JPH11269034A - Skin prepafation for external use for improving acne - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject new external preparation having excellent acne- improving and preventing effect by formulating at least one kind of compound selected from L-arginine as an active ingredient and its salts. SOLUTION: This external preparation comprises at least one kind of compound selected from L-arginine and its salts as an active ingredient. L-arginine salt includes e.g. hydrochloride, sulfate, metal salt of magnesium, etc., a salt with other amino acid. A formulating amount of the active ingredient is preferably 0.01-10 wt.% based on the external preparation. Ingredients used for conventional skin preparation for external use, e.g. aqueous ingredient, oily ingredient, alcohols, humectant, an ultraviolet light absorbent, a bleaching agent, etc., can be formulated in addition to the above essential ingredient in the range not impairing the above effect. The acne-improving and preventing effect includes healing and recovery of acne as well as inhibition of comedo formation and inhibition of keratotic plugging.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin for improving and preventing acne. More specifically, the present invention relates to a skin external preparation for improving and preventing acne, which has an effect of improving and preventing acne and pimples, while promoting the recovery of acne.

[0002]

2. Description of the Related Art Acne is a skin disease that mainly occurs in adolescents, and its formal name is acne vulgaris. Clinically, it causes chronic inflammatory changes in the pores, mainly in the pilosebaceous system. Is defined.

[0003] The pathogenesis is still largely unknown.
Generally, it is considered that the skin disease is a skin disease in which various factors are intricately intertwined while hypersecretion of sebum, keratinization of the hair follicle, and bacteria in the hair follicle play an important role.

[0004] Accordingly, as an external preparation for acne treatment, a cream containing, as an active ingredient, a sebum-suppressing / absorbing ingredient, a keratin softening / peeling ingredient, an antibacterial / bactericidal ingredient, and an anti-inflammatory ingredient, corresponding to the above factors. Ointments are often used.

[0005]

However, the effect of conventional active ingredients on the improvement and prevention of acne is not always sufficient, and various problems have been reported with existing remedies for acne.

For example, female hormones, which are sebum secretion inhibitory components, inhibit epidermal growth and reduce sebum secretion, but the side effects caused by this type of hormonal agent are not preferable for adolescent men and women. Absent.

[0007] Sulfur compounds such as sulfur and selenium disulfide, which are typical examples of the exfoliating and exfoliating components, do not have the side effects of the above-mentioned female hormones. May cause.

Further, crude drugs such as pyridoxine hydrochloride, peonies extract, and burdock extract having sebum-suppressing action, and Maika mosquito having sebum-absorbing action, even when used alone in a cream or ointment, are unlikely to have a sufficient sebum-suppressing effect. However, the effect of acne treatment was not always sufficient.

Further, sulfur, hinokitiol, photosensitive element 2
Antibacterial and bactericidal components such as No. 01 and berberine have an extremely high bactericidal activity against propionibacterium acnes, which is a resident bacterium, even in a test tube, but are actually incorporated into creams and ointments. When used for acne treatment, most do not exhibit the expected therapeutic effect.

[0010] Accordingly, the present invention provides a novel method for improving acne.
It is an object of the present invention to provide a prophylactic agent and an external preparation for skin for preventing and improving acne containing the same as an active ingredient.

In view of the above circumstances, the present inventors have conducted intensive studies on substances having an acne-improving / preventive effect, and as a result, have found that L-arginine or a salt thereof has an excellent acne-improving / preventive effect. As a result, the present invention has been completed.

[0012]

That is, the present invention provides an L-
The present invention relates to an external preparation for acne improvement containing at least one selected from arginine and salts thereof as an active ingredient.

[0013] The present invention also relates to a skin external preparation for suppressing comedone formation, comprising one or more selected from L-arginine and salts thereof as an active ingredient.

[0014] The present invention also relates to an external preparation for preventing keratotic plug formation, which comprises one or more selected from L-arginine and salts thereof as an active ingredient.

[0015]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail.

L-arginine used in the present invention is represented by the following chemical formula 1.

[0017]

Embedded image Is a proteinaceous basic amino acid represented by
It is known that F (natural moisturizing factor) is present in the stratum corneum of the epidermis as a component.

The salts of L-arginine used in the present invention include hydrochloride, sulfate, magnesium,
Examples thereof include, but are not limited to, metal salts such as calcium and potassium, and salts with other amino acids such as aspartic acid.

In the present invention, one or more selected from L-arginine and salts thereof are arbitrarily obtained and used, and the amount thereof is 0.1% in the skin external preparation of the present invention.
It is preferably from 005 to 20.0% by weight, more preferably from 0.01 to 10.0% by weight. If the amount is less than 0.005% by weight, no sufficient acne-improving / preventive effect is exhibited, while if it exceeds 10.0% by weight, no significant improvement in the effect is observed.

Although many applications of L-arginine to external preparations for skin or cosmetics are known, L-arginine is mainly used because basic amino acids containing L-arginine are excellent in stabilizing preparations or other active ingredients. It is only used for

In Japanese Patent Application Laid-Open No. Hei 6-279227, a stable external preparation for the skin having the effects of improving rough skin, healing wounds and preventing skin aging by using trehalose and one or more amino acids in combination is disclosed. And that it can provide cosmetics, but there is no report that L-arginine or a salt thereof alone promotes the recovery of acne and has an excellent effect of improving and preventing acne. The present invention has newly discovered that L-arginine or a salt thereof alone has the above effects.

The effect of the skin preparation for external use of the present invention for improving and preventing acne includes, in addition to acne healing and recovery, suppression of comed (corned) formation, suppression of keratin plug formation and the like.

The external preparation for skin for preventing and / or improving acne according to the present invention may contain, in addition to the above-mentioned essential components, if necessary, cosmetics, quasi-drugs, and the like as long as the effects of the present invention are not impaired.
Various components used in skin external preparations such as pharmaceuticals, for example, aqueous components, oily components, powder components, alcohols, humectants,
Thickeners, ultraviolet absorbers, whitening agents, preservatives, antioxidants,
Surfactants, fragrances, coloring agents, various skin nutrition agents, and the like can be appropriately compounded.

The dosage form of the external preparation for skin for preventing and improving acne of the present invention is not particularly limited. For example, any dosage form such as an ointment, a cream, a milky lotion, a lotion, a pack, and a bath preparation may be used. Can be.

[0025]

The present invention will be described in more detail with reference to the following examples, which should not be construed as limiting the invention thereto. In addition, the compounding amount is weight%.

(Example 1, Comparative Example 1) An external preparation for acne improvement was prepared by a conventional method based on the formulation shown in Table 1 below. Using these as test samples, the following actual use test was performed to evaluate the acne improvement effect. Table 1 shows the results.

[Actual use test] Subjects: 40 men and women aged 16 to 24 (20 per group) suffering from acne. 2. Test method: After thoroughly washing the face using a cosmetic soap, each group was applied with each test sample (external preparation for skin) only on the rash 2-3 times a day, and after 4 weeks, the affected area was observed. Was done. 3. Evaluation of overall improvement: Symptoms were improved by the external preparation for skin (test sample) before use (evaluation (a)), and symptoms were unchanged or worsened (evaluation (b)) In two stages. 4. Usefulness judgment: ：: More than 15 out of 20 (a) in the overall improvement evaluation
評 価: In the overall improvement degree evaluation, 10 to 14 out of 20 persons were (a)
Δ: Overall improvement degree evaluation, 5 to 9 out of 20 persons evaluated as (a) ×: General improvement degree evaluation, 4 out of 20 persons evaluated as (a)

[0028]

[Table 1]

As is clear from the results shown in Table 1, the external preparation for acne improvement of Example 1 containing L-arginine hydrochloride exhibited an excellent effect of preventing acne.

(Example 2) Cream (combination component) (% by weight) (1) Stearic acid 5.0 (2) Stearyl alcohol 4.0 (3) Isopropyl myristate 18.0 (4) Glycerin monostearin Acid ester 3.0 (5) Propylene glycol 10.0 (6) L-arginine aspartate 0.1 (7) Caustic potassium 0.2 (8) Sodium bisulfite 0.01 (9) Preservative appropriate amount (10) ) Appropriate amount of perfume (11) Residual ion-exchanged water (Preparation method) Add (5) to (7) to (11), dissolve, heat and maintain at 70 ° C (aqueous phase). On the other hand, (1) to (4),
(8) to (10) are mixed, heated and melted, and kept at 70 ° C. (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is maintained for a while to cause a reaction. Thereafter, the mixture was uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well to obtain a cream.

(Example 3) Cream (combination component) (% by weight) (1) Stearic acid 2.0 (2) Stearyl alcohol 7.0 (3) Hydrogenated lanolin 2.0 (4) Squalane 0 (5) 2-octyldodecyl alcohol 6.0 (6) polyoxyethylene (25 mol) stearyl alcohol 4.0 (7) isopropyl myristate 18.0 (8) glycerin monostearate 3.0 (9) Propylene glycol 10.0 (10) L-arginine aspartate 0.1 (11) Caustic potash 0.2 (12) Sodium bisulfite 0.01 (13) Preservatives proper amount (14) Fragrance proper amount (15) ions Exchange water residue (Preparation method) Add (9) to (11) to (15), dissolve, heat and maintain at 70 ° C (aqueous phase). On the other hand, (1) to (8),
(12) to (14) are mixed, melted by heating and maintained at 70 ° C. (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is maintained for a while to cause a reaction. Thereafter, the mixture was uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well to obtain a cream.

(Example 4) Cream (combination component) (% by weight) (1) Stearic acid 2.0 (2) Stearyl alcohol 7.0 (3) Hydrogenated lanolin 2.0 (4) Squalane 5. 0 (5) 2-octyldodecyl alcohol 6.0 (6) polyoxyethylene (25 mol) cetyl alcohol ether 3.0 (7) glycerin monostearate 2.0 (8) propylene glycol 5.0 (9) L-arginine 1.0 (10) Tranexamic acid 0.2 (11) Sodium bisulfite 0.03 (12) Ethyl paraben 0.3 (13) Flavor appropriate amount (14) Ion-exchanged water residue (Production method) (14) )), Add (8) to (10) and heat to maintain at 70 ° C. (aqueous phase). On the other hand, (1) to (7), (1)
1) to (13) are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase was added to the water phase to carry out preliminary emulsification, and after uniform emulsification with a homomixer, the mixture was cooled to 30 ° C. while stirring well to obtain a cream.

(Example 5) Cream (combination component) (% by weight) (1) Solid paraffin 5.0 (2) Beeswax 10.0 (3) Vaseline 15.0 (4) Liquid paraffin 41.0 ( 5) Glycerin monostearate 2.0 (6) Polyoxyethylene (20 mol) sorbitan monolaurate 2.0 (7) Soap powder 0.1 (8) Borax 0.2 (9) L-arginine hydrochloride Salt 3.0 (10) Sodium bisulfite 0.03 (11) Ethylparaben 0.3 (12) Appropriate amount of perfume (13) Residue of ion-exchanged water (Production method) (7)-(9) Add and heat 7
Keep at 0 ° C. (aqueous phase). On the other hand, (1) to (6), (10)
(12) is mixed, heated and melted, and kept at 70 ° C. (oil phase). The oil phase is gradually added to the aqueous phase while stirring to carry out the reaction. Thereafter, the mixture was uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well to obtain a cream.

(Example 6) Emulsion (combination component) (% by weight) (1) 2.5 stearic acid (2) cetyl alcohol 1.5 (3) Vaseline 5.0 (4) liquid paraffin 10.0 (5) Polyoxyethylene (10 mol) monooleate 2.0 (6) Polyethylene glycol (1500) 3.0 (7) Triethanolamine 1.0 (8) Carboxyvinyl polymer 0.05 ("Carbopol" 941 "; manufactured by BF Goodrich) (9) L-arginine aspartate 0.01 (10) Sodium bisulfite 0.01 (11) Ethyl paraben 0.3 (12) Perfume proper amount (13) Ion-exchanged water Dissolve (8) in a part of the remainder (Preparation method) (13) (A phase).
(6), (7), and (9) are added to the remaining (13), and the mixture is heated and dissolved and maintained at 70 ° C. (aqueous phase). On the other hand, (1)-
(5), (10) to (12) were mixed and melted by heating to 70
C (oil phase). Add oil phase to water phase, pre-emulsify,
The phase A was added, and the mixture was uniformly emulsified with a homomixer. After the emulsification, the mixture was cooled to 30 ° C. while stirring well to obtain an emulsion.

(Example 7) Emulsion (combination component) (% by weight) (1) Microcrystalline wax 1.0 (2) Beeswax 2.0 (3) Lanolin 20.0 (4) Liquid paraffin 10.0 (5) Squalane 5.0 (6) Sorbitan sesquioleate 4.0 (7) Polyoxyethylene (20 mol) Sorbitan monooleate 1.0 (8) Propylene glycol 7.0 (9) L-arginine Hydrochloride 8.0 (10) Tranexamic acid 1.0 (11) Sodium bisulfite 0.01 (12) Ethylparaben 0.3 (13) Flavor appropriate amount (14) Ion-exchanged water residue (Production method) (14) (8) to (10), and heat to maintain at 70 ° C. (aqueous phase). On the other hand, (1) to (7), (1)
1) to (13) are mixed, melted by heating and kept at 70 ° C. (oil phase). While stirring the oil phase, slowly add the aqueous phase, homogenize with a homomixer, and stir well at 30 ° C.
To give an emulsion.

(Example 8) Jelly (combination component) (% by weight) (1) 95% ethyl alcohol 10.0 (2) dipropylene glycol 15.0 (3) polyoxyethylene (50 mol) oleyl alcohol Ether 2.0 (4) Carboxyvinyl polymer 0.05 ("Carbopol 940"; manufactured by BF Goodrich) (5) Caustic soda 0.15 (6) L-arginine 0.1 (7) Sodium bisulfite 01 (8) Ethylparaben 0.3 (9) Fragrance appropriate amount (10) Ion-exchanged water residue (Preparation method) (4) is uniformly dissolved in (10), and (3) is added to the aqueous phase. Next, (1), (2) (7) to (9)
Was added, and neutralized with (5) and (6) to increase the viscosity to obtain jelly.

(Example 9) Jelly (combination component) (% by weight) (A phase) 95% ethyl alcohol 10.0 polyoxyethylene (20 mol) octyldodecanol 1.0 pantotenyl ethyl ether 0.1 Methylparaben 0.15 (B phase) Potassium hydroxide 0.1 (C phase) Glycerin 5.0 Dipropylene glycol 10.0 Sodium bisulfite 0.03 L-arginine magnesium salt 0.05 Carboxyvinyl polymer 0.2 (" Carbopol 940 "; BF Goodrich Co.) Ion-exchanged water residue (Preparation method) Dissolve A phase and C phase uniformly, and add A to C phase
Add phases and solubilize. Next, after the phase B was added, filling was performed to obtain jelly.

Example 10 Pack (combination component) (% by weight) (A phase) Dipropylene glycol 5.0 Polyoxyethylene (60 mol) hydrogenated castor oil 5.0 (B phase) Olive oil 5.0 Tocopherol acetate 0.2 Ethyl paraben 0.2 Fragrance 0.2 (Phase C) L-arginine sulfate 0.3 Sodium bisulfite 0.03 Polyvinyl alcohol 13.0 (Saponification degree 90, Polymerization degree 2000) Ethyl alcohol 7. 0 Ion-exchanged water residue (Preparation method) A phase, B phase, and C phase are each dissolved uniformly.
Add phase B to phase and solubilize. Next, after adding the phase C, the mixture was filled to obtain a pack.

(Example 11) Solid foundation (combination component) (% by weight) (1) Talc 43.1 (2) Kaolin 15.0 (3) Sericite 10.0 (4) Zinc white 7.0 (5) Titanium dioxide 3.8 (6) Yellow iron oxide 2.9 (7) Black iron oxide 0.2 (8) Squalane 8.0 (9) Isostearic acid 4.0 (10) POE sorbitan monooleate 3 0.0 (11) Isocetyl octoate 2.0 (12) L-arginine glutamate 0.5 (13) Preservatives proper amount (14) Flavor proper amount (Production method) Blend powder components of (1) to (7) And the oily components (8) to (11), (12)
After adding (14) and kneading well, the mixture was filled in a container and molded to obtain a solid foundation.

(Example 12) Emulsion type foundation (combination component) (% by weight) (powder part) Titanium dioxide 10.3 Sericite 5.4 Kaolin 3.0 Yellow iron oxide 0.8 Bengala 0.3 Black iron oxide 0.2 (oil phase) Decamethylcyclopentasiloxane 11.5 Liquid paraffin 4.5 Polyoxyethylene-modified dimethylpolysiloxane 4.0 (aqueous phase) Purified water 50.0 1,3-butylene glycol 4. 5 L-Arginine hydrochloride 1.5 Sorbitan sesquioleate 3.0 Preservatives Appropriate amount Flavors Appropriate amount (Preparation method) After heating and stirring the aqueous phase, a powder portion which has been sufficiently mixed and ground is added, and a homomixer treatment is performed. Further, the oil phase mixed by heating was added thereto, and the mixture was subjected to a homomixer treatment. Then, a flavor was added with stirring, and the mixture was cooled to room temperature to obtain an emulsion type foundation.

All of Examples 2 to 12 were excellent in the effect of improving and preventing acne.

[0042]

As described in detail above, the present invention provides a skin external preparation excellent in the effect of improving and preventing acne.

 ──────────────────────────────────────────────────続 き Continuing from the front page (72) Inventor Akira Ito 1050 Nippa-cho, Kohoku-ku, Yokohama-shi, Kanagawa Inside Shiseido Daiichi Research Center Co., Ltd.

Claims (3)

[Claims] 1. An acne-improving skin external preparation comprising, as an active ingredient, one or more selected from L-arginine and salts thereof. 2. A skin external preparation for suppressing comedone formation, comprising one or more selected from L-arginine and salts thereof as an active ingredient. 3. An external preparation for preventing keratotic plug formation, comprising one or more selected from L-arginine and salts thereof as an active ingredient.