JP2012206961A - Antibacterial agent and skin external preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a plant extract containing formulation which exhibits antibacterial activity to at least causative bacteria of skin inflammation.SOLUTION: An antibacterial agent and a skin external preparation contain an extract of Truenicorn as an active ingredient.

Description

  The present invention relates to an antibacterial agent and a skin external preparation.

Acne bacteria ( Propionibacterium acnes ) and staphylococci (Bacteria belonging to the genus Staphylococcus ) are known as skin resident bacteria, but are also deeply involved in skin inflammation.
Acne bacteria play a role in suppressing the invasion and propagation of pathogenic bacteria by degrading sebum into glycerin and fatty acids and keeping the skin weakly acidic, but if sebum continues to clog the pores, Acne bacteria proliferate as nutrition, and this triggers inflammation such as acne. Acne bacteria are known to produce porphyrins, and these porphyrins are also thought to be involved in acne deterioration.
On the other hand, staphylococci are present in human skin and intestines and are usually harmless. However, highly toxic substances such as Staphylococcus aureus are also known as causative bacteria such as suppuration and jumping of the wound, and enter the body through the wound to cause meningitis, pneumonia, peritonitis, sepsis, etc. May cause.

  In order to prevent and improve skin inflammation, it is important to effectively control the growth of pathogenic bacteria, and the development of a new drug useful for maintaining and improving skin health has been desired.

  An object of the present invention is to provide a plant extract-containing preparation that exhibits antibacterial activity at least against causative bacteria of dermatitis.

The present inventors have intensively studied in view of the above problems. As a result, it was found that an extract of unicorn ( True unicorn ) has antibacterial activity against germs causing dermatitis. The present invention has been completed based on this finding.

The present invention relates to an antibacterial agent and an external preparation for skin containing an extract of unicorn ( True unicorn ) as an active ingredient.

  The antibacterial agent and the external preparation for skin of the present invention exhibit excellent antibacterial activity against causative bacteria such as acne and staphylococci.

Hereinafter, the present invention will be described in detail based on preferred embodiments thereof.
Unicorn ( True unicorn ) is a plant belonging to the lily family Sokushinran.
Unicorn extract is known to exhibit physiological activities such as promotion of gastric mucus secretion, uterine tonicity, and uterine analgesia, and these physiological activities are attributed to the estrogenic action of diosgenin, a type of steroidal glycoside. It is considered. Unicorn extract has a track record of use as a supplement component and is excellent in safety.

The unicorn extract used in the present invention can be extracted from any part of the unicorn, for example, root, stem, whole grass, leaf, flower, etc., but it is preferable to extract from the root and underground part or stem.
In the preparation of the unicorn extract, each of the above parts can be used as it is or after dry pulverization, and these steam distillates or squeezed products may be used. Moreover, you may use what refine | purified these with essential oil etc. The unicorn extract used in the present invention may be an extract of any one of the above parts, or may be an extract from two or more parts. As the unicorn extract used in the present invention, a rhizome extract can be suitably used.

In the present invention, the method for obtaining the unicorn extract is not particularly limited, and a normal extraction method can be employed.
There is no restriction | limiting in particular in the solvent used for extraction, The solvent normally used for extraction of a plant component can be used. Examples of such solvents include water; alcohols such as methanol, ethanol, propanol, and butanol; polyhydric alcohols such as propylene glycol and butylene glycol; ketones such as acetone and methyl ethyl ketone; esters such as methyl acetate and ethyl acetate. Chain and cyclic ethers such as tetrahydrofuran and diethyl ether; Halogenated hydrocarbons such as dichloromethane, chloroform and dichloroethane; Hydrocarbons such as squalane, hexane, cyclohexane and petroleum ether; Aromatic hydrocarbons such as toluene Polyethers such as polyethylene glycol; and pyridines can be used, and a mixture of two or more of these can be used, but it is preferable to use a solvent containing an aqueous alcohol, and a solvent containing ethanol. It can be used to apply. The solvent containing ethanol is preferably an ethanol aqueous solution, preferably an ethanol aqueous solution having a concentration of 20 to 80% by mass, more preferably 30 to 70% by mass.

Further, normal conditions can be applied as the extraction conditions. For example, the specific part of the unicorn as the extraction raw material is preferably 0 to 100 ° C, more preferably 5 to 60 ° C, still more preferably 10 to 30 ° C, preferably 1 hour to 3 weeks, more preferably Can be obtained by immersing or heating to reflux in the above solvent for about 5 hours to 1 week.
The unicorn extract used in the present invention may be a unicorn extract obtained as described above, or a fraction obtained by further fractionating the unicorn extract by appropriate separation means such as column chromatography or precision distillation. May be minutes. Moreover, what diluted or concentrated the said extract and the said fraction may be used, and after drying the said extract and the said fraction by freeze-drying etc., it may be made into the powder or the paste form.
Moreover, a commercial item can also be used as a unicorn extract in this invention.

  The antibacterial agent and the external preparation for skin of the present invention may be the unicorn extract itself or may further contain other components. Examples of other ingredients include titanium oxide, calcium carbonate, purified water, lactose, starch, alcohol, surfactant, oily substance, moisturizer, skin anti-aging agent, whitening agent, polymer compound, preservative, thickener , Emulsifiers, medicinal ingredients, powders, ultraviolet absorbers, dyes, fragrances, emulsion stabilizers, pH adjusters and the like. Although there is no restriction | limiting in particular in content of the unicorn extract in the antibacterial agent and skin external preparation of this invention, It is preferable that it is 0.001-20 mass% in conversion of solid content, and is 0.005-10 mass%. It is more preferable.

  The antibacterial agent and external preparation for skin of the present invention exhibit excellent antibacterial activity against gram-positive bacteria, and can exhibit antibacterial activity against, for example, acne bacteria and staphylococci. The above “antibacterial” includes both concepts of inhibiting the growth of bacteria and killing the bacteria. The antibacterial agent and the external preparation for skin of the present invention can be suitably used as an antibacterial agent that acts on acne bacteria, staphylococci and the like which are causative bacteria of dermatitis. Examples of staphylococci that cause dermatitis include Staphylococcus aureus.

Antibacterial agents of the present invention can be pharmaceuticals, quasi drugs and cosmetics. There is no restriction | limiting in particular in the form of the antibacterial agent of this invention, According to a use, it can take forms, such as an external preparation for skin, an oral preparation, an injection, a nasal drop, a suppository, an instillation, an eye drop.
In the form of an external preparation for skin, a wide range such as aqueous solution, solubilization system, emulsification system, powder system, gel system, ointment system, cream, mist, aerosol, water-oil two-layer system, water-oil-powder three-layer system Can take form. In addition, examples of product forms in the form of external preparation for skin include facial cosmetics such as body cosmetics, lotions, emulsions, creams and packs, foundations, funny, blushers, lipsticks, eye shadows, eyeliners, mascaras, sunscreens, etc. Makeup cosmetics, makeup removers, skin cleansers such as facial cleansers and body shampoos, hair cosmetics such as hair rinses and shampoos, bath preparations, ointments, controlled release patches, patches, oil blotting paper, aromatic cosmetics, etc. Is mentioned.
Examples of oral dosage forms include tablets, granules, fine granules, powders, capsules, chewables, pellets, syrups, solutions, suspensions and inhalants.
The antibacterial agent of the present invention uses a unicorn extract as an antibacterial component and exhibits an antibacterial action against acne bacteria and staphylococci, which are inflammatory causes of dermatitis. This antibacterial action can prevent symptoms of dermatitis such as acne and suppuration, and can alleviate and improve these dermatitis.

The external preparation for skin of the present invention can be a pharmaceutical, a quasi-drug, and a cosmetic. There is no restriction | limiting in particular in the form of the skin external preparation of this invention, Aqueous solution type | system | group, solubilization type | system | group, emulsification type | system | group, powder type | system | group, gel type | system | group, ointment type | system | group, cream, mist, aerosol, water-oil two layer system, water-oil- It can take a wide variety of forms such as a powder three-layer system. In addition, the product form of the external preparation for skin of the present invention is also arbitrary, for example, facial cosmetics such as body cosmetics, lotions, emulsions, creams and packs, foundations, funny, blushers, lipsticks, eye shadows, eyeliners, Makeup cosmetics such as mascara and sunscreen, makeup remover, skin cleansers such as facial cleansers and body shampoos, hair cosmetics such as hair rinses and shampoos, bath preparations, ointments, controlled release patches, patches, oil blotting paper And aromatic cosmetics.
The topical skin preparation of the present invention uses a unicorn extract as an active ingredient (antibacterial ingredient) and exhibits an antibacterial action against acne bacteria and staphylococci, which are inflammatory causes of dermatitis. This antibacterial action can prevent symptoms of dermatitis such as acne and suppuration, and can alleviate and improve these dermatitis.

The amount of the external preparation for skin use of the present invention varies depending on the content of the unicorn extract, which is an active ingredient. For example, in the case of cream, ointment and liquid preparations, 0.001 to 20 mg per 1 cm ^{2 of} skin surface is used. Is preferred.

  EXAMPLES Hereinafter, although this invention is demonstrated further in detail based on an Example, this invention is not limited to this.

Production Example Preparation of Unicorn Extract 160.83 g of a unicorn rhizome pulverized product (obtained from Monteagle Herbs) was immersed in 800 mL of a 50% by mass aqueous ethanol solution for 3 days. The filtrate obtained by filtering this immersion liquid was concentrated using a rotary evaporator to obtain 11.82 g of a solid content. What dissolved this solid content in ethanol so that it might become a density | concentration of 10 mg / mL was used for the following test example as a unicorn extract.

Test Example Antibacterial Test Using the unicorn extract prepared in the above production example, antibacterial activity against acne bacteria was evaluated. Antibacterial activity was evaluated using a commercially available kit (trade name: BacTiter-Glo ^™ Microbial Cell Viability Assay, manufactured by Promega) for quantifying the amount of ATP using luciferase.
Specifically, 10 μL of Propionibacterium acnes JCM6425 strain cultured for 3 days at 37 ° C. using modified GAM medium (manufactured by Nissui Pharmaceutical Co., Ltd.), modified GAM medium 80 μL, and the above Unicorn extract (10 μL) was mixed in a well of a 96-well plate and anaerobically cultured at 37 ° C. for 20 hours. The concentration of the unicorn extract in this culture solution is 1 mg / mL. After incubation, 100 μL of BacTiter-Glo ^™ reagent was added to the wells, and the fluorescence intensity (excitation light: 488 nm) at 530 nm was quantified using a 1420 Multilabel Counter (manufactured by Wallac).
A similar test was conducted using a system in which ethanol was mixed instead of the unicorn extract as a negative control. In addition, a similar test was performed using a mixture of minocycline mixed at a concentration of 1 mg / mL instead of the unicorn extract as a positive control. This minocycline is a tetracycline antibiotic and is used as a therapeutic agent for acne and skin infections.
The results are shown in Table 1.

  As shown in Table 1, in the system in which the unicorn extract was present, the fluorescence intensity was lower than that of the negative control, and the growth of acne bacteria was remarkably suppressed. This growth inhibitory effect is about 5 times higher than that of the positive control, indicating that the unicorn extract is excellent in antibacterial activity.

(Prescription example)
As examples of the form of the external preparation for skin of the present invention, lotions, creams and ointments having the compositions shown below were prepared by ordinary methods.

1. Preparation of lotion A lotion having the following composition was prepared by a conventional method.
(Composition) (Composition: Mass%)
Unicorn extract 1
Glycerin 10
1,3-Butylene glycol 6
Citric acid 0.1
Sodium citrate 0.3
Ethyl alcohol 8
Polyoxyethylene hydrogenated castor oil (60EO) 0.5
Perfume
Water remaining
Total 100

2. Preparation of cream A cream having the following composition was prepared by a conventional method.
(Composition) (Composition: Mass%)
Unicorn extract 2
Monostearic glyceride 2
Polyoxyethylene sorbitan monolaurate (20EO) 2
Cetanol 7
Squalene 40
Propylene glycol 10
Liquid paraffin 10
Perfume
Water remaining
Total 100

3. Preparation of ointment An ointment having the following composition was prepared by a conventional method.
(Composition) (Composition: Mass%)
Unicorn extract 2
Sara beeswax 11
Liquid paraffin 22
Lanolin 10
Polysorbate 80 2
Olive oil 15
Preservative appropriate amount
Water remaining
Total 100

Claims (2)

An antibacterial agent containing an extract of unicorn ( true unicorn ) as an active ingredient. An external preparation for skin containing an extract of Unicorn ( True unicorn ) as an active ingredient.