KR102235754B1 - Cosmetics for the prevention and improvement of skin inflammation using anthelmintic - Google Patents

Abstract

Provided is a cosmetic composition comprising a mixture of praziquantel, mebendazole, albendazole, pyrantel, niclosamide and ivermectin, a catalyst, a cosolvent, and an antioxidant.

Description

Cosmetics for the prevention and improvement of skin inflammation using anthelmintic}

The present invention relates to a cosmetic for preventing and improving skin inflammation using an anthelmintic.

The skin is the primary barrier of the human body and protects the internal organs from temperature and humidity changes, ultraviolet rays, pollutants, and other stimuli of the external environment, and plays an important role in maintaining the body's homeostasis such as body temperature control.

Demodex mites are ectoparasites that are often observed under a microscope that infect the fur branch units of the skin. Among the various species reported, at least Demodex folliculorum and Demodex brevis are found on the outer surface of the human body.

The two Demodex species often coexist and preferentially gather in the same skin area of the face, cheeks, forehead, nose and ear canal, where active sebum secretion is beneficial to the environment and reproduction. Adult Demodex ticks have a life cycle of 14 to 18 days and eventually die afterwards, and their proliferation depends on successful mating by the adult tick.

Mating occurs in the opening of the hair follicle near the outer surface of the skin. After that, the pregnant female moves to the sebaceous gland, lays eggs, and becomes a larva and a first nymph. The first nymph goes to the opening of the hair follicle and becomes the second nymph, crawls out of the skin and reenters the hair follicle to become an adult.

Thus, during the life cycle, adult Demodex can successfully mate to produce the next generation, and the degree of infection in the host increases.

Demodex infection does not appear in healthy children, but increases in an age-dependent manner and is found in almost 100% of the skin of middle-aged adults unless eradication is taken. The incidence of demodex infection is higher in unhealthy skin than in normal skin. Excessive growth of these ticks is associated with skin diseases and hair loss.

Demodex is prevalent in limb mammals, particularly domestic animals, particularly dogs, and can cause follicular tick infections. Demodex mites enter the hair follicles and the sebaceous glands of animals, often causing severe dermatitis, infection and discomfort.

On the other hand, Demodex is a mite that is parasitic in the hair follicles and sebaceous glands of the skin, and a few to as many as dozens of them inhabit each pore, and they reproduce with fat in the sebaceous gland as food.

The fat component of soap and face wash used for cleansing remains on the skin after cleansing, and the fat component left on the skin causes the growth of Demodex. Hair loss can be initiated by the infestation of Demodex, and dry skin can turn into oily skin. Therefore, in the development of soaps, detergents, shampoos, and cosmetics, there is a need to develop a composition that has no side effects, is harmless to the human body, and is effective in removing demodex.

In order to reduce skin irritation caused by such various chemical substances, Korean Patent Publication No. 10-20120054149 has developed a number of products using natural substances. Natural ingredients have little side effects on the skin, but cosmetic products containing natural extracts do not sufficiently implement functionality and have problems in that the skin improvement activity is not maintained continuously.

Therefore, the need for development of cosmetic products having excellent functionality, bio-stability and skin improvement effect, has been steadily emerging.

Accordingly, the present invention is intended to solve various drawbacks and problems caused by the prior art in consideration of the above circumstances, and a cosmetic composition for the purpose of preventing, improving and treating Demodex acne, seborrheic dermatitis and transient spiny cell inflammation Is to provide.

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

According to an embodiment of the present invention in order to achieve the above object, comprising an anthelmintic mixture of praziquantel, mebendazole, albendazole, pyrantel and niclosamide, a catalyst, a co-solvent, and an antioxidant. A cosmetic composition is provided.

According to another embodiment of the present invention, the repellent mixture may further include ivermectin.

In addition, according to an embodiment of the present invention, with respect to 100 parts by weight of the anthelmintic mixture, praziquantel is 1 to 90 parts by weight, mebendazole is 1 to 90 parts by weight, albendazole is 1 to 90 parts by weight, The pyrantel may be 1 to 90 parts by weight, and the niclosamide may be 1 to 90 parts by weight.

According to another embodiment of the present invention, based on 100 parts by weight of the repellent mixture, ivermectin may be 1 to 90 parts by weight of a cosmetic composition.

In addition, according to an embodiment of the present invention, based on 100 parts by weight of the anthelmintic mixture, the catalyst may be 0.1 to 20 parts by weight, the co-solvent may be 1 to 50 parts by weight, and the antioxidant may be 0.1 to 20 parts by weight.

In this case, according to an embodiment of the present invention, the catalyst may be at least one of vitamin A, vitamin B, vitamin D, and vitamin E.

In addition, according to an embodiment of the present invention, the co-solvent may be at least one of glycol, glyceride, and ethyl oleate.

Meanwhile, according to an embodiment of the present invention, the antioxidant may be at least one of phenoxyethanol, methylparaben, and propylglycone.

The cosmetic composition of the present invention is effective in preventing, improving, and treating not only Demodex acne, but also seborrheic dermatitis and transient prickly cell inflammation.

In addition, compared to the conventional cosmetic composition, there is an effect of providing a cosmetic composition having excellent skin improvement and effective ingredient delivery effect, as well as excellent stability to the human body.

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

Hereinafter, the present invention will be described in detail. Prior to this, terms or words used in the present specification and claims are not limited to their usual or dictionary meanings and should not be construed, and the inventors appropriate the concept of terms to describe their own invention in the best way. It should be interpreted as a meaning and concept consistent with the technical idea of the present invention on the basis of the principle that it can be defined as such. Therefore, the configuration described in the embodiments described in the present specification is only the most preferred embodiment of the present invention, and does not represent all the technical spirit of the present invention, and various equivalents and equivalents that can replace them at the time of the present application It should be understood that there may be variations.

According to one embodiment of the present invention, a wide range of repellents, praziquantel, mebendazole, albendazole, pyrantel, and niclosamide anthelmintic mixture, catalyst , A co-solvent, a cosmetic composition comprising a sulfate agent is provided.

On the other hand, the present inventors through countless experiments, the cosmetic composition according to an embodiment of the present invention, based on 100 parts by weight of the repellent mixture, 1 to 90 parts by weight of praziquantel, 1 to 90 parts by weight of mebendazole, When containing 1 to 90 parts by weight of bendazole, 1 to 90 parts by weight of pyrantel, and 1 to 90 parts by weight of niclosamide, it prevents not only Demodex acne, but also seborrheic dermatitis and transient spiny cell inflammation without any side effects to the human body. , Improvement, and treatment effect.

Specifically, praziquantel, which can be applied to the present invention, is an anthelmintic substance that treats infections caused by parasites, and when applied to the skin, it is possible to prevent inflammation caused by demodex acne and transient spiny cells with almost no side effects. It can be improved and cured. Formula 1 below is the structural formula of praziquantel applicable to the present invention.

Formula 1

In addition, the praziquantel may contain 1 to 90 parts by weight based on 100 parts by weight of the repellent mixture, preferably 10 to 25 parts by weight, more preferably 10 parts by weight. In this case, when praziquantel is contained in an amount of less than 1 part by weight, the effect of delivering the active ingredient is insufficient, so that there is little effect such as improvement of skin inflammation, and when it is included in more than 90 parts by weight, there is a problem that may cause side effects.

On the other hand, mebendazole, which can be applied to the present invention, is an anthelmintic substance that treats parasite infectious insects by inhibiting the formation of microtubules in parasite cells and killing parasites. There is also an advantage in that it can prevent, improve, and treat demodex acne, inflammation caused by transient spiny cells, and the like. Formula 2 below is a structural formula of mebendazole applicable to the present invention.

Formula 2

In addition, the mebendazole may contain 1 to 90 parts by weight based on 100 parts by weight of the anthelmintic mixture, preferably 10 to 25 parts by weight, more preferably 20 parts by weight. At this time, when mebendazole is contained in an amount of less than 1 part by weight, the effective ingredient delivery effect is insufficient, and thus there is no effect such as improvement of skin inflammation, and when it is included in an amount exceeding 90 parts by weight, there is a problem that may cause side effects.

In addition, albendazole, which can be applied to the present invention, is an anthelmintic that kills parasites and treats infections caused by parasites. When used on the skin, there are few side effects, but effectively, Demodex acne, inflammation caused by transient prickly cells. It has the advantage of preventing, improving, and treating the back. Formula 3 below is the structural formula of albendazole applicable to the present invention.

Formula 3

In addition, the albendazole may contain 1 to 90 parts by weight based on 100 parts by weight of the anthelmintic mixture, preferably 10 to 25 parts by weight, more preferably 20 parts by weight. At this time, if the amount of albendazole is contained in an amount of less than 1 part by weight, the effective ingredient delivery effect is insufficient, and thus there is no effect such as improvement of skin inflammation, and if it is contained in an amount exceeding 90 parts by weight, there is a problem that may cause side effects.

Pyrantel applicable to the present invention is an anthelmintic substance that treats various unspecified parasitic infectious worms, and is a stable substance with almost no side effects when applied to the skin. It has the advantage of preventing, improving, and treating the back.

In addition, the pyrantel may contain 1 to 90 parts by weight based on 100 parts by weight of the anthelmintic mixture, preferably 10 to 25 parts by weight, more preferably 20 parts by weight. At this time, when the amount of pyrantel is contained in an amount of less than 1 part by weight, the effect of delivering the active ingredient is insufficient, and thus there is no effect such as improving skin inflammation, and when it is included in an amount exceeding 90 parts by weight, there is a problem that may cause side effects.

On the other hand, niclosamide applicable to the present invention is an anthelmintic substance for controlling tapeworms or pinworms, and when applied to the skin, it can prevent, improve, and treat demodex acne and inflammation caused by transient spiny cells while having few side effects. There is an advantage.

In addition, the niclosamide may contain 1 to 90 parts by weight based on 100 parts by weight of the anthelmintic mixture, preferably 10 to 25 parts by weight, more preferably 20 parts by weight. At this time, when niclosamide is included in an amount of less than 1 part by weight, the effective ingredient delivery effect is insufficient, and thus there is no effect such as improvement of skin inflammation, and when it is included in an amount exceeding 90 parts by weight, there is a problem that may cause side effects.

In addition, according to another embodiment of the present invention, the cosmetic composition of the present invention may further include ivermectin as an anthelmintic mixture, and at this time, ivermectin may be 1 to 90 parts by weight based on 100 parts by weight of the mixture.

Ivermectin, which can be applied to the present invention, is an anthelmintic that kills parasites, and when used on the skin, it can effectively remove the Demodex without side effects, and can be used to improve inflammation that causes facial flushing. Formula 4 below is a structural formula of albendazole applicable to the present invention.

Formula 4

In addition, the ivermectin may contain 1 to 90 parts by weight based on 100 parts by weight of the anthelmintic mixture, preferably 5 to 25 parts by weight, more preferably 10 parts by weight. At this time, when ivermectin is included in an amount of less than 1 part by weight, the effective ingredient delivery effect is insufficient, and thus there is no effect such as improvement of skin inflammation, and when it is included in an amount exceeding 90 parts by weight, there is a problem that may cause side effects.

Meanwhile, in the cosmetic composition according to an embodiment of the present invention, the catalyst is a stable material that does not cause a chemical reaction with the cosmetic composition to be applied together, and the material applied in the technical field can be applied without limitation, preferably vitamin A, vitamin B, vitamin D, and vitamin E may be used alone or in combination.

In this case, the catalyst may include 0.1 to 20 parts by weight, preferably 10 parts by weight, based on 100 parts by weight of the anthelmintic mixture. If this range is satisfied, there is an advantage of minimizing side effects and preventing, treating, and improving skin inflammation.

On the other hand, in the cosmetic composition according to an embodiment of the present invention, the co-solvent is a stable material that does not cause a chemical reaction with an anthelmintic mixture, a catalyst, and an antioxidant applied together, and a solvent applied in the art can be applied without limitation, and is not limited. Typical examples include glycol, glyceride, ethyl oleate, oleyl alcohol, isopropyl myristate, propylene glycol, octanol, migriol, and the like, and preferably glycol, glyceride, ethyl oleate alone or mixed Can be used.

At this time, the co-solvent may be used, including 1 to 50 parts by weight, preferably 50 parts by weight, based on 100 parts by weight of the anthelmintic mixture. If this range is satisfied, it has high solubility and can have relatively high skin permeability due to its physicochemical properties.

In addition, in the cosmetic composition according to an embodiment of the present invention, the antioxidant is a stable material that does not cause a chemical reaction with the compositions to be applied together, and the solvent applied in the technical field can be applied without limitation, and preferably Phenoxyethanol, methylparaben, and propylglycone may be used alone or in combination.

In this case, the antioxidant may be used, including 0.1 to 20 parts by weight, preferably 10 parts by weight, based on 100 parts by weight of the anthelmintic mixture. If this range is satisfied, there is an advantage of minimizing side effects and preventing, treating, and improving skin inflammation.

Hereinafter, the present invention will be further described through examples, but it is obvious that the present invention is not limited by the following examples.

Preparation Examples 1 to 5

To prepare an anthelmintic mixture mixed in the same ratio as in Table 1 below.

division Praziquantel Mebendazole Albendazole Pirantel Niclosamide Ivermectin Manufacturing Example 1 20 20 20 20 20 - Manufacturing Example 2 25 15 20 20 20 - Manufacturing Example 3 20 20 25 15 20 - Manufacturing Example 4 20 15 25 15 25 - Manufacturing Example 5 10 20 20 20 20 10

Example

A cosmetic composition was prepared by adding 100 parts by weight of the anthelmintic mixture of Preparation Example 1, 10 parts by weight of vitamin A, and 50 parts by weight of glycol and 10 parts by weight of phenoxyethanol to the reactor.

Example 2

A cosmetic composition was prepared in the same manner as in Example 1, except that the anthelmintic mixture of Preparation Example 2 was used.

Example 3

A cosmetic composition was prepared in the same manner as in Example 1, except that the anthelmintic mixture of Preparation Example 3 was used.

Example 4

A cosmetic composition was prepared in the same manner as in Example 1, except that the anthelmintic mixture of Preparation Example 4 was used.

Example 5

A cosmetic composition was prepared in the same manner as in Example 1, except that the anthelmintic mixture of Preparation Example 5 was used.

Comparative Example 1

100 parts by weight of praziquantel, 10 parts by weight of vitamin A, and 50 parts by weight of glycol and 10 parts by weight of phenoxyethanol were added to the reactor, followed by stirring to prepare a cosmetic composition.

Comparative Example 2

100 parts by weight of mebendazole, 10 parts by weight of vitamin A, and 50 parts by weight of glycol and 10 parts by weight of phenoxyethanol were added to the reactor, followed by stirring to prepare a cosmetic composition.

Comparative Example 3

100 parts by weight of albendazole, 10 parts by weight of vitamin A, and 50 parts by weight of glycol and 10 parts by weight of phenoxyethanol were added to the reactor, followed by stirring to prepare a cosmetic composition.

Comparative Example 4

100 parts by weight of pyrantel, 10 parts by weight of vitamin A, and 50 parts by weight of glycol and 10 parts by weight of phenoxyethanol were added to the reactor, followed by stirring to prepare a cosmetic composition.

Comparative Example 5

100 parts by weight of niclosamide, 10 parts by weight of vitamin A, and 50 parts by weight of glycol and 10 parts by weight of phenoxyethanol were added to the reactor, followed by stirring to prepare a cosmetic composition.

Performance evaluation

Evaluation Example 1-Skin cell stability test evaluation

In order to verify the skin safety of the samples obtained in Examples 1 to 5, an MTT assay experiment was performed on keratinocytes (HaCaT). The samples of Examples 1 to 5 were suspended in purified water at concentrations of 0, 1, 5, 10, 20, 50 and 100 μg/mL, and then cell viability was measured. Cytotoxicity was performed by modifying Mosmann's method of measuring cell viability using MTT {3-(4,5-dimethylthiazol-2-yl) -2-5-diphenyltetrazolium bromide} reagent. Keratinocytes (HaCaT) were dispensed in a 96-well plate at ^{a concentration of 1×10 4} cells/well and incubated at 37° C. and 5% CO ₂ for 48 hours. The culture medium was removed, and the samples were cultured in a medium treated by concentration for 48 hours, and then the medium was removed and washed repeatedly with PBS (Phosphatebuffered saline). MTT was dissolved in PBS at 5 mg/mL, 50νL was added, and incubated for 48 hours at _{37°C and 5% CO 2.} DMSO (dimethyl sulfoxide) was added to 100 νL per well, stirred for 10 minutes, and absorbance was measured at 540 nm. As a result of the measurement, cytotoxicity was not confirmed at all concentrations of each sample. The results suggest that the extract of the above example is not only harmless to human cells, but also has excellent safety.

Evaluation Example 2-Evaluation of the effect of reducing inflammation

The cosmetic compositions of Examples 1 to 5 and Comparative Examples 1 to 5 were suspended in purified water, diluted, and applied to the skin to evaluate the effect of reducing Demodex. To quantify sebum and observe Demodex, a digital light microscope (Advanced Microscopy Group Inc., USA), a slide glass, a cover glass, mineral oil (Bio-Rad, USA), and tweezers were used. During the experiment, sebum extracted from the nose was collected, placed on a slide glass, covered with a cover glass, and photographed, and the sebum was quantified through ImageJsoftware. After dissolving by dropping 20 μL of oil on the slide glass where sebum was collected, the cover glass was covered and the presence or absence of Demodex was observed using a Digitallightmicroscope. After 100 subjects were divided into 10 groups of 10 subjects, 1 g of sebum was collected, the average value of the number of Demodex was performed, and the results are shown in Table 2 below. Demodex is difficult to observe because it forms a transparent shape after dying at room temperature within a short period of time, so Demodex was read within a short period of time to observe in a living state.

division Before use after use Improvement rate (%) Example 1 12.6 9.5 24.5 Example 2 11.5 8.2 28.5 Example 3 10.7 7.7 27.9 Example 4 14.5 9.9 31.5 Example 5 15.2 9.6 36.7 Comparative Example 1 13.5 11.7 13.6 Comparative Example 2 13.4 11.2 14.6 Comparative Example 3 14.2 11.9 16.3 Comparative Example 4 16.2 13.6 15.9 Comparative Example 5 16.3 13.5 16.0

Evaluation Example 3-Evaluation of Demodex survival inhibition effect

The cosmetic compositions of Examples 1 to 5 and Comparative Examples 1 to 5 were suspended and diluted in purified water, and the effect of inhibiting Demodex survival was evaluated. After attaching the electron microscope to the CCD camera, it was connected to the computer. After separating the Demodex from the hair follicle using a blade, it was placed on a slide glass, and the extract of Example diluted to a concentration of 100 μg/mL was treated. The cover glass was covered and the movements of the Demodex body and legs were observed under three electron microscopes. The electron microscope used a low magnification to observe the appearance of the Demodex, and then gradually observed the detailed appearance at a high magnification to check the time and measure the survival time. In the experiment, the survival time was measured from the time the sample was dropped to the time when the Demodex body gradually shrunk and the movement was terminated, and is shown in Table 3 below.

division Survival time Example 1 14 minutes 30 seconds Example 2 14 minutes 50 seconds Example 3 13 minutes 30 seconds Example 4 12 minutes 30 seconds Example 5 11 minutes 30 seconds Comparative Example 1 21 minutes 30 seconds Comparative Example 2 22 minutes 10 seconds Comparative Example 3 21 minutes 50 seconds Comparative Example 4 22 minutes 00 seconds Comparative Example 5 22 minutes 10 seconds

Referring to Table 2, Examples 1 to 5 according to the present invention have excellent effects of inhibiting Demodex survival compared to Comparative Examples 1 to 5, and particularly, the effect of inhibiting Demodex survival of Example 5 containing ivermectin is remarkably excellent. I did.

The above description of the present invention is for illustrative purposes only, and those of ordinary skill in the art to which the present invention pertains will be able to understand that it is possible to easily transform into other specific forms without changing the technical idea or essential features of the present invention. will be. Therefore, it should be understood that the embodiments described above are illustrative and non-limiting in all respects. For example, each component described as a single type may be implemented in a distributed manner, and similarly, components described as being distributed may also be implemented in a combined form.

The scope of the present invention is indicated by the claims to be described later, and all changes or modified forms derived from the meaning and scope of the claims and their equivalent concepts should be construed as being included in the scope of the present invention.

Claims (2)

An anthelmintic mixture of praziquantel, mebendazole, albendazole, pyrantel, niclosamide and ivermectin;
Catalyst;
Common sale; And
Antioxidants; cosmetics for the prevention and improvement of skin inflammation using an anthelmintic containing. The method of claim 1,
With respect to 100 parts by weight of the anthelmintic mixture, ivermectin is a cosmetic for preventing and improving skin inflammation using 1 to 90 parts by weight of an anthelmintic.