Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/31—Brassicaceae or Cruciferae (Mustard family), e.g. broccoli, cabbage or kohlrabi
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/88—Liliopsida (monocotyledons)
  • A61K36/889—Arecaceae, Palmae or Palmaceae (Palm family), e.g. date or coconut palm or palmetto
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/678—Tocopherol, i.e. vitamin E
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/69—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing fluorine
  • A61K8/70—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing fluorine containing perfluoro groups, e.g. perfluoroethers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
  • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
  • A61K8/9783—Angiosperms [Magnoliophyta]
  • A61K8/9789—Magnoliopsida [dicotyledons]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
  • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
  • A61K8/9783—Angiosperms [Magnoliophyta]
  • A61K8/9794—Liliopsida [monocotyledons]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/08—Anti-ageing preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q7/00—Preparations for affecting hair growth
  • A61Q7/02—Preparations for inhibiting or slowing hair growth

Definitions

• the field of this invention concerns cosmetic compositions, particularly skin care related to skin hormonal imbalance.
• Mammalian skin and associated characteristics such as wrinkles and hair growth and loss, are significantly affected by hormones, and the individual skin responsiveness to their levels and ratios, since there is substantial interest in the treatment of skin and its associated characteristics, there have been numerous reports of treatment as palliatives and cures.
• Wrinkles are skin folds and creases caused by dermal thinning and loss of elasticity, which is a result of the aging process and/or exposure to noxious substances and/or physical factors such as UV radiation, all of which adversely affect the skin metabolism. Wrinkles are not a medical condition and as long as the substances employed to treat them are not systemically resorbed and systemically active, the preparations fall into the field of cosmetics.
• Topical and/or systemic application of estrogens of human origin have been shown to increase the skin collagen content and thus increase skin thickness as well as the concentration of skin mucopolysaccharides, which directly reduces the wrinkles' depth.
• giving mammalian estrogens systemically for the sole purpose of reducing the signs of skin aging would not be medically defensible.
• Dermatologists have explored topical estriol and 17- ⁇ -estradiol and found reduction in the wrinkle depth and increased hydration, but also, albeit to a degree, a systemic resorption resulting in a rise in prolactin (Schmidt et al., 1996 Int J Dermatol 35(9):669-74).
• topical mammalian estrogens for skin regeneration although effective, cannot qualify as a cosmetic preparation and are not authorized in cosmetic creams.
• the isoflavones which are found in a variety of plants, as are the flavonoids, were shown to have a much lower effect than the mammal estrogens.
• they are not resorbed systemically (Bayerl and Keil, 2002 Akt Dermatol 28:14-8).
• cosmetics There are many combinations of different ingredients in cosmetics, such as antioxidants, enzymes, phytoestrogens, emollients, humectants, and the like. Their ability to protect the skin and reduce the formation of wrinkles varies with the composition and its ingredients.
• IH idiopathic hirsutism
• IH i.e., excessive male-like pattern hair growth without underlying systemic endocrine pathology.
• IH is characterized either by higher sensitivity of the hair follicle androgen receptors to the androgens or by higher skin androgen levels.
• IH is considered a skin hyperandrogenetic syndrome in the cosmetic category since especially dark excessive facial hair is visible and leads to psychological distress.
• the current treatment is topical and/or systemic pharmacological, combined with mechanical removal including shaving, depilatories, waxing, plucking, laser, intense pulsed light, and/or electrolysis.
• Metformin primarily an antidiabetic treatment, known to be often associated with adverse gastrointestinal effects, is indicated only when IH is concomitant.
• the androgen-targeting drugs improve female IH either by suppression of the male hormone synthesis such as by inhibiting 5- ⁇ reductase conversion of testosterone to dihydrotestosterone (by finasteride), or by blocking the androgen receptors. Finasteride and antiandrogens are contra-indicated in women of childbearing age as they can cause feminization of the male fetus. Cyproterone acetate (CPA), a progestagen with anti-androgenic properties, carries the risk of hypertension, thromboembolism, diabetes mellitus, hypercholesterolemia and endometrial cancer. An antiandrogen of steroidal structure for topical use was recently published (see Labrie et al.).
• Non-steroidal blocking agents of the androgen receptor such as flutamide or bicalutamide, prevent the androgen binding.
• flutamide or bicalutamide When tested topically in male androgenetic alopecia they proved to be substantially systemically resorbed; they are not approved for IH therapy.
• the antiandrogens, RU 58841 and RU 56187, i.e., N-substituted aryl hydantoins or thiohydantoins were tested topically; they are nevertheless converted systemically into a common metabolite, which is strongly antiandrogenic.
• Topical eflornithine inhibits ornithine decarboxylase and thus the conversion of ornithine to putrescine, which regulate the anagen phase of the hair growth.
• IH can be considered a medical condition, but as long as the substances employed to treat IH are not dernally resorbed into the body to become systemically active, the preparations fall into the field of cosmetics.
• a topical cosmetic composition not resorbed systemically, reducing the hair diameter, color and rate of growth and not changing the appearance of the skin would be of benefit to women affected by unwanted body hair.
• a cosmetic preparation for application to the skin for treatment of hormone related characteristics employs substituted highly hydrophobic substances containing an alkarylpolyfluorocarbon, particularly a substituted phenyl, perfluoroacylamino- propanamide, with a physiologically acceptable lower alkanol as a vehicle, in conjunction with solubilizing additives, particularly refined vegetable oils and thereof derived triglyceride fractions, associated with the particular characteristic being treated.
• a facial care cosmetic preparation and its use for reducing or eliminating the female facial hair in hirsutism optionally employs a moisturizing agent.
• a facial care cosmetic preparation and its use for reducing wrinkles employs, in addition to the above, a mixture of natural extracts or fractions thereof and optionally conventional additive(s) particularly antioxidants.
• the preparations are substantially transparent non-irritating liquids which topically applied are rapidly resorbed into the skin to provide for the reduction of wrinkles and/or hirsutism.
• the preparations are not appreciably systemically resorbed.
• Facial care cosmetic preparations comprise an effective amount of a highly hydrophobic substance comprising an alkaryl polyfluorocarbon, particularly a substituted phenyl, perfluoroacylaminopropanamide, in conjunction with other components providing for auxiliary benefits and solubility, a lower alkanol and at least one refined oil, fraction thereof, and optionally an antioxidant.
• a highly hydrophobic substance comprising an alkaryl polyfluorocarbon, particularly a substituted phenyl, perfluoroacylaminopropanamide, in conjunction with other components providing for auxiliary benefits and solubility, a lower alkanol and at least one refined oil, fraction thereof, and optionally an antioxidant.
• the vehicle will comprise a major amount of at least one refined vegetable oil and an oil triglyceride fraction and a minor amount of a physiologically acceptable alkanol of from 2-3 carbon atoms.
• the refined oil and its triglyceridic fractions will be present in major amount in the facial cosmetic composition, generally at least about 50 wt. %, more usually at least about 60 wt. %, and may be up to about 95 wt. %.
• the refined oil will be vegetable oils such as grape seed, rapeseed, soybean oils and at least one of oil fractions of Cocos nucifera (C 6-10 triglycerides) and/or Glycine soja (soybean oil, medium chain triglycerides).
• the composition will comprise at least one, usually a combination, of plant natural extracts or fractions thereof, or synthetic composition equivalents, at least one antioxidant, but may be a mixture of two or more antioxidants, e.g., vitamins, and, as appropriate, other additives.
• the antioxidant will usually be tocopherol and optionally a moisturizing agent will be included.
• the preparations are at least substantially homogeneous. They are readily applied to the skin as a substantially transparent liquid where it does not cause irritation.
• the compositions can be used safely, repeatedly.
• the preparations are not resorbed systemically.
• the alkaryl polyfluorocarbon compound employed will preferably be a substituted phenyl, perfluoroacylaminopropanamide. For the most part, the phenyl substituents will be 4-nitro-3-trifluoromethyl.
• Compounds of particular interest are 4-nitro-3-trifluoromethylphenyl substituted perfluoroacylaminopropanamide, wherein the perfluoroacyl group is of from 2-3 carbon atoms and said propanamide group is substituted at the 2-carbon atom with at least one of hydroxyl and methyl.
• the compounds may or may not have one or more stereoisomeric centers.
• the compounds may be used as racemic mixtures or be resolved in their enantiomers and used as enantiomers.
• the subject compounds can be prepared in accordance with conventional ways, varying the particular procedure based on the particular side groups.
• a suitable synthetic method is described in Seligson et al. Drug Dev. Res. 59:292-306.
• the subject composition for wrinkle reduction employs effective amounts of a variety of physiologically acceptable natural extracts or fractions thereof, where these compositions have salutary effects for the skin and/or can serve in providing for a substantially uniform composition.
• Extracts that find application include Japanese knotweed, frankincense, non-saponifiable fractions from vegetable oils such as Brassica olifera (turnip, rape) and Glycine soja fractions, as a supply of phytoestrogens.
• free radical scavengers are used, either synthetic or natural, particularly the antioxidant vitamins, Vitamins A and E.
• moisturizing agents include high molecular weight fatty acid esters of at least about 18 carbon atoms and up to 40 carbon atoms.
• Various types of moisturizers can be used that fall into a variety of classes.
• Occlusive ingredients include petrolatum, mineral oil, paraffin, squalene, vegetable fats (cocoa butter), animal fats (lanolin), lanolin acid, stearic acid, lanolin alcohol, cetyl alcohol, phospholipids, silicones, etc.
• Humectants include glycerin, propylene glycol, urea, sodium lactate, sorbitol, pyrrolidone carboxylic acid, etc.
• Emollients include octyl dodecanol, hexyl dodecanol, oleyl alcohol, oleyl oleate, octyl stearate, PEG-7, glycerol cocoate, myristyl myristate, isopropyl myristate, stearyl isononanoate, isopropyl palmitate, or isopropyl stearate.
• Physiologically acceptable preservatives may also be used in the compositions, primarily for storage. purposes to inhibit the oxidation of the susceptible ingredients, e.g., BHT, BHA (a mixture of the isomers 3-tert-butyl-4-hydroxyanisole and 2-tert-butyl-4-hydroxyanisole), TBHQ (tert-butylhydroquinone), ethoxyquin (6-ethoxy-1,2-dihydro-2,2,4-trimethyl quinoline), propyl gallate (gallic acid, propyl ester), tocopherol, rosemary extract, etc.
• BHT susceptible ingredients
• BHA a mixture of the isomers 3-tert-butyl-4-hydroxyanisole and 2-tert-butyl-4-hydroxyanisole
• TBHQ tert-butylhydroquinone
• ethoxyquin 6-ethoxy-1,2-dihydro-2,2,4-trimethyl quinoline
• propyl gallate gallic acid, propyl
• compositions having substantially the same properties for the purpose of these compositions may be substituted for the specific compositions employed.
• These components will be used in an effective amount to provide the skin improvement and particularly the reduction in wrinkles or any hair except scalp hair.
• the subject compositions can be prepared using various protocols and orders of addition.
• a first mixture (A) is prepared in the polar solvent heated to a range of about 50 to 80° C., preferably 60° C. to which the natural extract components is added sequentially and stirred until dissolved, e.g., resveratrol followed by the Olibanum extract. The mixture is stirred until completely homogenous and set aside.
• Cocos nucifera oil triglyceride fraction (refined) at a mildly elevated temperature, generally in the range of about 35-50° C., is added the phenyl-perfluoroacylaminopropanamide and the mixture agitated for sufficient time to provide homogeneity, usually 20 minutes is adequate. To this mixture is then added the vegetable oil and the antioxidant preservative, followed by the vitamins. After stirring until the mixture appears homogeneous, the previously prepared mixture (A) is added dropwise with agitation to provide a concentrate that can be stored at below room temperature in a dark container.
• the phenyl-perfluoroacylaminopropanamide is added to the polar solvent and the mixture agitated for sufficient time to provide homogeneity, usually about 20 minutes.
• the vegetable oils and their triglyceride fractions as appropriate, the antioxidant preservative, followed optionally by the antioxidant, e.g., tocopherol.
• a moisturizing agent is desired, it is added slowly, e.g., dropwise, with agitation to provide a final mixture that can be stored at below room temperature in a dark container.
• compositions can be prepared having fewer than all of the components and the components added subsequently.
• the subject formulations are usually at least substantially free of hydroxyacids and in the case of the wrinkle composition also free of monocarboxylic acid esters finding use in other cosmetic compositions.
• Either the extracts or fractions thereof or the known active ingredient(s) may be used. Because of the economics, usually it will be preferred to use the natural extracts as the source of the active ingredient(s), rather than a substantially pure form, either obtained from a natural source or synthetic.
• the form of the extract used, when the active ingredient is known, will have at least about 50 wt. % of the active ingredient, and may have 70 wt. % or more.
• the equivalent composition obtained from a different source will have at least about 50%, usually at least about 70%, of the individual or mixture of the major component(s) of the natural extract or fraction thereof.
• the phenyl-polyfluoroacylaminopropanamides are described in U.S. Pat. No. 6,184,249.
• the active compounds that may be employed are substances, which affect the skin androgen receptors but are not appreciably resorbed systemically. Such compounds are exemplified by 2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl) phenyl]-3-(2,2,2-trifluoroacetylamino) propanamide(fluridil).
• the extract will usually have at least about 90% of trans-resveratrol (CAS No.: [501-36-0], 3,4′,5-trihydroxy-trans-stilbene, as a glycon (Piceid). Any other source of resveratrol may be used that provides at least a substantially equivalent amount of resveratrol. Synthetically prepared resveratrol is also acceptable.
• the extract from frankincense, Boswellia serrata is a terpenoid mixture having from about 60-70% of triterpenes, the major portion of which are boswellic acids, of which at least 10 to 30% (wt/wt) is ⁇ -boswellic acid, 5 to 20% (wt/wt) is acetyl- ⁇ -boswellic acid, 5 to 20% (wt/wt) is 11-keto- ⁇ -boswellic acid and 5 to 20% (wt/wt) is acetyl-11-keto- ⁇ -boswellic acid (CAS No. [8050-07-5]).
• boswellic acids of which at least 10 to 30% (wt/wt) is ⁇ -boswellic acid, 5 to 20% (wt/wt) is acetyl- ⁇ -boswellic acid, 5 to 20% (wt/wt) is 11-keto- ⁇ -boswellic acid and 5 to 20% (
• the phytoestrogens are readily available as a fraction derived from the vegetable oils rape- seed ( Brassica ) and/or soya ( Glycine soja ).
• the unsaponifiable fraction (CAS No. [91770-67-1]) of the appropriate vegetable oil is used as a source of phytoestrogens and will be substantially free of esters.
• the grape seed oil ( Vitis vinifera ) or the soybean oil is primarily a mixture of saturated and unsaturated fatty acids having as its main constituents linoleic and oleic acids (>80%). These acids could be used independently of the other ingredients or the mixture prepared synthetically. They are used in their refined form.
• Coconut oil ( Cocos nucifera ) provides primarily medium chain triglycerides where the acids are primarily C 6-10 saturated fatty acids, particularly caprylic and capric (CAS [73398-61-5]). It is used in its refined form.
• antioxidants may be used that are conventionally found in cosmetic formulations. Vitamins A and E in their commercially available forms are favored, since they also are known to provide salutary physiological effects on the skin, but other antioxidants may also be employed, such as compounds having phenolic hydroxy functions, ascorbic acid and its derivatives/esters; beta-carotene; catechins; curcumin; ferulic acid derivatives (e.g., ethyl ferulate or sodium ferulate); gallic acid derivatives (e.g., propyl gallate); lycopene; reductic acid; rosmarinic acid; tannic acid; tetrahydrocurcumin; tocopherol derivatives; uric acid; or any mixtures thereof
• Other suitable antioxidants are those having one or more thiol (—SH) functions, in either reduced or non-reduced form, such as glutathione, lipoic acid, thioglycolic acid, and other sulfhydryl compounds.
• the antioxidant may be inorganic, such as bisulfites, metabisulfites, sulfites, or other inorganic salts and acids containing sulfur. These antioxidants may be used in partial or complete replacement of the vitamins and the antioxidant preservative, and for the vitamins, usually partial if at all, and will generally be present in less than 50% of the amount indicated for the vitamins, usually less than 30% indicated for the vitamins, generally being present to up to about 2 parts, more usually not more than about I part, while for the antioxidant preservative, they may be used as a complete replacement.
• alkanol is used of from 2-3 carbon atoms, e.g., ethanol, propylene glycol and isopropanol, particularly the latter in an amount to provide at least substantial homogeneity to the formulation.
• preservatives in minor amount, usually not more than about 3 different preservatives.
• the antioxidants described above may serve as preservatives. More conventionally BHT, BHA, TBHQ, ethoxyquin, propyl gallate, and rosemary extract is employed.
• a particularly important aspect of this invention is the preferred formulation as described in the experimental section.
• the ingredient combination is formulated to solubilize all substances in a cosmetically acceptable medium.
• Several components but particularly the extracts from Boswellia serrata, as well as the Japanese knotweed extract, are highly insoluble in customary systems.
• the combination forms a homogenous solution in the subject mixture of medium chain triglycerides (caprylic/capric triglycerides) with fractions of purified grape seed oil and the addition of a minimal amount (less than 10%) of rubbing alcohol (isopropanol).
• the resulting mixture is a viscous liquid of oily appearance, which nevertheless becomes invisible on the skin within a short time after its topical application: the skin surface is not oily and the overall effect is that of high skin pliability and smoothness.
• additives and adjuvants are conventional in the cosmetic, pharmaceutical or dermatological field, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, solvents, fragrances, fillers, bactericides, odor absorbers and dyestuffs or colorants.
• the amounts of these various additives and adjuvants are those conventionally used in the field, and, for example, range from 0.01% to 10% of the total weight of the composition.
• Emulsifiers that may be used include glyceryl stearate, polysorbate 60, PEG-6/PEG-32/glycol stearate mixture, etc.
• Hydrophilic gelling agents include carboxyvinyl polymers (carbomer), acrylic copolymers such as acrylate/alkylacrylate copolymers, polyacrylamides, polysaccharides, such as hydroxypropylcellulose, natural gums and clays, and, as lipophilic gelling agents, representative are the modified clays such as bentones, fatty acid metal salts such as aluminum stearates and hydrophobic silica, or ethylcellulose and polyethylene.
• carboxyvinyl polymers carboxyvinyl polymers (carbomer), acrylic copolymers such as acrylate/alkylacrylate copolymers, polyacrylamides, polysaccharides, such as hydroxypropylcellulose, natural gums and clays, and, as lipophilic gelling agents, representative are the modified clays such as bentones, fatty acid metal salts such as aluminum stearates and hydrophobic silica, or ethylcellulose and polyethylene.
• Suitable fatty alcohols and acids include those compounds having from 10 to 20 carbon atoms. Especially preferred are such compounds such as cetyl, myristyl, palmitic and stearyl acids and alcohols.
• the polyols which may serve as emollients, are linear and branched chain alkyl polyhydroxyl compounds.
• propylene glycol, sorbitol and glycerin are preferred.
• polymeric polyols such as polypropylene glycol and polyethylene glycol. Butylene and propylene glycol are also useful.
• hydrocarbons which may serve as emollients, are those having hydrocarbon chains anywhere from 12 to 30 carbon atoms. Specific examples include mineral oil, petroleum jelly, squalene, and isoparaffins.
• thickeners are also categories of functional ingredients within the cosmetic compositions of the present invention.
• a thickener will usually be present in amounts anywhere from 0.1 to 20% by weight, preferably from about 0.5% to 10% by weight of the composition.
• Exemplary thickeners are cross-linked polyacrylate materials available under the trademark Carbopol. Gums may be employed such as xanthan, carrageenan, gelatin, karaya, pectin and locust beans gum. Under certain circumstances the thickening function may be accomplished by a material also serving as a silicone or emollient. For instance, silicone gums in excess of 10 centistokes and esters such as glycerol stearate have dual functionality.
• Powders may be incorporated into the cosmetic composition of the invention. These powders include chalk, talc, kaolin, starch, smectite clays, chemically modified magnesium aluminum silicate, organically modified montmorillonite clay, hydrated aluminum silicate, fumed silica, aluminum starch octenyl succinate and mixtures thereof.
• adjunct minor components may also be incorporated into the cosmetic compositions. These ingredients may include coloring agents, opacifiers and perfumes. Amounts of these other adjunct minor components may range anywhere from 0.001% up to 20% by weight of the composition.
• the subject compositions will be stored in containers that may be protected from light, by being opaque to incident light and may be sealed to minimize the oxygen present in the empty space. In light of the compositions cosmetic nature, the containers will be attractive, may have various shapes and come in a variety of sizes.
• the subject compositions may be supplied in conjunction with other skin formulations, as appropriate.
• the subject preferred compositions are characterized as being transparent liquids when applied to the skin. They are not absorbed systemically to any degree that can be found in the vascular system. They are found to have none to very low acute irritation potential in standard tests, and are safe for use with humans or other mammals. They have antimicrobial activity against a variety of organisms, inhibiting the growth of microorganisms in the composition.
• Mapping and depth measurement of periocular/temporal wrinkles by laser profilometry shows a smoothing effect on the cutaneous microrelief, revealed by a decrease in the median depth of microrelief furrows and a significant decrease in the complexity in a majority of the subjects.
• the volume of the wrinkles as measured by laser profilometry will be reduced in at least about 60 to 80, more usually at least about 70% of the subjects, and the depth of the wrinkle is reduced about 8-15 %, and most usually by at least 10%.
• Example 1 In a clinical study employing the composition of Example 1 (although the compositions of Examples 8 and 9 would be anticipated to act at least as effectively), in 9 out of ten facially hirsute women who used in absence of any other treatment the composition herein described, as 2 ml massaged once a day into the affected areas, a substantial thinning, loss of color and reduced face and neck hair growth were documented.
• vitamin E DL- ⁇ -tocopherol acetate
• 3,4-dihydro-2, 5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-2H-1-benzopyran-6-ol acetate 3.000 IU CAS No.: [7695-91-2]
• vitamin A retinol palmitate
• the test is based on inoculating the product with 5 strains, i.e., S. aureus, P. aeruginosa, E. coli, C. albicans and A. niger, incubation at 20° C. with the counts performed at 7, 14, 21 and 28 days.
• the antimicrobial (“preserving”) efficiency of the product is considered positive when at day 14 the bacterial counts (measured by concentration CFU/g) are reduced by at least 2 logs and in the following 14 days continue to drop or stay equal to the starting counts. For yeasts/moulds the counts must be equal or lower at day 14 and 28, compared to the initial count.
• the product thus meets the USP XXV criteria as efficiently preserving the bacterial and fungal sterility.
• the test is standard to detect possible cytogenetic damage, which induces the formation of micronuclei containing lagging chromosomes or their fragments.
• the preparation was administered topically to three dose groups (0.5, 1.5 and 4.5 ml/kg, 5 male and 5 female per group) of SKH-1 mice, once daily for 28 days.
• Peripheral blood was sampled at 36 and 48 hours after the last administration and the reticulocytes were analyzed for the presence or absence of micronuclei after staining.
• the composition intended for wrinkles was evaluated as an open study on 11 adult volunteers, after a single application to the skin in the scapular area, under a semi-occlusive patch for 48 hours.
• the observations aimed at detecting erythema+edema were used to calculate the acute irritation index (M.I.I.) according to the standard formula to rank the cosmetic product according to the scale: M.I.I ⁇ 0.20 Non-irritant (NI); 0.20-M.I.I ⁇ 0.50 Slightly irritant (SI); 0.50-M.I.I ⁇ 1 Moderately irritant (MI); M.I.I ⁇ 1 Irritant (I).
• the product was classified as NI, non-irritant.
• the data consists of complexity of the surface (or visual impact of a wrinkle in %),—maximum depth of the wrinkle (in mm),—volume of the wrinkle (in mm 3 ) and is analyzed by a paired t-test with significance limit of p ⁇ 0.05.
• the product has shown a distinct tendency to reduce the wrinkles after 28 days and after 56 days.
• the objective findings were paralleled with the subjective reports of the volunteers.
• Final formulation is prepared by addition of 40 g of grape seed oil to the stock concentrate, to make 100 g of “CARE: the solution for the face” product.
• vitamin E DL- ⁇ -tocopherol acetate
• 3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12 trimethyltridecyl)-2H-1-benzopyran-6-ol acetate 3.000 IU CAS No.: [7695-91-2]
• compositions provide for improved skin care.
• the compositions serve in reducing wrinkles and the ravages of age, sun and toxic substances, including smoking, and reduce unwanted facial hair growth.
• the compositions are safe, using components that have been shown to be acceptable to humans.
• a substantially homogeneous mixture is obtained that is readily applied to the skin to provide a transparent layer.
• the subject compositions can be used repeatedly without irritation to the skin or damage to the skin.

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• 2006
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• 2008
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