JP5437552B2 - Two-component mixed topical skin preparation - Google Patents

Description

  The present invention relates to a two-component mixed type skin external preparation, and more particularly, to a two-component mixed type skin external formulation excellent in stability of an emulsion after mixing, which contains ascorbic acid.

  Conventionally, skin preparations such as cosmetics are expected to have various improvements on the skin, such as promoting collagen growth, protecting skin tissue against external stimuli, suppressing skin pigmentation, and improving texture. Ascorbic acid has been blended.

  However, ascorbic acid is decomposed due to the presence of an aqueous component, the stability is remarkably lowered, and further, there is a problem that the appearance is changed to brown or an odor is generated due to the decomposition of ascorbic acid. For such a decrease in the stability of ascorbic acid, blending of an antioxidant or the like is conceivable, but even when an antioxidant or the like is actually blended, the effect is not sufficient.

  As a solution to the above problem, a cosmetic composition is known in which a hydrophilic carrier containing a gelling agent and powdered ascorbic acid are stored separately and mixed immediately before use (see Patent Document 1). However, this product does not satisfy the feeling of use, such as a sticky feeling when it is applied to the skin. Furthermore, when the composition after mixing is an emulsion, the storage stability of the emulsion is sufficient. There was a problem that was not.

Japanese Patent No. 2651366

  Therefore, there has been a demand for the development of an external preparation for skin such as cosmetics containing ascorbic acid that has no stickiness and has a good feeling of use and is excellent in the storage stability of the emulsion after mixing.

  In view of this situation, the present inventor has intensively studied, and as a result, in a two-component mixed skin external preparation used by mixing an oil-in-water emulsion solution and a solid preparation containing ascorbic acid, lysophospholipid as an emulsifier By using it as a liquid agent, a two-component mixed skin preparation with a stable ascorbic acid stability, a good emulsion storage stability, no stickiness with a fresh feeling of use, and a high skin improvement effect is obtained. As a result, the present invention has been completed.

That is, the present invention provides the following preparations (A) and (B)
(A) Oil-in-water emulsion solution containing lysophospholipid, oil agent and water (B) A solid agent containing ascorbic acid, wherein (A) and (B) are mixed and used It is a mixed skin external preparation.

  Since the present invention uses lysophospholipid as an emulsifier on the oil-in-water emulsion solution side, the emulsion obtained by mixing has excellent stability even in a low pH region after mixing with a solid agent containing ascorbic acid. It can be maintained.

  Therefore, the two-component mixed type skin external preparation of the present invention is excellent in the storage stability of the emulsion after mixing, and has a fresh feeling of use without stickiness. Moreover, since it contains ascorbic acid stably, it is excellent in the skin improvement effect.

  The two-component mixed skin external preparation of the present invention comprises two types of preparations, a liquid (A) and a solid (B), and the liquid (A) is an oil-in-water emulsion containing lysophospholipid, oil and water. It is.

  The lysophospholipid contained in the liquid preparation (A) of the present invention is one of enzyme-modified phospholipids, in which the ester bond at the 2-position of the phospholipid is hydrolyzed by phospholipase A2, Unlike phospholipids having fatty acids, they have single chain fatty acids and high HLB values. The lysophospholipid can be used without particular limitation as long as it is used in ordinary cosmetics. For example, soybean-derived lysophospholipid, soybean-derived hydrogenated lysophospholipid, egg yolk-derived lysophospholipid, egg yolk-derived hydrogenated lysophospholipid, and the like can be used, and one or more can be used as necessary.

  The content of lysophospholipid in the liquid agent (A) is preferably 0.01 to 5% by mass (hereinafter abbreviated as “%”), more preferably 0.1 to 3%. If it is less than 0.01%, the storage stability of the emulsion after mixing may not be sufficient, and if it exceeds 5%, a sticky feeling may occur.

  In addition, the oil agent contained in the liquid agent (A) is not particularly limited as long as it is used for a skin external preparation such as a normal cosmetic, and it can be used in any form of solid, paste, and liquid. be able to. For example, liquid oils include avocado oil, linseed oil, almond oil, olive oil, kyounin oil, wheat germ oil, sesame oil, rice germ oil, rice bran oil, safflower oil, soybean oil, corn oil, jojoba oil, macadamia nut oil , Mink oil, cottonseed oil, palm oil, liquid lanolin, reduced lanolin, lanolin alcohol, lanolin acetate, lanolin fatty acid isopropyl, squalane, squalene, liquid paraffin, pristane, polyisobutylene, undecylenic acid, oleic acid, linoleic acid, linolenic acid, isostearin Acid, 2-hexyldecyl adipate, N-alkyl glycol monoisostearate, isocetyl isostearate, trimethylolpropane triisostearate, ethylene glycol di-2-ethylhexanoate, 2-ethylhexane Cetyl, tri-2-ethylhexanoate trimethylolpropane, tetra-2-ethylhexanoate pentaerythritol, cetyl octoate, oleyl oleate, octyldodecyl oleate, neopentyl glycol dicaprate, 2-ethylhexyl succinate, stearic acid Isocetyl, butyl stearate, di-2-ethylhexyl sebacate, cetyl lactate, myristyl lactate, diisostearyl malate, glyceride triisostearate, glyceride tri-2-ethylhexanoate, glyceride monostearate, di-2-heptyl Undecanoic acid glyceride, methylpolysiloxane, methylphenylpolysiloxane, ethylpolysiloxane, ethylmethylpolysiloxane, ethylphenylpolysiloxane, octamethylsiloxane Examples of the paste oil include cocoa butter, shea butter, hydrogenated castor oil, hydrogenated coconut oil, lanolin, petrolatum, monostearic acid hydrogenated castor oil, and monohydroxystearin. Acid hardened castor oil, cholesteryl hydroxy stearyl, dipentaerythritol 12-hydroxystearate, dipentaerythritol stearate, dipentaerythritol rosin ester, N-lauroyl-L-glutamic acid-di (cholesteryl behenyl Octyldodecyl), macadam nut oil fatty acid phytosteryl, etc., for example, solid oils include carnauba wax, candelilla wax, whale wax, beeswax, ceresin, paraffin, paraffin wax, micro Crystalline wax, stearic acid, behenic acid, 12-hydroxystearic acid, cetyl palmitate, polyethylene glycol distearate, glyceryl tribehenate, stearyl-modified polysiloxane, etc. are included, and these oil agents are used alone or in combination of two or more. Can be used. Among these, since the feeling of use and the storage stability of the emulsion are improved, jojoba oil, squalane, cetyl 2-ethylhexanoate, cetyl octoate, oleyl oleate, neopentyl glycol dicaprate, methylpolysiloxane, methylphenyl Polysiloxane or the like is preferably used.

  Although the compounding quantity of the oil agent in a liquid agent (A) is not specifically limited, 0.1 to 50% is preferable. If it is this range, a favorable usability | use_condition can be obtained and the storage stability of an emulsion will also become favorable.

  Furthermore, as water contained in a liquid agent (A), if it is used for the normal skin external preparation, it can be used without being specifically limited. The blending amount in the liquid agent (A) is not particularly limited, but it is preferably in the range of 20 to 95% because it is not sticky and a fresh feeling is obtained.

  In addition to the above essential components, the solution (A) used in the present invention preferably further contains a salt having a pH buffering ability. By adding such a salt, the pH of the solution (A) is adjusted to 8. The pH after mixing with the solid agent (B) is maintained at 3 to 6 and the storage stability of each emulsion can be ensured. Examples of salts having pH buffering ability include sodium or potassium salts of organic acids such as citric acid, malic acid, tartaric acid, lactic acid, fumaric acid, succinic acid, maleic acid and acetic acid; sodium carbonate, sodium hydrogen carbonate, phosphoric acid Examples thereof include inorganic acid salts such as monosodium, disodium phosphate, sodium hydrogen phosphate, dipotassium phosphate, and potassium dihydrogen phosphate. Of these, sodium citrate, sodium malate, sodium succinate and the like can be preferably used.

  In the liquid agent (A), the blending amount when the salt having the pH buffering ability is blended is preferably 0.1 to 3%. By setting it as such a range, the storage stability of the emulsion after mixing will become favorable, and the favorable usability without a sticky feeling can be obtained.

  Furthermore, in the liquid agent (A), in addition to the above components, various components that are usually used in cosmetics, quasi drugs, pharmaceuticals, and the like can be appropriately blended as necessary, as long as the effects of the present invention are not impaired. it can. Examples of such optional components include alcohols, humectants, emulsifiers, emulsion stabilizers, thickeners, preservatives, powders, pigments, dyes, ultraviolet absorbers, fragrances, medicinal ingredients, and metal sequestering agents. Can be mentioned.

  The method for producing the liquid agent (A) is not particularly limited, and can be produced by mixing each component according to a conventional method to obtain an oil-in-water emulsion, for example, a homomixer or high-pressure emulsification. It can be manufactured using a machine.

  Moreover, it is preferable that the emulsion particle diameter of a liquid agent (A) is 30-500 nm. Within this range, the feeling in use and the storage stability are further improved. It is preferable to use the homomixer or the high-pressure emulsifier because the particle diameter can be adjusted.

  On the other hand, the solid agent (B) used in the present invention contains ascorbic acid as an essential component. Although content in this solid agent (B) of this ascorbic acid is not specifically limited, 5 to 100% is preferable.

  In the solid agent (B), in addition to the ascorbic acid, an optional solid agent component can be contained as necessary within a range not impairing the effects of the present invention. Examples of such solid agent components include excipients, binders, disintegrants, lubricants, fluidity promoters, medicinal ingredients, and the like.

  Among the above, examples of the excipient include starch, glucose, lactose, sucrose, mannitol, carboxymethylcellulose, corn starch, and maltose.

  Examples of the binder include starch, dextrin, gum arabic powder, gelatin, hydroxypropyl starch, methylcellulose, sodium carboxymethylcellulose, hydroxypropylcellulose, crystalline cellulose, ethylcellulose and the like.

  Furthermore, examples of the disintegrant include starch, hydroxypropyl starch, carboxymethylcellulose sodium, carboxymethylcellulose calcium and the like.

  Furthermore, examples of the lubricant include talc, waxes, hydrogenated vegetable oil, sucrose fatty acid ester, magnesium stearate, calcium stearate, aluminum stearate, and polyethylene glycol.

  Furthermore, examples of the fluidity promoter include light anhydrous silicic acid, magnesium silicate, aluminum magnesium silicate and the like.

  On the other hand, as solid medicinal ingredients, ascorbic acid derivatives such as L-ascorbic acid-2-phosphate sodium, L-ascorbic acid-2-magnesium phosphate, ascorbyl glucoside, arbutin, kojic acid, dipotassium glycyrrhizinate, etc. It can be illustrated.

  The dosage form of the solid agent (B) used in the present invention is not particularly limited and may be any of powder, granule, tablet and the like, but can be rapidly mixed with the liquid (A). Therefore, the powder form is preferable.

  Moreover, the manufacturing method of a solid agent (B) is not specifically limited, According to a conventional method, it can be set as the above dosage forms.

  The two-component mixed skin external preparation of the present invention is obtained by mixing and applying the liquid agent (A) and the solid agent (B) obtained as described above before use.

  The ratio of mixing the liquid agent (A) and the solid agent (B) should be appropriately set according to the form and composition of the cosmetic, but the ascorbic acid concentration after mixing (A) and (B) Is preferably 0.1 to 20%. When the ascorbic acid concentration is lower than 0.1%, a sufficient skin improvement effect may not be obtained. When the ascorbic acid concentration is higher than 20%, a sticky feeling may be produced and a good feeling of use may not be obtained.

  Moreover, it is preferable that the viscosity after mixing of (A) and (B) is 1-1000 mPa * s. If it is this range, it can be set as a feeling of fresh use without stickiness, but if it exceeds 1000 mPa · s, a fresh feeling of use may not be obtained. This viscosity means a viscosity at 25 ° C. measured by a B-type rotational viscometer (manufactured by Shibaura System Co., Ltd.).

  Furthermore, the pH after mixing (A) and (B) is preferably in the range of 3-6. If it is this range, since the stability of ascorbic acid is favorable, skin improvement effects, such as a texture improvement, can be made higher. On the other hand, if the pH is less than 3, there may be skin irritation, and if it exceeds 6, the storage stability of ascorbic acid may not be good.

  The method for mixing (A) and (B) is not particularly limited, and various methods can be used. For example, (A) and (B) are placed in the same container and mixed uniformly by shaking or stirring, or the other preparation is placed in one of the preparation containers and shaken or stirred. A method of uniformly mixing by stirring, a method of taking both on the palm and stirring them can be used.

  In the two-component mixed skin external preparation of the present invention, the emulsion is stable for a period of about 3 weeks after mixing even after mixing (A) and (B) as described above.

  In addition, the two-component mixed skin external preparation of the present invention can be a quasi-drug or a pharmaceutical product in addition to a general skin cosmetic. Also, the form after mixing is not particularly limited, and for example, it may be a milky lotion, a skin lotion, a cosmetic liquid, a sunscreen or the like.

  Since the two-component mixed skin external preparation of the present invention obtained as described above can stably contain ascorbic acid, it has a high skin improvement effect such as texture improvement. In addition, since the emulsion is stably maintained for a long period of time after mixing the liquid agent and the solid agent, it can be used not only for the preparation at the time of use but also for the one once prepared. It is excellent in convenience.

  EXAMPLES Next, although an Example and a comparative example are given and this invention is demonstrated still in detail, this invention is not restrict | limited at all by these.

Example 1
A two-component mixed type skin external preparation comprising a liquid agent and a solid agent having the composition shown in Table 1 below was prepared. About the liquid agent, it manufactured with the following manufacturing method. It mixed so that the ascorbic acid density | concentration after mixing of a liquid agent and a solid agent might become the density | concentration in a table | surface, and the viscosity and pH after mixing were measured with the following measuring method. Further, (1) storage stability, (2) feeling of use (freshness, non-stickiness) and (3) evaluation items for texture improvement effect were evaluated by the following methods. These results are shown together in Table 1.

(Liquid preparation method)
a: 1 to 7 are mixed and dissolved. (70 ° C)
b: Heat 8-12. (70 ° C)
c: b is added to a and emulsified. (70 ° C)
d: c is cooled to 40 ° C.
e: Disperse d with a high-pressure emulsifier.

[Measurement items and measurement method]
The viscosity and pH after mixing the liquid agent and the solid agent were measured. The viscosity was measured at 25 ° C. using a B-type rotational viscometer (manufactured by Shibaura System). Moreover, pH was measured using the glass electrode type hydrogen ion concentration meter (made by Horiba Ltd.).

[Evaluation item (1) and its evaluation method]
(1) Storage stability was evaluated according to the following standard a by visual observation of the appearance when stored at 25 ° C. after mixing the liquid agent and the solid agent.

(Standard a)
Evaluation details
◎; Separation and creaming are not observed in 3 weeks ○; Separation and creaming are observed in 3 weeks △; Separation and creaming are observed in 1 week ×; Separation and creaming are observed in 1 day

[Evaluation items (2) to (3) and their evaluation methods]
20 females with a make-up history of 10 years or more are used as a panel. (2) Ease of use (no wateriness, no stickiness) (3) Each evaluation item of texture improvement effect is evaluated on the basis of the following criteria b, Judged from the average score. (3) Concerning the texture improvement effect, continuous use for 2 weeks (1 ml of sample was applied to the entire face, twice a day in the morning and night), and the improvement effect of the skin condition (texture) before use was visually evaluated. Is.

(Standard b)
Score content 5 points: very good 4 points: good good 3 points: normal 2 points: bad 1 point: very bad (judgment)
Evaluation content ◎: Average score 4.5 points or more ○: Average score 3.5 points to less than 4.5 points △: Average score 2.5 points to less than 3.5 points ×: Average score 2.5 points

  As is apparent from the results in Table 1, the two-component mixed skin external preparations of the present invention products 1 to 8 have good storage stability, a fresh feeling of use and no stickiness, and a high texture improving effect. It was.

  Moreover, when the emulsion particle diameter of the liquid agent of this invention product 4 was measured with the submicron particle analyzer N5 (made by BECKMAN COULTER), it was 30-500 nm.

Example 2
Texture improving lotion Texture improving lotion was prepared by the following composition and production method.
(Composition)
Liquid (component) (%)
(1) Hydrogenated soybean lysophospholipid 0.1
(2) Squalane 0.2
(3) Dipentaerythritol fatty acid ester 0.05
(4) Trimethylolpropane triisostearate 0.05
(5) Dipropylene glycol 2.0
(6) Glycerin 3.0
(7) Purified water 10.0
(8) Sodium citrate 2.0
(9) Sodium hydroxide 0.04
(10) Preservative appropriate amount (11) perfume appropriate amount (12) ethyl alcohol 10.0
(13) Purified water Remaining solid formulation (component) (%)
(1) Ascorbic acid 60.0
(2) Glucose 40.0
Mix liquid and solid in a mass ratio of 29: 1 (ascorbic acid concentration 2%)

(Production method)
Solution a: 1 to 6 are mixed and dissolved. (70 ° C)
b: Heat 7 (70 ° C)
c: b is added to a and emulsified. (70 ° C)
d: c is cooled to 40 ° C.
e: Add 8 to 13 to d.
Mix solids 1-2.

  A two-component mixed cosmetic (pH = 4.2) in which 29 parts of a liquid agent and 1 part of a solid agent were mixed had good storage stability and a feeling of use, and had a high texture improving effect.

Example 3
Whitening Essence Whitening essence was prepared by the following composition and production method.
(Composition)
Liquid (component) (%)
(1) Hydrogenated egg yolk lysophospholipid 0.5
(2) Sodium stearoylmethyl taurine 0.05
(3) Liquid paraffin 5.0
(4) cholesterol hydroxystearate 0.5
(5) Propylene glycol 7.0
(6) Glycerin 3.0
(7) Purified water 20.0
(8) L-serine 1.0
(9) L-arginine 0.5
(10) Preservative appropriate amount (11) perfume appropriate amount (12) ethyl alcohol 5.0
(13) Purified water Remaining solid agent (component) (%)
(1) Ascorbic acid 30.0
(2) L-ascorbic acid-2-sodium phosphate 20.0
(3) Maltose 50.0
Mix liquid and solid at a mass ratio of 9: 1 (ascorbic acid concentration 3%)

(Production method)
Solution a: 1 to 6 are mixed and dissolved. (70 ° C)
b: Heat 7 (70 ° C)
c: b is added to a and emulsified. (70 ° C)
d: c is cooled to 40 ° C.
e: Disperse d with a high-pressure emulsifier.
f: Add 8 to 13 to e.
Mix solids 1-3.

  The two-component mixed cosmetic (pH = 4.0) in which 9 parts of the liquid agent and 1 part of the solid agent were mixed had good storage stability and usability, and had a high whitening effect.

The two-component mixed skin external preparation of the present invention has a fresh feeling of use without stickiness and is excellent in the storage stability of the emulsion. Moreover, since it can contain ascorbic acid stably and has skin improvement effects such as excellent texture improvement effect and whitening effect, it is extremely useful in beauty and medical treatment.

Claims (8)

The following formulations (A) and (B)
(A) Oil-in-water emulsion solution containing lysophospholipid, oil agent and water (B) A solid agent containing ascorbic acid, wherein (A) and (B) are mixed and used Mixed skin topical preparation.   The two-component mixed skin external preparation according to claim 1, wherein the viscosity after mixing of (A) and (B) is 1-1000 mPa · s at 25 ° C.   The two-component mixed skin external preparation according to claim 1 or 2, wherein the emulsion particle size of (A) is 30 to 500 nm.   The two-component mixed skin external preparation according to any one of claims 1 to 3, wherein the concentration of ascorbic acid after mixing (A) and (B) is 0.1 to 20% by mass.   The two-component mixed skin external preparation according to any one of claims 1 to 4, wherein the pH after mixing of (A) and (B) is 3-6.   The two-component mixed skin external preparation according to any one of claims 1 to 5, wherein the oil-in-water emulsion solution (A) further contains 0.1 to 3% by mass of a salt having a pH buffering ability. . The two-component mixed skin external preparation according to any one of claims 1 to 6, which is a cosmetic or quasi- drug.   The two-component mixed skin external preparation according to claim 1, wherein the oil-in-water emulsion liquid (A) does not contain oil droplets having a lamellar liquid crystal film.