JPH10265365A - External preparation for skin for pimple - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject medicine capable of treating pimple by including a combination of an extract of Eriobotorya japonica Lindl., and one or more of a keratin softening and releasing agent, an antiinflammatory agent, an antibacterial and antifungal agent, a sebum suppressing and absorbing agent and a protease inhibitor. SOLUTION: This medicine comprises one or more of a keratin softening and releasing agent, an antiinflammatory agent, an antibacterial and antifungal agent, a sebum suppressing and absorbing agent and a protease inhibitor and an extract of Eriobotorya japonica Lindl., as active ingredients. The keratin softening and releasing agent includes a betaine, sulfur, salicylic acid, etc., and its amount is 0.001-5 wt.% in the whole amount. The antiinflammatory agent includes glycyrrhizinic acid, indomethacin, etc., and its amount is 0.01-5 wt.%. The antibacterial and antifungal agent includes sulfur, hinokitiol, etc., and its amount is 0.01-5 wt.%. The sebum suppressing and absorbing agent includes an essence of burdock, etc., and its amount is 0.01-10 wt.%. The protease inhibitor includes tranexamic acid, etc., and is amount is 0.01-10 wt.%. The amount of the extract of Eriobotorya japonica Lindl. is 0.01-10 wt.%. Consequently pimple can be excellently treated under mild conditions to skin without causing hormone-like adverse effects.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a skin external preparation for acne having an excellent acne treatment effect.

[0002]

2. Description of the Related Art Acne is a skin disease that mainly develops during puberty, and its formal name is acne vulgaris. Clinically, "acne acne vulgaris" is a chronic inflammatory change that occurs in the pores mainly in the pilosebaceous system. Is defined. Although the pathogenesis is still largely unknown, it is generally considered to be a skin disease in which various factors are intricately intertwined while hypersecretion of sebum, keratinization of hair follicles, and bacteria in hair follicles play important roles. ing. Therefore,
Topical treatments for acne treatment include sebum suppression / absorption components, keratin softening / peeling components, antibacterial
Creams and ointments containing a bactericidal component and an anti-inflammatory component are generally widely used.

[0003]

However, various drawbacks have been reported for the existing acne remedies containing the various components described above. For example, a female hormone, which is a sebum secretion inhibitory component, suppresses epidermal growth and reduces sebum secretion, but the side effects caused by this kind of hormonal agent are not preferable for adolescent men and women. Also,
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. However, repeated use often causes skin irritation, bulkiness of the skin, and the like. Crude drugs such as pyridoxine hydrochloride, peony extract, and burdock extract, which have sebum-suppressing action, and mica, which has sebum-absorbing action, do not show sufficient sebum-suppressing and absorbing effects even when used alone in creams or ointments. The effect of the treatment was not always satisfactory. In addition, sulfur, hinokitiol,
Antimicrobial and bactericidal components such as Photosensitizer No. 201 and berberine exert an extremely high antibacterial activity against Propionibacterium acnes, which is a resident bacterium in the skin, even if they exhibit an extremely high antibacterial activity in a test tube. Most of them do not exhibit the expected therapeutic effect when used in ointments when used in the treatment of acne.

On the other hand, regarding the loquat extract, the applicant of the present application has previously found that the loquat extract is effective as a skin roughness inhibitor (Japanese Patent Publication No. 5-17206, Japanese Patent Application Laid-Open No. Hei 7-21538). .

[0005]

Means for Solving the Problems In view of the above circumstances, the present inventors have conducted intensive studies and as a result, have found that keratin softening and exfoliating agents, anti-inflammatory agents, antibacterial and bactericides, sebum suppressants and absorbents, protease inhibitors If you combine the loquat extract with the agent,
The present inventors have found that a skin external preparation for acne which has no hormone-like side effects, is gentle on the skin, and satisfactorily achieves the purpose of acne treatment has been found, and has completed the present invention.

[0006] That is, the present invention is to mix loquat extract with one or more selected from keratin softening and exfoliating agents, anti-inflammatory agents, antibacterial and bactericidal agents, sebum suppressing and absorbing agents, and protease inhibitors. A skin external preparation for acne, characterized by comprising:

Hereinafter, the configuration of the present invention will be described in detail. The loquat extract used in the present invention is obtained, for example, by the following method. Loquat leaf, fruit, bark or rhizome dried, heated to reflux with a solvent, for example, lower alcohols such as methanol and ethanol, hydrous lower alcohols or 1,3-butylene glycol, propylene glycol or hydrous polyhydric alcohols, It is obtained by concentrating the extract obtained by filtration.

In the present invention, the amount of the loquat extract to be added to the external preparation for acne is 0.00
It is preferably from 1 to 10.0% by weight, more preferably from 0.01 to 10.0% by weight. If it is less than 0.001% by weight, the effect of the present invention is not sufficient, and if it exceeds 10.0% by weight, no further increase in the effect is observed.

In the present invention, the keratin softening and exfoliating agent used in combination with the loquat extract is at least one of betaines, sulfur, selenium disulfide, salicylic acid, urea and their derivatives and salts. Is preferred. By combining and combining the loquat extract and the exfoliating and exfoliating agent, abnormal keratinization of the skin can be mildly suppressed, and keratotic plugs that cause comed formation can be removed.

The amount of the exfoliating and exfoliating agent added to the skin external preparation for acne is 0.0001 to 0.0001 to the total amount of the skin external preparation.
10.0% by weight is preferred, and 0.001 to 5.0% by weight
Is more preferred. If the amount is less than 0.0001% by weight, the desired softening and exfoliating effect on the stratum corneum is difficult to be exhibited, which is not preferable. On the other hand, if it exceeds 10.0% by weight, the solubility tends to be inferior.

In the present invention, anti-inflammatory agents used in combination with the loquat extract include glycyrrhizic acid, glycyrrhetinic acid, allantoin, indomethacin, epsilon aminocaproic acid, butyl flufenamate, azulene, camphor, zinc chloride, zinc white, Preferably, it is at least one of menthol, ibuprofen piconol, mefenamic acid and their derivatives and salts.
By blending the loquat extract and the anti-inflammatory agent in combination, it is possible to suppress the development of acne that is mild and highly inflammatory to the skin and to prevent deterioration.

The amount of the anti-inflammatory agent to be used in combination is preferably 0.001 to 10.0% by weight, more preferably 0.01 to 5.0% by weight, based on the whole external preparation for acne. 0.
If the amount is less than 001% by weight, the desired inflammation-suppressing effect is hardly exhibited, and if it exceeds 10.0% by weight, the acne-inhibiting effect commensurate with the blending amount tends not to be observed, which is not preferred.

In the present invention, the antibacterial and bactericidal agents used in combination with the loquat extract include sulfur, hinokitiol, triclosan, trichlorocarbanilide, chlorhexidine hydrochloride, chlorhexidine gluconate, halocarban, chlorophenesin, and the like. Benzethonium chloride,
Benzalkonium chloride, lysozyme chloride, alkyldiaminoethyl glycine hydrochloride, isopropylmethylphenol, benzoic acid, photosensitizer 201, thymol, hexachlorophen, berberine, thioxolone, yukinoshita extract, oak extract, ogon extract and derivatives and salts thereof Preferably, at least one of them is used.
By combining the loquat extract and the antibacterial / bactericide in combination, the growth of Propionibacterium acnes can be suppressed, and the acne can be prevented from spreading and becoming worse.

The amount of the combined antibacterial and bactericide is 0.001 to 10.0% by weight based on the total amount of the external preparation for acne.
Is preferable, and 0.01 to 5.0% by weight is more preferable.
If the amount is less than 0.001% by weight, the desired antibacterial and bactericidal effects are hardly exhibited, so that it is not preferable. Is not preferred.

In the present invention, as the sebum suppressant / absorbent used in combination with the loquat extract, burdock extract,
Oil-soluble burdock extract, peonies extract, sage extract, calendula officinalis, bodyid extract, cornflower extract, pyridoxine hydrochloride, pyridoxine dicaprylate, pyridoxine dipalmitate, pyridoxine glycyrrhizinate, pyridoxine dilaurate, pyridoxine tripalmitate, pyridoxal phosphate, HP -Β-
It is preferably at least one of CD, mica, pearlescent agent, talc, iron oxide, titanium oxide and derivatives and salts thereof. Combination of loquat extract and sebum suppressant / absorbent suppresses secretion of excessive sebum mildly to the skin and suppresses exacerbation of acne by suppressing free fatty acids that cause irritation can do.

The amount of the sebum suppressant / absorbent to be used in combination is preferably 0.001 to 30.0% by weight, more preferably 0.01 to 10.0% by weight, based on the whole external preparation for acne. If the content is less than 0.001% by weight, the desired sebum suppression / absorption effect is hardly exhibited, which is not preferable.
If the amount is more than 0% by weight, an increase in acne-suppressing effect commensurate with the amount is not likely to be recognized, which is not preferable.

In the present invention, protease inhibitors used in combination with the loquat extract include tranexamic acid, guanidinobenzoic acid, p-aminomethylbenzoic acid,
Guanidine, acetamide, benzamidine, antipine, plasminostreptin, leupeptin, aprotinin, bovine pancreatic basic trypsin inhibitor, soybean trypsin inhibitor, corn protease inhibitor, lima bean protease inhibitor and at least one of their derivatives and salts. Is preferred. Combination of loquat extract and protease inhibitor to increase keratin water content, suppress transdermal water loss, and improve skin resistance to improve acne-resistant skin Can be.

The amount of the protease inhibitor used in combination is
0.001 to 20.0 with respect to the whole external preparation for acne
% By weight, and more preferably 0.01 to 10.0% by weight. If the content is less than 0.001% by weight, the desired effect of suppressing rough skin is hardly exhibited, so that it is not preferable.
If the amount exceeds the above range, an increase in the acne-suppressing effect commensurate with the amount is not likely to be recognized, which is not preferable.

In addition to the above essential components, the skin external preparation for acne of the present invention includes components usually used in skin external preparations such as cosmetics and pharmaceuticals, such as aqueous components, oil components, powder components, and the like.
Alcohols, humectants, thickeners, ultraviolet absorbers, whitening agents, preservatives, antioxidants, surfactants, fragrances, coloring agents, various skin nutrition agents, and the like can be appropriately compounded as necessary.

The properties of the external preparation for acne of the present invention may be any of those conventionally applicable to external preparations for skin, such as creams, lotions, ointments, emulsions, packs, bath preparations, and the like. Absent.

[0021]

Next, the present invention will be described in more detail with reference to Test Examples and Examples, but the present invention is not limited thereto. Unless otherwise specified, the compounding amount is% by weight based on the whole skin external preparation. First, test methods and criteria used for evaluating the skin external preparation for acne of the present invention will be described.

Test Methods and Criteria (1) Drugs Used The skin acne-suppressing effect of a skin external preparation manufactured by a conventional method was measured based on the formulation of each skin external preparation described below. The loquat extract was prepared by the following method. 1 to 10 g of dried and crushed loquat leaf, 10 times the amount of water, 1,3-
After adding butylene glycol or a mixture thereof, the mixture was extracted at room temperature for 10 days, and the supernatant was filtered and concentrated to obtain a loquat extract.

(2) Target for Use 220 men and women between the ages of 16 and 24 suffering from acne.
(20 people per group) (3) Method of use and observation day After thoroughly washing the face using toilet soap, each topical skin preparation was applied only on the rash 2-3 times a day, and 4 weeks later The affected part was observed.

(4) Overall improvement degree The symptoms were divided into two stages: (a) indicating that the symptoms were improved by the drug used before use, and (b) indicating that the condition was unchanged or worsened.

(5) Evaluation of usefulness A: Out of 20 persons, (a) was 15 or more persons in overall improvement degree. ：: (a) out of 20 persons in overall improvement degree is 10 to 14 persons. B: 5 to 9 (a) out of 20 in overall improvement. C: Out of 20 persons (a) in the overall degree of improvement was 4 or less.

Examples 1 to 5 and Comparative Examples 1 to 6 A lotion type skin external preparation having the formulation shown in Tables 1 and 2 was prepared, and its usefulness was evaluated by the above-mentioned method. The results are also shown in Tables 1 and 2.

[0027]

[Table 1] ──────────────────────────────── Example Component / sample name ─────── １ 1 2 3 4 5 ──────────────────────────────── Loquat extract 1.0 1.0 1.0 1.0 1.0 Glycyrrhetic acid 0.05----Alanine betaine-1.0---Berberine--0.1--Burdock extract---0.2-Tranexamic acid----0.5 Sorbitol (70%) 3.0 3.0 3.0 3.0 3.0 Glycerin 5.0 5.0 5.0 5.0 5.0 POE (60) hydrogenated castor oil derivative 0.5 0.5 0.5 0.5 0.5 Ethanol 20.0 20.0 20.0 20.0 20.0 Purified water Residue Residue Residue Residue ───────────────────性 Usefulness ◎ ◎ ◎ ◎ ◎ ────────────────────────────── ─

[0028]

[Table 2] ───────────────────────────────── Comparative example Component / sample name ────── ───────────── 1 2 3 4 5 6 ─────────────────────────────── ── Loquat extract − − − − − 1.0 Glycyrrhetinic acid 0.05 − − − − − Alanine betaine − 1.0 − − − − − Berberine − − 0.1 − − − Burdock extract − − − 0.2 − − Tranexamic acid − − − − 0.5 − Sorbitol (70%) 3.0 3.0 3.0 3.0 3.0 3.0 Glycerin 5.0 5.0 5.0 5.0 5.0 5.0 POE (60) hydrogenated castor oil derivative 0.5 0.5 0.5 0.5 0.5 0.5 Ethanol 20.0 20.0 20.0 20.0 20.0 20.0 Purified water Residual Residual Residual Residual有用 Utility ○ △ △ × △ ○ ─────── ─────────────────────────

As shown in Tables 1 and 2, the loquat extract and keratin softening / peeling action, anti-inflammatory action, antibacterial / bactericidal action,
The external preparation for skin of the present invention, which contains a component having a sebum suppressing / absorbing action and an anti-skin roughening action, was more excellent in acne treatment effect than the lotion of each comparative example.

Examples of the external preparations for acne according to the present invention in various dosage forms are shown below. The external preparations for skin in each example were produced by a conventional method according to the specific dosage form. When the above-mentioned tests and evaluations were performed on the external preparations obtained in each of the examples, all the above-mentioned evaluations of the usefulness were “性”.

Example 6 Lotion (1) Lysine betaine 1.0% by weight (2) Peony extract 0.5 (3) Antipine 0.05 (4) Glycerin 4.0 (5) Loquat extract 1.0 ( 6) Photosensitizer 201 0.001 (7) 1,3-butylene glycol 4.0 (8) Ethanol 7.0 (9) Polyoxyethylene oleyl alcohol 0.5 (10) Methylparaben 0.05 (11) Citric Acid 0.01 (12) Sodium citrate 0.1 (13) Fragrance 0.05 (14) Purified water residue

Example 7 Cream (1) 3.5% by weight of cetostearyl alcohol (2) Squalane 40.0 (3) Beeswax 3.0 (4) Reduced lanolin 5.0 (5) Ethylparaben 0.3 (6) ) Polyoxyethylene (20) Sorbitan monopalmitate 2.0 (7) Stearic acid monoglyceride 2.0 (8) Fragrance 0.03 (9) Tranexamic acid hexylamide 5.0 (10) Loquat extract 2.0 (11) Sulfur 0.3 (12) Allantoin 0.05 (13) Arginine hydrochloride 0.5 (14) Pyridoxal phosphate 0.1 (15) Ornithine betaine 0.05 (16) 1,3-butylene glycol 5. 0 (17) Glycerin 5.0 (18) Purified water residue

Example 8 Emulsion (1) Tranexamic acid hydrochloride 1.0% by weight (2) Burdock extract 1.5 (3) Alanine betaine 0.05 (4) Stearic acid 1.5 (5) Cetyl alcohol 5 (6) beeswax 2.0 (7) loquat extract 1.0 (8) oak extract 0.1 (9) menthol 0.01 (10) polyoxyethylene (10) monooleate 1.0 (11) ) Glycerin monostearate 1.0 (12) Propylene glycol 5.0 (13) Ethanol 3.0 (14) Ethylparaben 0.3 (15) Fragrance 0.03 (16) Purified water residue

Example 9 Ointment (1) n-hexyl tranexamic acid hydrochloride 1.0% by weight (2) pyridoxine glycyrrhizinate 1.0 (3) γ-butyrobetaine 0.1 (4) stearyl alcohol 18.0 ( 5) Loquat extract 1.0 (6) Mokuro 20.0 (7) Polyoxyethylene (10) monooleate 0.25 (8) Glycerin monostearate 0.25 (9) Vaseline 40.0 ( 10) Purified water residue

Example 10 Pack (1) Acetamide 1.0% by weight (2) Pyridoxine tripalmitate 1.5 (3) Phenylalanyl betaine 0.1 (4) Polyvinyl alcohol 15.0 (5) Polyethylene glycol 3 0.0 (6) Loquat extract 2.0 (7) Ibuprofen piconol 0.01 (8) Zinc white 1.0 (9) Propylene glycol 7.0 (10) Ethanol 10.0 (11) Methyl paraben 0.05 (12) Fragrance 0.05 (13) Purified water residue

Example 11 Solid White Powder (1) 85.4% by weight of talc (2) Stearic acid 1.5 (3) Lanolin 5.0 (4) Squalane 5.0 (5) Sorbitan sesquioleate 2.0 (6) triethanolamine 1.0 (7) loquat extract 0.1 (8) p-aminomethylbenzoic acid 1.0 (9) pyridoxine dicaprylate 0.1 (10) betaine glutamate 0.1 (11) Pigment appropriate amount (12) Flavor appropriate amount

[0037]

As described above, according to the present invention,
It is possible to provide a skin external preparation having an excellent acne treatment effect.

Claims (6)

[Claims] 1. A composition comprising a loquat extract and one or more selected from the group consisting of keratin softening and exfoliating agents, anti-inflammatory agents, antibacterial and bactericidal agents, sebum suppressing and absorbing agents, and protease inhibitors. A topical skin preparation for acne. 2. The external preparation for acne according to claim 1, wherein the exfoliating and exfoliating agent is at least one of betaines, sulfur, selenium disulfide, salicylic acid, urea and their derivatives and salts. 3. The anti-inflammatory agent is glycyrrhizic acid, glycyrrhetinic acid, allantoin, indomethacin, epsilon aminocaproic acid, butyl flufenamic acid, azulene, camphor, zinc chloride, zinc white, menthol, ibuprofen piconol, mefenamic acid and derivatives thereof. The external preparation for acne according to claim 1, which is at least one of a salt and a salt. 4. An antibacterial / bactericidal agent comprising sulfur, hinokitiol, triclosan, trichlorocarbanilide, chlorhexidine hydrochloride, chlorhexidine gluconate, halocarban, chlorophenesin, benzethonium chloride, benzalkonium chloride, lysozyme chloride, hydrochloric acid An alkyl diaminoethyl glycine, isopropyl methyl phenol, benzoic acid, photosensitizer 201, thymol, hexachlorophen, berberine, thioxolone, saxifraga extract, oak extract, ogu extract, and derivatives and salts thereof. An external preparation for acne according to the above. 5. The sebum-suppressing / absorbing agent comprises burdock extract, oil-soluble burdock extract, peony extract, sage extract,
Calendula, bollige extract, cornflower extract, pyridoxine hydrochloride, pyridoxine dicaprylate, pyridoxine dipalmitate, pyridoxine glycyrrhizinate, pyridoxine dilaurate, pyridoxine tripalmitate, pyridoxal phosphate, HP-β-CD,
2. The external preparation for acne according to claim 1, which is at least one of mica, pearl, talc, iron oxide, titanium oxide and their derivatives and salts. 6. The protease inhibitor may be tranexamic acid, guanidinobenzoic acid, p-aminomethylbenzoic acid,
Guanidine, acetamide, benzamidine, antipine, plasminostreptin, leupeptin, aprotinin, bovine pancreatic basic trypsin inhibitor, soybean trypsin inhibitor, corn protease inhibitor, lima bean protease inhibitor and at least one of their derivatives and salts. The skin external preparation for acne according to claim 1.