GB2283421A - Anti-acne compositions - Google Patents

Anti-acne compositions Download PDF

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Publication number
GB2283421A
GB2283421A GB9322764A GB9322764A GB2283421A GB 2283421 A GB2283421 A GB 2283421A GB 9322764 A GB9322764 A GB 9322764A GB 9322764 A GB9322764 A GB 9322764A GB 2283421 A GB2283421 A GB 2283421A
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solubilizer
weight
polyethylene glycol
average
glycol based
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GB2283421B (en
GB9322764D0 (en
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John Michael Klusiatis
Diester Hans Josef Langsch
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Procter and Gamble Co
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Procter and Gamble Co
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/06Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/60Salicylic acid; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365Hydroxycarboxylic acids; Ketocarboxylic acids
    • 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
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • A61K8/368Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
    • 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
    • A61K8/39Derivatives containing from 2 to 10 oxyalkylene groups
    • 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
    • A61K8/67Vitamins
    • A61K8/671Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/10Washing or bathing preparations

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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)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Birds (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Dispersion Chemistry (AREA)
  • Cosmetics (AREA)

Abstract

A topical composition for the treatment of acne having an aqueous continuous phase optionally together with one or more disperse phases, wherein the aqueous continuous phase is in the form of a solution comprising acidic anti-acne active, surface-active solubilizer therefor and water, and wherein the aqueous continuous phase has a pH of from about 2 to about 4.5, and further wherein the surface-active solubilizer comprises one or more polyethylene based nonionic surfactants having an average HLB in the range from about 12 to about 19. The compositions exhibit improved anti-acne efficacy and excellent skin cleansing and mildness characteristics.

Description

ANTI-ACNE COMPOSITIONS Background of the Invention This invention relates to improved cosmetically acceptable compositions for topical application to the skin, particularly for the prevention or treatment of acne.
Acne is a follicular dermatosis. The comedo, which is the initial lesion of acne, resulting from the impaction of horny cells with the sebaceous follicle, develops in several stages. Primarily comedones develop first as microcomedones where the follicular ostium begins to be distended by horny material to form keratin plugs. The first visible lesion is the closed comedo or whitehead. Dilation of the follicular ostium by dark pigmented horny material marks the onset of an open comedo or blackhead.
Subsequent rupture of closed or open comedones results in formation of secondary comedones which are generally larger and more irregularly shaped.
The bricks of the horny framework of comedones are corneocytes (ie individual dead skin cells) which are held together by a cement-like substance of extracellular lipids. Closed and open comedones develop into the nodules and pustules identified with inflammatory acne.
Although there are multiple factors that appear to be operative in the pathogenesis of acne, it is the formation of keratin plugs (ie retention hyperkeratosis) that is the common denominator.
It is therefore apparent that a treatment directed at preventing or dissolving such keratin plugs (keratolysis) would reduce the compaction necessary to produce the comedo as well as helping to unseat existing comedones (comedolysis).
Salicylic acid is a well recognised anti-acne active ingredient which causes a reduction in intercellular cohesion of the corneocytes (see C Huber et al, Arch. Derm. Res 257, 293 - 297, 1977), thereby dissolving the existing keratin plugs as well as preventing the formation of new ones.
In order to best exert its keratolytic and comedolytic effect, the ideal antiacne composition should deliver and retain optimal concentrations of salicylic acid in the stratum corneum with less penetration through the skin and into the general circulation.
Since salicylic acid is virtually insoluble in water, however, it is difficult to incorporate into aqueous systems. Historically, high levels of alcohol and cleansing detergents have been used to solubilise salicylic acid.
However, these can lead to compositions which are irritating when applied topically to the skin. It would therefore be desirable to deliver the salicylic acid in soluble form from a mild, aqueous base.
It would also be desirable to incorporate perfumes and other essential oils into an aqueous anti-acne composition to improve product aesthetics and skin-care attributes. These materials also tend to be insoluble in water, however.
Anti-acne compositions containing salicylic acid, benzoyl peroxide and surfactant are disclosed in GB-A-2,018,589. GB-A-2,014,963 discloses an aqueous detergent composition for cleansing oily skin comprising a water-soluble salt of a N-acyl ester of sarcosine, a polyvinyl-pyrrolidone cosolubiliser and a protein and/or protein hydrolysate. The composition can also contain salicylic acid as a keratolytic agent and a buffer such as citric acid/citrate. There is no disclosure, however, of topical compositions containing solubilised acidic anti-acne actives in fully protonated form as specified herein.
Since acidic anti-acne agents are most active at low pH (when a high concentration of free acid is present in solution) it would be desirable to deliver the agent from an aqueous phase at a pH at which it exists significantly in protonated form. It is accordingly a primary object of this invention to provide a topical composition comprising a low pH aqueous solution of an anti-acne active.
It is also an object of the invention to provide a topical composition having improved anti-acne activity and excellent skin cleansing and mildness characteristics.
It is a further object of the invention to provide a topical composition comprising a low pH solution of an anti-acne active and additionally incorporating perfume and other essential oils.
Summary of the Invention In accordance with the present invention there is provided a topical composition for the treatment of acne comprising an aqueous continuous phase optionally together with on or more disperse phases and wherein the aqueous continuous phase is in the form of a solution comprising: a] from about 0. 1% to about 10% by weight of acidic anti- acne active; b] from about 0. 1% to about 30% by weight of surface-active solubilizer therefor; and c] water; wherein the aqueous continuous phase has a pH of from about 2 to about 4.5, and wherein the surface-active solubiliser comprises one or more polyethylene glycol based nonionic surfactants having an average HLB in the range from about 12 to about 19 and includes a primary nonionic surfactant solubilizer selected from polyethylene glycol based polyethoxylated animal and vegetable oils containing an average of from about 30 to about 200 ethyleneoxy moieties per mole of oil and polyethylene glycol based polyethoxylated Cg-C15 fatty alcohols containing an average of from about 3 to about 40 ethyleneoxy moieties per mole of alcohol, and mixture thereof.
The compositions of the present invention exhibit improved anti-acne activity, together with excellent cleansing and mildness characteristics.
All levels and ratios are by weight of total composition, unless otherwise indicated. Chain lengths, HLBs and degrees of ethoxylation are also specified on a weight average basis.
Detailed Description of the Invention The anti-acne composition according to the present invention comprises an aqueous continuous phase in the form of a solution comprising acidic anti-acne active, surface-active solubilizer and water. The composition can also comprise one or more disperse phases. However in preferred embodiments the composition is preferably in the form of an aqueous single phase system. In highly preferred embodiments, the composition also includes a solubilized oil component as discussed in detail below.
A first essential component herein is an acidic anti-acne active. Suitable anti-acne actives for use herein include salicylic acid, retinoic acid, azelaic acid, lactic acid, glycolic acid, pyruvic acid, flavinoids, and derivatives, and mixtures thereof. The anti-acne active used in the composition herein is preferably salicylic acid. The anti-acne active is present at a level of from about 0.1% to about 10%, preferably from about 0.1% to about 5%, more preferably from about 0.5 % to about 3 %, by weight of composition.
The anti-acne active is solubilised in water in the compositions of the invention. In preferred embodiments, the compositions are substantially free of lower (C1 - C4) alcohol, i.e. they comprise no more than about 5% alcohol.
A second essential ingredient herein is a surface-active solubilizer. This is essential from the viewpoint of solubilisation of the anti-acne active in water. The surface-active solubilizer used herein comprises one or more polyethyleneglycol based nonionic surfactants having an average HLB in the range from about 12 to about 19 and includes a primary nonionic surfactant solubilizer selected from polyethylene glycol based polyethoxylated animal and vegetable oils containing from about 30 to about 200 ethyleneoxy moieties per mole of oil and polyethylene glycol based polyethoxylated Cg-C15 fatty alcohols containing an average of from about 3 to about 40 ethyleneoxy moieties, and mixtures thereof.
Preferably, the surface-active solubilizer comprises a mixture of from about 0.1% to about 20% by weight of primary solubilizer and from about 0.1% to about 10% by weight of co-solubilizer, the co-solubilizer being selected from polyethylene glycol based polyethoxylated glyceryl ester nonionic surfactants having an average of from about 5 to about 25 ethyleneoxy moieties per mole of surfactant, and mixtures thereof.
Preferably, the co-solubilizer comprises a mixture of a first co-solubilizer component which is a polyethylene glycol based polyethoxylated glyceryl ester nonionic surfactant having an average of from about 5 to about 10 ethyleneoxy moieties per mole of surfactant and a second co-solubilizer component which is a polyethylene glycol based polyethoxylated glyceryl ester nonionic surfactant having an average of from about 15 to about 25 ethyleneoxy moieties per mole of surfactant.
A mixture of primary solubilizer and co-solubilizer as described above is valuable in the compositions of the invention from the viewpoint of solubilization of anti-acne active together with oil component.
In preferred embodiments, the compositions of the invention comprise a mixture of polyethylene glycol based nonionic surfactants wherein the mixture comprises from about 15% to about 50% by weight thereof of a primary polyethylene glycol based nonionic surfactant solubilizer selected from polyethylene glycol based polyethoxylated glyceryl fatty acid ester nonionic surfactants containing an average of from about 30 to about 50 ethyleneoxy moieties per mole of surfactants, and polyethyleneglycol based polyethoxylated Cg-C15 fatty alcohol nonionic surfactants containing an average of from about 5 to about 20 ethyleneoxy moieties per mole of surfactant, and mixtures thereof, from about 10% to about 45 % by weight thereof of a first polyethylene glycol based nonionic surfactant co-solubilizer which is a polyethoxylated glyceryl fatty acid ester nonionic surfactant containing an average of from about 5 to about 10 ethyleneoxy moieties per mole of surfactant and from about 0% to about 70% by weight thereof of a second polyethylene glycol based cosolubilizer which is a polyethoxylated glyceryl fatty acid ester nonionic surfactant containing an average of from about 15 to about 25 ethyleneoxy moieties per mole of surfactant.
Suitable polyethoxylated glyceryl fatty ester surfactants for use herein include those having the formula [I]:
wherein n is the average number of ethyleneoxy moieties per mole of surfactant and wherein R comprises an aliphatic radical having from about 5 to about 25 carbon atoms, preferably from about 7 to about 20 carbon atoms.
Suitable polyethoxylated glyceryl fatty ester surfactants include polyethyleneglycol derivatives of glyceryl cocoate, glyceryl caproate, glyceryl caprylate, glyceryl tallowate, glyceryl palmate, glyceryl stearate, glyceryl laurate, glyceryl oleate, glyceryl ricinoleate, and glyceryl fatty esters derived from triglycerides, such as evening primrose oil, palm oil, hydrogenated castor oil, almond oil, and corn oil.
Suitable polyethylene glycol based polyethoxylated C9-C15 fatty alcohols suitable for use herein include C9-C11 Pareth-3, C9-C11 Pareth-4, C9- Cl 1 Pareth-5, C9-C11 Pareth-6, C9-C11 Pareth-7, C9-Cl 1 Pareth-8, Cll-C15 Pareth-3, C11-C15 Pareth-4, Cil-Cis Pareth-5, C11-C15 Pareth-6, C1l-C15 Pareth-7, C1l-Cls Pareth-8, C11-C15 Pareth-9, Cli- ClS Pareth-lO, C11-C15 Pareth-11, C1l-Cls Pareth-12, C1l-Cls Pareth-13 and C11-C15 Pareth-14.
From the viewpoint of anti-acne active solubilisation and mildness and cleansing benefits the most preferred mixture of polyethyleneglycol based nonionic surfactants comprises from about 15% to about 50% by weight thereof of PEG 40 hydrogenated castor oil or C9-Cl 1 Pareth-8, from about 10% to about 45% by weight thereof of PEG 7 glyceryl cocoate and from about 0% to about 70% by weight thereof of PEG 20 glyceryl laurate. PEG 40 hydrogenated castor oil is commercially available under the tradename Cremophor (RTM) from BASF. PEG 7 glyceryl cocoate and PEG 20 glyceryl laurate are commercially available from Henkel under the tradenames Cetiol (RTM) HE and Lamacit (RTM) GML 20 respectively. C9-C11 Pareth-8 is commercially available from Shell Ltd under the tradename Dobanol (RTM) 91-8.
In addition, the compositions of the invention preferably comprise from about 0.01% to about 10% by weight of an oil component selected from essential, emollient and perfume oils, and mixtures thereof.
Suitable oils for use herein can be selected from water-insoluble silicones inclusive of non-volatile polyalkyl and polyaryl siloxane gums and fluids, volatile cyclic and linear polyalkylsiloxanes, polyalkoxylated silicones, amino and quaternary ammonium modified silicones, rigid cross-linked and reinforced silicones and mixtures thereof, C1-C24 esters of C8-C30 fatty acids such as isopropyl myristate and cetyl ricinoleate, beeswax, saturated and unsaturated fatty alcohols such as behenyl alcohol, hydrocarbons such as mineral oils, petrolatum and squalene, fatty sorbitan esters (see US-A-3988255, Seiden, issued October 26th 1976), lanolin and oil-like lanolin derivatives, animal and vegetable triglycerides such as almond oil, peanut oil, wheat germ oil, linseed oil, jojoba oil, oil of apricot pits, walnuts, palm nuts, pistachio nuts, sesame seeds, rapeseed, cade oil, corn oil, peach pit oil, poppyseed oil, pine oil, castor oil, soybean oil, avocado oil, safflower oil, coconut oil, hazlenut oil, olive oil, grapeseed oil, and sunflower seed oil, and C1-C24 esters of dimer and trimer acids such as diisopropyl dimerate, diisostearylmalate, diisostearyldimerate and triisostearyltrimerate.
The compositions of the invention are formulated so as to have a pH in the range from about 2 to about 4.5. The desired pH value can be obtained by use of appropriate cosmetically acceptable primary or dual buffer systems. A suitable buffering agent for use herein is sodium citrate.
The compositions of the invention can also be formulated as an aqueous gel system. It is preferable to use a gel system which provides optimum skin feel, spreadability, moisturisation, emolliency, rub-in and absorption characteristics. When formulated as gel systems the compositions herein additionally comprise a hydrophilic gelling agent at a level of from about 0.1% to about 20%, preferably from about 0.2% to about 2%, and more preferably from about 0.3 % to about 1% . The gelling agent preferably has a viscosity (1S6 aqueous solution, 200C, Brookfield RVT) of at least about 4000 cps, more preferably at least about 10,000 cps, and especially at least 50,000 cps.
Suitable hydrophilic gelling agents can generally be described as watersoluble or colloidally water-soluble polymers, and include cellulose ethers (e.g. hydroxyethyl cellulose, methyl cellulose, hydroxy propylmethyl cellulose, hydroxypropyl cellulose), polyvinylpyrrolidone, polyvinylalcohol, guar gum, hydroxypropyl guar gum and xanthan gum.
Such hydrophilic gelling agents are commercially available under the tradenames Klucell (RTM), Methocel (RTM) and Natrosol (RTM). A preferred hydrophilic gelling agent for use herein is Natrosol (RTM).
Other hydrophilic gelling agents for use herein are acrylic acid/ethyl acrylate copolymers and the carboxyvinyl polymers sold by the B.F.
Goodrich Company under the trade mark of Carbopol resins. These resins consist essentially of a colloidally water-soluble polyalkenyl polyether crosslinked polymer of acrylic acid crosslinked with from 0.75 % to 2.00% of a crosslinking agent such as for example polyallyl sucrose or polyallyl pentaerythritol. Examples include Carbopol 934, Carbopol 940, Carbopol 950 and Carbopol 980. Carbopol 934 is a water-soluble polymer of acrylic acid crosslinked with about 1% of a polyallyl ether of sucrose having an average of about 5.8 allyl groups for each sucrose molecule.
Also suitable for use herein are hydrophobically-modified cross-linked polymers of acrylic acid having amphipathic properties available under the trade name Carbopol 1382, Carbopol 1342 and Pemulen TR-1 (CTFA Designation: Acrylates/1S30 Alkyl Acrylate Crosspolymer). A combination of the polyalkenyl polyether cross-linked acrylic acid polymer and the hydrophobically modified cross-linked acrylic acid polymer is also suitable for use herein. The gelling agents herein are particularly valuable for providing excellent stability characteristics over both normal and elevated temperatures.
Neutralizing agents suitable for use in neutralizing acidic group containing hydrophilic gelling agents herein include sodium hydroxide, potassium hydroxide, ammonium hydroxide, monoethanolamine, diethanolamine and triethanolamine.
In the present compositions, humectants such as glycerine (sometimes known as glycerol or glycerin) can be present at a level of from about 0.5% to about 20%, preferably from about 1% to about 10%, more preferably from about 4% to about 8% by weight of composition.
Chemically, glycerine is 1,2,3- propanetriol and is a product of commerce. One large source of the material is in the manufacture of soap. Polyhydric alcohol humectants other than glycerol which can be added herein include sorbitol, propylene glycol, butylene glycol, hexylene glycol, ethoxylated glucose and hexanetriol.
The compositions of the present invention can also comprise a watersoluble polyglycerylmethacrylate lubricant. The water soluble polyglycerylmethacrylate lubricant suitable for use herein generally has a viscosity (10% aqueous solution, 200C, Brookfield RVT) of less than about 4000 cps, preferably less than about 1000 cps and more preferably less than about 500 cps. In addition, the polyglycerylmethacrylate lubricant preferably also has a viscosity (neat) in the range of from about 200 to about 5000 cps (Brookfield RVT, 200C), more preferably from about 500 to about 2000 cps and especially from about 700 to about 900 cps.
The polyglycerylmethacrylate lubricants which can be used in the compositions herein are available under the trademark Lubragel (RTM) from Guardian Chemical Corporation, 230 Marcus Blvd., Hauppage, N.Y. 11787. In general, Lubragels can be described as hydrates or clathrates which are formed by the reaction of sodium glycerate with a methacrylic acid polymer. Thereafter, the hydrate or clathrate is stabilized with a small amount of propylene glycol, followed by controlled hydration of the resulting product. Lubragels are marketed in a number of grades of varying glycerate: polymer ratio and viscosity. Preferred for use herein, however, is so-called Lubragel Oil which has a typical viscosity of about 800 cps. Other suitable Lubragels include Lubragel TW, Lubragel CG and Lubragel MS.
When present, the polyglycerylmethacrylate lubricant is preferably incorporated at a level of from about 0.1 % to about 10%, more preferably from about 0.2% to about 2%, and especially from about 0.3% to about 1% by weight of composition.
When the compositions of the invention are formulated in aqueous gel form they have a product viscosity of at least about 4,000 and preferably in the range from about 4,000 to about 300,000 cps, more preferably from about 20,000 to about 200,000 cps and especially from about 80,000 to about 150,000 cps (200C, neat, Brookfield RVT), and a yield point of at least 50 dynes/cm2 (Brookfield RVT, Spindle CP52, Plate Code A, 25 C).
The compositions of the invention can also be formulated as foams.
When formulated as foams, it is preferable to include a foam-stabilizer in the compositions. A suitable foam stabilizer for use herein is POLAWAX A31 commercially available from Croda. In addition, a propellant such as diethyl ether or propanelbutane can be added to foam compositions.
A number of additional water-soluble materials can be added to the compositions of the invention, however. Such materials include the other humectants such as sorbitol, propylene glycol, ethoxylated glucose and hexanetriol; proteins and polypeptides and derivatives thereof; watersoluble or solubilizable preservatives such as Germall 115, methyl, ethyl, propyl and butyl esters of hydroxybenzoic acid, EDTA, Euxyl (RTM) K400, Bromopol (2-bromo-2-nitropropane-1 ,3-diol) and phenoxypropanol; anti-bacterials such as Irgasan (RTM) and phenoxyethanol (preferably at levels of from 0.5% to about 5%); soluble or colloidally-soluble moisturising agents such as hyaluronic acid and starch-grafted sodium polyacrylates such as Sanwet (RTM) IM-1000, IM1500 and IM-2500 available from Celanese Superabsorbent Materials, Portsmith, VA, USA and described in USA-A-4,076,663; colouring agents, etc. The compositions can also contain low levels of insoluble ingredients added, for example for visual-effect purposes, e.g.
thermochromic liquid crystalline materials such as the microencapsulated cholesteryl esters and chiral nematic (non-sterol) based chemicals such as the (2-methylbutyl)phenyl 4-alkyl(oxy)benzoates available from Hallcrest, Glenview, Illinois 60025, U.S.A. Water is also present at a level of from about 50% to about 99.2%, preferably from about 80% to about 95% by weight of the compositions herein. The compositions of the invention can also contain from about 0.1% to about 10%, preferably from about 1% to about 5% of a panthenol moisturiser. The panthenol moisturiser can be selected from D-panthenol ([R]-2,4-dihydroxy-N-[3-hydroxypropyl]-3 ,3- dimethylbutamide), DL-panthenol, calcium pantothenate, royal jelly, panthetine, pantotheine, panthenyl ethyl ether, pangamic acid, pyridoxin, pantoyl lactose and Vitamin B complex.
Other water-soluble materials can be added to the compositions of the invention, such as for example a fluid copolymer of ethylene oxide and propylene oxide having a viscosity in the range of from 55 to 300,000 Saybolt Universal Seconds [S.U.S.], preferably from 100 to 2,000 S.U.S.
at 1000F, for example Ucon Fluid 75-H 450.
As described earlier, the compositions of the invention can also comprise one or more disperse phases. Suitable materials which can be included in the disperse phase are solid materials such as cyclodextrines, Bcyclodextrines, methylated and partially methylated 8-cyclodextrines and hydrophilic powders, eg. fumed silica, which improve aesthetics and active delivery.
Another optional ingredient of the compositions of the invention is trimethylglycine, otherwise sometimes known as betaine. When present, trimethylglycine is incorporated at a level of from about 1% to about 10% by weight, preferably from about 3 % to about 7% by weight.
Other optional ingredients which can be added to the compositions of the invention include skin soothing or anti-inflammatory agents such as Allantoin and Bisabolol and antimicrobials such as Biosol, Usnic acid and Citricidal.
The compositions of the invention are illustrated in the following Examples: Examples I-VII Ingredients I % II % m % IV % V % VI% VII% Cetiol HEl 4.3 5.0 4.5 5.2 4.0 4.0 4.0 Cremophor 3.7 0.0 0.0 4.0 3.7 4.0 0.0 RH 401 C9-Cll 0.0 4.0 3.7 0.0 0.0 0.0 3.7 Pareth 82 IJannacit 2.0 2.0 2.5 2.2 1.9 2.5 2.3 GML 203 Salicylic 2.0 2.0 2.0 2.0 2.0 2.0 2.0 Acid Natrosol 0.0 0.0 0.0 0.0 0.0 2.0 2.0 250HHR Bisabolol 1.0 1.0 1.0 1.0 1.0 1.0 1.0 Dimethicone 1.0 1.5 1.0 1.0 1.3 1.2 1.2 [0.65 cSt] Allantoin 0.1 0.09 0.15 0.1 0.12 1.0 1.0 Sodium 0.03 0.025 0.03 0.02 0.03 0.03 0.03 Citrate FD & 0.00125 0.00125 0.00125 0.00125 0.00125 0.00125 0.00125 Blue No 1 Ethanol 20.0 0.0 0.0 0.0 0.0 0.0 0.0 Deionised ---- ----------------------------- to 1 0 0 --- ------------------------------ water 1. Supplied by BASF 2. Supplied by Shell 3. Supplied by Henkel The lotion compositions of the above Examples (I-V) can be prepared as follows. In a first vessel, the solubilizer ingredients are combined with the acidic anti-acne active and the mixture is heated to 30-35 C to dissolve the salicylic acid. In a second vessel, the water is heated up to 70"C and the salicylic acid solution is added to the water vessel with stirring. The resulting mixture is cooled down and when the temparature drops below 35-40"C the remaining ingredients are added. rThe compositions are then ready for packaging.
The gel compositions of the above Examples (VI and VII) are prepared as follows. In a first vessel, the water is heated up to 70"C and the gelling agent is added until dissolved. In a second vessel, the solubilizer ingredients are combined with the acidic anti-acne active and the resulting mixture is heated to 30-35 0C to dissolve the salicylic acid. The salicylic acid solution is then added to the first vessel containing the water and gelling agent. The mixture is cooled down and at below 35-40"C the remaining ingredients are added. The compositions are then ready for packaging.
The above compositions exhibit improved anti-acne efficacy and superior cleansing and mildness characteristics when applied topically to the skin.

Claims (10)

1. A topical composition for the treatment of acne comprising an aqueous continuous phase optionally together with one or more disperse phases and wherein the aqueous continuous phase is in the form of a solution comprising: a] from about 0.1% to about 10% by weight of acidic anti- acne active; by from about 0. 1% to about 30% by weight of surface-active solubilizer therefor; and c] water; wherein the aqueous continuous phase has a pH of from about 2 to about 4.5, and wherein the surface-active solubiliser comprises one or more polyethylene glycol based nonionic surfactants having an average HLB in the range from about 12 to about 19 and includes a primary nonionic surfactant solubilizer selected from polyethylene glycol based polyethoxylated animal and vegetable oils containing an average of from about 30 to about 200 ethyleneoxy moieties per mole of oil and polyethylene glycol based polyethoxylated Cg-C15 fatty alcohols containing an average of from about 3 to about 40 ethyleneoxy moieties per mole of alcohol, and mixture thereof.
2. A topical composition according to Claim 1 wherein the acidic anti acne active is selected from salicylic acid, retinoic acid, azeleic acid, lactic acid, glycolic acid, pyruvic acid, flavinoids, and derivatives and mixtures thereof.
3. A topical composition according to Claim 1 or 2 wherein the acidic anti-acne active is salicylic acid.
4. A topical composition according to any of Claims 1 to 3 wherein the composition is substantially free of lower (C1-C4) alcohol.
5. A topical composition according to any of Claims 1 to 4 wherein the surface-active solubilizer comprises a mixture of from about 0. 1% to about 20% by weight of primary solubilizer and from about 0. 146 to about 10% by weight of co-solubilizer, the co- solubilizer being selected from polyethylene glycol based polyethoxylated glyceryl ester nonionic surfactants having an average of from about 5 to about 25 ethyleneoxy moieties per mole of surfactant, and mixtures thereof.
6. A topical composition according to any of Claims 1 to 5 wherein the co-solubilizer comprises a mixture of a first co-solubilizer component which is a polyethylene glycol based polyethoxylated glyceryl ester nonionic surfactant having an average of from about 5 to about 10 ethyleneoxy moieties per mole of surfactant and a second co-solubilizer component which is a polyethylene glycol based polyethoxylated glyceryl ester nonionic surfactant having an average of from about 15 to about 25 ethyleneoxy moieties per mole of surfactant.
7. A topical composition according to any of Claims 1 to 6 comprising from about 0.01% to about 10% by weight of an oil component selected from essential, emollient and perfume oils, and mixtures thereof.
8. A topical composition according to any of Claims 1 to 5 comprising from about 0. 1% to about 5% by weight of acidic anti-acne active.
9. A topical composition according to any of Claims 1 to 8 comprising a mixture of polyethylene glycol based nonionic surfactants wherein the mixture comprises from about 15% to about 50% by weight thereof of a primary nonionic surfactant solubilizer selected from polyethylene glycol based polyethoxylated glyceryl fatty acid ester nonionic surfactants containing an average of from about 30 to about 50 ethyleneoxy moieties per mole of surfactant and polyethylene glycol based polyethoxylated Cg-C15 fatty alcohol nonionic surfactants containing an average of from about 5 to about 20 moles of ethyleneoxy moieties per mole of surfactant, from about 10% to about 45 4b by weight thereof of a first co-solubilizer component which is a polyethylene glycol based polyethoxylated glyceryl fatty acid ester nonionic surfactant containing an average of from about 5 to about 10 ethyleneoxy moieties per mole of surfactant and from about 0% to about 70% by weight thereof of a second co-solubilizer component which is a polyethylene glycol based polyethoxylated glyceryl fatty acid ester nonionic surfactant containing an average of from about 15 to about 25 ethyleneoxy moieties per mole of surfactant.
10. A topical composition according to Claim 9 wherein the mixture of polyethylene glycol based nonionic surfactants comprises from about 15% to about 50% by weight thereof of PEG 40 hydrogenated castor oil or C9-Cl 1 Pareth-8, from about 10% to about 45% by weight thereof of PEG 7 glyceryl cocoate and from about 0% to about 70% by weight thereof of PEG 20 glyceryl laurate.
11 A topical composition according to any of Claims 1 to 10 wherein the composition is a single phase aqueous composition.
GB9322764A 1993-11-04 1993-11-04 Anti-acne compositions Expired - Fee Related GB2283421B (en)

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2299022A (en) * 1995-03-18 1996-09-25 Procter & Gamble Anti-acne cosmetic composition
WO1996039119A1 (en) * 1995-06-06 1996-12-12 Neutrogena Corporation Topical vehicles containing solubilized and stabilized azelaic acid
WO1999013857A1 (en) * 1997-09-16 1999-03-25 L'oreal Aqueous solutions of salicylic acid derivatives
WO2002028361A2 (en) * 2000-09-29 2002-04-11 Johnson & Johnson Consumer Companies, Inc. Compositions for cleansing skin and treating acne
WO2012131348A1 (en) * 2011-03-31 2012-10-04 Evocutis Plc Salicylic acid topical formulation

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2299022A (en) * 1995-03-18 1996-09-25 Procter & Gamble Anti-acne cosmetic composition
GB2299022B (en) * 1995-03-18 1999-03-31 Procter & Gamble Cosmetic compositions
WO1996039119A1 (en) * 1995-06-06 1996-12-12 Neutrogena Corporation Topical vehicles containing solubilized and stabilized azelaic acid
WO1999013857A1 (en) * 1997-09-16 1999-03-25 L'oreal Aqueous solutions of salicylic acid derivatives
WO2002028361A2 (en) * 2000-09-29 2002-04-11 Johnson & Johnson Consumer Companies, Inc. Compositions for cleansing skin and treating acne
WO2002028361A3 (en) * 2000-09-29 2002-07-04 Johnson & Johnson Consumer Compositions for cleansing skin and treating acne
WO2012131348A1 (en) * 2011-03-31 2012-10-04 Evocutis Plc Salicylic acid topical formulation

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Publication number Publication date
GB2283421B (en) 1997-11-26
GB9322764D0 (en) 1993-12-22

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