JPS62263120A - Plaster - Google Patents

Abstract

PURPOSE:A plaster which is liquid in application, shows a filmy state by drying after application and has improved water resistance and flexibility, containing a water-soluble high polymer, a polyhydric alcohol and a drug. CONSTITUTION:A plaster containing (A) a water-soluble high polymer such as PVA, polyvinylpyrrolidone, 2-hydroxyethyl (meth)acrylate (co)polymer, CMC or gum arabic, (B) a polyhydric alcohol such as polyethylene glycol, glycerin, etc., and (C) a drug which is absorbed with time to show medicinal effects. The amount of the component B used is 10-200pts.wt., preferably 20-70pts.wt. based on 100pts.wt. component A. Since the plaster shows a filmy state by drying, the plaster is not attached to materials to be brought into contact with the agent, the affected part is not exposed to air and causes no problem of reduction in active ingredient of drug resulting from adhesion to the materials and reduction in medicinal effects.

Description

DETAILED DESCRIPTION OF THE INVENTION (Field of Industrial Application) The present invention relates to a patch that is liquid at the time of application and forms a film upon drying after application, and particularly to a patch that is excellent in water resistance and flexibility.

(Prior Art) Transdermal transmucosal preparations for medical use include, for example, ointments, plasters such as tape preparations and patch preparations, and poultices.

However, when ointments are applied to the affected area, they tend to adhere to surfaces other than the affected area, such as skin or clothing, which may stain clothing or other objects they come in contact with, or reduce the effectiveness of the drug due to a decrease in the active ingredient. , and because the affected area is exposed.

Difficult to prevent the infiltration of germs (and unfavorable from a hygienic standpoint. Plates and poultices do not synchronize with the expansion and contraction of the skin, so they may cause pain when applied or may peel off after application. They may cause skin irritation. There is also.

Moreover, the appearance is impaired by pasting. Poultices have low adhesive properties and are easy to peel off even if they are fixed with a bandage.

In order to solve these drawbacks, a patch that is liquid at the time of application and forms a film after drying has been proposed.
A composition for a polymeric bandage is disclosed which comprises a dialkylaminoalkyl methacrylate/methacrylic ester copolymer and a plasticizer such as a glycol or a phthalate. However, since this composition is based on an acrylic copolymer, it lacks water resistance, and therefore, when used under high temperature and high humidity conditions such as summer, the adhesiveness decreases due to excessive sweating on the skin surface. cause.

For these reasons, compositions using polyvinyl alcohol as a base material instead of acrylic copolymers have been proposed.

This composition contains, for example, a combination of an external backing agent (disclosed in JP-A No. 52-44225) which is a mixture of polyvinyl alcohol and an ointment, polyvinyl alcohol, an analgesic and anti-inflammatory agent, and borax as a coating film-forming waterproofing aid. There is an analgesic liniment (disclosed in JP-A-52-79018). However, although these compositions have good water resistance, they lack flexibility. Therefore, the film formed by applying this to the skin and drying it is easily peeled off due to expansion and contraction of the skin.

(Problems to be Solved by the Invention) The present invention solves the above-mentioned conventional problems, and its purpose is to provide a patch with excellent water resistance and flexibility. Another object of the present invention is to provide a patch that does not adhere to objects it comes in contact with when applied. Still another object of the present invention is to provide a patch that does not expose the affected area.
To provide a patch that does not cause pain during application and is free from the risk of peeling off after application. Still another object of the present invention is to provide a patch whose appearance is not impaired by application.

(Means for Solving the Problems) The patch of the present invention is a liquid patch containing a water-soluble polymer, a polyhydric alcohol, and a drug.

After application 4. When dried, it takes on a film-like appearance, thereby achieving the above object.

Examples of water-soluble polymers include polyvinyl alcohol,
Polyvinylpyrrolidone, poly(2-machi) droxyethyl (meth)acrylate, a copolymer containing 50% by weight or more of 2-hydroxyethyl (meth)acrylate units, polyacrylic acid, polyethyleneimine, polyacrylamide, methylcellulose.

Hydroxyethylcellulose, carboxymethylsaylerose, gum arabic9. Tragane, rubber, and polyhydric alcohols include, for example, propylene glyconyl oligomer, propylene glyconyl oligomer, and propylene glyconyl oligomer.

Examples include glycerin 2 and butylene glycol.

Polyhydric alcohol is based on 100 parts by weight of water-soluble polymer,
10-200 parts by weight, preferably 20-200 parts by weight. This is the range of the 0fit portion. When the amount is less than 10 parts by weight, the flexibility of the resulting patch decreases. 200! If the amount exceeds i part, the viscosity of the patch will be too low and it will be difficult to apply it to the skin.

The drug contained in the adhesive patch of the present invention is a drug that is absorbed transdermally and exerts its medicinal effect, for example.

hydrocortiscin, prednisolone, varamethacin,
Beclomethasone propionate, flumethacin, betamethacin, beclomethasone propionate, dexcitacin, triamcinolone, triamcinolone acetonide,
Corticosteroids such as fluocinolone, fluocinolone acetonide, fluocinolone acetonide acetate, clobetasol propionate; acetaminophen.

mefenamic acid, flufenamic acid indomethacin.

Indomethacin, diclofenac, diclofenac sodium, alclofenac. tt'l inflammatory agents such as oxyphenbutacin, phenylbutacin, ibuprofen, flurbubrofen, salicylic acid, l-menthol, camphor and their combinations: such as phenobarbital, amobarbital, cyfrobarbital, etc. Hypnotic sedatives; fluphenazine, thioridazine,
Tranquilizers such as diazepam, lorazepam, flunitrazepam, and chlorpromazine; antihypertensive agents such as curnisin and kallikrein; antihypertensive diuretics such as hydrothiazide and bendroflumeshiazide; penicillin, oxytetracycline, fradiomycin sulfate, erythromycin, and chloramphenicol Antibiotics such as: lidocaine, pensicaine.

Anesthetic agents such as ethyl aminobenzoate; antibacterial agents such as benzalkonium chloride, nitrofurazone, nyscutin, acetosulfamine, clotrimazole; antifungal agents such as pentamycin, amphotericin B, pyrrolnidoline, clotrimazole; vitamins A, ergocalciferol, cholecalciferol, octothiamine,
Vitamin preparations such as riboflavin butyrate; anticonvulsants such as nitrazepam and mepropamate; nitroglycerin, diviridamol, isosorbite cinitrate, and erythritose tetranitrate.

Coronary vasodilators such as pentaerytose tetranitrate; and antihistamines such as diphenhydramine hydrochloride, chlorpheniramine, diphenylimidazole; α
- Naphthylthiocarbamate.

These include athlete's foot drugs such as N-methylthiocarbamate and N-β-naphthylthiocarbamate; and angina drugs such as diisosorbide nitrate.

Such a patch is manufactured by dissolving a water-soluble polymer in heated purified water, adding a polyhydric alcohol thereto, cooling it to room temperature, adding a drug, and mixing. The drug may be added in solid form or dissolved in a suitable solvent.

The patch of the present invention may further contain an absorption enhancer as necessary to promote transdermal absorption of the drug. Examples of the absorption enhancer include salicylic acid, urea, dimethyl sulfoxide, Dimethylacetamide, dimethylformamide, diethyl sebacate, and various surfactants are available. Absorption enhancers should be considered for skin adhesion, cohesion retention, etc.

It is contained in the patch in a range of 0.5 to 20% by weight.

To use the patch of the present invention, apply it to the skin to be applied using a brush, fingertips, spray, or the like.

All you have to do is leave it for a while and wait for it to dry naturally, thereby forming a drug-containing film layer that adheres to the skin surface.

(Example) The present invention will be described below with reference to examples.

(Anti-inflammatory drug) To 451 parts of purified water heated to 90°C, 20 parts by weight of polyvinylpyrrolidone (degree of polymerization 1000) was added and dissolved with stirring. After adding 10 parts by weight of propylene glycol to this solution and cooling it to room temperature, 10%
3 parts by weight of indomethacin-ethanol solution was added and stirred and mixed to obtain a patch.

The obtained patch was applied to the skin surface, spread thinly, and allowed to air dry to form a thick, uniform film.

The surface of this film has no viscosity, and the skin surface on which it is applied is
It remained stuck for more than 0 hours.

Polyvinyl alcohol (degree of polymerization: 1000) was added to 45 parts by weight of purified water heated to 90° C. with stirring and dissolved therein. After adding 10 parts by weight of ethylene glycol to this solution and cooling it to room temperature.

While stirring, 0.5 g of crystalline diclofenac sodium was added to obtain a patch.

The obtained patch was applied to the skin surface in the same manner as in Example 1 and dried to form a film. The surface of this film had no viscosity and remained adhered to the skin surface on which it was applied for a long period of time as in Example 1.

Examples - (athlete's foot medicine) To 45 parts by weight of purified water heated to 90°C, 20 parts by weight of hydroxyethyl cellulose was added and dissolved with stirring. After adding 10 parts by weight of glycerin to this solution and cooling it to room temperature, 3 parts by weight of urea as an absorption aid and a mixture of α-naphthylthiocarbamate, N-methylthiocarbamate and N-β-naphthylthiocarbamate as drugs were added. .3 parts by weight were added and stirred and mixed to obtain a patch.

The obtained patch was applied to the skin surface in the same manner as in Example 1 and dried to form a film. The surface of this film had no viscosity and remained adhered to the skin surface on which it was applied for a long period of time as in Example 1.

Ohashi Ren (angina medicine) Use isopropyl myristate in place of urea.

The patch was applied in the same manner as in Example 3, except that 3 parts by weight of diisosorbide nitrate was used in place of 0.3 parts by weight of the mixture of α-naphthylthiocarbamate, N-methylthiocarbamate and N-β-naphthylthiocarbamate. obtained the drug.

The obtained patch was applied to the skin surface in the same manner as in Example 1 and dried to form a film. The surface of this film had no viscosity and remained adhered to the skin surface on which it was applied for a long period of time as in Example 1.

(Effects of the Invention) The adhesive patch of the present invention has excellent water resistance and flexibility as described above. Moreover, after application, it becomes film-like due to drying, so
It does not adhere to objects it comes into contact with or expose the affected area, so it does not stain objects it comes in contact with, such as clothes. Since the contact object is not contaminated, there is no problem of the conventional method in which the active ingredient of the drug is reduced by the amount of the drug adhering to the contact object, resulting in a decrease in drug efficacy. Moreover, it is painful when applied.

There is no risk of peeling off after application, and the appearance is not impaired by application.As a result, the patch of the present invention can be effectively used as a medical patch.

that's all

Claims (1)

[Scope of Claims] 1. A liquid patch containing a water-soluble polymer, a polyhydric alcohol, and a drug, which forms a film upon drying after application. 2. The water-soluble polymer is polyvinyl alcohol, polyvinylpyrrolidone, poly2-hydroxyethyl (meth)
Among acrylates, copolymers containing 50% by weight or more of 2-hydroxyethyl (meth)acrylate units, polyacrylic acid, polyethyleneimine, polyacrylamide, methylcellulose, hydroxyethylcellulose, carboxymethylcellulose, gum arabic, gum tragacanth, gum karaya, and sodium alginate. The adhesive patch according to claim 1, which is at least one of the following. 3. The patch according to claim 1, wherein the polyhydric alcohol is at least one of propylene glycol, ethylene glycol, ethylene glycol oligomer, propylene glycol oligomer, glycerin, and butylene glycol. 4. The patch according to claim 1, wherein the polyhydric alcohol is contained in an amount of 10 to 200 parts by weight based on 100 parts by weight of the water-soluble polymer.