JP4575755B2 - Liquid for external use - Google Patents

Description

  The present invention relates to a liquid preparation for external use which is excellent in use feeling and stable over time without causing separation or sedimentation of components.

  Tocopherol is known to be effective in preventing skin aging because it has an antioxidant action and a blood circulation promoting action. On the other hand, it is known that silk powder has a skin protecting effect and a moisturizing effect, and also has a smooth feeling of use. Therefore, by blending both these components, a preparation having both effects is expected, and its realization is desired.

However, since tocopherol is an oil component and silk powder is a solid component, there is a problem that components are separated and settled over time when used as a liquid for external use.
In order to solve the above problems, a method is known in which for the purpose of dispersing tocopherol, a mixture of tocopherol and oil such as olive oil is emulsified with a surfactant, and the resulting emulsified particles are dispersed in a liquid agent. However, when fats and oils are blended in an external liquid preparation for the purpose of replenishing water, the skin surface is covered with fats and oils during application, and the transfer of moisture into the skin is hindered.

  Further, as a method for dispersing silk powder, a method using a thickener is common. However, even if silk powder is dispersed with a thickener, there is a problem that tocopherol, which is an oil component, is separated from water.

Further, a skin external preparation (Patent Document 1) containing hydrolyzed silk protein and seaweed extract for the purpose of improving dry skin, wrinkles and rough skin is disclosed, specifically, hydrolyzed silk protein aqueous solution, carboxyvinyl polymer and Examples include oil-in-water emulsified creams containing water-containing lotion and tocopherol, hydrolyzed silk protein aqueous solution, hydrogenated soybean phospholipid, carboxyvinyl polymer and water. However, hydrolyzed silk protein is different from silk powder.
JP 2003-176218 A

  An object of the present invention is to obtain an externally applied liquid preparation that contains tocopherol and silk powder, has an excellent usability, and has a stable dispersed state over time without causing separation or sedimentation.

  As a result of various investigations to solve the above-mentioned problems, it is excellent in feeling of use and stable as a preparation by containing phospholipid and xanthan gum in an external solution containing tocopherol, silk powder and 82 to 99% by weight of water. It has been found that an external liquid preparation having a state can be obtained.

  That is, the present invention provides a solution for external use containing tocopherol, silk powder, phospholipid, xanthan gum and water, and the water content is 82 to 99% by weight. From another viewpoint, it is a method of stably dispersing tocopherol and silk powder in an external liquid preparation containing water, wherein phospholipid and xanthan gum are blended in the external liquid preparation, and the water content is 82 to 99%. The present invention provides a method characterized by the following.

  According to the present invention, it has become possible to stably disperse tocopherol and silk powder, which have been difficult so far, in a liquid preparation.

  The external preparation of the present invention is an aqueous solution containing tocopherol, silk powder, phospholipid, xanthan gum and water.

  In the present invention, tocopherol includes tocopherol, tocopherol derivatives and salts thereof. For example, d-α-tocopherol, dl-α-tocopherol, d-α-tocopherol acetate, dl-α-tocopherol acetate, dl-α-tocopherol nicotinate, dl-α-tocopherol calcium succinate, d-α succinate -Tocopherol, succinic acid dl-α-tocopherol and the like. The amount of tocopherol blended is preferably 0.01 to 2% by weight, more preferably 0.02 to 1% by weight, and particularly preferably 0.05 to 0.5% by weight, based on the total amount of the external preparation. If it exceeds 2% by weight, it becomes sticky and the feeling of use becomes worse. If it is less than 0.01% by weight, a large amount of coating is required to obtain efficacy as an active ingredient such as an antioxidant action and a blood circulation promoting action. Therefore, the above range is preferable.

  In the present invention, the silk powder is a water-insoluble protein powder constituting silk fibers obtained from rabbit cocoons, and is mainly composed of fibroin. Examples of the silk powder include (as a commercial product) Silken G powder (Ichimaru Falcos) and Silk ID powder K-50 (Idemitsu Petrochemical). The silk powder as used in the present invention may be modified with a surface to have various additional effects. Examples include (as a commercial product) Silk ID Powder A-705 (Idemitsu Petrochemical), Silk ID Powder S-702 (Idemitsu Petrochemical), and Silk ID Powder L-710 (Idemitsu Petrochemical). The amount of the silk powder blended is preferably 0.01 to 10% by weight, more preferably 0.1 to 5% by weight, and particularly preferably 0.3 to 5% by weight with respect to the total amount of the liquid agent. If it exceeds 10% by weight, the dry feel derived from the powder becomes strong and the moist feeling decreases, and if it is less than 0.01% by weight, a large amount of coating may be required to obtain the effect. Is preferred.

In the present invention, the phospholipid is a complex lipid containing a phosphate residue, and examples thereof include natural phospholipids, synthetic phospholipids, and hydrogenated phospholipids obtained by hydrogenating naturally-derived phospholipids.
Examples of natural phospholipids include phospholipids extracted from microorganisms such as phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, lysophosphatidylcholine, sphingomyelin, egg yolk lecithin, soybean lecithin, and Escherichia coli. Examples of commercially available products include COATSOME NC-50 (NOF), presome (Nippon Seika) and the like.

  Examples of the synthetic phospholipid include dioleoylphosphatidylcholine, dilauroyl phosphatidylcholine, dimyristoyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoyl phosphatidylcholine, palmitoyl oleoyl phosphatidylcholine, and the like. Commercially available products include COATSOME MC-2020, COATSOME MC-4040, COATSOME MC-6060, COATSOME MC-8080, COATSOME MC-8181, COATSOME MC-6081 (NOF) and the like.

Examples of the hydrogenated phospholipid include hydrogenated soybean phospholipid, hydrogenated egg yolk phospholipid, hydrogenated phosphatidylcholine, hydrogenated phosphatidylserine, and the like. Commercial products include Resinol S-10, Resinol S-10E, Resinol S-10M, Resinol S-10EX, Resinol S-PIE (Nikko Chemicals), COATSOME
NC-21 (NOF), Phospholipon 100H, Phospholipon 90H, Phospholipon 80H, Phospholipon 90G (Phospholipid).

  Of these phospholipids, hydrogenated phospholipids are preferred. Specifically, a hydrogenated phospholipid having a hydrogenated phosphatidylcholine content of 70% or more, preferably 80% or more, more preferably 90% or more is preferable. Hydrogenated phosphatidylcholine is preferable in that the viscosity of the aqueous external liquid preparation is increased and a stable dispersion state is obtained.

  In the present invention, phospholipids can be used alone or in combination of two or more. The blending amount of the phospholipid is preferably 0.01 to 5% by weight, more preferably 0.1 to 2% by weight, and particularly preferably 0.3 to 1% by weight with respect to the total amount of the external solution. If it exceeds 5% by weight or less than 0.01% by weight, a stable dispersion effect of tocopherol may not be obtained.

  In the present invention, xanthan gum is a polysaccharide obtained by fermentation using a carbohydrate such as starch using a microorganism such as Xanthomonas. Xanthan gum includes purified, dried and powdered commercial products such as Keltrol, Keltrol T, Keltrol F, Kelzan, Kelzan S (Kelco Biopolymer), Neosoft XC, Neosoft XS (Taiyo Kagaku), and San Ace (Sanei). Source FFI) and the like. The blending amount of xanthan gum is preferably 0.005 to 1% by weight, more preferably 0.01 to 0.5% by weight, particularly preferably 0.1 to 0.4% by weight, based on the total amount of the external liquid preparation. is there. If it exceeds 1% by weight, the twist and stickiness are strong and the feeling of use becomes worse, and if it is less than 0.005% by weight, the intended dispersion effect may not be obtained.

  The amount of water used in the present invention is adjusted in accordance with the amount of the other compounding agents, but is preferably 82 to 99% by weight, more preferably 85 to 98% by weight, particularly with respect to the total amount of the external preparation. Preferably it is 90 to 96 weight%. If it exceeds 99% by weight, it may be difficult to obtain the effect of tocopherol or silk powder, and if it is less than 82% by weight, the skin may not be sufficiently moisturized.

  In addition, the external preparation mentioned here refers to a liquid applied to the skin, and examples thereof include those used for the purpose of replenishing deficient moisture in the skin and maintaining a moist skin condition. When the external use liquid preparation of this invention is used for such a use, it is preferable not to mix | blend oil components other than the essential component of this invention. However, a small amount of oil may be included as long as the effects of the present invention are not impaired.

  The external liquid preparation of the present invention can contain an active ingredient other than tocopherol, a neutralizing agent, a preservative, a stabilizer, a wetting agent, and the like, but it does not need to be contained. Moreover, what can be contained is not limited to these.

Other active ingredients other than tocopherol include anti-inflammatory agents such as potassium or ammonium salts of glycyrrhizic acid, antihistamines such as diphenhydramine hydrochloride used for the treatment of pruritus, anti-acne agents such as pionine, ascorbic acid or ascorbic acid derivatives, etc. Humectants such as hyaluronic acid, alge colloid, and trehalose.
Examples of neutralizing agents include organic acids such as citric acid, phosphoric acid, tartaric acid and lactic acid, inorganic acids such as hydrochloric acid, alkali hydroxides such as sodium hydroxide and potassium hydroxide, triethanolamine, diethanolamine and diisopropanolamine. And the like.

Examples of preservatives include p-hydroxybenzoates, benzalkonium chloride, and the like.

Examples of the stabilizer include sodium sulfite, sodium hydrogen sulfite, dibutylhydroxytoluene, butylhydroxyanisole, edetic acid and the like.
Examples of the wetting agent include polyhydric alcohols such as glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, isopropylene glycol, and polyethylene glycol.

  The pH of the external preparation of the present invention is usually preferably pH 4-8, more preferably pH 5.5-6.5, from the viewpoint of separation stability of the preparation, skin irritation and the like.

  The viscosity of the external liquid preparation of the present invention is preferably 0.05 Pa · s to 1 Pa · s, more preferably 0.1 Pa · s to 0.5 Pa · s. If it is less than 0.05 Pa · s, the silk powder and phospholipid fine particles may settle. Moreover, when it exceeds 1 Pa.s, fluidity | liquidity falls and elongation may worsen. The viscosity can be measured by, for example, a cone plate type rotational viscometer AR1000-N (TA instrument).

  The external preparation of the present invention can be produced by a usual method. For example, phospholipid and tocopherol are heated in polyhydric alcohol to 80 ° C. or more and completely dissolved, and then mixed with water until uniform. Furthermore, it can be prepared by adding silk powder and xanthan gum and mixing until uniform.

  EXAMPLES Hereinafter, the present invention will be described more specifically with reference to examples, but the present invention is not limited to these examples.

[Example 1]
Tocopherol acetate 0.2 g and hydrogenated soybean phospholipid 0.5 g (Phospholipon 90H: Phospholipid) were added to 5 g of 1,3-butylene glycol, and the mixture was well stirred and mixed at 80 ° C. To this solution, 30 g of purified water was added and well stirred and mixed (preparation solution A).

  Xanthan gum (Kelco Biopolymer) 0.28 g, sodium edetate 0.01 g, and methyl paraoxybenzoate 0.1 g were added to purified water 60 g, and well stirred and mixed. After thoroughly stirring and mixing this solution, 0.5 g of Preparation Solution A and Silk Powder (Silkgen G Powder: Ichimaru Falcos) are added, and after stirring and mixing, defoaming is performed under reduced pressure, and water is added to make a total amount of 100 g. As a result, an aqueous external preparation was obtained.

[Comparative Examples 1-5]
In the same manner as in Example 1, using the components shown in Table 1, external preparations of Comparative Examples 1 to 5 were obtained. The amount of each thickener used in Example 1 and each comparative example was adjusted so as to have the same viscosity (about 0.3 Pa · s). The sodium alginate of Comparative Example 3 is Kimika Argin IS (Kimika), the hydroxyethyl cellulose of Comparative Example 4 is HEC CF-Y (Sumitomo Seika), and the hydroxypropyl methylcellulose 2208 of Comparative Example 5 is Metroise 90SH-15000. (Shin-Etsu Chemical Co., Ltd.).

[Test example]
In order to examine the appearance stability of the prepared preparations, each preparation of Example 1 and Comparative Examples 1 to 5 was filled in a glass bottle, and after 1 week at 40 ° C., 2 weeks and 2 months later, 1 week at 60 ° C. The presence or absence of appearance changes (separation or sedimentation) after subsequent storage was confirmed. The case where the appearance change was not recognized was indicated by ○, and the case where the appearance change was observed was indicated by ×.

  The viscosity was measured under the following conditions using a cone plate type rotational viscometer AR1000-N (TA instrument). Adapter: 6 cm, 2 ° plate, 20 ° C., shear stress 2 Pa.

  When a phospholipid was not blended in a liquid preparation containing tocopherol, silk powder and water (Comparative Example 1), separation (tocopherol) was observed in the preparation immediately after preparation. Further, in the preparation not containing xanthan gum (Comparative Example 2), sedimentation of silk powder was observed immediately after preparation.

  In addition, the viscosity was adjusted to about 0.3 Pa · s using a polymer other than xanthan gum such as sodium alginate (Comparative Example 3), hydroxyethyl cellulose (Comparative Example 4), hydroxypropyl methylcellulose (Comparative Example 5), In all the results, a change in appearance was observed after storage at 40 ° C. for 1 week or 60 ° C. for 1 week, and the stability was poor.

  However, the formulation (Example 1) in which phospholipid and xanthan gum were blended with an external solution containing tocopherol, silk powder and water, no change in appearance was observed even after storage at 60 ° C for 1 week or after storage at 40 ° C for 2 months, It showed good stability.

  In addition, when the usability of Example 1 was evaluated, a smooth and moist feeling was imparted, and a better usability was also obtained.

Claims (2)

A liquid for external use comprising tocopherol, silk powder, phospholipid, xanthan gum and water, wherein the water content is 82 to 99% by weight. A method for stably dispersing tocopherol and silk powder in an external liquid preparation containing water, the step of mixing tocopherol and phospholipid with water to obtain a mixed solution, and the mixed solution obtained in the above step, includes the step of mixing the xanthan gum, and wherein the setting the content of water and 82-99% in the liquid for external use.