JPH06142178A - Tape agent and tape preparation having decreased stimulus on skin - Google Patents

Abstract

PURPOSE:To provide the tape agent and tape prepn. which hardly generate moistening, a rash, itching, etc., by sweating from the skin surface in spite of patching on the skin surface over a long time and produces decreased stimulus on the skin surface. CONSTITUTION:A tacky adhesive layer is formed on at least one surface of a porous supporting base having 40 to 98% pore volume regulated in JIS (Japanese Industrial Standards) L-1096. A porous supporting base having <=100mm stiffness and softness (45 deg. cantilever method) is preferably adopted for the layer in terms of flexibility, the flow-up characteristic to the skin and the stimulativeness to the skin. The tape prepn. for treatment and prevention of diseases is obtd. by incorporating a drug for percutaneous absorption into the tacky adhesive layer.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a tape preparation to be used by being stuck on the skin surface and a tape preparation containing a drug for percutaneous absorption. More specifically, the anchoring property between the adhesive layer and the support is good, Moreover, the present invention relates to a tape preparation and a tape preparation having little skin irritation, which hardly causes skin irritation such as stuffiness or rash on the skin surface when applied to the skin surface for a long time.

[0002]

2. Description of the Related Art As a tape agent to be applied to the skin surface, a tape agent for covering used for protecting the skin surface,
It is used in various applications such as tape preparations used to transdermally administer drugs for transdermal administration.However, since the patch surface is the skin surface, the development of the patch is easy to handle and skin. In addition to the ability to follow the movement of the surface (flexibility), non-irritancy to the skin is required. In particular, since these tapes may be applied for a relatively long time, it is an important required property that they do not give a feeling of discomfort or irritation to the skin after being applied to the skin surface.

In order to meet such demands, there has conventionally been proposed a tape preparation in which the thickness of the support is made as thin as possible to reduce the skin irritation caused by the edge portion of the support and further the skin followability is imparted. There is. However, when the thickness of the support is reduced, the above-mentioned required characteristics are satisfied, but the tape agent itself loses its self-supporting property, resulting in poor handleability at the time of application and wrinkling of the tape agent after application,
In addition, there is a problem in that the adhesive surfaces are stuck to each other at the time of application and cannot be applied neatly.

Further, when applied to the skin surface for a long time, since the skin surface is covered, sweating or the like causes the application surface to become stuffy, resulting in itching or rash and sometimes sickness.

Therefore, as a method for solving the above problem,
Various tapes and tape preparations have been proposed that use a porous sheet made of open cells or a cloth base material such as a non-woven fabric or a woven fabric as a support, while maintaining a proper self-supporting property while also providing air permeability. There is.

When a porous sheet of open cells is used as a support, only the aperture ratio on the surface of the support is usually regarded as a problem, but when the support has a large thickness, sufficient air permeability is obtained. However, it is necessary to consider the influence of the thickness of the support in order to prevent the sticking skin surface from getting stuffy. Also, when a cloth substrate such as a non-woven fabric is used as a support, only the weight of the cloth substrate in a certain area, that is, the so-called basis weight (basis weight) is only discussed. Also has a great effect.

[0007]

Therefore, the present inventors have repeatedly studied the relationship between the thickness of the support and the skin irritation such as stuffiness in a porous support such as an open-cell body or a cloth substrate. As a result, they have found that the pore volume in consideration of the thickness factor, not just the aperture ratio, has a correlation with the skin irritation, and have completed the present invention.

[0008]

SUMMARY OF THE INVENTION That is, the present invention is based on JISL.
The present invention provides a tape preparation having a low skin irritation, which is obtained by laminating an adhesive layer on at least one surface of a porous support having a pore volume of 40 to 98% specified in 1096. From the viewpoint of the balance of properties, a tape preparation in which the bending resistance of the porous support (according to the 45-degree cantilever method specified in JIS L-1096) is 100 mm or less is preferable.

Further, the present invention also provides a tape preparation containing a drug for percutaneous absorption in the adhesive layer of the above tape preparation.

The tape agent of the present invention is characterized by a support for laminating and supporting an adhesive layer on at least one side,
Its pore volume is 40-98%, preferably 50-95%
The one having the value of is used. The "pore volume" in the present invention refers to the pore volume specified in JIS L-1096, and is a value calculated by the following formula, which is different from the so-called porosity and opening rate.

[0011]

[Equation 1]

In the tape preparation of the present invention, the pore volume is adjusted to the above-mentioned range, and in order to reduce skin irritation, the air permeability (according to the A method defined in JIS L-1096) of the porous support is ³ to 500 cm ³ / cm ² / sec, preferably 5 to 400 cm ³ / cm ² / sec, further 50 to ³
It is preferable to adjust it to be 00 cm ³ / cm ² / sec.

When the pore volume of the porous support is less than 40%, the effect of reducing skin irritation is not sufficient, and when the pore volume exceeds 98%, the pressure-sensitive adhesive from the back surface of the support is Exudation and mechanical strength of the support may be insufficient. Further, when a drug for transdermal absorption is contained in a tape preparation, the drug from the back surface of the support may strike through to cause a decrease in content, which is not preferable.

Further, if the above-mentioned porous support is too rigid, it gives physical irritation to the skin surface in contact with the edge of the support, which is not preferable, and the flexibility of the 45 ° cantilever method defined in JIS L-1096 is not preferable. It is desirable that the value is 100 mm or less, preferably about 20 to 90 mm.

As such a porous support, the material is not limited as long as it satisfies the above-mentioned characteristics.
For example, polyester, nylon (polyamide), saran, polyethylene, polypropylene, polyvinyl chloride,
Those made of polytetrafluoroethylene, polyurethane, rayon, acrylic, vinylon, acetate, triacetate, etc. are adopted. The porous support of the present invention is a film or sheet made of such a material is subjected to a perforating treatment, or an optional foaming agent is added to form a film or sheet to form open cells, and further a polymer for a sheet, It can be obtained by mixing with a liquid component which is incompatible with this and forming it into a sheet, and then stretching or solvent extraction. Alternatively, the polymer powder for a sheet can be made porous by molding it into a sheet at a temperature at which it is not completely melted or fused. It can also be produced by processing fibers of the above materials into a cloth base material such as woven cloth, non-woven cloth, and knitted cloth.

The tape preparation of the present invention comprises an adhesive layer formed on at least one surface of the above-mentioned porous support. As the pressure-sensitive adhesive layer to be formed, an acrylic pressure-sensitive adhesive containing (meth) acrylic acid alkyl ester as a main component, as long as it is a pressure-sensitive adhesive for medical use that does not cause skin irritation to the pressure-sensitive adhesive itself because it contacts the skin surface. Rubber adhesives made of polyisobutylene, polyisoprene, polybutadiene, styrene / isoprene (or butadiene) / styrene block copolymers, vinyl ether adhesives containing vinyl alkyl ether as the main component, and polyorganosiloxane as the main component Any silicone-based pressure-sensitive adhesive or the like can be used. Of these adhesives, 50% by weight of (meth) acrylic acid alkyl ester is used from the viewpoints of quality stability, easy adjustment of adhesive strength, drug release, etc.
The acrylic pressure-sensitive adhesive obtained by the above polymerization can be preferably used. In addition, alkylene glycol and oils and fats, liquid surfactants, plasticizers, fatty acid esters, organic solvents that are compatible with the above-mentioned pressure-sensitive adhesive component to give a soft feeling when attached to the skin surface and further reduce irritation It is preferable to use an adhesive containing 20 to 70% by weight, preferably 40 to 60% by weight of an organic liquid component such as, and optionally subjected to crosslinking treatment to improve cohesive strength.

Since the pressure-sensitive adhesive layer in the present invention is a layer that directly contacts and covers the skin surface, it is preferable to prevent excessive stuffiness during application in order to reduce irritation to the skin. From such a point, the moisture permeability of the adhesive layer (40% by the cup method specified in JIS Z-0208)
It is more preferable to adjust the temperature (at 90 ° C. and 90% RH) to 200 g / m ² · 24 h or more.

Further, the adhesive layer in the present invention may contain a drug for percutaneous absorption to prepare a percutaneous absorption tape preparation for treating or preventing various diseases. As such a drug, any of a local drug and a systemic drug may be used as long as it exerts a pharmacological effect by being transdermally absorbed, and specifically, corticosteroids, analgesic and anti-inflammatory agents, hypnotics. Sedatives, tranquilizers, antihypertensives, antihypertensives, antibiotics, anesthetics, antifungals, vitamins, coronary vasodilators, antihistamines, antitussives, sex hormones, antidepressants, cerebral circulation improvers, antiemetics , Drugs such as antitumor agents and biomedical agents can be used. If necessary, these drugs may
More than one kind can be contained in combination. Further, in order to improve the solubility of the drug for transdermal absorption in the adhesive and the release due to diffusion transfer, the amount of the drug used is 0.4 g or less in 100 ml of water at room temperature. It is preferable to use a fat-soluble drug.

The content of these drugs for percutaneous absorption can be appropriately set according to the drug species and the purpose of administration, but it is usually 1 to 40% by weight, preferably 2 to 30% in the pressure-sensitive adhesive layer.
Approximately wt% is included. If the content is less than 1% by weight, a therapeutically effective amount of drug cannot be expected to be released.
If it exceeds 0% by weight, no further therapeutic effect can be expected, which is economically disadvantageous.

[0020]

As described above, since the tape preparation of the present invention is a tape preparation using a porous support having a specific pore volume, it has a proper self-supporting property at the time of application and has excellent handleability. It also has the effect of significantly improving skin irritation caused by stuffiness after application. Furthermore, in a tape preparation containing a drug for transdermal absorption in an adhesive layer, the drug can exert an expected pharmacological effect by an appropriate occlusive dressing therapy (ODT).

[0021]

EXAMPLES Examples of the present invention will be shown below and will be described more specifically. In the following, parts and% mean parts by weight and% by weight.

Example 1 95 parts of acrylic acid 2-ethylhexyl ester and 5 parts of acrylic acid were copolymerized in ethyl acetate under an inert gas atmosphere to prepare an acrylic pressure-sensitive adhesive solution.

The pressure-sensitive adhesive solution thus obtained was coated and dried on a polyester separator so that the thickness after drying was 40 μm, and the pressure-sensitive adhesive layer (moisture permeability 590 g / m ² ·.
24h) was prepared, and this adhesive layer was used as a support for a porous rayon nonwoven fabric (pore volume: 92%, air permeability: 208 cm).
The tape agent of the present invention was produced by transferring and laminating at ³ / cm ² / sec and a bending resistance of 35 mm).

Example 2 The support used in Example 1 was a porous polyester nonwoven fabric (pore volume 72%, air permeability 204 cm ³ / cm ² / se).
c, bending resistance 48 mm), except that the tape agent of the present invention was produced in the same manner as in Example 1.

Example 3 Solid content 5 of the acrylic pressure-sensitive adhesive solution prepared in Example 1
50 parts of isopropyl myristate was mixed with 0 part of the mixture, and the amount was adjusted to 0.
Add 2 parts ethyl acetoacetate aluminum diisopropylate as a 10% acetylacetone solution,
This was applied on a polyester separator so that the thickness after drying was 60 μm, and dried to form a crosslinked gel-like pressure-sensitive adhesive layer (water vapor transmission rate 500 g / m ² · 24 h), and this pressure-sensitive adhesive layer was supported. Porous rayon nonwoven fabric as a body (pore volume 92%, air permeability 208 cm ³ / cm ² / sec,
The tape agent of the present invention was produced by transferring and laminating to a bending resistance of 35 mm).

Example 4 The support used in Example 3 was a porous polyester nonwoven fabric (pore volume 72%, air permeability 204 cm ³ / cm ² / se).
c, bending resistance 48 mm), except that the tape agent of the present invention was produced in the same manner as in Example 1.

Example 5 The support in Example 1 was replaced with a porous polytetrafluoroethylene sheet (pore volume 54%, air permeability 6.5 cm ³ /
The tape agent of the present invention was produced in the same manner as in Example 1 except that the hardness was changed to cm ² / sec and the bending resistance of 40 mm).

Comparative Example 1 A porous polyurethane sheet (pore volume 38%, air permeability 76 cm ³ / cm ² / se was used as the support in Example 1).
c, bending resistance 28 mm), except that the tape was prepared in the same manner as in Example 1.

Comparative Example 2 The support used in Example 1 was replaced with a porous polyester sheet (pore volume 38%, air permeability 40 cm ³ / cm ² / se).
c, bending resistance 30 mm), except that the tape agent was prepared in the same manner as in Example 1.

Comparative Example 3 The support used in Example 3 was replaced with a porous polyurethane sheet (pore volume 38%, air permeability 76 cm ³ / cm ² / se).
c, bending resistance 28 mm) except that the tape agent was prepared in the same manner as in Example 3.

Example 6 The support used in Example 1 was a porous polyester non-woven fabric (pore volume 76%, air permeability 198 cm ³ / cm ² / se).
c, the bending resistance was 115 mm), and a tape preparation was prepared in the same manner as in Example 1.

Example 7 Styrene / isoprene / styrene block copolymer 10
A rubber-based pressure-sensitive adhesive solution was prepared by dissolving 0 part, 15 parts of polybutene, and 85 parts of a tackifying resin (trade name Alcon P-100, manufactured by Arakawa Industry Co., Ltd.) in toluene.

The pressure-sensitive adhesive solution thus obtained was coated and dried on a polyester separator so that the thickness after drying was 40 μm, and the pressure-sensitive adhesive layer (moisture permeability 172 g / m ² ·.
24h) was prepared, and a porous rayon nonwoven fabric (pore volume 92%, air permeability 208 cm) using this adhesive layer as a support was prepared.
The tape agent of the present invention was produced by transferring and laminating at ³ / cm ² / sec and a bending resistance of 35 mm).

Example 8 Example 8 was repeated except that 20 parts of isosorbide dinitrate was added to 80 parts of the solid content of the pressure-sensitive adhesive in the pressure-sensitive adhesive layer to form a drug-containing pressure-sensitive adhesive layer for transdermal absorption. A tape preparation of the present invention was prepared in the same manner as in Example 1.

Comparative Example 4 The support in Example 8 was replaced with a porous polyurethane sheet (pore volume 38%, air permeability 76 cm ³ / cm ² / se).
c, bending resistance 28 mm) except that the tape preparation was prepared in the same manner as in Example 8.

Comparative Example 5 A polyester sheet having a thickness of 12 μm (pore volume 0%, air permeability 1.9 × 10 ⁻⁷ cm ³ / c) was used as the support in Example 1.
A tape preparation was produced in the same manner as in Example 1 except that m ² / sec and bending resistance of 30 mm) were used.

The following tests were carried out using the tape preparations and tape preparations obtained in the above Examples and Comparative Examples. The results are shown in Table 1.

[Peeling feeling] Each sample cut into a size of 25 cm ² was stuck on the chest of 6 volunteers for 6 hours,
The sticking feeling at that time was evaluated according to the following criteria, and the average value was obtained. 3: Good with no discomfort.

2: There is some discomfort. 1: There is a feeling of strangeness.

[Skin Irritation] Each sample in the above patch feeling test was stuck for 24 hours, peeled off from the skin surface, and the skin surface was observed after 30 minutes, 4 hours, 24 hours, and 48 hours after peeling. The degree of skin irritation was judged based on the Japanese patch test standard, and the average of the scores was calculated.

(-) No reaction, score: 0.0 (±) Light erythema, score: 0.5 (+) Erythema, score of 1.0 (++) Erythema and edema, score: 2.0

[0042]

[Table 1]

 ─────────────────────────────────────────────────── --- Continuation of the front page (72) Inventor Takashi Kinoshita 1-2-1, Shimohozumi, Ibaraki City, Osaka Prefecture Nitto Denko Corporation

Claims (3)

[Claims] 1. A tape preparation having a low skin irritation, which is obtained by laminating an adhesive layer on at least one surface of a porous support having a pore volume of 40 to 98% specified in JIS L-1096. 2. The bending resistance (JISL-10) of the porous support.
100 according to the 45-degree cantilever method specified in 96)
The tape preparation according to claim 1, which has a size of not more than mm. 3. The tape preparation according to claim 1, wherein the adhesive layer contains a drug for percutaneous absorption.