JP2008019230A5 - - Google Patents

Description

The present invention relates to a skin external preparation, and more particularly relates to a useful skin external agent in a stable formulation of ceramide.

Formula 1 (wherein R 1 and R 2 each independently represents an alkyl group or an alkenyl group having 9 to 29 carbon atoms)

Alpha by methods such as the, .epsilon.-bis (γ-N- (10~30 carbon atoms) acyl Guru Tamil) is lysine may be used to manufacture, alpha, .epsilon.-bis (γ-N- (10 carbon atoms ~ 30) Acylglutamyl) lysine already exists in the market, and such a commercial product can be purchased and used. As such a commercially available product, “Perisea L-30” (manufactured by Asahi Kasei Corporation; α, ε-bis (γ-N-lauroylglutamyl) lysine) can be preferably exemplified. The thus-obtained α, ε-bis (γ-N- (C10-30) acylglutamyl) lysine has the property of easily forming a bimolecular film, and this action is an essential component described later. It excels in the action of forming a stable lipid duplex that incorporates. In order to exert such action, the skin external preparation is used in a total amount of one or more selected from α, ε-bis (γ-N- (C10-30) acylglutamyl) lysine. It is preferable to contain 0.005% by mass, more preferably 0.01% by mass, and 10% by mass as an upper limit, and more preferably 5% by mass with respect to the total amount. This is because if the amount of the component is too large, the effect reaches a peak, and there are cases where the degree of freedom of prescription is limited to the person, and if the amount is too small, the effect may not be achieved. Further, this content is preferably equal to or more than the total amount of ceramide described later, and more preferably doubled or more. Furthermore, the upper limit may be 6 times or less, more preferably 5 times or less.

The skin external preparation of this invention can contain the arbitrary components normally contained in skin external preparations, such as cosmetics, besides the said component. Such optional ingredients 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 Oil, wax, oil such as beeswax, canola wax, carnauba wax, ibotarou, lanolin, reduced lanolin, hard lanolin, jojoba wax, liquid paraffin, squalane, pristane, ozokerite, paraffin, ceresin, petrolatum , Hydrocarbons such as microcrystalline wax; higher fatty acids such as oleic acid, isostearic acid, lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, undecylenic acid; cetyl alcohol, stearyl alcohol, isostearyl Higher alcohols such as alcohol, behenyl alcohol, octyldodecanol, myristyl alcohol, cetostearyl alcohol; cetyl isooctanoate, isopropyl myristate, hexyldecyl isostearate, diisopropyl adipate, di-2-ethylhexyl sebacate, cetyl lactate, malic acid Diisostearyl, di-2-ethylhexanoic acid ethylene glycol, dicaprate neopentyl glycol, di-2-heptylundecanoic acid glycerin, tri-2-ethylhexanoic acid glycerin, tri-2-ethylhexanoic acid trimethylolpropane, tri Synthetic ester oils such as trimethylolpropane isostearate and pentane erythritol tetra-2-ethylhexanoate; dimethylpolysiloxane, methylphenylpoly Linear polysiloxanes such as oxane and diphenylpolysiloxane; cyclic polysiloxanes such as octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, and dodecamethylcyclohexanesiloxane; amino-modified polysiloxane, polyether-modified polysiloxane, alkyl-modified polysiloxane, Oil agents such as silicone oils such as modified polysiloxanes such as fluorine-modified polysiloxanes; Anionic surfactants such as fatty acid soap (sodium laurate, sodium palmitate, etc.), potassium lauryl sulfate, triethanolamine ether of alkyl sulfates; Cationic surfactants such as stearyltrimethylammonium, benzalkonium chloride, laurylamine oxide; imidazoline-based amphoteric surfactants (2-cocoyl-2-imida Zolinium hydroxide-1-carboxyethyloxy disodium salt, etc.), betaine surfactants (alkyl betaine, amide betaine, sulfobetaine, etc.), and amphoteric surfactants such as acylmethyltaurine; sorbitan fatty acid esters (sorbitan) Monostearate, sorbitan sesquioleate, etc.), glycerin fatty acids (glyceryl monostearate, etc.), propylene glycol fatty acid esters (propylene glycol monostearate, etc.), hardened castor oil derivatives, glycerin alkyl ethers, POE sorbitan fatty acid esters (POE sorbitan monooleate, polyoxyethylene sorbitan monostearate, etc.), POE sorbite fatty acid esters (POE-sorbitol monolaurate, etc.), POE glycerin fatty acid ester Tells (POE-glycerol monoisostearate, etc.), POE fatty acid esters (polyethylene glycol monooleate, POE distearate, etc.), POE alkyl ethers (POE2-octyldodecyl ether, etc.), POE alkyl phenyl ethers (POE nonylphenyl) Ethers, etc.), Pluronic types, POE / POP alkyl ethers (POE / POP2-decyltetradecyl ether, etc.), Tetronics, POE castor oil / hardened castor oil derivatives (POE castor oil, POE hardened castor oil, etc.), Nonionic surfactants such as sucrose fatty acid ester and alkyl glucoside; polyethylene glycol, glycerin, 1,3-butylene glycol, erythritol, sorbitol, xylitol, maltitol, propylene Polyhydric alcohols such as recall, dipropylene glycol, diglycerin, isoprene glycol, 1,2-pentanediol, 2,4-hexanediol, 1,2-hexanediol, 1,2-octanediol; sodium pyrrolidonecarboxylate Moisturizing ingredients such as lactic acid and sodium lactate; powders such as mica, talc, kaolin, synthetic mica, calcium carbonate, magnesium carbonate, anhydrous silicic acid (silica), aluminum oxide, barium sulfate, etc. whose surface may be treated Body, the surface may be treated, inorganic pigments such as bengara, yellow iron oxide, black iron oxide, cobalt oxide, ultramarine, bitumen, titanium oxide, zinc oxide; surface may be treated, mica Pearl agents such as titanium, fish phosphorus foil, bismuth oxychloride; red 202 which may be raked, red Color 228, Red 226, Yellow 4, Blue 404, Yellow 5, Red 505, Red 230, Red 223, Orange 201, Red 213, Yellow 204, Yellow 203, Blue 1 No., green 201, purple 201, red 204, etc .; organic powders such as polyethylene powder, polymethyl methacrylate, nylon powder, organopolysiloxane elastomer; para-aminobenzoic acid UV absorbers; anthranils Acid UV absorbers; salicylic acid UV absorbers ; cinnamic acid UV absorbers ; benzophenone UV absorbers; sugar UV absorbers; 2- (2′-hydroxy-5′-t-octylphenyl) benzotriazole; UV absorbers such as 4-methoxy-4′-t-butyldibenzoylmethane; lower alcohols such as ethanol and isopropanol Vitamins such as vitamin A or derivatives thereof, vitamin B ₆ hydrochloride, vitamin B ₆ tripalmitate, vitamin B ₆ dioctanoate, vitamin B ₂ or derivatives thereof, vitamin B ₁₂ such as vitamin B ₁₂ , vitamin B ₁₅ or derivatives thereof; Vitamin E such as α-tocopherol, β-tocopherol, γ-tocopherol, vitamin E acetate, vitamin D, vitamin H, pantothenic acid, pantethine, pyrroloquinoline quinone and the like; antibacterial agents such as phenoxyethanol are preferred It can be illustrated. The external preparation for skin of the present invention can be produced by treating these components according to a conventional method.

Similarly to the lotion cosmetic 1, a vesicle dispersion lotion cosmetic 3 as an external preparation for skin of the present invention was prepared according to the following formulation. This product was as stable as Lotion Cosmetic 1 in a storage test at 50 ° C. for 1 month. In addition, in the evaluation of usability, the goodness is score 5 (1 person), score 4 (2 persons), score 3 (0 person), score 2 (0 person), score 1 (0 person) The feeling was score 5 (1 person), score 4 (2 persons), score 3 (0 persons), score 2 (0 persons), and score 1 (0 persons).

Similarly to the lotion cosmetic 1, a vesicle-dispersed lotion cosmetic 4 as an external preparation for skin of the present invention was prepared according to the following formulation. This product was as stable as Lotion Cosmetic 1 in a storage test at 50 ° C. for 1 month. In addition, in the evaluation of usability, the goodness is score 5 (1 person), score 4 (2 persons), score 3 (0 person), score 2 (0 person), score 1 (0 person) The feeling was score 5 (1 person), score 4 (2 persons), score 3 (0 persons), score 2 (0 persons), and score 1 (0 persons).

Similarly to the lotion cosmetic 1, a vesicle dispersion lotion cosmetic 5 which is an external preparation for skin of the present invention was prepared according to the following formulation. This product was as stable as Lotion Cosmetic 1 in a storage test at 50 ° C. for 1 month. In addition, in the evaluation of usability, the goodness is score 5 (1 person), score 4 (2 persons), score 3 (0 person), score 2 (0 person), score 1 (0 person) The feeling was score 5 (1 person), score 4 (2 persons), score 3 (0 persons), score 2 (0 persons), and score 1 (0 persons).

Similarly to the lotion cosmetic 1, a vesicle-dispersed cream cosmetic 1 as an external preparation for skin of the present invention was prepared according to the following formulation. This was a vesicle dispersion in which a lipid bilayer was present around oil droplets, and was stable in a storage test at 50 ° C. for 1 month. In addition, in the evaluation of usability, the goodness of extension is score 5 (1 person), score 4 (2 persons), score 3 ( 0 person), score 2 (0 person), and score 1 (0 person). Were score 5 (2 persons), score 4 (1 person), score 3 (0 person), score 2 (0 person), and score 1 (0 person).

<Test Example 1>
About the said cosmetics cosmetics 2, the comparative example 2, and the comparative example 3, stability was investigated by the severe test. The severe test conditions were stored at 60 ° C. for 4 days. After storage, the sample was stored at 20 ° C. for 12 hours and observed. The observation items were the presence / absence of separation, the presence / absence of crystal precipitation, and the average particle diameter in five fields of view under the microscope. The results are shown in Table 10 . This shows that the cosmetic of the present invention is excellent in stability.

<Test Example 2>
The inhibitory effect of TEWL was investigated using the inner forearm of the panel. The inner part of the forearm is stripped 15 times with surgical tape to create rough skin of the model. Four 2cm x 4cm parts are created here, and TEWL is measured using "Tevameter" (Integral). After treatment with each cosmetic, TEWL (unit: mg / cm ² ) was measured again at an interval of 10 minutes. One site served as an untreated control. The results are shown in Table 11 . From this, it can be seen that the emulsion cosmetic 2 which is the external preparation for skin of the present invention has an excellent TEWL suppressing effect.