Cataplasm

Abstract

This cataplasm includes a support layer, an adhesive layer laminated on the support layer, and a release liner provided on a surface of the adhesive layer which is on the opposite side from the support layer. The adhesive layer contains a drug, water, gelatin, l-menthol, a (methyl acrylate)-(2-ethylhexyl acrylate) copolymer resin emulsion, and magnesium aluminometasilicate, wherein the amount of the (methyl acrylate)-(2-ethylhexyl acrylate) copolymer resin emulsion is 1.5-20 mass%, the amount of magnesium aluminometasilicate is 0.25-0.45 mass%, and the amount of gelatin is 1-3 mass% relative to the whole mass of the adhesive layer.

Description

Poultice

[0001] The present invention relates to a poultice.

[0002] A cataplasm is a type of adhesive patch produced by spreading a drug-containing adhesive layer on a support layer such as cloth, and the adhesive layer generally has a high moisture content. To achieve a high moisture content in the adhesive layer and ensure excellent shape retention and cohesion, the adhesive layer contains a water-soluble polymer such as gelatin, polyacrylic acid, neutralized polyacrylic acid, or polyvinyl alcohol. Furthermore, a cataplasm containing a cooling agent such as l-menthol can provide a cooling sensation upon use and exhibit pain-relieving and cooling effects (see, for example, Patent Documents 1 and 2).

[0003] It is known that cataplasms containing l-menthol may have the problem of l-menthol crystals precipitating in the adhesive layer. To solve this problem, for example, Patent Document 3 discloses that the content of menthol in a hydrogel composition is set to a specific amount, and one or more selected from silica and talc are blended into the hydrogel composition, thereby suppressing menthol precipitation.

[0004] JP 2020-132637 A JP 2019-81755 A JP 2022-75038 A

[0005] In the process of developing a cataplasm in which precipitation of l-menthol crystals is inhibited, the present inventors have found that in addition to precipitation of l-menthol crystals, problems such as uneven spreading during spreading, exudation of components of the adhesive layer from the backing layer after spreading, insufficient adhesion and liner releasability, and pain when peeling off the cataplasm after application to the skin may occur.

[0006] The present invention has been made in view of the problems associated with the above-mentioned prior art, and aims to provide a cataplasm that inhibits precipitation of 1-menthol crystals, spreads evenly, has excellent adhesion and liner releasability, inhibits bleeding, and suppresses pain when removed.

[0007] The present inventors have conducted extensive research to achieve the above-mentioned object, and as a result have found that, in an adhesive layer containing water, gelatin, l-menthol, a methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion, and magnesium aluminometasilicate, by adjusting the content of the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion within a predetermined range, a cataplasm in which precipitation of l-menthol crystals is inhibited can be obtained.

[0008] However, even though the content of the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion was within the specified range, new problems arose, such as unevenness during spreading of the adhesive layer, leaching of the components of the adhesive layer into the support layer after spreading, insufficient adhesion and liner releasability, and pain when removing the poultice.

[0009] As a result of intensive research into the above-mentioned problems, the present inventors have found that the above-mentioned problems can be solved by adjusting the blending amounts of magnesium aluminometasilicate and gelatin, among the components contained in the poultice of the present invention, to a predetermined range, and have thus completed the present invention.

[0010] That is, the present invention includes the following [1] and [2]. [1] A cataplasm comprising a support layer, a pressure-sensitive adhesive layer laminated on the support layer, and a release liner provided on the surface of the pressure-sensitive adhesive layer opposite the support layer, wherein the pressure-sensitive adhesive layer contains a drug, water, gelatin, 1-menthol, a methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion, and magnesium aluminometasilicate, wherein the content of the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion is 1.5% to 20% by mass, the content of the magnesium aluminometasilicate is 0.25% to 0.45% by mass, and the content of the gelatin is 1% to 3% by mass, based on the total mass of the pressure-sensitive adhesive layer. [2] The cataplasm according to [1], wherein the pressure-sensitive adhesive layer further contains at least one member selected from the group consisting of polyacrylic acid and neutralized polyacrylic acid.

[0011] According to the present invention, it is possible to provide a cataplasm that inhibits precipitation of 1-menthol crystals, spreads evenly, has excellent adhesion and liner releasability, inhibits bleeding, and reduces pain when removed.

[0012] Preferred embodiments of the present invention will be described in detail below.

[0013] A poultice according to a first embodiment of the present invention comprises a support layer, an adhesive layer laminated on the support layer, and a release liner provided on the surface of the adhesive layer opposite the support layer, wherein the adhesive layer contains a drug, water, gelatin, 1-menthol, a methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion and magnesium aluminometasilicate, and the content of the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion is 1.5% by mass to 20% by mass, the content of the magnesium aluminometasilicate is 0.25% by mass to 0.45% by mass, and the content of the gelatin is 1% by mass to 3% by mass, based on the total mass of the adhesive layer.

[0014] The support layer may be any layer capable of supporting a water-containing pressure-sensitive adhesive layer, and those well known to those skilled in the art may be used. Examples of the support layer include woven fabric (including knitted fabric), nonwoven fabric, resin film, foam sheet, and paper. When using woven fabric, nonwoven fabric, or resin film as the support layer, its material may include, for example, polyolefins such as polyethylene, polypropylene, and polybutylene, polyesters such as polyethylene terephthalate, rayon, polyurethane, and cotton, and these may be used alone or in combination of two or more, and may be a single layer or a laminate. Polyester is more preferably used as the material for the support layer.

[0015] The support layer is preferably a nonwoven fabric or a woven fabric, and particularly preferably a nonwoven fabric or a woven fabric having a predetermined elongation recovery rate (elongation elastic modulus). In this specification, "elongation recovery rate" refers to a value measured according to the description of JIS L1096:2010, and means "elongation elastic modulus at constant load" or "elongation elastic modulus at constant rate elongation." For example, "50% elongation recovery rate" refers to the elongation elastic modulus when elongated to an elongation rate of 50% (constant rate elongation), and "load at 50% elongation" refers to the load (constant load) required to elongate to an elongation rate of 50%. Using a nonwoven fabric or woven fabric having a predetermined elongation recovery rate is preferable because the support layer expands and contracts in accordance with the movement of the application site when applied to a moving part such as a joint.

[0016] When the support layer is a nonwoven fabric, the recovery rate of the nonwoven fabric at 50% elongation is, for example, 60 to 99%, preferably 65 to 95%, and more preferably 70 to 90%. The load at 50% elongation of the nonwoven fabric is, for example, 1 to 6 N / 50 mm in the longitudinal direction (long axis direction) and 0.1 to 3 N / 50 mm in the transverse direction (short axis direction). The basis weight of the support layer is preferably, for example, 80 to 150 g / m. ２ and 90 to 120 g / m ２ is preferable. A suitable thickness of the support layer is, for example, 0.5 to 2 mm. The basis weight and thickness of the support layer are measured in accordance with the standard of JIS L1906:2000. The bending resistance of the support layer (the bending resistance is measured by Method A (45° cantilever method) of JIS L1096:2010) can be, for example, 20 to 40 mm in the longitudinal direction (long axis direction) and 10 to 35 mm in the transverse direction (short axis direction), and is preferably 25 to 35 mm in the longitudinal direction (long axis direction) and 15 to 30 mm in the transverse direction (short axis direction).

[0017] The knitted fabric used as the support layer also includes knitted fabrics obtained by gathering stitches by circular knitting, warp knitting, weft knitting, etc. Knitted fabrics made of one or a combination of two or more materials such as polyester, nylon, polypropylene, and rayon are preferred, and among these, knitted fabrics made of polyethylene terephthalate, which has little interaction with drugs, are more preferred.

[0018] In particular, when the support layer is a woven fabric, the recovery rate at 50% elongation of the woven fabric is, for example, 60 to 99%, preferably 65 to 95%, and more preferably 70 to 90%. The load at 50% elongation is, for example, 1 to 5 N / 25 mm in the longitudinal direction (long axis direction) and 0.1 to 3 N / 25 mm in the transverse direction (minor axis direction). The bending resistance of the support layer can be, for example, 10 to 30 mm in the longitudinal direction (long axis direction) and 10 to 30 mm in the transverse direction (minor axis direction), and is preferably 15 to 25 mm in the longitudinal direction (long axis direction) and 15 to 25 mm in the transverse direction (minor axis direction).

[0019] The thickness of the woven fabric as the support layer is preferably 0.5 to 2 mm.

[0020] In particular, the basis weight is 80 to 150 g / m ２ When the polyethylene terephthalate woven fabric is used, the water contained in the adhesive is less likely to seep through the mesh of the woven fabric during spreading, and the anchoring property between the woven fabric and the adhesive is more excellent.

[0021] Furthermore, the polyethylene terephthalate woven fabric preferably has a longitudinal (longitudinal) modulus of 2 to 12 N / 50 mm and a transverse (minor axial) modulus of 2 to 8 N / 50 mm (modulus measurement method is in accordance with JIS L1018:1999). If the modulus is lower than 2 N / 50 mm, the woven fabric may stretch when the adhesive is spread, causing the adhesive to penetrate the mesh, resulting in a decrease in functionality as a cataplasm. If the modulus is higher than 12 N / 50 mm (longitudinal) or 8 N / 50 mm (transverse), the cataplasm may have poor stretchability and may not be able to follow the expansion of the skin when applied to a movable part.

[0022] The material of the release liner is not particularly limited, and liners made of materials generally known to those skilled in the art can be used. When a woven fabric, nonwoven fabric, knitted fabric, or resin film is used as the support layer, examples of the material of the release liner include polyethylene, polypropylene, polybutylene, polyethylene terephthalate, rayon, polyurethane, and paper, and these materials may be used alone or in combination of two or more. The material of the release liner is preferably polypropylene film.

[0023] The adhesive layer contains a drug, water, gelatin, 1-menthol, a methyl acrylate / 2-ethylhexyl acrylate copolymer resin emulsion, and magnesium aluminometasilicate.

[0024] The drug is not particularly limited as long as it is a drug that can be absorbed transdermally. Examples of the drug include non-steroidal anti-inflammatory drugs such as indomethacin, felbinac, flurbiprofen, diclofenac, diclofenac sodium, methyl salicylate, glycol salicylate, and ketoprofen, or esters thereof, antihistamines such as diphenhydramine, analgesics such as aspirin, acetaminophen, ibuprofen, and loxoprofen sodium, local anesthetics such as lidocaine, muscle relaxants such as suxamethonium chloride, antifungal agents such as clotrimazole, antihypertensives such as clonidine, vasodilators such as nitroglycerin and isosorbide dinitrate, vitamins such as vitamin A, vitamin E (tocopherol), tocopherol acetate, vitamin K, octotiamine, and riboflavin butyrate, prostaglandins, scopolamine, fentanyl, capsicum extract, and vanillylamide nonylate. Some drugs exist as two optical isomers, the R- and S-forms. The drug used in this embodiment may be any one of the optical isomers, or may be a mixture of the two optical isomers in any ratio. The drug may be in the form of a pharmaceutically acceptable salt, and examples of the pharmaceutically acceptable salt include inorganic base salts such as sodium salts, potassium salts, and calcium salts; organic base salts such as amine salts such as monoethanolamine and diethanolamine; inorganic acid salts such as hydrochloride, nitrate, and phosphate; and organic acid salts such as acetate, lactate, benzenesulfonate, and citrate.

[0025] The content of the drug in the adhesive layer may be an amount that allows the drug to exert its medicinal effect, and varies depending on the type of drug. For example, the content may be 0.5% by mass to 1.5% by mass for indomethacin, 0.5% by mass to 1.5% by mass for diclofenac sodium, 0.1% by mass to 1% by mass for ketoprofen, 0.5% by mass to 1.5% by mass for felbinac, and 0.1% by mass to 1% by mass for flurbiprofen.

[0026] The water content in the pressure-sensitive adhesive layer can be 30% by mass to 70% by mass, or may be 30% by mass to 60% by mass, or 35% by mass to 52% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0027] The gelatin content in the adhesive layer is 1% by mass to 3% by mass, preferably 1.25% by mass to 3% by mass, and more preferably 1.5% by mass to 3% by mass, based on the total mass of the adhesive layer.

[0028] The content of 1-menthol in the pressure-sensitive adhesive layer can be 0.5% by mass to 3% by mass, preferably 1% by mass to 2% by mass, and more preferably 1% by mass to 1.5% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0029] The methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion is an emulsion (aqueous emulsion) in which a methyl acrylate-2-ethylhexyl acrylate copolymer resin is dispersed in water. The content of the methyl acrylate-2-ethylhexyl acrylate copolymer resin in the emulsion can be 55% by mass to 65% by mass based on the total mass of the emulsion. The emulsion may contain an emulsifier, and examples of emulsifiers include polyoxyethylene nonylphenyl ether. The content of the emulsifier can be 1% by mass to 5% by mass based on the total mass of the emulsion. The content of the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion in the pressure-sensitive adhesive layer is 1.5% by mass to 20% by mass (corresponding to 0.825% by mass to 13% by mass as the methyl acrylate-2-ethylhexyl acrylate copolymer resin), preferably 2% by mass to 19% by mass (corresponding to 1.1% by mass to 12.35% by mass as the methyl acrylate-2-ethylhexyl acrylate copolymer resin) or 3% by mass to 20% by mass (corresponding to 1.65% by mass to 13% by mass as the methyl acrylate-2-ethylhexyl acrylate copolymer resin), and more preferably 3% by mass to 18% by mass (corresponding to 1.65% by mass to 11.7% by mass as the methyl acrylate-2-ethylhexyl acrylate copolymer resin). Commercially available methyl acrylate / 2-ethylhexyl acrylate copolymer resin emulsions include, for example, Nikazol TS-620 (trade name, manufactured by Nippon Carbide Industries Co., Ltd.) and BPW HW-2 (trade name, manufactured by Toyochem Co., Ltd.).

[0030] The content of magnesium aluminometasilicate in the pressure-sensitive adhesive layer is 0.25% by mass to 0.45% by mass, preferably 0.25% by mass to 0.43% by mass, and more preferably 0.28% by mass to 0.4% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0031] In the pressure-sensitive adhesive layer, the ratio of the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion content to the magnesium aluminometasilicate content is preferably 3.3:1 to 80:1 (equivalent to 1.815:1 to 52:1 as the methyl acrylate-2-ethylhexyl acrylate copolymer resin), more preferably 5.4:1 to 76:1 (equivalent to 2.97:1 to 49.4:1 as the methyl acrylate-2-ethylhexyl acrylate copolymer resin) or 6.6:1 to 80:1 (equivalent to 3.63:1 to 52:1 as the methyl acrylate-2-ethylhexyl acrylate copolymer resin), and even more preferably 7.5:1 to 72:1 (equivalent to 4.125:1 to 46.8:1 as the methyl acrylate-2-ethylhexyl acrylate copolymer resin). The ratio of the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion content to the gelatin content in the pressure-sensitive adhesive layer is preferably 0.5:1 to 20:1 (equivalent to 0.275:1 to 13:1 as the methyl acrylate-2-ethylhexyl acrylate copolymer resin), more preferably 0.75:1 to 16:1 (equivalent to 0.4125:1 to 10.4:1 as the methyl acrylate-2-ethylhexyl acrylate copolymer resin) or 1:1 to 20:1 (equivalent to 0.55:1 to 13:1 as the methyl acrylate-2-ethylhexyl acrylate copolymer resin), and even more preferably 1:1 to 12:1 (equivalent to 0.55:1 to 7.8:1 as the methyl acrylate-2-ethylhexyl acrylate copolymer resin).

[0032] The adhesive layer may contain, as other components, water-soluble polymers (excluding gelatin; the same applies hereinafter), cooling agents (excluding l-menthol; the same applies hereinafter), adhesion enhancers (excluding methyl acrylate / 2-ethylhexyl acrylate copolymer resin emulsion; the same applies hereinafter), solubilizing agents, crosslinking agents (excluding magnesium aluminometasilicate; the same applies hereinafter), fillers, moisturizing agents, stabilizers, preservatives, chelating agents, colorants, flavoring agents, pH adjusters, etc. In one embodiment of the present invention, the adhesive layer preferably does not contain propylene glycol.

[0033] Examples of adhesion enhancers include acrylic acid ester copolymers such as aminoalkyl methacrylate copolymer E. When the pressure-sensitive adhesive layer contains an adhesion enhancer, the content thereof is preferably 0.1% by mass to 1.0% by mass based on the total mass of the pressure-sensitive adhesive layer. It is preferable that the pressure-sensitive adhesive layer does not contain any adhesion enhancers other than the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion.

[0034] The water-soluble polymer is not particularly limited as long as it can retain moisture in the adhesive layer, and those generally known to those skilled in the art can be used. Examples of water-soluble polymers include polyacrylic acid, neutralized polyacrylic acid, polyvinyl alcohol, polyvinylpyrrolidone, sodium alginate, hydroxypropyl cellulose, sodium carboxymethylcellulose (carmellose sodium), methylcellulose, and carrageenan. A single water-soluble polymer may be used, or two or more may be used in combination. The neutralized polyacrylic acid may be a fully neutralized polyacrylic acid, a partially neutralized polyacrylic acid, or a mixture thereof. Examples of the neutralized polyacrylic acid include polyacrylic acid salts, such as sodium salts, potassium salts, calcium salts, and ammonium salts. The partially neutralized polyacrylic acid is a polymer chain in which structural units derived from acrylic acid and structural units derived from acrylic acid salts are present in any ratio. It is preferable to use a partially neutralized polyacrylic acid in which 50 mol% of the carboxy groups in a polymer chain are neutralized. The water-soluble polymer preferably contains at least one selected from the group consisting of polyacrylic acid and neutralized polyacrylic acid, and more preferably contains polyacrylic acid and neutralized polyacrylic acid. When the pressure-sensitive adhesive layer contains a water-soluble polymer, the content thereof is preferably 3% by mass to 15% by mass, more preferably 5% by mass to 13% by mass, and even more preferably 7% by mass to 11% by mass, based on the total mass of the pressure-sensitive adhesive layer. When the pressure-sensitive adhesive layer contains polyacrylic acid, the content thereof is preferably 1% by mass to 5% by mass, more preferably 2% by mass to 5% by mass, and even more preferably 2.5% by mass to 4.5% by mass, based on the total mass of the pressure-sensitive adhesive layer. When the pressure-sensitive adhesive layer contains neutralized polyacrylic acid, the content thereof is preferably 1% by mass to 5% by mass, more preferably 1.5% by mass to 4.5% by mass, and even more preferably 2% by mass to 4% by mass, based on the total mass of the pressure-sensitive adhesive layer.When the pressure-sensitive adhesive layer contains polyvinyl alcohol, the content thereof is preferably 1% by mass to 5% by mass, more preferably 1% by mass to 4% by mass, and even more preferably 1.5% by mass to 3.5% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0035] Examples of the refreshing agent include thymol, 1-isopulegol, and peppermint oil. One refreshing agent may be used alone, or two or more refreshing agents may be used in combination. When the pressure-sensitive adhesive layer contains a refreshing agent, the content thereof is preferably 1% by mass to 1.5% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0036] The solubilizing agent is not particularly limited as long as it can dissolve the drug, and examples thereof include surfactants such as crotamiton; N-methylpyrrolidone; polyalkylene glycols such as polyethylene glycol (PEG) and polybutylene glycol; oxyalkylene fatty acid esters such as polyethylene glycol monostearate; polyoxyalkylene sorbitan fatty acid esters such as polysorbate 80; sorbitan fatty acid esters such as sorbitan monooleate; and polyoxyethylene hydrogenated castor oil. These solubilizing agents may be used alone or in combination of two or more. When the adhesive layer contains a solubilizing agent, the content thereof is preferably 0.1% by mass to 3% by mass, more preferably 0.2% by mass to 1% by mass, and even more preferably 0.3% by mass to 0.7% by mass, based on the total mass of the adhesive layer.

[0037] The crosslinking agent is a component for adjusting the degree of progress of the crosslinking reaction between neutralized polyacrylic acids and between the neutralized polyacrylic acid and optionally added polyacrylic acid, and crosslinking agents commonly used in poultices can be used. Examples of crosslinking agents include aluminum compounds. When the adhesive layer contains a crosslinking agent, the content thereof is preferably 0.05% by mass to 1% by mass, more preferably 0.1% by mass to 0.7% by mass, and even more preferably 0.2% by mass to 0.5% by mass, based on the total mass of the adhesive layer. When the content of the crosslinking agent is within this range, a poulticet with better skin conformability can be obtained. It is preferable that the adhesive layer does not contain any crosslinking agent other than magnesium aluminometasilicate.

[0038] Examples of the filler include inorganic fillers such as silicic anhydride, titanium oxide, synthetic aluminum silicate, kaolin, talc, bentonite, magnesium aluminometasilicate, etc., and these may be used alone or in combination of two or more. When the pressure-sensitive adhesive layer contains a filler, the content thereof is preferably 0.1% by mass to 1.5% by mass, more preferably 0.2% by mass to 1% by mass, and even more preferably 0.3% by mass to 0.7% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0039] The humectant is not particularly limited as long as it can suppress evaporation of water from the pressure-sensitive adhesive layer over time. Examples of humectants include polyhydric alcohols such as glycerin, sorbitol, ethylene glycol, 1,4-butanediol, polyethylene glycol, and liquid paraffin. These humectants may be used alone or in combination of two or more. The humectant preferably contains at least one selected from the group consisting of glycerin and sorbitol, and more preferably contains glycerin and sorbitol. When the pressure-sensitive adhesive layer contains a humectant, the content thereof is preferably 15% by mass to 45% by mass, more preferably 20% by mass to 40% by mass, and even more preferably 25% by mass to 35% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0040] Examples of stabilizers include oxybenzone, dibutylhydroxytoluene (BHT), sodium edetate, UV absorbers (e.g., dibenzoylmethane derivatives), etc. When the pressure-sensitive adhesive layer contains a stabilizer, the content thereof is preferably 0.05% by mass to 1% by mass, more preferably 0.1% by mass to 0.6% by mass, and even more preferably 0.2% by mass to 0.6% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0041] Examples of preservatives include methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, butyl parahydroxybenzoate, 1,2-pentanediol, benzoic acid and its salts, salicylic acid and its salts, sorbic acid and its salts, dehydroacetic acid and its salts, 4-isopropyl-3-methylphenol, 2-isopropyl-5-methylphenol, phenol, hinokitiol, cresol, 2,4,4'-trichloro-2'-hydroxydiphenyl ether, 3,4,4'-trichlorocarbanilide, chlorobutanol, benzalkonium chloride, and benzethonium chloride. These preservatives may be used alone or in combination of two or more. When the pressure-sensitive adhesive layer contains a preservative, the content thereof is preferably 0.01% by mass to 1% by mass, more preferably 0.05% by mass to 0.5% by mass, and even more preferably 0.1% by mass to 0.2% by mass, based on the total mass of the pressure-sensitive adhesive layer.

[0042] Examples of chelating agents include edetic acid (also known as ethylenediaminetetraacetic acid, EDTA) or salts thereof, ascorbic acid, pyrophosphate, hexametaphosphate, gluconate, etc. These chelating agents may be used alone or in combination of two or more. A more specific example of an edetate is sodium edetate. When the adhesive layer contains a chelating agent, the content thereof is preferably 0.05% by mass to 1% by mass, more preferably 0.1% by mass to 0.6% by mass, and even more preferably 0.2% by mass to 0.6% by mass, based on the total mass of the adhesive layer.

[0043] The total mass of the adhesive layer is 200 g / m ２~1000g / m ２ and 400 g / m ２ ~1000g / m ２ and 400 g / m ２ ~650g / m ２ Preferably, 400 g / m ２ ~650g / m ２ When the total mass of the adhesive layer is within the above range, the thickness of the entire poultice can be reduced, the poultice can easily conform to the skin, and the difference in level with the peripheral edge when applied is reduced, so that the poultice tends to be less likely to peel off.

[0044] The pH of the adhesive layer is preferably 4 to 8, and more preferably 4.5 to 6. A pH of 4 or higher reduces skin irritation, while a pH of 8 or lower improves the moldability and shape retention of the poultice. In particular, when the backing layer is a woven fabric, particularly a knitted fabric, bleeding may occur during the formation of the adhesive layer, but a pH of 5 to 6.5 tends to suppress bleeding. The pH can be measured, for example, according to the pH measurement method in the General Test Methods of the Japanese Pharmacopoeia, using a glass composite electrode and diluting a sample 20 times with purified water.

[0045] The cataplasm can be produced, for example, by mixing a drug, water, gelatin, 1-menthol, a methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion, magnesium aluminometasilicate, and, if necessary, the optional components described above, to obtain a pressure-sensitive adhesive composition, spreading the pressure-sensitive adhesive composition uniformly on a release liner, and laminating a support layer thereon. Alternatively, the cataplasm may be produced by spreading the pressure-sensitive adhesive composition uniformly on a support layer, and laminating a release liner thereon.

[0046] Each component of the composition shown in each of the Examples and Comparative Examples in Tables 1 to 4 (the numerical value of each component in the tables represents mass %) was mixed to prepare a pressure-sensitive adhesive composition. Next, the obtained pressure-sensitive adhesive composition was applied to a pressure-sensitive adhesive layer having a mass per unit area of ​​500 g / m. ２The adhesive was spread evenly on a release liner (polypropylene film) so that the adhesive was in the range of 100 g / m². ２ ) are stacked to form a 140 cm ２ The plaster was then cut into a size of 10 cm x 14 cm to obtain a cataplasm. Nikazol TS-620 (trade name, manufactured by Nippon Carbide Industries Co., Ltd.) was used as the methyl acrylate / 2-ethylhexyl acrylate copolymer resin emulsion. Concentrated glycerin and D-sorbitol solutions listed in the Japanese Pharmacopoeia (18th Edition of the Japanese Pharmacopoeia) were used. Each cataplasm was evaluated for l-menthol precipitation, unevenness during spreading, bleeding, liner slippage, liner peelability, initial adhesion, adhesion over time, pain upon peeling, and residual adhesive layer using the following methods.

[0047] <Unevenness during spreading> The pressure-sensitive adhesive layer was observed during spreading and evaluated according to the following evaluation scores. A score of 2 or more was judged to be acceptable. 2. The surface and thickness are uniform over the entire surface of the pressure-sensitive adhesive layer (area: 90% or more), and there is no uneven spreading. 1. The surface and / or thickness are not uniform over a portion of the pressure-sensitive adhesive layer (area: more than 10%), and uneven spreading is observed.

[0048] In all of the following evaluations, the cataplasm was sealed in an aluminum packaging bag and allowed to stand at 25°C for 10 days or more, up to 15 days, and then the cataplasm was removed from the packaging bag and evaluated.

[0049] <L-menthol Deposition> The surface of the adhesive layer of the cataplasm was visually observed, and the presence or absence of crystalline precipitation of l-menthol was evaluated according to the following criteria. Evaluation was performed on 10 cataplasms, and the average score was taken as the evaluation result. A score (average value) of 2.0 or more was judged to be acceptable. 2. No precipitation 1. Presence of precipitation

[0050] <Bleeding> The area of ​​the portion where components of the adhesive layer had bled into the support layer was measured and evaluated according to the following evaluation scores. Five to 20 patches were evaluated, and the average of the scores was used as the evaluation result. A score (average) of 5.0 or more was judged to be acceptable. 5. No bleed-through 4. Slight bleed-through (area: less than 10%) 3. Slight bleed-through (area: 10% or more but less than 20%) 2. Heavy bleed-through (area: 20% or more but less than 30%) 1. Considerable bleed-through (area: 30% or more)

[0051] <Liner slippage> The degree of slippage between the adhesive layer of the cataplasm and the release liner was scored according to the following criteria. Five to 20 cataplasms were evaluated, and the average score was used as the evaluation result. A score (average value) of 4.0 or more was judged to be acceptable. 4. No liner slippage (slippage less than 0.5 mm) 3. Almost no liner slippage (slippage of 0.5 mm or more but less than 1.5 mm) 2. Obvious liner slippage (slippage of 1.5 mm or more) 1. Unmeasurable (liner layer fell off during the test)

[0052] <Liner Removability> The ease of peeling when peeling and removing the release liner from the cataplasm was scored according to the following criteria. Five to 20 cataplasms were evaluated, and the average score was used as the evaluation result. A score (average value) of 3.0 or more was judged to be acceptable. 5. Very easy to peel 4. Somewhat easy to peel 3. Acceptable removability 2. Somewhat difficult to peel 1. Very difficult to peel

[0053] <Initial Adhesion> The release liner was peeled off from the patch and applied to the elbows of 5 to 20 subjects. After bending the elbows 40 times, the adhesion of the adhesive layer to the skin was scored according to the following criteria. The average score of the 5 to 20 subjects was used as the evaluation result, and a score (average value) of 5.0 or more was judged to be acceptable. 6. No peeling 5. Peeling at the edge (less than 1 / 4) 4. Peeling of 1 / 4 or more but less than 1 / 3 3. Peeling of 1 / 3 or more but less than 1 / 2 2. Peeling of 1 / 2 or more 1. Falling off

[0054] <Adhesion over time> The release liner was peeled off from the patch and applied to the elbows of 5 to 20 subjects, and the adhesion of the adhesive layer to the skin after 4 hours and 6 hours was scored according to the following criteria. The average score of the 5 to 20 subjects was used as the evaluation result, and a score (average value) of 5.0 or more was judged to be acceptable. 6. No peeling 5. Peeling at the edge (less than 1 / 4) 4. Peeling of 1 / 4 or more but less than 1 / 3 3. Peeling of 1 / 3 or more but less than 1 / 2 2. Peeling of 1 / 2 or more 1. Falling off

[0055] <Pain upon removal> In the above-mentioned adhesion test over time, the patch was removed from the subject's elbow after 6 hours of application, and the pain experienced upon removal of the patch was scored according to the following criteria. The average score of 5 to 20 subjects was used as the evaluation result, and a score (average value) of 3.0 or more was judged to be acceptable. 4. None 3. Slightly (not noticeable) 2. Slightly painful 1. Very painful

[0056] <Adhesive layer remaining> In the above-mentioned test for pain at removal, the proportion of the adhesive layer remaining on the skin (area basis) after the cataplasm was removed was scored according to the following criteria. The average score of 5 to 20 subjects was used as the evaluation result, and a score (average value) of 3.0 or more was judged to be acceptable. 4. None 3. Slightly remaining (less than 1 / 10) 2. Slightly remaining (1 / 10 or more but less than 1 / 5) 1. Considerable remaining (1 / 5 or more)

[0057] The results are summarized in Tables 1 to 4. In the tables, A indicates that the acceptable conditions in the above evaluation are met, and B indicates that the acceptable conditions are not met.

[0058] As is clear from the results shown in Table 1, it was confirmed that in the cataplasm containing less than 1.5% by mass of methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion (Comparative Example 1), l-menthol crystals precipitated and the liner releasability was insufficient. On the other hand, in the cataplasms containing 3.0% to 25% by mass of methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion (Comparative Examples 2 to 6), although l-menthol crystal precipitation was inhibited, other problems arose, such as insufficient liner releasability, adhesion, bleeding, or pain upon removal.

[0059]

[0060] As is clear from the results shown in Table 2, the patches having a magnesium aluminometasilicate content of less than 0.25% by mass or more than 0.45% by mass (Comparative Examples 7, 8, 11, 12, and 15) and the patches having a gelatin content of less than 1% by mass or more than 3% by mass (Comparative Examples 7 to 15) were found to be insufficient in at least one respect: unevenness during spreading, adhesion, bleeding, and liner releasability.

[0061]

[0062]

[0063] As is clear from the results shown in Tables 3 and 4, the poultices of the present invention (Examples 1 to 8 and 14 to 18) were confirmed to be excellent in all evaluation items.

[0064] Furthermore, poultices (Examples 9 to 12) were produced in the same manner as in Example 4, except that diclofenac sodium (1.0% by mass), ketoprofen (0.3% by mass), felbinac (0.7% by mass), or flurbiprofen (0.33% by mass) was used instead of indomethacin, and the poultices were evaluated. All of the poultices of Examples 9 to 12 showed good results in all evaluation items.

[0065] Furthermore, a cataplasm (Example 13) was produced in the same manner as in Example 4, except that BPW HW-2 (trade name, manufactured by Toyochem Co., Ltd.) was used as the methyl acrylate / 2-ethylhexyl acrylate copolymer resin emulsion instead of Nikazol TS-620 (trade name, manufactured by Nippon Carbide Industries Co., Ltd.), and the cataplasm was evaluated. The cataplasm of Example 13 showed good results in all evaluation items.

Claims

1. A poultice comprising: a support layer; an adhesive layer laminated on the support layer; and a release liner provided on the surface of the adhesive layer opposite the support layer, wherein the adhesive layer contains a drug, water, gelatin, 1-menthol, a methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion, and magnesium aluminometasilicate, and the content of the methyl acrylate-2-ethylhexyl acrylate copolymer resin emulsion is 1.5% to 20% by mass, the content of the magnesium aluminometasilicate is 0.25% to 0.45% by mass, and the content of the gelatin is 1% to 3% by mass, based on the total mass of the adhesive layer.

2. The poultice according to claim 1, wherein the adhesive layer further contains at least one selected from the group consisting of polyacrylic acid and neutralized polyacrylic acid.

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