JP2003113039A - Exothermic composition and skin care preparation composition - Google Patents

Abstract

(57) Abstract: The present invention provides a heat-generating composition that maintains a warm sensation and is safe for the human body without skin irritation. The exothermic composition is characterized by containing polyethylene glycol having an average molecular weight of less than 350, polyethylene glycol having an average molecular weight of 350 or more, and a heating agent.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition which produces heat when contacted with moisture present in the air or on the skin, and more particularly to a composition for external preparation for skin.

[0002]

2. Description of the Related Art An external preparation for skin having heat generation has effects such as recovery of fatigue by accelerating blood circulation and activation of skin, and when it contains a medicinal component, it promotes transdermal absorption of the drug. You can expect an effect. As means for imparting exothermicity to a preparation, means applying a chemical reaction such as a redox reaction or a hydration reaction has been conventionally studied. Of these,
The hydration reaction is highly safe and has been applied to the field of external skin preparations.

As a composition which gives exothermicity by a hydration reaction, a composition containing a polyhydric alcohol such as polyethylene glycol, 1,3-butylene glycol or glycerin is known. However, the calorific value is not sufficient to feel warmth, and in particular, when the air is dry or when it is difficult to sweat, the warmth can hardly be felt. Further, as a cosmetic composition utilizing heat of hydration of anhydrous inorganic powder, for example, US Pat. No. 32550.
No. 680 and JP-A No. 2000-38333, compositions containing activated zeolite are disclosed in JP-A-6-3364.
A pack containing a phosphate or the like is known in Japanese Patent No. 13 publication. However, these compositions have a fever duration of about 1 to 2 minutes, and compositions containing an increased amount of the above-mentioned exothermic agent in order to maintain the thermal sensation of the preparation are temporarily hydrated. It becomes very hot and causes burns.
There was a safety issue.

[0004]

DISCLOSURE OF THE INVENTION The present invention provides a heat-generating composition which maintains a warm sensation and is free of skin irritation and safe for the human body.

[0005]

Means for Solving the Problems As a result of diligent studies on a heat-generating composition capable of increasing skin temperature during use, the present inventors have found that by combining a polyethylene glycol having a specific molecular weight with a heat-generating agent, contact with water can be achieved. It has been found that a suitable exothermic composition is obtained in which a moderate exotherm persists.

That is, the present invention has an average molecular weight of 350.
The present invention provides an exothermic composition characterized by containing less than polyethylene glycol, polyethylene glycol having an average molecular weight of 350 or more, and an exothermic agent. Hereinafter, the present invention will be described in detail.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION The exothermic composition of the present invention essentially comprises a low molecular weight polyethylene glycol having a weight average molecular weight of less than 350 and a high molecular weight polyethylene glycol having a weight average molecular weight of 350 or more. The low molecular weight polyethylene glycol is preferably a polyethylene glycol having an average molecular weight of 100 or more and less than 350, more preferably 200 or more and less than 350. The high molecular weight polyethylene glycol is preferably 350 or more and 100,000 or less, more preferably 350 or more and 6000 or less. The total content of polyethylene glycol (low molecular weight + high molecular weight) is 20 to 99% by mass, and more preferably 30 to 95% by mass of the total composition. In case of 20 mass% or less,
When the composition is applied to the skin, there may be problems in usability such as difficulty in spreading on the skin, and when it exceeds 99% by mass, the composition may be dripped from the skin when applied to the skin. The content ratio of the low molecular weight polyethylene glycol to the high molecular weight polyethylene glycol is 1:10 to 100: 1, more preferably 1: 5 to 5
It is 0: 1. Within this range, the composition is particularly well-suited to and spread on the skin, and a good composition free of skin irritation can be obtained.

As the exothermic agent used in the present invention, 25
Enthalpy of dissolution in water at ℃ (unit: kJmol
It is preferably an organic compound or an inorganic compound in which ^-1 ) is negative. A compound having an enthalpy of dissolution in water of −10 kJmol ⁻¹ or less is preferable. Preferred specific exothermic agents include sodium hydrogen phosphate (-24.0 kJmol ^-1 ) and magnesium sulfate (-
91.2 kJ mol ⁻¹ ), zinc sulfate (−80.3 kJ)
mol ⁻¹ ), calcium chloride (-81.3 kJmol
^-1 ), magnesium chloride (-159.8 kJmol)
^-1 ), sodium carbonate (-26.7 kJmol ^-1 )
Etc. When these exothermic agents are powders, the particle size is 0.1 to 4 from the viewpoint of hydration rate, feeling of use, manufacturability, and the like.
It is preferably 00 μm. The content of the exothermic agent in the composition is preferably 0.1 to 60% by mass, more preferably 1 to 40% by mass. If it is less than 0.1% by mass, sufficient exothermic properties may not be obtained, and 60% by mass
In that case, skin irritation may occur when the composition is applied to the skin.

Since the exothermic composition of the present invention is a composition which produces heat when contacted with moisture, the composition is preferably a non-aqueous composition containing substantially no water. However, a trace amount of water contained in the raw material of the composition may be mixed in a range that does not impair the effects of the present invention.

The heat-generating composition according to the present invention can be used as a coating agent for solutions, gels, ointments, etc.
It is preferable to use a patch in which the composition and the support are combined, because the warm feeling lasts well. Examples of the form of the patch include a form in which the composition is filled in a porous support, a form in which the composition is impregnated into a nonwoven fabric, a knit, or a sponge-like support, and a composition in which a nonwoven fabric, a knit, or a resin film is supported. Examples include a form applied to the body. Among the above, particularly preferred is a patch having a laminated structure in which a gel or an ointment is applied to a support. The gel or ointment can be obtained by thickening and gelating polyethylene glycol with a polymer compound or the like.

The polymer compound for gelling polyethylene glycol is one which dissolves in polyethylene glycol and exhibits a thickening effect. Specifically, for example, cellulose derivatives such as hydroxypropyl cellulose and hydroxymethylpropyl cellulose, (meth) acrylic acid (co) polymers such as polyacrylic acid, acrylic acid / acrylamide / ethyl acrylate copolymers, ,
The following formula

[0012]

[Chemical 1]

(In the formula, R1 represents a hydrogen atom or a methyl group, R2 represents an alkyl group having 10 to 30 carbon atoms, and a polymerization degree of 5
200 ethyleneoxy groups, sugar (chain) or sugar alcohol residues, or a mixture thereof, x and y each represent mol% of each unit in the copolymer, and x represents 50 to 99.9 mol%, y is 0.1 to 50 mol%), and synthetic polymer compounds such as an acrylic acid / methacrylic acid ester-based copolymer having a structure of polyvinylpyrrolidone.

These polymer compounds may be used either individually or in combination of two or more, preferably 0.1% in the total composition.
-40 mass%, more preferably 0.5-20 mass%. If the blending amount is too small, it is possible to obtain a gel having an appropriate hardness and having good compatibility with the skin and good adhesiveness when used as a patch.

The support used in the case of the patch is
It is not particularly limited as long as it is used in a patch, but for example, a non-woven fabric or woven fabric or knitted fabric using polyester or polypropylene fibers, or a laminated support obtained by laminating these with a polyethylene or polyurethane film. Can be used.

The exothermic composition of the present invention comprises a medicinal component, a moisturizer, an inorganic powder, a binding / thickening agent, a tackifier, a preservative, a solubilizer, an emulsifier, a stabilizer, and Skin absorption promoters, fragrances, pigments and the like can be added.

Examples of the medicinal component include 1-menthol, indomethacin, glycol salicylate, methyl salicylate, ketoprofen, flurbiprofen, ibuprofen, suprofen, loxoprofen, zaltoprofen, piroxicam, felbinac, salicylic acid, diphenhydramine, dibucaine, procaine, lidocaine. Examples include crude drug extracts such as vitamin E derivatives, glycyrrhetinic acid, ellagic acid, kojic acid, hydroquinone, and capsicum extract, salts thereof, and derivatives thereof. These may be used alone or in combination of two or more. The compounding amount is a medicinal effective amount.

Examples of moisturizing agents include d-sorbitol, ethylene glycol, propylene glycol, polyethylene glycol, polypropylene glycol, 1,
3-propanediol, 1,4-butanediol, maltitol, xylitol, polyethylene oxide, allantoin and the like can be mentioned. These may be used alone or in combination of two or more. The moisturizer is
For example, 0.1 to 70% by mass, preferably 1.0 to 45% by mass, is added to the entire composition.

Examples of the inorganic powder include kaolin, bentonite, montmorillonite, zinc oxide, titanium oxide,
Examples thereof include silicic acid anhydride, synthetic hydrotalcite, zeolite and the like. These may be used alone or in combination of two or more. The inorganic powder is, for example, 0.05 to 30 mass% with respect to the entire composition, and preferably 0.
5 to 15 mass% is added. By adding the inorganic powder, even better shape retention can be obtained.

Examples of the polymer which does not dissolve in polyethylene glycol include sodium polyacrylate, polyvinyl alcohol, polyacrylamide, sodium carboxymethyl cellulose, hydroxyethyl cellulose, methyl cellulose, carboxy vinyl polymer, methyl vinyl ether-maleic anhydride copolymer Na salt. Crosslinked products, corn starch, xanthan gum, arabic gum, tragacanth gum, karaya gum, guar gum, gelatin and the like can be mentioned. The binding / thickening agent is, for example, 0.01 to 40% by mass, preferably 0.
1 to 20 mass% is added.

Examples of the tackifier include rosin-based resins, terpene-based resins and phenol-based resins. The tackifier is, for example, 0.1 to 0.1 with respect to the whole.
60% by mass, preferably 0.5 to 30% by mass is added.

Examples of preservatives include methylparaben, propylparaben, thymol and the like. The preservative is, for example, 0.0 to the entire hydrogel composition.
It is added in an amount of 01 to 5% by mass, preferably 0.01 to 1% by mass.

Examples of the solubilizer include ethanol, liquid paraffin, squalane and the like. The dissolving agent is
For example, 0.5 to 60% by mass, preferably 1 to 30% by mass is added to the entire composition.

Examples of the surfactant include polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyoxyethylene glycol ether, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene. Examples thereof include alkyl ether, sorbitan fatty acid ester, glycerin fatty acid and the like. The surfactant is, for example, 0.05 to 3 with respect to the entire composition.
0% by mass, preferably 0.1 to 15% by mass is added. By adding the surfactant, the effect of improving the effectiveness and stability of the drug can be obtained.

The stabilizer is added in order to prevent fading and discoloration of the composition. Examples of the stabilizer include ethylenediamine disodium salt (EDTA disodium) and the like. The stabilizer is, for example, 0.001 to 10% by mass, preferably 0.0
05-2 mass% is added.

Examples of the transdermal absorption enhancer include crotamiton, benzyl alcohol and the like. The transdermal absorption enhancer is, for example, 0.05 to 20 with respect to the entire composition.
%, Preferably 0.1 to 10% by weight.

As the fragrance, for example, herb essential oils,
There are extracts, other lower alcohols, and aldehydes. Specifically, anise, angelica, benzoin, immortelle, chamomile, garlic, cardamom, galvanum, caraway, carrot seed, guaacwood, grapefruit, cypress, sandalwood. , Cedarwood, juniper, star anise, sage, geranium, celery, thyme, tarragon, turpentine, spruce, frankincense, violet, pine, parsley, birch, patchouli, rose, hissop, fennel, black pepper, bodaiju flower, myrrh, yarrow, Lemon,
Examples include lemongrass, rosemary, laurel, syringa, peach, cornflower, eucalyptus, yuzu, lavender, peppermint and the like. These can be used alone or in combination of two or more. The fragrance is, for example, 0.0005 to 10 mass% with respect to the entire composition,
Preferably, 0.001 to 5 mass% is added.

The type of dye is not particularly limited, and dyes described in the Legal Dye Handbook can be blended. For example, water-soluble dyes such as Blue No. 1, Yellow No. 4 and Red No. 102, and Blue No. 404. , Non-water-soluble / non-oil-soluble pigments such as Yellow No. 205, and the like. The dye is, for example, 0.00005 to 1% by mass, preferably 0.
0001 to 0.1 mass% is added.

[0029]

EXAMPLES The present invention will be specifically described below by showing Examples and Comparative Examples, but the present invention is not limited to the following Examples.

Each formulation was prepared with the composition shown in Tables 1-6. Each component was kneaded by a conventional method to obtain a composition.
The cosmetics, massage agents and ointments are stored in a suitable container, and the patch composition is evenly applied on the support so as to be 700 g / m ³ to form a pressure-sensitive adhesive layer, and then a patch is applied on the surface thereof. A plastic film was covered as a single liner to give a patch. Each formulation described above was evaluated for warmth during use and skin irritation by the following methods. The evaluation was carried out on 10 subjects, and the average score of each score was obtained.

<< Warmness during Use >> Each preparation was applied to the inside of the forearm of a subject, and the warmth immediately after use and the warmth after 5 minutes (10 minutes after application of the patch) were evaluated according to the following evaluation criteria. The amount of each agent used is 0.5 g for cosmetics, massage agents and ointments, and 10 cm x 14 c for patches.
The shape is m.

<< Skin Irritation (Spirit Feeling) >> Each preparation was applied to the inside of the forearm of a subject, and skin irritation during use was evaluated according to the following evaluation criteria. Regarding the amount of each agent used,
The cosmetic, the massage agent and the ointment had a shape of 0.5 g, and the patch had a shape of 10 cm × 14 cm.

[0033]

[Table 1]

[0034]

[Table 2]

[0035]

[Table 3]

[0036]

[Table 4]

[0037]

[Table 5]

[0038]

[Table 6]

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 47/02 A61K 47/02 47/04 47/04 47/34 47/34 A61P 3/00 A61P 3 / 00 9/00 9/00 17/00 17/00 43/00 105 43/00 105 C09K 5/16 C09K 5/00 JF Term (reference) 4C076 AA72 BB31 CC11 CC18 CC21 CC26 EE23A FF36 4C083 AA112 AA122 AB172 AB242 AB282 AB312 AB342 AB352 AB362 AB442 AC032 AC072 AC122 AC172 AC182 AC302 AC432 AC442 AC642 AC682 AC792 AC852 AD041 AD042 AD072 AD092 AD152 AD282 AD532 BB51 CC02 CC05 DD12 EE12 EE13

Claims (5)

[Claims] 1. An exothermic composition comprising polyethylene glycol having an average molecular weight of less than 350, polyethylene glycol having an average molecular weight of 350 or more, and an exothermic agent. 2. The exothermic composition according to claim 1, wherein the mixing ratio of polyethylene glycol having a molecular weight of less than 350 and polyethylene glycol having a molecular weight of 350 or more is 1:10 to 100: 1. 3. The exothermic composition according to claim 1, wherein the exothermic agent has a negative enthalpy of dissolution in water at 25 ° C. 4. The exothermic composition according to any one of claims 1 to 3, which is a skin external preparation. 5. A patch comprising the exothermic composition according to any one of claims 1 to 3 and a support.