JP2007230965A - Myocyte activator - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a means activating myocyte and to provide a means for applying the same in cosmetic or pharmaceutical field. <P>SOLUTION: The inventors found that an extract of Azuki beans (Vigna angularis (Willd) Ohwi et Ohashi) has the myocyte activating potential, and prepared a skin preparation for external use, a pharmaceutical for internal use or an injection agent by using the myocyte activator comprising the extract as an active component. Various efficacies on muscles are expected in combination of the use of the activator with muscle training. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention is an invention relating to a muscle cell activator that mainly takes the form of an external preparation for skin.

  Body muscle activity is usually not so conscious unless you exercise specifically. However, in fact, it is indispensable for human life, and when its function is reduced or inhibited by aging, trauma, etc., the importance is often reaffirmed.

  For example, considering this muscle activity for the face, there is a muscle on the face that moves the skin called facial muscles and is involved in the creation of facial expressions. It is thought that facial expression becomes poor and sagging occurs on the facial skin. The sagging of the facial skin is one of the major cosmetic problems. Conventionally, various cosmetic treatments such as massage have been performed, but no significant effect has been reported so far. In addition, the eyelids are opened and closed by the facial muscles such as the ocular muscles, the upper levator oculi muscles, the lower eyelid muscles, and the frontal muscles. It is thought to be. Making the eyes wide open is one of the main purposes of makeup, but in the past, makeup has been dealt with apparently.

Patent Document 1 below describes a facial electrical stimulation device for eliminating sagging of facial skin, etc., and Patent Document 2 mainly produces myocyte ATP production containing yeast extract for external use as an active ingredient. Accelerators are described.
Japanese Patent Laid-Open No. 2003-229884 JP 2001-10947 A

  An object of the present invention is to provide means for activating muscle cells and utilizing them in the field of beauty or medicine.

  As a result of intensive studies aimed at solving the above-mentioned problems, the present inventor found that the azuki bean extract has a desired excellent myocyte activation activity, and completed the present invention.

  That is, the present invention provides a muscle cell activator (hereinafter also referred to as “this drug”) containing azuki bean extract.

  This agent is an agent that activates muscle cells in the vicinity of the skin region, mainly by use on the skin.

  In the present invention, “muscle activation” means that the metabolic activity of muscle is improved, and this activation increases muscle mass, improves recovery efficiency of muscle damage, The effect by improving the metabolic activity of muscles, such as promotion of fat burning, becomes obvious.

  The azuki bean extract, which is an essential component of this agent, is a seed powder of azuki bean (Vigna angularis (Willd) Ohwi et Ohashi) or an extract thereof. Azuki seed powder is literally a powder obtained by physically pulverizing azuki bean seed (an example of a commercial product is Azuki powder (Ogi Pharmaceutical)). The extract of adzuki seed powder is an extract obtained by extracting the seed with an aqueous solvent such as water, a mixture of water and 1,3-butylene glycol, or a mixture of water and propylene glycol (commercially available). Examples of products include HP azuki bean extract and HB azuki bean extract (Yamamoto Fragrance / Cosmetchem).

  The present invention provides means for activating muscle cells and utilizing them in the field of beauty or medicine.

  The agent can be used as it is as a dried product of azuki bean extract, but can also be used in various modes. Below, the typical form using this agent is described.

(1) External composition An external composition is a composition mainly used with respect to a human epidermis. The most commonly used site is the face, but the entire body (leg, arm, neck, torso, scalp, etc.) can be the target. Further, in the face, the area around the eyes is one of the parts where the effects of the present invention can be exhibited most remarkably. The classification of the composition for external use according to the Pharmaceutical Affairs Law may be any of cosmetics, quasi-drugs, and pharmaceuticals.

The blending amount when this agent is used in a composition for external use varies depending on the specific aspect (dosage form, type of product, etc.) of the target composition for external use, and can be freely selected. In general, it is preferably blended in the range of 10 ⁻⁶ to 10% by mass in terms of solid content of azuki bean extract, and generally in the range of 10 ⁻⁴ to 1% by mass. It is particularly preferable that the blending is within the range of 10 ⁻³ to 10 ⁻² mass%. If this blending amount is less than 10 ⁻⁶ mass%, a sufficient myocyte activation effect is not exhibited, and even if the blending amount exceeds 10 mass%, the myocyte activation effect corresponding to the increase in the blending amount is achieved. There is a tendency that improvement is not recognized.

  The dosage form of the composition for external use in which this agent is blended is not particularly limited, but since the azuki bean extract, which is an essential component of this agent, is a water-soluble component, it is preferably a dosage form having at least an aqueous phase portion. It is. Specific examples include liquid agents, emulsions, creams, ointments, haptic agents, pack agents, gels, solubilizers, two-layer agents, three-layer agents, soaps, and the like. Also, it is one of preferred embodiments to be blended into a powder such as powdery foundation. Furthermore, it is also possible to mix | blend with an oil agent.

  In the composition for external use to which this agent is blended, the components usually used in the composition for external use of each aspect are preferably blended according to the purpose and dosage form, preferably so as not to impair the muscle cell activation effect of this agent can do.

  For example, oily raw materials such as fats and oils (liquid fats and oils, solid fats and oils), waxes, hydrocarbon oils, higher fatty acids, higher alcohols, ester oils, silicone oils; anionic surfactants, cationic surfactants, amphoteric surfactants, Surfactants such as nonionic surfactants, polymer surfactants, natural surfactants; polymer compounds such as thickener polymers, coating agent polymers; organic synthetic dyes (dyes, lakes, organic pigments), Colorants such as natural pigments, inorganic pigments (external pigments, colored pigments), pearlescent pigments, polymer powders, functional pigments; UV screening agents (UV absorbers, UV blocking agents); sequestering agents, fragrances, Mention may be made of cosmetic base materials such as water, lower alcohols and preservatives.

  In addition, various skin drugs (whitening agents, anti-wrinkle agents, skin roughening agents, antibacterial agents, various medicinal components derived from animals, plants and microorganisms, etc.) other than this agent can be added as necessary. .

  For example, by blending this agent into an external composition and using it on the skin, it is possible to activate muscle cells in the vicinity of the skin region using the external composition. Thereby, the sagging of the skin in the said skin area | region can be improved by activating a myocyte.

  Further, for example, by using this agent for muscle atrophy due to nonuse, it is possible to promote the recovery of muscle mass by activating the muscles in the part. Further, by using this agent on the skin in the vicinity of a muscle injury site, recovery from a disease accompanied by muscle damage can be promoted by activating myocytes in the injury site.

  One suitable use site of the agent is the face. By applying this agent to the face, sagging of the face can be reduced by activating myocytes in the applied part. Furthermore, the most suitable part in the face is a skin region around the eyes. That is, by applying this agent around the eyes, the amount of muscles such as the ocular muscles, the upper levator ani muscle, the lower eyelid muscles, and the like described above increases, and the width of the eye increases. It is possible to realize a “perfect” state.

  In parallel with the use of this agent, the purpose of use of this agent can be achieved more effectively by training the part that activates myocytes (internal composition and injectable composition described later) The same applies to objects).

  For example, in the case of increasing the amount of muscle atrophy due to nonuse with this agent, it is effective to perform appropriate rehabilitation exercises and strength training in parallel with the use of this agent.

  In addition, when this agent is used to activate facial muscle cells to reduce facial sagging or increase the width of eye opening, the facial movement is voluntarily performed by appropriate facial stretching exercises. By moving the muscles, the beauty effect of this drug can be further enhanced. As described above, in an aspect in which the present agent is used for cosmetic purposes, it is effective to provide the user with a facial motion manual, a DVD or video recording a moving image, and the like together with the present agent.

(2) Internal Composition By blending this preparation into an internal composition and taking it, muscle cells can be activated from the inside of the body and used for various rehabilitations and the like.

  As the simplest internal use composition, the form which takes the water (hot water) extract of azuki bean as it is can be illustrated (leaching agent). Moreover, it can be used as an extract obtained by concentrating the leaching agent. Furthermore, it is possible to mix this agent with powders, granules, fine granules, tablets, capsules, pills, emulsions, suspensions, liquids, spirits, syrups and the like. When this agent is blended with the internal composition, the blending amount is generally in the range of 0.01 to 80.0% by mass in terms of the solid content of azuki bean extract with respect to the composition. Preferably, it mix | blends in the range of 1.0-10.0 mass%. The dosage of this drug is preferably about 10 mg to 10 g per day in terms of solid content of azuki bean extract, and is usually taken about 1 to 5 times a day.

  In the composition for internal use to which this agent is blended, the components usually used in the composition for internal use of each embodiment are preferably used according to the purpose and dosage form so that the effect of activating the muscle cell of this agent is not impaired Can be blended.

  For example, examples of the basic agent include solvents such as purified water, ethanol, simple syrup, and vegetable oil; excipients such as lactose, sucrose, starch, dextrin, crystalline cellulose, talc, and titanium oxide. Furthermore, examples of the adjuvant include additives such as a solubilizer, an emulsifier, a suspending agent, a thickener, a plasticizer, a binder, a disintegrant, a lubricant, and a moisturizer. Moreover, a stabilizer, a preservative, a sweetener, a flavoring agent, a fragrance, a coloring agent, etc. can be illustrated.

(3) Injectable composition This preparation is formulated into an injectable composition, and this is administered into a tissue at a location where muscle cells are to be activated, for example, at a location where muscle atrophy has occurred. The rehabilitation effect can be improved by activating a part of myocytes. The blending amount when this agent is blended with an injectable composition is generally blended in the range of 10 ⁻⁴ to 10 ⁻¹ mass% in terms of solid content of azuki bean extract, and is generally blended with the composition. Preferably, it mix | blends in the range of 10 ^{< -3} > -10 ^<-2> mass%. In addition, the amount of this agent injected into the living body is preferably about 1 μg to 10 μg per day in terms of solid content of azuki bean extract, and is preferably injected once a day.

  In the injectable composition to which this agent is blended, the components usually used in the injectable composition of each aspect are blended according to the purpose, preferably so as not to impair the myocyte activation effect of this agent be able to.

  For example, distilled water for injection, buffer, isotonic agent, stabilizer, soothing agent, preservative, and the like can be used as the normal component.

  In addition, although the composition for injection can be used also as a liquid agent, it can also be made into a preparation type at the time of use.

  Hereinafter, the present invention will be described more specifically by way of examples. However, the present invention is not limited to these examples. In addition, unless otherwise indicated, the compounding quantity in the column of this Example is the mass% with respect to the compounding object. Moreover, unless otherwise indicated, the mass of azuki bean extract is displayed as a dry mass.

[Test Example] Myocyte Activation Test Human myofibroblasts (C2C12 cells) (Dainippon Pharmaceutical Co., Ltd.) were seeded on a plate with DMEM containing 10% FBS and cultured at 37 ° C. and 5% CO ² . After cell colonization, replace with low serum medium (DMEM containing 0.1% FBS). After 12 hours under the same culture conditions, add Alamar Blue to each plate to measure the respiratory activity of the test drug and cells. Further, the culture was further performed under the same conditions for 3 hours. After completion of this culture, the fluorescence of each plate was quantified with a plate reader. The results are shown in FIG. Compared to the control group to which no drug was added, azuki bean extract [Azuki powder (Oshiro Pharmaceutical Co., Ltd .: also used as “Azuki bean extract” in the following prescription example) is 10 ⁻⁵ (E-5) to 10 ⁻³ (E-3) In the case of adding mass%, it was found that muscle cells were activated with a significant difference particularly at 10 ⁻³ mass%. Instead of Azuki bean extract, hydrangea nozzle extract ^[10-2 wt%] obtained by a conventional method is activation of 99.1% of the muscle cells to the control, the Tougashiekisu ^[10-2 mass %] Was 102.5% activation of myocytes relative to the control, suggesting that the activation effect of myocytes is an effect unique to the azuki bean extract.

The formulation example of this invention is described below.
[Prescription Example 1-1] Emulsion (1)
Blending amount (% by mass)
Stearic acid 6.0
Sorbitan monostearate ester 2.0
Polyoxyethylene (20 mol)
Sorbitan monostearate 1.5
2- (2′-hydroxy-5′-methylphenyl)
Benzotriazole 8.0
Propylene glycol 10.0
Azuki end 1.0
Preservative / Antioxidant Appropriate amount Fragrance Appropriate amount Purified water remaining amount

<Production method>
Propylene glycol was added to purified water and heated to maintain 70 ° C. (aqueous phase). On the other hand, other components were mixed, heated and melted, and kept at 70 ° C. (oil phase). The oil phase was added to the aqueous phase with stirring to perform preliminary emulsification. Next, the emulsified particles of the system were made fine and uniform with a homomixer, and then rapidly cooled with good stirring to obtain an emulsion.

[Prescription Example 1-2] Emulsion (2)
Blending amount (% by mass)
Stearic acid 6.0
Sorbitan monostearate ester 2.0
Polyoxyethylene (20 mol)
Sorbitan monostearate 1.5
2- (2′-hydroxy-5′-methylphenyl)
Benzotriazole 8.0
Propylene glycol 10.0
Azuki end 0.1
Preservative / Antioxidant Appropriate amount Fragrance Appropriate amount Purified water remaining amount

<Production method>
Prepared in the same manner as in Formulation Example 1-1.

[Prescription Example 2-1] Cream (1)
Blending amount (% by mass)
Polyoxyethylene (20 mol)
Cetyl alcohol ether 1.0
Methylphenyl polysiloxane (20cs) 2.0
Liquid paraffin 3.0
2-Hydroxy-4-methoxybenzophenone 5.0
Azuki end 0.0001
Propylene glycol 5.0
Glycerin 2.0
Ethyl alcohol 15.0
Carboxyvinyl polymer 0.3
Hydroxypropyl cellulose 0.1
2-Aminomethylpropanol 0.1
Preservative Appropriate amount Fragrance Appropriate amount Purified water Appropriate amount

<Production method>
Propylene glycol was added to purified water and heated to maintain 70 ° C. (aqueous phase). On the other hand, other components were mixed, heated and melted, and kept at 70 ° C. (oil phase). The oil phase was added to the aqueous phase with stirring to perform preliminary emulsification. Next, the emulsified particles of the system were made fine and uniform with a homomixer, and then rapidly cooled with good stirring to obtain a cream.

[Prescription Example 2-2] Cream (2)
Blending amount (% by mass)
Polyoxyethylene (20 mol)
Cetyl alcohol ether 1.0
Methylphenyl polysiloxane (20cs) 2.0
Liquid paraffin 3.0
2-Hydroxy-4-methoxybenzophenone 5.0
Azuki end 0.001
Propylene glycol 5.0
Glycerin 2.0
Ethyl alcohol 15.0
Carboxyvinyl polymer 0.3
Hydroxypropyl cellulose 0.1
2-Aminomethylpropanol 0.1
Preservative Appropriate amount Fragrance Appropriate amount Purified water Appropriate amount

<Production method>
Prepared in the same manner as in Formulation Example 2-1.

[Prescription Example 3-1] Emulsified makeup base (W / O emulsified type) (1)
Blending amount (% by mass)
Organically modified montmorillonite 0.5
Cetyl isooctanoate 2.0
Octamethylcyclotetrasiloxane 2.0
Decamethylcyclopentasiloxane 5.0
Dimethylpolysiloxane (6cs) 5.0
Liquid paraffin 3.0
Dioctadecyldimethylammonium chloride 0.2
Polyoxyalkylene-modified organopolysiloxane 5.0
4-tert-Butyl-4'-methoxydibenzoylmethane 0.3
Glyceryl mono-2-ethylhexanoyl
Diparamethoxycinnamate 1.0
Fine particle titanium oxide 5.0
Oleyl alcohol 0.5
Stearic acid 0.5
Sorbitan diisostearate 4.0
Antioxidant appropriate amount perfume appropriate amount Talc 1.5
Nylon powder 1.0
Purified water Residual amount Sodium citrate 0.5
1,3-butylene glycol 5.0
Azuki end 0.0001

<Production method>
Sodium citrate, 1,3-butylene glycol, saikosaponin b2 and an antioxidant were added to purified water, and the mixture was heated and stirred at 70 ° C. (aqueous phase). Finely divided titanium oxide, talc and nylon powder were sufficiently mixed and pulverized (powder part). The other components were mixed, heated and melted and kept at 70 ° C. (oil phase). Add powder to the aqueous phase and add 70
Homomixer treatment at 0 ° C. Further, an oil phase was added, and the emulsified particles were finely homogenized with a homomixer, and then rapidly cooled with stirring to obtain an emulsified cosmetic base.

[Prescription Example 3-2] Emulsion type makeup base (W / O emulsion type) (2)
Blending amount (% by mass)
Organically modified montmorillonite 0.5
Cetyl isooctanoate 2.0
Octamethylcyclotetrasiloxane 2.0
Decamethylcyclopentasiloxane 5.0
Dimethylpolysiloxane (6cs) 5.0
Liquid paraffin 3.0
Dioctadecyldimethylammonium chloride 0.2
Polyoxyalkylene-modified organopolysiloxane 5.0
4-tert-Butyl-4'-methoxydibenzoylmethane 0.3
Glyceryl mono-2-ethylhexanoyl
Diparamethoxycinnamate 1.0
Fine particle titanium oxide 5.0
Oleyl alcohol 0.5
Stearic acid 0.5
Sorbitan diisostearate 4.0
Antioxidant appropriate amount perfume appropriate amount Talc 1.5
Nylon powder 1.0
Purified water Residual amount Sodium citrate 0.5
1,3-butylene glycol 5.0
Azuki end 0.01

<Production method>
Prepared in the same manner as in Formulation Example 3-1.

[Prescription Example 4-1] Powdery Foundation (1)
Blending amount (% by mass)
Fine particle titanium oxide 7.0
Talc 40.0
Mica remaining amount nylon powder 10.0
Red iron oxide 1.0
Yellow iron oxide 2.0
Black iron oxide 0.2
Dimethylpolysiloxane 1.0
2-ethylhexyl palmitate 9.0
Sorbitan sesquioleate 1.0
N, N-dimethyl PABA octyl ester 0.3
Azuki end 0.00001
Preservative Appropriate amount Antioxidant Appropriate amount Fragrance Appropriate amount

<Production method>
Fine particles of titanium oxide, talc, mica, nylon powder, red iron oxide, yellow iron oxide, black iron oxide, and psychogenin A were sufficiently pulverized and mixed in a blender (powder part). Dimethylpolysiloxane, 2-ethylhexyl palmitate, sorbitan sesquioleate, N, N-dimethyl PABA octyl ester, preservative and antioxidant were added to the powder part, and then the perfume was sprayed and mixed uniformly. This was pulverized with a pulverizer, filled in a container and molded to obtain a powdery foundation.

[Prescription Example 4-2] Powder Foundation (2)
Blending amount (% by mass)
Fine particle titanium oxide 7.0
Talc 40.0
Mica remaining amount nylon powder 10.0
Red iron oxide 1.0
Yellow iron oxide 2.0
Black iron oxide 0.2
Dimethylpolysiloxane 1.0
2-ethylhexyl palmitate 9.0
Sorbitan sesquioleate 1.0
N, N-dimethyl PABA octyl ester 0.3
Azuki end 0.1
Preservative Appropriate amount Antioxidant Appropriate amount Fragrance Appropriate amount

<Production method>
Prepared in the same manner as in Formulation Example 4-1.

[Prescription Example 5-1] Oily foundation (1)
Blending amount (% by mass)
Fine particle titanium oxide 10.0
Mica 22.4
Kaolin 10.0
Nylon powder 5.0
Red iron oxide 0.5
Yellow iron oxide 0.5
Black iron oxide 0.1
Liquid paraffin remaining amount Dimethylpolysiloxane 10.0
Sorbitan sesquioleate 2.0
Octyl methoxycinnamate 5.0
Azuki end 0.001
Perfume Appropriate amount Microcrystalline wax 6.0
Carnauba Arrow 3.0

<Production method>
Fine particles of titanium oxide, mica, kaolin, nylon powder, red iron oxide, yellow iron oxide and black iron oxide were thoroughly mixed and ground in a blender (powder part). Components other than the fragrance were mixed and heated and melted at 85 ° C. (oil phase). The powder was added to this oil phase with stirring. Next, add fragrance and thoroughly disperse, then fill this into a container.
Molded to obtain an oily foundation.

[Prescription Example 5-2] Oily foundation (2)
Blending amount (% by mass)
Fine particle titanium oxide 10.0
Mica 22.4
Kaolin 10.0
Nylon powder 5.0
Red iron oxide 0.5
Yellow iron oxide 2.0
Black iron oxide 0.1
Liquid paraffin remaining amount Dimethylpolysiloxane 10.0
Sorbitan sesquioleate 2.0
Octyl methoxycinnamate 5.0
Azuki end 0.0001
Perfume Appropriate amount Microcrystalline wax 6.0
Carnauba Arrow 3.0

<Production method>
Prepared in the same manner as in Formulation Example 5-1.

[Prescription Example 6] PVA pack
Blending amount (% by mass)
Ethanol 10.0
1,3-butylene glycol 6.0
Polyethylene glycol 4000 2.0
Olive oil 1.0
Macadamia nut oil 1.0
Phytosteryl hydroxystearate 0.05
Lactic acid 0.05
Sodium lactate 0.1
L-ascorbic acid sulfate disodium 0.1
α-Tocopherol 2-L-ascorbic acid phosphate diester potassium
0.1
Vitamin E acetate 0.1
Fish Collage 0.1
Chondroitin thorium sulfate 0.1
Sodium carboxymethylcellulose 0.2
Polyvinyl alcohol 12.0
Azuki end 0.01
Paraoxybenzoic acid ester Appropriate amount Purified water Residual fragrance Appropriate amount

<Production method>
Manufactured in a conventional manner.

It is drawing which showed the relationship between the density | concentration of the used azuki bean extract, and activation of a myocyte.

Claims (5)

A muscle cell activator containing azuki bean extract. The muscle cell activation agent according to claim 1, wherein the muscle cell activation agent is an agent that activates muscle cells in the vicinity of the skin region when used on the skin. The muscle cell activation agent according to claim 2, wherein the muscle cell activation agent is an agent that activates muscle cells in the vicinity of the skin region when used on the skin to improve sagging of the skin. Agent. 4. The muscle cell activator according to claim 2 or 3, wherein in the muscle cell activator, a skin region using the agent is a skin region around the eye. The width of the eye opening is increased by applying the muscle cell activator according to claim 3 to the skin area around the eye and stretching the eye area around the main training area. A beauty method.