JP2006045101A - Volatilization suppressing agent, volatile component-containing composition and patch - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a volatilization suppressing agent capable of suppressing volatilization of volatile components, and a volatile component-containing composition, a self-adhesive layer composition, and a patch capable of suppressing volatilization of the volatile components by utilizing the volatilization suppressing agent. <P>SOLUTION: In the patch 1 comprising a support 2, a self-adhesive layer 3 laminated on the back surface of the support 2 and a protective sheet 4 for protecting the self-adhesive layer 3, the self-adhesive layer composition constituting the self-adhesive layer 3 is caused to contain a medicine, the volatilization suppressing agent and a self-adhesive base agent. The volatilization suppressing agent is caused to contain a polyhydric alcohol, a nonionic surfactant, and when required, a filler having an average particle size of 0.1-50 μm. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

  The present invention mainly relates to a patch, a volatilization inhibitor that can be used in the patch, a volatile component-containing composition, and a composition for an adhesive layer.

  Usually, the adhesive layer of anti-inflammatory analgesic patches contains anti-inflammatory analgesics such as methyl salicylate and l-menthol. However, since these drugs are volatile, there is a problem that the duration of medicinal effects is short. It was.

To solve this problem, a film is laminated on the support of the anti-inflammatory analgesic patch, or a primer treatment is applied to the support to physically suppress the volatilization of the drug, or the drug is encapsulated in a microcapsule. (Patent Document 1) and the like.
Japanese Patent No. 3192494

  However, when a film is laminated on a support, there is a problem that the stretchability of the support is lost or the stress relaxation property is lowered, resulting in an uncomfortable feeling during use. Moreover, when performing a primer process, the one where the elasticity of a support body is low is preferable, As a result, a strange feeling will arise at the time of use similarly to the above.

  On the other hand, according to the method of encapsulating a drug in a microcapsule, the stretchability of the support can be maintained. However, the microcapsule itself is the heat at the time of forming the adhesive layer (during drying) or the release paper as a protective sheet. Or the pressure at the time of pasting with a release film may cause destruction of the drug.

  The present invention has been made in view of such a situation, and suppresses volatilization of a volatile component by using a volatilization inhibitor capable of suppressing volatilization of a volatile component and such a volatilization inhibitor. An object of the present invention is to provide a volatile component-containing composition, an adhesive layer composition, and a patch that can be used.

  In order to achieve the above object, first, the present invention provides a volatilization inhibitor comprising a polyhydric alcohol and a nonionic surfactant (claim 1).

  According to the said invention (invention 1), volatilization of the component which has volatility can be suppressed, and a volatile component can be released gradually.

  The volatilization inhibitor according to the invention (Invention 1) preferably further contains a filler having an average particle size of 0.1 to 50 μm (Invention 2).

  According to the said invention (invention 2), the volatilization inhibitory effect of a volatile component becomes further excellent.

  In the above inventions (Inventions 1 and 2), the polyhydric alcohol is preferably a polyalkylene glycol (Invention 3). In the above invention (Inventions 1 to 3), the nonionic surfactant is preferably a sorbitan fatty acid ester (Invention 4), and the sorbitan fatty acid ester is sorbitan monostearate. Preferred (claim 5).

  2ndly, this invention provides the component which has volatility, and the said volatilization inhibitor (Claims 1-5), The volatile component containing composition characterized by the above-mentioned (Claim 6) is provided.

  In the said invention (invention 6), the volatilization inhibitor can suppress volatilization of the component which has volatility, and can release a volatile component gradually.

  In the above invention (invention 6), the volatile component may be a transdermal drug (invention 7) or an anti-inflammatory analgesic (invention 8).

  According to the above inventions (Inventions 7 and 8), the persistence of the drug efficacy can be prolonged. In addition, the component which has volatility in this invention is not limited to a chemical | medical agent, For example, a fragrance | flavor, a deodorant, a disinfectant, an antibacterial agent, an insecticide, an insecticide, an organic solvent etc. may be sufficient.

  3rdly, this invention provides the adhesion layer composition characterized by including the chemical | medical agent which has volatility, the volatilization inhibitor in any one of Claims 1-5, and an adhesive base ( Claim 9).

  According to the said invention (invention 9), since volatilization of the volatile chemical | medical agent can be suppressed and a volatile chemical | medical agent can be released gradually, the sustainability of a medicinal effect can be lengthened.

  In the said invention (invention 9), the said adhesive base may contain an ABA type | mold block copolymer and a tackifier (invention 10). Such an adhesive base is preferable from the viewpoint of transdermal absorbability when the drug is a transdermally absorbable drug.

  Fourthly, the present invention provides a patch comprising a support and an adhesive layer containing the adhesive layer composition according to claim 9 or 10 formed on the support. (Claim 11).

  According to the said invention (invention 11), since volatilization of a volatile chemical | medical agent can be suppressed and a volatile chemical | medical agent can be released gradually, the sustainability of a medicinal effect can be lengthened.

  In the above invention (invention 11), the support may be made of a stretchable material (invention 12). In this invention (invention 12), in order to suppress the volatilization of the drug, the conventional film lamination or primer treatment on the support is not required, so the stretchability of the support is not inhibited.

  According to the volatilization inhibitor and the volatile component-containing composition of the present invention, volatilization of the volatile component can be suppressed and the volatile component can be released gradually. Moreover, according to the adhesive layer composition and the patch of the present invention, volatilization of the volatile drug can be suppressed and the volatile drug can be released gradually, so that the persistence of the drug effect can be prolonged. And since the film lamination and primer treatment to a support body like the past are not required, even if a support body has a stretching property, the stretching property is not inhibited.

Hereinafter, embodiments of the present invention will be described.
FIG. 1 is a cross-sectional view of a patch according to an embodiment of the present invention.

  As shown in FIG. 1, the patch 1 according to the present embodiment includes a support 2, an adhesive layer 3 laminated on the back side of the support 2, and a protective sheet 4 that protects the adhesive layer 3. The However, the protective sheet 4 is peeled off when the patch 1 is used.

  The adhesion layer 3 in this embodiment consists of a composition containing a volatile chemical | medical agent, a volatilization inhibitor, and an adhesive base. When the patch 1 according to this embodiment is for transdermal administration, for example, a drug such as an anti-inflammatory analgesic or a skin stimulant is selected as the volatile drug. Examples of anti-inflammatory analgesics include salicylic acid drugs such as methyl salicylate and glycol salicylate. Examples of skin stimulants include terpene drugs such as menthol and camphor, and these drugs are volatile. Have

  The content of the drug in the adhesive layer composition varies depending on the type of drug and the dose based thereon, but is usually preferably 0.5 to 15% by mass, and particularly preferably 1 to 12% by mass. If the content of the drug is too small, the desired medicinal effect cannot be obtained, and if the content of the drug is too large, there may be a problem of side effects.

  The volatilization inhibitor contains a polyhydric alcohol, a nonionic surfactant, and optionally a filler. The polyhydric alcohol means an organic compound having two or more hydroxyl groups in the molecule. For example, trihydric alcohols such as glycerin, pentahydric alcohols such as arabitol, xylitol and adonitol, hexavalent alcohols such as sorbitol and annitol. Further, alkylene glycols such as ethylene glycol, propylene glycol, and 1,3-butylene glycol, and polyalkylene glycols such as polyethylene glycol and polypropylene glycol can be used.

  Among the polyhydric alcohols, polyalkylene glycols, particularly polyethylene glycol are preferable. The number average molecular weight of polyethylene glycol is preferably 1,000 to 100,000, particularly preferably 2,500 to 50,000. The solidification temperature of polyethylene glycol is preferably 25 ° C. or higher, and particularly preferably 30 to 60 ° C. When the solidification temperature of polyethylene glycol is 25 ° C. or higher, polyethylene glycol becomes solid at room temperature, and bleeding from the adhesive layer can be suppressed.

  The content of the polyhydric alcohol in the adhesive layer composition is preferably 0.1 to 5.0% by mass, and particularly preferably 0.2 to 3.0% by mass. If the content of the polyhydric alcohol is less than 0.2% by mass, the volatilization suppressing action is not sufficient, and if the content of the polyhydric alcohol exceeds 5.0% by mass, the adhesive strength of the adhesive layer may be reduced. .

  Nonionic surfactants include, for example, propylene glycol fatty acid esters, sorbitan fatty acid esters, polyethylene glycol fatty acid esters, and the like, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbitol fatty acid esters, polyoxyethylene castor oil, polyoxyethylene castor oil, Oxyethylene hydrogenated castor oil, ether ester type such as polyoxyethylene glycerin fatty acid ester, polyoxyethylene alkyl ether and its phosphate, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene alkylphenyl ether, polyoxyethylene lanolin alcohol Among them, ester type, particularly sorbitan fatty acid ester is preferable.

  Examples of sorbitan fatty acid esters include sorbitan monooleate, sorbitan monostearate, sorbitan sesquioleate, sorbitan coconut oil fatty acid sorbitan, sorbitan monopalmitate, sorbitan tristearate, sorbitan trioleate, polyoxyethylene sorbitan monolaurate, Examples include polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan tristearate, polyoxyethylene sorbitan trioleate, polyoxyethylene sorbitan triisostearate Among them, sorbitan monostearate is particularly preferable.

  The content of the nonionic surfactant in the pressure-sensitive adhesive layer composition is preferably 1 to 10% by mass, and particularly preferably 1.5 to 8% by mass. When the content of the nonionic surfactant is less than 1% by mass, the volatilization suppressing action is not sufficient, and when the content of the nonionic surfactant exceeds 10% by mass, the adhesive strength of the adhesive layer is reduced. There is.

  Examples of the filler include zinc white, titanium oxide, silica, calcium carbonate, aluminum hydroxide, barium sulfate, clay, and talc. The average particle size of these fillers is preferably from 0.1 to 50 μm, particularly preferably from 0.5 to 35 μm. When the average particle diameter of the filler exceeds 50 μm, the dispersion of the adhesive layer composition may be insufficient, or clogging may occur during coating. Further, when the average particle size of the filler is less than 0.1 μm, secondary aggregation is likely to occur when the adhesive layer composition is stirred and mixed, and as a result, the apparent particle size may increase.

  When using a filler, the content of the filler in the adhesive layer composition is preferably 0.5 to 20% by mass, particularly preferably 1 to 15% by mass. If the content of the filler is less than 0.5% by mass, it is difficult to sufficiently improve the volatilization suppressing action, and if the content of the filler exceeds 20% by mass, the adhesive strength of the adhesive layer may be reduced. .

  As the adhesive base, rubber adhesives, acrylic adhesives, silicone adhesives and the like can be generally used. However, when the drug is a transdermal drug, the transdermal absorbability is used. From this point of view, it is preferable to use a rubber-based pressure-sensitive adhesive. The rubber-based pressure-sensitive adhesive is composed of an ABA block copolymer as a rubber elastic component, a tackifier, a softener for improving the sticking feeling as required, and an antioxidant for preventing deterioration. It is preferable to contain an agent.

  Examples of the ABA type block copolymer include styrene-isoprene-styrene copolymer, styrene-butylene-styrene copolymer, styrene-ethylene-butylene-styrene copolymer, styrene-olefin-styrene copolymer. Examples thereof include a polymer, polyisoprene, polybutene, and polyisobutylene.

  The content of the rubber elastic component in the rubber-based pressure-sensitive adhesive is preferably 5 to 50% by mass, and particularly preferably 7 to 45% by mass. When the content of the rubber elastic component is less than 5% by mass, the cohesive force of the adhesive layer composition decreases, and when the content of the rubber elastic component exceeds 45% by mass, the adhesive force of the adhesive layer may be too low. There is.

  Examples of the tackifier include rosin resins, polyterpene resins, coumarone / indene resins, petroleum resins, terpene phenol resins, alkylphenol resins, styrene resins, phenol resins, xylene resins, and the like.

  The content of the tackifier in the rubber-based pressure-sensitive adhesive is preferably 10 to 70% by mass, and particularly preferably 15 to 60% by mass. When the content of the tackifier is less than 10% by mass, the adhesive strength of the adhesive layer decreases, and when the content of the tackifier exceeds 70% by mass, the cohesive force of the adhesive layer composition may be too low. There is.

  Examples of the softener include light liquid paraffin, liquid paraffin, liquid polybutene, mineral oil, lanolin, liquid polyisoprene, hexamethyltetracosane, hexamethyltetracosahexane, α-olefin oligomer, castor oil, olive oil, peanut oil, palm Oil, coconut oil, medium chain fatty acid glyceride, isopropyl palmitate and the like.

  When the softener is used, the content of the softener in the rubber-based pressure-sensitive adhesive is preferably 5 to 70% by mass, and particularly preferably 8 to 60% by mass. If the content of the softening agent is less than 5% by mass, the adhesive force of the adhesive layer becomes too high, and if the content of the softening agent exceeds 70% by mass, the cohesive force of the adhesive layer composition may become too low. There is.

  Examples of the antioxidant include butylhydroxytoluene, 2,6-di-t-butyl-4-methylphenol, 2,5-di-t-butylhydroquinone, mercaptobenzimidazole, 1,1-bis (4- Hydroxyphenol) cyclohexane, phenyl-β-naphthylamine and the like.

  When using an antioxidant, the content of antioxidant in the rubber-based pressure-sensitive adhesive is preferably 0.1 to 10% by mass, and particularly preferably 0.2 to 5% by mass. When the content of the antioxidant is less than 0.1% by mass, the stability of the adhesive layer composition is deteriorated, and when the content of the antioxidant exceeds 10% by mass, the skin may be stimulated.

  The pressure-sensitive adhesive base in the pressure-sensitive adhesive layer composition is preferably the remainder other than the above-mentioned chemicals and volatilization inhibitors, and other additives that can be contained in the pressure-sensitive adhesive layer composition (for example, preservatives, ultraviolet absorbers, etc.). .

  The thickness of the pressure-sensitive adhesive layer 3 may be appropriately selected according to the purpose and site of use of the patch, the type of the drug, etc., but it is usually preferably 20 to 1000 μm, particularly 30 to 300 μm. preferable.

  The support 2 is preferably made of a material having flexibility and shrinkage in consideration of followability to the applied skin, but is not limited to such a material. A preferred material for the support 2 is a stretchable woven fabric, and conventionally known materials can be used.

  The thickness of the support 2 may be appropriately selected according to the purpose and site of use of the patch, the kind of the drug, etc., but it is usually preferably 10 to 1000 μm, particularly 20 to 800 μm. preferable.

  As the protective sheet 4, a conventionally known release paper or release film in which the surface on the pressure-sensitive adhesive layer 3 side is subjected to release treatment with a silicone release agent or the like can be used.

  In order to produce the patch 1, for example, by the hot melt method, the adhesive layer composition is applied to the release treatment surface of the protective sheet 4 with a coating machine such as a die coater, a knife coater, or a roll coater, and cooled. What is necessary is just to bond the support body 2 to the formed adhesion layer 3. FIG.

  In the patch 1 described above, a volatilization inhibitor containing a polyhydric alcohol, a nonionic surfactant, and optionally a filler can suppress the volatilization of the drug and allow the drug to be released slowly. Can be prolonged. And since the film lamination and primer treatment to a support body like the past are not required, even if the support body 2 has a stretching property, the stretching property is not inhibited.

  In addition, although this embodiment demonstrated the patch 1 provided with the adhesion layer 3 containing a chemical | medical agent, this invention is not limited to this, A fragrance | flavor, a deodorizing agent, a disinfectant, an antibacterial instead of a chemical | medical agent Volatile components such as agents, insect repellents, insecticides, and organic solvents may be used. Moreover, the composition containing the chemical | medical agent and volatilization inhibitor in this embodiment does not necessarily need to be used for the patch 1, and may be used as a cream or lotion, for example. In this case, the composition may include a third component as necessary.

  EXAMPLES Hereinafter, although an Example etc. demonstrate this invention further more concretely, the scope of the present invention is not limited to these Examples etc.

[Examples 1-5, Comparative Examples 1-2]
100 parts by mass of a polyterpene resin (Yasuhara Chemical Co., Ltd., YS Resin PX1150), 100 parts by mass of a styrene-isoprene-styrene copolymer (Kuraton Polymer Co., Ltd., KRATOND-1107), and liquid paraffin (Sanko Chemical Co., Ltd., 350- S) 40 parts by mass were melted and mixed under heating at 160 ° C. to obtain an adhesive base.

  To the obtained adhesive base, methyl salicylate (manufactured by Kanto Chemical Co., Inc.) as a drug, polyethylene glycol (PEG) 4000 (manufactured by Kanto Chemical Co., Ltd., number average molecular weight: 2700-3400, freezing point: 53-57 ° C.), Sorbitan monostearate (manufactured by Kao Corporation) and silica (manufactured by Tokai Mineral Co., Ltd., ES-D25, average particle size: 25 μm) are added at a blending ratio (mass basis) shown in Table 1 and uniformly dispersed. Until stirred.

The obtained adhesive layer composition was subjected to a release treatment with a 75 μm-thick polyethylene terephthalate release film (SP-PET7501, manufactured by Lintec Co., Ltd.) with a silicone-based release agent. The spread coating was carried out so as to be 100 μm. And the support body which consists of a polyester woven fabric of 103 g / m < ² > of fabric weights was bonded together to the adhesive layer formed in this way, and the patch was obtained.

[Test example]
The patches obtained in Examples and Comparative Examples were cut into 50 mm × 50 mm, the release film was peeled off and the exposed adhesive layer was placed on the upper side, and left at room temperature for 2 hours. The drug content in the subsequent adhesive layer was measured using liquid chromatography (measuring device: LC-10A manufactured by Shimadzu Corporation, mobile phase: methanol / water = 60/40, column: ODS), and the initial content was measured. The ratio of the drug content after standing for 2 hours to the drug content was calculated as the residual rate. The results are shown in Table 1.

  From Table 1, it was found that in the patches obtained in the examples, a remarkably large amount of the drug remained as compared with the patches obtained in the comparative examples.

  The present invention can be preferably used for a patch in which an adhesive layer contains a volatile drug such as an anti-inflammatory analgesic.

It is sectional drawing of the patch which concerns on one Embodiment of this invention.

Explanation of symbols

DESCRIPTION OF SYMBOLS 1 ... Patch 2 ... Support body 3 ... Adhesive layer 4 ... Protective sheet

Claims (12)

  A volatilization inhibitor comprising a polyhydric alcohol and a nonionic surfactant.   The volatilization inhibitor according to claim 1, further comprising a filler having an average particle size of 0.1 to 50 µm.   The volatilization inhibitor according to claim 1 or 2, wherein the polyhydric alcohol is polyalkylene glycol.   The volatilization inhibitor according to any one of claims 1 to 3, wherein the nonionic surfactant is a sorbitan fatty acid ester.   The volatilization inhibitor according to claim 4, wherein the sorbitan fatty acid ester is sorbitan monostearate.   A volatile component-containing composition comprising a component having volatility and the volatilization inhibitor according to claim 1.   The volatile component-containing composition according to claim 6, wherein the volatile component is a transdermally absorbable drug.   The volatile component-containing composition according to claim 6, wherein the volatile component is an anti-inflammatory analgesic.   A pressure-sensitive adhesive layer composition comprising: a volatile drug; the volatilization inhibitor according to claim 1; and a pressure-sensitive adhesive base.   The pressure-sensitive adhesive layer composition according to claim 9, wherein the pressure-sensitive adhesive base contains an ABA type block copolymer and a tackifier.   A patch comprising: a support; and an adhesive layer containing the adhesive layer composition according to claim 9 or 10 formed on the support. The patch according to claim 11, wherein the support is made of a stretchable material.

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