RU2812523C1 - Composition of medicinal product for stimulating hair growth - Google Patents

Abstract

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to the treatment and prevention of baldness. The composition of the medicinal product for stimulating hair growth consists of, in wt.%: 0.002–0.1% of Trehalose; 250–450 kDa of Sodium hyaluronate from 0.5 to 5.0%; 0.001–0.1% of Acetyl Tetrapeptide-3; 0.001–0.1% of Acetyl Hexapeptide-18; 0.001–0.1% of Octapeptide-2; 0.001–0.1% of Oligopeptide-42; 14.500–19.494% of Deionized water and 12 80% of Nutrient medium 199/DMEM F.

EFFECT: invention provides a stimulating effect on the cellular structures of the hair, reducing the amount of hair loss and enhancing hair growth.

1 cl, 4 dwg, 4 tbl, 3 ex

Description

The invention relates to the composition of a medicinal product for the treatment and prevention of baldness.

There is a known RF patent for invention No. 2 535 120 “WAYS TO REDUCE HAIR LOSS AND/OR STIMULATE THEIR GROWTH AND/OR RESTORATION OF GROWTH.”

A method of reducing hair loss and/or promoting or restoring hair growth, comprising the steps of applying to the skin of a mammal in need of such treatment a safe and effective amount of a composition containing from about 0.1% to about 100% (by weight) of an additive containing:

a. from about 0.01% to about 99.98% (by weight of the additive) sodium pyruvate;

b. from about 0.01% to about 99.98% (by weight of additive) antioxidant; And

c. from about 0.01% to about 99.98% (by weight of additive) of the mixture

fatty acids or a source of a fatty acid mixture comprising at least 7 unsaturated or saturated fatty acids selected from the group consisting of butyric acid, caproic acid, caprylic acid, capric acid, lauric acid, myristic acid, myristoleic acid, palmitic acid , palmitoleic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidic acid, gadoleic acid, pentadecanoic acid, margaric acid, margaroleic acid, behenic acid, dihomolinoleic acid, arachidonic acid and lignoceric acid.

There is a well-known RF patent for invention No. 2 309 730 “THE MEANS FOR STIMULATING HAIR GROWTH, ITS VARIANTS AND METHOD FOR ITS OBTAINING.”

1. Use of pantothenic acid derivatives, namely ammonium salts with PEPTIDES, formula I

Enlarged image (opens in a separate window)

where X=OH, Trp; Y=OH, Trp,

as a hair growth stimulator.

2. Use of pantothenic acid derivatives, namely pantothenic acid conjugates with peptides, formula II

Enlarged image (opens in a separate window)

where X=OH, Trp; Y=OH, Trp,

as a hair growth stimulator.

The Russian Federation patent for invention No. 2 671 511 “COSMETIC COMPOSITION FOR HAIR AND SCALP CARE (OPTIONS)” is known.

The invention relates to the cosmetic industry and is a cosmetic composition for hair and scalp care containing lupine proteins, mint aqueous extract, orange fruit aqueous extract, sweet clover aqueous extract, vitamin PP, a complex consisting of sodium lactate and the following amino acids: sodium pyroglutamate , arginine, aspartic acid, glycine, alanine, serine, valine, proline, threonine, isoleucine, histidine, phenylalanine, a transdermal carrier, which is a low molecular weight HYALURONIC ACID with a molecular weight of less than 130 kDa, a preservative and water, and the components in the composition are in a certain ratio in wt.%. The invention provides an expansion of the arsenal of hair and scalp care products, is hypoallergenic, non-toxic, is highly effective against hair loss, as well as eliminating the causes of alopecia, seborrhea, enhances hair growth, reduces treatment time, ensures long shelf life without the use of antibiotics and other toxic and hazardous to health preservatives, does not require mandatory rinsing after use.

The disadvantages of the proposed solutions are that the above formulations do not affect the entire spectrum of the pathogenesis of alopecia, preventing hair loss and/or stimulating their growth in certain types of alopecia.

The objective of the present invention is to create a drug for stimulating hair growth, which accelerates hair growth and stimulates improvement in the quality of hair in diffuse alopecia after infections; alopecia caused by taking certain medications; alopecia in deficiency conditions; alopecia in chronic diseases; hair loss after pregnancy and after breastfeeding; androgenetic alopecia; fragility, thinning, thinning of hair; graying of hair; dry scalp; seborrheic dermatitis of the scalp.

The technical result achieved by the proposed composition of the drug for stimulating hair growth is:

• acceleration of hair growth;

• noticeable reduction in hair loss;

• increasing hair thickness;

• improving hair quality;

• reduction of gray hair;

• moisturizing the scalp.

The task has been solved, the technical result has been achieved due to the fact that the composition of the drug for stimulating hair growth includes components that influence the pathogenesis of the main types of alopecia: diffuse hair loss and androgenic alopecia and have a stimulating effect on the cellular structures of the hair, due to which the proposed product has a pronounced aesthetic effect, manifested by a pronounced decrease in the amount of hair falling out, increased hair growth on the scalp, thickening of the hair shaft, their shine, absence of seborrhea, dryness, flaking of the scalp. In this case, the components are used in the following mass% ratio: Trehalose from 0.002 to 0.1%; Sodium hyaluronate 250-450 kDa from 0.5 to 5.0%; Acetyl Tetrapeptide-3 from 0.001 to 0.1%; Acetyl Hexapeptide-18 from 0.001 to 0.1%; Octapeptide-2 from 0.001 to 0.1%; Oligopeptide-42 from 0.001 to 0.1%; Deionized water from 14.500 to 19.494% and Nutrient medium 199/DMEM F – 12 80%.

A person loses approximately 100 hairs every day; an increase in this number may indicate pathological processes in the body.

Hair density varies from person to person and in different areas of the body. It depends on age, gender, race, etc.

Hair goes through 3 main growth phases: anagen, catagen and telogen. Anagen is the phase of active hair growth - its duration ranges from 2 to 5 years. During the day, hair lengthens by an average of 0.1–0.4 mm, and women's hair grows faster than men's. During the catagen phase, growth slows down and lasts from 4 to 6 weeks. During the telogen phase, hair growth stops, its life cycle ends, and it falls out. This period lasts 2–3 months and during this time conditions are created for the start of a new anagen phase.

Partial hair loss, or total baldness, or hirsutism or hypertrichosis occur due to disturbances in the hair cycle. Increased hair loss occurs for several reasons: during the period of hormonal changes in the body, after using certain medications, after suffering serious illnesses, etc. - this occurs due to a disruption in the supply of necessary nutrients to the hair and a reduction or premature completion of the hair growth phase (anagen).

Taking nonsteroidal anti-inflammatory drugs, anticoagulants, thyreostatics, antidepressants, cytostatics, beta-blockers, interferon alpha drugs, anticonvulsants, antiparkinsonians, anthelmintics, antiherpetic, antiviral, antibacterial drugs, neuroleptics, oral contraceptives, etc. can lead to increased hair loss.

80% of cancer patients taking cytotoxic drugs experience hair loss within 10 days of starting treatment.

Infectious, autoimmune, systemic diseases, endocrine pathologies also lead to excessive hair loss.

As a person ages, hair growth on the scalp may be stable, but the anagen phase tends to decrease. Hair becomes thinner and brittle.

Hair loss occurs in males and females at any age, and can be represented by both diffuse hair loss (telogen and anogen effluvium) and androgenetic alopecia (male-pattern hair loss).

Insolation, dry air, the use of a hot hair dryer, aggressive shampoos, and dyes can also have a negative impact on the condition of the hair. This occurs due to disruption of the “tile-like” arrangement of hair scales, leading to splitting of the hair shaft and increased fragility.

Increased hair loss causes stress and can lead to psychological disturbances.

The invention is illustrated by the following figures:

In fig. 1 – images are presented for example 1 (before A and after B of using the drug for hair stimulation, respectively).

In fig. 2 – images are presented for example 2 (before A and after B of using the drug for hair stimulation, respectively).

In fig. 3 – images are presented for example 3 (before A and after B of using the drug for hair stimulation, respectively).

In fig. 4 – images are presented for example 3 (before A and after B of using the drug for hair stimulation, respectively).

For the proposed composition of the drug to stimulate hair growth, the following components are used:

• Trehalose TREHALOSE is a non-reducing sugar formed from two glucose units linked by a 1-1 alpha bond, giving it the name α-D-glucopyranosyl - (1→1) - α-D-glucopyranoside. The binding makes trehalose very resistant to acid hydrolysis and therefore stable in solution at high temperatures, even under acidic conditions. The main function is hydration: trehalose has high moisture-binding properties, as well as the function of protecting proteins and other structural molecules: this natural disaccharide perfectly prevents their drying out and degradation.

• Sodium Hyaluronate 250-450 kDa Sodium Hyaluronate 250-450 kDa Sodium hyaluronate is the sodium salt of hyaluronic acid, a glycosaminoglycan found in various human connective tissues. Sodium hyaluronate is a voluminous additive to the intracellular matrix, replenishing the deficiency of hyaluronic acid in tissues and eliminating skin dehydration.

• Acetyl Tetrapeptide-3 Acetyl Tetrapeptide -3 Biomimetic peptide of 4 amino acids, a signal peptide derivative that stimulates changes in tissues. The peptide acts directly on the hair follicle.

The main function of acetyltetrapeptide-3 is the synthesis of key components of the extracellular matrix in the skin tissues of the scalp. According to research, the expression of type III collagen increased by 65%, and the expression of laminins (structural proteins of the extracellular matrix that form a reliable attachment of the hair in the follicle) - by as much as 285%. The result is a strengthening of the extracellular matrix “substrate” to firmly fix the hair follicle in the skin.

Acetyl Tetrapeptide-3 reduces microinflammation around the hair follicles and inhibits an enzyme called 5-alpha reductase, which is involved in the synthesis of the hormone dihydrotestosterone, leading to androgenic alopecia. The study showed a 46% increase in the ratio of the growth phase of the hair follicle to the regression phase, causing the hair to become noticeably thicker.

• Acetyl Hexapeptid-18 Acetyl Hexapeptid - 18 normalizes microcirculation in the area of hair follicles.

This peptide is capable of restoring impaired microcirculation at any stage: be it a narrowing of blood vessels (spasms) leading to sclerotic changes in microvessels, or a pathological dilatation of blood vessels and stagnation of blood flow in the blood vessels.

Thus, the peptide has unique characteristics that allow it to act in two directions: expand spasmodic capillaries and narrow dilated capillaries. Dilation of blood vessels leads to blood stagnation, accumulation of blood cells in the blood vessels and their diapedesis, and this worsens the condition of the hair follicle and blocks its blood supply.

These processes have a receptor mechanism, which means that the peptide interacts directly with the receptors of the vascular walls and stabilizes their tone.

Hexapeptide 18 provides stabilization of mast cells (mast cells): it blocks their degranulation and the release of biologically active elements.

Among other important characteristics, the peptide has a powerful lymph-stimulating effect.

The skin's ability to restore and maintain microcirculation is stimulated by the flow of lymph in the numerous lymphatic capillaries of the skin.

Hexapeptide 18 has the highest level of lymph stimulating activity of all known agents of this type, and it has no undesirable side effects (diapedesis of erythrocytes and leukocytes, microhemorrhages, blood stasis in capillaries). The peptide causes activation of the walls and valves of lymphatic vessels, which leads to their intense contraction, and subsequently, an increase in the intensity of lymph flow.

Increased lymphatic flow helps remove toxins from the skin, reduce puffiness and remove excess water from interstitial tissues.

• Octapeptid-2 Octapeptid-2 is a bilayer encapsulated biomimetic peptide that helps increase cell growth and migration. Activates the stem cells of the hair follicle, stimulating the appearance of new hair. Octapeptide-2 - stimulates the proliferation of dermal fibroblasts, increasing the size of hair follicles and increases the production of vascular endothelial growth factor, accelerating hair formation.

• Oligopeptide-42 Acetyl Oligopeptide - 42 improves microcirculation and increases fibroblast proliferation. Activates the stem cells of the hair follicle, stimulating the appearance of new hair. Stimulates the proliferation of dermal fibroblasts, increasing the size of the hair follicle, and increases the production of vascular endothelial growth factor, accelerating hair formation.

• Deionized water Deionized water is water purified from impurity ions. Such water has a high resistivity. It is a liquid from which all charged particles of impurities have been artificially removed - this is the purest compound of hydrogen and oxygen known to science: it consists of 99.99999991% H2O molecules.

Key Features:

high resistivity – reaches 18 MOhm/cm and is a characteristic indicator of the degree of impurity removal;

extremely low electrical conductivity due to the fact that the salt concentration in DI tends to zero;

maximum degree of purification - the already mentioned 99.9... percent, smoothly flowing from the two previous parameters;

impressive chemical activity (due to which DM water even needs to be kept in a fluoroplastic container) - absorbs charged particles of gases, acidic residues, and metals contained in the air;

universal solubility - absorbs everything just listed (thus becoming contaminated).

Even spring water is not suitable for preparing masks, creams, and gels, since it still contains heavy metal ions, salts, and microorganisms. Pharmaceuticals need a highly purified liquid that can accelerate the mechanisms of cell division. This is what DI became: it promotes the healing of pustules, traces of pustules, wounds, slowing down the aging process and the formation of wrinkles, without having a negative bacteriological effect.

It also helps to launch skin rejuvenation processes and generally improve its condition, which is why it is included in various cosmetics. Its separate advantage is that it extends the shelf life of cosmetics.

Method of obtaining:

The process of obtaining Deionized water is completely carried out in laboratory conditions, using standardized equipment of the Aqualab AL-1 UF water treatment system.

The process of isolating Deionized water is a four-step process:

1. A stream of H2O from an artesian well (or other natural source) is driven through a distiller - this is the primary purification, which allows the removal of foreign mechanical impurities, molecules with complex compounds, and bacteria.

2. The resulting liquid undergoes preliminary reverse osmosis, that is, it is passed through a membrane and combined filters, and reaches the state of distillate.

3. The main stage is the passage of liquid through the installation with a loading of resin - either cation exchanger R-H or anion exchanger R-OH. This makes it possible to completely remove foreign charged particles.

4. The separated DI is poured into a fluoroplastic container in which it is stored.

As a result, DM water is obtained, consisting of 99.9(9)% H2O molecules.

The resulting Deionized water undergoes all necessary tests to ensure compliance with the necessary parameters: resistance coefficient, etc.

This water treatment system is necessary to obtain completely purified water, free of all kinds of impurities. Such impurities include organic substances, inorganic ions, gases, microorganisms contained in it in dissolved and suspended form. Water treatment is carried out in accordance with the existing international standard that determines the quality of water that can be used in the production of cosmetics.

• Nutrient medium 199/DMEM F - 12 – vitamin – mineral – amino acid solution – helps eliminate deficiencies and stabilize the level of essential minerals, vitamins and amino acids in the skin.

Table No. 1. The principle of action of the components of the drug to stimulate hair growth is presented.

Component Operating principle Trehalose TREHALOSE The main function is moisturizing: it has high moisture-binding properties, as well as protecting proteins and other structural molecules: this natural disaccharide perfectly prevents them from drying out and degradation. Sodium hyaluronate 250-450 kDa
Sodium Hyaluronate 250-450 kDa It is a voluminous additive to the intracellular matrix, replenishing the deficiency of hyaluronic acid in tissues, eliminating skin dehydration. Acetyl Tetrapeptide-3 Acetyl Tetrapeptide-3 The main function is the synthesis of key components of the extracellular matrix in the skin tissues of the scalp. According to studies conducted in the manufacturer's laboratory, the expression of type III collagen increased by 65%, and the expression of laminins (structural proteins of the extracellular matrix that form a reliable attachment of the hair in the follicle) - by as much as 285%. The result is a strengthening of the extracellular matrix “substrate” for strong hair rooting. Acetyl Hexapeptid-18 Acetyl Hexapeptid - 18 Normalizes vascular tone, helps restore blood supply, frees blood vessels from the accumulation of blood cells, which leads to an increase in the speed of blood flow, while simultaneously improving the inflow and outflow of blood in microcapillaries. These processes have a receptor mechanism, which means that the peptide interacts directly with the receptors of the vascular walls. Octapeptid-2 Helps increase cell growth and migration. Activates hair follicle stem cells, stimulating the appearance of new hair, stimulates the proliferation of dermal fibroblasts, increasing the size of the hair follicle, and increases the production of vascular endothelial growth factor, accelerating hair formation. oligopeptide-42
Acetyl Oligopeptide - 42 Activates the stem cells of the hair follicle, stimulating the appearance of new hair. Stimulates the proliferation of dermal fibroblasts, increasing the size of the hair follicle, and increases the production of vascular endothelial growth factor, accelerating hair formation. Deionized water
Deionized water Helps to launch skin rejuvenation processes and generally improve its condition. It is a liquid from which all charged particles of impurities have been artificially removed; it is the purest compound of hydrogen and oxygen known to science: it consists of 99.99999991% H2O molecules. Nutrient medium 199/DMEM F - 12 Vitamin-mineral-amino acid complex helps eliminate deficiencies and stabilize the level of essential vitamins, minerals and amino acids in the skin.

The proposed invention, due to its composition, allows you to expand the range of effects on all parts of the pathogenesis of alopecia, namely: hair loss due to deficiency of microelements and vitamins, stress, negative effects of medications, hair loss after illnesses, as well as due to hormonal changes, including hair loss after pregnancy and lactation and due to increased sensitivity of hair to androgens (Androgenic alopecia). The proposed invention has a stimulating effect both at the cellular level, and also has a pronounced aesthetic effect, thus making it possible to stabilize and/or stop hair loss in the shortest possible time, has a stimulating effect on hair follicles, preventing their miniaturization, promotes thickening of the hair shaft, preventing fragility and dull color, stops hair graying, moisturizes the scalp, preventing the development of dryness and seborrhea.

The composition of the drug for stimulating hair growth consists of: Trehalose TREHALOSE, Sodium hyaluronate 250-450 kDa Sodium Hyaluronate 250-450 kDa, Acetyl Tetrapeptide-3 Acetyl Tetrapeptide -3, Acetyl Hexapeptid-18 Acetyl Hexapeptid – 18, Octapeptid-2 Octapeptid-2, oligopeptide-42 Acetyl Oligopeptide – 42, Nutrient medium 199/ DMEM F-12 199/ DMEM F-12, Deionized water, with the components used in the following mass% ratio: Trehalose from 0.002 to 0.1%; Sodium hyaluronate 250-450 kDa from 0.5 to 5.0%; Acetyl Tetrapeptide-3 from 0.001 to 0.1%; Acetyl Hexapeptide-18 from 0.001 to 0.1%; Octapeptide-2 from 0.001 to 0.1%; Oligopeptide-42 from 0.001 to 0.1%; Deionized water from 14.500 to 19.494% and Nutrient medium 199/DMEM F – 12 80%.

The authors conducted studies proving that the proposed composition of the drug for stimulating hair growth works at the following ratios, wt %:

Table No. 2

Component mass % Trehalose 0.002 Sodium hyaluronate 250-450 kDa 0.5 Acetyl Tetrapeptide-3 0.001 Acetyl Hexapeptide-18 0.001 Octapeptide-2 0.001 oligopeptide-42 0.001 Deionized water 19,494 Nutrient medium 199/DMEM F-12 up to 80

Table No. 3

Component mass % Trehalose 0.1 Sodium hyaluronate 250-450 kDa 5.0 Acetyl Tetrapeptide-3 0.1 Acetyl Hexapeptide-18 0.1 Octapeptide-2 0.1 oligopeptide-42 0.1 Deionized water 14,500 Nutrient medium 199/DMEM F-12 80

Table No. 4

Component mass% Trehalose 0.01 Sodium hyaluronate 250-450 kDa 1.0 Acetyl Tetrapeptide-3 0.01 Acetyl Hexapeptide-18 0.01 Octapeptide-2 0.01 oligopeptide-42 0.01 Deionized water 18,950 Nutrient medium 199/DMEM F-12 80

The invention is illustrated by the following examples of the use of the proposed composition of the drug to stimulate hair growth on the scalp, the volume used: 2 - 5 ml of the proposed composition in one procedure with an interval of 1 time in 14 days.

Example 1.

The patient is a man, 28 years old. Complaints of significant hair thinning in the parietal and frontotemporal areas over the past two years. From the medical history: somatically healthy, denies chronic diseases, denies bad habits, denies taking medications. I contacted a cosmetologist with complaints about a decrease in the amount of hair on the scalp. A preliminary diagnosis was made: Androgenic alopecia, unspecified. 3 procedures were carried out with the drug of the intended composition, 2.5 ml per procedure, with an interval of 14 days between procedures. No concomitant external or internal therapy was carried out.

Result after use (three procedures): cessation of hair loss, increased hair growth and thickness over the entire surface of the scalp. (see Fig. 1 A, B)

Example 2.

The patient is a man, 50 years old. Complaints of hair loss in the occipital-parietal region of the head. From the anamnesis: according to him, he is healthy, denies chronic diseases, denies bad habits, denies taking medications. Notes gradual, slow hair loss and a pronounced decrease in the amount of hair over 5 years. I contacted a cosmetologist with complaints of hair loss in the occipital-parietal area of the head. A preliminary diagnosis was made: Androgenic alopecia, unspecified. 4 procedures were carried out with the drug of the intended composition, 2.5 ml per procedure, with an interval of 14 days between procedures. No concomitant external or internal therapy was carried out.

Result after use (four procedures): cessation of hair loss, increased growth and a marked increase in hair density in the occipital-parietal region of the head. (see Fig. 2 A, B)

Example 3.

The patient is a woman, 36 years old. Complaints of diffuse hair loss over the entire surface of the scalp. From the medical history: somatically healthy, denies bad habits, denies taking medications at the time of examination. Over the course of a year, after suffering an acute respiratory viral infection, he notices constant hair loss and a significant decrease in the volume and thickness of the hair, its fragility and dull color, the appearance of depigmented (gray) hair, dryness and flaking of the scalp. I contacted a cosmetologist with complaints about hair loss over the entire surface of the scalp, dull hair color, fragility and flaking of the scalp. A preliminary diagnosis was made: Non-scarring hair loss, unspecified. 3 procedures were carried out with the drug of the intended composition, 2.5 ml per procedure, with an interval of 14 days between procedures. No concomitant external or internal therapy was carried out.

Result after use (three procedures): cessation of hair loss, increased growth, marked reduction in hair fragility, reduction in the amount of depigmented (grey) hair, elimination of dryness and flaking of the scalp. (see Fig. 3 A, B and Fig. 4 A, B)

All the examples given confirm the fulfillment of the task, namely: the creation of a drug to stimulate hair growth, which accelerates hair growth and stimulates improvement in the quality of hair in diffuse alopecia after infections; alopecia caused by taking certain medications; alopecia in deficiency conditions; alopecia in chronic diseases; hair loss after pregnancy and after breastfeeding; androgenetic alopecia; fragility, thinning, thinning of hair; graying of hair; dry scalp; seborrheic dermatitis of the scalp.

All of the above examples confirm the industrial applicability of the proposed composition of the drug for stimulating hair growth.

Claims (2)

The composition of the drug for stimulating hair growth consists of: Trehalose (TREHALOSE), Sodium Hyaluronate 250-450 kDa, Acetyl Tetrapeptide-3, Acetyl Hexapeptid - 18 , Octapeptid-2, oligopeptide-42 (Acetyl Oligopeptide – 42), Nutrient medium 199/ DMEM F-12 (199/ DMEM F-12), Deionized water, and the components are used in the following wt.% ratio: Trehalose from 0.002 to 0.1 Sodium hyaluronate 250-450 kDa from 0.5 to 5.0 Acetyl Tetrapeptide-3 from 0.001 to 0.1 Acetyl Hexapeptide-18 from 0.001 to 0.1 Octapeptide-2 from 0.001 to 0.1 Oligopeptide-42 from 0.001 to 0.1 Deionized water from 14,500 to 19,494 Nutrient medium 199/DMEM F 12 80