JP5222708B2 - Topical skin preparation - Google Patents

Description

  The present invention relates to an aqueous gel-like skin external preparation.

There are various types of external preparations applied to the skin, such as patches, ointments, creams, and lotions. Among these, aqueous gel preparations are pharmaceutical forms that are generally regarded as viscoelastic semisolids containing a relatively large amount of water and lower alcohol, and contain active ingredients such as cosmetics, hairdressing agents, and antipruritics. It is used for cleaning materials such as cleansing. As a base for aqueous gel preparations, water-soluble vinyl polymers are frequently used. For example, Patent Document 1 contains an alkyl-modified carboxyvinyl polymer, an oil component and glycyrrhizinate, and is substantially surface active. A preparation having good emulsification stability and containing no agent is disclosed.
JP-A-8-217625

  However, in such an aqueous gel preparation, when applied on the skin, the oil-soluble component does not spread, and the water-soluble active ingredient such as an anti-inflammatory agent does not necessarily reach the inflamed part such as a pore. There was a problem of not working. An object of the present invention is to solve these problems.

  By using a specific volatile silicone and a specific nonionic surfactant in combination, the present inventors can increase the amount of the water-soluble anti-inflammatory agent supplied to the pores and skin crevice, and are not sticky. It has been found that a smooth and smooth preparation can be obtained.

The present invention provides an aqueous gel-like skin external preparation containing the following components (A) to (E).
(A) 2-20% by mass of volatile silicone selected from tris (trimethylsiloxy) methylsilane, tetrakis (trimethylsiloxy) silane, and linear dimethylpolysiloxane having a viscosity at 25 ° C. of 1 to 3 mm ² / s,
(B) nonionic surfactant 0.1-10 mass% of HLB1-7,
(C) 0.01-5% by mass of an acrylic acid polymer selected from polyacrylic acid, cross-linked polyacrylic acid, acrylic acid / alkyl methacrylate copolymer and alkyl methacrylate ether copolymer,
(D) 0.03 to 5% by mass of a water-soluble anti-inflammatory agent,
(E) Water.

  The aqueous gel-like skin external preparation of the present invention can increase the amount of water-soluble components supplied to pores and skin grooves, exhibits high anti-inflammatory action, is non-sticky, smooth and maintains a smooth feeling. it can.

(A) Volatile silicone:
The volatile silicone of component (A) used in the aqueous gel-like skin external preparation of the present invention is tris (trimethylsiloxy) methylsilane (abbreviated “TM3”), tetrakis (trimethylsiloxy) silane (abbreviated “QM4”) and 25 The viscosity at 1 ° C. is selected from 1 to 3 mm ² / s, and generally the boiling point in terms of normal pressure is in the range of 100 to 300 ° C. Specific examples of such volatile silicones, TM3, QM4, hexamethyldisiloxane, octamethyltrisiloxane, dimethylpolysiloxane having a viscosity of 2 mm ² / s, a straight-chain dimethylpolysiloxane and dimethylpolysiloxane of viscosity 3 mm ² / s Is mentioned.
Among them, 2 mm ² / s linear dimethylpolysiloxane, TM3, and QM4 are preferable in terms of feeling and enhancing the distribution of the water-soluble anti-inflammatory agent to the skin grooves and pores.
The viscosity of silicone is measured using a flow-down viscometer such as Ubbelohde.

  The volatile silicone of the component (A) can be used alone or in combination of two or more, and is 2 to 20% by mass, preferably 3 to 10% by mass, more preferably 4 to 8% by mass in the total composition. Contained. If it is less than 2% by mass, the effect of improving the distribution of the water-soluble anti-inflammatory agent to pores and skin grooves tends to be reduced, and if it exceeds 20% by mass, the feeling of use tends to deteriorate.

(B) Nonionic surfactant:
The nonionic surfactant of component (B) used for the aqueous gel-like skin external preparation of the present invention has an HLB of 1 to 7, preferably an HLB of 2 to 5. Specific examples of such nonionic surfactants include fatty acid (poly) glycerin esters, sorbitan fatty acid ester ethoxylates, sucrose fatty acid esters, polyoxyethylene hydrogenated castor oil, and the like. In addition, HLB of surfactant is calculated | required by multiplying the inorganic / organic ratio value of an organic conceptual diagram method 20 times.

  As the nonionic surfactant of component (B), fatty acid (poly) glycerin ester is preferable. The fatty acid (poly) glycerin ester has a structure in which glycerin (condensate thereof) and fatty acid are bonded by an ester bond, and those represented by the general formula (1) are preferable.

[Wherein, n is an integer of 1 to 20, A is independently a hydrogen atom or a linear or branched acyl group having 12 to 22 carbon atoms, and at least one of A is a hydrogen atom; At least one of them is a linear or branched acyl group having 12 to 22 carbon atoms.
In general formula (1), the degree of condensation of glycerol represented by n + 1 is preferably 2 to 21, more preferably 2 to 10. Among them, a condensation degree of 2 (n = 1), that is, a partial fatty acid ester of diglycerin is preferable. The polyglycerin as a skeleton is generally a mixture having different degrees of condensation, and n is an average value.

  In general formula (1), A represents a hydrogen atom or a long-chain acyl group, and it is necessary to have at least one hydrogen atom and an acyl group. The number of acyl groups and hydroxyl groups in the molecule is not particularly limited, but an HLB in the range of 1 to 7 is preferable because it has an effect of improving distribution to pores and skin grooves.

  The acyl group preferably has 12 to 22 carbon atoms, more preferably 16 to 22 carbon atoms, and particularly preferably 18 carbon atoms. The acyl group may be saturated or unsaturated, and may be linear or branched. However, if the melting point is too high, the preparation may become unstable. Therefore, the acyl group is preferably branched or unsaturated.

  Specific examples of the fatty acid (poly) glycerin ester include diglyceryl diisostearate, diglyceryl triisostearate, and diglyceryl monooleate.

  The nonionic surfactant of a component (B) can use 1 type (s) or 2 or more types, and is 0.1-10 mass% in the whole composition, Preferably it contains 0.2-5 mass%. If the amount is less than 0.1% by mass, the effect of improving the distribution of the anti-inflammatory agent to pores and skin grooves tends to decrease. If the amount exceeds 10% by mass, the formulation tends to be inferior in use feeling, for example, the stickiness is deteriorated.

(C) Acrylic acid polymer:
The acrylic polymer of component (C) used in the aqueous gel-like skin external preparation of the present invention is selected from polyacrylic acid, crosslinked polyacrylic acid, acrylic acid / alkyl methacrylate copolymer, and alkyl methacrylate ether copolymer. It is what Specific examples of such an acrylic acid polymer include Carbopol 980, Carbopol 981, Carbopol ETD2020 (manufactured by Lubrizol Advanced Materials); Pemulen TR-1, Pemulen TR-2 (manufactured by Lubrizol Advanced Materials); Examples include Aculin 88 (Rohm & Haas).

  As the component (C), one or more acrylic acid-based polymers can be used, and the total composition is 0.01 to 5% by mass, preferably 0.05 to 2% by mass, more preferably 0.1 to 0%. 0.5% by mass is contained. If it is less than 0.01% by mass, the stability of the preparation cannot be obtained.

(D) Water-soluble anti-inflammatory agent:
The anti-inflammatory agent of component (D) used in the aqueous gel-like skin external preparation of the present invention is water-soluble, such as glycyrrhizic acid and its salt, glycyrrhetinic acid and its salt, bufexamac, ε-aminocaproic acid, yeast extract , Lactoferrin, lactoferricin, azulene derivatives and plant extracts. A preferred water-soluble anti-inflammatory agent is glycyrrhizic acid and its salts.

  One or more water-soluble anti-inflammatory agents of component (D) can be used, and the total composition is 0.03 to 5% by mass, preferably 0.05 to 2% by mass, more preferably 0.07 to 1%. It is contained by mass. If it is less than 0.05% by mass, the anti-inflammatory effect tends to be reduced, and if it exceeds 10% by mass, the preparation tends to be inferior in stability.

(E) Water:
The aqueous gel-like skin external preparation of the present invention contains water. Ordinary clean water such as ion-exchanged water or distilled water is used. Natural water, deep ocean water, or the like may be used.
Water is preferably contained in the total composition in an amount of 60 to 97 mass%, particularly 65 to 95 mass%.

The aqueous gel-like skin external preparation of the present invention can further contain (F) silicone having a viscosity at 25 ° C. of 6 to 100 mm ² / s. In addition to component (A), component (F) exhibits the effect of distributing (D) a water-soluble anti-inflammatory agent in the skin groove and pores, and also remains on the skin after component (A) has volatilized. Thus, it is possible to continuously improve the touch. The preferred viscosity is 6 to 50 mm ² / s, more preferably 6 to 30 mm ² / s. When the viscosity exceeds 100 mm ² / s, the water-soluble anti-inflammatory agent is poorly distributed in the skin grooves and pores.

  Specific examples of such silicone include linear dimethylpolysiloxane, polydimethylsiloxane in which a part of the methyl group is substituted with a hydrogen atom, an alkyl group, a phenyl group, a cyanoethyl group, a perfluoroalkyl group, or the like.

  As the component (F) silicone oil, one or more kinds can be used, and it is preferable to contain 0.5 to 10% by mass, particularly 1 to 8% by mass in the total composition.

Moreover, the mixing ratio of component (A) and component (F) is not particularly limited, but it is preferable that the viscosity of the oil phase formed from these components is low. A preferable viscosity of the oil phase is 0.5 to 50 mm ² / s, more preferably 0.5 to 30 mm ² / s at 25 ° C.

The aqueous gel-form skin external preparation of this invention can contain the various components normally used for cosmetics, a quasi-drug, and a pharmaceutical other than the said component. Specific examples of such components include humectants, ultraviolet absorbers, whitening agents, antiperspirants, bactericides, pigments, spherical powders, plate powders, stabilizers, and fragrances.
In addition, branched dimethylpolysiloxane, polymethylsilsesquioxane, trimethylsiloxysilicic acid, cross-linked polydimethylsiloxane elastomer and the like can be contained within a range not impairing the effects of the present invention.

  The aqueous gel-like skin external preparation of the present invention may contain a surfactant, but preferably contains no surfactant other than the component (B), and particularly contains substantially no anionic surfactant. Is preferred. The content of the anionic surfactant is preferably 0.5% by mass or less, particularly preferably 0.1% by mass or less.

  The aqueous gel-like skin external preparation of the present invention may contain salts, but (D) the distribution of the water-soluble anti-inflammatory agent to the pores is enhanced, and the stability of the product and the feeling during use In order to achieve a high degree of compatibility, it is preferable that the content be less. The preferable content of salt other than the neutralized salt of component (D) and component (C) is 5% by mass or less, more preferably 0.02 to 4% by mass.

  The pH of the aqueous gel-like skin external preparation of the present invention is preferably in the range of 5 to 8, and particularly preferably in the range of pH 5.5 to 7, since suitable usability can be obtained.

The aqueous gel-like external skin solvent of the present invention exhibits the appearance of a transparent, translucent to milky white liquid having a feeling of elasticity. A preferred viscosity range is 1,000 to 30,000 mPa · s at 25 ° C. Within this range, the usability is good, which is preferable.
The viscosity is measured at 25 ° C. with a Brookfield viscometer.

  The aqueous gel-form skin external preparation of this invention can be manufactured by a normal method. For example, it can be obtained by preparing an aqueous dispersion of component (C), an aqueous phase component mixture other than component (C), and an oil phase component mixture, mixing them, and then adjusting the pH by adding an alkaline agent. There is no restriction | limiting in the machine used for stirring, A normal propeller type mixer, a disper, a homomixer, an ultrasonic disperser, a high-pressure homogenizer, a vibration mixer, a static mixer etc. can be used.

  The aqueous gel-like skin external preparation of the present invention is an O / W emulsified composition and exhibits an elastic gel-like appearance. Depending on the oil droplet size and content of the oil component mainly composed of silicone, it can be translucent to white cream.

  In the aqueous gel-type skin external preparation of the present invention, the reason why (D) the distribution of the water-soluble anti-inflammatory agent to the skin groove and pores is not clear, but the surface activity of high HLB usually used in O / W preparations is not clear One reason is considered to be the use of a low HLB surfactant instead of the agent.

Example 1 and Comparative Example 1
An aqueous gel-like skin external preparation having the composition shown in Table 1 was produced by the following production method. Here, acridine orange is a water-soluble fluorescent agent. The obtained external preparation for skin was applied to a pig skin 4 cm × 4 cm, dried 200 μg, and then observed with a fluorescent stereomicroscope. The results are shown in FIG.

(Manufacturing method)
After uniformly mixing the water phase component and the polymer component, the oil phase component was dispersed in the water phase component with a propeller. A mixture of an aqueous phase component and a surfactant was gradually added to this while stirring, and further emulsified with a homomixer and then defoamed to obtain the desired aqueous gel-like skin external preparation.

  From the result of FIG. 1, it was confirmed that the water-based gel external preparation of the present invention spreads to every corner of pores and shallow skin grooves.

Example 2 and Comparative Example 2
The aqueous gel external preparation for skin shown in Table 2 was produced in the same manner as in Example 1. The obtained external preparation for skin was applied to the shin part immediately after hair removal, and the appearance immediately after and after 18 hours was observed. The results are shown in FIG.

  From the results of FIG. 2, it was confirmed that redness was clearly reduced when the aqueous gel-like skin external preparation of Example 2 was applied as compared with the application part of Comparative Example 2.

Examples 3-9, Comparative Examples 3-6
The aqueous gel-like skin external preparation shown in Table 3 was produced in the same manner as in Example 1 and evaluated by the following method. The results are also shown in Table 3.

(Evaluation method)
(1) Dispersibility in pores and skin grooves:
A water-soluble fluorescent agent (acridine orange) was added to each aqueous gel-like skin external preparation so as to be 0.001% by mass in the total composition, and this was applied to pig skin so as to be 50 μg / cm ² . The state after 30 minutes was observed with a stereoscopic fluorescence microscope, and the amount transferred to pores and skin grooves was visually confirmed.
A: Water-soluble components are dispersed in the details of pores and skin grooves.
○: Water-soluble components are slightly dispersed in the details of pores and skin grooves.
Δ: Water-soluble components are slightly dispersed in the pores and skin grooves.
X: Water-soluble components are dispersed throughout the skin.

(2) Anti-inflammatory effect:
After removing the shin area (4cm x 4cm) of 10 specialist panels, apply 200µg of each aqueous gel-like skin external preparation, evaluate the next morning's skin condition according to the following criteria, find the average score of the following, It was shown by the standard.
4; inflammation of pores is improved.
3; inflammation of pores is slightly improved.
2; pore inflammation is slightly improved.
1; inflammation of pores is not improved at all.
(Double-circle): Average 3.5-4.0.
A: Average 2.5 to 3.4.
Δ: Average 1.5 to 2.4.
X: Average 1.0-1.4.

(3) No stickiness:
The stickiness of the skin when 1 g of each aqueous gel-like skin external preparation was applied to the upper arm of 10 specialist panels was subjected to a sensory evaluation according to the following criteria, and the average score was obtained and indicated by the following criteria.
4; There is no stickiness.
3; There is not much stickiness.
2; There is a little stickiness.
1; there is stickiness.
(Double-circle): Average 3.5-4.0.
A: Average 2.5 to 3.4.
Δ: Average 1.5 to 2.4.
X: Average 1.0-1.4.

(4) Smoothness of the next morning's skin:
1 g of each aqueous gel-like skin external preparation was applied to the upper arm of 10 specialist panels, and the smoothness of the next morning's skin was subjected to sensory evaluation according to the following criteria, and the average score was obtained and indicated by the following criteria.
4; Smooth.
3; Somewhat smooth.
2; Not very smooth.
1; not smooth.
(Double-circle): Average 3.5-4.0.
A: Average 2.5 to 3.4.
Δ: Average 1.5 to 2.4.
X: Average 1.0-1.4.

Example 10 (Aqueous gel-like external preparation for skin)
An aqueous gel-like skin external preparation having the following composition was produced in the same manner as in Example 1.
(Ingredient) (mass%)
Dimethicone (2mm ² / s) 10.0
Diglyceryl diisostearate (HLB3.0)
(Cosmall 42V (Nisshin Oillio Group) 0.5
Acrylic acid / alkyl methacrylate copolymer (Pemulene TR-1, manufactured by Lubrizol Advanced Materials) 0.3
Dipotassium glycyrrhizinate 0.1
86% glycerin 8.0
Potassium hydroxide solution 0.2
Ethanol 5.0
Perfume
Purified water residue
Total 100

Example 11 (Aqueous gel-like external preparation for skin)
An aqueous gel-like skin external preparation having the following composition was produced in the same manner as in Example 1.
(Ingredient) (mass%)
Dimethicone (1.5mm ² / s) 15.0
POE (5) hydrogenated castor oil (HLB6.0)
(NIKKOL HCO-5, manufactured by Nikko Chemicals) 0.4
Acrylic acid / alkyl methacrylate copolymer (Pemulene TR-1, manufactured by Lubrizol Advanced Materials) 0.2
Cross-linked polyacrylic acid (Carbopol 980, manufactured by Lubrizol Advanced Materials) 0.1
Dipotassium glycyrrhizinate 0.1
Aloe extract 0.1
86% glycerin 5.0
Potassium hydroxide 0.2
Ethanol 3.0
Perfume
Purified water residue
Total 100

Example 12 (Aqueous gel-like external preparation for skin)
An aqueous gel-like skin external preparation having the following composition was produced in the same manner as in Example 1.
(Ingredient) (mass%)
Methyl trimethicone (1.5 mm ² / s) 15.0
Diglyceryl triisostearate (HLB1.3)
(Cosmall 43V, manufactured by Nisshin Oillio Group) 0.3
Acrylic acid / alkyl methacrylate copolymer (Carbopol ETD2020, manufactured by Lubrizol Advanced Materials) 0.3
Asunaro Extract 3.0
Chamomile extract 1.0
86% glycerin 5.0
1,3-butylene glycol 3.0
Potassium hydroxide 0.2
Ethanol 3.0
Perfume
Purified water residue
Total 100

In Example 1 and Comparative Example 1, it is a figure when the aqueous gel-form skin external preparation is apply | coated to a pig skin, and it observes with the fluorescence stereomicroscope. In Example 2 and Comparative Example 2, it is a figure which shows the external appearance immediately after application | coating of a skin external preparation, and 18 hours after.

Claims (6)

Aqueous gel-like external preparation for skin containing the following components (A) to (E) (A) Tris (trimethylsiloxy) methylsilane, tetrakis (trimethylsiloxy) silane, and a straight chain having a viscosity at 25 ° C. of 1 to 3 mm ² / s 2-20% by mass of volatile silicone selected from dimethylpolysiloxane,
(B) nonionic surfactant 0.1-10 mass% of HLB1-7,
(C) 0.01-5% by mass of an acrylic acid polymer selected from polyacrylic acid, cross-linked polyacrylic acid, acrylic acid / alkyl methacrylate copolymer and alkyl methacrylate ether copolymer,
(D) 0.03 to 5% by mass of a water-soluble anti-inflammatory agent,
(E) Water. Furthermore, (F) The aqueous gel-form skin external preparation of Claim 1 containing 0.5-10 mass% of silicone whose viscosity in 25 degreeC is 6-100 mm < ² > / s. The aqueous gel-form skin external preparation according to claim 1 or 2, wherein the nonionic surfactant of component (B) is a fatty acid (poly) glycerin ester represented by the general formula (1).
[Wherein, n is an integer of 1 to 20, A is independently a hydrogen atom or a linear or branched acyl group having 12 to 22 carbon atoms, and at least one of A is a hydrogen atom; At least one of them is a linear or branched acyl group having 12 to 22 carbon atoms.   The aqueous gel-form skin external preparation of Claim 3 whose acyl group shown by A in General formula (1) is a C16-C22 acyl group.   In formula (1), n is 1, The aqueous gel-form skin external preparation of Claim 3 or 4.   The aqueous gel-form skin external preparation according to any one of claims 1 to 5, wherein the water-soluble anti-inflammatory agent of component (D) is glycyrrhizic acid and / or a salt thereof.