KR101346125B1 - A functional cosmetic composition for comprising organometallic compound containing zinc and iron as an effective component - Google Patents

Abstract

The present invention relates to a pharmaceutical composition and functional cosmetics for the prevention or treatment of itching and acne comprising an organometallic compound containing zinc and iron as an active ingredient. When the pharmaceutical composition and the functional cosmetic composition of the present invention are applied to itching and acne, it has an effect of alleviating or treating the above symptoms without side effects in a short time.

Description

A functional cosmetic composition comprising an organometallic compound containing zinc and iron as an active ingredient {A FUNCTIONAL COSMETIC COMPOSITION FOR COMPRISING ORGANOMETALLIC COMPOUND CONTAINING ZINC AND IRON AS AN EFFECTIVE COMPONENT}

The present invention relates to a functional cosmetic composition for the prevention or treatment of pruritus and acne comprising an organometallic compound containing zinc and iron as an active ingredient.

Skin is the largest organ in the body and is exposed to the outside, so it is an immune organ that is sensitive to various external stimuli. For this reason, various diseases accompanied by itching occur frequently on the skin. Representative skin diseases accompanied by itching are contact dermatitis including atopic dermatitis and febrile pruritus, urticaria, psoriasis and the like. These itching-related diseases are often scratched and scratched, which is accompanied by skin infections caused by bacterial infection and secondary infections caused by external allergens. As a result, immune cells such as T-cells and macrophages are activated to secrete various cytokines and neuropeptides, including IL-1, causing itching. Scratching again causes the symptoms of dermatitis to amplify and develop into a more serious condition.

It is estimated that 10-20% of the world's population suffers from itching, and the incidence rate is continuously increasing due to factors such as the increase of airborne allergens caused by recent environmental pollution. It is a social problem. In addition, skin itching (senile pruritus) in the elderly is also a symptom that occurs in most elderly people. In addition, it is estimated that at least 20-30% of the population will suffer from itching, including other diseases that cause skin itching. Itching is therefore the most common and important symptom of bothering humans. However, no drug has been developed so far to free itching. The only drug is antihistamine, which causes skin itch due to the involvement of histamine, IL-1 and other cytokines, neuropeptides (serotonin, acethycholine, substance P) and various inflammatory substances (leukotrines, prostaglandins). (J. Clin. Invest. 2006, 116 (5): 1174-1185).

Conventionally, in order to ameliorate the itch, a lipid complex of ceramide for moisturizing and restoring the skin barrier is applied (Korean Patent Publication No. 2001-0044622), oral administration of an antihistamine to treat the itch, a steroid for anti-inflammatory Methods such as application of agents have been generally used, and methods of applying oligosaccharides to improve skin immune status (Korean Patent Publication No. 2000-0029754) have been proposed, but topical and systemic drugs such as steroids, There are problems such as drowsiness due to oral administration of antihistamines, immunosuppressants, and the like, lowered immunity and safety to the skin according to topical administration, stability when formulating the composition for external application of the skin, and its use is also limited and its effects are insignificant.

Therefore, there is no side effect on the human body, and there is an urgent need for the development of substances that can alleviate or heal skin itching, which is one of the important challenges that humanity must solve.

Next, the cause of acne is not known exactly, but a combination of causes rather than one cause. The excess of male hormones during puberty stimulates the secretion of sebaceous glands and the epithelium of the hair follicles causes dyskerosis (abnormal keratinization with incomplete and immature keratinization), clogging the hair follicles and causing them to stiffen in the follicles (comedone). Sebum) is formed. Among the bacteria residing in hair follicles, propionibacterium acnes, in particular, secrete lipolytic enzymes, which break down triglycerides in sebum to form free fatty acids and stimulate hair follicles. In addition, the immunological response to Propionibacterium acnes contributes to the inflammatory response of acne.

It is well known that there is a family history of acne outbreaks. However, its exact genetic form is not yet clear. It is well known that many components of cosmetics can cause acne. In addition, the use of oily substances, excessive detergents and soaps contained in pomade can also cause acne. Acne usually begins in puberty, with men usually between 15 and 19 years old and women between 14 and 16 years old. About 80% of them disappear until the middle of 20 years old, but sometimes even after 30-40 years.

The primary symptom of acne is scalp (stiffened sebum in the hair follicles). There are two types of scalp: open scalp with open inlet and closed scalp with open inlet, which is black due to melanin deposition. White color If the scalp is old, inflammation occurs around it. Depending on the degree of inflammation, red acne (papulesy), pimples (purulent), nodules, cysts, etc. are formed. It is characterized by a mixture of rashes.

When acne becomes inflamed, it first turns red and then turns brown over time. If acne is left to inflame, or squeeze out, the sebum will burst into the skin, causing bumpy skin or concave scars (convex and concave scars). Acne scars are very sharp and deeply cut at the edges of other scars, and in practice, the scar bottom is often connected to the fat layer. The damage to the skin is widespread and scars are often connected to each other.

Acne treatment can be divided into two categories: medication, eating medicine and surgical treatment. Topical medications are direct antiseptics for acne bacteria, modified from topical antibiotics (Klymycin and erythromycin) and vitamin A to prevent the production of free fatty acids. Skin regeneration ointment (tretinoin, adapalene) that exfoliates keratin and releases sebum well, and strong antibacterial agent reduces bacterial populations and acne ointment (benzoyl peroxide) that has a slight anti-inflammatory and lytic effect. . There are two main types of medicine to take: antibiotics that help to kill acne and reduce inflammation, and retinoids made from modified vitamin A, commonly known as locutan. Retinoids are well known as sebum control agents because they reduce sebum secretion, but this drug is not only sebum control but also causes other acne, such as abnormal keratinization (abnormal keratinization with incomplete and immature keratinization), inflammatory reactions, bacterial growth, etc. It helps block all the paths of acne outbreaks. However, pregnancy can cause fetal malformation, so contraception is necessary from one month before the start of the drug to one month after the discontinuation. Surgical treatments include injection therapy, symptom extrusion, and dermabrasion. Large acne is scary to look at, but it is more likely to remain scars, so treatment with injection therapy will reduce scarring. If your acne is very hard and your skin is hardened, you can inject the diluted triamcinolone directly into the area so that the acne disappears quickly and no scars remain. As a side effect, the skin may shrink, but after 6 to 12 months, you do not have to worry too much. Too much squeezing acne often leaves a scar after the treatment. The reason for this is that the inflammation is weakened by excessively squeezing and destroying the oil glands walls weakened by the inflammation. However, extruded treatments performed by dermatologists do not cause these side effects because they clean the pores and clean the pores with hot steam and then squeeze acne with a special device.

Finally, atopic dermatitis is a common skin disorder with unexplained strong pruritus and a combination of dry skin, erythema and inflammation (Lancet. 1998; 351: 1715-1715). Atopic dermatitis is a chronic disease that causes great discomfort for long-term life. It occurs mainly in infants and infants. It occurs in 10 to 15% of all infants and infants, with the incidence in the atopy group being 60% in infants less than 1 year and 85% in infants less than 5 years (Lancet. 1998; 351: 1715-1721). 40% of children with atopic dermatitis gradually improved with growth, but the incidence rate of adults was about 1 to 3% of all adults due to pollution and environmental pollution caused by rapid industrialization (Immunol. Allergy. Cli. North Am. 2002; 22: 1 ~ 24), and the incidence rate has been increased two to three times as before the industrialization (Lancet. 2003; 361: 151 ~ 160). For this reason, many researchers are interested in reducing the clinical symptoms of atopic dermatitis.

Although clinical symptoms of atopic dermatitis may vary from person to person, the most common symptoms are first, severe itching, second, the patient's skin remains dry, and third, dry skin. Loss of the protective function of the skin surface makes it easier to invade the skin of irritants from outside, and this invasion causes the skin to reject and cause an inflammatory reaction (Lancet. 1998; 351: 1715 ~ 1721, J. Pediatr. Health Care. 2002; 16; 143--145).

Although many studies have been conducted to date on the causes and treatments of atopic dermatitis, there is no definite theory about the precise pathogenesis and effective treatment methods due to the conflicting research data and complexity of the disease itself. Therefore, therapeutic agents for atopic dermatitis, which have been developed to date, include topical anti-inflammatory agents such as steroids, tacrolimus, pimecrolimus, immunosuppressive agents such as antihistamines and cyclosporin. In addition, the use of hypo-allergenic moisturizers and photochemistry using ultraviolet rays as an adjuvant therapy are also being carried out in the clinic. However, these therapies or therapies help to control the symptoms to a proper level rather than the fundamental treatment, and thus do not fully satisfy the needs of patients with atopic dermatitis so far.

The present invention has been made to solve the problems of the prior art as described above, the problem to be solved in the present invention is to provide a pharmaceutical composition and a functional cosmetic composition effective in the prevention and treatment of itching and acne without side effects will be.

In order to solve the above problems, the present invention provides a functional cosmetic composition containing an organometallic compound prepared as an active ingredient comprising the following steps:

(1) dissolving 1-3 parts by weight of citric acid with respect to 100 parts by weight of water;

(2) adding zinc and iron at concentrations of 1000 to 3000 ppm and 10000 to 30000 ppm, respectively;

(3) reacting at 50 to 60 ° C. for 48 to 72 hours; And

(4) purifying after obtaining a supernatant.

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When the functional cosmetic composition of the present invention is applied to itching and acne, it has the effect of alleviating or healing the above symptoms without side effects in a short time.

1 is a graph showing a mass spectrum of an organometallic compound containing zinc and iron of the present invention.

Hereinafter, the present invention will be described in detail.

The inventors of the present invention have repeatedly studied the development of substances to alleviate or treat the symptoms of itching and acne, and as a result, organometallic compounds containing a certain amount of zinc and iron alleviate itching and acne within a short period of time without side effects. It was confirmed that there is an effect to treat.

Accordingly, the present invention provides a pharmaceutical composition for the prevention or treatment of itching and acne containing an organometallic compound prepared as an active ingredient comprising the following steps:

(1) dissolving 1-3 parts by weight of an organic acid based on 100 parts by weight of water;

(2) adding zinc and iron at concentrations of 1000 to 3000 ppm and 10000 to 30000 ppm, respectively;

(3) reacting at 50 to 60 ° C. for 48 to 72 hours; And

(4) purifying after obtaining a supernatant.

The organic acid of step (1) is preferably citric acid (citric acid). If the amount of the organic acid added to the water is less than 1 part by weight, there is a problem that the reactant is too small to sufficiently obtain an organometallic compound serving as an active ingredient. If the content is more than 3 parts by weight, the solubility is low, and the reaction time is reduced. There is a problem that becomes too long.

Zinc and iron in step (2) react with the organic acid molecules dissolved in water to form a zinc, iron and organic acid complex. In this case, the content of zinc and iron to be added is preferably in a concentration of 1000 ~ 3000ppm and 10000 ~ 30000ppm, respectively, the composition containing the organometallic compound prepared in the above concentration range was confirmed that the most effective in itching and acne.

Under the reaction conditions of step (3), the reaction of the composition comprising the organometallic compound of the present invention is completed. Specifically, the reaction temperature is carried out at 50 ~ 60 ℃, the reaction time is too long when the reaction is carried out at a temperature of less than 50 ℃, the reaction rate is faster if the reaction is carried out at a temperature exceeding 60 ℃ but side reactions There is little improvement in the itching and acne of the result. The reaction time is 48 to 72 hours, and when the reaction is performed for less than 48 hours, the metal and the organic acid cannot react sufficiently, and when the reaction time exceeds 72 hours, a side reaction proceeds to be a problem.

Step (4) is a step of purifying the reaction product completed in step (3), after separating the supernatant from the precipitate to purify the supernatant containing the organometallic compound of the present invention by filtration, chromatography, etc. Can be.

The mass spectrometry results of the products obtained through the above steps (1) to (4) are shown in FIG. 1, and the molecular weight of the organometallic compound of the present invention was found to be 472.

In addition, the components of the organometallic compound of the present invention are shown in Table 1 below.

Name of circle Component content (%) Atomic mass C 15.72 111 O 66.91 154 H 3.37 168 N - - S - - Fe 11 11 Zn 3 3

The composition containing the organometallic compound obtained according to the production method of the present invention comprises 1 to 14% by weight based on the total weight of the pharmaceutical composition.

For the prevention and treatment of itching and acne containing the composition containing the organometallic compound of the present invention as an active ingredient The pharmaceutical composition may further comprise suitable carriers, excipients and diluents commonly used in the manufacture of pharmaceutical compositions. The pharmaceutical composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, granules, fine granules, powders, hard capsules, soft capsules, syrups, emulsions, suspensions or solutions, and the like. May be administered as a pharmaceutical composition for oral administration of oral injection, intravenous, intramuscular or subcutaneous injection, mucus, suppository, transdermal absorbent, transmucosal absorbent, nasal drops, ear drops, eye drops, inhalants, creams It is also possible to administer it as a pharmaceutical composition for parenteral administration, such as ointment and pape. The formulation prepared as a pharmaceutical composition in powder form may be dissolved at the time of use and used as an injection or a mucus. In particular, the pharmaceutical compositions of the present invention may preferably be in the form of paste ointments, creams, milks, powders, powders, penetration pads, solutions, gels, sprays, lotions or suspensions.

For the preparation of pharmaceutical compositions, additives for the preparation of solids or liquids may be used. The preparation additive may be either organic or inorganic.

When preparing oral solid preparations, excipients, additional binders, disintegrants, lubricants, colorants, and the like are added to the main medicine, and then tablets, coated tablets, granules, powders, capsules are prepared by conventional methods. Formulations in the form of can be prepared. Examples of the excipient to be used include lactose, sucrose, saccharine, glucose, corn starch, starch, talc, sorbit, crystalline cellulose, dextrin, kaolin, calcium carbonate and silicon dioxide. Examples of the binder include polyvinyl alcohol, polyvinyl ether, ethylcellulose, methylcellulose, gum arabic, tragacanth, gelatin, shellac, hydroxypropylcellulose, hydroxypropylmethylcellulose, calcium citrate, Dextrin, pectin, and the like. Examples of the lubricant include magnesium stearate, talc, polyethylene glycol, silica, and hydrogenated vegetable oil. Any coloring agent may be used as long as it is usually allowed to be added to pharmaceuticals. These tablets and granules can be suitably coated with sugar (sugar coating), gelatin coating, and others as required. If necessary, preservatives, antioxidants and the like may be added.

For preparing liquid preparations for oral administration, for example, emulsions, syrups, suspensions, and solutions, inert diluents commonly used, such as water or vegetable oils, may be used. In addition to the inert diluent, auxiliary agents such as wetting agents, suspending aids, sweeteners, fragrances, coloring agents or preservatives may be added to the formulation. After preparing the liquid formulation, it may be filled into capsules of absorbable material such as gelatin.

Examples of the solvent or suspending agent for use in the preparation of a parenterally administrable preparation, such as an injection or suppository, include water, propylene glycol, polyethylene glycol, benzyl alcohol, ethyl oleate, and lecithin. Examples of the base used in the production of suppositories include cacao butter, oil cacao butter, laurin butter, and wipesol. The preparation method of the preparation is not particularly limited, and any of the methods commonly used in the art can be used.

In the case of injections, diluents such as water, ethyl alcohol, macrogol, propylene glycol, citric acid, acetic acid, phosphoric acid, lactic acid, sodium lactate and sulfuric acid, sodium citrate, PH adjusting agents and buffers such as sodium and sodium phosphate, and stabilizers such as sodium pyrosulfite, ethylenediamine acetic acid, thioglycolic acid and thio lactic acid. In this case, a sufficient amount of salt, glucose, mannitol, or glycerin may be added to the preparation to prepare an isotonic solution, and it is also possible to use conventional dissolution aids, no-tainting agents, or local anesthetics.

In the case of ointments, for example, in the form of pastes, creams and gels, conventionally used bases, stabilizers, wetting agents, preservatives and the like can be incorporated as required, and the components can be mixed by a conventional method . As the base, for example, white petrolatum, polyethylene, paraffin, glycerin, cellulose derivatives, polyethylene glycol, silicon and bentonite can be used. As the preservative, methyl p-hydroxybenzoate, ethyl p-oxybenzoate, propyl p-hydroxybenzoate and the like can be used. In the case of the form of a sticking agent, the above ointment, cream, gel, paste or the like can be applied to a conventional support by a conventional method. As the support, a film or a foam sheet such as a woven or nonwoven fabric made of cotton, staple fiber and chemical fiber, flexible polyvinyl chloride, polyethylene and polyurethane can be suitably used.

The dosage of the pharmaceutical composition of the present invention is not particularly limited, but in the case of oral administration, it is usually 0.1 to 500 mg / kg, preferably 1 to 100 mg / kg per kg, as the weight of the substance as an active ingredient per adult. have. It is preferable to appropriately increase or decrease this dosage depending on the age, condition and symptoms of the patient. The daily dose may be administered once or in two or three times a day at appropriate intervals or may be administered intermittently at intervals of several days. When used as an injection, the weight of the substance as an active ingredient per adult may be usually 0.01 to 10 mg / kg, preferably 0.1 to 1 mg / kg per kg. However, since the dose of the pharmaceutical composition of the present invention is determined in consideration of various factors such as the administration route, the patient's age, sex, weight, and the severity of the patient, the dose is limited in any aspect to the scope of the present invention. Should not be construed as doing.

In addition, the present invention provides a functional cosmetic composition containing the organometallic compound prepared by including each of the above steps as an active ingredient.

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The cosmetic composition according to the present invention may be formulated as an external preparation for skin or cosmetics.

The external preparation for skin may be an ointment, a warning agent, a spray, a suspension, an emulsion, a cream, a gel or the like.

The cosmetics may include basic cosmetics, makeup cosmetics, body cosmetics, shaving cosmetics, and the like. Examples of the basic cosmetics include creams, lotions, packs, massage creams, emulsions, etc. Examples of the makeup cosmetics include foundations, makeup bases, lipsticks, eyeshadows, eyeliners, mascara, eyebrow pencils, and the like. Examples of cosmetics include soaps, liquid detergents, baths, sunscreen creams, sun oils, and the like. Examples of shaving cosmetics include aftershave and shaving creams, but are not limited thereto.

Components included in the cosmetic composition of the present invention may include components commonly used in cosmetic compositions in addition to the composition comprising the organometallic compound of the present invention as an active ingredient, for example, antioxidants, stabilizers, solubilizers, vitamins Conventional adjuvants such as pigments and perfumes, and carriers. In addition, the cosmetic composition may further include a skin absorption promoting substance to enhance the effect.

When the formulation of the present invention is a paste, cream or gel, an animal oil, vegetable oil, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as the carrier component .

In the case where the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. Especially, in the case of a spray, a mixture of chlorofluorohydrocarbons, propane / Propane or dimethyl ether.

When the formulation of the present invention is a solution or an emulsion, a solvent, a dissolving agent or an emulsifying agent is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, , 3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid esters.

In the case where the formulation of the present invention is a suspension, a carrier such as water, a liquid diluent such as ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Cellulose, aluminum metahydroxide, bentonite, agar or tracant, etc. may be used.

When the formulation of the present invention is an interface-active agent-containing cleansing, the carrier component is selected from aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters.

The composition containing the organometallic compound contained in the cosmetic composition of the present invention is preferably contained in 1 to 14% by weight based on the total dry composition weight.

[ Example ]

Hereinafter, the examples are only for illustrating the present invention in more detail, and the scope of the present invention is not limited by these examples according to the gist of the present invention, and modifications, substitutions, and insertions commonly known by those skilled in the art It will be apparent to those skilled in the art that the present invention may be included in the scope of the present invention.

1. Preparation of a composition comprising an organometallic compound

1000 ml of water was added to a 5 L reactor, followed by dissolving 20 g of citric acid. Zinc and iron were added to the final concentration of 2000 ppm and 20000 ppm, respectively, into the aqueous citric acid solution, and stirred at 50 ° C. for 72 hours. After the precipitate was removed through the filter paper and the supernatant was purified by chromatography, a cream formulation was prepared such that the composition of the present invention was at a concentration of 10% by weight.

2. Experimental group  Screening and Application

Ten patients each had itching, acne, millet spots, erosion, and pigmentation. After applying the cream prepared in Example 1 to the lesion site once a day, the number and duration of patients whose symptoms were observed were examined, and the results are shown in Table 2.

Symptom ＼ Treatment Period 1 day 3 days 1 week 2 weeks 3 weeks Itching 9 people 1 person acne 2 people 8 people Millet 1 person 7 people 2 people Erosion 1 person 6 people 3 people Pigmentation 2 people 8 people

As shown in Table 2, the composition containing the organometallic compound of the present invention showed a remarkable improvement by only one administration in the case of itching, 3 days for acne and millet spots, 1 week for erosion In the case of pigmentation, it can be seen that a three-week administration shows a therapeutic effect.

Claims (4)

delete delete (a) dissolving 1-3 parts by weight of citric acid with respect to 100 parts by weight of water;
(b) adding zinc and iron at concentrations of 1000 to 3000 ppm and 10000 to 30000 ppm, respectively;
(c) reacting at 50-60 ° C. for 48-72 hours and
(d) functional cosmetic composition containing an organometallic compound prepared as an active ingredient, comprising the step of obtaining and purifying the supernatant. delete

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