KR102302131B1 - Composition for hair tonic or treating or preventing hair loss - Google Patents

Abstract

Disclosed is a pharmaceutical composition for preventing or treating hair loss that includes a ceramide component and a spicule capable of penetrating the pharmaceutical composition into the inside of the scalp, which facilitates penetration of an active component into the inside of the scalp. The pharmaceutical composition for preventing or treating hair loss according to an embodiment of the present invention can include a ceramide.

Description

Prevention, treatment, or composition for hair growth of hair loss {Composition for hair tonic or treating or preventing hair loss}

The present invention relates to a composition for prevention, treatment, or hair growth of hair loss, and more particularly, penetration of an active ingredient into the inside of the scalp, including a spicule that can penetrate it into the inside of the scalp with a ceramide component It relates to a pharmaceutical composition for the prevention or treatment of easy hair loss.

Testosterone is involved in the normal aspects of male physical characteristics such as increase in skeletal muscle, genital development, spermatogenesis, and sexual desire, and dihydrotestosterone is involved in the negative aspects of acne, sebum increase, hair loss, and prostatic hyperplasia. It is known to be caused by tissue involvement. Among them, research on hair loss, which occurs a lot in men, has been conducted for a long time, but the mechanism of hair loss and hair growth has not yet been accurately elucidated.

Hair is a living organism that regularly repeats the cyclical changes of growth, regression, and resting phases, and since each hair repeats independent creation and extinction, it always maintains a constant number of hairs. The number of hair is determined from birth, but after puberty, the process of hair growth due to the influence of sex hormones is often mistaken for an increase in the number. The growth phase is the period in which hair grows due to active cell division and activity of hair follicles, and it lasts for about 2-6 years, accounting for about 85% of the total hair. During the growth phase, hair follicle cells are surrounded by dermal papilla of stromal cells and have a circular shape, and cell division for the generation of new hair is active. The catagen stage is a period in which hair follicle growth activity stops and rapidly atrophys, and the shape of the hair at this time is similar to a club. It takes about 2-3 weeks and accounts for about 5% of the total hair. The resting phase is a period in which the cell activity of the hair follicles completely disappears. During the period of 2-3 months, it is pushed out by the growing hair that grows from the base of the resting hair, or naturally falls out by mechanical action such as combing or washing the hair. . In general, alopecia refers to an increase in the number of abnormal hair loss due to the shortening of the proportion of hair in the growth phase and more hair in the degenerative phase or telogen phase during this cycle.

The causes of alopecia, in which hair falls out from the scalp, are various, and are broadly divided into male hormone action, mental stress, lipid peroxide accumulation in the scalp, drug side effects, chronic diseases such as leukemia or tuberculosis, side effects caused by radiation therapy, nutrition deficiency, etc. In addition, in recent years, hair loss, which has been known to be a problem for men, is increasing in demand for prevention and treatment of female hair loss and young people's hair loss.

Drugs currently used as hair growth and hair growth agents include vasodilators to circulate sufficient blood to the scalp, female hormones to inhibit the action of male hormones, and 5α- to convert testosterone into 5-dihydrotesteone (5-DHT). There are testosterone activity inhibitors that inhibit reductase. The vasodilators include capronium chloride, minoxidil, and various plant extracts, the female hormone agents include estrogen, estradiol, and progesterone, and the male hormone activity inhibitors include finasteride and pentadecanoic acid.

However, due to insufficient effects or side effects of the treatment for hair loss, there is a need for a more effective and safe treatment for hair loss or development of a drug for hair growth. Minoxidil administered for topical or oral use causes irritation to the skin such as erythema, inflammation, infection, irritation, or pain of the scalp. There are problems such as In addition, finasteride has disadvantages such as erectile dysfunction and a decrease in sexual desire due to the effect of inhibiting male hormone activity.

On the other hand, phytosphingosine is one of the structures constituting ceramide, which occupies more than 40% of the elements constituting the lipid bilayer of the stratum corneum of the skin. Therefore, phytosphingosine is absorbed into the body and promotes ceramide synthesis, prevents moisture evaporation by itself, and moisturizes the skin. However, since these ceramide components correspond to organic substances with large molecules, when used for external use on the skin, their absorption is limited, so the effect is also limited.

(0001) Republic of Korea Patent No. 10-2134538 (0002) Republic of Korea Patent No. 10-2196084

The present invention has been devised to solve the above problems, and an object of the present invention is to provide a hair loss prevention composition having excellent penetration into the scalp.

Another object of the present invention is to provide a hair loss prevention composition that has a ceramide component as a main component and minimizes side effects of the human body compared to the existing hair loss prevention composition using a hormone inhibitor as a main component.

The problems of the present invention are not limited to the problems mentioned above, and other problems not mentioned will be clearly understood by those skilled in the art from the following description.

The pharmaceutical composition for preventing or treating hair loss according to an embodiment of the present invention for solving the above problems may include a ceramide.

In one embodiment, the composition for the prevention, treatment or hair growth of the hair loss, 0.5 to 3 parts by weight of ceramide; Spicule 0.2 to 1.5 parts by weight; 1-3 parts by weight of glycerin; 1 to 3 parts by weight of aroma oil; 10-20 parts by weight of ethanol, 0.1-2 parts by weight of menthol; and 40 to 60 parts by weight of distilled water, wherein the ceramide has a structure of the following Chemical Formula 1,

[Formula 1]

(In Formula 1, R is hydrogen or COR1, R1 is C1-C6 alkyl)

The spicule, (i) washing the collected sponge, then drying the moisture content to less than 10% by weight; (ii) heating the dried sponge by immersing it in water at a temperature of 90 to 100° C. for 10 to 40 minutes; (iii) immersing the heated sponge in an acidic solution of pH 2 to 4 for 10 to 20 days; (iv) separating the acidic solution and the solid content of the sponge, then washing the solid content with water repeatedly 2 to 5 times; (v) immersing the washed solids in water and then washing them using ultrasonic waves; (vi) immersing the sponge in a basic solution of pH 8 to 10 for 1 to 5 days after the ultrasonic cleaning is completed; (vii) separating the basic solution and the solid content, then washing the solid content with water repeatedly 2 to 5 times; and (viii) immersing the washed solids in water and then washing them using ultrasonic waves, wherein the acidic solution is lemon juice, citron juice, sugar citron juice, orange juice and vinegar. It is a mixture of one or more selected from the group comprising the steps of washing the basic solution after separating the shell; calcining the washed clam shells at a temperature of 800 to 1200 °C; pulverizing the calcined shellfish; mixing the pulverized clam shells with 1000 to 5000 parts by weight of water based on 100 parts by weight of the clam shells, and then leaving them to stand for 2 to 10 days; And it is a solution prepared by a method comprising the step of separating the solid content of the shellfish, the ultrasonic wave has a frequency of 20 ~ 130kHz, the aroma oil is lavender, rosemary, eucalyptus, cypress, bergamot, sandalwood, rose and It is one or more extracts selected from the group of lemons, and the composition for prevention, treatment or hair growth of hair loss may further include an emulsifier, a sunscreen, a moisturizer, a preservative, a pH adjuster, a thickener or other additives.

According to an embodiment of the present invention, as it contains a ceramide component as an active ingredient, it is a pharmaceutical for preventing or treating hair loss that has a high effect of improving hair loss while minimizing side effects of the human body compared to a hair loss prevention composition using a conventional hormone inhibitor. compositions can be provided.

In addition, by including the spicule having a porous needle-like structure extracted from the sponge, it is possible to easily penetrate the spicule, a polymer material, into the stratum corneum. It is possible to provide a composition for prevention, treatment or hair growth of hair loss.

In addition, it is possible to provide a pharmaceutical composition for preventing or treating hair loss that can minimize skin irritation caused by chemicals by using only natural acidic and natural basic materials when preparing porous spicules.

In addition, it contains a large amount of needle-type spicules, and when applied to the scalp, it improves blood circulation to the scalp by stimulation by needle-type spicules to provide a pharmaceutical composition for preventing or treating hair loss that can maximize hair growth and hair growth effects. can

The effect according to the present invention is not limited by the contents exemplified above, and more various effects are included in the present invention.

1 is a view showing a pharmaceutical composition for preventing or treating hair loss according to an embodiment of the present invention.
Figure 2 is a photograph showing the experimental results of mice of the pharmaceutical composition for the prevention or treatment of hair loss according to an embodiment of the present invention.

Hereinafter, various embodiments will be described in more detail with reference to the accompanying drawings. The embodiments described herein may be variously modified. Certain embodiments may be depicted in the drawings and described in detail in the detailed description. However, the specific embodiments disclosed in the accompanying drawings are only for easy understanding of various embodiments. Therefore, the technical spirit is not limited by the specific embodiments disclosed in the accompanying drawings, and it should be understood to include all equivalents or substitutes included in the spirit and scope of the invention.

Terms including an ordinal number, such as first, second, etc., may be used to describe various elements, but these elements are not limited by the above-described terms. The above terminology is used only for the purpose of distinguishing one component from another component.

In this specification, terms such as "comprises" or "have" are intended to designate that the features, numbers, steps, operations, components, parts, or combinations thereof described in the specification exist, but one or more other features It should be understood that it does not preclude the possibility of the presence or addition of numbers, steps, operations, components, parts, or combinations thereof. When a component is referred to as being “connected” or “connected” to another component, it is understood that the other component may be directly connected or connected to the other component, but other components may exist in between. it should be On the other hand, when it is mentioned that a certain element is "directly connected" or "directly connected" to another element, it should be understood that the other element does not exist in the middle.

Meanwhile, as used herein, a “module” or “unit” for a component performs at least one function or operation. And “module” or “unit” may perform a function or operation by hardware, software, or a combination of hardware and software. In addition, a plurality of “modules” or a plurality of “units” other than a “module” or “unit” to be performed in specific hardware or to be executed in at least one processor may be integrated into at least one module. The singular expression includes the plural expression unless the context clearly dictates otherwise.

In addition, in describing the present invention, when it is determined that a detailed description of a related known function or configuration may unnecessarily obscure the gist of the present invention, the detailed description thereof will be abbreviated or omitted.

The present invention relates to a pharmaceutical composition for preventing or treating hair loss comprising a ceramide.

The ceramide may have a structure of Formula 1 below.

[Formula 1]

(In Formula 1, R is hydrogen or COR1, R1 is C1-C6 alkyl)

In the case of Chemical Formula 1, it has a structure corresponding to phytosphingosine used as a moisturizer and a treatment for acne among ceramides, and its derivative has the same or greater effect as minoxidil on the prevention, treatment, or hair growth of hair loss, but on the skin of conventional minoxidil. The composition according to the present invention was developed by discovering that it is preferable because there is no side effect such as irritation or careful administration to hypertensive patients.

The compound of Formula 1 may be prepared using conventional knowledge known in the field of organic chemistry, for example, S. Li, W.K. Wilson, G. J. Schroepfer, Chemical synthesis of D-ribo-phytosphingosine-1-phosphate, a potential modulator of cellular processes. J. Lipid Res. 40: 117-125, 1999.

It was demonstrated in the following Examples that the compound of Formula 1 is effective in treating, preventing, and restoring hair loss. Specifically, the compound of the present invention was tested for hair growth using balb/c mice. As a result, the compound of the present invention exhibited a hair growth effect equal to or greater than that of Rogaine 5% (minoxidil 5% solution, Johnson & Johnson) currently being licensed as a hair loss treatment by the FDA. In addition, the angiogenesis activity of the compound of the present invention was measured by a chorioallantoic membrane (CAM) assay, phosphate buffer solution as a negative control, sphingosine-1-phosphate as a positive control, and TMP, an angiogenesis inhibitor as an inhibitory control. (trimethylphytosphingosine) was compared. As a result, the compound of the present invention exhibited a remarkably excellent effect in promoting angiogenesis. Accordingly, the compound of Formula 1 of the present invention may have effects on hair loss treatment, prevention, and hair growth by promoting angiogenesis.

The composition according to the present invention can be used as a combination preparation by further including other hair loss prevention, treatment, or hair growth drugs or adjuvants. Other drugs or adjuvants include retinoic acid, minoxidil, finasteride, zinc peptide, zinc oxide, biotin, genistein, onion extract, pumpkin seed oil, Emu oil, Green tea extract, willow bark extract, and the like, but is not limited thereto.

The composition of the present invention may be formulated and administered in any dosage form including, but not limited to, oral administration preparations, injections, suppositories, transdermal administration preparations, and nasal administration preparations, preferably the skin covered with the scalp or hair It may be formulated in a form suitable for topical application to the site. Examples of such preparations for topical administration include, but are not limited to, liposomes, nanoemulsions, shampoos, hair conditioners, or hair lotions. Preferably, the effect is promoted by an increase in absorption through the skin, especially the scalp, and for convenience of use, it is preferably formulated as a liposome, nanoemulsion or shampoo.

The composition of the present invention may include about 0.5 parts by weight to 3 parts by weight of the ceramide based on the entire composition, which may be increased or decreased depending on the type of the compound of Formula 1 above.

Upon topical administration, the compound of Formula 1 may be administered by applying the compound of Formula 1 to the site for hair loss prevention, treatment, or hair growth once or twice a day. When the ceramide component is 1 part by weight, the daily application amount is about 0.5-3 mg, and may be increased or decreased depending on the area of the application site. Such dosage and frequency may be appropriately increased or decreased according to the patient's age, sex, and the degree of hair loss. In particular, in the case of extensive hair loss under the age of 40 (severe hair loss progresses in more than 10% of the total area), it is preferable to prioritize improvement of hair loss by increasing the weight ratio of the ceramide component, but there is no side effect on hair loss or local hair loss in women over 70 years old In view of the above, it is preferable to apply a product in which the weight part of the ceramide is reduced.

The compound of Formula 1 or a pharmaceutically acceptable salt thereof according to the present invention is not only excellent in the effect on the treatment, prevention, or hair growth of hair loss, but also has a simple chemical structure and can be easily prepared by synthesis, so it is economical and , liposomes, can be easily delivered to hair follicles when formulated as lipid microsphere preparations such as nanoemulsions. In addition, there is no skin irritation and no side effects compared to minoxidil and finasteride, which are other previously used hair loss treatment agents, which is very preferable.

The spicule is called a hydrolyzed sponge and is a component prepared by separating and purifying only the incus of the sponge. These spicules not only have a needle-like structure, but also have many pores on the surface, so they can be used as carriers for active ingredients by using these pores.

In addition, the spicule is divided into two types, Megascleres and Microscleres, depending on the size, and Megascleres is visually distinguishable with a size of 60-2,000 μm. The microscleres have a size of 10 to 60 μm and can be observed using a microscope. In the present invention, it is preferable to use a micro-class spicule having a size of 50 to 60 μm. At this time, if the size of the spicule is less than 50㎛, the porosity may decrease, the delivery ability of the active ingredient may be reduced, and if it exceeds 60㎛, it may cause irritation to the skin.

In particular, as the spicule of the present invention has a needle-like structure, it can stimulate not only the stratum corneum layer but also the epidermis layer by the pressure applied to the scalp when applied to the scalp. can be improved In the case of improvement of blood circulation by such stimulation, it has the same effect as that of minoxidil, and the same effect of improving blood circulation can be expected without side effects such as prevention of collagen synthesis.

In addition, the existing spicule uses strong acids and strong bases such as hydrochloric acid to separate organic parts except for the incus, but in this case, it has high productivity, but has the disadvantage that it can irritate the skin due to the strong acids and strong bases remaining in the pores. have. Therefore, in the present invention, it is preferable to separate the spicules using acids and bases obtained from natural substances instead of the strong acids and bases.

To this end, the spicule, (i) washing the collected sponge, and then drying the moisture content to less than 10% by weight; (ii) heating the dried sponge by immersing it in water at a temperature of 90 to 100° C. for 10 to 40 minutes; (iii) immersing the heated sponge in an acidic solution of pH 2 to 4 for 10 to 20 days; (iv) separating the acidic solution and the solid content of the sponge, then washing the solid content with water repeatedly 2 to 5 times; (v) immersing the washed solids in water and then washing them using ultrasonic waves; (vi) immersing the sponge in a basic solution of pH 8 to 10 for 1 to 5 days after the ultrasonic cleaning is completed; (vii) separating the basic solution and the solid content, then washing the solid content with water repeatedly 2 to 5 times; and (viii) immersing the washed solids in water and then washing them using ultrasonic waves.

The step (i) is a step of washing the collected sponge and then drying it so that the moisture content is less than 10% by weight, washing foreign substances present on the surface of the clarification, and then drying it. In this case, in the case of the sponge, it may be dried so that the moisture content is less than 10% by weight, preferably less than 7% by weight. Through such drying, the mucus component that is always present on the surface of the sponge can be more easily removed, and in the drying process as described above, decomposition and tissue destruction of the organic components contained in the sponge occur, so that the subsequent process will be more easily performed. can

The step (ii) is a step of heating the dried sponge by immersing it in water at a temperature of 90 to 100° C. for 10 to 40 minutes to promote the denaturation of the protein component by heating the dried sponge. This is a step that facilitates In general, except for the skeleton of minerals, most of the rest of the animal is composed of protein. In the case of this protein, since it plays a role of connecting the skeleton, it is composed of a very hard tissue, but when it is heated, the protein is denatured and can be easily separated from the skeleton. Using this, in the case of the present invention, protein denaturation can be induced by immersing the dried sponge in water at a temperature of 90 to 100° C., that is, boiling water, so that protein separation can be facilitated. In this case, when the immersion time is less than 10 minutes, it may be difficult to separate the protein, and when the immersion time exceeds 40 minutes, the decomposed protein may be adsorbed to the supply part of the incus.

The step (iii) is a step of immersing the heated sponge in an acidic solution of pH 2 to 4 for 10 to 20 days, and is a step of removing organic matter present in the heated sponge using an acid. In general, when an organic material comes into contact with an acid, its decomposition rate is accelerated and can be removed. However, in the existing spicule manufacturing method, hydrochloric acid is mainly used to remove it, but this may have a problem that hydrochloric acid remains in the pores of the spicule and may cause skin irritation. Therefore, in the present invention, it is preferable to prepare the spicules using natural acidic substances such as lemon juice, citron juice, sugar citron juice, orange juice and vinegar. That is, the sponge after the heating has been completed may be immersed in the lemon juice, citron juice, sugar citron juice, orange juice and vinegar. In this case, if the immersion period is less than 10 days, it may be difficult to remove the organic matter, and if it exceeds 20 days, the incus may be decomposed by acid. Also, when organic matter is removed using an acid as described above, a portion of the incus may be dissolved to further increase the porosity of the incus. In addition, when the acidic solution is less than pH2, the incus may be decomposed due to its strong affinity or may irritate the skin due to the remaining acidic solution.

After the step (iii) is completed, (iv) the acid solution and the solid content of the sponge are separated, and then the solid content may be repeatedly washed with water 2 to 5 times. The incus and the organic component may be separated by the acidic solution, and most of the organic component may be changed to a dissolved state in the saline solution. Therefore, when separating the solids as described above, the solids may be mostly composed of the incus, and the next step may be performed by washing them several times.

The step (v) is a step (v) of immersing the washed solids in water and then washing them using ultrasonic waves. It is a step of removing foreign substances including organic matter adhering to the incuses using ultrasonic waves.

At this time, since the ultrasonic waves are better transmitted in water, the solid content may be immersed in water for smooth delivery of the ultrasonic waves. In addition, the ultrasonic wave may have a frequency of 20 to 130 kHz, and it is possible to perform the cleaning as described above only in the frequency range.

The step (vi) is a step of immersing the sponge in a basic solution of pH 8 to 10 for 1 to 5 days after the ultrasonic cleaning is completed. Although most organic matter can be removed through the acidic solution immersion process, it is preferable to use a basic solution to finally remove the organic matter. In particular, in the case of a basic solution, it not only has the property of easily decomposing the protein of the sponge, but also can neutralize the acidic solution present in the pores of the spicule.

In this case, in the case of the conventionally used basic solution, a strong base, that is, sodium hydroxide or potassium hydroxide was used for convenience of use, but in this case, the residual basic solution may irritate the skin. Therefore, in the present invention, it is preferable to prepare a basic solution using calcium carbonate and use it. In particular, in the case of the spicule of the present invention, since it can be used in contact with the skin, the calcium carbonate can also be used that is manufactured using shellfish rather than an industrially synthesized product.

Looking at this in detail, the basic solution includes the steps of separating the shells and then washing; calcining the washed clam shells at a temperature of 800 to 1200 °C; pulverizing the calcined shellfish; mixing the pulverized clam shells with 1000 to 5000 parts by weight of water based on 100 parts by weight of the clam shells, and then leaving them to stand for 2 to 10 days; And it may be a solution prepared by a method comprising the step of separating the solid content of the shellfish.

The shell of the clam is composed of a large amount of calcium carbonate as a main component, and most of it is treated as waste. Therefore, when calcium carbonate is extracted from these shells and used, desired effects can be achieved while contributing to resource recycling and environmental protection. The clam shells may be washed and organic matter removed, and then calcined at a temperature of 800 to 1200 °C. Through this, organic matter present in the shell may be oxidized and removed, and only calcium carbonate may remain. At this time, if the firing temperature is less than 800 ℃, smooth firing may not be performed, and if it exceeds 1200° C., energy consumption may increase, and calcium carbonate may be decomposed by firing, thereby reducing the yield.

After the calcination is completed as described above, it can be pulverized, mixed with 1000 to 5000 parts by weight of water based on 100 parts by weight, and then left to stand for 2 to 10 days to prepare an aqueous calcium carbonate solution. At this time, when water is used in less than 1000 parts by weight, the amount of the aqueous solution to be prepared is reduced and the efficiency may be reduced. .

The ultrasonic cleaning-completed solids may be added to the basic solution prepared as described above and immersed for 1 to 5 days. At this time, when immersed for less than 1 day, it is difficult to expect an effect due to the basic solution, and when added for more than 5 days, there is no further effect and the manufacturing efficiency is reduced.

When the washing with the basic solution is completed as described above, the spicule can be manufactured through the ultrasonic washing and water washing steps in the same way as the steps after washing with the acidic acid solution.

The spicule prepared as described above may be mixed with the ceramide, particularly phytosphingosine having the structure of Formula 1, before being mixed with other raw materials. Through this, the ceramide component can be adsorbed to the porous part of the spicule, and this can mean that the ceramide component can be preferentially delivered to the lower stratum corneum of the scalp than other components.

The spicule may contain 0.2 to 1.5 parts by weight relative to 100 parts by weight of the composition for preventing, treating, or restoring total hair loss. When the content of the spicule is less than 0.2 parts by weight, it is difficult to expect the effect of the speculum, and when it exceeds 1.5 parts by weight, the scalp stimulation by the spicule is strong, and troubles such as inflammation or itching may occur on the scalp.

The aroma oil (aroma herb extract) is selected from the group of lavender, rosemary, eucalyptus, cypress, bergamot, sandalwood, rose and lemon to relieve tension and cramps of the scalp and to calm and relax the skin and nerves due to the fragrance. One or more extracts may be used.

For example, lavender oil has the function of improving skin and relieving muscle tension and stress, and also serves as a solubilizer.

In addition, eucalyptus oil enhances skin absorption, promotes blood circulation, and has moisturizing properties. This eucalyptus oil also has a function of adjusting the viscosity when dissolving fat-soluble as a non-ionic thickener.

Cypress oil is effective for muscle relaxation, and bergamot oil has the ability to improve and soothe the skin. Sandalwood oil replenishes moisture to the skin and soothes the skin, while rose oil gives elasticity to the skin, provides moisture and nutrition, and relaxes and calms muscle tension. The sandalwood and rose oil also serves to adjust the pH when dissolving fat-soluble.

As described above, a composition containing one selected from the above aromatic oils or a mixture thereof as a main component may be prepared according to the purpose or use required by the user. 1 to 3 parts by weight of the aromatic oil may be used based on 100 parts by weight of the composition for prevention, treatment or hair growth of total hair loss. When the aromatic oil is mixed in less than 1 part by weight, it is difficult to expect the effect of the aroma oil. can happen

The glycerin is added to improve the viscosity of the pharmaceutical composition for the prevention or treatment of hair loss and to moisturize the scalp, and may contain 1 to 3 parts by weight. When the glycerin is included in less than 1 part by weight, it is difficult to maintain the viscosity of the composition for prevention, treatment or hair growth of hair loss. difficult.

Purified water, ethanol, or a mixture thereof may be used as the solvent for the composition for preventing, treating, or restoring hair loss, or a mixture thereof may be used. In particular, such a solvent is a factor determining the formulation of the composition for preventing, treating, or restoring hair loss, and when the content of the solvent is lowered, the viscosity of the composition for prevention, treatment or hair growth of the hair loss increases, so that a cream or ointment type formulation is used. On the contrary, when the content of the solvent is increased, the viscosity of the composition for preventing, treating or restoring hair loss is lowered to have a liquid formulation or can be easily mixed with a base such as shampoo.

The menthol is intended to loosen the stiff scalp and give a refreshing feeling to the scalp. However, when used excessively, there is a risk of irritation to the skin, so 0.1 to 2 parts by weight of the composition for prevention, treatment or hair growth of hair loss parts by weight are used. When the menthol is included in less than 0.1 parts by weight, it is difficult to expect the effect of menthol, and when it is included in more than 20 parts by weight, it gives a strong stimulation to the scalp, and side effects such as erythema on the scalp may occur.

The pharmaceutical composition for preventing or treating hair loss may further include an emulsifier, a sunscreen, a moisturizer, a preservative, a pH adjuster, a thickener or other additives.

The emulsifier is included in the pharmaceutical composition for preventing or treating hair loss so that a water-soluble component for supplying moisture and a fat-soluble component for maintaining it are mixed well without separation, and polysorbate 80, cetyl PG/P It is selectively used among sebum-10/dimethicone. The polysorbate 80 (Polysorbate 80; product name Tween 80) and cetyl PEG / PG-10 / dimethicone (Cetyl PEG / PPG-10/1 Dimethicone) are water-soluble nonionic surfactants that easily dissolve poorly soluble components and It helps to stabilize the emulsion of other ingredients. When the emulsifier is used excessively, the viscosity of the pharmaceutical composition for preventing or treating hair loss obtained according to the present invention is increased, and the contents do not flow out well when used in a container, so that the applicability to the skin is reduced and the water-soluble part (water-soluble component) Since it becomes difficult to deliver the cooling feeling expressed from the scalp to the scalp, 0.01 to 1.0 parts by weight may be used with respect to 100 parts by weight of the pharmaceutical composition for the prevention or treatment of hair loss.

The sunscreen is added to reflect or absorb ultraviolet rays generated from the sun, and may include a component that reflects ultraviolet rays and a component that absorbs ultraviolet rays. In particular, since damage to the scalp due to ultraviolet rays is known to be a major cause of hair loss, it is preferable to prevent damage to the scalp by ultraviolet rays by adding the sunscreen.

The component for reflecting ultraviolet rays serves to reduce ultraviolet rays reaching the skin by reflecting incident ultraviolet rays to the outside, and a metal oxide, particularly titanium oxide or zinc oxide, may be used. Although the metal oxide has excellent efficiency in reflecting ultraviolet rays, it has a white color by itself, which may cause whitening when applied to the skin.

It is a substance that reacts to incident ultraviolet rays used to absorb ultraviolet rays and causes a chemical reaction. It is a substance that absorbs ultraviolet rays and converts them into energy (light or heat) that does not harm the body. Materials used to absorb these ultraviolet rays are ethylhexylmethoxycinnamate, butylmethoxydibenzoylmethane (avobenzone), benzophenone-3 (oxybenzone), terephthalylidene dicamphorsulfonic acid, homosalate, and ethylhexyl. Silsalicylate, diethylaminohydroxybenzoylhexylbenzoate, bis-ethylhexyloxyphenolmethoxyphenyltriazine, cetylethylhexanoate, polyhydroxystearic acid, isostearic acid or a combination thereof may be used. have. Components that absorb these UV rays do not cause cloudiness, but they are made of organic components, which can cause skin troubles on sensitive scalps.

The UV blocker may be used by selecting one of a component that reflects UV rays or a component that absorbs UV rays, but a component that reflects UV rays and a component that absorbs UV rays to increase UV protection and reduce cloudiness caused by metal oxides It is preferable to use it by mixing. In particular, the component that reflects the ultraviolet rays has a high sunscreen effect, but when it is included in a pharmaceutical composition for the prevention or treatment of hair loss, it is easy to appear white turbidity due to its characteristic white color, and the component that absorbs ultraviolet rays does not show turbidity. Since organic ingredients can cause skin trouble, it is important to combine them to achieve the optimal UV protection effect. To this end, the weight ratio of the component that reflects the ultraviolet rays and the component that absorbs the ultraviolet rays may be 1:1 to 1:10. When the ratio is 1:1, that is, when the UV-reflecting component is included more than the UV-absorbing component, the UV blocking effect may be increased, but white turbidity occurs, and the UV-reflecting component and the UV-absorbing component When the weight ratio of the components exceeds 1:10, the UV blocking effect is lowered, and skin troubles may occur due to many organic components.

The humectant is included to supply moisture to the scalp when using the pharmaceutical composition for the prevention or treatment of hair loss and at the same time prevent evaporation of moisture present in the scalp. have.

The sealant is a component that prevents evaporation of moisture by forming a moisture-impermeable film on the scalp. Mineral oil, petrolatum jelly, jojoba oil, lanolin, cocoa butter) , olive oil, paraffin, silicone oil, triglycerides, palmitates, and myristates may be used.

The humectant contains moisture by itself, and serves to absorb moisture and supply it to the scalp. In general, the humectant absorbs moisture in the atmosphere and supplies moisture to the scalp, but when the moisture in the atmosphere is less than 60%, it cannot absorb moisture in the atmosphere, so it can absorb moisture below the dermis and supply it to the scalp surface. . Such humectants include glycerin, hyaluronic acid, chitosan, chondroitin sulfate, heparin sulfate, propylene glycol, butylene glycol, sorbitol, polyethylene glycol, methylpropanediol, lactate, urea, amino acid, sodium 2-pyrrolidone-5-carboxylic acid (PCA) acid) and the like may be used.

The barrier replacement agent supplements the lipid component between the keratinocytes connecting the stratum corneum and the stratum corneum to prevent evaporation of moisture inside the scalp, and may include ceramide, cholesterol, various fatty acids, and the like.

The emollient fills the gaps between the falling off keratinocytes and at the same time softens the keratinocytes, and forms a permeable membrane on the scalp surface to make the scalp soft and smooth. As the softening agent, glycol stearate, glyceryl stearate, soy sterol, and the like may be used. The moisturizing agent may be used in an appropriate combination of the components listed above, but preferably 1 to 10 parts by weight of methylpropanediol. When the methylpropanediol is included in an amount of less than 1 part by weight, the moisturizing effect is low, and even after using the pharmaceutical composition for the prevention or treatment of hair loss, a rough feeling may remain on the scalp, and when it exceeds 10 parts by weight, the prevention or treatment of hair loss After using the pharmaceutical composition for use, it may be difficult to use because there is a lot of stickiness.

The preservative is added to extend the storage period of the pharmaceutical composition for the prevention or treatment of hair loss, and it is also possible to use a preservative of an existing paraben component. It is preferable to use Preservatives usable in the present invention include ethanol, nucleic acid diol, benzoic acid, paraoxybenzoic acid, imidazolini urea, triclosan, sulfur, chlorphenesin, and the like. In the case of the preservative, since the activity of each species and microorganism is different depending on each component, it is preferable to use a mixture of 2 to 5 types rather than using them alone, and most preferably 0.5 to 3 parts by weight of nucleic acid diol and chlorpe. It can be used by mixing 0.1 to 1 part by weight of Nesin. In the above weight range, the preservative may exert the maximum effect, and when it is out of the above weight range, the preservative effect may be lowered or the sensitivity to a specific microorganism may be reduced.

The pH adjusting agent adjusts the acidity of the pharmaceutical composition for preventing or treating hair loss, and is used to maintain the acidity during storage, and a buffer solution in which an acid, a base, or a salt thereof is mixed may be used. In general, the pH adjusting agent is an organic acid such as citric acid, succinic acid, tartaric acid, lactic acid, malic acid, fumaric acid, maleic acid, glycolic acid, and citric acid, an inorganic acid such as hydrochloric acid, sulfuric acid, phosphoric acid, nitric acid, sodium salt of these acids, potassium salt, or It can be used alone or in mixture of two or more of ammonium salts and arginine. In particular, in the case of general acids or bases such as hydrochloric acid and sulfuric acid, the ionization degree is high, so the pH maintenance effect is low, and it may irritate the skin. In addition, the pH adjusting agent may further include triethanolamine, sodium chloride, sodium hydroxide, potassium hydroxide, and the like.

The thickener is added to form a formulation by increasing the viscosity of the composition for preventing, treating, or restoring hair loss, and xanthan gum, konjac gum, gellan gum, locust locust bean gum, fenugreek gum, karaya gum, gum tragacanth, gum arabic, acacia gum, guar gum ), cellulose derivatives, pectin, starch, chitins, agar, carrageenan, etc. may be used, and may preferably contain 0.01 to 3 parts by weight of xanthan gum. When the xanthan gum is included in less than 0.01 parts by weight, the formulation is not smoothly formed and flows like water, so it is difficult to use it on the scalp as a composition for preventing, treating or restoring hair loss, and when it contains more than 3 parts by weight, the formulation is hard It is difficult to apply on the scalp by taking an appropriate amount, and it may also be difficult to apply it evenly on the scalp surface.

In addition, the present invention may include other additives in addition to the above components. The other additives may include metal ion sequestrants, functional ingredients, ester oil, fragrances, pigments, etc., which enhance the characteristic effect of the composition for preventing, treating or hair growth of the present invention, or preventing or treating hair loss. Alternatively, it may serve to increase the commercial value of the composition for hair growth.

The metal ion sequestrant is added to prevent the elution of metal ions that occur during long-term storage. may play a role in increasing Disodium EDI or nitrilotriacetic acid may be used as the sequestering agent for metal ions, and preferably, 0.01 to 0.1 parts by weight of disodium EDITEA may be included. When the disodium EDIT is included in less than 0.01 parts by weight, the metal ion sequestration effect may not appear. The cost competitiveness of the pharmaceutical composition for prevention or treatment may be reduced.

The functional ingredient is used to enhance the specific effect of the hair loss prevention, treatment or hair growth composition, and may be added for additional effects such as dandruff improvement, oil control, and nutritional supplementation in addition to hair loss prevention. The functional ingredient can be added without limitation as long as it is a component exhibiting the above effect, but preferably niacinamide, trinexamic acid, licoric acid, arbutin, adenosine, retinol, retinyl palminate, polyethoxyleritiretin It may include amide, various peptides, various vitamins, and the like, and preferably contains 0.1 to 0.8 parts by weight of niacinamide and 0.01 to 0.1 parts by weight of adenosine. Within the above range, the pharmaceutical composition for preventing or treating hair loss can maximize the effect of improving hair loss.

The pigment is used for preventing, treating, or controlling the color of the hair growth composition for hair loss, and may include a dye or a pigment, preferably a pigment. The pigment may include at least one of an organic pigment and an inorganic pigment. The inorganic pigment is silicic acid-based, silicic anhydride-based, magnesium silicate-based, talc-based, sericite-based, mica-based, kaolin-based, bengala-based, clay-based, bentonite-based, titanium coated mica-based, bismuth oxychloride-based, zirconium oxide-based , magnesium oxide, zinc oxide, titanium oxide, aluminum oxide, calcium sulfate, barium sulfate, magnesium sulfate, calcium carbonate, magnesium carbonate, iron oxide, ultramarine, chromium oxide and chromium hydroxide One or more of the pigments may be included. The organic pigment is polyamide-based, polyester-based, polypropylene-based, polystyrene-based, polyurethane-based, vinyl resin-based, urea resin-based, phenolic resin-based, fluororesin-based, silicon resin-based, acrylic resin-based, melamine resin-based, epoxy resin-based, polycarbonate resin-based, It may include at least one of divinylbenzene/styrene copolymer type, silk powder type, cellulose type, CI pigment yellow type, and CI pigment orange type organic pigment.

The perfume is used to increase the marketability of the pharmaceutical composition for the prevention or treatment of hair loss while hiding the chemical scent due to the above ingredients and at the same time to have a specific fragrance, and is usually used for the prevention or treatment of hair loss. The ingredients used in the composition may be used.

Hereinafter, preferred embodiments of the present invention will be described so that those of ordinary skill in the art can easily implement them with reference to the accompanying drawings. In addition, in the description of the present invention, if it is determined that a detailed description of a related known function or a known configuration may unnecessarily obscure the gist of the present invention, the detailed description thereof will be omitted. In addition, certain features presented in the drawings are enlarged, reduced, or simplified for ease of description, and the drawings and components thereof are not necessarily drawn to scale. However, those skilled in the art will readily appreciate these details.

Example 1

Liposomes containing N-acetylphytosphingosine-1-phosphate (NAPS-1-P) were prepared. NAPS-1-P is S. Li, W.K. Wilson, G. J. Schroepfer, Chemical synthesis of D-ribo-phytosphingosine-1-phosphate, a potential modulator of cellular processes. J. Lipid Res. 40: 117-125, prepared from N-acetylphytosphingosine according to the method described in 1999 and used.

After heating the sponge with boiling water for 20 minutes, the sponge was separated, and the separated sponge was immersed in lemon juice for 15 days. After the immersion was completed, the solid was separated, and water was supplied to the solid and washed using an ultrasonic wave of 70 kHz. After ultrasonic washing was completed, it was washed three times with water, and the washed solid was immersed in an aqueous calcium carbonate solution prepared from shellfish for 3 days. After 3 days had elapsed, the solid was separated and washed 3 times with water to prepare spicules.

The NAPS-1-P, spicule and other ingredients were combined in the ratio of Table 1 below to prepare an external preparation for the scalp.

ingredient Example 1 Example 2 Example 3 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Cypress Oil One bergamot oil One sandwood oil One rose oil One One lavender oil One One eucalyptus oil One One One menthol One One One One One One One ethanol 5 5 Iropropanol 5 mineral oil 15 spicule One 1.5 1.5 - - - - NAPS-1-P 0.5 0.5 One One glycerin 5 5 5 5 5 5 5 Carbomer 0.1 0.1 0.1 0.1 0.5 0.5 0.2 polyacrylate 0.3 0.3 0.3 0.3 0.5 triethanolamine 0.1 0.1 0.1 0.1 0.5 0.5 0.2 Disodium EDIT 0.05 0.05 0.05 0.05 0.05 0.05 0.05 methylparaben 0.1 0.1 0.1 0.1 0.1 0.1 0.1 Propylparaben 0.1 0.1 0.1 0.1 0.1 0.1 0.1 Purified water 100 100 100 100 100 100 100

test example

After purchasing a 5-6 week old mouse, some hair on the back was removed, and then hair removal cream was applied to completely remove the existing hair. Mice that were not completely depilated were excluded from the experiment, and after hair removal, 3 mice were randomly bred per cage, and a total of 16 cages were used.

After hair removal, the composition containing NAPS-1-P prepared in Examples 1 to 3 and Comparative Examples 1 to 4 and commercially available minoxidil (Comparative Example 5) were applied to the hair-removed area once a day after hair removal was left for about a day. . After 10, 15, and 25 coats were applied, the hairs of mice were collected, and the length was measured and compared to determine the degree of hair growth promotion.

10 episodes Episode 15 Episode 25 Example 1 0.4mm 1.6mm 3.5mm Example 2 0.6mm 1.9mm 3.9mm Example 3 0.6mm 2.1mm 4.7mm Comparative Example 1 0.4mm 1.1mm 2.2mm Comparative Example 2 0.2mm 0.8mm 1.1mm Comparative Example 3 0.3mm 0.9mm 1.3mm Comparative Example 4 0.2mm 0.9mm 1.2mm Comparative Example 5 0.4mm 1.8mm 3.6mm

As shown in Table 2, in the case of the example of the present invention, it was found that the same or superior mimic growth promotion as minoxidil of Comparative Example 5 was performed. Comparative Example 1 not using the spicule was found to have a superior effect than Comparative Examples 2 to 4 not using the spicule and NAPS-1-P, but it was found to have a inferior effect compared to the Example of the present invention. It was shown that the combined effect of NAPS-1-P and Spicule was the best.

In the above, preferred embodiments of the present invention have been illustrated and described, but the present invention is not limited to the specific embodiments described above, and it is common in the technical field to which the present invention pertains without departing from the gist of the present invention as claimed in the claims. Various modifications are possible by those having the knowledge of, of course, these modifications should not be individually understood from the technical spirit or prospect of the present invention.

Claims (2)

In the pharmaceutical composition for preventing or treating hair loss comprising ceramide,
The pharmaceutical composition for preventing or treating hair loss,
Compared to 100 parts by weight of purified water,
0.5 to 1 part by weight of N-acetylphytosphingosine-1-phosphate (NAPS-1-P) as a ceramide;
1 to 1.5 parts by weight of spicule;
5 parts by weight of glycerin;
1 part by weight of rose oil;
1 part by weight of lavender oil;
1 part by weight of eucalyptus oil; and
1 part by weight of menthol;
includes,
The N-acetylphytosphingosine-1-phosphate (NAPS-1-P) has the structure of Formula 1 below,
[Formula 1]

(In Formula 1, R is hydrogen or COR1, R1 is C1-C6 alkyl)
The spicule is
(i) washing the collected sponge and then drying the water content to less than 10% by weight;
(ii) heating the dried sponge by immersing it in water at a temperature of 90 to 100° C. for 10 to 40 minutes;
(iii) immersing the heated sponge in an acidic solution of pH 2 to 4 for 10 to 20 days;
(iv) separating the solid content of the acid solution and the sponge, and then washing the solid content with water repeatedly 2 to 5 times;
(v) immersing the washed solids in water and then washing them using ultrasonic waves;
(vi) immersing the sponge in a basic solution of pH 8 to 10 for 1 to 5 days after the ultrasonic cleaning is completed;
(vi i) separating the basic solution and the solid content, then washing the solid content with water repeatedly 2 to 5 times; and
(viii) immersing the washed solids in water and then washing them using ultrasonic waves;
It is manufactured by a manufacturing method comprising
The acidic solution is a mixture of at least one selected from the group consisting of lemon juice, citron juice, sugar citron juice, orange juice and vinegar,
The basic solution is
separating the shells and then washing them;
calcining the washed clam shells at a temperature of 800 to 1200 °C;
pulverizing the calcined shellfish;
mixing the pulverized clam shells with 1000 to 5000 parts by weight of water based on 100 parts by weight of the clams, and then leaving them to stand for 2 to 10 days; and
separating the solid content of the clam shell;
It is a solution prepared by a method comprising
The ultrasonic wave has a frequency of 20 to 130 kHz,
The pharmaceutical composition for preventing or treating hair loss is a pharmaceutical composition for preventing or treating hair loss, characterized in that it further comprises an emulsifier, a sunscreen, a moisturizer, a preservative, a pH adjuster and a thickener. delete

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