JP2023053571A - Skin warming topical agent - Google Patents

Abstract

To provide a skin warming topical agent that provides warmth to the skin which has a warming effect that can be sufficiently maintained by providing not only a short-time warming sensation but also an excellent blood flow promotion effect can improve the symptoms of congestion and pigmentation around the eyes referred to as "bags" under the eyes, and moreover has a comfortable feel and high safety that does not require rinsing after use around the eyes.SOLUTION: A skin warming topical agent comprises a polyhydric alcohol-in-oil emulsified composition containing a heat-of hydration generating component (A) as the dispersion phase which is a blend of 2 water-soluble polyhydric alcohols with different valences and an oil agent (B) as the continuous phase which is an emulsifying composition, for example, the heat-of-hydration generating component (A) is included as a mix of dihydric water-soluble polyhydric alcohol (A1) such as propylene glycol and a trihydric water-soluble polyhydric alcohol (A2) such as glycerin at a ratio (mass ratio) of A1/A2=10/1 to 1/110, and the oil agent (B) and a surfactant (C) are further included as essential components.SELECTED DRAWING: None

Description

Applied for application of Article 30, Paragraph 2 of the Patent Act Date of publication of website: October 21, 2020 Website address: https://www. scconline. org/ifscc2020/

TECHNICAL FIELD The present invention relates to a skin-warming external preparation that is used in warm-feeling massage preparations and the like, and that generates heat of hydration with moisture in the skin to impart warmth to the skin.

In general, preparations for warming massage, which are skin preparations for external use such as cosmetics, are recognized to have effects such as promotion of blood circulation, acceleration of metabolism, relaxation effects, etc. due to their warming action on the skin.

The heat-generating mechanism of preparations for warming massage consists of (1) heat of hydration by the hydroxyl groups of polyols, (2) heat of hydration of anhydrous inorganic substances, and (3) sensory stimulation via activation of TRP channels such as vanillylbutyl and capsaicin. is well known.

Regarding (2) above, the powdery anhydrous inorganic substance may physically damage the skin and mucous membranes, and it is necessary to be careful not to get it in the eyes, especially when massaging the face.
Regarding (3), the temperature of the skin does not actually rise, and if it gets into the eyes, severe sensory irritation may occur, so it cannot be applied to eye preparations even if it is supposed to be washed away. In other words, (3) is not suitable as a heat generation mechanism for eye preparations in terms of functionality, usability, and safety, and cannot be applied to preparations that remain on the skin such as the face after use, that is, "leave-on preparations." .

Regarding (1) above, depending on the type of polyol, the hydrating power may be weak and the warm feeling may not be felt, and if glycerin or the like with strong hydrating power is used, the feeling of application will be poor due to excessive stickiness. In addition, if a thickener is added in consideration of usability, the stringiness becomes stronger and it becomes difficult to spread, resulting in a more sticky feel in use. In addition, if it is stored in a poorly airtight container, it may absorb moisture during storage before use and lose its warming effect.

In order to utilize the exothermic mechanism of (1) in this way, various improvements are required. (Patent Document 1).

Also known is a polyol-in-silicone emulsion in which a hydration heat-generating component composed of a polyol is used as a dispersed phase (internal phase) and emulsified using an alkyldimethicone copolyol, which is a nonionic polysiloxane copolymer (Patent Document 2).

Furthermore, a warming cosmetic containing a powder at a high ratio of 9 to 45% by mass, using a moisturizing agent such as a polyhydric alcohol as an exothermic substance, and using a polyhydric alcohol as an internal phase. Hydric alcohol type warming cosmetics are known (Patent Document 3).

JP-A-2003-261433 Japanese Patent Publication No. 2005-501022 WO2018/159773

However, the skin warming topical composition described in Patent Document 1 described above has a sticky feeling when using glycerin as a polyhydric alcohol with a high heat of hydration that constitutes the continuous phase (external phase). It is easy to absorb moisture during storage, and it is difficult to ensure quality stability of external preparations.

The polyol-in-silicone emulsion described in Patent Document 2 has the effect of imparting moisture to cosmetics such as foundation and lipstick, and has the effect of imparting physical stability and color stability to solid formulations. A solid preparation does not require a warm sensation due to the heat of hydration, and does not require continuous control of the heat of hydration.

In addition, the warming cosmetic disclosed in Patent Document 3 contains a high proportion of powder as an essential ingredient, and contains one or more polyhydric alcohols such as glycerin, dipropylene glycol, and polyethylene glycol as moisturizing agents. The problem of improving the promoting effect and the means therefor are not indicated.

Since such warming cosmetics contain a large amount of powder blended for the purpose of make-up like foundation, it is a leave-on product for warming massage that is used for safe and sufficient massage, including around the eyes. Use as a formulation is difficult.

By the way, congestion and pigmentation around the eyes, called "dark circles", are symptoms caused by fatigue, irregular lifestyle, overwork, lack of sleep, etc., and give the impression of being older than the actual age. There is a demand for the development of warming cosmetics that can be improved.

Accordingly, an object of the present invention is to solve the above-described problems and to provide a skin-warming external preparation that provides not only a short-term warming sensation but also a sufficiently long-lasting warming effect and excellent blood flow. It has a stimulating effect, which can improve the symptoms of congestion and pigmentation around the eyes, which are called "dark circles". It is intended to be a skin temperature-sensitive external preparation with a feeling of use.

In order to solve the above problems, a heat-of-hydration-generating component (A) composed of two or more polyhydric alcohols with different valences, an oil agent (B), and a surfactant (C) are essential components, A skin-warming external preparation comprising a polyhydric alcohol-in-oil emulsified composition having the hydration heat-generating component (A) as a dispersed phase and an oil agent (B) as a continuous phase.

The skin warmth-sensitive topical preparation of the present invention configured as described above comprises a heat-of-hydration-generating component (A) comprising two or more polyhydric alcohols having different valences, and a polyhydric alcohol-in-oil emulsion as a dispersed phase. Since it is dispersed in the composition, the polyhydric alcohol of the heat-of-hydration-generating component (A) that is in frictional contact with the skin hydrates with moisture contained in the skin to generate heat.

At that time, two or more polyhydric alcohols with different valences undergo hydration reactions with different exothermic speeds and calorific values. Heat is generated, and as a result, an excellent effect of promoting blood flow with a sufficiently long-lasting warming effect can be obtained.

In particular, two or more water-soluble polyhydric alcohols with different valences of the heat-of-hydration-generating component (A) are combined with one or more water-soluble polyhydric alcohols (A1) of dihydric or tetravalent or higher and trihydric When the hydration heat-generating component (A) is contained in a ratio (mass ratio) of A1/A2 = 10/1 to 1/110 in combination with the water-soluble polyhydric alcohol (A2), the above excellent blood flow It is easy to obtain effects such as a promotion effect.

In addition, since the skin-warming external preparation of the present invention comprises an emulsified composition in which the predetermined hydration heat-generating component (A) is the dispersed phase and the oil agent (B) is the continuous phase, it does not have the stickiness peculiar to polyols. , the deactivation due to moisture absorption from the outside over time is small, and there is no need to include anhydrous inorganic powder that damages the skin. Therefore, it has low skin irritation, is comfortable to apply, does not require washing after massage, and is highly safe even when used as a leave-on product around the eyes.

In order to obtain a skin temperature-sensitive external preparation that can stably exhibit such properties, the dihydric water-soluble polyhydric alcohol (A1) is propylene glycol, and the trihydric water-soluble polyhydric alcohol ( Preferably A2) is glycerin.

The skin heat-sensitive topical preparation of the present invention preferably contains a polyether-modified silicone as an emulsion stabilizer so that the emulsified particles do not separate even at slightly higher temperatures than room temperature.

The above-mentioned skin-warming topical preparation generates hydration heat even without containing powdery anhydrous inorganic substances, so that it does not damage the skin, is comfortable to apply, and does not need to be washed away from the skin after use. It is a skin warming external preparation that can be safely used for warming massage around the eyes.

In addition, the skin warming external preparation of the present invention contains a physiologically active ingredient in addition to the above-mentioned essential ingredients, thereby allowing the physiologically active ingredient to act on the skin in a state where blood flow is promoted, thereby efficiently exhibiting a physiologically active effect. can be enhanced.

Such a skin-warming topical preparation can efficiently generate heat of hydration from moisture contained on the surface and inside of the skin when well massaged on the skin, so that it can be used for eye massage with a blood flow-promoting effect. It can be used as a skin warm-sensitive external preparation such as a cream.

The present invention provides an emulsified composition having a disperse phase of hydration heat-generating components in which two or more kinds of water-soluble polyhydric alcohols having different valences are blended, and an oil agent as a continuous phase. Since it is an external preparation, it does not absorb moisture during storage before use and does not lose its warming effect. It has the advantage of being able to sufficiently sustain the generation of heat by Japanese heat and being applicable as an eye massage cream.

Chart showing the relationship between the number of reciprocations and the coefficient of dynamic friction of jigs coated with Example 1 and Comparative Example 1 in a friction measuring machine A chart showing the results of sensory evaluation of Example 1 and Comparative Example 1 in five items (warm feeling, pleasant warm feeling, ease of spreading, stickiness, and massaging property). Chart showing the relationship between the elapsed time after application and massage to the face and blood flow in Comparative Examples 1 and 2 Chart showing the relationship between the elapsed time after application and massage to the face and blood flow in Example 1 and Comparative Example 2

A skin-warming external preparation that is an embodiment of the present invention comprises a heat-of-hydration-generating component (A) containing two or more water-soluble polyhydric alcohols with different valences, an oil (B), and a surfactant. (C) as an essential component, the hydration heat-generating component (A) as a dispersed phase, and the oil (B) as a continuous phase.

The two or more water-soluble polyhydric alcohols having different valences may be divalent or higher polyhydric alcohols capable of generating heat of hydration. polyhydric alcohols can be employed.

Two or more types of water-soluble polyhydric alcohols with different valences are blended in order to efficiently utilize the heat of hydration of the water-soluble polyhydric alcohols for promoting blood flow. In addition, in order to maintain the calorific value as long as possible, it is preferable to employ a hydration heat-generating component (A) containing a larger amount of polyhydric alcohol with a lower valence than a polyhydric alcohol with a higher valence.

For example, a dihydric or tetrahydric or higher water-soluble polyhydric alcohol (A1) and a trihydric water-soluble polyhydric alcohol (A2) are mixed at a ratio (mass ratio) of A1/A2 = 10/1 to 1/110. A hydration heat-generating component (A) can be used.

The dihydric water-soluble polyhydric alcohol (A1) is a water-soluble polyhydric alcohol used as a moisturizing agent in cosmetics, and is a chain aliphatic hydrocarbon or a cyclic aliphatic hydrocarbon. A so-called diol compound having a structure in which two carbon atoms are substituted with one hydroxy group, and a lower polyhydric alcohol having 5 or less carbon atoms are preferred for the required water solubility.

Specific examples of the dihydric water-soluble polyhydric alcohol (A1) used in the present invention include ethylene glycol, diethylene glycol, propylene glycol, propanediol, dipropylene glycol, 1,3-butylene glycol and hexylene glycol. , and one or more of these can be used in combination.

The trihydric water-soluble polyhydric alcohol (A2) is a water-soluble polyhydric alcohol used as a moisturizing agent in cosmetics, and is a lower polyhydric alcohol having 5 or less carbon atoms. Preferred for the required water solubility, representative examples include glycerin, 1,2,4-butanetriol, and the like.

Water-soluble polyhydric alcohols having a valence of 4 or more include sugar alcohols such as tetravalent erythritol, pentavalent xylitol, hexavalent sorbitol, and inositol.
Polyhydric alcohols, which are well-known water-soluble polymer compounds such as polyethylene glycol, can also be used. For example, polyethylene glycol having a number average molecular weight of about 200 to about 20,000 is commercially available for use in pharmaceuticals and the like.

Regarding the blending ratio (mass ratio) of the above-mentioned dihydric, tetrahydric or higher water-soluble polyhydric alcohol (A1) and the trihydric water-soluble polyhydric alcohol (A2), A1/A2 = 10/1 A ratio of ~1/110 is preferable in order to efficiently and sustainably generate heat of hydration when in contact with moisture, and considering the calorific value and its persistence, A1/A2 = 10/2 is more preferable. to 1/100, more preferably A1/A2=10/3 to 1/80.

In addition, the oil agent (B) used in the present invention is not particularly limited as long as it is a cosmetic oil capable of suppressing evaporation of water from the skin to keep the skin moist and flexible. For example, hydrocarbon oils such as α-olefin oligomers, silicone oils such as squalane and dimethylpolysiloxane, and other well-known emollient oils, solid oils, and silicone elastomers that can be used as substitutes for sebum. You can also

The surfactant (C) blended in the present invention is also called an emulsifier blended for the purpose of obtaining an emulsion, and nonionic surfactants, anionic surfactants, etc. can be used. .
As nonionic surfactants, those widely used as emulsifiers, solubilizers, and thickeners in creams, milky lotions, emulsified foundations, lotions, etc. can be used. Examples include glycerin fatty acid esters, sorbitan fatty acid esters, polyoxyethylene alkyl ethers, ethylene oxide-propylene oxide block copolymers, and the like.

As the anionic surfactant, well-known anionic surfactants for cosmetic applications can be employed. Amino acid salts are included.

The physiologically active ingredient used in the present invention is a component that can be added to the dispersed phase or the continuous phase, and by adding the physiologically active ingredient to the skin in which blood flow is promoted, the physiologically active effect can be efficiently achieved. can be enhanced.

Such physiologically active ingredients include, for example, anti-roughness agents, whitening agents, anti-aging agents, antioxidants, anti-inflammatory agents, various vitamins and their derivatives, hair restorers, and various plant or animal extracts.

In order to correspond to the lipophilicity or hydrophilicity of the physiologically active ingredient, the hydration heat-generating component (A) of the dispersed phase is a water-soluble lower polyhydric alcohol, so the hydrophilic physiologically active ingredient is added to the dispersed phase. Alternatively, a lipophilic bioactive ingredient may be added to the continuous phase containing the oil.

Specific examples of lipophilic physiologically active ingredients include ceramide, glycyrrhizic acid, glycyrrhetinic acid, amino acids, sugars, mucopolysaccharides, hydrolyzed proteins, sphingolipids, phospholipids, ascorbyl palmitate, ascorbyl stearate, and tetraisopalmitic acid. Ascorbyl, 3-O-cetylascorbic acid, rucinol, retinol, vitamin A acid, alkylglyceryl ethers, ε-aminocaproic acid derivatives and the like.

Hydrophilic bioactive ingredients include ascorbic acid and its derivatives, water-soluble salts thereof, other water-soluble vitamins, whitening agents such as arbutin, ellagic acid, and tranexamic acid, and natural moisturizing factors such as amino acids. (NMF), salts of glycyrrhizic acid, water-soluble collagen, elastin, zinc glycine complex, nicotinamide, anti-aging agents and anti-inflammatory agents such as ε-aminocaproic acid, various vitamins and their derivatives, water-soluble substances such as various plant extracts sexual component.

[Example 1, Comparative Examples 1 and 2]
The skin temperature-sensitive external preparations composed of the polyol-in-oil emulsion compositions of Example 1 and Comparative Examples 1 and 2 consisted of the essential components listed below as raw materials, including a dihydric water-soluble polyhydric alcohol (A1), a trihydric A water-soluble polyhydric alcohol (A2), an oil agent (B), and a nonionic surfactant (C) are blended so as to have the composition shown in Table 1, and mixed and emulsified by a conventional method for cosmetic massage creams. Then, it was prepared into a soft cream. A1/A2 (mass ratio) of Example 1 was A1/A2=9.8/1.

(A1): propylene glycol (A2): glycerin (B): dimethylpolysiloxane (dimethicone), decamethylcyclopentasiloxane, (diphenyldimethicone/vinyldiphenyldimethicone/silsesquioxane) crosspolymer (C): (dimethicone/ vinyl dimethicone) crosspolymer, polyethylene glycol/polypropylene glycol-19/19 dimethicone

In order to examine the degree of heat generation due to heat of hydration, comfortable feeling of use, warm massage properties, and excellent blood flow promoting effect in the obtained examples and comparative examples, the following friction evaluation tests, sensory tests regarding warmth and usability were conducted. It was evaluated by an evaluation test, a moisture absorption test, and a blood flow measurement test.

<Friction evaluation test>
For the skin temperature-sensitive external preparations of Example 1 and Comparative Example 1, the coefficient of dynamic friction during application massage was measured with a friction measuring machine to examine differences in usability depending on the type of polyol.

The test conditions were as follows: Example 1 or Comparative Example 1 was applied to the load cell of a friction measuring machine (surface property measuring machine) that reciprocated by pressing the load cell against the contact surface, and a load of 50 g and a reciprocating distance of 10 cm were applied at room temperature. The number of times and the dynamic friction coefficient were determined, and the results are shown in FIG.

As is clear from the results shown in FIG. 1, compared to Comparative Example 1, which consists of an emulsion in which the internal phase is the sole component of glycerin (A2), the internal phase contains propylene glycol (A1) and glycerin (A2). The coefficient of dynamic friction of Example 1, which was used as a mixed component in the ratio, was stably low after the number of reciprocating frictions was 5 times, and it was found that a smooth and light feeling was obtained during massage.

<Sensory evaluation test on warmth and usability>
Regarding Example 1 and Comparative Example 1, 9 people were asked for each item of (1) warmth, (2) comfortable and lasting warmth, (3) ease of spreading, (4) stickiness, and (5) massaging properties. A sensory test was conducted by expert panelists, and the results are shown in FIG.

All items were evaluated on a 5-point scale of poor (-2 points), somewhat poor (-1 point), normal (0 points), somewhat good (+1 point), and good (+2 points). is shown in the figure.

As is clear from the results shown in FIG. 2, in terms of (1) warm feeling and (2) comfortable and lasting warm feeling, Example 1 has a stronger temporary warming effect than Comparative Example 1. Although felt, Example 1 was better in terms of a pleasant and lasting warming effect. From this, it can be seen that the generation of hyperthermia due to the heat of hydration of the emulsion whose internal phase is composed of a water-soluble polyhydric alcohol containing propylene glycol (A1) and glycerin (A2) is sufficiently sustained.

Similarly, in terms of (3) spreadability, (4) stickiness, and (5) massaging properties, Example 1 was superior to Comparative Example 1 by about 1.8 to 2 points or more.

Regarding the stickiness, a comparison was made between a single component of glycerin as a reference example and Comparative Example 1, and the tackiness (stickness: gf) was examined at the number of times of spreading from 0 to 60 times using the friction measuring machine. The results are shown in Table 2.

As is clear from the results shown in Table 2, the tackiness of Comparative Example 1 comprising the polyol-in-oil emulsified composition was 10.0% even after spreading up to the expected usual number of times of spreading (30 times). There was no significant change between 33 gf and 17.78 gf, confirming less stickiness than glycerin between 18.40 gf and 37.86 gf.

<Moisture absorption test>
As a reference test, the hygroscopicity of glycerin alone and each sample of Comparative Example 1 was examined. That is, 50 g of each sample was placed in a 140 ml glass bottle and left uncovered in a room at 25° C. for one week. After one week, the water content of each sample was measured by the Karl Fischer method.

As a result, the moisture content of Comparative Example 1 was 0.16% at the beginning of the test and 2.25% after the test, but the moisture content of the glycerin sample was 0.22% at the beginning of the test and 6.43% after the test. had increased to Similar results were also obtained for Example 1, indicating that the hygroscopicity of the skin temperature-sensitive external preparation of the present invention is lower than that of glycerin alone.
With such low hygroscopicity, it can be seen that the quality of products such as cosmetics can be maintained for a long period of time from storage and distribution to the time of use by consumers.

<Blood flow measurement test>
(Test 1) Comparative Example 1 (left side) and Comparative Example 2 (right side) were applied to the left and right cheeks of the subject's face, respectively, left for 1 minute, massaged for 1 minute, and then left for 6 minutes. Blood flow values were measured by laser speckle imaging blood flow meter at . This test was conducted in a room at 24±1° C. and 50±5% humidity during the daytime from 1:00 pm to 4:00 pm. The results are shown in FIG.
(Test 2) The blood flow value was measured in the same manner as above, except that Example 1 (left side) and Comparative Example 2 (right side) were applied to the left and right cheeks of the subject's face, respectively. 4.

As is clear from the results shown in FIG. 3, Comparative Example 1 showed a higher blood flow value than Comparative Example 2 (placebo with water as the internal phase), but left for 6 minutes after massage. There was no particularly conspicuous peak within the time, and no increase in blood flow was observed.

Moreover, as is clear from the results of FIG. 4, within the 6-minute standing time after the massage, in Example 1, an increase in the blood flow value was observed after 240 seconds and 360 seconds, and after 460 seconds, the blood flow value increased. Returned to state blood flow values. In Comparative Example 2, which was applied and massaged on the right cheek, the blood flow was increased to some extent, presumably induced by the effect of increased blood flow on the left cheek.

Comprehensive examination of these results reveals that Comparative Example 1, which consists of an emulsion containing glycerin (A2) as the sole component of the internal phase, imparts a temporary or instantaneous warming effect to the skin during massage, but lasts longer. Since there is no warming effect, blood flow does not increase.

On the other hand, Example 1, which consists of an emulsion in which the internal phase is a mixed component of propylene glycol (A1) and glycerin (A2) at a predetermined ratio, gives a continuous feeling of warmth after massage and promotes blood flow. It was a skin heat-sensitive topical preparation with a sufficiently long-lasting warming effect so that not only a short-time warming sensation but also an excellent effect of promoting blood flow could be obtained.

Propylene glycol does not have an instantaneous warming effect, but by mixing propylene glycol and glycerin in a predetermined ratio and controlling the hydration speed relatively slowly and continuously, it gives a lasting warming effect. , was considered to have a positive effect on the promotion of blood flow in the skin.

[Prescription example]
Table 3 below summarizes formulation examples of massage creams other than those of the above-described examples, which are skin-warming agents for external use and are also suitable for use on the main parts of the body and around the eyes. In all cases, similar to the examples, a comfortable feeling of use, a warm massage property, and an excellent effect of promoting blood flow were observed.

Claims (7)

A hydration heat generating component (A) containing two or more water-soluble polyhydric alcohols with different valences, an oil agent (B), and a surfactant (C) as essential components, A skin-warming external preparation comprising a polyhydric alcohol-in-oil emulsified composition comprising component (A) as a dispersed phase and oil agent (B) as a continuous phase. The heat-of-hydration-generating component (A) is a mixture of one or more water-soluble polyhydric alcohols (A1) having a valence of 2 or 4 or more and a water-soluble trihydric alcohol (A2) to generate heat of hydration. The skin temperature-sensitive external preparation according to claim 1, which is component (A). The hydration heat-generating component (A) is composed of one or more water-soluble polyhydric alcohols (A1) having a valence of 2 or 4 or more and a water-soluble polyhydric alcohol (A2) having a valence of 3 or more, and A1/A2=10/ 2. The skin temperature-sensitive external preparation according to claim 1, wherein the hydration heat-generating component (A) is blended at a ratio (mass ratio) of 1 to 1/110. 4. The skin temperature sensitivity according to claim 2 or 3, wherein the dihydric, tetrahydric or higher water-soluble polyhydric alcohol (A1) is propylene glycol, and the trihydric water-soluble polyhydric alcohol (A2) is glycerin. External agents. The skin temperature-sensitive external preparation according to any one of claims 1 to 4, wherein the surfactant (C) is a polyether-modified silicone. The skin temperature-sensitive external preparation according to any one of claims 1 to 5, which contains a physiologically active ingredient in addition to the essential ingredients. The skin temperature-sensitive topical preparation according to any one of claims 1 to 6, wherein the skin temperature-sensitive topical preparation is an eye massage cream.

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