JP6185278B2 - Composition for external use - Google Patents

Description

  The present invention relates to a composition for external use containing propynyl butylcarbamate, an oily gelling agent and an oil. More specifically, by adding propynyl iodide butylcarbamate and an oily gelling agent to the oil, it has a high antiseptic effect and increases the hardness of the composition for external use. Therefore, the present invention has less irritation. It is a composition for external use having excellent usability and formulation stability.

  Cosmetics and other external compositions are contaminated with various germs, etc., during the distribution stage from production to the user's hand, or while being used in the user's hand, resulting in deterioration of the product There is. In order to prevent contamination by such germs, a preservative such as paraben is usually blended. In addition, since there are many scenes where the required antiseptic effect differs depending on the pH of the composition for external use, the situation in which the composition is used, and the type and blending amount of the coexisting components, a plurality of preservatives are used in combination. There is a case.

Here, with regard to propynyl butylcarbamate, which is known as a preservative that can be blended in such an external composition, 2-methylisothiazolin-3-one and 5-chloro-2-methyl, which are bactericides, are further used. A technique for improving the antiseptic effect by combining with isothiazoline-3-one (Patent Document 1), a technique for improving the antiseptic effect by combining with an antibacterial cationic polymer (Patent Document 2), and a dihydric alcohol. A technique for improving the antiseptic effect by combining with 1,2-hexanediol, 1,2-octanediol or 1,2-decanediol (Patent Document 3) has been reported.
However, some preservatives may have a limited amount added to the composition from the viewpoint of irritation, and the composition is good while ensuring sufficient antiseptic effect and formulation stability. There was a problem that it was difficult to give a feeling of use.

  In addition, an oily gelling agent may be blended in the external composition in order to improve the shape, feel and formulation stability of the composition. For example, lip composition such as solid or paste containing a large amount of oil, oil-in-water composition such as emulsion or cream in which oil is dispersed in water, or water dispersed in oil The oily gelling agent is used for a water-in-oil type external composition such as a milky liquid or cream, or a liquid or gel oil cleansing blended with a large amount of oil.

Oily gelling agents are known to have problems such as insufficient thickening when blended into an external composition, brittle mass due to interaction with coexisting components, and poor usability. Yes. In particular, in products such as lip cosmetics that are molded into a stick and are repeatedly used from a container, it is important to ensure the formability of the preparation and the shape retention that can maintain the shape during the period of use.
In order to solve such problems, a technique for improving gel performance by adding a block-type alkylene oxide derivative to an external composition containing an oily gelling agent has been reported (Patent Document 4). However, there is no description of adding propynyl butylcarbamate propylene to an external composition containing an oily gelling agent, and sufficient satisfaction may not be obtained in terms of use feeling, formulation stability, etc. There was still room for improvement.

JP-T-2002-523339 Special table 2009-513650 gazette Japanese translation of PCT publication No. 2008-517037 JP 2010-100555 A

  In the present invention, in view of the above-mentioned problems, the composition for external use has good usability and formulation stability by reducing irritation and increasing hardness while ensuring a high antiseptic effect. Another object is to provide a composition for external use. Furthermore, the present invention provides an external composition having a high shape-retaining property by increasing hardness in the above composition, particularly in a stick-shaped external composition that can be repeatedly used by being drawn out of a container. Objective.

  As a result of intensive studies to solve the above problems, the present inventors have added propynyl butyl carbamate and an oily gelling agent to the oil agent, and in addition, a synergistically high antiseptic effect can be obtained, and an external composition Since the hardness of the product also increases, it has been found that an external composition having little irritation and good usability and formulation stability can be obtained. That is, since a high antiseptic effect can be obtained synergistically, the content of propynyl butylcarbamate and oily gelling agent in the composition can be reduced, and the hardness of the composition is also increased synergistically. Therefore, even when applied to the application site, it has good adhesion, it is easy to apply and has a good feeling of use, and when it is molded into a stick shape, it can be fed out of the container even during use The inventors have found that a composition for external use having a preparation stability capable of stably maintaining a good appearance without causing breakage or peeling of the preparation can be obtained, and the present invention has been completed.

That is, the present invention includes the following components (A), (B) and (C):
(A) butyl carbamate propynyl iodide,
(B) Oily gelling agent (C) It is related with the composition for external use containing an oil agent.

The present invention also relates to an external composition in which the oily gelling agent of the component (B) is one or more selected from amino acid oily gelling agents and fatty acid dextrins.

  In the present invention, the amino acid oily gelling agent is at least one of lauroylglutamic acid stearylamide, N-lauroyl-L-glutamic acid dibutylamide, and N-2-ethylhexanoyl-L-glutamic acid dibutylamide. It relates to a composition for external use.

  The present invention also relates to an external composition, wherein the fatty acid dextrin is one or more of dextrin palmitate, dextrin myristate, or dextrin octanoate.

  The present invention also relates to a composition for external use, wherein the component (C) oil is one or more selected from hydrocarbon oils, ester oils, higher alcohols, and natural oils.

  The present invention also relates to an external composition for lips containing the components (A), (B) and (C).

  The present invention also relates to a stick-shaped external composition containing the components (A), (B) and (C).

The present invention also provides the components (A), (B) and (C):
(A) butyl carbamate propynyl iodide,
(B) It is related with the method of enhancing the antiseptic effect with respect to the fungus of an external composition by containing an oil-based gelling agent (C) oil agent.

The present invention also provides the components (A), (B) and (C):
(A) butyl carbamate propynyl iodide,
(B) Oily gelling agent (C) It is related with the method of increasing the hardness of an external composition by containing an oil agent.

  By including the component (A) propynyl iodide butylcarbamate, the component (B) oily gelling agent, and the component (C) oily agent, an external composition having a high antiseptic effect and less irritation can be obtained. Moreover, the composition for external use of this invention has the basic performance which was excellent in the usability | use_condition, formulation stability, etc. by the hardness of the composition for external use increased.

  In the present invention, the composition for external use means that applied to the skin, scalp, lips, etc., and contains 0 to 99.9% by weight of water, with the total weight of the composition for external use being 100% by weight. To do.

  The component (A) propynyl butylcarbamate is an antibacterial component exhibiting an antiseptic effect and is useful against bacteria or fungi.

Component (A) propynyl butylcarbamate is also called IPBC (3-iodo-2-propynylbutylcarbamate). Further, salts and derivatives of butyl carbamate propynyl iodide can be used in the same manner as butyl carbamate propynyl iodide. Preferably used is propynyl iodide butylcarbamate.
Examples of commercially available products include “GLYCASIL”, “GLYCASIL 2000”, “GLYCASIL L”, and “GLYCASIL S” (all manufactured by Lonza).

  The oily gelling agent of component (B) improves the feeling of use and formulation stability of the external composition by increasing the hardness of the external composition.

  Examples of the oily gelling agent of component (B) include lauroyl glutamic acid stearylamide, N-lauroyl-L-glutamic acid dibutylamide, N-2-ethylhexanoyl-L-glutamic acid dibutylamide, dicaproyllysine laurylamine salt , Dicaproyl lysine lauryl ester, dicaproyl lysine lauroyl phenylalanine lauryl amide, dibutylethylhexanoylglutamide and other amino acid oily gelling agents; palmitic acid dextrin, myristic acid dextrin, octanoic acid dextrin, (palmitic acid / ethylhexane Acid) fatty acid dextrins such as dextrin; inulin stearate; dibenzylidene sorbitol, tribenzylidene sorbitol, dibenzylidene xylitol, paramethoxybenzylidene Condensates of benzaldehydes such as bitol with pentavalent or higher alcohols; metal soaps such as calcium stearate, calcium palmitate, lithium 2-ethylhexanoate, aluminum 12-hydroxystearate; 12-hydroxystearic acid; glycerin and behen Examples include, but are not limited to, oligomers obtained by condensing mixed fatty acids composed of acids and eicosane diacids; polyamide resins and the like.

  The oily gelling agent of component (B) is preferably an amino acid-based oily gelling agent or a fatty acid dextrin, more preferably an amino acid-based oily gelling, from the viewpoint of the usability of the composition for external use and the stability of the preparation. It is an agent.

  As the amino acid-based oily gelling agent, lauroyl glutamic acid stearylamide, N-lauroyl-L-glutamic acid dibutylamide, N-2-ethylhexanoyl-L-glutamic acid are used from the viewpoint of the feeling of use of the composition for external use and the stability of the preparation. Dibutylamide is preferred, and N-lauroyl-L-glutamic acid dibutylamide is more preferred.

  As the fatty acid dextrin, dextrin palmitate, dextrin myristate, and dextrin octanoate are preferable, and dextrin palmitate is more preferable from the viewpoint of the usability of the composition for external use and the stability of the preparation.

The component (B) used in the present invention is not particularly limited as long as it is generally used in the pharmaceutical, quasi-drug or cosmetic field, and two or more kinds may be used in combination.
For example, as a commercially available product, a trade name “GP-1 (component name; N-lauroyl-L-glutamic acid dibutylamide)” (manufactured by Ajinomoto Co., Inc.), a trade name “EB-1 (component name; N-2-ethylhexa) Noyl-L-glutamic acid dibutylamide) ”(manufactured by Ajinomoto Co., Inc.), trade name“ Leopard KL2 (display name: dextrin palmitate) ”(manufactured by Chiba Flour Mills), trade name“ Leopard TL2 (display name: dextrin palmitate) ” (Made by Chiba Flour Mills), trade name “Leopard MKL2 (display name: dextrin myristate)” (produced by Chiba Flour Mills), trade name “Leopard TT2 (display name: dextrin palmitate / dextrin octanoate)” (Chiba Flour Mills) ), Trade name “Leopard ISK2 (display name: inulin stearate)” (manufactured by Chiba Flour Mills), trade name “HI Rate PAM (component name; polyamide resin) "(manufactured by Higher Alcohol Industry Co., Ltd.), trade name" Silva Clear A200V component name; polyamide resin "(Arizona Chemical Co., Ltd.), trade name" Silva Clear A2614V component name; polyamide resin) "(Manufactured by Arizona Chemical Co., Ltd.), trade name" Versamide 930 component name; polyamide resin "(manufactured by Cognis) GP-1, Leopard KL2, and Leopard MKL2 are preferable, and GP-1 is more preferable.

  The oil agent of component (C) is used to dissolve propynyl butylcarbamate iodide of component (A) and oily gelling agent of component (B).

  Examples of the component (C) oil include hydrocarbon oils, ester oils, higher alcohols, silicone oils, higher fatty acids, natural oils such as animal and vegetable oils and essential oils. From the viewpoint of the feeling of use of the composition for external use and the stability of the preparation, hydrocarbon oils, ester oils, higher alcohols and natural oils are preferable, and hydrocarbon oils and higher alcohols are more preferable.

  As the hydrocarbon oil, paraffinic hydrocarbons and olefinic hydrocarbons are used, for example, squalane, squalene, ceresin, paraffin, pristane, microcrystalline wax, liquid paraffin, petrolatum, hydrogenated polyisobutene, light liquid paraffin, etc. It is done. Preferred are liquid paraffin, petroleum jelly, hydrogenated polyisobutene, and light liquid paraffin.

  As ester oils, synthetic esters, esters of higher alcohols and higher fatty acids are used, for example, diisobutyl adipate, 2-hexyldecyl adipate, di-2-heptylundecyl adipate, isostearyl isostearate, Trimethylolpropane triisostearate, cetyl 2-ethylhexanoate, neopentyl glycol di-2-ethylhexanoate, trimethylolpropane tri-2-ethylhexanoate, pentaerythritol tetra-2-ethylhexanoate, cetyl octanoate, Oleyl oleate, octyldodecyl oleate, decyl oleate, neopentyl glycol dicaprate, 2-ethylhexyl succinate, isocetyl stearate, butyl stearate, diisopropyl sebacate, cetyl lactate Tetradecyl lactate, octyl dodecyl lactate, isopril pyr myristate, octyl dodecyl myristate, cetyl myristate, myristyl myristate, octyl palmitate, 2-ethylhexyl palmitate, 2-hexyldecyl palmitate, 2-heptyl undecyl palmitate, Cholesteryl 12-hydroxystearate, phytosteryl oleate, diisostearyl malate, pentaerythritol tetrarosinate, dimer dilinoleyl diisostearate, dimer dilinoleate (isostearyl / phytosteryl), dimer dilinoleyl dimer dilinoleate , Dimer dilinoleyl hydrogenated rosin condensate, dimer dilinoleic acid (phytosteryl / isostearyl / cetyl / stearyl / behenyl), dimer dilinol Die merge linoleyl bis (phytosteryl / behenyl / isostearyl), triisostearate Polyglyceryl-2 and the like. Preferred are cetyl 2-ethyl hexanoate, diisostearyl malate, dimer dilinoleyl dimer dilinoleate, and polyglyceryl-2 triisostearate.

  Examples of the higher alcohol include octyldodecanol, isostearyl alcohol, oleyl alcohol, stearyl alcohol, cetanol, behenyl alcohol, lanolin alcohol, and the like. Preferably, it is octyldodecanol or isostearyl alcohol.

  Examples of the silicone oil include higher alkoxy-modified silicones such as dimethylpolysiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane, octamethylcyclotetrasiloxane, octamethylcyclopentasiloxane, decamethylcyclohexasiloxane, stearoxysilicone, Examples include alkyl-modified silicones and higher fatty acid ester-modified silicones.

  As the higher fatty acid, a saturated or unsaturated linear or branched fatty acid having 12 to 22 carbon atoms can be used. For example, isostearic acid, oxystearic acid, oleic acid, stearic acid, palmitic acid, behenic acid, Examples include myristic acid, lauric acid, lanolinic acid, linoleic acid, and linolenic acid.

  Examples of natural oils include avocado oil, linseed oil, almond oil, olive oil, cacao oil, beef tallow, giraffe oil, wheat germ oil, sesame oil, rice germ oil, rice bran oil, safflower oil, soybean oil, evening primrose oil, camellia oil Oil, corn oil, rapeseed oil, horse fat, persic oil, palm oil, palm kernel oil, castor oil, sunflower oil, pork fat, grape oil, jojoba oil, macadamia nut oil, mink oil, meadow foam oil, cottonseed oil, molasses, Examples include coconut oil, hydrogenated coconut oil, peanut oil, lanolin, egg yolk oil, and rosehip oil. Avocado oil, jojoba oil, grape oil, lanolin, evening primrose oil, macadamia nut oil, and meadow foam oil are preferable.

  Since the composition for external use containing the component (A) propynyl iodide butylcarbamate, the component (B) oily gelling agent, and the component (C) oily agent of the present invention has a synergistically high antiseptic effect, the composition for external use The content of component (A) propynyl iodide butylcarbamate can be reduced.

The content of the component (A) of the present invention is preferably 0.00001% by weight or more, more preferably 0.0001% by weight or more, further preferably 0.001% by weight or more based on the total amount of the composition for external use. is there. If it is 0.00001 wt% or more, a sufficient antiseptic effect can be obtained.
The content of component (A) is preferably 0.1% by weight or less, more preferably 0.05% by weight or less, and still more preferably 0.03% by weight or less. If it is 0.1% by weight or less, an external composition having a sufficient antiseptic effect and low irritation can be obtained.

  The content of the component (A) of the present invention is preferably 0.00001 wt% or more and 0.1 wt% or less, more preferably 0.0001 wt% or more and 0.05 wt% with respect to the total amount of the composition for external use. % By weight or less, more preferably 0.001% by weight or more and 0.03% by weight or less.

  The composition for external use containing the component (A) propynyl iodide butylcarbamate, the component (B) oily gelling agent, and the component (C) oily agent of the present invention synergistically increases the hardness, Since the content of the component (B) oily gelling agent in the composition can be reduced, a good feeling of use can be obtained.

The content of the component (B) of the present invention is preferably 0.1% by weight or more, more preferably 0.5% by weight or more, and further preferably 1% by weight or more based on the total amount of the composition for external use. If it is 0.1 weight% or more, the composition for external use which has sufficient antiseptic effect and hardness can be obtained.
The content of component (B) is preferably 20% by weight or less, more preferably 15% by weight or less, and still more preferably 10% by weight or less. If it is 20% by weight or less, a composition for external use having good feeling in use or stability of preparation can be obtained.
When the component (B) is N-lauroyl-L-glutamic acid dibutylamide, the content is preferably 0.1% by weight or more, more preferably 0.5% by weight or more, and more preferably 0.5% by weight or more, based on the total amount of the composition for external use. Preferably it is 1 weight% or more. If it is 0.1% by weight or more, sufficient hardness can be obtained.
The content of component (B) is preferably 10% by weight or less, more preferably 7.5% by weight or less, and still more preferably 5% by weight or less. If it is 10 weight% or less, the composition for external use with a feeling of use or good formulation stability is obtained.

The content of the component (B) of the present invention is preferably 0.1% by weight or more and 20% by weight or less, more preferably 0.5% by weight or more and 15% by weight or less with respect to the total amount of the composition for external use. More preferably 1% by weight or more and 10% by weight or less.
When the component (B) is N-lauroyl-L-glutamic acid dibutylamide, the content is preferably 0.1% by weight or more and 10% by weight or less, more preferably 0.5% by weight based on the total amount of the composition for external use. It is not less than 7.5% by weight and more preferably not less than 1% by weight and not more than 5% by weight.

The content of the component (C) of the present invention is preferably 0.1% by weight or more, more preferably 0.5% by weight or more, and further preferably 1% by weight or more based on the total amount of the composition for external use. If it is 0.1 weight% or more, a component (A) butyl carbamate propynyl iodide can fully be dissolved.
The content of component (C) is preferably 99% by weight or less, more preferably 90% by weight or less, and still more preferably 80% by weight or less. If it is 99 weight% or less, the external composition of a favorable usability | use_condition is obtained.

  The content of the component (C) of the present invention is preferably 0.1 wt% or more and 99 wt% or less, more preferably 0.5 wt% or more and 90 wt% or less, with respect to the total amount of the composition for external use. More preferably 1% by weight or more and 80% by weight or less.

In the composition for external use of the present invention, the content ratio (A) / (B) of the component (A) and the component (B) is preferably 0.00001 or more, more preferably 0.0001 or more, and still more preferably. It is 0.0005 or more. If it is 0.00001 or more, sufficient antiseptic effect and hardness can be obtained.
Moreover, ratio (A) / (B) of content of a component (A) and a component (B) becomes like this. Preferably it is 2 or less, More preferably, it is 0.2 or less, More preferably, it is 0.02 or less. If it is 2 or less, an external composition with little irritation and good formulation stability or feeling in use can be obtained.

  In the composition for external use of the present invention, the content ratio (A) / (B) of the component (A) and the component (B) is preferably 0.00001 or more and 2 or less, more preferably 0.0001 or more and 0.2. Hereinafter, it is still more preferably 0.0005 or more and 0.02 or less.

The composition for external use of the present invention can be used for a product to be applied directly to an application site. Such a composition is stored in a stick-shaped feeding container, and an appropriate amount of the composition is delivered at the time of use, applied to the application site, applied, and after use, the delivered preparation is fed as it is and stored as needed. Because it is used in operation, a composition having formulation stability that can stably maintain a good appearance without causing formulation breakage or peeling even if it is used or unwound from a container is useful. is there.
In addition, when the composition for external use according to the present invention is used as, for example, a composition for lips, it is often applied by pressing the composition directly onto the lips and stored as it is without cleaning the coated surface. The composition according to the present invention, which is stored in a state where saliva or skin pieces and the like are attached to the composition and is more likely to propagate germs, can ensure a sufficient antiseptic effect at the time of use.
On the other hand, even if the composition for lips contains a large amount of an oil agent, it can be applied to the lips by adding an oily gelling agent to impart an appropriate viscosity to the composition or by making it solid. The effect of improving the retention of the composition, the effect of suppressing the phase separation and improving the stability of the preparation can be imparted.
Furthermore, the lip is a very sensitive part of the human body, and the applied composition may enter the oral cavity, so the blending of each component may be limited in terms of feeling of use and taste. For this reason, since preservative effect and hardness increase synergistically by blending component (A) propynyl iodide butylcarbamate and component (B) oily gelling agent, a viewpoint that these blending amounts can be suppressed. Therefore, the composition for external use according to the present invention is very useful.

  The composition for external use of the present invention can contain components generally used in the pharmaceutical, quasi-drug or cosmetic field within a quantitative and qualitative range that does not impair the effects of the present invention.

  The composition for external use of the present invention is various components generally used in the pharmaceutical, quasi-drug or cosmetic field, for example, surface activity within the quantitative and qualitative range without impairing the effects of the present invention. Agent, moisturizer, stabilizer, irritation reducer, blood circulation promoter, scrub agent, thickener other than component (B), preservative, antioxidant, colorant, pearlescent agent, dispersant, chelating agent , PH adjuster, fragrance, UV absorbing component, UV scattering component, cleaning component, antibacterial component other than component (A), anti-inflammatory component, astringent component, vitamins, peptide or derivative thereof, amino acid or derivative thereof, horny soft component A cell activation component can be blended. In addition, these components can be mix | blended combining 1 type single or 2 types or more arbitrarily. Furthermore, these components can be mixed with a known base or carrier according to a conventional method and blended into the external composition of the present invention, and the external composition of the present invention containing these components is produced. Can do.

  Examples of the surfactant include sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, diglycerol sorbitan penta-2-ethylhexylate, and diglycerol sorbitan tetra-2-ethylhexylate. Sorbitan fatty acid esters; propylene glycol fatty acid esters such as propylene glycol monostearate; polyoxyethylene hydrogenated castor oil 40 (HCO-40), polyoxyethylene hydrogenated castor oil 50 (HCO-50), polyoxyethylene hardened Hardened castor oil derivatives such as castor oil 60 (HCO-60), polyoxyethylene hydrogenated castor oil 80; polyoxyethylene (20) sorbitan (polysorbate 20) monolaurate, monostearate Polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene (20) sorbitan (polysorbate 60), polyoxyethylene monooleate (20) sorbitan (polysorbate 80), polyoxyethylene (20) sorbitan isostearate; Glyceryl alkyl ether; alkyl glucoside; polyoxyalkylene alkyl ether such as polyoxyethylene cetyl ether; amines such as stearylamine and oleylamine; polyoxyethylene / methylpolysiloxane copolymer; Examples thereof include silicone surfactants such as lauryl PEG-9 polydimethylsiloxyethyl dimethicone and PEG-9 polydimethylsiloxyethyl dimethicone.

Examples of humectants include polyhydric alcohols such as glycerin, 1,3-butylene glycol, propylene glycol, polyethylene glycol, and diglycerin trehalose; sodium hyaluronate, heparin analog, chondroitin sulfate sodium, collagen, elastin, keratin, Polymer compounds such as chitin and chitosan; amino acids such as glycine, aspartic acid and arginine; natural moisturizing factors such as sodium lactate, urea and sodium pyrrolidonecarboxylate; lipids such as ceramide, cholesterol and phospholipid; chamomile extract , Plant extract extracts such as hamamelis extract, tea extract and perilla extract.

  Examples of the stabilizer include sodium polyacrylate, dibutylhydroxytoluene, butylhydroxyanisole and the like.

  Examples of the irritation reducing agent include gum arabic, polyvinyl pyrrolidone, licorice extract, sodium alginate and the like.

  Examples of the blood circulation promoter include acetylcholine, ictamol, caffeine, capsaicin, cantalis tincture, gamma oryzanol, ginger tincture, gingeron, cephalanthin, assembly extract, tannic acid, red pepper tincture, trazoline, tocopherol nicotinate, benzyl nicotinate Examples include esters.

  Examples of scrubbing agents include apricot kernel powder, almond shell powder, apricot kernel powder, sodium chloride granules, olive kernel powder, dried seawater granules, candelilla wax, walnut shell powder, cherries kernel powder, coral powder, charcoal powder, Examples include hasp shell powder, polyethylene powder, and silicic anhydride.

  Examples of thickeners other than component (B) include guar gum, locust bean gum, carrageenan, xanthan gum, carboxymethylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinyl alcohol, polyvinylpyrrolidone, and carboxyvinyl polymer. , Alkyl methacrylate copolymer, polyethylene glycol, (hydroxyethyl acrylate / acryloyldimethyltaurine Na) copolymer, (acryloyldimethyltaurine ammonium / vinylpyrrolidone) copolymer, and the like.

  Preservatives include, for example, benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, benzyl paraoxybenzoate , Methyl paraoxybenzoate, phenoxyethanol and the like.

  Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, erythorbic acid, L-cysteine hydrochloride, and the like.

  Examples of the colorant include inorganic pigments and natural pigments.

  Examples of the pearl luster imparting agent include ethylene glycol distearate, ethylene glycol monostearate, and triethylene glycol distearate.

  Examples of the dispersant include sodium pyrophosphate, sodium hexametaphosphate, polyvinyl alcohol, polyvinyl pyrrolidone, methyl vinyl ether / maleic anhydride crosslinked copolymer, and organic acid.

  Examples of the chelating agent include EDTA · disodium salt and EDTA · calcium disodium salt.

  Examples of pH adjusters include inorganic acids (hydrochloric acid, sulfuric acid, etc.), organic acids or salts thereof (lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, sodium succinate, etc.), inorganic bases (potassium hydroxide). And sodium hydroxide), and organic bases (such as triethanolamine, diisopropanolamine, and triisopropanolamine).

  Examples of ultraviolet ray absorbing components include octyl triazone, diethylaminohydroxybenzoyl hexyl benzoate, dimethoxybenzylidene dioxoimidazolidine propionate octyl, paramethoxycinnamate 2-ethylhexyl, t-butylmethoxydibenzoylmethane, phenylbenzimidazole sulfonic acid, etc. Is mentioned.

  Examples of ultraviolet scattering components include hydrous silicic acid, zinc silicate, cerium silicate, titanium silicate, zinc oxide, zirconium oxide, cerium oxide, titanium oxide, iron oxide, silicic anhydride, and other inorganic compounds. Covered with inorganic powders such as hydrous silicic acid, aluminum hydroxide, mica and talc, compounded with resin powders such as polyamide, polyethylene, polyester, polystyrene and nylon, and with silicone oil and fatty acid aluminum salts, etc. Processed ones are listed.

  As washing components, soaps selected from alkali metal salts such as potassium laurate, potassium myristate, potassium palmitate or sodium stearate, alkanolamide salts or amino acid salts; amino acids such as cocoyl glutamate Na and cocoyl methyl taurine Na Surfactants; ether sulfates such as laureth sulfate Na; ether carboxylates such as lauryl ether acetate Na; sulfosuccinate esters such as alkylsulfosuccinate Na; coconut oil fatty acid monoethanolamide, coconut oil fatty acid Fatty acid alkanolamides such as ethanolamide; Monoalkyl phosphate salts such as sodium lauryl phosphate and polyoxyethylene lauryl ether sodium phosphate; Palm oil fatty acid amidopropyl Betaines such as methylaminoacetic acid betaine, lauryldimethylaminoacetic acid betaine, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, laurylhydroxysulfobetaine and lauroylamidoethylhydroxyethylcarboxymethylbetaine hydroxypropyl phosphate Type amphoteric surfactants; amino acid type amphoteric surfactants such as sodium laurylaminopropionate.

  Antibacterial components other than component (A) include chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, ethanol, benzethonium chloride, cresol, gluconic acid and its derivatives, popidone iodine, potassium iodide, iodine, isopropylmethylphenol, triclocarban, Examples include triclosan, photosensitizer 101, photosensitizer 201, paraben, phenoxyethanol, 1,2-pentanediol, alkyldiaminoglycine hydrochloride, pyroctoolamine, miconazole and the like.

  Examples of the anti-inflammatory component include glycyrrhetinic acid, glycyrrhizic acid derivatives, allantoin, azulene, aminocaproic acid, and hydrocortisone.

  Examples of the astringent component include zinc oxide, zinc sulfate, allantoin hydroxyaluminum, aluminum chloride, zinc sulfocolate and tannic acid.

  Vitamins such as dl-α-tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol succinate, dl-α-tocopherol calcium succinate; riboflavin, flavin mononucleotide, flavin adenine dinucleotide Vitamin B2 such as riboflavin butyrate, riboflavin tetrabutyrate, sodium riboflavin 5′-phosphate, riboflavin tetranicotinate; nicotinic acid dl-α-tocopherol, benzyl nicotinate, methyl nicotinate, β-nicotinic acid β- Nicotinic acids such as butoxyethyl and 1- (4-methylphenyl) ethyl nicotinate; ascorbigen-A, ascorbyl stearate, ascorbyl palmitate, dipalmitate -Vitamin Cs such as ascorbyl; Vitamin Ds such as methyl hesperidin, ergocalciferol and cholecalciferol; Vitamin Ks such as phylloquinone and farnoquinone, γ-oryzanol, dibenzoylthiamine, dibenzoylthiamine hydrochloride; thiamine hydrochloride , Thiamine cetyl hydrochloride, thiamine thiocyanate, thiamine lauryl hydrochloride, thiamine nitrate, thiamine monophosphate, thiamine lysine salt, thiamine triphosphate, thiamine monophosphate phosphate, thiamine monophosphate, thiamine diphosphate Vitamin B1 such as thiamine diphosphate hydrochloride, thiamine triphosphate, thiamine triphosphate monophosphate; pyridoxine hydrochloride, pyridoxine acetate, pyridoxal hydrochloride, 5'- Vitamin B6 such as pyridoxal phosphate and pyridoxamine hydrochloride; Vitamin B12 such as cyanocobalamin, hydroxocobalamin and deoxyadenosylcobalamin; Folic acid such as folic acid and pteroylglutamic acid; Nicotinic acids such as nicotinic acid and nicotinamide; Pantothenic acid Pantothenic acids such as calcium pantothenate, pantothenyl alcohol (panthenol), D-panthecine, D-panthetin, coenzyme A, pantothenyl ethyl ether; biotins such as biotin and bioticin; ascorbic acid, sodium ascorbate, Vitamin C which is an ascorbic acid derivative such as dehydroascorbic acid, sodium ascorbate phosphate, magnesium ascorbate phosphate; carnitine, ferulic acid, α-lipoic acid Such as vitamin-like effect factors such as orotic acid, and the like.

  Peptides or derivatives thereof include keratin-degrading peptide, hydrolyzed keratin, collagen, fish-derived collagen, atelocollagen, gelatin, elastin, elastin-degrading peptide, collagen-degrading peptide, hydrolyzed collagen, hydroxypropylammonium chloride hydrolyzed collagen, elastin-degrading peptide , Conchiolin degrading peptide, hydrolyzed conchiolin, silk proteolytic peptide, hydrolyzed silk, lauroyl hydrolyzed silk sodium, soy proteolytic peptide, hydrolyzed soy protein, wheat protein, wheat proteolytic peptide, hydrolyzed wheat protein, casein degrading peptide Acylated peptides (palmitoyl oligopeptide, palmitoyl pentapeptide, palmitoyl tetrapeptide, etc.).

  As amino acids or their derivatives, betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, β-alanine, threonine, glutamic acid, glutamine, asparagine, aspartic acid, cysteine, cystine, methionine Leucine, isoleucine, valine, histidine, taurine, γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, carnitine, carnosine, creatine and the like.

  Examples of the keratin soft component include lactic acid, salicylic acid, salicylic acid glycolic acid, gluconic acid, citric acid, malic acid, fruit acid, phytic acid, urea, and sulfur.

  Cell activation components include amino acids such as γ-aminobutyric acid and ε-aminocaproic acid: vitamins such as retinol, thiamine, riboflavin, pyridoxine hydrochloride and pantothenic acids: α-hydroxy acids such as glycolic acid and lactic acid: tannin, Examples include flavonoids, saponins, allantoin, and photosensitizer 301.

  The form of the composition for external use of the present invention may be a known form of pharmaceuticals, cosmetics or quasi-drugs, for example, liquids, suspensions, emulsions, creams, ointments, gels, liniments, Examples thereof include a sheet agent obtained by impregnating a chemical liquid into a sheet such as a lotion agent, an aerosol agent, a powder agent, a poultice agent, and a nonwoven fabric, and a stick agent such as a lipstick. Among them, preferably used are liquids, emulsions, creams, ointments, gels and sticks, and particularly preferably sticks.

  In addition, more detailed and specific forms of the composition for external use of the present invention include skin lotion, milky lotion, cream, serum, cosmetic for sunscreen, basic makeup such as pack, hand cream, body lotion and body cream. Cosmetics for cleaning such as facial cleansers, makeup removers, body shampoos, shampoos and rinses; makeup cosmetics such as foundations, makeup bases, lip balms, lipsticks and teak colors; bathing agents and the like. As a preferable form, it is used in the form of a lip balm, a cosmetic liquid or a makeup remover, and particularly preferably a lip balm.

The hardness at room temperature of the external composition of the present invention is preferably 1 g or more, more preferably 10 g or more, and even more preferably 100 g or more, when measured using a texture analyzer. If it is 1 g or more, formulation stability can be obtained.
Moreover, the hardness at room temperature of the external composition of the present invention is preferably 2000 g or less, more preferably 1000 g or less, and even more preferably 800 g or less when measured using a texture analyzer. If it is 2000 g or less, a formulation with a good feeling of use is obtained.

  The hardness at room temperature of the external composition of the present invention is preferably 1 g or more and 2000 g or less, more preferably 10 g or more and 1000 g or less, and even more preferably 100 g or more and 800 g or less when measured using a texture analyzer.

In addition, the present invention enhances the antiseptic effect of the composition for external use by adding propynyl iodide of component (A), oily gelling agent of component (B) and oil preparation of component (C) to the composition for external use. The method of making it.
Since propynyl iodide butylcarbamate exerts a preservative effect against contamination of the externally applied composition by bacteria or fungi, the externally applied composition whose antiseptic effect is enhanced by the method for enhancing antiseptic effect of the present invention is Contamination by fungi, preferably fungi, particularly preferably Candida albicans can be effectively suppressed.

The present invention also relates to a method for enhancing the hardness of an external composition by adding propynyl butylcarbamate iodide as component (A), an oily gelling agent as component (B), and an oil agent as (C) to the external composition. Is also included.
The kind of each component used for the hardness enhancement method, the method of using the external composition, its hardness, and the like are as described for the external composition of the present invention.

  Moreover, this invention relates to the antifungal composition containing the said component (A), (B) and (C) with a high antiseptic effect with respect to fungi.

  Next, the present invention will be specifically described with reference to test examples and prescription examples, but the present invention is not limited to the following test examples and prescription examples.

(Preparation example)
Each component shown in Tables 1 to 3, Table 5, Tables 7 to 9 and Table 11 was mixed in a predetermined amount (% by weight), and then dissolved with heating and stirring to obtain a uniform mixture. The mixture was cooled to about 25 ° C. to obtain compositions of Examples and Comparative Examples.

(Test Example 1 Preservative efficacy test)
A composition was prepared according to the above method using the components listed in Table 1.
About these compositions, antiseptic action was evaluated according to the 16th revision Japanese Pharmacopoeia reference information preservation efficacy test method. Specifically, a fungal solution was prepared using Candida albicans (ATCC 10231), which is a common contaminant of external compositions. The bacterial solution was inoculated into the composition to 10 ⁴ to 10 ⁵ CFU / mL and stored at 25 ° C. The composition was sampled 24 hours after inoculation, and the number of viable bacteria was determined by measuring the number of bacteria in the composition by a plate agar smearing method. The number of viable bacteria in the product was shown as a ratio.

As shown in Table 1, the composition of propynyl butylcarbamate iodide and light liquid paraffin showed a slight preservative effect 24 hours after the inoculation (Comparative Example 1-2). Further, in the composition of N-lauroyl-L-glutamic acid dibutylamide and light liquid paraffin, the bacteria tended to grow slightly (Comparative Example 1-3). On the other hand, in Example 1-1 in which both components of butylcarbamic acid propynyl iodide and N-lauroyl-L-glutamic acid dibutylamide were blended with light liquid paraffin, the number of bacteria was significantly reduced and a high antiseptic effect was exhibited. It was.
From this, it was confirmed that a high preservative effect was exhibited by combining propyleneyl butylcarbamate and oily gelling agent with the oil.

(Test Example 2 Storage efficacy test)
A composition was prepared according to the above method using the components listed in Table 2.
About these compositions, antiseptic action was evaluated according to the 16th revision Japanese Pharmacopoeia reference information preservation efficacy test method. Specifically, each fungal solution was prepared using the fungus Candida albicans (ATCC 10231). The bacterial solution was inoculated into the composition to 10 ⁴ to 10 ⁵ CFU / mL and stored at 25 ° C. Sampling the composition 24 hours after inoculation, and determining the number of viable bacteria by measuring the number of bacteria in the composition by a plate agar smearing method, the number of viable bacteria of Comparative Example 2-1 as 100, each composition The number of viable bacteria in the product was shown as a ratio.

As shown in Table 2, as in Test Example 1, the composition of propynyl butylcarbamate and light liquid paraffin showed a slight preservative effect 24 hours after inoculation (Comparative Example 2-2). ). Further, in the composition of N-lauroyl-L-glutamic acid dibutylamide and light liquid paraffin, even in the case of 0.25% N-lauroyl-L-glutamic acid dibutylamide, as in Test Example 1, there is a tendency for some bacteria to grow slightly. (Comparative Example 2-3). In contrast, in Example 2-1, in which both components of butylcarbamic acid propynyl iodide and N-lauroyl-L-glutamic acid dibutylamide were blended with light liquid paraffin, the number of bacteria was remarkably reduced, and high antiseptic effect showed that.
From this, it was confirmed that even when the oil agent was combined with propynyl butylcarbamate iodide and a low concentration oily gelling agent, a high preservative effect was exhibited.

(Test Example 3 Composition Hardness Test)
Using the components shown in Table 3, a composition was prepared according to the above method, and with the composition being fluid at high temperature, 10 g of each formulation was poured into a 6 cm diameter glass petri dish, allowed to cool at room temperature, and hardened. The sample was used as a measurement sample.
The hardness of the composition was measured using a texture analyzer (product name: TA.XT.plus Texture Analyzer (manufactured by Stable Micro Systems)). The probe used in this measurement is a Φ10 mm cylinder probe, and specific measurement conditions are as shown in Table 4 below.

After the probe comes into contact with the sample surface and starts to push down the sample surface, the distance measured by the probe is measured as the stress when crushing, and the maximum value is recorded as the hardness.
N-lauroyl-L-glutamic acid dibutylamide in any case where the blending amount is 0.25 or 5%, when propynyl butylcarbamate is not blended (Comparative Example 3-1 and Comparative Example 3-2) In comparison, when propynyl iodide butylcarbamate was blended (Example 3-1 and Example 3-2), it was confirmed that the hardness increased synergistically.

(Test Example 4 Composition Hardness Test)
Using the components shown in Table 5, a measurement sample was prepared in the same manner as in Test Example 3, and the hardness was measured with a texture analyzer using a Φ10 mm cylinder probe. Specific measurement conditions are as shown in Table 6 below.

Even when the blending amount of N-lauroyl-L-glutamic acid dibutylamide was 2.5%, as in Test Example 3, it was confirmed that the hardness increased synergistically by blending propynyl butylcarbamate. .
Therefore, since the hardness of the composition increases by combining the oil agent with the oily gelling agent and propynyl butylcarbamate, it is possible to obtain the desired hardness even if the amount of the oily gelling agent is reduced. It was confirmed. From this, it can be said that even when molded into a stick shape, it is possible to obtain a composition having a desired hardness in consideration of usability and moldability.

(Test Example 5 Storage efficacy test)
A composition was prepared according to the above method using the components listed in Table 7.
About these compositions, antiseptic action was evaluated according to the 16th revision Japanese Pharmacopoeia reference information preservation efficacy test method. Specifically, each fungal solution was prepared using the fungus Candida albicans (ATCC 10231). The bacterial solution was inoculated into the composition so as to be 10 ⁴ to 10 ⁵ CFU / mL> and stored at 25 ° C. The composition was sampled 16 hours after inoculation, and the number of viable bacteria was determined by measuring the number of bacteria in the composition by a plate agar smearing method. The number of viable bacteria in the product was shown as a ratio.

As shown in Table 7, the composition of butyl carbamate propynyl iodide alone showed an antiseptic effect 16 hours after bacterial inoculation, as in Test Example 1 (Comparative Example 4-2). In addition, in the case of N-lauroyl-L-glutamic acid dibutylamide at 2.5%, there was a tendency for some bacteria to grow as in Test Example 1 (Comparative Example 4-3). On the other hand, in Example 4-1, in which both components of butylcarbamic acid propynyl iodide and N-lauroyl-L-glutamic acid dibutylamide were blended, the number of bacteria was remarkably reduced and a high antiseptic effect was shown.
From this, it was confirmed that even when a high concentration of propynyl iodide butylcarbamate and an oily gelling agent was combined with the oil agent, a synergistic high antiseptic effect was exhibited.

(Test Example 6 Storage efficacy test)
A composition was prepared according to the above method using the components listed in Table 8.
About these compositions, antiseptic action was evaluated according to the 16th revision Japanese Pharmacopoeia reference information preservation efficacy test method. Specifically, each fungal solution was prepared using the fungus Candida albicans (ATCC 10231). The bacterial solution was inoculated into the composition to 10 ⁴ to 10 ⁵ CFU / mL and stored at 25 ° C. The composition was sampled 16 hours after inoculation, and the number of viable bacteria was determined by measuring the number of bacteria in the composition by a plate agar smearing method. The number of viable bacteria in the product was shown as a ratio.

As shown in Table 8, the composition of propynyl iodide butylcarbamate alone showed no antiseptic effect 24 hours after inoculation (Comparative Example 5-2). In addition, dextrin palmitate showed a slight preservative effect in the case of 10% (Comparative Example 5-3). On the other hand, in Example 5-1, in which both components of propynyl butylcarbamate iodide and dextrin palmitate were blended, the number of bacteria was remarkably reduced and a high antiseptic effect was shown.
From this, it was confirmed that even when a low concentration of propynyl iodide butylcarbamate and an oily gelling agent were combined with the oil agent, a synergistic high antiseptic effect was exhibited.

(Test Example 7 Composition Hardness Test)
Using the components shown in Table 9, a composition was prepared according to the above method, and with the composition being fluid at high temperature, 10 g of each formulation was poured into a 6 cm diameter glass petri dish, allowed to cool at room temperature, and hardened. The sample was used as a measurement sample.
The hardness of the composition was measured using a texture analyzer (product name: TA.XT.plus Texture Analyzer (manufactured by Stable Micro Systems)). The probe used in this measurement is a Φ10 mm cylinder probe, and specific measurement conditions are as shown in Table 10 below.

After the probe comes into contact with the sample surface and starts to push down the sample surface, the distance measured by the probe is measured as the stress when crushing, and the maximum value is recorded as the hardness.
When the amount of N-lauroyl-L-glutamic acid dibutylamide is 1, 2.5, or 5%, propynyl iodide butylcarbamate is not blended (Comparative Example 6-1 and Comparative Example 6-2). In comparison with Comparative Example 6-3), when propynyl butylcarbamate was added (Example 6-1, Example 6-2, and Example 6-3), the hardness increased synergistically. Confirmed to do.

(Test Example 8 composition hardness test)
Using the components shown in Table 11, a measurement sample was prepared in the same manner as in Test Example 7, and the hardness was measured with a texture analyzer using a Φ10 mm cylinder probe. Specific measurement conditions are as shown in Table 12 below.

Even when the blending amount of dextrin palmitate was 5 or 10%, it was confirmed that the hardness increased synergistically by blending propynyl butylcarbamate propylene as in Test Example 7.
Therefore, since the hardness of the composition increases by combining the oil agent with the oily gelling agent and propynyl butylcarbamate, it is possible to obtain the desired hardness even if the amount of the oily gelling agent is reduced. It was confirmed. From this, it can be said that even when molded into a stick shape, it is possible to obtain a composition having a desired hardness in consideration of usability and moldability.

  Based on the following formulation example, mixing and heating and stirring were performed to obtain an external composition. All of these compositions for external use have a synergistically enhanced antiseptic effect, synergistically increase the hardness of the composition, have low irritation, and have excellent usability and formulation stability. .

Formulation Example 1
(Ingredient) (wt%)
1. Octild decanol 30
2. Liquid paraffin 20
3. Diisostearyl malate 20
4). N-lauroyl-L-glutamic acid dibutylamide 10
(GP-1)
5. Butynyl carbamate propynyl iodide (IPBC) 0.01
6). Dimer linoleic acid Dimer linoleyl 19.99
Total 100

Formulation Example 2
(Ingredient) (wt%)
1. Isostearyl alcohol 20
2. Hydrogenated polyisobutene 20
3. Jojoba oil 20
4). N-2-Ethylhexanoyl-L-glutamic acid dibutylamide 5
(EB-1)
5. Butynyl carbamate propynyl iodide (IPBC) 0.01
6.2 Cetyl 2-ethylhexanoate 24.99
Total 100

Formulation Example 3
(Ingredient) (wt%)
1. Polyglyceryl-2 triisostearate-20
2. Octyldodecyl lactate 10
3. Vaseline 15
4). Dextrin myristate (Leopearl MKL2) 10
5. Butynyl carbamate propynyl iodide (IPBC) 0.01
6.2 Cetyl 2-ethylhexanoate 44.99
Total 100

Formulation Example 4
(Ingredient) (wt%)
1. Isostearyl alcohol 20
2. Octyldodecyl lactate 10
3. Vaseline 15
4). Dextrin myristate (Leopearl MKL2) 1.5
5. N-lauroyl-L-glutamic acid dibutylamide 3
(GP-1)
6). Butynyl carbamate propynyl iodide (IPBC) 0.01
7. Cetyl 2-ethylhexanoate 50.49
Total 100

Claims (10)

An external composition comprising (A) propynyl iodide butylcarbamate, (B) an oily gelling agent and (C) an oily agent ( excluding those in the form of an emulsion) .   (B) As an oil-based gelling agent, the composition for external use of Claim 1 containing 1 type, or 2 or more types chosen from an amino acid oil-based gelling agent and fatty acid dextrin is contained.   The amino acid-based oily gelling agent includes at least one of lauroyl glutamic acid stearylamide, N-lauroyl-L-glutamic acid dibutylamide, or N-2-ethylhexanoyl-L-glutamic acid dibutylamide. The external composition according to claim 2.   The composition for external use according to claim 2, comprising at least one of dextrin palmitate, dextrin myristate, or dextrin octanoate as the fatty acid dextrin.   (C) Oil composition is 1 type, or 2 or more types chosen from hydrocarbon oil, ester oil, higher alcohol, and natural oil, The external composition in any one of Claims 1-4 characterized by the above-mentioned.   The composition for external use according to any one of claims 1 to 5, wherein the composition is for lips.   The composition for external use according to any one of claims 1 to 6, wherein the composition is in a stick form.   The external composition according to any one of claims 1 to 7, wherein the hardness at room temperature is 100 g or more and 2,000 g or less as measured by a texture analyzer. The external composition (A) iodopropynyl butylcarbamate, (B) an oily gelling agent and wherein the (C) be contained oil, the method enhancing the antiseptic effect against fungi in topical compositions (however, the External compositions do not include those in the form of emulsions) . A method for increasing the hardness in an external composition (provided that the external composition comprises (A) propynyl iodide butylcarbamate, (B) an oily gelling agent, and (C) an oil) . Does not include those in the form of emulsions) .