WO2010062103A2

WO2010062103A2 - Topical skin composition and method for preparing same

Info

Publication number: WO2010062103A2
Application number: PCT/KR2009/006960
Authority: WO
Inventors: 양근영
Original assignee: Yang Gean Yung
Priority date: 2008-11-26
Filing date: 2009-11-25
Publication date: 2010-06-03
Also published as: WO2010062103A3; KR20100059188A; WO2010062103A9

Abstract

Provided are a topical skin composition and a method for preparing same, the composition comprising pumice, alum, iron sulfate, calamine, borneol, Xanthii Fructus extract, Sophorae Radix extract, Radix Rubiae extract, Phellodendri Cortex extract, Rhus gall extract, gentamycin sulfate, betamethasone dipropionate and badger oil. The composition of the present invention is effective for such skin diseases as atopic dermatitis, athlete's foot, and eczema, and has an advantage of a low risk of adverse reaction and relapse. The composition of the present invention may be effectively prepared by the preparation method of the present invention.

Description

External skin composition and preparation method thereof

The present invention relates to an external composition for skin, and more particularly, to an external skin composition having an advantage of being effective in skin diseases such as atopic dermatitis, athlete's foot, eczema, and having low side effects and recurrence.

The external skin composition is an effective composition for skin diseases, and is a composition showing an effective effect on atopic dermatitis, athlete's foot, eczema and the like among skin diseases.

Atopic dermatitis is an abnormality in the stratum corneum, the outermost protective wall of the skin. The main symptoms of atopic dermatitis are erythema, edema / papulation, and oozing / crust. ), Epidermal peeling, lichenification and dryness.

The acute phase forms blisters in the epidermis, while the chronic phase develops thickening of the skin and skin. Atopic dermatitis takes the stages of infancy and infancy, and symptoms of infancy begin at two to three months of age, with reddening and rashes on the face, spreading to the whole frozen soup, neck, limbs and whole body. do. About 75% of infantile atopic dermatitis is lost in two stones, but about 25% of infants develop childhood atopic dermatitis and sometimes develop new ones.

To date, atopic dermatitis mainly consists of pharmacotherapy such as steroids, antihistamines and antibiotics. Steroids have anti-inflammatory and immunosuppressive effects and have excellent effects, but are often relapsed when discontinued, and long-term use is known to have side effects such as skin atrophy, vasodilation, discoloration, and purpura.

Therefore, there is a demand for the development of a composition having excellent effects on skin diseases such as atopic dermatitis, low recurrence, and low side effects. The inventor of the present invention has completed the present invention after a long time research effort.

Therefore, the technical problem to be achieved by the present invention is to provide an external composition for skin effective in skin diseases such as atopic dermatitis, less side effects, and low recurrence.

In addition, another technical problem to be achieved by the present invention is to provide a method for producing an external composition for skin effective in atopic dermatitis and the like, less side effects and low recurrence.

On the other hand, other unspecified objects of the present invention will be further considered within the range that can be easily inferred from the following detailed description and effects.

The present invention is an external skin composition comprising an anatomical stone, alum, green spots, sensitized stone, yongnae, changja extract, red ginseng extract, cheoncho extract, baekbaek extract, ginseng extract, gentamicin, dipropionate betamethasone, and badger oil To provide.

Anatomical stone (pumex) in the composition of the present invention is a porous silicate mineral ([SiO ₂ ] x) formed by the solidification of rocks spewed from volcanoes, which are essential minerals calcium, iron, zinc, copper, nickel, It contains chromium, cobalt, vanadium, and selenium. It is known to cure swelling by treating lumps and bumps on the skin and extreme abdominal pain.

Alumen in the composition of the present invention is a double salt formed by sulfates of monovalent metals such as alkali metals, thallium, and ammonium other than aluminum sulfate and lithium, and is also called alum. The substitution of other trivalent metal ions is also called alum in a broad sense, and is known to be effective for hemostasis, bleeding, insecticidal detoxification, convergence, antibacterial, trichomonas vaginitis, and liquor improvement.

Melanterium of the composition of the present invention is a sulfate mineral containing monoclinic ferric sulfate, the main component is ferrous sulfate (FeSO ₄ · 7H ₂ O), moisture, insecticide, It is known to have an effect such as blood.

Calamina (조성물 石; Calamina) of the composition of the present invention has been described as having the efficacy of nominal, probationary, salty, lichen, baptismal, detoxification, etc. in synonym.

Borneol (조성물; Borneol) in the composition of the present invention has been described as having the efficacy of saengjong, blue heat pain, etc. in synonym.

Changzai extract in the composition of the present invention as a solvent extract of Changza, Xanthii Fructus is described in the synonym as having a potency, such as mountain breeze, insecticide, pain, detoxification.

The ginseng extract of the composition of the present invention is a solvent extract of the ginseng, and the ginseng (苦蔘) (Sophorae Radix) has been described as having the effect of the insecticidal insects, chungpung insect, blue heat humidity.

Cheoncho extract in the composition of the present invention is a solvent extract of Cheoncho, Cheoncho (川椒; Zanthoxhli Pericarpium) has been described as having the efficacy of insecticide, dehumidification pain, etc. in synonym.

The sulfur extract of the composition of the present invention is a solvent extract of sulfur white, sulfur white (黃柏; Phellodendri Cortex) has been described as having the effects of detoxification, blue heat humidity, etc. in synonym.

The gall bladder extract of the composition of the present invention is a gall bladder solvent extract, the gall bladder (五倍子; Galla Rhois) has been described as having the effect of hemostasis, detoxification, etc. in synonym.

Gentamicin sulfate in the composition of the present invention is a sulfate of an aminoglycoside-based compound having antibacterial activity, and is used to treat seborrheic dermatitis, fungus or virus secondaryly infected with primary skin infections such as infectious impetigo and purulent bacteria. It is used for the treatment of secondary skin infections such as duplicate infection caused by infection.

Betamethasone Dipropionate in the composition of the present invention is an anti-inflammatory corticosteroid, a compound of formula C ₂₈ H ₃₇ FO ₇ , and has a therapeutic effect such as psoriasis, seborrheic dermatitis, irritable dermatitis, contact dermatitis, eczema, etc. Known.

Badger oil (Melis Sebum) of the composition of the present invention is known to have the effect of lubrication, swelling detoxification, etc., in addition to the skin protective action in the composition of the present invention acts as a base and can penetrate the skin.

The gentamicin sulfate, dipropionate betamethasone, and badger oil may be purchased or manufactured from commercially available products.

The dissected stones, alum, green spots, sensitized stones, and chalcedony can be pulverized and used in powder form. Preferably, the particle size of the powder is 300 to 500 mesh. That is, it is possible to use a powder that passes through the mesh 300 mesh sieve and does not pass through the 500 mesh sieve.

The fine particles having a particle diameter of 500 mesh sieve may be absorbed by the skin or may block pores, and the coating particles may not have good coating feeling.

The extract may be extracted with water or an organic solvent, or a mixed solvent thereof. The organic solvent may be any solvent that can be used in general, preferably a polar solvent such as water, C1-4 alcohol (for example, methanol, ethanol and the like) or a mixture thereof.

The extraction can be carried out by conventional methods such as hot water extraction, it can be used by lyophilizing the extract. In addition, the extract can be used more purified by conventional fractionation or chromatography.

The composition of the present invention has an effect on skin diseases, and has an effective effect on atopic dermatitis, athlete's foot, eczema and the like.

Accordingly, the present invention provides a method for improving atopic dermatitis and administering the composition to a subject.

The composition of the present invention is 50 to 200 parts by weight of the alum, 50 to 200 parts by weight, 50 to 200 parts by weight, 50 to 200 parts by weight of the sensitized stone, 50 to 200 parts by weight of the chalcedony extract 50 ~ 200 parts by weight, the ginseng extract 50 ~ 200 parts by weight, the Cheoncho extract 25 ~ 200 parts by weight, the baekbaek extract 50 ~ 200 parts by weight, the gall bladder extract 50 ~ 200 parts by weight, the gentamicin sulfate 0.1 ~ 1 parts by weight 5 to 20 parts by weight of the dipropionate betamethasone, and 4000 to 16000 parts by weight of the badger oil.

Changzai extract, Gosam extract, cheoncho extract, yellowish white extract, and quinine extract in the composition of the present invention may be a mixed extract extracted by mixing Changja, red ginseng, cheoncho, baekbaek, and quintet, dissecting the composition comprising the mixed extract 50 to 200 parts by weight of the alum, 50 to 200 parts by weight of the green spot, 50 to 200 parts by weight of the sensitized stone, 50 to 200 parts by weight of the bracts, 225 to 1000 parts by weight of the mixed extract, the sulfuric acid It may be 0.1 to 1 parts by weight of gentamicin, 5 to 20 parts by weight of the betamethasone dipropionate, and 4000 to 16000 parts by weight of the badger oil.

The composition of the present invention, in addition to the above-mentioned effective ingredient, may further include a substance exhibiting additional atopic dermatitis improving action known in the art.

The composition of the present invention may be applied to the human body in various ways or forms, but is preferably applied topically to the skin, and has an external skin formulation. That is, ointments, gels, creams, linings, lotions, liquids, or aerosols.

The composition of the present invention may be a pharmaceutical composition.

The pharmaceutical composition comprises a pharmaceutically acceptable carrier.

Pharmaceutically acceptable carriers may be used by mixing one or more of lactose, dextrose, sucrose, starch, saline, sterile water, Ringer's solution, buffered saline, dextrose solution, maltodextrin solution, glycerol, ethanol, and the like. If desired, other conventional additives such as antioxidants, buffers, bacteriostatics, stabilizers, etc. may be added. Diluents, dispersants, surfactants, solvents, disintegrants, sweeteners, binders, coatings, swelling agents, lubricants, lubricants or flavoring agents may additionally be added. Furthermore, it may be preferably formulated according to each disease or component by any suitable method in the art or using methods disclosed in Remington's Pharmaceutical Science (Recent Edition), Mack Publishing Company, Easton PA.

When formulated into an ointment, in addition to the composition of the present invention can be prepared by appropriately mixing the ointment, other additives and the like. The ointment and other additives may be appropriately selected from higher fatty acids or esters thereof, lead, surfactants, higher alcohols, silicone oils, hydrocarbons, water, humectants, and anti-infective agents.

The pharmaceutical composition of the present invention is by parenteral administration, preferably topical application by application.

The pharmaceutical composition of the present invention may be prepared in an external dermal formulation, i.e. powder, gel, ointment, cream, liquid or aerosol formulation.

In the pharmaceutical composition according to the present invention, the dosage of the active ingredient may be adjusted within the range of 0.1 mg / kg to 1000 mg / kg based on an adult weight of 60 kg. However, the optimum dosage to be administered can be easily determined by those skilled in the art, and the type of disease, the severity of the disease, the amount of active ingredients and other ingredients contained in the composition, the type of formulation, and the age, weight, general health of the patient It may be adjusted according to various factors including the condition, sex and diet, time of administration, and the rate of secretion of the composition, the duration of treatment, and the drugs used simultaneously.

In addition, the composition of the present invention may be a cosmetic composition.

The cosmetic composition of the present invention may include components conventionally included in the cosmetic composition, and may include, for example, conventional auxiliaries such as antioxidants, stabilizers, solubilizers, vitamins, pigments and flavors, carriers, and the like.

The cosmetic composition may be prepared in any of the formulations conventionally prepared, and may be prepared, for example, as a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, cleansing, spray, or the like.

In addition, the present invention comprises the steps of (a) pulverizing anatomical stone, alum, green spots, sensitized stone, and chalcedony; (b) distilling Changja, red ginseng, cheoncho, baekbaek, and gallengja in water and then heating to obtain a hot water extract; (c) mixing gentamicin sulfate, betamethasone dipropionate, and badger oil to obtain a mixture; And (d) mixing the ground powder of step (a), the hot water extract of step (b), and the mixture of step (c).

Specifically, the production method of the present invention is as follows, anatomical stone, alum, green spot, sensitized stone, chalcedony, changja, red ginseng, cheoncho, baekbaek, galleng, gentamicin sulfate, dipropionate betamethasone, and badger The content of oil is the same as in the composition of the present invention.

50 to 200 parts by weight of alum, 50 to 200 parts by weight of alum, 50 to 200 parts by weight of unreacted stone, and 50 to 200 parts by weight of pulverum are mixed and pulverized with a grinder in step (a). A pulverized product having a particle size of 300 to 500 mesh can be produced.

The window of step (b) was prepared by heating the mature fruit of Xanthium strumarium L. at 120 to 170 ° C. for 10 to 40 minutes to remove thorns, and the root of the ginseng (Sophora flavescens AIT.) After washing with water, it is immersed in rice water for 8 to 12 hours, it can be prepared by drying for 20 to 40 days at 10-30 ℃ temperature.

The hot water extract in the step (b) is Changja, Gosam, Cheoncho, Yellow and White, and five ginseng in a weight ratio of 50 to 200: 50 to 200: 25 to 200: 50 to 200: 50 to 200, and then mixed with respect to the mixture After immersing the mixture in purified water having a volume ratio of 3-7 times, the mixture is heated at 90-120 ° C. for 4-6 hours, the solids are filtered off, and heated and concentrated at 90-120 ° C. for 4-6 hours. .

Badger oil in step (c) may be prepared by heating the fat of badger at a temperature of 500 ~ 800 ℃ 1.5 ~ 4 hours, the mixture of step (c) is a gentamicin sulfate, dipropionate betamethasone, and badger oil It may be mixed in a weight ratio of 0.1 to 1: 5 to 20: 4000 to 16000. Badger oil may be added in step (d) to match the total amount of the composition.

The hot water extract mixed in step (d) may be 225 to 1000 parts by weight based on 100 parts by weight of the anatomical stone of step (a).

The mixing of the steps (c) and (d) may be mixed using a known mixer, etc., and after the step (d), the finished product may be manufactured by further packaging the product.

The composition of the present invention is effective in skin diseases such as atopic dermatitis, athlete's foot, eczema, and has the advantage of low side effects and low recurrence. Moreover, the composition of this invention can be manufactured effectively by the manufacturing method of this invention.

1 is a photograph of the skin condition before using the composition of Example 1.

Figure 2 is a photograph of the skin condition after using the composition of Example 1 for 5 months.

Examples are provided to help understand the present invention. The following examples are merely provided to more easily understand the present invention, but the contents of the present invention are not limited by the examples.

Example 1 Preparation of External Skin Composition

(1-1) Anatomy Stone (Daegwang Construction Material, Chuncheon, Korea) 6.4g, Baekban (Daegwang Construction Material, Chuncheon, Korea) 6.4g, Nokban (Daegwang Construction Material, Chuncheon, Korea) 6.4g Korea) 6.4g, and yonggyong (Daegwang building materials, Chuncheon, Korea) 6.4g was pulverized and pulverized to prepare a powder of 300 ~ 500 mesh.

(1-2) Changza (Daegwang Building, Chuncheon, Korea) 10g, Gosam (Daegwang Building, Chuncheon, Korea) 10g, Cheoncho (Daegwang Building, Chuncheon, Korea) 5g, Hwangbaek (Daegwang Building, Chuncheon, Korea) 10g, and Pour purified water that is three times the total volume of the drug into 10g of Ohbaeja (Daegwang building materials, Chuncheon, Korea), heat it to 100 ° C for 5 hours, filter the liquid and heat the filtrate to 100 ° C until it reaches 25g. A mixed extract was prepared.

The window was used to remove the burned thorns by heating the dog nose to 170 ℃ for 25 minutes in a pan.

The ginseng was washed with the root of the ginseng, immersed in rice water for 10 hours, and then used to dry for 30 days at 25 ~ 28 ℃.

(1-3) A mixture was prepared by mixing 25 mg of gentamicin sulfate (Korea Pharmaceutical Association, Seoul, Korea), 600 mg of dipropionate betamethasone (Korea Pharmaceutical Association, Seoul, South Korea), and badger oil. Badger oil was used as the oil (1.8kg) obtained by heating 8.5kg fat of wild badger captured in Gangwon-do and heating at 600 ℃ for 2 hours, and badger oil was used to make the final composition total 500g. .

(1-4) The powder of (1-1) and the extract of (1-2) were mixed with the mixture of (1-3) to prepare an external composition for skin.

Comparative Example 1 Preparation of Gentamicin Sulfate, Betamethasone Dipropionate, and Badger Oil-Containing Composition

In the same manner as in the preparation of the mixture in Example (1-3), the composition of Comparative Example 1 was prepared.

<Comparative Example 2> Preparation of Changjaza, Gosam, Cheoncho, Yellowish White, and Ginseng Extract and Badger Oil-Containing Composition

Comparison by mixing the extract prepared in the same manner as the extract preparation method of Example (1-2) and the badger oil (the remaining amount so that the final composition is a total of 500g) prepared in the same manner as the badger oil of Example (1-3) The composition of Example 2 was prepared.

Comparative Example 3 Preparation of Anatomic Stone, Aluminous Table, Green Plate, Nogam Stone, Dragon Head, and Badger Oil-Containing Composition

Mixing the ground powder prepared in the same manner as in the milled product preparation of Example (1-1) and the badger oil (the remaining amount of the final composition totaling 500 g) prepared in the same manner as the badger oil of Example (1-3) To prepare a composition of Comparative Example 3.

Comparative Example 4 Preparation of Changjaza, Red Ginseng, Cheoncho, Yellowish White, and Ginseng Extract, and Anatomical Stones, Alum, Green Spots, Nogamstones, and Brain and Badger Oil-Containing Compositions

A composition of Comparative Example 4 was prepared in the same manner as in Example 1, except that gentamicin sulfate and betamethasone dipropionate were not used.

Comparative Example 5 Preparation of Badger Oil

500 g of badger oil prepared in the same manner as in Example (1-3) were prepared.

Experimental Example 1 Atopic Dermatitis Improvement Effect Confirmation Experiment 1

100 patients (5-50 years old male and female) suffering from atopic dermatitis were tested for atopic dermatitis improvement effect for 4 weeks using the composition of Example 1 and the compositions of Comparative Examples 1-5. The composition of Example 1 was to be used for 50 people, each of the compositions of Comparative Examples 1 to 5 was to be used for 10 people, three times a day to spread thinly on the affected area. If the symptom disappeared during the test, it was no longer used.

The effect was assessed using the Atopic Improvement Test (Local SCORAD) before and after using each composition.

A total of 6 clinical evaluation items were 1) Erythema, 2) Edema / Papulation, 3) Oozing / Crust, 4) Excoriation, 5) Lichenification , 6) Dryness, and each item was evaluated in four stages (0 = no symptom, 1 = negative symptom, 2 = medium symptom, 3 = severe symptom) depending on the degree. Then, the values of all six items were summed and evaluated.

The improvement rate for each individual was calculated by Equation 1 below, and the average improvement rate was obtained by dividing the total improvement rate for each individual by the number of subjects (Equation 2). The results are shown in Table 1.

[Equation 1]

% Improvement = {(Sum of 6 items before use-Sum of 6 items after use) / Sum of 6 items before use} × 100 (%)

[Equation 2]

Average improvement rate (% / person) = total improvement rate (%) ÷ number of people (person)

Table 1

	% Improvement	Audience Count	% Average improvement
Example 1	3416.35	50	68.33
Comparative Example 1	161.12	10	16.11
Comparative Example 2	183.34	10	18.33
Comparative Example 3	166.68	10	16.67
Comparative Example 4	305.53	10	30.55
Comparative Example 5	122.22	10	12.22

From the results of Table 1, it can be seen that the composition of Example 1 has an excellent effect of improving atopic dermatitis compared to the cases of Comparative Examples 1 to 5.

Among the subjects using the composition of Example 1, 17 patients with athlete's foot and 20 patients with eczema were used for athlete's foot and eczema, and the symptoms were reported to be improved.

In addition, 50 of the subjects using the composition of Example 1 was used for the composition of Example 1 in the same manner for an additional 4 to 5 months until complete cured, 6 months after cure if atopic dermatitis recurrence and side effects Was investigated. As a result, a case of recurrence or side effects of atopic dermatitis was not investigated.

One of the subjects who used the composition of Example 1 for 5 months was photographed before and after 5 months of use, and the results are shown in FIGS. 1 and 2. 1 is a photograph of the skin condition before use, Figure 2 is a photograph of the skin condition after 5 months of use. As a result, it can be confirmed that atopic dermatitis is improved by using the composition of Example 1.

From these results, it was confirmed that the composition of the present invention is effective in atopic dermatitis and the like, and has no problem of recurrence or side effects.

Claims

Skin external composition comprising anatomical stone, alum, green spot, sensitized stone, cerebrum, changja extract, red ginseng extract, cheoncho extract, baekbaek extract, gallant extract, gentamicin sulfate, dimethionate betamethasone, and badger oil.
According to claim 1, wherein the composition is a composition for improving atopic dermatitis.
The skin external composition of claim 1, wherein the anatomical stone, the alum, the green spot, the sensitized stone, and the head of the brain have a particle size of 300 to 500 mesh.
According to claim 1, 50 to 200 parts by weight of the alum, 50 to 200 parts by weight, 50 to 200 parts by weight, 50 to 200 parts by weight of the sensitized stone, 50 to 200 parts by weight of the bractite, the Changza extract 50 to 200 parts by weight, 50 to 200 parts by weight of the ginseng extract, 25 to 200 parts by weight of the cheoncho extract, 50 to 200 parts by weight of the baekbaek extract, 50 to 200 parts by weight of the gall bladder extract, 0.1 to 1 weight of the gentamicin sulfate Part, 5 to 20 parts by weight of the betamethasone dipropionate, and 4000 to 16000 parts by weight of the badger oil.
The composition of claim 1, wherein the Changjaja extract, the Ginseng extract, the Cheoncho extract, the Yellow White extract, and the Goongja extract are hot water extracts obtained by mixing Changja, Gosam, Cheoncho, Yellow and White, and the Gobae.
According to claim 5, 50 to 200 parts by weight of the alum, 50 to 200 parts by weight, 50 to 200 parts by weight, 50 to 200 parts by weight of the sensitized stone, 50 to 200 parts by weight of the brain powder, the hot water extract 225 to 1000 parts by weight, 0.1 to 1 parts by weight of the gentamicin sulfate, 5 to 20 parts by weight of the betamethasone dipropionate, and 4000 to 16000 parts by weight of the badger oil.
The composition of claim 1, wherein said composition is a pharmaceutical composition.
The composition of claim 1, wherein the composition is a cosmetic composition.
(a) pulverizing anatomical stone, alum, green spots, sensitized rocks, and brains to obtain a pulverized product;

(b) distilling Changja, red ginseng, cheoncho, baekbaek, and gallengja in water and then heating to obtain a hot water extract;

(c) mixing gentamicin sulfate, betamethasone dipropionate, and badger oil to obtain a mixture; And

(d) a method for preparing an external composition for skin comprising the step of mixing the pulverized product of step (a), the hot water extract of step (b), and the mixture of step (c).
10. The method according to claim 9, wherein the pulverization of step (a) is pulverized so that the particle size of the pulverized product is 300 to 500 mesh.
10. The method according to claim 9, wherein the window box of step (b) is removed by heating.
10. The method according to claim 9, wherein the ginseng of step (b) is washed with the roots of the ginseng, immersed in rice water, and dried.