JP5208398B2 - Antiseptic skin external preparation - Google Patents

Description

  The present invention relates to an external preparation for skin, and more particularly to an external preparation for skin suitable for cosmetics.

  Having antiseptic power is one of the important basic factors in skin preparations such as cosmetics. In order to obtain such preservative power, benzoic acid esters, benzalkonium chloride, glucuron are used. A method has been adopted in which an antiseptic such as chlorhexidine acid is contained to provide antiseptic power. Among these, since benzalkonium chloride and chlorhexidine glucuronate are cationic components, there are restrictions on their use depending on formulation components, and there is a background that benzoic acid esters have been widely used. However, in recent years, there are experts who are concerned about the safety of benzoic acid esters, and relying on benzoic acid esters for preservative power is not a favorable situation from the standpoint of corporate crisis management. Therefore, it can be said that a means for realizing antiseptic power instead of benzoic acid ester is desired.

  As a method for embodying antiseptic power in place of such benzoic acid esters, for example, phenoxyethanol, isoprene glycol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol and the like A method using a combination with a monohydric alcohol (see, for example, Patent Document 1 and Patent Document 2) has been developed, but in an emulsification system or the like, sometimes the antiseptic effect is significantly reduced. The current situation is that the cause is not well understood. In benzoic acid esters, it is known that antiseptics become micelles and are deactivated by phospholipids or polyoxyethylene addition type nonionic surfactants (see, for example, Patent Document 3). It is also known that such a phenomenon hardly occurs in the combination of phenoxyethanol and antibacterial polyhydric alcohol. It is known that inactivation of such antibacterial components by phospholipids or polyoxyethylene addition type nonionic surfactants occurs not only in benzoic acid esters but also in antifungal agents (for example, The only combination of phenoxyethanol and antibacterial polyhydric alcohol was considered to be an exception.

On the other hand, a phosphoric acid chelating agent is contained in a skin external preparation for the purpose of sequestering metal, and is used for suppressing an oxidation reaction mediated by a metal as a catalyst. In such case, as an example phenoxyethanol is involved, for example, phenoxyethanol that have been known to suppress art with phosphoric acid chelating agent oxidation, to inactivated by hydrogen peroxide (e.g., Patent Document 5 See ).
Further, 1,2-octane purpose of enhancing the antimicrobial properties of the diol, that is also known techniques allowed to contain the skin external preparation (e.g., see Patent Document 6).

However, even in such a situation, in the emulsification system etc., sometimes the combination of antibacterial polyhydric alcohol and phenoxyethanol preservatives significantly reduces the antiseptic effect, and the cause However, it has not been known at all that the effect is caused by phospholipids or polyoxyethylene-added nonionic surfactants, and the effect becomes significant due to the relationship with other components. 1) Phospholipid, 2) polyoxyethylene addition type nonionic surfactant, 3) phenoxyethanol , 4) antibacterial polyhydric alcohol, and 5 ) phosphate ester There is no known compound containing a chelating agent, and it is therefore completely known that such a combination of preparations can suppress the effect of reducing the preservative power due to the nonionic surfactant of phospholipid or polyoxyethylene addition type. It wasn't.

JP-A-10-53510 Japanese Patent Laid-Open No. 11-322591 Japanese Patent Laying-Open No. 2005-8591 WO2002 / 010440 JP 2003-335614 A JP 2005-132759 A

  The present invention has been made under such circumstances, and an object of the present invention is to provide a means for suppressing a significant decrease in the antiseptic effect of a combination of antibacterial polyhydric alcohol and phenoxyethanol, which sometimes occurs. To do.

In view of such a situation, the present inventors have eagerly pursued research for a means for suppressing a significant decrease in the antiseptic effect in the combination of antibacterial polyhydric alcohol and phenoxyethanol, which sometimes occurs. As a result, such a decrease in preservative power tends to occur in the presence of phospholipid and polyoxyethylene addition type nonionic surfactants, and even in the presence of such components, phosphate ester chelating agents It has been found that such a decrease in the preservative power can be suppressed by containing, and the present invention has been completed. That is, this invention is as showing to the prescription shown below.
(1) 1) a phospholipid selected from lecithin, lysolecithin or their hydrogenated product, and 2) a polyoxyethylene fatty acid ester or polyoxyethylene sorbitan fatty acid ester having an average added mole number of polyoxyethylene of 10 to 30 One or more polyoxyethylene addition type nonionic surfactants selected from polyoxyethylene alkyl (alkenyl) ether, polyoxyethylene fatty acid glyceryl, and polyoxyethylene hydrogenated castor oil, and 3) phenoxyethanol When, 4) 1,3-butanediol, isoprene glycol, in the one or more antimicrobial polyhydric alcohol and skin external agents containing is selected from 1,2-pentanediol, further 5) Hydroxyethane diphosphonic acid, amino trimethylene phosphate Features acid, phosphono butane tricarboxylic acid, phytic acid, a phosphoric acid ester-based chelating agent selected from those salts which are tri-phosphonomethyl amine oxides and physiologically acceptable in that it contains 0.01 to 1 wt% And skin external preparation. (2) The skin external preparation according to (1), wherein the polyoxyethylene addition-type nonionic surfactant is a polyoxyethylene sorbitan fatty acid ester.
( 3) The external preparation for skin according to (1) or (2) , which does not contain a benzoic acid ester.

  According to the present invention, it is possible to suppress a significant decrease in the antiseptic effect of the antibacterial polyhydric alcohol and phenoxyethanol preservative combination that sometimes occurs.

The skin external preparation of the present invention is a skin external preparation containing a phospholipid, a polyoxyethylene addition type nonionic surfactant, phenoxyethanol, and an antibacterial polyhydric alcohol. It contains an agent. That is, in skin external preparations, phospholipids and polyoxyethylene addition type nonionic surfactants are antibacterial polyvalents such as phenoxyethanol, 1,3-butanediol, isoprene glycol, and 1,2-pentanediol. It has the action of reducing the antibacterial activity of alcohol, and prevents such a decrease in antibacterial activity (preservative power) by adding a phosphate ester chelating agent.

The phospholipids of interest of the skin external preparation of the present invention, lecithin of soybean or egg and Motogen include lysolecithin or their hydrogenated products. Such components can be contained for ordinary purposes. That is, it can be used as a component for strengthening the interface, as a component for forming a liquid crystal structure by forming a double film, as a component for forming a vesicle in a vesicle dispersion system, or as an emulsifier. Moreover, the content should just contain the quantity suitable for such a purpose, for example, 0.1-5 mass% with respect to the skin external preparation whole quantity, More preferably, 0.5-2 mass% is preferable. It can be illustrated.

Examples of the polyoxyethylene addition-type nonionic surfactant to be used as a skin external preparation of the present invention include polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene alkyl (alkenyl) ether, polyoxy polyoxyethylene fatty acid glyceryl, polyoxyethylene hydrogenated castor oil and the like, particularly, polyoxyethylene sorbitan fatty acid esters are preferable, among them, polyoxyethylene sorbitan oleate ester. Moreover, 10-30 are mentioned as an average addition mole number of polyoxyethylene, and 15-25 are especially preferable. This is because the polyoxyethylene addition-type nonionic surfactant in such a form has a remarkable degree to reduce the antibacterial power (preservative power) of phenoxyethanol and antibacterial polyhydric alcohol. The polyoxyethylene addition-type nonionic surfactant can be contained in a generally known amount range for a generally known purpose. As the purpose, for example, it can be preferably exemplified as a component for solubilization, a component for emulsification, a component for washing, or a component for dispersion. For example, 0.01 to 10% by mass is preferable, and 0.1 to 7% by mass is more preferable.

In the skin external preparation of the present invention, the phospholipid及beauty polyoxyethylene-added nonionic surfactant, as a preservative to impair antimicrobial, containing phenoxyethanol. In the external preparation for skin of the present invention, phenoxyethanol preferably contains the amount usually used, specifically 0.05 to 1% by mass, preferably 0.1 to 0.5% by mass. More preferred.

In the external preparation for skin of the present invention, in addition to the phenoxyethanol, it is a component that imparts antiseptic power to the preparation system, and the antibacterial property is impaired by the nonionic surfactant of the phospholipid and polyoxyethylene addition type. Contains ingredients . Such components, 1,3-butanediol, isoprene glycol, include antimicrobial polyhydric alcohols such as 1,2-pentanediol, preferred content of such components, in total, relative to the total amount of the skin treatment composition 0.1 to 15% by mass, and more preferably 0.5 to 5% by mass.

The external preparation for skin of the present invention is characterized by containing a phosphate ester chelating agent as an essential component. Examples of the phosphoric acid ester-based chelating agent, selected hydroxycarboxylic diphosphonic acid, amino tri methylene phosphonic acid, phosphono butane tricarboxylic acid, phytic acid, tri-phosphonomethyl amine oxides and physiologically acceptable salts thereof Can be mentioned . These can contain only the seed | species, and can also contain it in combination of 2 or more type. Such components have the preservative combination of antimicrobial polyhydric alcohol and phenoxyethanol, it caused Coll by phospholipids及beauty polyoxyethylene-added nonionic surfactant, the effect of inhibiting the significant decrease in the preservative effect. In order to achieve such an effect, the total amount is 0.01 to 1% by mass, and more preferably 0.02 to 0.5% by mass, based on the total amount of the external preparation for skin. This is because if the amount is too small, the above effect may not be achieved, and if the amount is too large, the effect reaches a peak, and the degree of freedom of the formulation system may be reduced. The inclusion of such components, methylparaben, without containing parabens such as butylparaben, the presence of the phospholipid及beauty polyoxyethylene-added nonionic surfactants, the skin has a sufficient antiseptic topical It can be used as an agent. For this reason, it is preferable to use a paraben-free external preparation for the skin which does not contain parabens, since safety can be further improved.

In the external preparation for skin of the present invention, in addition to the above-mentioned components, such optional components that can be used in normal external preparations for skin include, for example, macadamia nut oil, avocado oil, corn oil, Olive oil, rapeseed oil, sesame oil, castor oil, safflower oil, cottonseed oil, jojoba oil, coconut oil, palm oil, liquid lanolin, hydrogenated coconut oil, hydrogenated oil, owl, hydrogenated castor oil, beeswax, candelilla wax, carnauba wax, ibotarou Oils, waxes such as lanolin, reduced lanolin, hard lanolin, jojoba wax; hydrocarbons such as liquid paraffin, squalane, pristane, ozokerite, paraffin, ceresin, petrolatum, microcrystalline wax; oleic acid, isostearic acid, lauric acid, Myristic acid, palmitic acid, steari Higher fatty acids such as acid, behenic acid, undecylenic acid; higher alcohols such as cetyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol, octyldodecanol, myristyl alcohol, cetostearyl alcohol; cetyl isooctanoate, isopropyl myristate, isostearic acid Hexyldecyl acid, diisopropyl adipate, di-2-ethylhexyl sebacate, cetyl lactate, diisostearyl malate, ethylene glycol di-2-ethylhexanoate, neopentyl glycol dicaprate, glycerin di-2-heptylundecanoate, Glycerin tri-2-ethylhexanoate, trimethylolpropane tri-2-ethylhexanoate, trimethylolpropane triisostearate, tetra-2- Synthetic ester oils such as pentyl erythritol tilhexanoate; chain polysiloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane and diphenylpolysiloxane; cyclics such as octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane and dodecamethylcyclohexanesiloxane Polysiloxanes; amino-modified polysiloxanes, polyether-modified polysiloxanes, alkyl-modified polysiloxanes, fluorine-modified polysiloxanes and other silicone oils such as silicone oils; fatty acid soaps (sodium laurate, sodium palmitate, etc.), Anionic surfactants such as potassium lauryl sulfate and alkylethanol triethanolamine ether; stearyltrimethylammonium chloride, benzalkonium chloride, laur Cationic surfactants such as rilamine oxide; imidazoline-based amphoteric surfactants (such as 2-cocoyl-2-imidazolinium hydroxide-1-carboxyethyloxy disodium salt), betaine-based surfactants (alkyl betaines, Amphibetaine, sulfobetaine, etc.), amphoteric surfactants such as acylmethyltaurine; sorbitan fatty acid esters (sorbitan monostearate, sorbitan sesquioleate, etc.), glycerin fatty acids (glyceryl monostearate, etc.), propylene glycol fatty acid Nonionic surfactants such as esters (propylene glycol monostearate, etc.), hydrogenated castor oil derivatives, glycerin alkyl ether, sucrose fatty acid ester, alkyl glucoside; polyethylene glycol, glycerin, erythri Polyol, sorbitol, xylitol, maltitol, propylene glycol, dipropylene glycol, diglycerin, 2,4-hexanediol, etc .; moisturizing ingredients such as sodium pyrrolidone carboxylate, lactic acid, sodium lactate; Mica, talc, kaolin, synthetic mica, calcium carbonate, magnesium carbonate, anhydrous silicic acid (silica), aluminum oxide, barium sulfate and the like, which may be treated; the surface may be treated, Bengala, yellow iron oxide, black iron oxide, cobalt oxide, ultramarine, bitumen, titanium oxide, zinc oxide inorganic pigments; pearlizing agents such as mica titanium, fish phosphorus foil, bismuth oxychloride, etc. whose surface may be treated Class: Red No. 202, Red No. 228, Red No. 226, Yellow No. 4, Blue which may be raked 404, Yellow 5, Red 505, Red 230, Red 223, Orange 201, Red 213, Yellow 204, Yellow 203, Blue 1, Green 201, Purple 201, Red 204 Organic powders such as polyethylene powder, organic powders such as polymethyl methacrylate, nylon powder, and organopolysiloxane elastomers; paraaminobenzoic acid UV absorbers; anthranilic acid UV absorbers; salicylic acid UV absorbers ; Acid UV absorbers ; benzophenone UV absorbers; sugar UV absorbers; 2- (2'-hydroxy-5'-t-octylphenyl) benzotriazole, 4-methoxy-4'-t-butyldibenzoylmethane UV absorbers such as ethanol; lower alcohols such as ethanol and isopropanol; vitamin A or its derivatives; B ₆ hydrochloride, vitamin B ₆ tripalmitate, vitamin B ₆ dioctanoate, vitamin B ₂ or derivatives thereof, vitamin B _12, vitamin B such as vitamin B ₁₅ or a derivative thereof; alpha-tocopherol, beta-tocopherol, .gamma. Preferred examples include vitamins such as tocopherol and vitamin E acetate, vitamins D, vitamin H, pantothenic acid, panthetin, pyrroloquinoline quinone and the like; and antibacterial agents such as phenoxyethanol.

  The skin external preparation of this invention can be manufactured by processing the said component in accordance with a conventional method. As the preparation of the external preparation for skin of the present invention, any preparation that is usually used for external preparations for skin can be applied without particular limitation, for example, lotion, emulsion, essence, cream, gel, peel-off pack, Preferred examples include oil gel, solid white powder, loose powder, emulsified powder dispersion dosage form, and two-phase dispersion dosage form. In addition, the external preparation for skin is not particularly limited as long as it is externally applied to the skin, and examples thereof include cosmetics including quasi-drugs, external preparations for skin, and external items for skin. Particularly preferred are cosmetics. This is because cosmetics require a much longer period of use and thus require higher stability and safety.

  Hereinafter, the present invention will be described in more detail with reference to examples, but it is needless to say that the present invention is not limited to such examples.

The cosmetic of the present invention was produced according to the following formulation. That is, each of the components i, b, and c is weighed and heated to 80 ° C., gradually b is added to emulsify with agitation, neutralized by addition of c under agitation, and cooled by stirring. The emulsion 1 (cosmetics) which is an external preparation for skin was obtained. Similarly, Comparative Example 1 in which POE (20) sorbitan sesquiolate and POE (20) behenyl ether in Emulsion 1 were replaced with decaglycerin monooleate and lecithin in water was compared, and Hydroxyethanediphosphonic acid in Emulsion 1 was replaced with water. Comparative Example 3 in which POE (20) sorbitan sesquioleate and POE (20) behenyl ether in Emulsion 1 and Emulsion 1 were replaced with decaglycerin monooleate and lecithin and hydroxyethanediphosphonic acid with water was also prepared in the same manner.

<Test Example 1>
About the said emulsion 1 and Comparative Examples 1-3, the antibacterial property with respect to fungi (Aspergillus niger (Aspergillus niger)) with which antiseptic | preservative is hard to work was investigated. That is, as the medium, SDA medium was used. In the method, 0.1 ml of the sample was smeared on the above plate medium, inoculated with a platinum loop, the number of colonies was counted from 1 day after the inoculation, and ranked according to the following rank. That is, rank 0: 0, rank 0.5: 1-10, rank 1: 11-200, rank 1.5: 201-500, rank 2: 501-1000, rank 2.5: 100-3000, rank 3 : Ranks of 3001-5000, Rank 3.5: 5001-10000, Rank 4: 10000. The results are shown in Table 2. This shows that POE (20) sorbitan sesquiolate and lecithin reduce the antibacterial properties of phenoxyethanol and 1,2-pentanediol, and hydroxyethanediphosphonic acid suppresses this antibacterial activity reducing action.

  Emulsions 2-5 were produced according to emulsion 1 and the formulation shown below. Moreover, it evaluated similarly to Test Example 1.

Accordance with the formulations shown in emulsions 1 and below, to produce an emulsion 6-8. Moreover, it evaluated similarly to Test Example 1.

  The present invention can be applied to external preparations for skin such as cosmetics.

Claims (3)

1) a phospholipid selected from lecithin, lysolecithin or a hydrogenated product thereof;
2) Polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene alkyl (alkenyl) ether, polyoxyethylene fatty acid glyceryl, and polyoxyethylene cured, having an average addition mole number of polyoxyethylene of 10 to 30 One or more polyoxyethylene addition type nonionic surfactants selected from castor oil;
3) with phenoxyethanol ;
4) In a skin external preparation containing one or more antibacterial polyhydric alcohols selected from 1,3-butanediol, isoprene glycol, and 1,2-pentanediol ,
5 ) a phosphate ester chelating agent selected from hydroxyethanediphosphonic acid, aminotrimethylenephosphonic acid, phosphonobutanetricarboxylic acid, phytic acid, triphosphonomethylamine oxide and physiologically acceptable salts thereof; A skin external preparation characterized by containing 0.01-1 mass% .   The skin external preparation according to claim 1, wherein the polyoxyethylene addition-type nonionic surfactant is a polyoxyethylene sorbitan fatty acid ester. The external preparation for skin according to claim 1 or 2 , characterized in that it does not contain a benzoic acid ester.