WO2001070271A2 - Compositions de base stables utiles pour preparer des compositions topiques sans tensioactifs - Google Patents

Compositions de base stables utiles pour preparer des compositions topiques sans tensioactifs Download PDF

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Publication number
WO2001070271A2
WO2001070271A2 PCT/US2001/009317 US0109317W WO0170271A2 WO 2001070271 A2 WO2001070271 A2 WO 2001070271A2 US 0109317 W US0109317 W US 0109317W WO 0170271 A2 WO0170271 A2 WO 0170271A2
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composition
base composition
base
dispersion
weight
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PCT/US2001/009317
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English (en)
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WO2001070271A3 (fr
Inventor
James M. Willmott
Timothy K. Crawford
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Collaborative Technologies, Inc.
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Priority to AU2001245954A priority Critical patent/AU2001245954A1/en
Publication of WO2001070271A2 publication Critical patent/WO2001070271A2/fr
Publication of WO2001070271A3 publication Critical patent/WO2001070271A3/fr

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Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • 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
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic 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
    • A61K8/67—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
    • 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
    • A61K8/73—Polysaccharides
    • 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
    • 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 acid-stable base compositions for preparing surfactant free topical, oral, nasal, anal, ophthalmic, or vaginal compositions and a method for preparing such surfactant free compositions.
  • Physiologically active agents are compounds which cause a physiological change to the body following their application. Examples of such agents include alpha hydroxy acids, antioxidants, and vitamins.
  • Aesthetic modifying agents are materials that impart desirable tactile, olfactory, taste or visual properties to the surface to which the composition is applied.
  • aesthetic modifying agents include silicone fluids and derivatives thereof, waxes, botanical (vegetable) oils, hydrocarbon-based oils, esters and fragrances.
  • stable emulsions are commonly employed to deliver physiologically active agents and aesthetic modifying agents. These emulsions form either spherical micelles of one or more hydrophobic liquid materials in water or spherical droplets of water in a hydrophobic fluid.
  • Such emulsions are typically formed by separately preparing an oil phase and a water phase.
  • the hydrophobic ingredients are dissolved in a suitable oil phase and the hydrophilic ingredients are dissolved in water.
  • the two phases are heated to at least 70° C and mixed together.
  • Emulsifying agents are usually added to the mixture in order to reduce the surface tension between the oil and water phases, thereby making the combination of the two phases more stable.
  • the mixture is then slowly cooled to ensure the formation of crystalline structures which enhance the stability of the emulsion.
  • Emulsions prepared by this method usually have a homogeneous opaque white appearance and a smooth or pleasant feeling upon application to the skin or other epithelial surface.
  • a significant drawback of emulsions is their requirement for surfactants.
  • Surfactants damage the skin's natural barrier and the lipid bilayer of epithelial cell membranes leaving tissue vulnerable and irritating the skin. The damaged barrier permits the passage of other materials that can cause irritation, increase skin sensitivity and bring about allergic reactions.
  • the literature is replete with clinical evidence of the damaging consequences that can occur with the use or overuse of surfactants.
  • lowering the surface tension of a topical preparation generally increases the surface exposure of the active agent or aesthetic modifying agent to oxygen and other destabilizing materials.
  • the instability of the preparation may decrease the efficacy of the retinol.
  • the instability of an unsaturated fatty acid as an aesthetic modifying agent leads to color changes in the preparation and malodor.
  • Typical emulsions are time consuming to prepare, require heating, are produced in multiple phases, are slow cooling, and often require high shear conditions to get the particle size small enough for maximum stability. Larger batches may require 8 to 24 hours to process and can take several days to set up. It is also often difficult to control the process parameters for preparing the emulsion. If any factors such as the heating, cooling or mixing rates are not carefully duplicated, the preparation may have different properties than the preceding batches of the same product. As a result, the stability of the emulsion may vary from batch to batch. Often the difference of a single parameter is significant enough to cause the product to be outside the established optimum specifications. These batches then have to be either discarded or re-worked.
  • the lack of reproducibility is especially problematic when the product contains a physiologically active agent. Lack of reproducibility can effect product performance and end user satisfaction. The lack of reproducibility also results in products having different aesthetic properties which the end user will perceive as a lack of quality and will ultimately lead to consumer dissatisfaction or reduced compliance.
  • Emulsions are typically expensive to manufacture. This is due to a variety of factors including the energy to heat the batch, the specialized equipment required to process the emulsion, such as specialized pumps and cooling/heating equipment, and the time the process ties up equipment and personnel. Moreover, such emulsions cannot be easily processed or customized at the point of purchase. Since most skin care preparations are prepackaged and have predetermined dosages, dermatologists cannot readily administer to patients varying dosages of an active agent. As a result, a patient may need to apply two or more different skin care preparations since a single preparation with all of the prescribed active agents may not be available.
  • Some dermatologists prepare their own skin care preparations. These skin care preparations typically have poor aesthetic properties resulting in poor patient compliance. Thus, it would be desirable for dermatologists to be able to quickly and easily prepare skin care preparations having varying dosages of active agents and an aesthetically pleasing appearance.
  • Present cosmetic products contain predetermined amounts of active agents. Customers cannot pick and choose which ingredients to include in these products. Many customers do not purchase certain cosmetic products because of an allergic reaction with one or more of the ingredients included in the product. For example, many customers are allergic to various fragrances. It would therefore be advantageous to prepare the cosmetic product at the point of sale without the fragrances. Also, customers may have to apply two or more different cosmetic products to get a desired effect since a single product with the desired combination of active agents and/or aesthetic modifying agents may not be on the market. Many cosmetic products are sold in only one form, such as a spray, gel or lotion. Customers, however, may prefer other forms of the cosmetic product. Prior to the present invention, it was not practical to prepare custom cosmetic products at the point of sale.
  • the present invention relates to a base composition for preparing a substantially surfactant free composition for topical, oral, nasal, anal, ophthalmic, or vaginal application.
  • the base composition comprises sclerotium gum and carrageenan.
  • compositions containing the base composition of the present invention are stable at a pH of about 3.0 and lower.
  • the base compositions are also compatible with cationic dispersions, i.e., unlike prior compositions, mixtures of the base composition and a cationic dispersion do not result in the formation of aggregates or the separation of water and hydrophobic ingredients in the composition.
  • compositions for topical, oral, nasal, anal, ophthalmic, or vaginal application comprising the base composition of the present invention and at least one dispersion comprising suspended particles of a hydrophobic active agent, a hydrophobic adjuvant, or a combination thereof.
  • the composition is substantially free of emulsifying surfactants and the suspended particles have a diameter less than about 500 nm.
  • the composition comprises at least one cationic dispersion.
  • the composition has a pH of less than about 5, preferably a pH of less than about 4, and more preferably a pH of less than about 3.
  • Yet another embodiment is a method of preparing a composition for topical, oral, nasal, anal, ophthalmic, or vaginal application.
  • the method comprises mixing (a) the base composition of the present invention, and (b) at least one dispersion comprising suspended particles of a hydrophobic active agent, a hydrophobic adjuvant, or a combination thereof.
  • the composition prepared is substantially free of emulsifying surfactants and the suspended particles have a diameter less than about 500 nm.
  • Mixing may be performed with a propeller mixer or manually, i.e., by hand.
  • the base composition is premanufactured.
  • the composition prepared contains at least one cationic dispersion. Since the composition is simple and quick to prepare, custom cosmetic compositions may be prepared at the point of sale for customers in minutes. Prior to the present invention, such products would take hours to be prepared.
  • the present invention relates to a base composition for preparing a substantially surfactant free composition for topical, oral, nasal, anal, ophthalmic, or vaginal application.
  • the base composition comprises sclerotium gum and carrageenan.
  • the weight ratio of sclerotium to carrageenan ranges from about 1 :0.8 to about 1 :3.
  • the weight ratio preferably ranges from about 1 : 1 to about 1:1.5 and more preferably is about 1 : 1.33.
  • the base composition typically contains from about 0.5 to about 10% by weight of sclerotium gum and from about 0.5 to about 12% by weight of carrageenan, based upon 100% total weight of base composition.
  • the base composition contains from about 1 to about 4% by weight of sclerotium gum and from about 1 to about 5% by weight of carrageenan, based upon 100% total weight of base composition.
  • the base composition contains about 1.5% by weight of sclerotium gum and about 2.0% by weight of carrageenan, based upon 100% total weight of base composition.
  • the base composition may further comprise additional rheology modifying agents.
  • the base composition does not contain rheology modifying agents which are not effective in acidic environments, such as, for example, carbomer, acrylate/alkyl acrylate crosspolymers, and carboxymethylcellulose.
  • Preferred rheology modifying agents include, but are not limited to, phosphorylated starch derivatives, acrylates/vinyl isodecanoate crosspolymer, xanthan gum, locust bean gum, guar gum, and any combination of any of the foregoing.
  • phosphorylated starch derivative includes, but is not limited to, starches containing a phosphate group.
  • Suitable phosphorylated starch derivatives include, but are not limited to, hydroxyalkyl starch phosphates, hydroxyalkyl distarch phosphates, and any combination of any of the foregoing.
  • Non-limiting examples of hydroxyalkyl starch phosphates and, hydroxyalkyl distarch phosphates include hydroxyethyl starch phosphate, hydroxypropyl starch phosphate, hydroxypropyl distarch phosphate, and any combination of any of the foregoing.
  • the base composition comprises a hydroxyalkyl distarch phosphate and more preferably hydroxypropyl distarch phosphate.
  • compositions for topical, oral, nasal, anal, ophthalmic, or vaginal application comprising the base composition of the present invention and at least one dispersion comprising suspended particles of a hydrophobic active agent, a hydrophobic adjuvant, or a combination thereof.
  • the composition is substantially free of emulsifying surfactants and the suspended particles have a diameter less than about 500 nm.
  • the composition for application only contains water-soluble ingredients and/or dispersions of hydrophobic active agents and/or hydrophobic adjuvants.
  • hydrophobic ingredients which are not in the form of a dispersion are not included in the composition, or at least not in any substantial amounts.
  • compositions may be incorporated into the composition.
  • hydrophobic ingredients to be included in the final composition are added as dispersions (i.e. a dispersion of the hydrophobic ingredient is prepared before it is mixed with the base composition and the dispersion).
  • the composition contains a cationic dispersion.
  • the composition may have a pH of less than about 5 and even a pH of less than about 4, about 3, or about 1.
  • the composition contains from about 0.01 to about 60% by weight, preferably from about 5 to about 85% by weight, and more preferably from about 0.4 to about 6% by weight of the base composition, based upon 100% weight of total composition.
  • composition for topical, oral, nasal, anal, ophthalmic, or vaginal application may be prepared by mixing (a) the base composition of the present invention, and (b) at least one dispersion comprising suspended particles of a hydrophobic active agent, a hydrophobic adjuvant, or a combination thereof.
  • the composition prepared is substantially free of emulsifying surfactants and the suspended particles have a diameter less than about 500 nm.
  • the composition preferably comprises less than about 3% by weight and more preferably less than about 1% by weight of dispersion initiator, based upon 100% weight of total composition.
  • the composition may be a cream, gel, or lotion, serum or spray.
  • the base composition is premanufactured, i.e., prepared at a location remote from where the mixing step is performed or prepared in large quantities.
  • large quantities is herein defined as a quantity greater than that needed to produce a single final product and is preferably many multiples times that.
  • the base composition is typically premanufactured in large batches.
  • Mixing is generally performed at a temperature of from about 15 to about 30° C, preferably at a temperature of from about 20 to about 30° C, and most preferably at ambient temperature. Since the hydrophobic active agent or hydrophobic adjuvant is added to the base composition as a dispersion, heating and other expensive processing steps are not required to obtain a homogenous final composition. Preferably, the composition is not heated.
  • the dispersion is generally a homogenous fluid which is stable for a commercially relevant period of time.
  • the dispersion typically remains stable for at least 2 months and preferably at least 6 months at ambient temperature and in many cases at least 2 weeks and preferably at least 2 months at elevated temperature (50° C).
  • the dispersion is prepared by mixing from about 0.1% to about 70% by weight of hydrophobic active agent and/or hydrophobic adjuvant with from about 30% to about 99.9% by weight of aqueous phase under high pressure and high shear conditions, based upon 100% weight of total dispersion.
  • Suitable high pressure and high shear dispersions are sold under the tradename SanSurf ® by Collaborative Laboratories, Inc. of East Setauket, NY.
  • the aqueous phase contains water and, optionally, other hydrophilic adjuvants. More preferably, the mixing is performed with shearing at a pressure from about 9,000psi to about 25,000 psi to form a dispersion having an average particle size ranging from about 50nm to about 500 nm.
  • the base composition may be prepared by methods known in the art.
  • hydrophobic active agent or hydrophobic adjuvant is an active agent or adjuvant which has a non polar property which makes it essentially insoluble in water or water and polar solvent solution.
  • Hydrophobic active agents and hydrophobic adjuvants of the present invention include, but are not limited to, partially and fully hydrophobic active agents and partially and fully hydrophobic adjuvants.
  • hydrophobic active agents encompassed by the present invention include compounds and complexes which contain a hydrophobic moiety.
  • composition of the present invention may also include non-hydrophobic active agents and non-hydrophobic adjuvants.
  • the dispersion containing the suspended particles generally contains from about 0.01 to about 70% by weight of oil, based upon 100% weight of total dispersion. Preferably, the dispersion contains from about 1.0 to about 50% by weight of oil, based upon 100% weight of total dispersion.
  • the oil component of the composition may include active agents and adjuvants which are oils.
  • the dispersion is a suspension of liquid or solid particles of colloidal size or larger in a liquid medium.
  • the dispersion contains suspended particles, such as oil particles (or oil droplets), having a diameter less than about 500 nm.
  • the diameter of the suspended particles preferably ranges from about 50 nm to about 500 nm and more preferably from about 250 to about 500 nm.
  • the oil droplets contain one or more lipophilic materials.
  • the oil droplets may have a charge as determined by zeta potential measurements.
  • the oil droplets may be prepared by ultra high shear mixing or microfluidization.
  • Preferred oil containing dispersions are sold under the tradename SanSurf ® by Collaborative Laboratories, Inc. of East Setauket, NY, and DermasomesTM by Microfluidics Corp. of Newton, MA.
  • Suitable active agents include, but are not limited to acid stable, anti-acne agents, antimicrobial agents, antiinflammatory agents, analgesics, antierythemal agents, antipruritic agents, antiedemal agents, antipsoriatic agents, antifungal agents, skin protectants, sunscreen agents, vitamins, antioxidants, scavengers, antiirritants, antibacterial agents, antiviral agents, antiaging agents, protoprotection agents, hair growth enhancers, hair growth inhibitors, hair removal agents, antidandruff agents, anti-seborrheic agents, exfoliating agents, wound healing agents, anti-ectoparacitic agents, sebum modulators, immunomodulators, hormones, botanicals, moisturizers, astringents, cleansers, sensates, antibiotics, anesthetics, steroids, tissue healing substances, tissue regenerating substances, amino acids, peptides, minerals, ceramides, biohyaluronic acids, and any combination of any of the foregoing.
  • Preferred anti-acne agents include, but are not limited to, salicylic acid, retinoic acid, alpha-hydroxy acids, benzyl peroxide, sodium sulfacetamide, clindamycin, and any combination of any of the foregoing.
  • Preferred combinations of anti-acne agents to be incorporated in the composition include salicylic acid, retinoic acid, and hydrocortisone; sodium sulfacetamide and clindamycin; salicylic acid and clindamycin; salicylic acid, alpha- hydroxy acids, and tetrahydrozoline.
  • Suitable antimicrobial agents include, but are not limited to, benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, chloroxylenol, cloflucarban, fluorosalan, hexachlorophene, hexylresorcinol, iodine complex, iodine tincture, para- chloromercuriphenol, phenylmercuric nitrate, thimerosal, vitromersol, zyloxin, triclocarban, triclosan, methyl-benzethonium chloride, nonyl phenoxypoly(ethyleneoxy) ethanol-iodine, para-chloro-meta-xylenol, providone-iodine complex, poloxamer-iodine complex, triclorcarban, undecoylium chloride-iodine complex, and any combination of any of the foregoing.
  • Suitable anti-inflammatory agents include, but are not limited to, alidoxa, allantoin, aloe vera, aluminum acetate, bismuth subnitrate, boric acid, calamine, casein, cellulose, microporous, cholecatciferol, cocoa butter, cod liver oil, colloidal oatmeal, cystein hydrochloride, dexpanthenol, dimethicone, glycerin, kaolin, lanolin, live yeast cell derivative, mineral oil, peruvian balsam, petrolatum, protein hydrolysate, racemethionine, shark liver oil, sulfur, talc, tannic acid, topical starch, vitamin A, vitamin E, white petrolatum, zinc acetate, zinc carbonate, zinc oxide, hydrocortisone, betamethasone, ibuprofen, indomethicin, acetyl salicylic acid, tacrolimus, flucoinolone acetonide, sodium sulfacetamide,
  • Suitable analgesics include, but are not limited to, diphenhydramine, tripeiennamine, benzocaine, dibucaine, lidocaine, tetracaine, camphor, menthol, phenol, resorcinol, matacresol, juniper tar, methylsalicylate, turpentine oil, capsicum, methyl nicotinate, b-glucan, and any combination of any of the foregoing.
  • Suitable antierythemal agents include, but is not limited to, tetrahydrozoline and hydracortisone.
  • Suitable antipruritic agents include, but are not limited to, benadryl, pramoxine, antihistamines, and any combination of any of the foregoing.
  • Suitable antiedemal agents include, but are not limited to, pregnenalone acetate, tanin glyrosides, and any combination of any of the foregoing.
  • Suitable antipsoriatic agents include, but are not limited to, caleipotriene, coal tar, anthralin, vitamin A, and any combination of any of the foregoing.
  • Preferred combinations of antipsoriatic agents include, but are not limited to, hydrocortisone, retinoic acid, and alpha hydroxy acid; dovonex, salicylic acid, and a sunscreen agent; indomethicin, salicylic acid, and urea; anthralin and salicylic acid; and anthralin and indomethicin.
  • Other suitable antipsoriatic agents include, but are not limited to, caleipotriene, coal tar, anthralin, vitamin A, and any combination of any of the foregoing.
  • Suitable antifungal agents include, but are not limited to, clioquinol, haloprogin, miconazole nitrate, clotrimazole, metronidazole, tolnaftate, undecylenic acid, iodoquinol, and any combination of any of the foregoing.
  • Suitable skin protectants include, but are not limited to, cocoa butter, dimethicone, petrolatum, white petrolatum, glycerin, shark liver oil, allantoin, and any combination of any of the foregoing.
  • Suitable sunscreen agents include, but are not limited to, ethylhexyl methoxycinnamate, avobenzone, benzophenone-3, octacrylene, titanium dioxide, zinc oxide, and any combination of any of the foregoing.
  • Suitable antioxidants include, but are not limited to, scavengers for lipid free- radicals and peroxyl radicals quenching agents, and any combination of any of the foregoing.
  • Suitable antioxidants include, but are not limited to, tocopherol, BHT, beta carotene, vitamin A, ascorbic acid, ubiquinol, ferulic acid, azelaic acid, thymol, catechin, sinapic acid, EDTA, lactoferrin, rosmariquinone, hydroxytyrosole, sesamol, 2-thioxanthine, nausin, malvin, carvacone, chalcones, glutathione isopropyl ester, xanthine, melanin, guanisone, lophorphyrins, 8-hydroxyxanthine, 2-thioxanthione, vitamin B 12 , plant alkaloids, catalase, quercetin, tyrosine, SOD, cysteine, methi
  • Suitable vitamins include, but are not limited to, vitamin E, vitamin A palmitate, vitamin D, vitamin F, vitamin B 6 , vitamin B 3 vitamin B 12 vitamin C, ascorbyl palmitate, vitamin E acetate, biotin, niacin, DL-panthenol, and any combination of any of the foregoing.
  • a preferred sunscreen agent is a mixture of ethylhexyl methoxycinnamate, butyl methoxydibenzoylmethane, cyclomethicone, phospholipids, and water, and is available as Solarease ® from Collaborative Laboratories, Inc. of East Setauket, NY.
  • Suitable amino acids include, but are not limited to, glycine, serine, and any combination of any of the foregoing.
  • composition preferably includes at least one aesthetic modifying agent.
  • An aesthetic modifying agent is a material which imparts desirable tactile, olfactory, taste or visual properties to the surface to which the composition is applied.
  • the aesthetic modifying agent may be hydrophobic or hydrophilic.
  • the aesthetic modifying agent is preferably hydrophobic and is more preferably an oil, wax, solid or paste.
  • a dispersion of one or more hydrophobic aesthetic modifying agents is preferably prepared before the hydrophobic aesthetic modifying agents are incorporated into the composition.
  • the hydrophobic aesthetic modifying agents may be dispersed into an aqueous phase by methods known in the art, such as by ultra high shear mixing and microfluidization.
  • the final composition may be prepared by mixing the dispersions containing the hydrophobic aesthetic modifying agents with the base composition and any other adjuvants.
  • an aesthetic modifying agent is a mono, di, tri or poly alkyl ester or ether of a di, tri, or polyhydroxy compound, such as ethylene glycol, propylene glycol, glycerin, sorbitol or other polyol compound.
  • esters and ethers include, but are not limited to, saturated and unsaturated, linear and branched vegetable oils, such as soybean oil, babassu oil, castor oil, cottonseed oil, Chinese tallow oil, crambe oil, perilla oil, danish rapeseed oil, rice bran oil, palm oil, palm kernel oil, olive oil, linseed oil, coconut oil, sunflower oil, safflower oil, peanut oil and corn oil.
  • Preferred saturated and unsaturated vegetable oils are those having fatty acid components with 6 to 24 carbon atoms.
  • a more preferred vegetable oil is soybean oil.
  • hydrophobic aesthetic modifying agent is a compound having the formula C n H (2n+2.m) where n is an integer greater than or equal to 6 and m is 0 or an even integer no greater than n.
  • Such compounds include, but are not limited to, saturated and unsaturated, linear, branched, and cyclic hydrocarbon chains.
  • Preferred examples of such compounds include, but are not limited to, mineral oil, petrolatum, permethyl fluids, polybutylenes, and polyisobutylenes.
  • hydrophobic aesthetic modifying agent has the formula
  • R is a saturated or unsaturated, linear, branched or cyclic C,-C 24 alkyl
  • R 2 is hydrogen or a saturated or unsaturated, liner, branched or cyclic C,-C 24 alkyl
  • n is an integer from 0 to 20.
  • aesthetic modifying agents include, but are not limited to, isopropyl palmitate and diisopropyl adipate.
  • silicone may provide lubrication and/or shine to the composition.
  • the silicone is insoluble in water.
  • Suitable water-insoluble silicone materials include, but are not limited to, polyalkylsiloxanes, polyarylsiloxanes, polyalkylarylsiloxanes, polysiloxane gums and polyethersiloxane copolymers. Examples of suitable silicone materials are disclosed in U.S. Patent Nos. 4,788,006; 4,341,799; 4,152,416; 3,964,500; 3,208,911; 4,364,837 and 4,465,619, all of which are incorporated herein by reference.
  • Another suitable hydrophobic material which can be suspended in the composition has the formula
  • R is a saturated or unsaturated, linear, branched or cyclic alkyl having 2 to 24 carbon atoms
  • M (+) is N + R 2 R 3 R 4 R 5 ;
  • R 2 , R 3 and R 4 are hydrogen or a saturated or unsaturated, linear or branched alkyl or hydroxyalkyl having from 1 to 10 carbon atoms;
  • R 5 is a saturated or unsaturated, linear, branched or cyclic alkyl or substituted alkyl having 2 to 24 carbon atoms.
  • An example of such a material is lauramine oleate.
  • Suitable adjuvants for the composition include but are not limited to pH adjusters, emollients, conditioning agents, chelating agents, gelling agents, viscosifiers, colorants, fragrances, odor masking agents, UV stabilizer, preservatives, and any combination of any of the foregoing.
  • Preferred pH adjusters include, but are not limited to, aminomethyl propanol, aminomethylpropane diol, triethanolamine, citric acid, sodium hydroxide, acetic acid, potassium hydroxide, lactic acid, and any combination of any of the foregoing.
  • Suitable conditioning agents include, but are not limited to, cyclomethicone, petrolatum, dimethicone, dimethiconol, silicone, quaternary amines and any combination of any of the foregoing.
  • the composition preferably contains less than about 0.5% by weight of preservatives, based upon 100% weight of total composition. More preferably, the composition contains from about 0.25 to about 0.5% by weight of preservatives, based upon 100% weight of total composition.
  • Deionized water (A) was heated to about 55-60° C.
  • Propylene glycol and sclerotium gum were added to the water and mixed with a Silverson mixer for about 15 minutes. The speed of the mixer was increased as the viscosity of the solution increased.
  • Example 1 carrageenan and glycerin were added to the solution and mixed until the solution was uniform and homogeneous. Germazide ® MPB was then added to the solution and mixed until the solution was uniform and homogeneous to yield the base composition. In Examples 2 and 3, carrageenan was added to the solution and mixed until the solution was uniform and homogeneous. Germazide ® MPB and glycerin were added to the solution and mixed until the solution was uniform and homogeneous to yield the base composition.
  • the sclerotium gum was AmigelTM available from Alban Muller International of Montreuil, France.
  • the sclerotium gum was ClearogelTM CS 11 available from M.M.P., Inc. of South Plainfield, NJ.
  • Germazide ® MPB is a mixture of phenoxy ethanol, chlorphenesin, glycerin, methylparaben, and benzoic acid and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • GermabenTM II is a mixture of propylene glycol, diazolidinyl urea, methylparaben, and propylparaben and is available from Sutton Laboratories of Chatham, NJ.
  • Table 2 contains examples of sclerotium/carregeenum base variants which failed to support surfactant free formulations for topical, oral, nasal, anal, opthalmic or vaginal compositions.
  • Table 3 is an example of sclerotium/carregeenum base variants which failed to support surfactant free formulations for topical, oral, nasal, anal, opthalmic or vaginal compositions.
  • Table 4 is an example of a surfactant-free formulation using a sclerotium/carregeenum base variant which failed.
  • Table 5 is an example of a surfactant-free formulation using a sclerotium/carregeenum base variant which failed.
  • Table 6 is an example of a surfactant-free formulation using a sclerotium/carregeenum base variant which failed.
  • Table 7 is an example of three surfactant-free formulations using sclerotium/ carregeenum base variants which failed.
  • An anti-aging/hype igmentation serum having the formulation of Table 8 below was prepared as follows. All of the ingredients, except the Aculyn 44TM and Chisso beads, were mixed with a propeller mixer until the mixture was smooth and uniform. The Aculyn 44TM and Chisso beads were added to the mixture and mixed until the mixture was smooth and uniform to form the serum. Table 8
  • Cyclomethicone is a mixture of water, cyclopentasiloxane and phospholipids and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • Polysynlane is a mixture of water, hydrogenated polyisobutene, and phospholipids and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • 7 - SanSurf ® C.A.P. is a mixture of water, cetearyl alcohol, and phospholipids and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • CatezomesTM Petrolatum-50 is a mixture of water, petrolatum, and stearamidopropyl dimethylamine stearate and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • 9 - Satin Finish is a mixture of water, phenyl trimethicone, cyclomethicone, dimethiconol, phospholipids, carbomer, and triethanolamine and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • 10 - Retinol CatezomesTM is a mixture of water, retinol, PEG-4, behenamidopropyl dimethylamine behenate and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • Grape Seed Extract is a mixture of glycerin, water, and Vitis Vinifera (grape) seed extract and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • the Advanced Moisture Complex is a mixture of glycerine , water, sodium PCA, urea, trichalese, polyquatemium 51 and sodium hyaluronate and is available from Collaborative Laboratories, Inc. of East Setauket, NY.
  • 14 - Aculyn 44TM is a copolymer of polyurethane and polyethylene glycol or polyetherurethanes and is available from Rohm & Haas Co., Inc. of Philadelphia, PA. 15 - Chisso beads are cellulose acetate and are available from Collaborative Laboratories, Inc. of East Setauket, NY. 16 - Melarrest ® A is a mixture of glycerin, lactic acid, kojic acid, ascorbic acid, and polyvinylpyrrolidone and is available from Collaborative Laboratories, Inc. of East Setauket, NY.

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Abstract

La présente invention concerne une composition de base utile pour préparer une composition sensiblement dépourvue de tensioactifs destinée à une application topique, orale, nasale, anale, ophtalmique ou vaginale. La composition de base comprend de la gomme de sclérotium et du carragaheen. Les formules contenant la composition de base selon la présente invention sont stables à un pH d'environ 3,0 ou moins. Les compositions de base sont également compatibles avec des dispersions cationiques, c'est-à-dire que contrairement aux compositions de l'art antérieur, des mélanges de la composition de base et d'une dispersion cationique ne donnent pas lieu à la formation d'agrégats ou à la séparation de l'eau et des ingrédients hydrophobes de la composition. Une autre forme de réalisation de la présente invention concerne une composition destinée à l'application topique, orale, nasale, ophtalmique ou vaginale qui contient la composition de base selon l'invention et au moins une dispersion comprenant des particules en suspension d'un agent actif hydrophobe, d'un adjuvant hydrophobe ou d'une combinaison de ces derniers. La composition est sensiblement dépourvue de tensioactifs dispersants et les particules en suspension ont un diamètre inférieur à environ 500 nm. La composition contient de préférence au moins une dispersion cationique. Selon une forme de réalisation préférée de l'invention, la composition a pH inférieur à 5 environ, qui est de préférence inférieur à 4 environ et qui plus préférablement encore est inférieur à 3 environ. Une autre forme de réalisation concerne un procédé de préparation de la composition selon la présente invention.
PCT/US2001/009317 2000-03-23 2001-03-23 Compositions de base stables utiles pour preparer des compositions topiques sans tensioactifs WO2001070271A2 (fr)

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EP1297822A2 (fr) * 2001-09-28 2003-04-02 Kosé Corporation Composition cosmétique comprenant de la vitamine A ou un dérivé de celle-ci
WO2004028501A1 (fr) * 2002-09-30 2004-04-08 Johnson & Johnson Consumer France S.A.S. Preparations epaississantes comprenant de la gomme de sclerote et un copolymere
FR2853243A1 (fr) * 2003-04-02 2004-10-08 Blc Thalgo Cosmetic Lab Composition cosmetique ou dermatologique obtenue par lyophilisation de polysaccharides d'origine biotechnologique et de composes actifs d'origine marine
FR2876581A1 (fr) * 2004-10-20 2006-04-21 Interpharm Dev Composition bioadhesive a liberation programmee
EP1875895A1 (fr) 2006-07-07 2008-01-09 Johnson & Johnson Consumer France SAS Compositions à viscosité augmentée comprenant des électrolytes
EP1967180A1 (fr) * 2007-03-06 2008-09-10 Almirall Hermal GmbH Composition topique contenant un agoniste du recepteur de rétinoides
FR2929847A1 (fr) * 2008-04-11 2009-10-16 Dermatologique Uriage Lab Composition dermatologique et/ou cosmetique protectrice de la peau et des muqueuses
FR2929846A1 (fr) * 2008-04-11 2009-10-16 Dermatologiques D Uriage Lab Composition dermatologique et/ou cosmetique protectrice cutanee
FR2931659A1 (fr) * 2008-06-02 2009-12-04 Oreal Procede de prevention de l'apparition de mauvaises odeurs lors d'un procede de deformation permanente des cheveux
FR2936150A1 (fr) * 2008-09-19 2010-03-26 Dermathologiques D Uriage Lab Nouvelles compositions dermatologiques protectrices de la peau et des muqueuses
WO2011012394A1 (fr) * 2009-07-31 2011-02-03 Evonik Stockhausen Gmbh Produit pour la protection de la peau, en particulier contre les substances nocives hydrophobes (lipophiles), ainsi que contre les substances nocives hydrophiles (lipophobes)
FR2983730A1 (fr) * 2011-12-12 2013-06-14 Oreal Composition cosmetique comprenant une combinaison de scleroglucane et de caroube, et utilisations.
CN105879025A (zh) * 2015-11-19 2016-08-24 李锁霞 一种免疫佐剂组合物及其制备方法
FR3061003A1 (fr) * 2016-12-27 2018-06-29 L'oreal Composition cosmetique comprenant une dispersion d'huile dans une phase aqueuse gelifiee
WO2019002929A3 (fr) * 2017-06-27 2019-04-11 Lifestyles Healthcare Pte. Ltd. Lubrifiant naturel
CN115245470A (zh) * 2021-04-27 2022-10-28 山东本真化妆品有限公司 水包油乳液及其在对抗婴儿湿疹中的用途

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WO2001054663A2 (fr) * 2000-01-31 2001-08-02 Collaborative Technologies, Inc. Compositions topiques ne contenant pas de tensioactif et procede de preparation rapide de ces dernieres

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Publication number Priority date Publication date Assignee Title
WO1998044898A1 (fr) * 1997-04-09 1998-10-15 Reckitt & Colman France Compositions depilatoires, leur preparation et leur utilisation
WO2001054663A2 (fr) * 2000-01-31 2001-08-02 Collaborative Technologies, Inc. Compositions topiques ne contenant pas de tensioactif et procede de preparation rapide de ces dernieres

Cited By (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1297822A2 (fr) * 2001-09-28 2003-04-02 Kosé Corporation Composition cosmétique comprenant de la vitamine A ou un dérivé de celle-ci
EP1297822A3 (fr) * 2001-09-28 2003-05-07 Kosé Corporation Composition cosmétique comprenant de la vitamine A ou un dérivé de celle-ci
WO2004028501A1 (fr) * 2002-09-30 2004-04-08 Johnson & Johnson Consumer France S.A.S. Preparations epaississantes comprenant de la gomme de sclerote et un copolymere
FR2853243A1 (fr) * 2003-04-02 2004-10-08 Blc Thalgo Cosmetic Lab Composition cosmetique ou dermatologique obtenue par lyophilisation de polysaccharides d'origine biotechnologique et de composes actifs d'origine marine
EP1466591A1 (fr) * 2003-04-02 2004-10-13 Laboratoires BLC Thalgo Cosmetic Composition cosmétique ou dermatologique obtenue par lyophilisation de polysaccharides d'origine biotechnologique et de composés actifs d'origine marine
WO2006043005A2 (fr) * 2004-10-20 2006-04-27 Interpharm Development Sa Composition bioadhesive a liberation programmee
US20160235715A1 (en) * 2004-10-20 2016-08-18 Care & Pharma Perspectives Sa Pasty Bio-Adhesive Sustained Release Compositions
WO2006043005A3 (fr) * 2004-10-20 2007-04-05 Interpharm Dev Sa Composition bioadhesive a liberation programmee
US10646435B2 (en) * 2004-10-20 2020-05-12 Care & Pharma Perspectives Sa Pasty bio-adhesive sustained release compositions
FR2876581A1 (fr) * 2004-10-20 2006-04-21 Interpharm Dev Composition bioadhesive a liberation programmee
EP1875895A1 (fr) 2006-07-07 2008-01-09 Johnson & Johnson Consumer France SAS Compositions à viscosité augmentée comprenant des électrolytes
EP1967180A1 (fr) * 2007-03-06 2008-09-10 Almirall Hermal GmbH Composition topique contenant un agoniste du recepteur de rétinoides
WO2008107193A1 (fr) * 2007-03-06 2008-09-12 Almirall Hermal Gmbh Composition topique contenant un agoniste du récepteur rétinoïde pour le traitement de l'acné
FR2929846A1 (fr) * 2008-04-11 2009-10-16 Dermatologiques D Uriage Lab Composition dermatologique et/ou cosmetique protectrice cutanee
FR2929847A1 (fr) * 2008-04-11 2009-10-16 Dermatologique Uriage Lab Composition dermatologique et/ou cosmetique protectrice de la peau et des muqueuses
FR2931659A1 (fr) * 2008-06-02 2009-12-04 Oreal Procede de prevention de l'apparition de mauvaises odeurs lors d'un procede de deformation permanente des cheveux
FR2936150A1 (fr) * 2008-09-19 2010-03-26 Dermathologiques D Uriage Lab Nouvelles compositions dermatologiques protectrices de la peau et des muqueuses
WO2011012394A1 (fr) * 2009-07-31 2011-02-03 Evonik Stockhausen Gmbh Produit pour la protection de la peau, en particulier contre les substances nocives hydrophobes (lipophiles), ainsi que contre les substances nocives hydrophiles (lipophobes)
CN102470094A (zh) * 2009-07-31 2012-05-23 赢创斯托豪森有限公司 护肤剂，特别是针对疏水性(亲油性)和针对亲水性(疏油性)有害物质的护肤剂
US8673879B2 (en) 2009-07-31 2014-03-18 Evonik Degussa Gmbh Skin protectant, particularly against hydrophobic (lipophilic) and against hydrophilic (lipophobic) harmful substances
FR2983730A1 (fr) * 2011-12-12 2013-06-14 Oreal Composition cosmetique comprenant une combinaison de scleroglucane et de caroube, et utilisations.
CN105879025A (zh) * 2015-11-19 2016-08-24 李锁霞 一种免疫佐剂组合物及其制备方法
WO2018122165A1 (fr) * 2016-12-27 2018-07-05 L'oreal Composition cosmétique comprenant une dispersion d'huile dans une phase aqueuse gélifiée
FR3061003A1 (fr) * 2016-12-27 2018-06-29 L'oreal Composition cosmetique comprenant une dispersion d'huile dans une phase aqueuse gelifiee
WO2019002929A3 (fr) * 2017-06-27 2019-04-11 Lifestyles Healthcare Pte. Ltd. Lubrifiant naturel
EP3644963A4 (fr) * 2017-06-27 2021-03-10 LifeStyles Healthcare Pte. Ltd. Lubrifiant naturel
CN115245470A (zh) * 2021-04-27 2022-10-28 山东本真化妆品有限公司 水包油乳液及其在对抗婴儿湿疹中的用途

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