BR102017007699A2 - product for baldness and hair loss treatment and cosmetic formulation - Google Patents

Abstract

The present invention deals with a baldness treatment product and formulations and more specifically for solutions that can reduce and eliminate androgenic alopecia, areata, telogen effluvium and hair loss for common causes, promoting hair growth and nutrition. The product comprises the use of atraric acid, palmitic acid, chlorogenic acid, oleic acid, linoleic acid, cordianol a, cordianol c, cordialin a, ptychopetalum olacoides benth extract, resveratrol, yeast and beer malt for the treatment and prevention of fall. hair and baldness of any kind being feasible for topical application by liquid or solid media acting to inhibit alpha-5 reductase activity by blocking dht receptors in the hair follicle, inhibiting prostaglandin d2 receptors and providing cleansing, nutrition and protection for healthy follicle growth and proper functioning of the hair cycle.

Description

(54) Title: PRODUCT FOR THE TREATMENT OF HAIR AND HAIR LOSS AND COSMETIC FORMULATION (51) Int. CL: A61K 8/63; A61K 8/97; A61K 8/37; A61K 8/34; A61K 8/99; (...) (73) Holder (s): ENÉAS RICARDO DE MORAIS GOMES, JOHN ALLEF MACHADO FREITAS (72) Inventor (s): JOHN ALLEF MACHADO FREITAS; ENÉAS RICARDO DE MORAIS GOMES (85) Date of the Start of the National Phase:

04/13/2017 (57) Abstract: The present invention deals with a product and formulations for the treatment of baldness and more specifically for solutions that can reduce and eliminate androgenic alopecia, areata, telogen effluvium and hair loss due to common causes, promoting hair growth and nutrition. The product comprises the use of atraric acid, palmitic acid, chlorogenic acid, oleic acid, linoleic acid, cordianol A, cordianol C, cordialin A, Ptychopetalum olacoides Benth extract, resveratrol, yeast and beer malt for the treatment and prevention of fall of hair and baldness of any kind being viable for topical application by liquid or solid medium acting to inhibit alpha-5 reductase activity, by blocking DHT receptors in the hair follicle, by inhibiting prostaglandin D2 receptors and by providing cleaning, nutrition and protection for healthy follicle growth and the proper functioning of the hair cycle.

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PRODUCT FOR THE TREATMENT OF HAIR AND HAIR LOSS AND COSMETIC FORMULATION

DESCRIPTIVE REPORT

FIELD OF THE INVENTION [001] The present invention deals with a product and formulations for the treatment of baldness and more specifically for viable solutions for cosmetics, which can reduce and eliminate androgenic alopecia, areata, telogen effluvium and hair loss due to common causes, promoting hair growth and nutrition.

ANTERIORITIES [002] Since the beginning of human civilization, hair has been a means of exhibition and personalization and this has been perpetuated until contemporary society, where the appearance of hair is associated with our perception of health, self-confidence and well-being, For all these reasons, the search for effective treatments for hair problems, such as baldness, is incessant.

[003] In this context, it is known that there are a variety of factors that can affect the hair growth cycle and cause temporary or permanent hair loss, called alopecia which causes excessive hair loss and shortening the angina phase of follicles and prolonging the telogen phase. It is known that the main cause of male pattern hair loss, also known as androgenic alopecia is the hormone DHT, dihydrotestosterone which in genetically predisposed individuals is the result of the conversion of testosterone by 5-a-reductase and which binds to androgen receptors in dermal papilla causing changes at the molecular level that result in miniaturization of the follicles and altering the hair growth cycle. In addition, another factor related to hair loss and baldness is the excessive oiliness of the scalp, an effect caused by

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2/11 prostaglandin D2 in hair follicle receptors, being related to 90% of patients with baldness.

[004] Alopecia is caused by multiple factors including, hormonal imbalances, general and capillary nutritional deficiencies, stress, chemotherapy and mainly, genetic inheritance. Baldness is also attributed to advanced age and reduced mitotic capacity of hair follicles. Although there are already treatments approved by FDA and ANVISA such as Minoxidil and Finasteride (Proscar ®), for the use of patients with baldness, the existence of unwanted effects in a small portion of individuals such as reduced libido, erectile dysfunction and rapid restoration of baldness after discontinuation of treatment characterizes a challenge on the part of the pharmaceutical industry to create a product or a more efficient treatment without presenting the negative points of the reference treatments, nor causing any side effect, also characterizing an opportunity to carry out innovation and to provide improvements for patients who are eager to treat their hair problem in a practical, safe and effective way. In this way, the present invention aims to solve the challenge of solving the problems of hair loss and baldness in order to minimize the incidence of collateral problems, without giving up efficiency using a multifactorial approach combined with practicality through cosmetic solutions.

[005] A series of products have already been created for this purpose, highlighting some inventions related to the present invention:

[006] The patent CA2717806 A1 - Composition and uses for influencing hair growth, cites a product that contains options for androgen receptor inhibitors, 5-a-reductase inhibitors that converts testosterone to DHT (dihydrotestosterone) and aromatase inhibitors derived from plants to promote hair growth. The document cites as an example of DHT blockers Pygeum afrícanum, Saw Palmetto (Serenoa repens) as active ingredients of plant origin to promote hair growth and prevent androgenic alopecia, however such an invention does not take into account

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3/11 considering the use of prostaglandin D2 inhibitors, presented in the present invention, which are compounds capable of reducing excessive oiliness, a predominant factor in patients with baldness and hair loss in general. The patent WO 2002051426 A2 - Compositions and methods for treating sexual dysfunction, enhancing sexual function, increasing testosterone levels, and improving muscle strength and mass, describes the use of plant extracts with testosterone precursor activities, aromatase and 5-α-reductase inhibitors for the treatment of sexual dysfunction by promoting improvement of blood flow and muscle tone. A mechanism similar to the one that provides erectile dysfunction occurs in hair follicles, which suffer miniaturization and obstruction caused by DHT binding to androgen receptors in the dermal papilla causing hair loss in individuals with baldness. Among the compounds used for the treatment of sexual dysfunction is the extract of Marapuama (Ptychopetalum olacoides) that is used by indigenous populations in the Amazon Forest to combat erectile dysfunction, as a nervous tonic and that in the present invention is used as a tonic for hair growth .

[007] The document US005674510A - Hair treatment solution and other publications and method of using same, describes cosmetic formulations to reduce hair loss and promote hair growth in individuals with alopecia, using natural compounds such as grapefruit juice, acetic acid, powdered garlic and brewer's yeast to be used directly in the affected area, which features topical products without adverse effects such as atopic dermatitis and psoriasis or erectile dysfunction. In said patent, the use of brewer's yeast provides nutrients such as vitamin B, chromium, iron, calcium, niacin, riboflavin, folic acid and essential amino acids for hair growth and the proper functioning of the hair cycle, as in the present invention. However, in the formulation described, it does not act in a way to block DHT receptors or 5-α-reductase inhibitors, nor active principles for combating excessive oiliness caused by

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4/11 prostaglandin D2 which are the key factors for the treatment of alopecia and hair loss and which are part of the present invention.

[008] The patent US20090047371A1 - Pharmaceutical composition comprising curcumin and resveratrol and uses thereof in medical field, describes a pharmaceutical composition with the combination of resveratrol and curcumin for the treatment of processes related to aging and vascular diseases such as prostate cancer, carcinoma, skin diseases such as psoriasis and related to capillaries such as hair loss. In the patent in question, resveratrol is described as a polyphenol present in the skins and seeds of grapes and other plant species with a high antioxidant and anti-inflammatory power and which presents therapeutic and preventive activity for skin and capillary diseases such as alopecia, however presents the use of resveratrol in combination with 5-a-reductase inhibitors, DHT receptor blockers and vasodilators as a therapeutic alternative for the prevention, reduction and treatment of alopecia and hair loss, nor does it describe it as capable of reducing the excessive oiliness of the leather hairy.

[009] EP19840300631 - Fatty acid containing hair tonic composition, describes a hair tonic to effectively promote hair growth using among other active principles linoleic acid, oleic acid, arachidonic acid, lauric acid, palmitic acid -caprylic, as sources of inhibitors of the enzyme 5-a-reductase to be used in the form of a cosmetic solution, as well as used in the present invention in which the active principles oleic acid, palmitic acid, linoleic acid are used as inhibitors of the aforementioned enzyme as a treatment for hair loss and baldness. However, unlike the present invention, the cited patent does not address hair loss as a multifactorial factor, combining the use of 5-a-reductase inhibitors with DHT receptor blockers, vasodilators and agents to reduce excessive oiliness.

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GENERAL DESCRIPTION [010] The present invention is a solution for hair treatment that in the appropriate amounts can completely and effectively treat and nourish the hair of individuals with alopecia and hair loss due to different causes without promoting any negative effect. The solution can be treated in the form of cosmetics to prevent, reduce and eliminate alopecia, by stopping hair loss, promoting hair growth, nutrition and reducing the excessive oiliness of the scalp of individuals suffering from temporary hair loss or definitive, for any causes without showing any side effects during treatment, these effects include, but are not limited to, dry scalp, eczema such as seborrhea, contact dermatitis or atopic dermatitis.

[011] The product to treat or prevent alopecia and hair loss can be administered by the individual in an effective dosage to perform the treatment or prevention in which the product must have at least one or a combination of the following components: atraric acid, oleic acid, cordialin, cordianol A, cordianol C, chlorogenic acid, linoleic acid, resveratrol, palmitic acid, Ptychopetalum olacoides Benth extract, malt and brewer's yeast.

[012] The formulation of the present invention promotes its therapeutic activity on hair loss of male and female androgenetic alopecia, telogen effluvium, alopecia areata and other causes of hair loss propitiate the loss of hair loss through interaction with the production of DHT in the scalp, as well as by blocking the binding of DHT to its receptor in the hair follicle and by promoting increased blood flow in the follicles. In addition, the formulation acts by inhibiting prostaglandin D2 receptors and providing nutrients that enhance hair growth.

[013] The formulation of the present invention blocks 5-alpha-reductase, the enzyme involved in the production of dihydrotestosterone (DHT) from testosterone.

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6/11 [014] Hereby, the formulation presented in the present invention prevents 5-alpha-reductase, an enzyme that converts testosterone to DHT. For this reason, DHT levels in the scalp are reduced, as well as by blocking DHT binding to its receptor in the dermal papillae, an effect produced by the following substances and their relative concentrations: 0.1% - 3% atraric acid; oleic acid 0.1% - 5%; cordialin A 0.1% - 4%; 0 0.1% - 4% cordianol A; cordianol C 0.1% - 4%; chlorogenic acid 0.1% - 4%; linoleic acid 0.5% - 5%; palmitic acid 0.5% - 3%, present in the invention in question. What provides the maximization of the results, the normalization of the hair growth cycle and the reversal of hair loss due to baldness. [015] Furthermore, resveratrol as described in the formulation of the present formulation in concentrations between 0.5% - 3% by weight of the product acts by inhibiting the binding of prostaglandin D2 to its receptors in the hair follicle, which reduces excessive oiliness scalp, one of the main factors related to baldness, present in 90% of cases of hair loss and alopecia.

[016] The formulation also promotes vasodilation of the vessels surrounding the hair follicles by means of resveratrol between 0.5% - 3% and by the extract of Ptychopetalum olacoides Benth in concentrations between 1% - 7.5%, by increasing vasodilation and promote an increase in nervous tone in the region, allowing for a greater blood and nutrient supply for the proper growth of the hair. Another factor that allows the greater supply of nutrients and the development of the hair cycle in a healthy way is provided by the use of malt to be used in concentrations between 1% - 10% providing carbohydrates, minerals, fatty acids and amino acids that are essential for nutrition capillary growth and adequate growth, in addition to having antioxidant activity that allows to reduce capillary damage caused by inflammation in the scalp resulting from stress, bacterial, fungal infections and unregulated immune processes as occurs in alopecia areata and telogen effluvium.

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7/11 [017] Beer yeast is rich in essential amino acids, proteins, minerals and B vitamins, in addition to cleaning the scalp by removing residues that can cause hair follicle obstruction and, consequently, follicle atrophy and hair loss. In addition, its use in concentrations between 0.5% - 4% helps to remove excess oil from the scalp, as well as the previously described activity attributed to resveratrol.

[018] Because it is a broad spectrum formulation for the various causes of hair loss and baldness such as telogen effluvium, alopecia areata and androgenic alopecia, the formulation has anti-inflammatory and antioxidant activity, reducing capillary damage caused by common causes such as nutritional deficiency, stress and inflammatory process resulting from hormonal or immunological dysregulation. The effects of the formulation of the present invention may not be immediately visible. For this reason, the formulation must be applied regularly to obtain an optimal result.

[019] The components can be prepared in solid form (as in the form of pills, tablets or powders) or in liquid form (solutions, suspensions or emulsions) and can be used in combination with conventional adjuvants for pharmaceutical and / or cosmetic operations such as (ex: deionized water, methyl alcohol, ethyl alcohol), disintegrants, binders, non-stick, glidants, lubricants, antioxidants, buffering agents, dyes, flavoring agents, coating agents, solvents, osmotic agents, viscosity agents, waxes, wetting agents, solubilizers, stabilizers, chelators, vehicles, preservatives, surfactants, deodorants, bulking agents, hydrophilic polymers, tonicity regulating agents, pH acid control agents, alcohols, reducing sugars, non-reducing sugars. These agents can be presented, generally in amounts between 0.1% - 3% of atraric acid; 0.1% - 5% oleic acid; 0.1% - 4% cordialin A; 0.1% - 4% cordianol A; 0.1% - 4%

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8/11 cordianol C; 0.5% - 3% ciorogemco acid; 0.5% - 5% linoleic acid; 0.5% - 3% resveratrol; 0.5% - 3% palmitic acid; 1% - 7.5% - extract of Ptychopetalum olacoides Benth; 1% - 10% malt; beer yeast 0.5% - 4% by weight, and preferably in quantities between 0.5 - 3% For administration, these active ingredients can be combined with one or more adjuvants according to their form of presentation and route administration. The compounds can be mixed with lactose, sucrose, powdered starch, cellulose esters of alkanoic acids, stearic acid, talc, magnesium stearate, magnesium oxide, sodium and calcium salts of phosphoric and sulfuric acids, acacia, gelatin, alginate sodium, polyvinylpyrrolidone and / or polyvinyl alcohol, and compressed or encapsulated for conventional administration. Alternatively, the compounds of the invention can be dissolved in saline, water, methanol, polyethylene glycol, propylene glycol, colloidal solutions of carboxymethylcellulose, ethanol, corn oil, peanut oil, cottonseed oil, sesame oil, tragacanth and / or several plugs. Other adjuvants and modes of administration are well known in the pharmaceutical art. The carrier or diluent may include retardant material, such as glyceryl monostearate or glyceryl stearate alone or with a wax, or other materials well known in the art.

[020] For topical administration, the active ingredients can be formulated directly on the scalp. Conventional forms for this purpose include dressings, lotions, creams, pastes, gels, sprays, aerosols, shampoos, ointments and transdermal patches. The percentage by weight of the active ingredients presented in the present invention, can vary according to several factors but must be used in the following concentrations 0.1% - 3% of atraric acid; 0.1% - 5% oleic acid; 0.1% - 4% cordialin A; 0.1% - 4% cordianol A; 0.1% - 4% cordianol C; 0.5% - 3% chlorogenic acid; 0.5% - 5% linoleic acid; 0.5% - 3% resveratrol; 0.5% - 3% palmitic acid; 1% 7.5% - Ptychopetalum olacoides Benth- extract, 1% -10% malt; beer yeast - 0.5% - 4% of the total volume of the formulation. Dosages of forms

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Solid 9/11 for oral administration may include, but not be limited to, the use of capsules, tablets, pills, powders, granules and pills. In such solid dosage forms, the active ingredients can be mixed with at least one inert diluent such as sucrose, lactose or starch. Such dosage forms may also comprise, as is conventional, additional substances other than inert diluents, for example, lubricating agents such as magnesium stearate. In the case of capsules, tablets and pills, the dosage forms can also comprise buffering agents. Tablets and pills can also be prepared with enteric coatings.

[021] Liquid dosage forms for oral administration may include viable emulsions for use in pharmaceutical formulations, solutions, suspensions, serums, elixirs containing inert diluents commonly used as water. Such compositions can comprise adjuvants, such as wetting agents, emulsifiers and suspending agents, sweeteners, flavors and flavoring agents.

[022] The dosage for the product for treatment or prevention of hair loss and alopecia described in the present invention with the substances with therapeutic activities described are based on several factors, including weight, age, sex, medical condition of the individual and the degree the condition of hair loss or baldness, as well as the route of administration and the particular compound to be used. Thus, the dosage may vary but must be presented in the following values according to each of the ingredients: 1% atraric acid; 0.1% - 1% oleic acid; 1% cordialin A; 1% cordianol A; 1% cordianol C; 1% chlorogenic acid; 1% linoleic acid; 2% resveratrol; 1% palmitic acid; 3% - extract of Ptychopetalum olacoides Benth; 5% malt; beer yeast - 2%. For example, for the treatment of alopecia using the composition for subcutaneous or topical application and can be applied to the area affected by hair loss or baldness one or more times a day if necessary.

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10/11 [023] In general, the present invention relates to a product for the treatment or prevention of alopecia and hair loss of various types, in which it presents effective active principles to treat and prevent alopecia completely and effectively be it of the type alopecia areata, androgenic alopecia of male or female pattern, telogenic effluvium and hair loss caused by genetic factors, stress, capillary malnutrition, by inflammatory processes, infections by microorganisms and / or hormonal factors. The effects of the formulation of the present invention may not be immediately visible. For this reason, the formulation must be applied regularly to obtain an optimal result.

PREFERRED EMBODIMENTS [024] The formulation of the present invention can be made available (outlined) in several formats, which are feasible for administration to the individual in a practical way. The formulation should preferably be used topically with direct application on the scalp, being possible the application in the form of shampoos, creams, ointments, gels, sprays and aerosols for hair.

[025] The amount of each component present in the formulation is selective for an excellent therapeutic effect. Preferably, the formulation should contain the following quantity of the active ingredients:

[026] 0.1% - 3% atraric acid; 0.1% - 5% oleic acid; 0.1% - 4% cordialin A; 0.1% - 4% cordianol A; 0.1% - 4% cordianol C; 0.5% - 3% chlorogenic acid; 0.5% - 5% linoleic acid; 0.5% - 3% resveratrol; 0.5% - 3% palmitic acid; 1% - 7.5% - extract of Ptychopetalum olacoides Benth; 1% -10% malt; beer yeast - 0.5% - 4% [027] Preferably the formulation contains:

[028] 1% atraric acid; 0.1% -1% oleic acid; 1% cordialin A; 1% cordianol A; 1% cordianol C; 1% chlorogenic acid; 1% linoleic acid; 2% resveratrol; 1% palmitic acid; 3% - extract of Ptychopetalum olacoides Benth; 5% malt; beer yeast - 2%.

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11/11 [029] As mentioned earlier, the formulation for topical application can be administered in the form of shampoos, creams, spray, aerosols, ointments and hair gels. For all forms of administration, the ingredients must be combined with typical excipients for the preparation of cosmetics such as thinners (eg, deionized water, methyl alcohol, ethyl alcohol), disintegrants, binders, anti-adherents, glidants, lubricants, antioxidants, buffering, dyes, flavoring agents, coating agents, solvents, osmotic agents, viscosity agents, waxes, wetting agents, solubilizers, stabilizers, chelators, vehicles, preservatives, surfactants, deodorants, bulking agents, hydrophilic polymers, tonicity regulating agents , pH acidity control agents, alcohols, reducing sugars, non-reducing sugars. The ingredients of the present invention can be obtained from synthetic, semi-synthetic or natural sources in the form of liquid extracts, dry extracts, oils, infusion, distillation, alcoholic solutions, alcohols, hydrocarbons, decoction, digestion, maceration and glycolic extracts.

[030] The ideal dosage to be applied is up to twice a day, during or after washing the hair.

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Claims (7)

1. Product for the treatment of baldness and hair loss characterized by having atraric acid, oleic acid, chlorogenic acid, linoleic acid, resveratrol, cordialin A, cordianol C, cordianol A, palmitic acid, Ptychopetalum olacoides Benth extract, yeast and malt beer, which can be used alone or in combination 2. Product for the treatment of baldness and hair loss according to claim 1, characterized by the association with one or more active ingredients of natural, synthetic and / or semi-synthetic origin 3. Product for the treatment of baldness and hair loss according to claims 1 and 2, characterized in that they are in the form of liquid extracts, dry extracts, oils, infusion, distillation, alcoholic solutions, alcohols, oils, decoction, digestion, maceration and / or glycolic extracts can be used alone, or in combination with excipients 4. Product for the treatment of baldness and hair loss according to claims 1,2 and 3, characterized by containing dosages between 0.1% - 3% of atraric acid; 0.1% - 5% oleic acid; 0.1% - 4% cordialin A; 0.1% - 4% cordianol A; 0.1% - 4% cordianol C; 0.5% - 3% chlorogenic acid; 0.5% - 5% linoleic acid; 0.5% - 3% resveratrol; 0.5% - 3% palmitic acid; 1% - 7.5% - extract of Ptychopetalum olacoides Benth; 1% - 10% malt; 0.5% - 4% brewer's yeast, individually or combined with one or more active ingredients together Petition 870170024642, of 4/13/2017, p. 7/20 2/2 Product according to claim 3, characterized in that the excipients belong to a group comprising diluents, disintegrants, binders, anti-adherents, glidants, lubricants, antioxidants, buffering agents, dyes, flavoring agents, coating agents, solvents, osmotic agents, viscosity agents, waxes, wetting agents, solubilizers, stabilizers, chelators, vehicles, preservatives, surfactants, deodorants, bulking agents, hydrophilic polymers, tonicity regulating agents, local anesthetics, pH control agents, alcohols, sugars reducing, non-reducing sugars or mixtures thereof 6. Product for the treatment of baldness and hair loss according to claims 1, 2 and 3, characterized in that it is in the form of a solution, suspension, emulsion, capsule (hard or gelatinous), tablet, gel, cream, lotion, spray, aerosol, ointment, implant, microcapsule, nanocapsule, microsphere, nanosphere, microemulsion, nanoemulsion and / or liposomes Product according to claims 1, 2 and 3 characterized by the active principle comprising at least one inhibitor of DHT receptors, muscle tonic, nervous tonic, and / or inhibitor of prostaglandin D2 receptors, which can be used alone or combined with each other, or in combination with 5alpha reductase inhibitors, vasodilators, p450 aromatase inhibitors and / or antioxidant Petition 870170024642, of 4/13/2017, p. 8/20 1/1