JPS63179812A - External preparation for skin - Google Patents

Abstract

PURPOSE:To obtain a remedy for skin diseases specifically showing inhibitory action on sebum secretion and mild effects on soborrhoeic dermatitis such as skin diseases caused by excess secretion of sebum without affecting other organs, containing an extract of propolis as an active ingredient. CONSTITUTION:A remedy for skin diseases containing >=about 0.001wt.%, preferably <=about 10wt.% calculated as a dried component based on a total composition of an extract of propolis, obtained by extracting propolis which is a resinous substance collected from plants by bees and called as bee resin with about 10 times as much a mixed solution of water and a hydrophilic solvent (e.g. alcohol such as methanol, ethanol, or acetone) or the hydrophilic solvent as propolis and distilling away the solvent by distillation, etc., as an active ingredient. Since the remedy permeates skin extremely well, shows excellent reversible and partial inhibitory action on sebum secretion and does not provide irritation at all, the remedy for skin diseases suitable for the above-mentioned diseases is obtained.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an external preparation for skin. More specifically, the present invention relates to an external preparation containing an extract of propolis as an active ingredient, and is a skin disease treatment agent that shows mild effects on seborrheic diseases such as dermatitis and rosacea caused by excessive secretion of sebum.

[Prior Art] Propolis has been used as a traditional folk medicine since ancient times, and its functions and effects have recently been elucidated mainly in Eastern European countries. There are many reports on its antibacterial, hemostatic, scarring, anti-inflammatory, antioxidant, local anesthetic, and tumor growth inhibitory effects. The main components of propolis are flavones, flavanones, aromatic alcohols, aromatic aldehydes, coumarins, etc. The composition and content of these substances vary depending on where propolis is produced, and it is said that their effects also differ. .

On the other hand, to date, no compound has been known that specifically inhibits sebum secretion and does not affect other organs.

The sebum suppressant sibrothyrone acetate is available for oral administration, but oral administration often has greater side effects than topical application. Also, due to its anti-androgenic properties, sibrothyrone acetate can only be used by women.

[Problems to be Solved by the Invention] The present inventors were researching compounds that specifically inhibit sebum secretion and do not affect other organs, and discovered that propolis extract was used as an active ingredient. The present invention was completed based on the discovery that an external preparation prepared by the above methods can achieve this objective.

[Means for Solving the Problems] That is, the present invention is a sebum external preparation characterized by containing an extract of propolis as an active ingredient.

Hereinafter, the configuration of the present invention will be explained in detail.

Propolis used in the present invention
As mentioned above, s) is a tar-like substance collected from plants by bees, and is also called bee tar.

Generally, during beekeeping, large amounts of bee adhere to the frames and crevices of hives, so they are collected by scraping them off.

The above-mentioned extract or extract from propolis is produced as follows. Propolis is extracted by immersing it in a mixture of water and a hydrophilic solvent or in a hydrophilic solvent (generally, an extract having an amount of about 10 times the weight of propolis is used) to obtain a propolis extract. Examples of the hydrophilic solvent include alcohols such as methanol and ethanol, and acetone. A propolis extract is obtained by removing the solvent from the propolis extract by distillation or other methods. The amount of the extract (residue after distilling off the extraction solvent) is approximately 0.001% (wt%) or more in the entire composition. Although the upper limit of the blending amount is not particularly limited, from the viewpoint of commercial value such as coloring, it is preferable that the blending amount of propolis and its extract is up to about 10% in total as the dry residue.

In addition to propolis extract, the external skin preparation of the present invention contains sulfur, hinokitiol, triclosan, trichlorocarbanilide, chlorhexidine hydrochloride, chlorhexidine gluconate, halocarpan, chlorophenesine, benzethonium chloride, benzalkonium chloride, Antibacterial agents such as lysozyme, alkyldiaminoethylglycine hydrochloride, isopropylmethylphenol, benzoic acid, Photosensor No. 201, thymol, hexachlorophene, berberine, thioxolone, vitamins such as vitamin AlB2, B6, E5 biotin, nicotinic acid, and salicylic acid. , exfoliating agents such as resorcin, clycyrrhetinic acid, glycyrrhizic acid, allantoin, epsilon aminocaproic acid, butyl flufenamate, azulene, camphor, zinc chloride, zinc white, menthol, indomethacin, ibuprofen piconol, mefenamic acid, and their derivatives. Anti-inflammatory agents, zinc and its compounds, lactic acid, and oils, surfactants, water, ethanol, humectants, thickeners, fragrances, pigments, etc. may be added as appropriate to the extent that they do not impair the effects of the present invention, although they vary depending on the properties. Can be blended.

The sebum suppressant of the present invention may be in any form as long as it can be applied to the outer skin, such as a cream, ointment, or lotion.

[Effects of the Invention] The propolis extract of the present invention exhibits a very good reversible and local sebum suppressing effect. The compound also penetrates the skin very well and is completely non-irritating, making it particularly suitable for the treatment of seborrheic diseases. This activity is specifically directed towards sebum,
It has no effect on any other organs.

(Margin below) [Example] Example 1 Lotion 1) Sorbitol (70%) 3.
0g2) Glycerin 5.
0g3) Water 70.0
g4) Pyridoxine hydrochloride 0.5
g5) Propolis extract 1.0
g6) Polyoxyethylene (hereinafter referred to as POE) hydrogenated castor oil derivative 0.5g7) Ethanol
20.0g8) Fragrance
Mix and dissolve appropriate amounts of the ingredients 1), 2), 3), and 4), and add the mixed solution of 5), 6), 7), and 8) with stirring to obtain a lotion as a uniform solution.

Example 2 Lotion 1) Sorbitol (70%) 3.0g 2) Glycerin 5.0g3
) Water 70.5g4)
Glycyrrhizic acid 0.5g5) Propolis extract 0.5g6)
P OE hydrogenated castor oil derivative 0.5g7)
Ethanol 20.0g8)
Fragrance Appropriate amount 1) 2) 3
) Mix and dissolve the ingredients in 4) and add to this 5) 6)? )8)
Add the mixed solution while stirring to obtain a lotion as a homogeneous solution.

Example 3 Emulsion 1) Setanol 1.5g
2) Stearic acid 1.0g
3) Palmitic acid 0.5g
4) Liquid lanolin 1.0g
5) Squalane 2.0g6
) Isopropyl myristate 1.0g7
) Glyceryl monostearate 1.5g8)
Tween 20 0.5g9
) Berberine 0.5g10
) Propylene glycol 3.0g11
) Polyethylene glycol 400 2.0 g
l2) Triethanolamine 1.0g
13) Propolis extract (dry residue) 2.0
g14) Purified water 82.5
Each component of g1) to 9) was mixed to obtain a mixture. Separately,
Components 10) to 14) were mixed to obtain a mixture. Each mixture was separately heated and dissolved at 70°C, mixed and emulsified using an emulsifier, and then cooled by heat exchange to obtain an emulsion.

Example 4 Cream 1) Beeswax 11.0g
2) Paraffin wax 6.0g
3) Lanolin 3.0g
4) Isopropyl myristate 6.0g5) Squalane 8.0g6) Liquid paraffin 27.5g7) Propolis extract 1.5g8) Allantoin 0.5g9) P OE
Sorbitan monostearate 1.5g10) Sorbitan monostearate 4.0g11) Preservative
Appropriate amount 12) Propylene glycol
2.0g13) Borax
1.0g14) Water
28.0 gl)2)3)4)5)6)7)
8) Mix the ingredients of 9) 10) 11) and 12) and heat at about 75°C.
13) 1.
Add the mixture of 4) while stirring, cool, add an appropriate amount of fragrance at 55°C, continue stirring until 45°C, and leave to obtain a cream.

Example 5 Ointment 1) Solid paraffin 10°0g
2) Peace wax 10.0g
3) Squalane 10.0g
4) Propolis extract 1.0g
5) Resorcinol 0.1g
6) Zinc white 0.5g7
) Perfume Appropriate amount 8) Vaseline 68.4 g The above ingredients were mixed, the mixture was heated and dissolved at 80° C., and then cooled with stirring to obtain an ointment.

Example 6 Hair tonic 1) Ethanol 51.5g
2) Hinokitiol 0.3g
3) Vitamin E 0.5
g4) Niracol HCO-60 1.0g 5) Fragrance Appropriate amount6) Propolis extract 0.7g7) Purified water 45.0g8) Glycerin 1.0g9) Pigment Appropriate amount1) 3) 3
)4) and 5) were dissolved at room temperature to obtain an alcohol phase.

6)? ) The mixed liquid of 8) and 9) was dissolved under heating and cooled to obtain an aqueous phase. The alcohol phase was added to the aqueous phase and solubilized to obtain a hair tonic.

Next, the effects of the present invention will be explained in more detail by giving clinical examples.

(Medicine used) A lotion-type skin external preparation obtained by the following formulation and manufacturing method was used.

1) Propolis extract 1.0g2
) P OE (60 mol) Hydrogenated castor oil 2
．． 0g3) Glycerin 10・
0g4) Dipropylene glycol 10.0
g5) 113-butylene glycol 5.0g6
) Polyethylene glycol 1500 5.0 g
7) Cetyl isophutane) 10.0g
8) Squalane 5.0g9
) Methylparaben 1.0g10
) Carboxyvinyl polymer 0.3g11)
Sodium hexametaphosphate 0.08g12)
Ion exchange water 11. ．． 0g13
) Potassium hydroxide 0.12g14
) Ion exchange water 39.5g1)2
) 3) 4) 5) 6) are heated and dissolved at 60°C. 7 for this
) Add and mix 8) and 9) heated and dissolved at <60°C, and process with a homomixer to make a gel. Next, 10) and 11) dissolved in 12) were gradually added to this gel and dispersed with a homomixer, then 13) dissolved in 14) was added and mixed, and emulsified with a homomixer to form a lotion. A type of external preparation for skin was obtained.

(Targets for Use and Observation Period) The product was used for 4 weeks by 20 patients with seborrheic dermatitis between the ages of 15 and 30.

(How to use) After thoroughly washing your face with soap, apply the above-mentioned lotion-type skin preparation once a day only on the sebum.
It was applied ~3 times.

(Measurement of sebum) The total amount of sebum before use and after 4 weeks of use was measured by collecting sebum using the glass cup method and using the gravimetric method [Ohokawa, H., et al.
l.

Anal, Biochem, 95.351358 (1
979)].

The amount of sebum was expressed as a relative ratio as shown in the following formula.

Total sebum amount before use (blank below) (Results) Case number Age Gender Sebum reduction rate 1 20 Female 10 2 21 Female 11 3 23 Female 10 4 23 Male 8 5 17 Female 6 6 20 Male 10 7 15 Female 15 8 29 Female 12 9 30 Male 4 10 18 Female 8 11 21 Female 8 12 24 Female 3 13 24 Female 7 Case number Age Sex Sebum reduction rate 14 26 Male 915 2
5 Female 6 16 25 Male 5 17 28 Female 2 18 26 Female 4 19 22 Male 5 20 25 Female 2 Results of clinical tests on 20 people, 6 males and 14 females, showed that the average sebum reduction rate was 7.3%. The effectiveness of the skin external preparation of the present invention was demonstrated.

Claims (1)

[Claims] A skin preparation for external use that has a sebum suppressing effect and is characterized by containing an extract of propolis as an active ingredient.