an amount of 0.05 to 1.5 wt.-%, most preferably in an amount of 0.1 to 1.0 wt.-%, based on the total weight of the composition.
  • compositions according to the present invention may comprise an additional amount of a preservation booster such as hydroxyacetophenone, caprylyl glycol, pentylene glycol, 1 ,2 hexanediol, decylene glycol, monoglycerides such as glyceryl laurate, propylene glycol caprylate, propylene glycol heptanoate as well as mixtures thereof.
  • a preservation booster such as hydroxyacetophenone, caprylyl glycol, pentylene glycol, 1 ,2 hexanediol, decylene glycol, monoglycerides such as glyceryl laurate, propylene glycol caprylate, propylene glycol heptanoate as well as mixtures thereof.
  • the preservation booster is preferably used in an amount of 0.01 to 2 wt.-%, more preferably in an amount of 0.05 to 1.5 wt.-%, most preferably in an amount of 0.1 to 1.0 wt.-%, based on the total weight of the composition.
  • the cosmetic compositions according to the present invention are in particular skin care preparations, functional preparations and / or hair care preparations such as most in particularly skin or hair care preparations.
  • Examples of skin care preparations are, in particular, light protective preparations (sunscreen preparations), anti-ageing preparations, preparations for the treatment of photo-ageing, body oils, body lotions, body gels, treatment creams, skin protection ointments, moisturizing preparations such as moisturizing gels or moisturizing sprays, face and/or body moisturizers, as well as skin lightening preparations.
  • light protective preparations unsunscreen preparations
  • anti-ageing preparations preparations for the treatment of photo-ageing
  • body oils body lotions, body gels, treatment creams, skin protection ointments
  • moisturizing preparations such as moisturizing gels or moisturizing sprays
  • face and/or body moisturizers as well as skin lightening preparations.
  • Examples of functional preparations are cosmetic compositions containing active ingredients such as hormone preparations, vitamin preparations, vegetable extract preparations, anti-ageing preparations, and/or antimicrobial (antibacterial or antifungal) preparations without being limited thereto.
  • Examples of hair care preparations which are suitable according to the invention and which may be mentioned are shampoos, hair conditioners (also referred to as hair rinses, hairdressing compositions, hair tonics, hair regenerating compositions, hair lotions, water wave lotions, hair sprays, hair creams, hair gels, hair oils, hair pomades or hair brilliantines. Accordingly, these are always preparations which are applied to the hair and the scalp for a shorter or longer time depending on the actual purpose for which they are used.
  • the hair care preparations according to the invention are supplied as shampoos, these can be clear liquids, opaque liquids (with pearly luster effect), in cream form, gel-like or else in powder form or in tablet form, and as aerosols.
  • the surfactant raw materials on which these shampoos are based can be anionic, cationic, nonionic and amphoteric in nature and also be present in combinations of these substances.
  • anionic surfactants suitable for the incorporation into the shampoo preparations according to the present invention are C 10-20 alkyl- and alkylenecarboxylates, alkyl ether carboxylates, fatty alcohol sulfates, fatty alcohol ether sulfates, alkylolamide sulfates and sulfonates, fatty acid alkylolamide polyglycol ether sulfates, alkanesulfonates and hydroxyalkanesulfonates, olefinsulfonates, acyl esters of isothionates, alpha-sulfo fatty acid esters, alkylbenzenesulfonates, alkylphenol glycol ether sulfonates, sulfosuccinates, sulfosuccinic monoesters and diesters, fatty alcohol ether phosphates, protein-fatty acid condensation products, alkyl monoglyceride sulfates and sulfon
  • Suitable cationic surfactants are quaternary ammonium salts such as di(Cio--C 24 alkyl)dimethylammonium chloride or bromide, preferably di (Ci 2 -Ci 8 alkyl)- dimethylammonium chloride or bromide; Cio-C 24 -alkyldimethylethylammonium chloride or bromide; Cio-C 24 -alkyltrimethylammonium chloride or bromide, preferably cetyltrimethylammonium chloride or bromide and C 2 o-C 24 -alkyltrimethylammonium chloride or bromide; C 10 -C 24 4 -alkyldimethylbenzylammonium chloride or bromide, preferably Ci 2 -Ci 8 -alkyldime methylbenzylammoniumchloride; N-(Ci 2 -Cie- alkyl)pyridinium chloride or bromide, preferably N- (C
  • Suitable nonionic surfactants which can be used as detergent substances are fatty alcohol ethoxylates (alkylpolyethylene glycols); alkylphenol polyethylene glycols; alkyl mercaptan polyethylene glycols; fattyamine ethoxylates (alkylaminopolyethylene glycols); fatty acid ethoxylates (acylpolyethylene glycols); polypropylene glycol ethoxylates (Pluronic); fatty acid alkylolamides (fatty acid amide polyethylene glycols); sucrose esters; sorbitol esters and polyglycol ether.
  • fatty alcohol ethoxylates alkylpolyethylene glycols
  • alkylphenol polyethylene glycols alkyl mercaptan polyethylene glycols
  • fattyamine ethoxylates alkylaminopolyethylene glycols
  • fatty acid ethoxylates acylpolyethylene glycols
  • Pluronic fatty
  • amphoteric surfactants which can be added to the shampoos are N- (Ci 2 -Ci 8 -alkyl)-.beta.-aminopropionates and N-(Ci 2 -Ci 8 -alkyl)-.beta.- iminodipropionates as alkali metal and mono-, di- and trialkylammonium salts; N- acylamidoalkyl-N,N-dimethylacetobetaine, preferably N-(C8-Ci8-acyl)amidopropyl-N, N-dimethylacetobetaine; Ci 2 -Ci 8 -alkyldimethylsulfopropylbetaine; amphoteric surfactants based on imidazoline (commercial name: Miranol ® , Steinapon ® ), preferably the sodium salt of 1 -(p-carboxymethyloxyethyl)-1-(carboxymethyl)-2- laurylimi
  • the hair care preparations according to the invention can additionally contain further additives customary in hair care such as for example perfumes, colorants, also those which simultaneously dye or tint the hair, solvents, opacifying agents and pearly luster agents, for example esters of fatty acids with polyols, magnesium and zinc salts of fatty acids, dispersions based on copolymers, thickening agents such as sodium, potassium and ammonium chloride, sodium sulfate, fatty acid alkylolamides, cellulose derivatives, natural rubbers, also plant extracts, protein derivatives such as gelatin, collagen hydrolysates, polypeptides with a natural or synthetic basis, egg yolk, lecithin, lanolin and lanolin derivatives, fats, oils, fatty alcohols, silicones, deodorizing agents, substances with antimicrobial activity, substances with antiseborrhoeic activity, substances with keratolytic and keratoplastic effect, such as, for example, sulfur, salicylic acid and enzymes as well as further
  • the topical cosmetic compositions according to the present invention are advantageously O/W emulsions, W/O emulsions and / or gels such as shower gels.
  • topical compositions in the form of O/W emulsions, W/O emulsions and / or gels according to the present invention are skin care preparation intended for the treatment of acne or for maintaining a healthy skin homeostasis and / or for maintaining skin microbiome balance.
  • O/W emulsions according to the present invention advantageously comprise (i) phytantriol in an amount selected in the range of about 0.01 to 3 wt.-%, preferably in the range of 0.025 to 2 wt.-%, most preferably in the range of 0.04 to 1.5 wt.-%, based on the total weight of the composition, (ii) glyceryl caprylate in an amount selected in the range of about 0.01 to about 2 wt.-%, preferably in the range of 0.05 to 1 .
  • one or more synthetic polymers may be used as an emulsifier such as for example, PVP eicosene copolymer, acrylates/C 10-3o alkyl acrylate crosspolymer, acrylates/steareth-20 methacrylate copolymer, PEG-22/dodecyl glycol copolymer, PEG-45/dodecyl glycol copolymer, and mixtures thereof.
  • PVP eicosene copolymer acrylates/C 10-3o alkyl acrylate crosspolymer
  • acrylates/steareth-20 methacrylate copolymer acrylates/steareth-20 methacrylate copolymer
  • PEG-22/dodecyl glycol copolymer PEG-45/dodecyl glycol copolymer, and mixtures thereof.
  • the O/W-emulsifier is selected from the group of cetyl phosphates such as in particular potassium cetyl phosphate (commercially available as Amphisol® K), glyceryl stearate (and) PEG 100 stearate (commercially available as Arlacel® 165) and/ or polyalkylenglycolether such as in particular laureth-35 (lauryl alcohol with 35 EO units; commercially available as Brij® 35).
  • the at least one O/W emulsifier is preferably used in an amount of about 0.001 to 10 wt.-%, more preferably in an amount of 0.1 to 7 wt.-% with respect to the total weigh of the composition.
  • the cosmetic composition in the form of a O/W emulsion contains advantageously at least one co emulsifier selected from the list of alkyl alcohols such as Cetyl Alcohol (Lorol C16, Lanette 16) Cetearyl Alcohol (Lanette® O), Stearyl Alcohol (Lanette® 18), Behenyl Alcohol (Lanette® 22), Glyceryl Monostearate, Glyceryl Myristate (Estol® 3650), Hydrogenated Coco- Glycerides (Lipocire Na10) without being limited to this and mixtures thereof.
  • alkyl alcohols such as Cetyl Alcohol (Lorol C16, Lanette 16) Cetearyl Alcohol (Lanette® O), Stearyl Alcohol (Lanette® 18), Behenyl Alcohol (Lanette® 22), Glyceryl Monostearate, Glyceryl Myristate (Estol® 3650), Hydrogenated Coco- Glycerides (Lipocire Na10) without being limited to this and mixtures thereof.
  • the O/W emulsion in addition comprises propanediol selected in an amount of 0.01 to about 10 wt.-%, preferably in the range of 0.5 to 7.5 wt.-%, most preferably in the range of 1 to 5 wt.-%, based on the total weight of the composition.
  • W/O emulsions according to the present invention advantageously comprise (i) phytantriol in an amount selected in the range 0.01 to 3 wt.-%, preferably in the range of 0.025 to 2 wt.-%, most preferably in the range of 0.04 to 1.5 wt.-%, based on the total weight of the composition, (ii) glyceryl caprylate in an amount selected in the range of about 0.01 to about 2 wt.-%, preferably in the range of 0.05 to 1 .
  • W/Si- emulsifiers are Lauryl Polyglyceryl-3 Polydimethylsiloxyethyl Dimethicone and/or PEG-9 Polydimethylsiloxyethyl Dimethicone and/or Cetyl PEG/PPG-10/1 Dimethicone and/or PEG-12 Dimethicone Crosspolymer and/or PEG/PPG-18/18 Dimethicone.
  • the at least one W/O emulsifier is preferably used in an amount of about 0.001 to 10 wt.-%, more preferably in an amount of 0.2 to 7 wt.-% with respect to the total weigh of the composition.
  • the W/O emulsion in addition comprises propanediol selected in an amount of 0.01 to about 10 wt.-%, preferably in the range of 0.5 to 7.5 wt.-%, most preferably in the range of 1 to 5 wt- %, based on the total weight of the composition.
  • Gel preparations according to the present invention advantageously comprise (i) phytantriol in an amount selected in the range of 0.01 to 3 wt.-%, preferably in the range of 0.025 to 2 wt.-%, most preferably in the range of 0.04 to 1.5 wt.-%, based on the total weight of the composition, (ii) glyceryl caprylate in an amount selected in the range of about 0.01 to about 2 wt.-%, preferably in the range of 0.05 to 1 . 5 wt.-%, most preferably in the range of 0.1 to 1 wt.-%, based on the total weight of the composition, (iii) water and (iv) at least one water soluble thickener.
  • Such water- soluble thickeners are well known to a person skilled in the art and are e.g. listed in the "Handbook of Water soluble gums and resins" by Robert L. Davidson (Me Graw Hill Book Company (1980)).
  • Particularly suitable water soluble thickeners are selected from the group consisting of polyacrylic acids (e.g. commercially available under the tradename Carbomer or Carbopol ® ), homopolymers of 2-Acrylamido-2- methylpropansulfonic acid (e.g. commercially available as Rheothik ® 1 1-80), acrylate copolymers (e.g.
  • the water-soluble thickener is used in an amount of about 0.001 to 10 wt.- %, more preferably in an amount of 0.2 to 7 wt.-%, based on the total weigh of the composition.
  • the gel preparation in addition comprises propanediol selected in an amount of 0.01 to about 10 wt.-%, preferably in the range of 0.5 to 7.5 wt.-%, most preferably in the range of 1 to 5 wt.-%, based on the total weight of the composition.
  • the topical compositions according to the present invention furthermore comprise glycerin in an amount selected in the range of 0.1 to 15 wt.-%, preferably in the range of 0.5 to 10 wt.-%, most preferably in the range of 1 to 5 wt.-%, based on the total weight of the composition.
  • the topical compositions according to the present invention furthermore comprise xanthan gum as thickener in an amount selected in the range of 0.001 to 2 wt.-%, preferably in the range of 0.01 to 1 wt.-%, most preferably in the range of 0.1 to 0.5 wt.-%, based on the total weight of the composition.
  • xanthan gum as thickener in an amount selected in the range of 0.001 to 2 wt.-%, preferably in the range of 0.01 to 1 wt.-%, most preferably in the range of 0.1 to 0.5 wt.-%, based on the total weight of the composition.
  • solutions of the respective active(s) in ethanol are prepared and further dissolved in physiological serum with 0.85 wt.-% NaCI in the concentrations as outlined in table 1 under sterile conditions.
  • Samples containing phytantriol were solubilized in physiological serum supplemented with 10 wt.-% ethanol, samples containing glyceryl caprylate only were solubilized in physiological serum supplemented with 1 wt.-% ethanol.
  • the solutions of the active(s) were deposed in 96-deep well plates (1.6 ml/well).
  • the wells are contaminated with the Propionibacterium acnes at 2.5*10 5 to 5.6*10 5 cfu/ml to obtain the initial contamination as outlined in table 1. After the contamination, each well was thoroughly mixed to ensure a homogeneous distribution of Propionibacterium acnes. Then each plate was incubated at 22°C for 24h. The counting of the (remaining) population is carried out 24h after contamination.
  • the combination of phytantriol and glyceryl caprylate is suitable to suppress microbial growth in a typical cosmetic formulation, which effect is further enhanced by the addition of propanediol.

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  • Pharmacology & Pharmacy (AREA)
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EP18800091.3A 2017-11-16 2018-11-07 Topische zusammensetzungen Pending EP3709955A1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17202147 2017-11-16
PCT/EP2018/080386 WO2019096635A1 (en) 2017-11-16 2018-11-07 Topical compositions

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Publication number Priority date Publication date Assignee Title
EP3970803A1 (de) * 2020-09-22 2022-03-23 Beiersdorf AG Kosmetische zusammensetzung mit geringer osmolalität
WO2023242006A1 (en) * 2022-06-15 2023-12-21 Dsm Ip Assets B.V. Use of uv filters for the treatment of acne

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Publication number Priority date Publication date Assignee Title
US6284234B1 (en) * 1998-08-04 2001-09-04 Johnson & Johnson Consumer Companies, Inc. Topical delivery systems for active agents
AU4647300A (en) * 1999-04-19 2000-11-02 Procter & Gamble Company, The Skin care compositions containing combination of skin care actives
FR2861989B1 (fr) * 2003-11-07 2005-12-30 Oreal Utilisation cosmetique du phytantriol comme agent empechant ou reduisant l'adhesion des microorganismes sur la surface de la peau et/ou des muqueuses
ATE422350T1 (de) * 2003-12-12 2009-02-15 Straetmans Chemische Produkte Anisinsäure und glyceride enthaltende zusammensetzungen

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