RU2759897C2 - Hair composition containing minoxidil and humic acids - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: group of inventions relates to treatment and prevention of conditions and disorders associated with hair loss. The composition for treatment and prevention of conditions and disorders associated with hair loss includes minoxidil and humic acids in a ratio from 14 to 1 to 5 to 1, wherein the amount of minoxidil and humic acids is 5 to 7 g and 0.5 to 1 g per 500 ml of the composition, respectively. Also disclosed is another variant of implementation of the composition for treatment and prevention of conditions and disorders associated with hair loss.

EFFECT: group of inventions provides an expansion in the range of special purpose preparations.

10 cl, 3 ex

Description

The technical field to which the invention relates

The present invention relates to compositions that contain minoxidil and humic acids for use in the treatment and prevention of conditions and disorders associated with hair loss.

State of the art

The constant increase in the number of people with excessive hair loss, which is a consequence of various types of baldness (alopecia), especially severe forms, is becoming an increasingly urgent problem in dermatology and aesthetic medicine. Alopecia in men, and even more so in women, very often leads to a decrease in the quality of life and impaired psychosocial adaptation. Beautiful thick hair is not only the best natural decoration for a person, but also an important indicator of his health - this is a medical fact. Therefore, the problem of alopecia is one of the areas of drug development.

According to statistics from the World Health Organization (WHO), every second person, 60% of men and 58% of women, notice an increase in hair loss.

Separately, I would like to note that no folk remedies and shampoos for baldness with real alopecia do not help, and if they give any effect, then, as a rule, temporary and after the cessation of use of the drug, the baldness disease increases. Therefore, the development of a particular drug - an anti-alopecia cream is relevant today.

The market for this group of drugs is represented mainly by the substance minoxidil and pentoxidil, which have worked well for external use. After using for one week, hair loss is significantly reduced, and after six months of use, new hair begins to actively appear. It is produced mainly in the form of water-alcohol solutions in sprays (preparations of Aleran, Regain, Generolon). According to preliminary studies carried out in the laboratory of the Nizhny Novgorod State Medical Academy, the bioavailability of this form is low, since the skin, including the head, is susceptible not to hydrophilic, but to lipophilic substances. Therefore, the preferred dosage forms are ointments, emulsions, creams, which are not currently available in pharmacies.

Disclosure invention

The present invention provides compositions for use in the treatment and prevention of hair loss conditions and disorders.

In one embodiment, the present invention provides a composition for the treatment and prevention of conditions and disorders associated with hair loss, comprising minoxidil and humic acids in a weight ratio of 14 to 1 to 5 to 1.

In one embodiment of the present invention, the composition comprises Active Ingredients:

minoxidil,

humic acids,

burdock oil,

poppy oil

D-panthenol,

Knotweed extract,

extract (CO2) nettle,

extract (CO2) hops,

gotu-kola (CO2) extract.

In another embodiment of the present invention, the composition comprises, in addition to the active substances, auxiliary substances selected from:

soybean oil,

Emuvil,

Polysorbat 80,

preservative,

perfume fragrance,

purified water.

In one embodiment, the present invention includes a composition with the following active ingredient composition:

minoxidil - 5-7 g,

humic acids - 0.5-1 g,

burdock oil - 0.5-2 g,

poppy oil - 0.3-1.5 g,

D-panthenol - 0.5-1 g,

Knotweed extract - 0.3-0.7 g,

nettle extract (CO2) - 0.3-0.7 g,

hop extract (CO2) - 0.3-0.7 g,

gotu-kola (CO2) extract - 0.3-0.7 g.

In one embodiment, the composition of the present invention includes excipients in the following amounts:

soybean oil - 1-3 g,

Emuvil - 2-4 g,

Polysorbate 80 - 0.5-1 g,

preservative (potassium sorbate) - 1.2 g,

perfumery fragrance -0.03 g,

purified water - the rest.

In a preferred embodiment of the present invention, a composition for use in the treatment and prevention of conditions and disorders associated with hair loss comprises:

Active ingredients: minoxidil - 5-7 g

humic acids - 0.51 g,

burdock oil - 0.5-2 g,

poppy oil - 0.3-1.5 g,

D-panthenol - 0.5-1 g,

Knotweed extract - 0.3-0.7 g,

nettle extract (CO2) - 0.3-0.7 g,

hop extract (CO2) - 0.3-0.7 g,

gotu-kola (CO2) extract - 0.3-0.7 g,

Excipients: soybean oil - 1-3 g,

Emuvil - 2-4 g,

Polysorbate 80 - 0.5-1 g,

preservative (potassium sorbate) - 1.2 g,

perfumery fragrance -0.03 g, purified water - up to 500 ml.

Active ingredients

Minoxidil

It represents crystals of white or off-white color, which easily dissolve in water to a solution saturation of 5 mg / ml (that is, a 5% solution), as well as in ethanol and propylene glycol. It is the minoxidil solution that is the active component of drugs that restore hair growth.

Minoxidil solution primarily relaxes the blood vessels by dilating them. This increases the blood flow to the hair follicles and enhances their activity at the cellular level. As a result, hair loss is slowed down or completely

stops and healthy hair growth is enhanced. In addition, the minoxidil solution increases the phase of active hair growth, and thus stimulates the hair follicle to produce normal hair. Considering that this process takes a certain amount of time, then the effect of the drug will be noticeable in about the 2-3rd month of use. As a rule, at the 12th month of application, the number of hairs in the phase of active growth reaches its maximum, and then does not increase, and the effect of the drug is stabilized.

Clinical trials have shown that drugs containing minoxidil solution do not always have the desired effect on patients. Sometimes (usually when used on long-term bald areas of the scalp), minoxidil can only cause a small fuzz instead of a full-fledged hairline. But still, with female androgenic alopecia or the initial stage of male androgenic alopecia, the effectiveness of the drug is quite high. The results are much more noticeable if the patient is female, and the earlier the stage of alopecia, the stronger the effect of the use of mincosidil is (this also applies to male patients).

Humic acids

Humic acids are a group of naturally occurring amorphous dark-colored high-molecular aromatic acids, which are released during acidification of an alkaline solution from peat, soil, brown and weathered coal. They are united by a common type of structure, but they have certain differences depending on the nature of the initial substance.

Humic acids activate protein metabolism, normalize the energy metabolism of cells, exhibit a fairly high antifungal activity, and also affect the regeneration processes of the skin and hair follicle

Burr oil

Burdock oil is a very effective natural remedy for hair treatment. Oil not only improves the appearance of damaged hair, it is about a deeper result - hair loss is reduced, the hair structure itself is restored and their further growth is stimulated.

Burdock oil contains:

• vitamins A, C, P, E, B.

• inulin - well cleanses the scalp. In addition, it removes slags, heavy metals, and radionuclides from the human body.

• saturated acids (stearic, palmitic, oleic, etc.).

• minerals and trace elements.

As can be seen from the composition, the beneficial components of burdock oil make it possible to treat almost all diseases of the hair and scalp, such as seborrhea, alopecia, dandruff, excessive dryness or, conversely, oily skin, increased fragility of hair, split ends.

Poppy oil

Poppy seed oil is good for the condition of the hair. By nourishing and moisturizing hair and scalp, it smoothes hair scales, temporarily glues split hair ends, and has a conditioning effect. Poppy seed oil makes combing easier, eliminates dullness and adds shine to the hair.

D-panthenol

D-panthenol is a B vitamin. It accelerates regeneration processes, moisturizes the skin and repairs damaged areas. Improves tissue regeneration when applied externally. It is used in all cosmetic formulations: skin and hair care products, children's cosmetics, aftershave creams, sunscreen cosmetics. Softens the drying effect of the components of the cream.

Action in hair products:

• creates a protective film that has a long-lasting moisturizing effect.

• improves hair styling, penetrates hair follicles and hair strands.

• reduces the formation of damaged hair. Increases hair thickness.

• makes hair shine.

• soothes itching and scalp infections. Heals dry, fine hair and sensitive skin.

CO2 nettle extract

Nettle is one of the plants rich in vitamins, micro and macroelements, biologically active substances. Nettle extract (CO2) contains vitamin C, carotene, flavonoids, phytoncides, choline, formic acid, sterols, histamine, a large amount of calcium, potassium and magnesium salts, trace elements (iron, chromium, copper, manganese, aluminum, vanadium, sulfur, silicon ), chlorophyll (up to 5%), tannins (more than 2%), organic acids, essential oil, sitosterol, phenol carboxylic acids, porphyrins, starch (up to 10%), vitamins B1, B2, B3, B5, K, E, PP.

Nettle extract helps against hair loss, stimulates blood circulation in the scalp and strengthens hair roots, protects dry hair from brittleness, and is effective against seborrhea.

CO2 hop extract

CO2 hop extract contains typical hop compounds myrcene (30-50%) and myrcene, linalool, geraniol, farnesene, caryophyllene, luparol, luparenol, esters of formic, acetic, butyric acid, phytosterols.

In this pharmaceutical composition, the extract restores the fat balance of the hair and scalp, improves metabolic processes in the epidermis, and prevents dandruff and hair loss.

Composition: Natural product 100%. Contains triterpene saponins: asiaticoside (its metabolite - asiatic acid) - has the highest antioxidant activity) and madecassoside (metabolite - madecassonic acid); phytosterols, beta-sitosterol, stigmasterol, campesterol; derivatives of R-1 barrigenol; polyacetylene compounds - incl. acetoxycentellinol, tannins; flavonoids - rutin, kaempferol, quercetin; betulinic acid. Contains a small percentage of caffeine, which increases cell metabolism, increases fat hydrolysis and the release of adrenaline; is a source of catecholamines, magnesium, vitamins A, B, E, K.

Properties: Powerful antioxidant; Possesses dermatoprotective properties, stimulates collagen production; Regenerates skin cells, improves blood microcirculation in the dermis; Regulates water-salt and fat metabolism; Possesses antimicrobial, anti-inflammatory and antiviral activity; Helps strengthen connective tissue

Implementation of the invention

The market for preparations containing minoxidil is presented mainly in the form of aqueous-alcoholic solutions in sprays.

As you know, aqueous-alcoholic solutions of minoxidil have very good bioavailability and permeability through the cell walls, which is also not very good, since additional pressure will be exerted on the hair follicles. Therefore, the first priority was to reduce the bioavailability of minoxidil. There are several ways to solve this problem, the most simple and preferable for minoxidil is the enclosure in a polymer complex based on polyacrylic acid derivatives. However, after the studies carried out, it turned out that the release of minoxidil does not pass completely and the effect of its use is significantly reduced by the polymer component. To modify the polymer complex (to improve the structural and mechanical properties and the completeness of the release of minoxidil), it was proposed to use humic acids. In addition, humic acids - have a bactericidal effect, the ability to positively change metabolic processes, increase the mitotic activity of cells.

Humic acids were obtained from peat by means of alkaline hydrolysis at pH 8.5-9.5, using mild technology, followed by acidification to pH 5-7. As a result, the resulting humic acids contain not only a humic complex of three basic acids, but also all the active substances of the original peat: lipids (including salts of high molecular weight fatty acids and phytosterol), minerals.

Reduction of the amount of secondary products of peat destruction due to mild hydrolysis makes it possible to multiply the content of the humic complex and other biologically active substances and significantly increase the efficiency of minoxidil.

In the course of further research, a new polymer-humic complex of minoxidil was developed with unexpectedly increased efficacy.

It has been shown that the polymer-humic complex of minoxidil, first of all, dilates blood vessels. This increases blood flow to the hair follicles and enhances their activity at the cellular level. As a result, the process of hair loss stops or slows down altogether, and the growth of healthy hair, respectively, is enhanced. Minoxidil in the form of a polymer-humic complex increases the phase of active hair growth, and thus stimulates the hair follicle to produce normal hair.

In turn, in the developed compositions containing polymer complexes, the bioavailability of minoxidil was reduced and the prolongation of action was increased by enclosing it in polymer-humic complexes formed by chemically complementary reticular and linear macromolecules ( complexes of synthetic linear polyelectrolytes (polyacrylic acid salts) with humic acids ), which in turn reduced the risk of excessive pressure on the hair follicle and ensured prolonged action.

Thus, a biologically active polymer complex with minoxidil was developed, which increases blood flow to the hair follicles and enhances their activity at the cellular level. As a result, hair loss slows down or stops altogether, and healthy hair growth is enhanced.

The next task that had to be solved was the study of the biocompatibility of the components of the polymer complex. The biocompatibility of the components of the polymer complex can be assessed by various methods, but in this case it would be most expedient to use the method for assessing cytotoxicity. To assess the cytotoxicity of the polymer complex, the cell suspension was added to Petri dishes and left for 2-3 hours for cell attachment. After that, the samples of the components of the polymer complex were placed in the same Petri dishes and the samples were incubated. After a certain time, polymer samples were removed from the incubation Petri dishes and a biochemical test was performed in accordance with

instructions. The optical density was measured on a spectrophotometer at a wavelength of 450 nm. The measurement was carried out on the 1st, 2nd, 3rd and 4th days of cultivation.

The resulting polymer complexes do not exhibit cytotoxic properties and therefore can be used as a carrier for minoxidil.

In addition, an emulsion base for the cream was developed based on a polymer composition with burdock and poppy oil, which have a good effect on the condition of the hair. In their composition, oils contain more than 70% linoleic and linolenic acids, about 30% oleic acid, palmitic and stearic acids, as well as phytosterols, flavonoids and other useful physiologically active substances. The presence of such a valuable component in the cream makes it possible to increase metabolic reactions, lowers cholesterol and triglyceride levels (this property can play an important role for people with high cholesterol levels), and reduces the risk of excess pressure around the hair follicle. Also, auxiliary substances were selected to create the cream (Emulsifiers, stabilizers, pH regulators, preservatives, antioxidants).

Example 1. Androgenic alopecia

Testing of the cream containing the composition according to the invention was carried out on 15 men aged 35 to 50 years. The duration of alopecia is from 1 to 10 years. Of 15 men, 13 have hair growth, the rest have various psychomatic pathologies.

Example 2. Seborrheic alopecia

Testing of the cream containing the composition according to the invention was carried out on 20 patients aged 35 to 45 years. The duration of alopecia is from 3 months to 10 years. A positive effect was noted in 87% of patients, in the rest - no effect.

Example 3. Oily seborrhea, hair loss

The lotion containing the composition according to the invention was tested on 20 patients aged 18 to 37 years. In all cases, the patients noted a decrease in hair loss, an improvement in their condition. In addition, the condition of the scalp improved, and after a two-week course of application, there was a significant strengthening of the hair and the absence of dandruff.

As a result of studies on the physiological activity of the developed compositions, it was shown that in men the polymer-humic complex with 6% minoxidil is much more effective than the complex with 3% minoxidil, and in women the polymer-humic complex with 6% minoxidil is comparable to 3% minoxidil (subjectively a single application of a complex with 6% minoxidil is perceived better).

Claims (13)

1. Composition for the treatment and prevention of conditions and disorders associated with hair loss, including minoxidil and humic acids in a ratio of 14 to 1 to 5 to 1, where the amount of minoxidil and humic acids is 5-7 g and 0.5-1 g respectively for 500 ml of the composition. 2. A composition according to claim 1, in which minoxidil and humic acids are present in an amount of 5-7 g and 0.5-1 g, respectively, per 500 ml of the composition. 3. The composition of claim 1 further comprising at least one of the following active substances:. Burdock oil, poppy oil, D-panthenol, Polygonum avian extract, the extract (CO _2), nettle extract (CO ₂₎ hop Gotu kola ( CO ₂ ) extract. 4. Composition according to any one of paragraphs. 1-3, additionally containing at least one of the following auxiliary substances: soybean oil, Emuvil, Polysorbate 80, preservative, perfume fragrance, purified water. 5. Composition according to any one of paragraphs. 1-3, containing per 500 ml: Minoxidil 5-7 g Humic acids 0.5-1 g Burdock oil 0.5-2 g Poppy oil 0.3-1.5 g D-panthenol 0.5-1 g Knotweed extract 0.3-0.7 g Extract (СО ₂ ) nettle 0.3-0.7g Hop extract (СО ₂₎ 0.3-0.7 g Gotu-kola (CO ₂ ) extract 0.3-0.7 g 6. Composition according to claim 4, containing, per 500 ml of composition: Soybean oil 1-3 g Emuvil 2-4 g Polysorbate 80 0.5-1 g Preservative 1.2 g Perfume fragrance 0.03 g 7. Composition for the treatment and prevention of conditions and disorders associated with hair loss, containing 500 ml: Minoxidil 5-7 g Humic acids 0.5-1 g Burdock oil 0.5-2 g Poppy oil 0.3-1.5 g D-panthenol 0.5-1 g Knotweed extract 0.3-0.7 g Extract (СО ₂ ) nettle 0.3-0.7 g Hop extract (СО ₂₎ 0.3-0.7 g Gotu-kola (CO ₂ ) extract 0.3-0.7 g Soybean oil 1-3 g Emuvil 2-4 g Polysorbate 80 0.5-1 g Preservative 1.2 g Perfume fragrance 0.03 g Purified water Rest 8. Composition according to any of the preceding claims in the form of a cream. 9. A composition according to any one of the preceding claims in the form of a lotion. 10. A composition according to claim 6 or 7, wherein the preservative is potassium sorbate.