JPH1179937A - Skin lotion for pimple treatment - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a pimple-treating/preventing agent excellent in a pimple- treating preventing effect by including L-ornithine. SOLUTION: This agent comprises one or more kinds of L-ornithine shown by the formula and/or its salts (hydrochloride, hydrosulfate, metal salts of Mg, Ca, K, etc., salts of other amino acids such as aspartic acid). The agent is obtained by including 0.005 to 20.0 wt.%, pref. 0.01 to 10.0 wt.% of the above any compounds, optionally formulating an aqueous component, oil component, powder component, alcohol, moisture-holding agent, thickener, ultraviolet ray absorbent, bleaching agent, preservatives, antioxidant, surface active agent, perfume, coloring agent, various nutritive agents for skin, etc., with the compounds.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an acne-improving / preventing agent and an external acne-improving skin preparation containing the same. More specifically, an acne ameliorating / preventing agent containing one or more of L-ornithine and / or its salts as an active ingredient, and a combination thereof to promote the recovery of acne and to reduce acne / pimples The present invention relates to a skin external preparation for acne improvement having an improving and preventing 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, which is clinically defined as a chronic inflammatory change that occurs in the pores mainly in the pilosebaceous system. Have been.

[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, an anti-inflammatory ingredient, etc., corresponding to each of 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 decrease sebum secretion, but the side effects caused by this kind of hormone 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 side effects like the above-mentioned female hormones. May cause.

Further, crude drugs such as pyridoxine hydrochloride, peony extract, and burdock extract having sebum-suppressing action, and Maikaika having a sebum-absorbing action, have a sufficient sebum-inhibiting and absorbing effect even when used alone in a cream or ointment. 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 can exert extremely high bactericidal activity against propionibacterium acnes, which is a resident bacterium in the skin, but they are actually incorporated into creams and ointments. Most do not exhibit the expected therapeutic effect when used in acne treatment.

[0010] In view of the above circumstances, the present inventors have conducted intensive studies on substances having an acne-improving / preventing effect, and
The present inventors have found a new finding that L-ornithine or a salt thereof has an excellent acne-improving / preventing effect, and have completed the present invention.

An object of the present invention is to provide a novel acne improving / preventing agent and an external skin preparation for acne improvement containing the same as an active ingredient.

[0012]

That is, the present invention provides an L
-It provides an acne-improving / preventive agent comprising one or more of ornithine and / or salts thereof.

[0013] The present invention also provides an external preparation for acne improvement characterized by containing one or more of L-ornithine and / or salts thereof as an active ingredient.

Further, the present invention is characterized in that the content of L-ornithine or a salt thereof is 0.005 to 20.0% by weight based on the total amount of the external preparation for acne improvement. And a skin external preparation.

[0015]

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS The configuration of the present invention will be described below in detail.

L-Ornithine used in the present invention is a substance represented by the following chemical formula, which is a non-protein basic amino acid, and is known to be present in the stratum corneum of the epidermis as a component of a natural moisturizing component. ing.

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The salts of L-ornithine used in the present invention include, as those usually used, hydrochlorides, sulfates,
Examples include metal salts such as Mg, Ca, and K, and salts with other amino acids such as aspartic acid, but the present invention is not limited to these.

In the present invention, the above-mentioned L-ornithine,
Alternatively, one or two or more salts thereof may be arbitrarily selected and used. The amount of the salt to be added to the external preparation for acne improvement is preferably 0.005 to 20.0% by weight based on the total amount of the external preparation. 01 to 10.0% by weight is more preferred. 0.
If the content is less than 005% by weight, no sufficient acne-improving / preventing effect is exhibited, and even if 10.0% by weight or more is added, the effect is not so greatly improved.

Examples of application of L-ornithine to external preparations for skin or cosmetics are disclosed in JP-A-52-156787 and JP-A-1-928.
No. 5, JP-A-6-32718, etc., but basic amino acids containing mainly L-ornithine have been used because they are excellent in stabilizing preparations or other active ingredients. It's just

In Japanese Patent Application Laid-Open No. 6-279227,
It is described that by using trehalose and one or more amino acids in combination, it is possible to provide stable external preparations and cosmetics having the effects of improving rough skin, healing wounds, and preventing skin aging and having stable effects.

However, there is no report that L-ornithine or a salt thereof promotes the recovery of acne and has an excellent effect of improving or preventing acne. The present invention relates to the fact that L-ornithine or a salt thereof has the above effect. Is a use invention that has been completed as a result of newly discovering.

In addition to the above-mentioned essential components, the skin external preparation for acne improvement 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, alcohols, and moisturizers. Agents, thickeners, UV absorbers,
A whitening agent, a preservative, an antioxidant, a surfactant, a fragrance, a coloring agent, various skin nutrients, and the like can be appropriately blended as necessary, and can be produced by a conventional method according to the dosage form.

The skin external preparation for acne improvement of the present invention refers to a cosmetic, pharmaceutical or quasi-drug applied to the outer skin for the purpose of acne improvement and prevention, for example, ointments, creams, emulsions, lotions and the like. , Packs, bath agents, etc.
Conventionally, any type may be used as long as it is used for an external preparation for skin, and the dosage form is not particularly limited.

[0024]

EXAMPLES Next, the present invention will be described in detail with reference to examples, but it goes without saying that the technical scope of the present invention is not limited to these examples. The compounding amount is% by weight.

Based on the formulation shown in Table 1, a skin external preparation for acne improvement was produced by a conventional method, and the following actual use test was carried out to measure the acne improvement effect. The results are shown in "Table 1".

Object of use: 40 men and women (20 per group) suffering from acne from 16 to 24 years old. Method of use and date of observation: After thoroughly washing the face with toilet soap, apply each skin external preparation only on the rash 2 times a day.
3 times, and the affected area was observed 4 weeks later. Evaluation of overall improvement: The symptoms were classified 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. Usefulness judgment: A: Out of 20 persons (a) in the overall improvement degree evaluation, 15 or more persons. ：: 10 to 14 (a) out of 20 persons in the overall improvement degree evaluation
Name. Δ: 5 to 9 out of 20 persons (a) in the overall improvement degree evaluation. X: (a) out of 20 persons in the overall improvement degree evaluation was 4 persons or less.

[0027]

[Table 1]------------------------------------------------] -----------Ingredients Example 1 Comparative example 1 -L-ornithine hydrochloride 3.0-glycerin 1.0 1.0 1,3-butylene glycol 4.0 4.0 ethanol 7.0 7.0 citric acid 0.15 0.15 Polyoxyethylene (20 moles) Oleyl alcohol 0.5 0.5 Purified water Residue Residue ------------------------------ -1-1 group ◎ × 2 groups ◎ ×---------------------------- ----------------------------------- Over over over over over over over over over over over over over over over over

As is clear from Table 1, the skin external preparation for improving acne of Example 1 in which L-ornithine hydrochloride was blended exhibited an excellent effect of preventing acne.

Other examples of the external preparation for acne improvement according to the present invention will be described below, all of which have excellent acne improvement and prevention effects.

Example 2 Cream (Formulation) Weight% Stearic Acid 5.0 Stearyl Alcohol 4.0 Isopropyl Myristate 18.0 Glycerin Monostearate 3.0 Propylene Glycol 10.0 L-Ornithine Aspartate 0 .1 Caustic potash 0.2 Sodium bisulfite 0.01 Preservatives Appropriate amount Fragrance Appropriate amount Ion-exchanged water Residue (Preparation method) Add propylene glycol, L-ornithine aspartate and caustic potash to ion-exchanged water, heat, and heat to 70 ° C. Keep (aqueous phase). The other components are mixed, melted by heating 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. Then, homogenize uniformly with a homomixer,
Cool to 30 ° C with good stirring.

Example 3 Cream (Prescription)% by Weight Stearic Acid 2.0 Stearyl Alcohol 7.0 Hydrogenated Lanolin 2.0 Squalane 5.0 2-Octyldodecyl Alcohol 6.0 Polyoxyethylene (25 mol) Cetyl Alcohol ether 3.0 Glycerin monostearate 2.0 Propylene glycol 5.0 L-ornithine 1.0 Tranexamic acid 0.2 Sodium bisulfite 0.03 Ethyl paraben 0.3 Perfume Appropriate amount Ion exchange water Residue (Preparation method) Ion Add L-ornithine, tranexamic acid, and propylene glycol to the exchanged water, and heat to maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). Add the oil phase to the water phase, pre-emulsify, homogenize with a homomixer, and stir well at 30 ° C.
Cool down to

Example 4 Cream (Formulation) Weight% Solid paraffin 5.0 Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) Sorbitan monolauryl Acid ester 2.0 Soap powder 0.1 Borax 0.2 L-ornithine hydrochloride 3.0 Sodium bisulfite 0.03 Ethyl paraben 0.3 Perfume Appropriate amount Ion exchange water Residue (Production method) L-ornithine hydrochloride in ion exchange water Add salt, soap powder, borax and heat to maintain at 70 ° C (aqueous phase). The other components are mixed, melted by heating 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 is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well.

Example 5 Emulsion (Formulation) Weight% Stearic acid 2.5 Cetyl alcohol 1.5 Vaseline 5.0 Liquid paraffin 10.0 Polyoxyethylene (10 mol) Monooleate 2.0 Polyethylene glycol 1500 3.0 Triethanolamine 1.0 Carboxyvinyl polymer 0.05 (Product name: Carbopol 941, BFGoodrich Chemical company) L-Ornithine potassium salt 0.01 Sodium bisulfite 0.01 Ethyl paraben 0.3 Fragrance Appropriate ion exchange Water residue (Preparation method) Dissolve the carboxyvinyl polymer in a small amount of ion-exchanged water (phase A). Polyethylene glycol 1500 and triethanolamine, L-
Ornithine potassium salt is added, and the mixture is heated and dissolved and kept at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, pre-emulsification is performed, phase A is added, and the mixture is uniformly emulsified with a homomixer. After the emulsification, the mixture is cooled to 30 ° C. while stirring well.

Example 6 Emulsion (Formulation)% by weight Microcrystalline wax 1.0 Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 Mol) sorbitan monooleate 1.0 propylene glycol 7.0 L-ornithine hydrochloride 5.0 tranexamic acid methylamide 1.0 sodium bisulfite 0.01 ethyl paraben 0.3 perfume appropriate amount ion exchange water residue (production method) ion Add L-ornithine hydrochloride, tranexamic acid methylamide, and propylene glycol to the exchange water,
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The aqueous phase is gradually added while stirring the oil phase, and after uniform emulsification with a homomixer,
Cool to 30 ° C with good stirring.

Example 7 Jelly (Formulation) Weight% 95% Ethyl alcohol 10.0 Dipropylene glycol 15.0 Polyoxyethylene (50 mol) Oleyl alcohol ether 2.0 Carboxyvinyl polymer 0.05 (Product name: Carbopol 940, BFGoodrich Chemical company) Caustic soda 0.15 L-ornithine 0.1 Sodium bisulfite 0.01 Ethyl paraben 0.3 Perfume Appropriate amount Ion-exchange water Residue (Preparation method) Carbopol 940 is uniformly dissolved in ion-exchange water , Polyoxyethylene (50 mol) oleyl alcohol ether is added to the aqueous phase. Next, after adding other components, the mixture is neutralized with caustic soda and L-ornithine to increase the viscosity.

Example 8 Jelly (Formulation) Weight% (A phase) 95% Ethyl alcohol 10.0 Polyoxyethylene (20 mol) Octyldodecanol 1.0 Pantothenyl ethyl ether 0.1 Methyl paraben 0.15 ( (B phase) Potassium hydroxide 0.1 (C phase) Glycerin 5.0 Dipropylene glycol 10.0 Sodium bisulfite 0.03 L-ornithine magnesium salt 0.05 Carboxyvinyl polymer 0.2 (Product name: Carbopol 940 BF Goodrich Chemical company) 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 is added, filling is performed.

Example 9 Pack (Formulation) Weight% (A phase) Dipropylene glycol 5.0 Polyoxyethylene (60 mol) Hardened castor oil 5.0 (B phase) Olive oil 5.0 Tocopherol acetate 0.2 Ethylparaben 0.2 Fragrance 0.2 (Phase C) L-Ornithine sulfate 0.3 Sodium bisulfite 0.03 Polyvinyl alcohol 13.0 (Saponification degree 90, Degree of polymerization 2,000) Ethyl alcohol 7.0 Ion exchange 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 to this, filling is performed.

[0038] (Preparation method) Powder components of talc to black iron oxide are sufficiently mixed in a blender, and squalane to an oil component of isocetyl octanoate, L-ornithine glutamate, a preservative,
After adding a flavor and kneading well, the mixture is filled into a container and molded.

[0039] (Preparation method) After heating and stirring the aqueous phase, a powder portion sufficiently mixed and pulverized is added and homogenized. Further, the oil phase mixed by heating is added, and the mixture is treated with a homomixer. Then, a fragrance is added with stirring, and the mixture is cooled to room temperature.

[0040]

According to the present invention, it is possible to provide an external preparation for acne improvement which is excellent in the effect of improving and preventing acne.

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

Claims (3)

[Claims] 1. An acne ameliorating / preventing agent comprising one or more of L-ornithine and / or salts thereof. 2. An external preparation for acne improvement, comprising one or more of L-ornithine and / or salts thereof as an active ingredient. 3. The content of L-ornithine or a salt thereof is 0.005 to 0.005 relative to the total amount of the external preparation for acne improvement.
The external preparation for acne improvement according to claim 2, which is 20.0% by weight.