JPH0425931B2 - - Google Patents

Description

BACKGROUND TECHNICAL FIELD OF THE INVENTION The present invention relates to a novel base composition for external use, and more particularly to a base composition for external use that hardens itself to form a film when applied to the skin. This invention relates to the base composition used.

Prior art and its problems Conventionally, as a base composition for external use that forms a film on the skin, water-insoluble film-forming polymers and 2.0
Aqueous emulsions with ~50% by weight of water-soluble film-forming polymers (JP 50-25725) and hydrophilic water-insoluble polymers, high-boiling plasticizers and/or organic solvents of the polymers and aqueous A coating material (Japanese Unexamined Patent Publication No. 55-28918) consisting of a liquid is known.

These base compositions are suitable for topical use on the skin,
Since it forms a continuous film on the skin, it has the advantage that unlike ointments, the applied drug does not contaminate clothing or the like, nor is it rubbed off by them.

However, conventional film-forming bases do not necessarily have sufficient affinity for the skin, and there has been a desire for an external base with better adhesion.

OBJECTS OF THE INVENTION Therefore, the first object of the present invention is to provide an external base composition that has excellent adhesion to the skin and forms a stable film on the skin or wound surface that does not peel off easily.

A second object of the present invention is to provide an external base composition that forms a moisture permeable film.
If the film formed on the skin has moisture permeability, the moisture of sweat will escape to the outside air, so the film will not peel off even if you sweat.

Other objects of the invention will become apparent from the detailed description below.

DETAILED DESCRIPTION OF THE INVENTION In order to achieve the above object, the present invention has the configurations described in the following sections.

(1) A water-soluble film-forming polymer, a water-soluble adhesive polymer that is compatible with the film-forming polymer, and a high-boiling point plasticizer of the film-forming polymer and the adhesive polymer. The film-forming polymer is polyvinyl alcohol with a degree of polymerization of 300 to 2000, and the adhesive polymer is a vinyl pyrrolidone-vinyl acetate copolymer.
A polyhydric alcohol is used as the high-boiling plasticizer, and the weight ratio of the high-boiling plasticizer to the sum of the film-forming polymer and the adhesive polymer is in the range of 10:1 to 1:1. Characteristic external base composition.

(2) The external base composition according to item 1, wherein the vinylpyrrolidone to vinyl acetate ratio of the vinylpyrrolidone-vinyl acetate copolymer is in the range of 1:4 to 4:1.

(3) The external base composition according to item 1, wherein the polyhydric alcohol is a glycol having 2 or 3 carbon atoms.

(4) The external base composition according to item 1, wherein the aqueous liquid is water or hydrous ethanol.

(5) The external base composition according to item 1, wherein the weight ratio of the film-forming polymer to the adhesive polymer is in the range of 1:4 to 4:1.

(6) The external base composition according to item 1, wherein the aqueous liquid is in the range of 40 to 80% by weight of the total components.

In the composition of the present invention, water-soluble film-forming polymers used as film-forming components include:
A water-soluble polymer substance that is not toxic or irritating to the skin is used, and polyvinyl alcohol with a degree of polymerization of 300 to 2000 is used.

The water-soluble adhesive polymer used as the adhesive component is a water-soluble polymer that is compatible with the film-forming component, provides appropriate adhesiveness, and does not have toxic irritation to the skin. Solution polymerization of the substances vinylpyrrolidone and vinyl acetate in ethanol is used, and it is particularly preferred that the ratio of vinylpyrrolidone to vinyl acetate is in the range of 1:4 to 4:1. Solution polymerization of the above pyrrolidone-vinyl acetate copolymer, acrylic acid, acrylic acid ester, and methacrylic acid ethanol in an ester, and a polymer solution whose water solubility is improved by neutralizing this polymer with an alkanolamine solution. (acrylic resin alkanolamine liquid) can also be used. It is preferable to use polyvinyl alcohol as the film-forming polymer of the present invention because it dissolves well in the ethanol solution of these polymers. As the acrylic ester and methacrylic ester, esters of acrylic acid or methacrylic acid and a linear or branched alkanol having 1 to 18 carbon atoms are used. As high-boiling plasticizers, polyhydric alcohols are used, preferably glycols with 2 or 3 carbon atoms, such as propylene glycol or ethylene glycol, or glycerin. These plasticizers have the effect of plasticizing the polymer and dissolving the medicinal ingredient.

Water (preferably distilled water) or an aqueous ethanol solution is used as the aqueous liquid.

In the composition of the present invention, the ratio of each component is not critical, but in order to form a stable film in a short time and improve the release of the contained medicinal ingredients, it is necessary to use a film-forming polymer and an adhesive. The weight ratio of the polymer is in the range of 1:4 to 4:1, and the weight ratio of the high boiling point plasticizer to the sum of the film-forming polymer and the adhesive polymer is in the range of 1:4 to 4:1.
10:1 to 1:1 range, 40% of total components are aqueous liquids
It is desirable that the content be in the range of 80% by weight. Specifically, the film-forming polymer accounts for 5 to 35% by weight of the composition, preferably 10 to 25% by weight, and the adhesive polymer accounts for 5 to 35% by weight of the composition.
35% by weight, preferably 10-25%, high-boiling plasticizers up to 20%, preferably 2-15%, aqueous liquids 40-80%. When an aqueous ethyl alcohol solution is used as the aqueous liquid, the amount of ethyl alcohol is within a range that does not cause precipitation of the film-forming polymer. The adhesive polymer is preferably a vinyl pyrrolidone-vinyl acetate copolymer dissolved in ethyl alcohol with a water content of 1% or less at a concentration of 10 to 60% by weight.

The composition of the present invention can contain various medicinal ingredients conventionally used as external medicines. For example, antibiotics such as oxytetracycline, chlortetracycline, and neomycin sulfate, antihistamines such as diphenhydramine, anesthetics such as benzocaine and lidocaine, antibacterial agents such as iodine, nitrofurazone, benzalkonium chloride, and tolnaftate, and hydrocortisone. , corticosteroids such as triamcinolone acetonide, indomethacin flupiprofen, non-steroidal anti-inflammatory drugs such as Pfuexamac, etc. These drugs are included in the compositions of the invention at pharmaceutically effective concentrations. The concentration range is not particularly limited, but is usually 0.01 to 20% by weight of the total composition. The medicinal ingredients are absorbed into the human body through the film formed when the composition of the present invention is applied onto the skin or wound surface.

The composition of the present invention is prepared according to conventional methods. For example, a film-forming polymer may be dissolved in an aqueous liquid, to which a tacky polymer and a high-boiling plasticizer may be added to form a homogeneous composition. Desired medicinal ingredients are appropriately mixed during or after the preparation of the composition.

Each component of the present invention is substantially dissolved in water,
The composition is a semi-solid with appropriate hardness, is stored in a sealed container such as a tube, and is applied to the skin or wound surface in the same manner as a conventional ointment or cream. It dries within 1 to 10 minutes after application, forming a flexible film. The film adheres to the skin for 1 to 24 hours, causing no discomfort or discomfort, and does not interfere with daily life. After use, the coating can be easily removed by peeling off with fingers or washing with water.

Next, the present invention will be explained in more detail with reference to Examples.

Example 1 250 g of polyvinyl alcohol with a degree of polymerization of 500 to 600 ("Poval PA-05" manufactured by Shin-Etsu Chemical Co., Ltd.) and 550 g of distilled water
100 g of vinylpyrrolidone-vinyl acetate copolymer (Rubisco VA64 manufactured by BASF) and 100 g of glycerin were added and stirred to obtain a homogeneous composition.

The external base composition thus obtained has a suitable semi-solidity like an ointment and can be easily spread on the skin.

When this external base composition was evaluated on the flexor side of a person's forearm, the time it took to form a film on the skin (dry to the touch) was approximately 2 minutes and 30 seconds, and it remained fixed on the skin for 8 to 12 hours. No falling off due to friction such as clothing was observed.

In addition, in the primary skin irritation test of this external base composition,
When judged based on the Draize method, it was 0.2 or less, and the irritation was extremely slight.

Effects of the Invention According to the present invention, it has excellent adhesion to the skin,
An external base composition is provided that forms a stable film on the skin or wound surface that does not peel off easily.

Since the composition of the present invention uses an adhesive polymer that is compatible with the film-forming polymer, it has excellent adhesion to the skin.

According to the present invention, an external base composition that forms a moisture permeable film is provided.

Since the film has moisture permeability, the moisture of sweat is released into the outside air, so that it does not cause stuffiness or rash even after long-term use. Also, it does not cause any discomfort or discomfort to the skin.

According to the present invention, an external base composition with excellent release properties of medicinal ingredients is provided.

When the composition of the present invention contains a medicinal ingredient and is applied to the skin or wound surface, the drug absorption into the human body is superior to that of conventional ointments, creams, or film-forming external preparations.

Furthermore, according to the invention, toxicity to the skin,
A non-irritating external base composition is provided.

As described above, according to the present invention, the usability is good and
Moreover, an external base composition with high therapeutic effects is provided.

Claims (1)

[Scope of Claims] 1. A water-soluble film-forming polymer, a water-soluble adhesive polymer that is compatible with the film-forming polymer, and a combination of the film-forming polymer and the adhesive polymer. The film-forming polymer is polyvinyl alcohol with a degree of polymerization of 300 to 2000, the adhesive polymer is vinylpyrrolidone-vinyl acetate copolymer, and the high-boiling plasticizer is polyvinyl alcohol. and the weight ratio of the high-boiling plasticizer to the sum of the film-forming polymer and the adhesive polymer is from 10:1 to 1:1.
A base composition for external use, characterized in that the composition is within the range of 2. The external base composition according to claim 1, wherein the vinylpyrrolidone to vinyl acetate ratio of the vinylpyrrolidone-vinyl acetate copolymer is in the range of 1:4 to 4:1. 3. The external base composition according to claim 1, wherein the polyhydric alcohol is a glycol having 2 or 3 carbon atoms. 4. The external base composition according to claim 1, wherein the aqueous liquid is water or hydrated ethanol. 5. The external base composition according to claim 1, wherein the weight ratio of the film-forming polymer to the adhesive polymer is in the range of 1:4 to 4:1. 6. The external base composition according to claim 1, wherein the aqueous liquid is in the range of 40 to 80% by weight of the total components.