JPS6360908A - Skin drug for external use - Google Patents

Abstract

PURPOSE:To obtain a skin drug for external use, by blending Cuscuta seed with an antimicrobial agent or keratinous peeling agent, excellently permeable into the skin without giving irritation or hormonal side effect and particularly effective in preventing, curing and treating pimples and preventing dandruff by applying to the scalp. CONSTITUTION:A skin drug for external use obtained by blending powdered Cuscuta seed which is a crude drug or an extracted essence prepared by extracting the powdered Cuscuta seed with water or an aqueous alcohol, e.g., ethanol, at 15-25 deg.C with sulfur, hinokitiol, photosensitive element No.201, antimicrobial agent, e.g. thioxolone, etc., and/or keratinous peeling agent, e.g. salicylic acid, resorcin, etc. The amount of the blended powdered Cuscuta seed or essence thereof (residue obtained by distilling away the extracting solvent) is >=0.005wt% in the total composition. The amount of the blended antimicrobial agent is 0.001-10wt% and the amount of the blended keratinous peeling agent is 0.01-20wt%. Furthermore, other adjuvants may be blended. The above- mentioned drug is used in the form, e.g. cream, ointment, lotion, tonic, etc., applicable to the integument.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an external skin preparation. More specifically, the present invention is characterized by blending the herbal drug Toshishi or its extract with antibacterial agents such as sulfur, hinokitiol, photosensor No. 201, and thioxolone, and/or exfoliating agents such as salicylic acid and resorcinol. The present invention relates to a skin preparation for external use, which is particularly effective in the prevention, treatment, and treatment of acne, and can also be used on the scalp to effectively prevent dandruff.

[Prior art] Acne is a skin disease that mainly occurs during adolescence and is called zamaro vulgaris.Clinically, it is characterized by chronic inflammatory changes that occur in the pores, mainly in the pilosebaceous system. Defined.
□ The etiology of acne is still unclear, and although it is a skin disease in which various factors are intricately intertwined, in general,
Excessive sebum secretion, hair follicle keratinization, and bacteria within the hair follicle are thought to play important roles.

Therefore, creams and ointments containing sebum secretion inhibitors and antibacterial agents are commonly used as external preparations for treating acne. However, existing acne treatment agents containing various drugs have various drawbacks. For example, ethinyl estradiol, a sebum secretion inhibitor, inhibits epidermal growth and reduces sebaceous gland secretion, but the side effects caused by hormones are not desirable for adolescents. Also, for example, sulfur,
Antibacterial agents such as hinokitiol, Photosensor No. 201, and resorcinol have shown to be extremely effective against Propionibacterium acnes, a bacteria resident on the skin, in vitro (r); When combined into ointments and used to treat acne, most of the time they do not exhibit the expected therapeutic effect.

[Problems to be Solved by the Invention] The present inventors have proposed that the effects of conventional antibacterial agents or exfoliating agents be increased on the skin, and that they are particularly effective in preventing, treating, and treating acne. While researching compounds that can be used to effectively prevent dandruff, we discovered that the herbal medicine Toshishi or its extract and, for example, sulfur,
The present invention was completed based on the discovery that an external skin preparation characterized by containing hinokitiol, Photosensor No. 201, and an antibacterial agent such as berberine, or a keratin exfoliant such as salicylic acid or resorcinol can achieve this objective.

[Means for Solving the Problems] That is, the present invention is a skin preparation for external use, which is characterized in that it contains Toshishi or an extract thereof, and an antibacterial agent and/or a keratin exfoliant. Such external skin preparations are particularly effective in preventing, treating, and treating acne, and can also be used on the scalp to effectively prevent dandruff.The structure of the present invention will be described in detail below.

The toshishi used in the present invention is mainly the seeds of Kassula japonica, used alone as a tonic or tonic, or as a Chinese herbal preparation.
It is used as a component of crude drug preparations, and most of them are taken internally, and there are only a few examples of its use in external preparations.

In the present invention, it is obtained by extraction using toshishi powder or water or aqueous alcohol, such as ethanol, usually at 15 to 25°C. The blending amount is approximately 0.005% of the total composition, including the extract (residue after distilling off the extraction solvent).
% (weight %) or more. The upper limit of the amount to be blended is not particularly limited, but from the viewpoint of commercial value such as coloring, it is preferable to blend up to about 10% in total as a dry residue.

On the other hand, specific antibacterial agents that can be incorporated in the present invention are as follows.

Sulfur, hinokitiol, triclosan, trichlorocarbanilide, chlorhexidine hydrochloride, chlorhexidine cluconsanate, halocarpan, chlorophenesin,
Benzethonium chloride, benzalkonium chloride, lysozyme chloride, alkyldiaminoethylglycine chloride, isopropylmethylphenol, benzoic acid, photosensitizer No. 201, thymol, hexachlorophene, berberine, resorcin φ thioxolone and their derivatives.

The blending amount is 0.001% or more and 10% or less, preferably 0.01% or more and 5% or less.

Further, as the exfoliating agent that can be used in the present invention, specifically, the following exfoliants are used.

Sulfur, salicylic acid, resorcinol, thioxolone, dibenzothiophene and their derivatives.

In the present invention, any one or more selected from the group consisting of these antibacterial agents and exfoliating agents may be used.

The blending amount is approximately 0.01% or more and 20% or less.

The skin external preparation of the present invention includes toshishi or an extract thereof;
In addition to antibacterial agents or exfoliants, zinc and its compounds, agents such as lactic acid, and depending on the dosage form, oils, surfactants, water, ethanol, humectants, thickeners, fragrances, pigments, etc. can be appropriately blended within a range that does not impair the effects of the present invention.

The external preparation for skin of the present invention may be in any form as long as it can be applied to the skin, such as cream, ointment, lotion, or tonic.

[Effects of the invention] A skin preparation for external use containing toshishi or its extract and an antibacterial agent or exfoliating agent penetrates the skin very well, does not cause any irritation or hormonal side effects, and is particularly effective in preventing acne.
It works effectively for treatment and treatment, and can also be used on the scalp to effectively prevent acne. [Example] Example 1 Lotion Sorbitol (70%) 3.0g Glycerin 5. ○g resorcinol
0.02g water
TO,og Mix and dissolve these ingredients, add allantoin 0.18g Toshishi extract 1.0g polyoxyethylene hydrogenated castor oil derivative 0.5g ethanol 20.3g fragrance
Add an appropriate amount of the mixed solution while stirring to obtain a lotion as a homogeneous solution.

Example 2 Cream beeswax 10.0g paraffin wax 6.0g lanolin
3.0g isopropyl myristate
6.0g squalane
8.0g liquid paraffin 26.0g
Toshishekis 0.1g sulfur
2. Og lysozyme chloride
1.0g polyoxyethylene sorbitan dried sonostearate 2.
0g sorbitan monostearate 4.2g preservative Appropriate amount Mix these ingredients, heat at about 75°C to dissolve, and then heat to about 75°C Propylene glycol 2. ○g Borax
0.7g water
Add 29.0g of the mixture while stirring, cool, add an appropriate amount of fragrance at 55°C,
Continue stirring until 5°C and leave to obtain cream.

Example 3 Hair tonic ethanol 55.0g Hinokitiol 0.5g Nikkor HCO
-60 1.0g fragrance
Dissolve an appropriate amount at room temperature and prepare for alcohol use.
Na.

Toshishi extract 0.5g purified water
42.0g glycerin
1.0g dye
An appropriate amount of the mixture was dissolved under heating and cooled to obtain an aqueous phase.

The alcohol f was added to the aqueous phase and solubilized to obtain a hair tonic.

Example 4 Ointment solid paraffin 10. og peace wax 10.0g squalane
10.0g Toshishi extract
1.0g sulfur
2.0g fragrance Appropriate amount Vaseline 67.0g The above ingredients were mixed, and the mixture was heated and dissolved at 80°C, and then cooled with stirring to obtain an ointment.

The effects of the present invention will be explained in detail by briefly giving clinical examples.

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

Toshishi extract 2.0gP, O,
E, (60 moles) hydrogenated castor oil 2.0 g glycerin 10.0 g dipropylene glycol 10. Ogl, 3-butylene glycol 5.0g polyethylene glycol 1500 5
．． 08 and above are heated and melted at 60'C. Add to this 1.0g of resorcinol and 10.0g of squalane.
5.0g methylparaben
Add and mix 1.0g of the solution heated to <60'C, and process with a homomixer to form a gel.

Next, add 0.25 g of carboxyvinyl polymer and 0.03 g of sodium hexametaphosphate to this gel, and add ion-exchanged water.
10. Gradually add the solution dissolved in OG and disperse with a homomixer, then add and mix 0.12g of potassium hydroxide dissolved in 38.6g of ion-exchanged water, emulsify with a homomixer, and make a lotion type for external use on the skin. obtained the drug.

In addition, as a control drug, an external preparation containing only Toshishiki extract or only resorcinol was used.

Case No. 1 to 10 Case No. containing only resorcinol,
11-20 Case No. 21-20 Contains only toshishi extract
30 Contains resorcinol + Toshishishi extract.A total of 30 men and women should use this product for about 1 month.

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

(112 observation items and observation dates) The three symptoms of acne, papules, and pustules were observed, and the severity of acne vulgaris was determined by combining the severity of each individual finding: severe, moderate, and mild. Divided into stages. Follow-up observations were made before treatment, 91 weeks after treatment, 2 weeks after treatment, 3 weeks after treatment, and 4 weeks after treatment.

(Overall improvement level) The degree of improvement in symptoms due to the drug used compared to before use: markedly relieved (++), considerably relieved (y), somewhat relieved (+),
It was divided into 5 stages: no change (±) and worsening (-).

(Usefulness) Based on the overall degree of improvement, it was judged as extremely useful (1+), quite useful (sort of), somewhat useful (+), and ineffective (±).

(Leaving space below) (Results) The clinical test results of a total of 30 people (7 men and 23 women) showed that out of 10 people who used only the external preparation containing Photosensor No. 201, 3 (30%) said it was 10 (somewhat useful), ± ( 7 people (70$) said it was ineffective), and 3 out of 10 people who used topical preparations containing only toshishi extract said it was + (slightly useful).
(30%), ± (invalid) 7 (70%), photosensitive element 2
Of the 10 people who used external preparations containing No. 01 Toshishishi extract, 'n+(
3 people (30%) said it was extremely useful, 4 people said it was quite useful (40%), and 3 people (30%) said it was + (slightly useful), proving the effectiveness of the present invention in treating acne.

Claims (1)

[Claims] 1. A skin preparation for external use, characterized in that it contains toshishi or an extract thereof, and an antibacterial agent and/or a keratin exfoliant.