JP2003119124A - Base fabric for percutaneous medicine and skin cataplasm - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a base fabric for a percutaneous medicine, lasting the cooling effect and the medicinal effect of the percutaneous medicine for a long period, and having improved adhesiveness with the percutaneous medicine, and further to provide a skin cataplasm. SOLUTION: This skin cataplasm 1 has the base fabric 10 for the percutaneous medicine, and a medicine-coated layer 20. The base fabric 10 for the percutaneous medicine has a base material layer 11, and a coat layer 12 laminated on the surface of the base material layer 11. The medicine-coated layer 20 is formed on the coat layer 12 side. The base material layer 11 is composed of a polyurethane obtained by a usual reaction of a diisocyanate with a polyol, and optionally extending the chain of the polyurethane. The coat layer 12 contains a water-soluble acrylic resin and a polyalkyleneimine. The medicine- coated layer 20 contains a nonsteroidal antiinflammatory agent of a percutaneously absorbable medicine, usable for myalgia and arthrodynia.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a base fabric for a transdermal drug and a skin patch used for the use of a transdermal drug.

[0002]

2. Description of the Related Art Conventionally, a percutaneous drug such as a head cooling sheet when a fever is generated and a haptic for muscle pain and joint pain has been widely used. At present, a non-woven fabric is used as a base fabric for a transdermal drug to which the above transdermal drug is applied. This non-woven fabric is stretchable in order to cope with the expansion and contraction of the skin when it is applied to joints and the like. Nonwoven fabrics are generally fibrous, and the transdermal drug physically penetrates into the fibrous layer to increase the adhesive strength. Is designed so that no transdermal drug remains on the skin.

On the other hand, a transdermal drug has an important function of removing heat and cooling by evaporating evaporated components such as water. Therefore, the transdermal drug base fabric must be constructed in consideration of this point as well. I have to. Therefore, in order to cool the transdermal drug or maintain the medicinal component for a long time, there is a technique of using a film having moisture permeability as a base fabric for the transdermal drug.

[0004]

However, in the technique of the above-mentioned film having moisture permeability, when it is actually used as a base fabric, the adhesive strength with the transdermal drug is insufficient, and the transdermal drug does not adhere to the skin when peeled off. There is a problem of remaining.

An object of the present invention is to provide a transdermal drug base cloth and a skin patch for maintaining a cooling effect of a transdermal drug and a medicinal component for a long time and improving adhesiveness with the transdermal drug. Especially.

[0006]

Means for Solving the Problems The inventors of the present invention have conducted intensive studies to develop a base fabric for a transdermal drug having the above-mentioned preferable properties, and as a result, have identified a coat layer to be laminated on a moisture-permeable film. It was found that by selecting the material of, the cooling effect of the transdermal drug and the medicinal component are maintained for a long time, and the adhesiveness with the transdermal drug is improved. The present invention has been completed based on such findings.

That is, the base fabric for a transdermal drug of the present invention is a base fabric for a transdermal drug to which a transdermal drug is applied, and a moisture-permeable film and the moisture-permeable film on the side to which the transdermal drug is applied. And a coat layer laminated on the film, wherein the coat layer contains a water-soluble acrylic resin and polyalkyleneimine. here,
Examples of the moisture permeable film include a moisture permeable film obtained by forming a hygroscopic resin into a film, and a microporous film such as a polyolefin resin.

As the moisture permeable film formed of a hygroscopic resin, a polyurethane moisture permeable film or a polyamide elastomer elastomer moisture permeable film having a polyether block is preferably used. In particular, in the base fabric for a transdermal drug product of the present invention, it is preferable that the moisture permeable film is made of polyurethane. Where polyurethane is
By the usual reaction of diisocyanate and polyol,
Known products obtained by chain extension can be adopted as necessary.

Examples of the diisocyanate capable of forming polyurethane include diphenylmethane diisocyanate, dicyclohexylmethane diisocyanate, tolylene diisocyanate, tridene diisocyanate and hexamethylene diisocyanate. As a polyol,
Polyester-based polyols such as polyethylene adipate, polybutylene adipate, polycaprolactone and polycarbonate; and polyether-based polyols such as polyoxytetramethylene glycol. Chain extenders include ethylene glycol, butanediol, hexanediol and the like.

According to this, since the moisture permeable film is made of polyurethane, it can be a base fabric for a transdermal drug which has elasticity and strength, and is excellent in abrasion resistance, oil resistance and adhesiveness.

The microporous film is not particularly limited, and is usually a polyolefin-based resin microporous film, particularly a polyethylene-based or polypropylene-based resin microporous film, the manufacturing method thereof is arbitrary, and a known film is known. Is used. This polyolefin resin microporous film is, for example, a filler or plasticizer is eluted from a film made of a polyolefin resin containing an inorganic filler, an organic filler or a plasticizer with a solvent to form a microporous structure. And a film obtained by stretching a film made of a polyolefin resin containing an inorganic filler or an organic filler in at least one axial direction.

Among these, a film obtained by stretching a film made of a polyolefin resin containing an inorganic filler or an organic filler described below in at least one axial direction is preferably used. Examples of the polyolefin resin used in the present invention include high-density polyethylene, medium-density polyethylene, ethylene-α-olefin copolymer, high-pressure low-density branched polyethylene, polypropylene, and copolymers of propylene and other olefins or these. For example, a mixture of polyolefins. Among them, polyethylene resin is preferable.

As the filler contained in the polyolefin resin, an inorganic or organic filler is used, for example, calcium carbonate, talc, clay, kaolin, silica, diatomaceous earth, magnesium carbonate, barium carbonate, barium sulfate, calcium sulfate. , Calcium sulfite, calcium hydroxide, magnesium hydroxide, aluminum hydroxide,
Inorganic fillers such as zinc oxide, calcium oxide, magnesium oxide, titanium oxide, mica, alumina, zeolite and glass powder, and organic fillers such as wood powder, cellulose powder, high melting point resin powder and crosslinked resin powder are used.

The average particle size of these fillers is usually 30 μm or less, preferably 0.2 to 10 μm. Here, if the particle size is too small, the dispersibility and moldability are inferior, and if it is too large, the denseness of the micropores of the stretched film may deteriorate, the moisture permeability may become too high, and the uniformity may deteriorate. If necessary, a plurality of these may be contained. Further, these fillers may be surface-treated with a fatty acid or a fatty acid metal salt in order to improve dispersibility in the polyolefin resin and stretchability of the film.

Further, if necessary, other resins, elastomers and various additives commonly used in the filler-containing polyolefin resin film can be blended. For example, ethylene-propylene copolymer elastomer, liquid or solid hydrocarbon resin, active hydrogen-containing liquid polybutadiene, plasticizer, radical generator, heat stabilizer, ultraviolet absorber, higher fatty acid, its ester, its amide, its metal. Examples thereof include lubricants such as salts, colorants, flame retardants and the like.

The polyolefin resin is pelletized by using a Banbury mixer, a kneading extrusion molding machine and the like together with a predetermined amount of filler and various additives. The pellets are used to form a film using a T-die extrusion molding machine and an inflation molding machine. The formed film is stretched at least uniaxially by about 1.5 to 10 times. Stretching may be performed in multiple stages, or may be biaxially stretched.

The stretching of the film is carried out, for example, in a temperature range of 100 ° C. lower than the melting point of the polyolefin resin to 20 ° C. lower than the melting point. By this stretching, the strength of the film is improved and the microporosity is formed. By heat-treating this stretched film, the dimensional accuracy of the film can be improved. Further, the laminated surface of the film may be subjected to surface treatment such as corona treatment or frame treatment for improving adhesiveness.

The moisture permeability of the moisture permeable film can be appropriately selected according to the kind of the drug, for example, 300 to 100.
Practically preferred is 00 g / cm ² · 24 hours. Also,
As a method of measuring the moisture permeability, a method based on JIS L1099 can be adopted.

As the material of the coat layer, a material containing a water-soluble acrylic resin and polyalkyleneimine can be adopted. The water-soluble acrylic resin is preferably a water-soluble acrylic resin containing a polymer composed of unsaturated carboxylic acid. Here, as the unsaturated carboxylic acid, acrylic acid, methacrylic acid, itaconic acid, maleic acid, fumaric acid and the like can be adopted, but acrylic acid and / or methacrylic acid are preferable. Incidentally, the water-soluble acrylic resin is a polymer containing the unsaturated carboxylic acid, the carboxyl group in the polymer is alkyl esterified,
Alternatively, it refers to a resin neutralized with a base and solubilized in water.

As the polyalkyleneimine, polyethyleneimine, polypropyleneimine and the like can be adopted, but polyethyleneimine is preferable. As the polyethyleneimine, ethyleneimine homopolymer, modified polymer, graft copolymer and the like can be used. According to this, since it is the coat layer containing the water-soluble acrylic resin and the polyalkyleneimine, the adhesiveness between the moisture-permeable film and the transdermal drug can be improved.

As the coating method of the coat layer, known methods such as gravure coating, Meyer bar coating, doctor blade coating, reverse roll coating, air knife coating, calendar coating, skies coating and kiss coating can be adopted. Among these, gravure coating is preferable because it can coat a certain amount and a certain thickness. The thickness of the coat layer is not particularly limited as long as the adhesiveness to the drug can be kept good, and can be set appropriately.

The transdermal drug is not particularly limited as long as it is a drug that can be absorbed through the skin. For example, non-steroidal anti-inflammatory drugs, corticosteroids,
Antihistamines, antipruritics, antihypertensives, anesthetics, antifungals, antiepileptics, coronary vasodilators, hormones, anti-inflammatory /
There are analgesics and topical stimulants. The non-steroidal anti-inflammatory agent, piroxicam, phenylbutazone, acetylsalicylic acid, flufenamic acid, mefenamic acid, ibuprofen, ketoprofen, flurbiprofen,
Examples include sulindac, indomethacin, diclofenac, amphenac, fenbufen, tinolidine, and emorfazone.

Examples of corticosteroids include prednisolone, propionic acid and clobetasol. Antihistamines include diphenhydramine, diphenylimidazole, chlorpheniramine and the like. Antipruritic agents include crotamiton. Antihypertensive agents include clonidine, nifedipine, propranolol and the like.

The anesthetics include lidocaine and benzocaine, the antifungal agents include clotrimazole and pentamycin, and the antiepileptic agents include nitrozepam and meprobamate. Coronary vasodilators include nitroglycerin and isosorbide dinitrate, and hormones include estradiol. Anti-inflammatory / analgesic agents include methyl salicylate, glycol salicylate, glycyrrhizinic acid, glycyrrhetinic acid, borneol, oat powder, berberyl hydrochloride and the like.

As local stimulants, capsicum (powder, extract, tincture), capsaicin, nonyl vanillylamide, turpentine oil, dl-camphor, benzyl nicotinate,
Examples include β-butoxyethyl nicotinate, peppermint oil, l-menthol and eucalyptus oil.

In practice, the above-mentioned transdermal drug is contained in an adhesive or the like and applied on the coat layer. Examples of the adhesive to be contained include (meth) acrylic acid alkyl ester (co) polymers; rubber-based polymers such as styrene-isoprene-styrene block copolymers, styrene-butadiene rubber, polybutene, polyisobrene, butyl rubber and natural rubber; And silicone-based polymers.

Examples of the monomer capable of forming the (meth) acrylic acid alkyl ester (co) polymer include (meth)
Examples thereof include alkyl acrylates and polymerizable monomers copolymerizable therewith. As the (meth) acrylic acid alkyl ester, a (meth) acrylic acid alkyl ester having an alkyl group having 1 to 18 carbon atoms is used, which includes methyl (meth) acrylate, ethyl (meth) acrylate, and butyl (meth) acrylate. , 2-ethylhexyl (meth) acrylate, dodecyl (meth) acrylate and the like.

As the above-mentioned polymerizable monomer, (meth) acrylic acid, vinylpyrrolidone, diacetone acrylamide, (poly) ethylene glycol (meth) acrylate, (poly) propylene glycol (meth) acrylate, 2-hydroxyethyl ( (Meth) acrylate, vinyl acetate styrene, etc. The (meth) acrylic acid alkyl ester (co) polymer is prepared by a usual method such as solution polymerization or bulk polymerization. The above rubber-based adhesive includes
Tackifiers, liquid rubbers, softeners, etc. are added as necessary.

The skin patch of the present invention is a skin patch prepared by applying a transdermal drug to a transdermal drug base fabric, wherein the transdermal drug base fabric is water-soluble on a moisture-permeable film made of polyurethane. It is characterized in that it comprises a coat layer composed of a water-soluble acrylic resin and polyalkyleneimine. According to the present invention as described above, the transdermal drug base fabric is composed of a coating layer containing a water-soluble acrylic resin and polyalkyleneimine on a moisture-permeable film made of polyurethane.・ The effect can be obtained.

[0030]

BEST MODE FOR CARRYING OUT THE INVENTION Embodiments of the present invention will be described below with reference to the drawings. FIG. 1 shows a skin patch 1 according to an embodiment of the present invention. The skin patch 1 comprises a base fabric 10 for transdermal drug and a drug coating layer 20. The base fabric 10 for transdermal drug is a moisture permeable film 11
And a coat layer 12 laminated on the surface of the base material layer 11,
It is configured with. The drug coating layer 20 is the coat layer 12
Formed on the side.

The moisture permeable film 11 is composed of polyurethane obtained by chain extension, if necessary, by a usual reaction between diisocyanate and polyol. The coat layer 12 is configured to contain a water-soluble acrylic resin and polyalkyleneimine. The coating with the coat layer 12 uses a gravure coater. The drug coating layer 20 is a drug that can be absorbed through the skin,
It is composed of a non-steroidal anti-inflammatory drug used in the case of muscle pain or joint pain.

The skin patch 1 is produced by the following procedure. First, a composition that contains a water-soluble acrylic resin and polyalkyleneimine is coated on a polyurethane sheet that will be the base material layer 11 using a gravure coater. Then, the coating composition is formed by drying the contained composition for a predetermined temperature and time. Further, a non-steroidal anti-inflammatory drug, which is a transdermal drug, containing an adhesive such as a rubber polymer is applied on the coat layer 12 in a predetermined amount to a predetermined thickness to form the drug coating layer 20. .

The skin patch 1 of this embodiment is attached to the back part of the neck as shown in FIG. 2 (A) so that the drug coating layer 20 comes into contact with the skin, or as shown in FIG. As shown in B), it is used by being attached to the inner part of the elbow.

According to this embodiment as described above, the following effects can be obtained. (1) The base fabric 10 for transdermal drug comprises a moisture permeable film 11 and
And a coat layer 12, and the coat layer 12 comprises
By including a water-soluble acrylic resin and polyalkyleneimine, the cooling effect of the transdermal drug and the medicinal component are maintained for a long time, and the adhesiveness with the drug coating layer 20 containing the transdermal drug is improved. be able to. (2) Since the base material layer 11 is made of polyurethane, the skin patch 1 having elasticity and strength, and good abrasion resistance, oil resistance, and adhesiveness can be obtained. Further, since polyurethane has elasticity, it can be used as the skin patch 1 that deforms in response to body movements.

The present invention is not limited to the above-mentioned embodiments, and modifications and improvements within the range in which the object of the present invention can be achieved are included in the present invention. For example, although the moisture permeable film 11 is made of polyurethane in the above embodiment, the moisture permeable film 11 is not limited to this, and a polyolefin resin, for example, a microporous film such as polyethylene or polypropylene is used. Can be adopted.

As a method of forming the coat layer 12, gravure coating was adopted in the above embodiment,
Not limited to this, Meyer bar coating, doctor blade coating, reverse roll coating,
Air knife coating, calendar coating,
Known methods such as squeeze coating and kiss coating can be adopted.

Although the drug coating layer 20 is configured to contain a non-steroidal anti-inflammatory agent in the above-mentioned embodiment, the drug coating layer 20 is not limited to this. Corticosteroids, antihistamines, antipruritic agents, antihypertensive agents, Anesthesia agents, antifungal agents, antiepileptic agents, coronary vasodilators, hormones, antiphlogistic / analgesics and local stimulants can be adopted. In addition, the specific structure, shape, and the like when carrying out the present invention may be other structures and the like as long as the object of the present invention can be achieved.

[0038]

EXAMPLES The present invention will be described more specifically below with reference to examples and comparative examples. The present invention is not limited to the contents of the embodiment. In the above embodiment, the skin patch 1 was produced under the following specific conditions.

[Example 1] [1] Moisture permeable film 11 Moisture permeable urethane (thickness 40 μm) coat layer 12 Water-soluble acrylic resin and polyalkyleneimine-containing composition (Idemitsu Protein Coat FG 501) [2] Coat layer 12 The coating layer 12 was formed on the moisture-permeable film 11 by gravure coating with a gravure coater at a dry base of 0.0075 g / m ² and dried at 80 ° C. for 30 seconds. [3] Formation of drug coating layer 20 After the coating layer 12 is formed, a non-steroidal anti-inflammatory drug that is a transdermal drug containing a pressure sensitive adhesive such as a rubber polymer is applied to form the drug coating layer 20. It is formed.

Example 2 [1] Moisture Permeable Film 11 Moisture Permeable Polyethylene (Thickness 32 μm) Coat Layer 12 Similar to Example 1, the moisture permeable polyethylene is a film made of a polyethylene resin containing an inorganic filler. It is a film obtained by uniaxially stretching. [2] Formation of coat layer 12 The same procedure as in Example 1 was carried out. [3] Formation of Drug Coating Layer 20 The same procedure as in Example 1 was carried out.

[0041] [2] No formation of coat layer 12 [3] Formation of drug coating layer 20 A non-steroidal anti-inflammatory drug which is a transdermal drug containing an adhesive such as a rubber polymer on the moisture-permeable film 11. By coating, the drug coating layer 20 is formed.

[0042] [2] No formation of coat layer 12 [3] Formation of drug coating layer 20 The procedure of Comparative Example 1 was repeated.

In each of the examples and comparative examples described above, the moisture permeability of the moisture permeable film 11 alone or after the formation of the coat layer 12 was measured by the method according to JIS L1099. The adhesiveness with the transdermal drug forming the drug coating layer 20 was evaluated by a practical evaluation in which the drug was applied to the skin and peeled off. Table 1 shows the above measurement conditions and evaluation results.

[0044]

[Table 1]

Comparing Examples 1 and 2 with Comparative Examples 1 and 2, it can be seen that Examples 1 and 2 have good adhesiveness to a transdermal drug.

[0046]

EFFECTS OF THE INVENTION According to the present invention, a translucent drug is constituted by comprising a moisture permeable film and a coat layer, and the coat layer comprises a water-soluble acrylic resin and polyalkyleneimine. It is possible to maintain the cooling effect and the medicinal component for a long time and improve the adhesiveness with the transdermal drug.

[Brief description of drawings]

FIG. 1 is a diagram showing a skin patch of one embodiment of the present invention.

FIG. 2 is a diagram showing a usage example of the skin patch in the embodiment of FIG.

[Explanation of symbols]

1 skin patch 10 Transdermal drug base fabric 11 Breathable film 12 coat layer 20 Drug coating layer

Claims (3)

[Claims] 1. A transdermal drug base fabric to which a transdermal drug is applied, comprising a moisture-permeable film and a coat layer laminated on the moisture-permeable film on the side to which the transdermal drug is applied. The base layer for a transdermal drug, characterized in that the coating layer comprises a water-soluble acrylic resin and a polyalkyleneimine. 2. The base fabric for a transdermal drug according to claim 1, wherein the moisture-permeable film is made of polyurethane. 3. A skin patch in which a transdermal drug is applied to a transdermal drug base fabric, wherein the transdermal drug base fabric is made of polyurethane and a water-soluble acrylic resin and polyalkyleneimine are formed on a moisture-permeable film. A skin patch comprising a coat layer containing: