JP4960004B2 - Ubidecalenone-containing cosmetic in vesicle dispersion dosage form - Google Patents

Description

  The present invention relates to a cosmetic, and more particularly to a cosmetic suitable for a cosmetic in the form of a phospholipid vesicle dispersion.

Ubidecarenone is also known as coenzyme Q10, and is known as an important component that resists aging of the living body. Ubidecarenone has a structure in which 10 isoprenes are added, and because of this structure, it has an excellent antioxidant action, and it is thought that this antioxidant action is responsible for the anti-aging action. Because of the structure in which the double bond lasts long, it must be said that it is unstable against oxidation. For this reason, many pharmaceutical preparations have been made to prevent ubidecalenone from undergoing oxidative degradation before use, and one of them has devised a method using a production intermediate included in phospholipid (for example, (See Patent Document 1 and Patent Document 2). In such an inclusion form, the stability of ubidecarenone is certainly improved, but there are cases where the stabilization effect is impaired at the stage of processing into a liposome or emulsion form at the stage of formulation. This is presumably because a third component that destabilizes ubidecalenone invades into the ubidecalenone / phospholipid-stabilized inclusion body in the process of forming a liposome or emulsion. That is, it can be said that development of a technique for stably dispersing phospholipid microspheres including ubidecarenone itself in a cosmetic preparation has been desired.

  On the other hand, it is already known that trehalose contributes to the stabilization of various preparations (see, for example, Patent Document 3 and Patent Document 4), and, when present together with phospholipids, liposomes encapsulating unstable substances. It is also known that it is suitable for the formation of vesicles (see, for example, Patent Document 5). However, there is no dispersion stabilization of vesicles produced by phospholipids or the like, which does not have an inner aqueous phase in phospholipid microspheres. unknown.

  Furthermore, there is no known cosmetic composition having 1) ubidecalenone and 2) trehalose.

JP-A-5-163136 JP 2004-51627 A Japanese Patent Laid-Open No. 11-12150 JP 2002-154951 A JP 2005-179313 A

  The present invention has been made under such circumstances, and an object of the present invention is to provide a technique for stably dispersing phospholipid microspheres including ubidecarenone itself in a cosmetic preparation.

In view of such circumstances, the present inventors have sought for a technique for stably dispersing phospholipid microspheres including ubidecalenone itself in cosmetic preparations, and as a result of earnest research efforts, the present inventors have included trehalose. As a result, the inventors have found that such vesicle formation can be promoted and vesicle dispersion can be stabilized, and the present invention has been completed. That is, the present invention is as follows.
(1) Contains 1) phospholipid microspheres including ubidecarenone and 2) trehalose
Cosmetics, wherein the phospholipid spherules are manufactured by dissolving phospholipids or phospholipids and sterols by heating, cooling to 60 ° C., and then adding ubidecarenone. Fee.
(2) The cosmetic according to (1), wherein the phospholipid microspheres contain hydrogenated lecithin and phytosterol .
(3) The cosmetic according to (1) or (2), further comprising an alkyl-modified carboxyvinyl polymer and / or a salt thereof .
(4) The cosmetic according to any one of (1) to (3) , which does not contain a nonionic surfactant .
(5) The cosmetic according to any one of (1) to (4) , further comprising trimethylglycine .

  According to the present invention, it is possible to provide a technique for stably dispersing phospholipid microspheres including ubidecarenone itself in a cosmetic preparation.

(1) Ubidecarenone which is an essential component of the cosmetic of the present invention The cosmetic of the present invention is characterized by containing ubidecarenone as an essential component. Ubidecarenone is a component that activates the antioxidant mechanism in the living body and exerts an anti-aging action, and the preferred content of such component is 0.0001 to 0.03% by mass, more preferably 0.001. 0005 to 0.01% by mass. Since such a component is a coenzyme, it works effectively at a low blending amount as long as stability can be ensured. Such an ingredient is used in advance as an intermediate included in a composition mainly composed of phospholipid such as lecithin, phosphatidylglycerol, phosphatidylethanolamine, phosphatidylinositol, or lyso form thereof. The phospholipid is preferably exemplified by hydrogenated lecithin having high oxidative stability. As these base sources, there are soybeans and egg yolks, and any of them can be used, but those based on soybeans are preferable. When such hydrogenated lecithin is used, it is preferable to contain sterols for the purpose of enhancing the compatibility or enhancing the structure maintaining property of the formed microspheres. Phytosterols such as sterol, sitosterol, and stigmasteranol can be preferably exemplified. Of these, phytosterol is particularly preferred. The mass ratio of ubidecarenone, phospholipid, and sterol is preferably 0.1: 99.9 to 3:97, more preferably 0.5: 99.5 to 2:98, as the mass ratio of ubidecarenone to other components. . The mass ratio of phospholipid to sterol is preferably 95: 5 to 80:20, more preferably 93: 7 to 85:15. Such inclusions as production intermediates are prepared by previously dissolving components other than ubidecarenone by heating and cooling to around 60 ° C., and then containing ubidecarenone, and then adding agitation and cooling as desired. do it. Since such a composition is a solid, it can be pulverized in advance before it is contained in cosmetics, and the pulverized product can be contained, and it is preferable to contain it in such a form. Of course, the melt can be sprayed and solidified to form a powder.

<Production Example 1>
Inclusion bodies were made according to the following recipe. That is, the component (a) is heated to 80 ° C. and uniformly dissolved, then cooled to 60 ° C. with stirring, the component (b) is added to the mixture, stirred and mixed, and extruded and granulated with an extrusion granulator. The mixture was left to cool and solidified, and the solidified product was pulverized with a mixer and then pulverized with a jet mill to obtain production intermediate 1.

(2) Trehalose which is an essential component of the cosmetic of the present invention The cosmetic of the present invention is characterized by containing trehalose as an essential component. Such a component has an action of stably dispersing the phospholipid microspheres including ubidecarenone itself. Further, when mixing a phospholipid in an aqueous carrier, prevent the migration of such as emulsions or liposomes, have the effect of maintaining the base Shikuru form. The vesicles are small spheres that do not have an aqueous phase inside, and have an action of stably retaining fat-soluble active ingredients and the like in the spheres. By containing trehalose in the cosmetic, it becomes easy to maintain such a vesicle form, so that the fat-soluble active ingredient can be stably contained in the aqueous system. In order to exert such an effect, trehalose is preferably contained 0.5 to 2 times by mass, more preferably 0.7 to 1.5 times by mass with respect to the total mass of phospholipid microspheres. is there. Since such components also affect the usability of cosmetics, from that viewpoint, it is preferable to contain 0.01 to 1% by mass, more preferably 0.05 to 1%, based on the total amount of cosmetics. 0.5% by mass.

(3) Cosmetics of this invention The cosmetics of this invention contain the said essential component, It is characterized by the above-mentioned. The cosmetic of the present invention can be applied regardless of the type as long as it is usually used in cosmetics. Examples thereof include lotions, emulsions, essences, creams, and packs. Particularly preferred is a dosage form that is not an emulsion dosage form or a dosage form containing liposomes. This is because there are cases where emulsion particles and liposomes are associated with vesicles which are essential components, and vesicles migrate to emulsions and liposomes. In such forms, the effects of the present invention may be impaired. Because. In order to avoid such a situation, in the cosmetic of the present invention, sorbitan fatty acid esters (such as sorbitan monostearate and sorbitan sesquioleate), glycerin fatty acids (such as glyceryl monostearate), propylene glycol fatty acid esters ( propylene glycol monostearate, etc.), hardened castor oil derivatives, glycerin alkyl ether, POE sorbitan fatty acid esters (POE sorbitan monooleate, monostearate Porioki shea sorbitan, etc.), POE sorbitol fatty acid esters (POE- sorbit monolaurate Rate), POE glycerin fatty acid esters (POE-glycerin monoisostearate, etc.), POE fatty acid esters (polyethylene glycol monooleate, POE distearate, etc.) POE alkyl ethers (POE2-octyldodecyl ether, etc.), POE alkylphenyl ethers (POE nonylphenyl ether, etc.), Pluronic types, POE / POP alkyl ethers (POE / POP2-decyltetradecyl ether, etc.), Tetronic , POE castor oil / hardened castor oil derivatives (POE castor oil, POE hardened castor oil, etc.), non-ionic surfactants such as nonionic surfactants such as sucrose fatty acid esters and alkyl glucosides. .

  In order to prevent the dispersed vesicles from settling, it is preferable to give the system a viscosity of 1000 to 5000 mPa · s, more preferably 2000 to 4000 mPa · s. For this reason, as a thickener, It is preferable to contain an alkyl-modified carboxyvinyl polymer and / or a salt thereof. This is because the carboxyvinyl polymer and / or its salt, which is usually used as a thickener, is affected by the polarization of the phospholipid and may not exhibit a thickening effect. Such alkyl-modified carboxyvinyl polymer already has a commercial product as a raw material for cosmetics, and such a commercial product can be purchased and used. Preferred examples of such commercially available products include “Pemlen TR-1”, “Pemlen TR-2”, and “Carbopol 1382” manufactured by BF Goodrich. These salts can be used without particular limitation as long as they are used in cosmetics, for example, alkali metal salts such as sodium salts and potassium salts, alkaline earth metal salts such as calcium salts and magnesium salts. Preferred examples include organic amine salts such as ammonium salt, triethylamine salt, triethanolamine salt, and monoethanolamine salt, and basic amino acid salts such as lysine salt and alginate. The content of the alkyl-modified carboxyvinyl polymer and a salt thereof necessary for creating the viscosity range is 0.05 to 2% by mass, and more preferably 0.1 to 1% by mass.

In addition to the components described so far, the cosmetic of the present invention can contain optional components that are usually used in cosmetics within a range that does not impair the effects of the present invention. Examples of such optional ingredients include 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, and hardened coconut oil. Oil, wax, oils such as beeswax, molasses, hydrogenated castor oil, beeswax, candelilla wax, carnauba wax, ibotarou, lanolin, reduced lanolin, hard lanolin, jojoba wax; , 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 betaines, amide betaines, sulfobetaines, etc.), and amphoteric surfactants such as acylmethyl taurine; polyethylene glycol, glycerin, 1 , 3-butylene glycol, erythritol, sorbitol, xylitol, maltitol, propylene glycol, dipropylene glycol, diglycerin, isoprene glycol, 1,2-pentanediol, 2,4-hexanediol, 1,2-hexanediol, 1 Polyhydric alcohols such as 1,2-octanediol; moisturizing ingredients such as sodium pyrrolidonecarboxylate, lactic acid, sodium lactate; surface-treated mica, talc, kaolin, synthetic mica, calcium carbonate, charcoal Powders such as magnesium, silicic anhydride (silica), aluminum oxide, barium sulfate; surface may be treated, bengara, yellow iron oxide, black iron oxide, cobalt oxide, ultramarine, bitumen, titanium oxide, Zinc oxide inorganic pigments; surface treated pearl agents such as titanium mica, fish phosphorus foil, bismuth oxychloride; red 202, red 228, red 226 optionally raked Yellow 4, Blue 404, Yellow 5, Red 505, Red 230, Red 223, Orange 201, Red 213, Yellow 204, Yellow 203, Blue 1, Green 201, Purple Organic dyes such as No. 201 and Red No. 204; Organic powders such as polyethylene powder, polymethyl methacrylate, nylon powder, organopolysiloxane elastomer; Paraaminobenzoic acid System ultraviolet absorbers; anthranilic acid UV absorbers; salicylic acid type ultraviolet absorbers; cinnamic acid-based ultraviolet absorbents; benzophenone ultraviolet absorbers; sugar-based ultraviolet absorbent; 2- (2'-hydroxy-5'-t- UV absorbers such as octylphenyl) benzotriazole and 4-methoxy-4′-t-butyldibenzoylmethane; lower alcohols such as ethanol and isopropanol; vitamin A or derivatives thereof, vitamin B6 hydrochloride, vitamin B6 tripalmi Vitamin Bs such as Tate, Vitamin B6 dioctanoate, Vitamin B2 or its derivatives, Vitamin B12, Vitamin B15 or its derivatives; Vitamin E such as α-tocopherol, β-tocopherol, γ-tocopherol, vitamin E acetate, vitamin D , Vitamin H, pantothenic acid, pantethine, pyrrolo Preferred examples include vitamins such as quinoline quinone; antibacterial agents such as phenoxyethanol; amino acids such as hydroxyproline, glutamic acid, arginine, aspartic acid, and trimethylglycine; and derivatives thereof. In particular, trimethylglycine has a moisturizing action and also has an action of suppressing the association of vesicles. Therefore, it is preferable to contain such a component, and a preferable content thereof is 0.05 to 2% by mass. More preferably, it is 0.1-0.5 mass%. The cosmetic of the present invention can be produced by treating such components according to a conventional method.

  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.

An essence cosmetic, which is a cosmetic of the present invention, was prepared according to the formulation shown below. In other words, the ingredients (a) and (b) were heated to 80 ° C., (c) was added to (a), and the mixture was stirred and dispersed. This material is a cosmetic form semitransparent phospholipid globules are dispersed in a viscosity lotion, a viscosity of 2500 mPa · s (B-type viscometer, No. 4 rotor, 12 rpm) was. Similarly, Comparative Example 1 in which trehalose was replaced with water was also produced. About Essence cosmetics 1 and the comparative example 1, it centrifuged at 1000 rpm for 1 minute, the blackboard was laid down, and it observed from the upper 90 degree angle, and confirmed the presence or absence of sedimentation. No sediment was observed in the essence cosmetic 1, but sedimentation was clearly observed in Comparative Example 1. From this, it was found that trehalose stabilized vesicle dispersion. Further, after essence cosmetic 1 and Comparative Example 1 were stored at 40 ° C. for 3 months, the size of the dispersed spherules was observed under a microscope. In Comparative Example 1, the average was 153 μm, and it was found that the association and fusion of microspheres occurred.

  In the same manner as in Example 1, an essence cosmetic 2 as a cosmetic of the present invention was produced according to the formulation shown below. The viscosity of this product was 1700 mPa · s, and centrifugation was performed at 1000 rpm for 1 minute, the blackboard was laid down, and observed from an angle of 90 degrees at the top, and the presence or absence of sedimentation was confirmed. The average particle size of the microspheres after storage at 3 ° C. for 3 months was 78 μm, suggesting that association and fusion began to occur. It can be seen that it is preferable to contain an alkyl-modified carboxyvinyl polymer and / or a salt thereof.

  In the same manner as in Example 1, an essence cosmetic 2 as a cosmetic of the present invention was produced according to the formulation shown below. This product has a viscosity of 2700 mPa · s, centrifuged at 1000 rpm for 1 minute, laid on a blackboard, and observed from the upper 90 ° angle to confirm the presence or absence of sedimentation. The average particle size of the microspheres after storage at 3 ° C. for 3 months was 65 μm, suggesting that association and fusion began to occur. It can be seen that it is preferable to contain trimethylglycine.

  The present invention can be applied to cosmetics.

Claims (5)

A cosmetic comprising 1) phospholipid microspheres including ubidecarenone , and 2) trehalose ,
A cosmetic material, wherein the phospholipid microspheres are produced by heating and dissolving phospholipids or phospholipids and sterols, cooling to 60 ° C., and then adding ubidecarenone . The phospholipid spherules, characterized in that it is one containing the hydrogenated lecithin and phytosterols, cosmetic composition according to claim 1. The cosmetic according to claim 1 or 2 , further comprising an alkyl-modified carboxyvinyl polymer and / or a salt thereof. Characterized in that it does not contain a nonionic surfactant, cosmetic according to any one of claims 1-3. Furthermore, trimethylglycine is contained, Cosmetics in any one of Claims 1-4 characterized by the above-mentioned.