KR100925675B1 - A medicine of external use for improving diseases caused by trouble of blood circulation - Google Patents

Abstract

The present invention relates to a skin external preparation for improving blood circulation disorders. The present invention relates to an external preparation for skin circulation disorders, which is excellent in improving various blood circulation disorders by preparing an external preparation for skin and preparing the external preparation for application to the skin. There is an excellent effect of providing agents with efficacy.

Blood circulation, blood circulation disorder, blood circulation disorder, spicy taste, external skin preparation

Description

External medicine for improving blood circulation disorders {a medicine of external use for improving diseases caused by trouble of blood circulation}

The present invention relates to a skin external preparation for improving blood circulation disorders, and more particularly, to a skin external preparation having excellent efficacy in improving various blood circulation disorders.

Blood circulation is the flow of blood in a certain direction in the animal's body, depending on the activity of the heart, and if the blood circulation is disturbed, side effects and diseases will be followed. Representative examples include degenerative arthritis and hand and foot numbness that are common in old age. In addition, blood circulation acts to supply oxygen and nutrients to each organ and muscle of the whole body, and thus can directly and indirectly affect diseases of all organs and muscles.

The present invention has been made in view of these points to provide a skin external preparation having excellent efficacy in improving various blood circulation disorders by applying or adhering to the skin based on a hot component.

Accordingly, an object of the present invention is to provide an external preparation for skin having excellent efficacy in improving various blood circulation disorder diseases by applying or adhering to skin with a hot component as a main ingredient.

Hereinafter, the present invention will be described in detail.

The present invention provides an external skin preparation for improving blood circulation disorders.

Blood circulation disorders in the present invention mainly refers to degenerative arthritis that can be caused by a variety of causes, such as elbows, fingers, knees, toes, etc. In addition, blood circulation is not smooth, rhinitis that can occur in the cartilage area, meningitis , Osteomyelitis, cystitis and the like.

The external skin preparation of the present invention is most preferably supplied as a liquid product such as an ointment or a transparent lotion, but another preferred liquid product type may be a cream or a transparent gel, and the solid agent may be an adhesive in the form of a paste.

The skin external preparation for improving blood circulation disorders of the present invention contains hot pepper extract, green onion extract, garlic extract, and gardenia extract as a main ingredient, and dextrin or its extract in order to maintain efficacy for a long time by enclosing the hot component. A similar substance shall be mix | blended.

In order to obtain the skin lotion of the transparent lotion or the transparent gel in the present invention, in particular, the hot ingredient may be extracted or chemically synthesized from hot pepper extract, leek extract, garlic extract or gardenia extract.

Capsaicin analogues such as capsaicin, capsicoside, capsaicinoid, tugarasitinki, dihydroxycapsaicin, capxanthine, etc. as the chemically synthesized pungent component; Nicotinic acid benzyl, nicotinic acid beta -Butkysiethyl, N-asyrwaniramide, and nonyl acid and niramide, and one or two or more thereof may be used in combination.

Cyclodextrins that can be blended as the inclusion substance of the hot component include α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin, δ-cyclodextrin, and the cyclodextrin derivatives include methylcyclodextrin and hydroxyethyl. Cyclodextrin, marsyl-α-cyclodextrin, hydroxyethyl-β-cyclodextrin, triacetyl-β-cyclodextrin, and these may be used alone or in combination of two or more thereof.

In order to improve blood circulation disorder as the external preparation for skin of the present invention, the mixing ratio of the pungent ingredient and the inclusion material is not particularly limited, but is preferably 0.05 to 0.1: 0.1 to 10.

If the ratio of the inclusion material in the compounding ratio is too small, the persistence of the efficacy is lowered, if too large, the drug efficacy is reduced.

On the other hand, fragrances, colorants, and refreshing agents may be added to the hot component and the cyclodextrin in a range that does not impair the efficacy of the present invention.

The external skin preparation of the present invention is made of a lotion, cream, ointment, gel or adhesive, and the mechanism of disease improvement effect is that the pungent ingredient gives warmth to the dermis of the skin, and as a result, the blood circulation of capillaries By promoting the activation of cartilage cells in the inflammation site and the intracellular metabolism of the inflammation site, it has been shown to give a direct augmentation effect of the disease improvement effect or to increase the indirect synergy effect.

The blending amount of the pungent ingredient of the present invention is not particularly limited, but the blending amount is preferably 0.01 to 0.1% of the entire skin external preparation, and especially 0.01 to 0.05% of the formulation used in a relatively small amount of transdermal cells such as fingers, elbows and knees. It is preferable that the formulation used in a relatively large number of transdermal cells such as the head, nose and feet is 0.05 to 0.1%. If the amount of the pungent ingredient is too small, transdermal absorbency may be lowered, and if too large, skin irritation may occur.

In addition, the blending amount of the clathrate substance for the drug sustainability of the pungent component is preferably 0.1 to 10% of the entire skin external preparation.

If the blending amount of cyclodextrins, which are clathrates with respect to the spicy ingredient, is too small, the sustainability of the sufficient thermal effect is lowered. If the blending amount is too high, uniform blending of the warming substance is difficult and uniformity of the drug is inferior.

In addition, the external preparation for skin of the present invention is more effective when a small amount of a refreshing agent is added to the above-mentioned heat substance.

The refreshing agent that can be used at this time may include limonene, terpinolene, p-mentan, menthol and 0.001 ~ 0.005 parts by weight based on 0.05 ~ 0.1 parts by weight of the plant extract or the chemically synthesized spicy ingredient containing the hot component good.

The external preparation for skin of the present invention may also be prepared by adding an appropriate chemical as an optional component, depending on the dosage form. For example, in the case of liquid formulations such as ointments and lotions, solvents, oils, glycols, surfactants and water-soluble polymers can be blended as the substrate.

As the solvent, for example, water, ethanol, propyl alcohol, isopropyl alcohol, benzyl alcohol, acetone can be selected.

The oil component may be selected from, for example, lecithin, lanolin, hydrogenated oil, myristic acid, isopropyl myristin, isopropyl palmitate, squalene stearyl alcohol, oleyl alcohol and silicone oil. Among them, glycerol, propylene glycol, polyethylene glycol, polypropylene glycol can be selected and used.

As the surfactant, for example, castor oil, esters, ethers can be selected and used.

As the water-soluble high molecular compound, for example, sodium carboxymethyl cellulose, polyvinyl alcohol, methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyvinylpyrrolidone, polyacrylic acid can be used.

On the other hand, the above-mentioned high-molecular compounds may be used as the water-soluble adhesive when preparing the skin external preparation of the present invention, in addition to kaolin, bentonite, montmorillonite, titanium oxide, zinc oxide, aluminum hydroxide, silicic anhydride, etc. Alternatively, a mixture of two or more inorganic powders, propylene glycol, glycerin, sorbitol, and one or two or more moisturizing agents of sodium lactate and water may be used.

In the adhesive (so-called pars) formulation, the water-soluble adhesive is composed of a water-soluble polymer compound, an inorganic powder, and a moisturizing ratio of 1 to 2%, 0.1 to 0.2%, and 0.1 to 0.2% of the total amount of the base.

Natural rubber, synthetic isoprene rubber, polyvinyl ether, polyurethane, and polybutadiene are used as the rubber adhesive, and polyorganoshirokisan is suitable as the silicone resin adhesive.

In the case of the gel product of the present invention, a gelling agent such as carboxyvinyl polymer and glycerin monooleate is added to the component.

In any of the formulations, the external skin preparation of the present invention may have a pH of 3.0 to 8.0 and particularly preferably adjusted to 5.0 to 6.0. Too low or too high a pH can make it difficult to relieve skin irritation.

Hereinafter, the concrete configuration and operation of the present invention will be described in detail with reference to Examples and Experimental Examples, but the scope of the present invention is not limited thereto.

Example  1: present invention Blood circulation disorder  For improving disease External skin preparation  Produce

Each component was formulated at the same compounding ratio as in Table 1 to prepare the external preparations 1 to 6 of the present invention.

Skin external composition composition ratio of the present invention (unit: parts by weight) division ingredient One 2 3 4 5 6 Spicy ingredients Capsaicin 0.05 0 0 0.1 0 0.05 Capsiccoside 0 0.05 0 0 0.05 0.05 Benzyl nicotinate 0 0 0.05 0 0.05 0 Inclusion material α-cyclodextrin 0.1 0 0 10 0 2 Methylcyclodextrin 0 0.05 0 0 5 2 Hydroxyethyl-β-cyclodextrin 0 0 0.05 0 3 2 Refreshing agent Limonene 0 0.001 0 0 0 0.005 menthol 0 0 0.005 0 0 0

Example  2: present invention Blood circulation disorder  For improving disease External skin preparations  Ointment Preparation

Using the external preparation for skin in Example 1, an ointment composition 7 to 12 were obtained according to a conventional method at a compounding ratio as shown in Table 2 below.

Ointment composition ratio (unit: weight%) division ingredient 7 8 9 10 11 12 External skin preparation One 0.15 0 0 0 0 0 2 0 0.101 0 0 0 0 3 0 0 0.105 0 0 0 4 0 0 0 10.1 0 0 5 0 0 0 0 8.1 0 6 0 0 0 0 0 6.105 menstruum water Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount ethanol 7.0 7.0 7.0 7.0 7.0 7.0 oil lecithin 1.0 1.0 1.0 1.0 1.0 1.0 Squalene stearyl alcohol 0.5 0.5 0.5 0.5 0.5 0.5 Glycols glycerin 6.0 6.0 6.0 6.0 6.0 6.0 Polyethylene Glycol 20.0 20.0 20.0 20.0 20.0 20.0 Surfactants Castor oil 3.0 3.0 3.0 3.0 3.0 3.0 Water Soluble Polymer Carboxymethylcellulose sodium 5.0 5.0 5.0 5.0 5.0 5.0

Comparative example  1: ointment manufacture

It does not include the skin external preparation of Example 1, only 7.0% by weight of ethanol, 1.0% by weight of lecithin, 0.5% by weight of squalene stearyl alcohol, 6.0% by weight of glycerin, 20.0% by weight of polyethylene glycol, 3.0% by weight of castor oil, carboxy 5.0 wt% sodium methyl cellulose and the residual amount of water were combined to prepare an ointment according to a conventional method.

Example  3: present invention Blood circulation disorder  For improving disease External skin preparations  Used Clear lotion  Produce

Using the external preparation for skin, prepared in Example 1, a transparent lotion composition 13-18 was obtained according to a conventional method at a compounding ratio as shown in Table 3 below.

Transparent lotion composition composition ratio (unit: weight%) division ingredient 13 14 15 16 17 18 External skin preparation One 0.15 0 0 0 0 0 2 0 0.101 0 0 0 0 3 0 0 0.105 0 0 0 4 0 0 0 10. 0 0 5 0 0 0 0 8.1 0 6 0 0 0 0 0 6.105 menstruum water Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Benzyl alcohol 7.0 7.0 7.0 7.0 7.0 7.0 oil lanolin 1.0 1.0 1.0 1.0 1.0 1.0 Myristic acid isopropyl 0.5 0.5 0.5 0.5 0.5 0.5 Glycols Propylene glycol 6.0 6.0 6.0 6.0 6.0 6.0 Polypropylene Glycol 20.0 20.0 20.0 20.0 20.0 20.0 Surfactants Castor oil 3.0 3.0 3.0 3.0 3.0 3.0 Water Soluble Polymer Polyacrylic acid 3.0 3.0 3.0 3.0 3.0 3.0

Comparative example  2: Clear lotion  Produce

Without the external skin preparation of Example 1, only benzyl alcohol 7.0% by weight, lanolin 1.0% by weight, isopropyl myristin 0.5% by weight, propylene glycol 6.0%, polypropylene glycol 20.0% by weight, castors 3.0% by weight of oil, 5.0% by weight of polyacrylic acid and the residual amount of water were combined to prepare a transparent lotion according to a conventional method.

Example  4: present invention Blood circulation disorder  For improving disease External skin preparations  Used Cream  Produce

Using the skin external preparation prepared in Example 1, cream compositions 19 to 24 were obtained according to a conventional method at a compounding ratio as shown in Table 4 below.

Cream composition ratio (unit: parts by weight) division ingredient 19 20 21 22 23 24 External skin preparation One 0.15 0 0 0 0 0 2 0 0.101 0 0 0 0 3 0 0 0.105 0 0 0 4 0 0 0 10.1 0 0 5 0 0 0 0 8.1 0 6 0 0 0 0 0 6.105 menstruum water Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Benzyl alcohol 7.0 7.0 7.0 7.0 7.0 7.0 oil lanolin 1.0 1.0 1.0 1.0 1.0 1.0 Myristic acid isopropyl 0.5 0.5 0.5 0.5 0.5 0.5 Glycols Propylene glycol 20.0 20.0 20.0 20.0 20.0 20.0 Polypropylene Glycol 20.0 20.0 20.0 20.0 20.0 20.0 Surfactants Castor oil 3.0 3.0 3.0 3.0 3.0 3.0 Water Soluble Polymer Polyacrylic acid 7.0 7.0 7.0 7.0 7.0 7.0

Comparative example  3: Cream  Produce

Without the external skin preparation of Example 1, only benzyl alcohol 7.0% by weight, lanolin 1.0% by weight, isopropyl myristin 0.5% by weight, propylene glycol 6.0%, polypropylene glycol 20.0% by weight, castors 3.0 wt% of oil, 7.0 wt% of polyacrylic acid, and remaining water were combined to prepare a cream according to a conventional method.

Example  5: present invention Blood circulation disorder  For improving disease External skin preparations  Used Transparent gel  Produce

Using the external preparation for skin, prepared in Example 1, a transparent gel composition 25 to 30 was obtained according to a conventional method at a compounding ratio as shown in Table 5 below.

Transparent gel composition blending ratio (unit: parts by weight) division ingredient 25 26 27 28 29 30 External skin preparation One 0.15 0 0 0 0 0 2 0 0.101 0 0 0 0 3 0 0 0.105 0 0 0 4 0 0 0 10.1 0 0 5 0 0 0 0 8.0 0 6 0 0 0 0 0 6.105 menstruum water Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount ethanol 7.0 7.0 7.0 7.0 7.0 7.0 oil lecithin 1.0 1.0 1.0 1.0 1.0 1.0 Squalene stearyl alcohol 0.5 0.5 0.5 0.5 0.5 0.5 Glycols glycerin 6.0 6.0 6.0 6.0 6.0 6.0 Polyethylene Glycol 20.0 20.0 20.0 20.0 20.0 20.0 Surfactants Castor oil 3.0 3.0 3.0 3.0 3.0 3.0 Water Soluble Polymer Carboxymethylcellulose sodium 3.0 3.0 3.0 3.0 3.0 3.0 Gelling agent Carboxy Vinyl Polymer 5.0 5.0 5.0 5.0 5.0 5.0

Comparative example  4: Transparent gel  Produce

It does not include the skin external preparation of Example 1, only 7.0% by weight of ethanol, 1.0% by weight of lecithin, 0.5% by weight of squalene stearyl alcohol, 6.0% by weight of glycerin, 20.0% by weight of polyethylene glycol, 3.0% by weight of castor oil, carboxy Sodium methylcellulose 3.0% by weight, carboxyvinyl polymer 5.0% by weight and the residual amount of water was combined to prepare a transparent gel according to the usual method.

Example  6: present invention Blood circulation disorder  For improving disease External skin preparations  Manufacture of used adhesive (pas)

Using the external preparation for skin in Example 1, the adhesive compositions 31 to 36 were obtained according to a conventional method at a compounding ratio as shown in Table 6 below.

Adhesive composition compounding ratio (unit: parts by weight) division ingredient 25 26 27 28 29 30 External skin preparation One 0.15 2 0.101 3 0.105 4 10.1 5 8.1 6 6.105 Water Soluble Polymer Compound Methylcellulose 0.5 0.5 0.5 0.5 0.5 0.5 Polyacrylic acid 1.0 1.0 1.0 1.0 1.0 1.0 Inorganic powder kaoline 0.1 0.1 0.1 0.1 0.1 0.1 Titanium oxide 0.1 0.1 0.1 0.1 0.1 0.1 Moisturizer Propylene glycol 0.1 0.1 0.1 0.1 0.1 0.1 glycerin 0.05 0.05 0.05 0.05 0.05 0.05 menstruum water Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount Remaining amount

Comparative example  5: adhesive preparation

It does not include the skin external preparation of Example 1, but only 0.5% by weight of methyl cellulose, 1.0% by weight of polyacrylic acid, 0.1% by weight of kaolin, 0.1% by weight of titanium oxide, 0.1% by weight of propylene glycol, 0.05% by weight of glycerin and the balance After mixing and stirring water, the mixture was uniformly applied to 100 g / m 2 on the nonwoven fabric and faced with a polyethylene film to prepare an adhesive according to a conventional method.

Experimental Example  1: present invention Blood circulation disorder  For improving disease External skin preparations  Of the used agents Warmth  Sustained Effect Survey

In order to investigate the effect of warming on the formulations prepared above, 10 males and females in their 20s and 50s were randomly extracted, and a five-point comparative scale method (five points, feels too strong warmth; four points, strong warmth; 3) Score, feels warmth; 2 points, feels weak warmth; 1 point, feels very weak warmth; 0 points, does not feel warmth) and averaged.

The ointment, the clear lotion, the cream and the clear gel were evaluated every hour by applying 1g / 10cm2 to the knee, and the adhesive was attached every 10 cm2 to the knee. The results are shown in Tables 7 to 11 below.

Warming effect investigation result of ointment 7 8 9 10 11 12 Comparative Example 1 After 0.5 hour 2.3 2.5 2.0 2.6 2.0 2.4 0 1 hour later 3.8 3.5 3.7 3.2 3.4 3.6 0 3 hours later 4.0 4.2 4.1 4.3 3.9 4.0 0 6 hours later 2.0 2.5 2.1 2.3 2.6 2.3 0

Investigation result of warming lotion agent 13 14 15 16 17 18 Comparative Example 2 After 0.5 hour 2.0 1.9 2.3 2.2 2.3 2.4 0 1 hour later 3.6 3.4 3.5 3.6 3.7 3.4 0 3 hours later 4.0 4.3 4.0 4.1 4.3 3.9 0 6 hours later 2.9 2.0 1.9 2.3 2.2 2.4 0

Warming effect investigation result of cream 19 20 21 22 23 24 Comparative Example 3 After 0.5 hour 2.9 2.1 2.2 2.3 1.6 2.3 0 1 hour later 3.3 3.4 3.2 3.0 3.4 3.9 0 3 hours later 4.3 3.9 4.3 4.0 4.1 4.2 0 6 hours later 2.6 2.3 2.1 1.9 2.2 2.3 0

Investigation result of transparency gel agent 25 26 27 28 29 30 Comparative Example 4 After 0.5 hour 2.9 2.3 2.3 2.2 1.9 2.6 0 1 hour later 3.6 3.2 3.0 3.2 3.2 3.0 0 3 hours later 4.2 4.3 4.0 4.1 4.0 4.4 0 6 hours later 2.3 2.2 2.3 2.6 2.4 2.7 0

Warming effect investigation result of adhesive 31 32 33 34 35 36 Comparative Example 5 After 0.5 hour 2.3 2.6 2.4 2.1 2.2 2.5 0 1 hour later 3.6 3.5 3.4 3.3 3.8 3.4 0 3 hours later 4.0 4.3 4.4 4.0 4.0 4.2 0 6 hours later 2.2 2.3 2.6 2.7 2.1 1.9 0

Experimental Example  2: present invention Blood circulation disorder  For improving disease External skin preparations  Investigation of the Arthritis Improvement Effect of the Used Agents

In order to investigate the effects of arthritis treatment on the above-prepared preparations, 10 male and female patients with arthritis in their 50's and 60's were randomly extracted. Score 3, feel the effect; score 2, feel the weak effect; score 1, feel the weak effect; score 0, do not feel the effect) and averaged.

The ointment, the transparent lotion, the cream, and the transparent gel were evaluated by applying 1 g / 10 cm 2 to the knee, and the adhesive was evaluated by adhering to the knee with a width of 10 cm 2. The results are shown in Table 12 below.

Arthritis improvement effect findings division Arthritis improvement effect Ointment 7 4.0 8 3.9 9 4.5 10 3.7 11 2.9 12 3.7 Comparative Example 1 0.1 Clear lotion 13 3.5 14 4.3 15 4.0 16 2.9 17 3.5 18 3.8 Comparative Example 2 0 Cream 19 4.0 20 3.7 21 3.9 22 2.7 23 4.0 24 3.9 Comparative Example 3 0 Transparent gel 25 3.5 26 3.9 27 4.2 28 4.0 29 3.9 30 3.5 Comparative Example 4 0 Adhesive 31 4.0 32 4.1 33 3.9 34 2.8 35 3.1 36 3.5 Comparative Example 5 0.2

Through Table 12, it was confirmed that the symptoms of arthritis were significantly improved in the preparations using the skin external preparations for improving blood circulation disorders of the present invention containing the hot component.

Experimental Example  3: present invention Blood circulation disorder  For improving disease External skin preparations  Investigation of Rhinitis Improvement Effect

In order to investigate the effects of arthritis treatment on the preparations above, 10 random male and female patients in their 20s and 50s were randomly extracted and 5 point comparative scale method (5 points, very strong effect; 4 points, strong effect) Score 3, feel the effect; score 2, feel the weak effect; score 1, feel the weak effect; score 0, do not feel the effect) and averaged.

The ointment, the transparent lotion, the cream, and the transparent gel were evaluated by applying 1 g / 10 cm 2 to the nose and the like, and the adhesive was evaluated by attaching the nose to the width of 5 cm 2. The results are shown in Table 13 below.

Rhinitis improvement effect findings division Rhinitis improvement effect Ointment 7 4.2 8 3.5 9 4.0 10 3.6 11 3.0 12 3.5 Comparative Example 1 0 Clear lotion 13 3.9 14 4.0 15 4.1 16 3.9 17 3.8 18 3.9 Comparative Example 2 0 Cream 19 4.2 20 4.0 21 3.7 22 3.5 23 4.4 24 4.0 Comparative Example 3 0 Transparent gel 25 3.9 26 3.7 27 4.0 28 4.1 29 4.0 30 3.8 Comparative Example 4 0 Adhesive 31 3.9 32 4.0 33 3.7 34 4.0 35 3.2 36 3.0 Comparative Example 5 0

Through Table 13, it was confirmed that the symptoms of rhinitis are significantly improved in the preparations using the skin external preparations for improving blood circulation disorders of the present invention containing the hot component.

As described in detail through the above Examples and Experimental Examples, the present invention relates to a skin external preparation for improving blood circulation disorders, preparations for the preparation of a skin external preparation mainly based on the pungent ingredient and can be applied or adhered to the skin It is a very useful invention in the pharmaceutical industry, because it has an excellent effect of providing a formulation having excellent efficacy in the improvement of various blood circulation disorder diseases by manufacturing.

Claims (3)

A skin external preparation for improving the thermosensitizing effect, arthritis and rhinitis, wherein any one or a mixture of mexicoside and benzyl nicotinate and dextrin are mixed in a blending ratio of 0.05 to 0.1: 0.1 to 10. The external preparation for skin according to claim 1, further comprising 0.001 to 0.005 parts by weight of a refreshing agent with respect to 0.05 to 0.1 parts by weight of the hot component. delete