JP5022568B2 - Essence dosage form topical skin 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 (including quasi-drugs) in an essence dosage form.

In skin external preparations such as cosmetics, an essence dosage form having a viscosity of 10000 mPascal · second or more is a very useful dosage form because the skin external preparation can be administered accurately without spreading to the site to be administered. It can be said. This can be said to be more remarkable in types of cosmetics such as quasi-drugs that have clearer efficacy and effects. In such an essence dosage form, it can be said that a particularly big problem is a decrease in viscosity over time. In particular, cationized cellulose scan, in the polymethacrylate polymer component or its salt containing the nitrogen atom such as acryloyl lysine, such time thinning problems likely to occur, it can be said that a countermeasure is required. These polymer compounds containing nitrogen atoms and / or their salts are useful as components for skin protection cosmetics because of their excellent affinity for skin and water retention.

  Usually, in the essence dosage form skin external preparation, as the component for maintaining the viscosity, a carboxyvinyl polymer which may be alkyl-modified and / or a salt thereof is used. This is a component with extremely good viscosity stability over time in the field of external preparation for skin, but even if such a component is used, it contains the above-mentioned polymer containing nitrogen atom or a salt thereof. In the essence dosage form, it is said that the effect is not achieved.

  As the thickener other than the carboxyvinyl polymer and / or salt thereof which may be alkyl-modified, in the field of external preparation for skin, xanthan gum, carboxymethylcellulose and / or salt thereof, locust bean gum, gum arabic Polyacrylic acid and / or a salt thereof, polyvinyl alcohol and the like are known, and any of these is said to decrease in viscosity over time.

  On the other hand, carrageenan is old, like the carboxyvinyl polymer and / or salt thereof, xanthan gum, carboxymethylcellulose and / or salt thereof, locust bean gum, gum arabic, polyacrylic acid and / or salt thereof, and polyvinyl alcohol. From this, it is a component that is used as a thickening agent in skin external preparations such as cosmetics. However, such a component does not reduce viscosity even in the presence of a polymer compound containing nitrogen atoms and / or a salt thereof. It has never been known that there is an action capable of stably maintaining the viscosity. Skin external preparations that handle carrageenan and the above-mentioned polymer containing a nitrogen atom in parallel as one of the constituents are already known (for example, Patent Document 1, Patent Document 2, Patent Document 3, (See Patent Documents 4 and 5), but there is no known technique for directly incorporating the polymer compound containing nitrogen atom and / or a salt thereof and carrageenan into a skin external preparation. However, it has not been known at all that such an external preparation for skin is extremely excellent in the stability of viscosity with time.

JP 2004-339144 A JP 2004-300106 A Japanese Patent Laid-Open No. 2004-262851 JP 2004-149463 A JP 2004-075552 JP

The present invention has been made under such circumstances, excellent bioactivity, cationized cellulose scan, in the skin external preparation containing a polymer or its salt containing the nitrogen atom such as poly methacryloyl lysine, its It is an object of the present invention to provide a technique for improving the viscosity stability over time.

In view of such circumstances, the present inventors have found that excellent bioactivity, cationized cellulose scan, in the skin external preparation containing a polymer or its salt containing the nitrogen atom such as port Increment Tactile Leroy Le lysine, its viscosity As a result of diligent research efforts in search of a technique for improving the aging stability of the skin, an external skin preparation containing 1) carrageenan and 2) a specific nitrogen-containing polymer and / or salt thereof is The inventors have found that it has characteristics and have completed the invention. That is, the present invention is as follows.
(1) Viscosity is an essence dosage form of the external preparation for skin is more than 10000MPascal · sec, 1) and carrageenan 0.5-3 wt%, 2) port Increment Tak Leroy Le lysine is selected from cationic cellulose and Polyquaternium 61 The skin external preparation characterized by containing the 1 type, or 2 or more types of nitrogen-containing polymer and / or its salt.
(2) The skin external preparation according to (1), wherein the content of the nitrogen-containing polymer and a salt thereof is 0.1 to 10% by mass.
(3) The skin external preparation according to (1) or (2), which is a cosmetic.
(4) The external preparation for skin according to any one of (1) to (3), wherein the pH is 6.5 or less.

According to the present invention, is excellent in physiological activities, cationized cellulose scan, in the skin external preparation containing a polymer or its salt containing the nitrogen atom such as port Increment Tactile Leroy Le lysine, improving an aging stability of the viscosity technology Can be provided.

(1) Carrageenan which is an essential component of the external preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing carrageenan as an essential component. Carrageenan is a polysaccharide based on red algae such as the genus Tunomata, and has galactose as a main constituent monosaccharide and a sulfate group. Carrageenan has long been used in cosmetics as a thickener. Carrageenan as a cosmetic raw material is sold by various manufacturers. For example, “Delta Gel C80”, “Delta Gel C200”, “Delta Gel S80”, “Delta Gel S200” of Nippon Biocon Co., Ltd., “Carrageenan” of Nippon Carrageenan Industry Co., Ltd. (Registered Trademark) FA "and the like can be preferably exemplified, and any of these can be used, and particularly preferred is" CGPam (Registered Trademark) FA "sold by Dainippon Pharmaceutical Co., Ltd. This is because this product is particularly excellent in stability improvement effect. In the external preparation for skin of the present invention, such a component has an action of maintaining the viscosity of the system for a long period of time. To exhibit such effects, the carrageenan Ru is contained 0.5-3 wt% against the total amount of the skin treatment composition. This is for realizing an appropriate viscosity and for realizing the stabilizing action.

(2) the external preparation for skin of the nitrogen-containing polymer present invention is an essential component of the skin external preparation of the present invention, one or more nitrogen-containing selected from Po Increment Tactile Leroy Le lysine, cationic cellulose and Polyquaternium 61 It contains a polymer and / or a salt thereof as an essential component. As such a nitrogen-containing polymer, since a commercial product already exists as a cosmetic raw material, such a commercial product can be purchased and used. As such a commercially available product, Po Rikuotaniumu 61 (Ripideyua PMB; manufactured by NOF CORPORATION) can be preferably exemplified. Examples of the salt include mineral acid salts such as hydrochloride, sulfate, nitrate, phosphate and carbonate, and organic acid salts such as citrate, oxalate and acetate. In the external preparation for skin of the present invention, such a nitrogen-containing polymer and / or salt thereof may contain only one species or may contain two or more species in combination. In the external preparation for skin of the present invention, such a nitrogen-containing polymer and / or a salt thereof is familiar with the skin, forms a moisturizing film on the skin, improves the skin barrier function, and also breaks the peptide on the skin. And has the effect of repairing such disconnection. By such an action, the skin external preparation of the present invention is imparted with a rare and rare skin protecting action. In order to exert such effects in the external preparation for skin of the present invention, the nitrogen-containing polymer and / or salt thereof is 0.1 to 10% by mass based on the total amount of the external preparation for skin, in total. More preferably, the content is 1 to 5% by mass.

(3) The skin external preparation of this invention The skin external preparation of this invention contains the said essential component, It is characterized by the above-mentioned. The topical skin preparation of the present invention can be applied without particular limitation as long as it is externally administered to the skin. Examples thereof include cosmetics (including quasi-drugs), pharmaceutical compositions for external use on skin, and miscellaneous goods. Among these, cosmetics are particularly preferable, and quasi drugs are particularly preferable. As the dosage form of the preparation, a high-viscosity dosage form having a viscosity of 10,000 mPascal · second or more, a dosage form generally referred to as an essence dosage form, is employed. This is because, by adopting such a dosage form, it is possible to accurately administer to the local site where the effect of the active ingredients blended at the same time is necessary, and to limit the administration range. At this time, the pH is preferably not more than 6.5 which is close to that of the skin.

In the external preparation for skin of the present invention, in addition to the above-mentioned essential components, any formulation component that is usually used in external preparations for skin can be contained. Examples of such optional components, e.g., macadamia nut oil, Abou transient oil, corn oil, olive oil, rapeseed oil, sesame oil, castor oil, safflower oil, cottonseed oil, jojoba oil, coconut oil, palm oil, liquid lanolin, cured Oils such as coconut oil, hydrogenated oil, owl, hydrogenated castor oil, beeswax, candelilla wax, carnauba wax, ibotarou, lanolin, reduced lanolin, hard lanolin, jojoba wax, waxes, liquid paraffin, squalane, pristane, ozokerite, paraffin, ceresin , Hydrocarbons such as petrolatum, 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 Alcohol, behenyl alcohol, octyldodecanol, higher alcohol such as myristyl alcohol, cetostearyl alcohol, etc., 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 Loxane, linear polysiloxane such as diphenylpolysiloxane, cyclic polysiloxane such as octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, dodecamethylcyclohexanesiloxane, amino-modified polysiloxane, polyether-modified polysiloxane, alkyl-modified polysiloxane, Oil agents such as silicone oil such as modified polysiloxane such as fluorine-modified polysiloxane, anionic surfactants such as fatty acid soap (sodium laurate, sodium palmitate, etc.), potassium lauryl sulfate, triethanolamine ether of alkyl sulfate, chloride 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.), amphoteric surfactants such as acylmethyltaurine, sorbitan fatty acid esters (sorbitan) Monostearate, sorbitan sesquioleate, etc.), glycerin fatty acids (eg, glyceryl monostearate), propylene glycol fatty acid esters (eg, propylene glycol monostearate), 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 alkylphenyl 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 Polyols such as recall, dipropylene glycol, diglycerin, isoprene glycol, 1,2-pentanediol, 2,4-hexylene glycol, 1,2-hexanediol, 1,2-octanediol, pyrrolidone carboxylic acid Moisturizing ingredients such as sodium, lactic acid, sodium lactate, guar gum, quince seed, galactan, gum arabic, pectin, mannan, starch, xanthan gum, curdlan, methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, methyl hydroxypropyl cellulose, hydroxyethyl guar gum, Carboxymethyl guar gum, dextran, locust bean gum, succinoglucan, caronic acid, chitin, chitosan, carboxymethyl chitin, agar, polyvinyl alcohol Thickener such as coal, polyvinylpyrrolidone, carboxyvinyl polymer, sodium polyacrylate, polyethylene glycol, bentonite, etc., surface may be treated, mica, talc, kaolin, synthetic mica, calcium carbonate, magnesium carbonate, anhydrous silica Powders such as acid (silica), aluminum oxide, barium sulfate, inorganic pigments of which the surface may be treated, bengara, yellow iron oxide, black iron oxide, cobalt oxide, ultramarine, bitumen, titanium oxide, zinc oxide The surface may be treated, pearl agents such as titanium mica, fish phosphorus foil, bismuth oxychloride, red 202, red 228, red 226, yellow 4, which may be raked, Blue 404, Yellow 5, Red 505, Red 230, Red 223, Orange 201, Red 213, Yellow Organic powders such as No. 04, Yellow No. 203, Blue No. 1, Green No. 201, Purple No. 201, Red No. 204, polyethylene powder, polymethyl methacrylate, nylon powder, organopolysiloxane elastomer, Paraaminobenzoic acid UV absorbers, anthranilic acid UV absorbers, salicylic acid UV absorbers, cinnamic acid UV absorbers, benzophenone UV absorbers, sugar UV absorbers, 2- (2'-hydroxy-5 ' -T-octylphenyl) benzotriazole, ultraviolet absorbers such as 4-methoxy-4'-t-butyldibenzoylmethane, lower alcohols such as ethanol and isopropanol, vitamin A or a derivative thereof, vitamin B ₆ hydrochloride, vitamin B ₆ tripalmitate, vitamin B ₆ dioctanoate, vitamin B ₂ or induction thereof , Vitamin B such as vitamin B _12, vitamin B ₁₅ or a derivative thereof, alpha-tocopherol, beta-tocopherol, .gamma.-tocopherol, vitamin E such as vitamin E acetate, vitamin D, vitamin H, pantothenic acid, pantethine, Preferred examples include vitamins such as pyrroloquinoline quinone. Of these, particularly preferred are one or two selected from 1,2-pentanediol, isoprene glycol, 1,2-hexanediol, 2,4-hexylene glycol, and 1,2-octanediol. That's it. Since these polyhydric alcohols have antibacterial properties, the content of components such as parabens that sometimes cause transient stimulation can be reduced by containing them. The preferable content of such components is 1 to 10% by mass, more preferably 2 to 5% by mass. A form containing such a mass ratio and containing no parabens is a particularly preferred form. The external preparation for skin of the present invention can be produced by treating such optional components and essential components according to a conventional method.

  Hereinafter, the present invention will be described in more detail with reference to examples, but it goes without saying that the present invention is not limited to such examples.

[Reference Example 1]
In accordance with the formulation shown below, is a skin Hadagaiyo agent, it was to create a cosmetics (quasi-drug). That is, the components of a and b are heated to 80 ° C. and mixed well, and then a b is gradually added to b under stirring, and then stirred and cooled to obtain an essence form (viscosity: 41000 mPascal · second; B-type viscosity). A total of No. 4 rotor, 20 ° C., pH 6.24) was obtained. In this, Carrageenan was replaced with Comparative Example 1 (viscosity: 34000 mPascal · second, pH 6.15) substituted with gum arabic, 20% carboxyvinyl polymer (neutralized by adding 1 ml of 10% potassium hydroxide aqueous solution after addition). Example 2 (viscosity 38000 mPascal · second, pH 8.2) and Comparative Example 3 (viscosity 36000 mPascal · second, pH 6.15) substituted with xanthan gum were also prepared in the same manner.

Icarrageenan 1% by mass
("Ceepe gum (registered trademark) FA")
1,3-butanediol 5% by mass
Glycerin 3% by mass
1,2-hexanediol 3% by mass
Ethanol 5% by mass
2 Polyvinylpyrrolidone 2% by mass
10% aqueous citric acid solution 0.1% by mass
Sodium citrate 0.1% by mass
80.8% by mass of water

The cosmetic 1 and Comparative Examples 1 to 3 produced as described above were subjected to a storage test for 1 month at 5 ° C, 20 ° C and 40 ° C. Table 1 shows the results of measuring the viscosity at a constant weight of 20 ° C. after completion of the storage test. It supersedes any, skin Hadagaiyo agent is found to be excellent in stability.

[Reference Example 2]
In accordance with the following formulation in the same manner as the cosmetics 1, to produce a cosmetic 2 to 5 is a leather Hadagaiyo agent, was subjected to a storage test. The results are shown in Table 2. From this, it can be seen that all the samples have excellent stability. The pH of cosmetic 2 was 6.30, cosmetic 3 was 5.95, cosmetic 4 was 5.90, and cosmetic 5 was 5.80.

Icarrageenan 1% by mass
("Ceepe gum (registered trademark) FA")
1,3-butanediol 5% by mass
Glycerin 3% by mass
Ingredients in Table 2 3% by mass
Ethanol 5% by mass
2 Polyvinylpyrrolidone 2% by mass
10% aqueous citric acid solution 0.1% by mass
Sodium citrate 0.1% by mass
80.8% by mass of water

[Reference Example 3]
In accordance with the following formulation in the same manner as the cosmetics 1, to produce a cosmetic 6, which is a skin Hadagaiyo agent, it was subjected to a storage test. The result is a is 40500mPascal · seconds viscosity before storage, after 1 month storage is, 5 ℃ (42000mPascal · sec), 20 ℃ (39000mPascal · sec.), Ri 40 ℃ (38000mPascal · sec.) Der, skin Hadagaiyo The stability of the agent was confirmed.

Icarrageenan 1% by mass
("Ceepe gum (registered trademark) FA")
1,3-butanediol 5% by mass
Glycerin 3% by mass
1,2-hexanediol 3% by mass
Ethanol 5% by mass
Ropolymethacryloyloxyethyl phosphorylcholine
2% by mass
10% aqueous citric acid solution 0.1% by mass
Sodium citrate 0.1% by mass
80.8% by mass of water

[ Example 1 ]
Similarly to cosmetic 1, cosmetic 7 as an external preparation for skin of the present invention was produced according to the following formulation, and a storage test was conducted. The results are the 39000MPascal · sec viscosity before storage, after 1 month storage is, 5 ℃ (38000mPascal · sec), 20 ℃ (36000mPascal · sec), Ri 40 ℃ (35000mPascal · sec) der, the present invention The stability of the external preparation for skin was confirmed.

Icarrageenan 1% by mass
("Ceepe gum (registered trademark) FA")
1,3-butanediol 5% by mass
Glycerin 3% by mass
1,2-hexanediol 3% by mass
Ethanol 5% by mass
Locationized cellulose 1% by mass
10% aqueous citric acid solution 0.1% by mass
Sodium citrate 0.1% by mass
81.8% by mass of water

[ Example 2 ]
In the same manner as cosmetic 1, cosmetic 8 as an external preparation for skin of the present invention was produced according to the following formulation, and a storage test was conducted. As a result, the viscosity before storage was 40000 mPascal · second, and after storage for 1 month, it was 5 ° C. (41000 mPascal · second), 20 ° C. (39000 mPascal · second), and 40 ° C. (37000 mPascal · second). The stability of the topical skin preparation was confirmed.

Icarrageenan 1% by mass
("Ceepe gum (registered trademark) FA")
1,3-butanediol 5% by mass
Glycerin 3% by mass
1,2-hexanediol 3% by mass
Ethanol 5% by mass
Ropolymethacryloyl lysine 1% by mass
10% aqueous citric acid solution 0.1% by mass
Sodium citrate 0.1% by mass
81.8% by mass of water

[ Example 3 ]
In the same manner as cosmetic 1, cosmetic 9 , which is an external preparation for skin of the present invention, was produced according to the following prescription and subjected to a storage test. As a result, the viscosity before storage was 37000 mPascal · second, and after storage for 1 month, it was 5 ° C. (35000 mPascal · second), 20 ° C. (33000 mPascal · second), and 40 ° C. (30000 mPascal · second). The stability of the topical skin preparation was confirmed.

Icarrageenan 1% by mass
("Ceepe gum (registered trademark) FA")
1,3-butanediol 5% by mass
Glycerin 3% by mass
1,2-hexanediol 3% by mass
Ethanol 5% by mass
Ropolyquaternium 61 1% by mass
10% aqueous citric acid solution 0.1% by mass
Sodium citrate 0.1% by mass
81.8% by mass of water

  The present invention can be applied to cosmetics such as quasi drugs.

Claims (4)

A skin external preparation in the form of an essence dosage form having a viscosity of 10,000 mPascal · sec or more, which is selected from 1) carrageenan 0.5 to 3% by mass and 2 ) polymethacryloyllysine , cationized cellulose and polyquaternium 61 A skin external preparation comprising two or more types of nitrogen-containing polymers and / or salts thereof.   Content of the said nitrogen-containing polymer and its salt is 0.1-10 mass%, The skin external preparation of Claim 1 characterized by the above-mentioned.   The external preparation for skin according to claim 1 or 2, which is a cosmetic.   The skin external preparation according to any one of claims 1 to 3, wherein the pH is 6.5 or less.