MX2008002745A - Novel skin care compositions - Google Patents
Novel skin care compositionsInfo
- Publication number
- MX2008002745A MX2008002745A MXMX/A/2008/002745A MX2008002745A MX2008002745A MX 2008002745 A MX2008002745 A MX 2008002745A MX 2008002745 A MX2008002745 A MX 2008002745A MX 2008002745 A MX2008002745 A MX 2008002745A
- Authority
- MX
- Mexico
- Prior art keywords
- parts
- skin
- composition
- refined
- fraction
- Prior art date
Links
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- 235000019172 retinyl palmitate Nutrition 0.000 description 1
- 239000011769 retinyl palmitate Substances 0.000 description 1
- 229940092258 rosemary extract Drugs 0.000 description 1
- 235000020748 rosemary extract Nutrition 0.000 description 1
- 239000001233 rosmarinus officinalis l. extract Substances 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- BPQQTUXANYXVAA-UHFFFAOYSA-N silicate Chemical compound [O-][Si]([O-])([O-])[O-] BPQQTUXANYXVAA-UHFFFAOYSA-N 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 230000036560 skin regeneration Effects 0.000 description 1
- 230000000391 smoking Effects 0.000 description 1
- 239000001540 sodium lactate Substances 0.000 description 1
- 235000011088 sodium lactate Nutrition 0.000 description 1
- 230000003381 solubilizing Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-M stearate Chemical compound CCCCCCCCCCCCCCCCCC([O-])=O QIQXTHQIDYTFRH-UHFFFAOYSA-M 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 231100000803 sterility Toxicity 0.000 description 1
- 230000004936 stimulating Effects 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 229940086735 succinate Drugs 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
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- 201000010874 syndrome Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000002194 synthesizing Effects 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 235000015523 tannic acid Nutrition 0.000 description 1
- 229920002258 tannic acid Polymers 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- 150000003505 terpenes Chemical class 0.000 description 1
- 230000001225 therapeutic Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229960002663 thioctic acid Drugs 0.000 description 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 150000003611 tocopherol derivatives Chemical class 0.000 description 1
- 239000003440 toxic substance Substances 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 229960000200 ulipristal Drugs 0.000 description 1
- OOLLAFOLCSJHRE-ZHAKMVSLSA-N ulipristal acetate Chemical compound C1=CC(N(C)C)=CC=C1[C@@H]1C2=C3CCC(=O)C=C3CC[C@H]2[C@H](CC[C@]2(OC(C)=O)C(C)=O)[C@]2(C)C1 OOLLAFOLCSJHRE-ZHAKMVSLSA-N 0.000 description 1
- 235000021122 unsaturated fatty acids Nutrition 0.000 description 1
- 150000004670 unsaturated fatty acids Chemical class 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 235000019871 vegetable fat Nutrition 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 229950004578 vitamin A palmitate Drugs 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 150000003700 vitamin C derivatives Chemical class 0.000 description 1
- 238000004018 waxing Methods 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 230000005186 women's health Effects 0.000 description 1
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- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 1
Abstract
Skin care compositions are provided comprising a highly hydrophobic substance, an alkaryl polyfluorocarbon, particularly a substituted phenyl-polyfluoroacylamino propanamide, an alkanol and refined oils and the oil triglyceride fractions in sufficient amount to provide substantial homogeneity. When employed for hirsutism, optionally antioxidants and moisturizer are added. For use against wrinkles, additionally vitamins, antioxidants and a mixture of extracts of naturally occurring substances are present.
Description
NEW COMPOSITIONS FOR SKIN CARE FIELD OF THE INVENTION The field of this invention relates to cosmetic compositions, particularly skin care related to a hormonal skin imbalance. BACKGROUND OF THE INVENTION The skin and associated characteristics of mammals, such as wrinkles and growth and hair loss, are significantly affected by hormones, and the skin responsiveness of individuals to their levels and indices, and from the substantial interest in the Treatment of the skin and its associated characteristics, numerous reports of treatments as palliative and cures have emerged. 1. Wrinkle reduction: Wrinkles are folds and lines in the skin caused by thinning of the skin and loss of elasticity, which is the result of the aging process and / or exposure to harmful substances and / or physical factors such as UV radiation, all of which adversely affect the skin's metabolism. Wrinkles are not a medical condition and as long as the substances used to treat them are not systematically reabsorbed and are systematically active, the preparations fall within the field of cosmetics. There are many claims towards inventions to reduce or eliminate non-surgical wrinkles, but Ref .: 190425
there are few systematic studies that support such claims. The amount of available facial creams containing a variety of substances is plethora, many of which are either inefficient or induce side effects at efficacy levels. Thus, it is known that a topical vitamin C, tretinoin, or isotretinoin, while transiently improving the wrinkles caused by aging and photodamage, have a considerable incidence of irritation. The induction of paralysis of muscle fibers for cosmetic purposes by substances that block neuromuscular junctions is not physiologically acceptable and has its own particular toxicity. The topical and / or systemic application of estrogens of human origin has been shown to increase the collagen content in the skin and thereby increase the thickness of the skin as well as the mucopolysaccharide concentration of the skin, which directly reduces the depth of the skin. wrinkles However, providing mammalian estrogens systematically for the sole purpose of reducing the signs of skin aging would not be medically defensible. Demartologists have explored estriol and topical 17-ß-estradiol and have found a reduction in wrinkle depth and increased hydration, but also, notwithstanding to a degree, a systemic reabsorption that results in an increase in prolactin ( Schmidt et al., 1996
Int J Dermatol 35 (9): 669-74). Therefore, topical mammalian estrogens for skin regeneration, even when effective, can not be qualified as a cosmetic preparation and are not authorized in cosmetic creams. Certain phytoestrogens, especially isoflavones, which are found in a variety of plants, such as flavonoids, have been shown to have a much smaller effect than mammalian estrogens. However, in a topical application they are not systematically reabsorbed (Bayer and Keil, 2002 Akt Dermatol 28: 14-8). There are many combinations of different ingredients in cosmetics, such as antioxidants, enzymes, phytoestrogens, emollients, humectants, and the like. Their abilities to protect the skin and reduce the formation of wrinkles vary with the composition and its ingredients. There is, therefore, a need for an effective and safe cosmetic that reduces wrinkles, has minimal or no side effects and does not result in a change in skin coloration, for example, that is substantially transparent when applied 2. Compositions that affect the growth of female facial hair (idiopathic hirsutism): Approximately eight percent of women are affected by idiopathic hirsutism (IH), in this case, excessive hair growth with a
pattern similar to that of man without an underlying systemic endocrine pathology. The HI is considered a hyperandrogenic skin syndrome in the cosmetic category since especially the excessively dark facial hair is visible and leads to psychological distress. The current treatment is pharmacological by topic and / or systemic, combined with a mechanical elimination that includes shaving, waxing, plucking, laser, intense pulse light, and / or electrolysis. Metformin, mainly in an antidiabetic treatment, known to be frequently associated with adverse gastrointestinal effects, is indicated only when IH is concomitant. Androgen-targeted drugs improve female HI by either suppressing the synthesis of the male hormone such as by inhibiting the conversion of 5-a reductase from testosterone to dihydrotestosterone (by finasteride), or by blocking androgen receptors. Finasteride and antiandrogens are contraindicated in women during pregnancy because they can cause the feminization of male fetuses. Cyproterone acetate (CPA), a progestogen with antiandrogenic properties, carries the risk of hypertension, thromboembolism, diabetes mellitus, hypercholesterolemia and endometrial cancer. Recently, an antiandrogen with a steroid structure was published for topical use (see Labrie et al.).
spheroids of the androgen receptor, such as flutamide or bicalutamide, prevent androgen ligation. When evaluated topically in male androgenetic alopecia they proved to be substantially systematically reabsorbed; they are not approved for an IH therapy. The antiandrogens, RU 58841 and RU 56187, in this case, aryl hydantoins or N-substituted thiohydantoins were evaluated topically; however, they are converted systemically into a common metabolite, which is strongly antiandrogenic. The topical eflornithine inhibits ornithine decarboxylase and thus the conversion of ornithine to putrescine, which regulates the anagen phase of hair growth. Mechanical depilation by clamping and epilators can potentially exacerbate IH by stimulating the growth of coarser and rougher hair, which makes subsequent treatments more difficult and occasionally induces folliculitis and trauma to the hair shaft and skin. IH can be considered a medical condition, but as long as the substances used to treat the IH are not reabsorbed dermally in the body to become systemically active, the preparations fall within the field of cosmetics. A cosmetic topical composition that is not systemically reabsorbed, reduces the diameter, color and speed of hair growth and does not change the appearance
of the skin would be beneficial for women affected by unwanted body hair. Relevant Literature For wrinkles, the use of natural extracts and their fractions have found wide use in cosmetics: resveratrol, WO04 / 026, 222, WO01 / 30314; Soy glycine,
US Patent Applications nos. 2004/0191350,
2005/0048105, 2005/0112153; grapeseed oil, O01 / 17495; Boswellia serra ta, application for North American Patent no. 2005/01213559 and WO00 / 0578393; and Cocos nucífera, North American Patent no. 6,551,656. Fluridil has previously been employed in useful formulations in a variety of conditions where its effect on skin receptors is desirable (US Patent No. 6,184,249, which is specifically incorporated herein by reference,
Sovak et al., 2001 WO 01/58854; 2002 Dermatol Surg 28: 678-85;
Seligson et al., 2003 Drug Dev Res 59: 292-306). Relevant Literature References of interest for treating wrinkles include US Patents Nos. 5,889,054, 6,139,829, and
1,180,133. A discussion on hormone substitution is found in Sator et al., 2004 Exp Dermatol 13 Suppl 4: 36-40.
For the IH, see Goodheart H., "Hirsutism: Pathogenesis and Causes," Women's Health Prim Care 2000, 3: 329-37; Azziz R., "The evaluation and management of hirsutism," Obstet
Gynecol 2003, 101: 995-1007; Shenenberger D, Utecht L., "Removal of unwanted facial hair," Am Fam Physician 2002, 66: 1907-11; and Dawber R. P., "Guidance for the management of hirsutism," Current Medical Research and Opinion, 2005, 21: 1227-1234 (8). Also, D. Cousty-Berlin et al., "Preliminary Pharmacokinetics and Metabolism of Novel Non-steroidal Antiandrogens in the Rat: Relation of their Systemic Activity to the Formation of a Common Metabolite," Steroid Biochem Molec Biol 1994, 51: 47- 55, and Labrie et al., "Topical antiandrogenic steroids," US 2004/0224935, Nov. 11, 2004. SUMMARY OF THE INVENTION A cosmetic preparation to be applied to the skin for the treatment of hormone-related characteristics employs substituted highly hydrophobic substances that they contain an alkarylpolyfluorocarbon, particularly a perfluoroacylamino-propanamide, substituted phenyl, with a physiologically acceptable lower alkanol as a carrier, together with solubilizing additives, particularly refined vegetable oils and triglyceride fractions derived therefrom, associated with the characteristic being treated . A cosmetic facial care preparation and its use to reduce or eliminate female facial hair in hirsutism optionally employs a wetting agent. A cosmetic preparation of facial care and its use to reduce wrinkles uses, in addition to the above, a
mixture of natural extracts or fractions thereof and optionally additive (s) particularly antioxidants. The preparations are substantially non-irritating transparent liquids which, applied by topic, are rapidly reabsorbed into the skin to provide wrinkle reduction and / or hirsutism. The preparations are not reabsorbed appreciably systemically. DETAILED DESCRIPTION OF THE INVENTION Cosmetic facial care preparations are provided. These compositions comprise an effective amount of a highly hydrophobic substance comprising an alkaryl polyfluorocarbon, particularly a perfluoroacylaminopropanamide, substituted phenyl, together with other components that provide benefits and solubility auxiliary, a lower alkanol and at least one refined oil, fraction thereof , and optionally an antioxidant. (By effective amount is considered a sufficient amount to provide a therapeutic effect). The vehicle will comprise a greater amount of at least one refined vegetable oil and a triglyceride fraction of oil and a minor fraction of a physiologically acceptable alkanol of from 2-3 carbon atoms. The refined oil and its triglyceride fractions will be present in greater amount in the facial cosmetic composition, generally at least about 50% by weight, more usually at
less 60% by weight and can be up to about 95% - by weight. The refined oil will be vegetable oils such as grapeseed, rapeseed, soybean oils and at least one of the fractions of cocoa nucifera oil (triglycerides C6-? O) and / or glycine soy (soybean oil, triglycerides of medium chain). For wrinkle reduction, the composition will comprise at least, usually a combination, natural plant extracts or fractions thereof, or equivalent synthetic compositions, at least one antioxidant, but may be a mixture of two or more antioxidants, by example, vitamins, and, as appropriate, other additives. For facial hair reduction, the antioxidant will usually be tocopherol and optionally a moisturizing agent will be included. The preparations are at least substantially homogeneous. They are quickly 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 reabsorbed systemically. The alkaryl polyfluorocarbon compound employed will preferably be a perfluoroacylaminopropanamide, substituted phenyl. For the most part, the phenyl substituents will be 4-nitro-3-trifluoromethyl. Compounds of particular interest are perfluoroacylaminopropanamide 4-nitro-3-trifluoromethylphenyl
substituted, wherein the perfluoroacyl group is from 2-3 carbon atoms and the propanamide group is substituted on the carbon atom 2 with at least one of the hydroxyl and methyl. Compounds of particular interest are also described in U.S. 6,184,249 and 6,472,415, referenced above. In particular, these compounds comprise substituted phenylalanines comprising a 2-hydroxyl, 2-methylpropionyl group and a polyfluoroamido. These compounds include those of
Wherein: X is nitro (N02), cyano (CN), or halogen, preferably F, Cl and Br, more preferably fluorine and chlorine, most preferably fluorine; V is CX3, wherein X is halogen preferably F, Cl and Br, more preferably fluorine and chlorine, and V is most preferably CF3; Z is (CF2) nCF3 wherein n is from 0 to 9, preferably from
0 to 5, most preferably 0 to 2. These compounds specifically bind to the androgen receptor and have activity in blocking hormone receptors, preferably
hormone receptors in the decrease of androgen receptors (eg, androgen receptors) of skin on the surface of cells and a low resorption when they are applied by topics, while they are active topically. These compounds may or may not have one or more stereoisomeric centers. The compounds can be used as racemic mixtures or be resolved in their enantiomers and used as enantiomers. These subject compounds can be prepared in accordance with conventional manners, the particular process varying based on the particular side groups. An appropriate 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, wherein these compositions have healthy effects for the skin and / or can function to provide a substantially uniform composition. Extracts that find application include the Japanese polygon, incense (frankincense), fractions that can not saponify from vegetable oils such as Brassica olifera (turnip, wedge) and soy glycine fractions, as a source of phytoestrogens. Additionally, free radical scavengers are used, whether synthetic or natural, particularly antioxidant vitamins,
Vitamins A and E. For hirsutism, wetting agents include high molecular weight fatty acid esters of at least 18 carbon atoms and up to 40 carbon atoms. Various types of humectants can be used which 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. The humectants include glycerin, propylene glycol, urea, sodium lactate, sorbitol, pyrrolidone carboxylic acid, etc. Emollients include octyl dodecanol, hexyl dodecanol, oleyl alcohol, oleyl oleate, otyl stearate, PEG-7, glyceryl cocoate, myristyl myristate, isopropyl myristate, isyl isononanoate, isopropyl palmitate, or isopropyl stearate. Pharmaceutically acceptable preservatives may also be used in the compositions, primarily for storage purposes to inhibit the oxidation of the susceptible ingredients, for example, BHT, BHA (a mixture of the 3-tert-butyl-4-hydroxyanisole and 2-tert isomers). -butyl-4-hydroxyanisole), TBHQ (tert-butylhydroquinone), ethoxyquin (quinoline 6-ethoxy-l, 2-dihydro-2, 2,4-trimethyl), propyl gallate (gallic acid, propyl ester), tocopherol , extract of
rosemary, etc. To vary the grades, other substances that have substantially the same properties for the purposes of these compositions can be substituted for the specific compositions employed. These components will be used in an effective amount to provide an improvement in the skin and particularly in the reduction of wrinkles or in any hair except scalp. The following table indicates the categories of materials and intervals in the care of the skin care reducing composition. Table 1.
The following table indicates the categories of materials and intervals in the hirsutism reducing composition. Table 2
The subject compositions can be prepared with the use of various protocols and addition arrangements, for the wrinkle reducing compositions, conveniently, a first mixture (A) is prepared in the polar solvent heated at a range of approximately 50 to 80 ° C. , preferably 60 ° C in which the natural extract component is added sequentially and stirred until dissolved, for example, resveratrol followed by the Olibanum extract. The mixture is stirred until it is completely homogeneous and allowed to stand. To the triglyceride fraction of stirred (refined) coconut oil at a moderately elevated temperature, generally in the range
about 35-50 ° C, the phenyl-perfluoroacylaminopropanamide is added and the mixture is stirred for a 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 shows to be homogeneous, the previously prepared mixture (A) is added by dripping with stirring to provide a concentrate that can be stored at a lower temperature than ambient in a dark container. For the hirsutism compositions, the phenyl-perfluoroacylaminopropanamide is added to the polar solvent and the mixture is stirred for a sufficient time to provide homogeneity, usually 20 minutes. To this mixture are then added the vegetable oils and their triglyceride fractions, as appropriate, the antioxidant preservative, optionally followed by the antioxidant, for example, tocopherol. If a wetting agent is desired, it is added slowly, for example, by dripping, with stirring to provide a final mixture which can be stored at below ambient temperatures in a dark container. Several precursor compositions can be prepared so that they have less than all of the components and the components are subsequently added.
Unlike other formulations, the subject formulations are usually at least substantially free of hydroxy acids and in the case of the wrinkle composition it is also free of monocarboxylic acid esters which is used in other cosmetic compositions. Any of the extracts or fractions thereof or the known active ingredient (s) can be used. For economic reasons, it will usually be preferred to use the natural extracts as the source of the active ingredient (s), rather than a substantially pure form, whether obtained from a natural or synthetic source. The form of the extract used, when the active ingredient is known, will have at least about 50% by weight of the active ingredient, and can have 70% 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. Phenyl-perfluoroacylaminopropanamides are described in US Patent no. 6,184,249. The active compounds that can be used are substances, which affect skin androgen receptors but are not reabsorbed appreciably systemically. Such compounds are exemplified by 2-hydroxy-2-methyl-N- [4-nitro-3- (trifluoromethyl) phenyl] -3- (2,2,2-
trifluoroacetylamino) propanamide (fluridil). In the case of a Japanese polygon, the extract will usually have at least about 90% trans-resveratrol (CAS No.: [501-36-0], 3, 4 ', 5-trihydroxy-trans-stilbene, as a glycone) (Piceid) Any other source of resveratrol can be used in a way that provides at least a substantially equivalent amount of resveratrol.Synthetically prepared resveratrol is also acceptable.Incense extract, Boswellia serra ta, is a terpenoid mixture having from about 60-70% triterpenes, the main portion of which are boswellic acids, of which at least 10 to 30% (w / w) is ß-boswellic acid , from 5 to 20% (w / w) is acetyl-ß-boswellic acid, 5 to 20% (w / w) is 11-keto-ß-bos-lustric acid and 5 to 20% (w / w) is acid acetyl-11-keto-ß-boswellic (CAS No. [8050-07-5]) These extracts have found wide use as food supplements and in cosmetics as reported in the literature for a wide variety of indications, with many anecdotal reports of success Phytoestrogens are readily available as a fraction derived from rape seed oil (Brassica) and / or soybean (soy glycine) In the subject formulation, the fraction that can not be saponified (CAS No. [91770 -67-1] of the appropriate vegetable oil is used as a source of
phytoesens and will be substantially free of esters. Grapeseed oil (Vitis vinifera) or soybean oil is mainly a mixture of saturated or unsaturated fatty acids whose main constituents are linoleic and oleic acids (> 80%). These acids could be used independently of the other ingredients or the synthetically prepared mixture. They are used in their refined form. Coconut oil (Cocos nucifera) mainly provides medium chain triglycerides in which the acids are mainly saturated fatty acids Ce-iOf, particularly caprylic and capric (CAS [73398-61-5]). It is used in its refined form. Various antioxidants can be used as conventionally used in cosmetic formulations. Vitamins A and E in their commercially available forms are favored, since they are known to provide healthy physiological effects on the skin, but other oxidants may also be employed, such as compounds having phenolic hydroxy functions, ascorbic acids and their derivatives / esters; beta-carotene; catechin, curcumin, ferulic acid derivatives (for example, ethyl ferulate or sodium ferulate); gallic acid derivatives (e.g., propyl gallate); lycopene; reductive acid; acid
rosmarinic; tannic acid, tetrahydrocucumin; tocopherol derivatives; uric acid; or any mixture thereof. Other suitable antioxidants are those having one or more thiol (--SH) functions, in any 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 organic salts containing sulfur. These antioxidants can be used in partial or complete replacement of the vitamins and antioxidant preservative, and for vitamins, usually partial if and that will generally be present in less than 50% of the amount indicated for vitamins, usually less than 30 % indicated for vitamins, is generally present up to about 2 parts, more usually no more than about 1 part, while for the antioxidant preservative it can be used as a complete replacement. An alkanol is used of from 2-3 carbon atoms, for example, ethanol, propylene glycol and isopropanol, particularly the latter in an amount to provide at least substantial homogeneity to the formulation. Conservatives will also usually be included in minor amounts, usually no more than about 3 different preservatives. The antioxidants described above can function as preservatives. Plus
Conventionally, BHT, BHA, TBHQ, ethoxyquin, propyl gallate, and rosemary extract are used. A particularly important aspect of this invention is the preferred formulation according to that described in the experimental section. The combination of ingredients is formulated to solubilize all substances in a cosmetically acceptable medium. Several components, but particularly the extracts of Bos ella serrata, as well as the Japanese polygon extract, are highly insoluble in standard systems. The combination forms a homogeneous solution in the target mixture of medium chain triglycerides (caprylic / capric trglycerides) with fractions of purified grape seed oil and the addition of a minimum amount (less than 10%) of rectified alcohol (isopropanol). The resulting mixture is a viscous liquid of oily appearance, which nonetheless becomes invisible on the skin in a short period after its topical application: the skin surface is not oily and the total effect is that of high flexibility and softness of the skin. In addition to the ingredients numbered above, there are other additives that are included for specific purposes. These additives and adjuvants are conventional in the cosmetic, pharmaceutical or dermatological field, such as hydrophilic or lipophilic gelation agents, hydrophilic or lipophilic active agents, solvents, fragrances,
fillers, bactericides, odor absorbers and inks or dyes. The amounts of these various additives and adjuvants are those conventionally used in the field, for example, in the range from 0.01% to 10% of the total weight of the composition. Emulsifiers that can be used include glyceryl stearate, polysorbate 60, glycol stearate / PEG-6 / PEG-32 mixture, etc. Hydrophilic gelling agents include carboxyvinyl (carbomer) polymers, acrylic copolymers such as acrylate / alkyl acrylate copolymers, polyacrylamides, polysaccharides, such as hydroxypropylcellulose, natural gums and clays, and, as lipophilic gelation agents, representative are modified clays. such as bentones, metal salts of fatty acids such as aluminum stearates and hydrophobic silica, or ethylcellulose and polyethylene. Suitable alcohols and fatty acids include those compounds having from 10 to 20 carbon atoms. Especially preferred are compounds such as cetyl, myristyl, acids and alcohols of palmitic and stearyl alcohols. Among the polyols, which can function as emollients, are branched-chain alkyl polyhydroxyl compounds. For example, propylene glycol, sorbitol and glycerin are preferred. They can also be
Useful are polymeric polyols such as polypropylene glycol and polyethylene glycol. Butylene and propylene glycol are also useful. Exemplary hydrocarbons, which can function as emollients, are those having hydrocarbon chains at any of from 12 to 30 carbon atoms. Specific examples include mineral oil, petrolatum, squalene, and isoparaffins. Another category of functional ingredients within the cosmetic compositions of the present invention are thickeners. A thickener will usually be present in any amounts from 0.1 to 20% by weight, preferably from about 0.5% to 10% by weight of the composition. Exemplary thickeners are crosslinked polyacrylate materials available under the trademark Carbopol. Gums can be used such as xanthan, carrageenan, gelatin, carayá, pectin and locust bean gum. Under certain circumstances the thickening function can be achieved with a material that also functions as a silicone or emollient. For example, silicone gums in an excess of 10 centistokes and esters such as glycerol stearate have a double functionality. Powders can be incorporated into the cosmetic composition of the invention. These powders include ash, talc, kaolin, starch, smectite clays, silicate
chemically modified aluminum magnesium, organically modified montmorillonite clay, hydrous aluminum silicate, fumed silica, octenyl aluminum starch succinate and mixtures thereof. Other minor adjuncts may also be incorporated into the cosmetic compositions. These ingredients may include coloring agents, opacifiers and perfumes. The amounts of these other minor components attached may be in the range of from 0.001% to 20% by weight of the composition. The object compositions will be stored in containers that can be protected from light, being opaque to impinge the light and can be sealed to minimize the oxygen present in the empty space. In view of the cosmetic nature compositions, the containers will be attractive, can have various shapes and be in a variety of sizes. The subject compositions may be supplied in conjunction with other skin formulations, as appropriate. Preferred subject compositions are characterized in that they are clear liquids when applied to the skin. They are not absorbed systemically to some degree that can be found in the vascular system. They have been found to have from nothing to a very low acute irritation potential in standard tests, and are safe to use with humans or other mammals. They have an antimicrobial activity
against a variety of organisms, which inhibit the growth of microorganisms in the composition. It has been found that they are effective through subjective and objective tests, which are described by users because they provide a sensation of wetting and lifting. A mapping and depth measurement of periocular / temporal wrinkles by laser profilometry shows a leveling effect in the skin micro-relief, revealed by a decrease in the average depth of the micro-relief grooves and a significant decrease in complexity in a majority of the subjects. With a group of test subjects to provide a p-value of less than 0.1, in the course of 50 days the volume of wrinkles as measured by laser profilometry will be reduced by at least about 60 to 80, more usually by at least 70% of the subjects, and the depth of the wrinkle is reduced by approximately 8-15%, and most usually by at least 10%. 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 equally effective), in 9 out of ten facial hairy women who used the composition described herein in the absence of any another treatment, according to 2 mi by massage
once a day in the affected areas, a substantial thinning, loss of color and a reduction in hair growth on face and neck are documented. The following examples are provided by way of illustration and not by way of limitation. EXPERIMENTATION Example 1 A typical composition of 100 g of the novel cosmetic skin care preparation 0.5 g of Japanese polygon extract (minimum 95% trans-resveratrol); 3, 4 ', 5-trihydroxy-trans-stilbene, CAS No .: [501-36-0] 0.5 g of incense extract (Olibanum) -Boswellia serra ta (60-70% of triterpenes) CAS No .: [ 8050-07-5] 0.5 g of vegetable oil extract Brassica oleífera / Glicina soya (fractions that can not saponify CAS [91770-67-1]) 3.0 of vitamin E (DL-α-tocopherol acetate); 3, 4-dihydro-2, 5, 7, 8-tetramethyl-2- (4,8,13-trimethyltridecyl) -2H-l-benzopyran-6-ol acetate, 3,000 IU CAS No .: [7695-91 -2] 1.2 g of vitamin A (retinol palmitate); 3, 7-dimethyl-9- (2,6,6-trimethyl-l-cyclohexene-1-yl) 2,4,6,8-nonatetraene-1-ol palmitate, 2,000,000 IU, CAS No .: [79 -81-2] 2.0 g of fluridil CAS No .: [260980-89-0] 0.1 g of BHT (butylated hydroxytoluene), 2,6-Di-tert-butyl-4-
methylphenol CAS No .: [128-37- 0] 5.0 g of rectified alcohol (isopropanol), CAS No .: [67-63-0] 40.0 g of refined grape seed oil, CAS No .: [8024-22 -4] 47.2 g of refined oil (Cocos nucifera) medium chain triglycerides Caprilicos / Cepricos Example 2. Ocular toxicity: Effects on ocular fibroblasts Rabbit corneal fibroblasts, to which Neutral Red in vitro was added, are exposed to the product in 15, 25 and 50% of concentrations for 1 minute. Cell viability is measured by Optical Density. The culture medium works as a negative control. An IC50 of less than 50% was found, which indicates that the product has a very low toxicity towards the ocular mucosa membranes, and is equivalent to the products sold in the same category. Example 3. Evaluation of antimicrobial properties The test according to USP XXV, is based on the inoculation of the product with 5 varieties, in this case, S. aureus, P. aeruginosa, E. coli, C. albicans and A. Niger , an incubation at 20 ° C with the count executed in 7, 14, 21, and 28 days. The anti-microbial ("conservation") efficiency of
product is considered positive when on day 14 the bacterial counts (measured by concentration of CFU / g) are reduced by at least 2 records and in the following 14 days it continues decreasing or remains the same as the starting count. For yeast / molds the counts should be the same or lower on day 14 and 28, compared to the initial count. Table 3. MEASURED CONCENTRATIONS (CFU / g)
The product in that manner meets the criteria of USP XXV as an efficient conservative of bacterial and fungal sterility. Example 4 In vitro mutagenic determination The test is standard for detecting genetic damage, which induces the formation of micronuclei containing discontinuous chromosomes in their fragments. For this purpose, the preparation was
administered by topic to three dose groups (0.5, 1.5 and 4.5 ml / kg, 5 males and 5 females per group) of SKH-1 mice, once a day for 28 days. Peripheral blood was sampled at 36 and 48 hours after the last administration and reticululocytes were analyzed for the presence or absence of micronuclei after inking. No increase in the frequency of micronucleated polychromatic erythrocytes was detected and the product was therefore judged to be non-mutagenic. Example 5. Single patch test of 48 hours in volunteers The predicted composition for wrinkles was evaluated according to an open study in 11 adult volunteers, after a single application to the skin in the scapular area, under a semi-occlusive patch for 48 hours. hours. The observations aimed at detecting erythema + edema were used to calculate the acute irritation index (M.I.I.) in accordance with the standard formula to issue a grade to the cosmetic product according to the scale: M.I.I. < 0.20 Non-irritating (NI, for its acronym in English); 0.20 M.I.I. < 0.50 Slightly irritating (SI); 0.50 - M.I.I. < 1 Moderately irritating (MI); M.I.I. = 1
Irritating (I). The product was classified as NI, non-irritant. Example 6 Safety and efficacy after 28 and 56 days in volunteers On day 0, 28 and 56 in 24 volunteers, a. Skin safety was assessed through a clinical examination with the demartologist focused on detecting signs of irritation such as erythema, edema, and urticaria. No significant results were reported. b. The Laser perimeter was carried out in a predetermined skin area and its wrinkles, to determine the maximum or average depth, complexity, volume and isotropy. A precision grabber was used, which operates without surface contact to assess the geometrical parameters of the wrinkle and micro-relief of the global skin area. The data consist of complexity of the surface (or visual impact of a wrinkle in%), maximum depth of the wrinkle (in mm), - volume of the wrinkle (in mm3) and are analyzed by a paired t-test with limit of significance of p = 0.05. The results are summarized in the following table:
Table 4
In conclusion, the product has shown a different tendency to reduce wrinkles after 28 days and after 56 days. The objective results were analyzed in parallel with the subjective reports of the volunteers. Example 7. Preparation of lOOg of the anti-wrinkle composition: To 5.0 g of propan-2-ol at 60 ° C was added 0.5 g of Polygon extract (90-95% resveratrol glycol) CAS 501 36 0 and stirred until dissolved, then 0.5 g of Olibanum extract was added, dissolved and the solution was left
rest (sun, A). To 47.2 g of the medium chain triglyceride fraction of coconut oil at 40 ° C was added 2.0 g of furidyl (CAS 260980-89-0) and stirred for 20 minutes. 0.5 g of the vegetable oil extract (fraction that can not be saponized) and 0.1 g of BHT are added followed by 3.0 g of vitamin E and 1.2 g of vitamin A. The mixture is stirred until homogeneity and the sun. A then it is added by dripping, under agitation. The resulting solution functions as a reserve concentrate, which can conveniently be kept under nitrogen in closed dark vessels, at 15 ° C max. The final formulation is prepared by adding 40 g of grape seed oil to the reserve concentrate, to make 100 g of product "CARE: the solution for the face". Examples of antihirsutism compositions: Example 8. A typical composition of 100 g applicable to hirsutism * 1.0 g of oleyl oleate (octadec-9-enyl ester of octadec-9-enoic acid) CAS [3687-45-4] 3.0 g vitamin E (DL-α-tocopherol acetate); 3, 4-dihydro-2, 5, 7, 8-tetramethyl-2- (4, 8, 12 trimethyltridecyl) -2H-l-benzopyran-6-ol acetate, 3,000 IU CAS No .: [7695-91- 2] 2.0 g fluridil CAS No .: [260980-89-0] 5.0 g rectified alcohol (isopropanol), CAS No .: [67-63-0]
41. 5 g soybean oil, CAS No .: [8001-22-7] 47.5 g refined oil (coco nucifera) medium chain triglycerides Caprilic / Capric * All ingredients other than fluridil are listed in the "Inactive Ingredients Database" for Approved Drug Products "from the FDA (http: // www. accessdata.fda.gov/scripts/cder/iig/index.cfm). Example 9. 100 g of a typical cosmetic oil composition applicable to hirsutism * 2.0 g fluridil CAS No .: [260980-89-0] 6.0 g rectified alcohol (isopropanol), CAS No .: [67-63-0] 42.0 g of soybean oil, CAS No .: [8001-22-7] 50.0 g of refined oil (coco nucifera) medium chain triglycerides Caprilic / Capric * All ingredients other than fluridil are listed in the "Ingredients Database" Inactive for Approved Drug Products "from the FDA (http: // www. Accessdata.fda.gov/scripts/cder/iig/index.cfm). Example 10. Composition for skin tested in clinical hirsutism. Ten women with facial hirsutism from 25 to 68 years of age were recruited in the Department of Dermatology,
Palacky University Hospital, Olomouc, Czech Republic. On day 0, photographic documentation of the area was obtained
affected and blood samples to evaluate total testosterone and sex hormone binding globulin (SHBG) in serum. Subjects were instructed to apply 2 ml of product as a thin layer over the affected area (upper lip, chin, as appropriate) daily, at night. On day 90 there were no changes in the hormonal parameters; and the two dermatologists who independently evaluated the images concurred that hair growth, coloration and diameter were substantially reduced in 9 subjects. There were no local or septic side effects. It is evident from the above results that the subject compositions provided improved skin care. The compositions worked to reduce wrinkles and the ravages of age, sun and toxic substances, which include smoking, and to reduce the growth of facial hair. The safe compositions, using components that have been shown to be acceptable to humans. Although they use a mixture of hydrophobic and hydrophilic substances, a substantially homogeneous mixture is obtained which is easily applicable to the skin to provide a clear coat. The subject compositions can be used repeatedly without irritating the skin or damaging the skin. All publications and patent applications cited in this specification are incorporated herein by reference
as if each individual publication or patent application were specifically and individually indicated to be incorporated as a reference. Although the above invention has been described in some detail by way of illustration and exemplified for purposes of clarity of understanding, it should be apparent to those skilled in the art in light of the teachings of this invention that certain changes and modifications may be made to it without departing from the spirit or scope of the appended claims. It is noted that in relation to this date, the best method known to the applicant to carry out the aforementioned invention, is that which is clear from the present description of the invention.
Claims (14)
- CLAIMS Having described the invention as above, the content of the following claims is claimed as property: 1. A skin care composition of cosmetically acceptable components for the topical treatment of wrinkles or hirsutism, characterized in that it comprises: an effective amount of a 3-nitro-3-trifluoromethylphenyl substituted physiologically acceptable perfluoroacylaminopropanamide, wherein the perfluoroacyl group is from 2-3 carbon atoms and the propanamide group is substituted on the carbon atom 2 with at least one of the hydroxyl and methyl; a vehicle comprising a greater amount of at least one refined oil of natural origin, a fraction of triglyceride oil and sufficient alkanol of from 2-3 carbon atoms to provide at least one substantially homogeneous mixture; an effective amount of at least one physiologically acceptable antioxidant; and when a skin composition is for the treatment of hirsutism, the skin composition further optionally comprises a humectant; When the skin composition is for wrinkle treatment, the skin composition further comprises at least one plant extract of natural origin or fraction thereof.
- 2. A composition in accordance with the claim1, characterized in that it is for the treatment of wrinkles and comprises a mixture of at least 3 natural extracts, fractions thereof or compositional equivalents, selected from the group consisting of Japanese polygon, incense, a fraction can not saponise from Brassica oleifera and / or Glycine soya.
- 3. A composition in accordance with the claim
- 2, characterized in that refined oils of grape seed and nucifera Cocos are present. Four . A composition according to claim 2, characterized in that the antioxidants are vitamins.
- 5. A composition according to claim 2, characterized in that the alkanol is isopropanol.
- 6. A composition according to claim 1, characterized in that it is for the treatment of hirsutism and comprises refined oils of Glycine soya and Cocos nucifera.
- 7. A cosmetic composition for the skin of cosmetically acceptable components characterized in that it comprises in parts by weight: 0.5-5 parts 2-hydroxy-2-methyl-N- [4-nitro-3- (trifluoromethyl) phenyl] -3- ( 2, 2, 2-trifluoroacetylamino) propanamide; 0.5-5 parts of natural extracts selected fromgroup consisting of Japanese polygon, incense, and a fraction that can not be saponized from Brassica oleifera and / or Glycine soya; 50 - 95 parts of refined oil of grape seed and / or cocoa nucifera; 2 - 10 parts of antioxidants; and 2.5-10 parts of an alkanol of from 2-3 carbon atoms in an amount sufficient to provide a substantially homogeneous mixture.
- 8. A composition according to claim 7, characterized in that the antioxidants are Vitamins A and E.
- 9. A composition according to claim 7, characterized in that the alkanol is isopropanol.
- A composition according to claim 7, characterized in that Japanese polygon and incense are present, and a fraction that can not be saponized from at least one of Brassica oleifera and Glycine soya.
- 11. A cosmetic composition for the skin of cosmetically acceptable components, characterized in that it comprises in parts by weight: 1-4 parts of 2-hydroxy-2-methyl-N- [4-nitro-3- (trifluoromethyl) phenyl] -3 - (2, 2, 2-tri-luoroacetylamino) propanamide; a total of 0.75 - 3 parts of natural Japanese polygon extracts, incense, and a fraction that can notSaponizing of Brassi ca oleifera and / or Glycine soya; 30 - 50 parts of refined grape seed oil; 0.5 - 2 parts of antioxidants; and 3 - 7.5 parts of an alkanol of from 2-3 carbon atoms in an amount sufficient to provide a substantially homogeneous mixture.
- 12. A cosmetic composition for the skin characterized in that it comprises in parts by weight: 0.5 part of 2-hydroxy-2-methyl-N- [4-nitro-3- (trifluoromethyl) phenyl] -3- (2, 2, 2 -trifluoroacetylamino) propanamide; 0.5 parts of a Japanese polygon extract, 0.5 parts of an incense extract, 0.5 parts of a fraction that can not be saponized from Brassica oleifera and / or Glycine soya, 40 parts of refined grape seed oil, approximately 47 parts of fraction of refined Coconut oil, nucifera, (medium chain triglycerides) 1.3 parts of Vitamin A, 3 parts of Vitamin E, and 5 parts of isopropanol.
- 13. A cosmetic composition for the skin of cosmetically acceptable components characterized in that it comprises in parts by weight: 0.5 - 5 parts of 2-hydroxy-2-methyl-N- [4-nitro-3-(trifluoromethyl) phenyl] -3- (2,2,2-trifluoroacetylamino) ropanamide; at least 80 parts of refined Glycine Soybean Oil and / or Coconut Nucifera; 2 - 10 parts of antioxidants; and 2.5-10 parts of an alkanol of from 2-3 carbon atoms in an amount sufficient to provide a substantially homogeneous mixture. A composition according to claim 13, characterized in that the refined oil is present from 85-95 parts, the antioxidant is tocopherol and is present in from 2-6 parts, and a humectant is present in an effective amount.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US60/713,882 | 2005-09-01 | ||
US11509485 | 2006-08-24 |
Publications (1)
Publication Number | Publication Date |
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MX2008002745A true MX2008002745A (en) | 2008-09-02 |
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