JPS63255219A - Antipruritic plaster - Google Patents

Abstract

PURPOSE:To obtain an antipruritic plaster exhibiting effective and continuous antipruritic effect, by compounding diphenhydramine or chlorpheniramine maleate to a plaster base. CONSTITUTION:A plaster base is compounded with diphenhydramine of formula I or chlorpheniramine maleate of formula II. The base is a rubber-based sticking component added with a tackifier resin (e.g. petroleum resin or rosin), a softener (e.g. liquid rubber) and an antioxidant (e.g. butylhydroxyanisole) or an acrylic sticking resin such as acrylic ester polymer.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to an anti-pruritic plaster containing diphenhydramine or chlorpheniramine maleate as an anti-pruritic ingredient.

[Prior Art] Diphenhydramine and chlorpheniramine maleate are both types of antihistamines and have antipruritic effects. For this reason, it has conventionally been used as a therapeutic agent for itching associated with skin diseases, insect bites, etc. in the form of ointments, liquid solutions for application, or oral preparations. The structural formulas of these compounds are shown below.

Diphenhydramine C+tH*tON: 2 5 5CI6HI@N
2C1-04H404:390 [Problems to be Solved by the Invention] The use of the above-mentioned conventional dosage form has the following problems.

(b) In ointments, if the compatibility between the drug and the base is poor, it is inevitable that the medicinal ingredients will precipitate as crystals.
As a result, not only the necessary medicinal effect cannot be obtained, but also the sustainability of the action is extremely poor, and furthermore, the stickiness of the ointment itself may stain clothes.

(b) In liquid preparations for application, the solvent evaporates due to body temperature, and the medicinal ingredients easily crystallize as in the case of ointments.
It is difficult to obtain sufficient medicinal efficacy as well as its sustainability.

(c) In oral preparations, the drug is absorbed from the intestinal tract, enters the bloodstream, and is then transported to the affected area, so the drug is dispersed throughout the body. As a result, the concentration of the drug that reaches the affected area is low, making it difficult to obtain a sufficient pharmacological effect, and furthermore, the drug may reach or pass through areas other than the affected area, easily causing side effects such as rash, nausea, nervousness9 headaches, or dry mouth. Easy to invite.

The present invention was made in view of these circumstances, and
Ointment! ! ! The object of the present invention is to provide an antipruritic plaster that solves all of the above-mentioned disadvantages caused by the use of liquid preparations for cloth and oral preparations, and exhibits sufficient medicinal efficacy and is excellent in its persistence.

[Means for Solving the Problems] The gist of the present invention is to incorporate diphenhydramine or chlorpheniramine maleate.

[Effect] The present invention focuses on the fact that diphenhydramine and chlorpheniramine maleate have the effect of suppressing the development of histamine-induced vascular permeability, and by incorporating these drugs into a plaster base, the antipruritic effect can be efficiently achieved. And it is something that can be demonstrated continuously.

In the present invention, a local anesthetic, an anti-inflammatory agent, an antibacterial agent, a flavoring agent, etc. can also be added in addition to the above-mentioned drugs.

In this case, dibucaine, lidocaine, etc. can be used as the local anesthetic.

Anti-inflammatory agents include cortisone and cortisone acetate.

Corticosteroids such as hydrocortisone, hydrocortisone acetate, prednisolone, dexamethacin, pentamethacin, etc. can be used. As the antibacterial agent, chlorhexidine gluconate, chlorhexidine hydrochloride, decalium chloride, isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, etc. can be used. Moreover, menthol etc. can be used as a flavoring agent.

Figure 1 shows a) Hahydrocortisone 0.5 g 0.25 g O
g Crotamiton 5.0g 2.5g 0g
Diphenhydramine 1. Og 0.5g Og dibucaine 3.0g 1.5g 0g1-
This study investigated the rate of advanced inhibition of histamine-induced vascular permeability when a plaster obtained by melting and kneading Mentor Az 5.0 g 2.5 g Og was applied for 2 hours. As is clear from FIG. 1, the inhibition rate of A and K is about 80%, indicating that it definitely has superior medicinal efficacy compared to Bracebo.

Furthermore, FIG. 2 shows the results of investigating the advanced inhibition rate of histamine-induced vascular permeability for each sample using the following components.

(a) Muhi (manufactured by Ikeda Gendo Co., Ltd.) 100 mg (
b) Hydrocortisone 0.125% Crotamiton 2.5% Diphenhydramine 0.5% Dibucaine 0.5% 1-menthol 2.5% (c) Diphenhydramine 1.0% Dibucaine
0.5% l-menthol S, O% (d) Chlorpheniramine maleate 1.0% Tocopherol acetate o, s% Gelcol salicylate 1.0% (e) Chlorpheniramine 0.5% Tocopherol acetate 0.5 % Glycol salicylate 1.0% As is clear from the results in Figure 2, samples using diphenhydramine or chlorpheniramine maleate (b
) to (e) showed inhibition rates comparable to sample (a).

Next, the plaster base material will be explained. As the plaster base of the present invention, a rubber-based adhesive component with adhesion-imparting resin, a softener, and an antioxidant can be used, or an acrylic adhesive such as an acrylic ester polymer. Resins can also be used. In the former case, the rubber adhesive component is natural rubber or styrene-butadiene copolymer.

Synthetic rubbers such as styrene-isoprene-styrene block copolymers and silicone rubber can be used. As the adhesion-imparting resin, resins such as petroleum resin, rosin, hydrogenated rosin, ester gum, or alicyclic saturated hydrocarbon resin can be used. As the softening agent, liquid rubber higher fatty acid esters such as bolybdenum, polyisobutylene, isopropyl myristate, silicone, liquid paraffin, animal and vegetable oils, etc. can be used. As the antioxidant, butylhydroxyanisole, dibutylhydroxytoluene, guaiacol esters, nordihydroguaiatic acid, etc. can be used. On the other hand, in the latter case, that is, when an acrylic adhesive is used as the base material, it is possible to produce a plaster with good adhesiveness without using an adhesive component or a softener.

Therefore, in this case, the drug and the base may be kneaded to form a paste, and any of the components of the base may be added only when particularly necessary.

In the former case, it is preferable that the amount of the rubber adhesive component in the base material is 20 to 50% (wt%, same hereinafter) based on the total amount of the paste; if it is less than 20%, the cohesive force will be insufficient; If the tackifying resin exceeds 25 to 65%, the amount of other components blended will be insufficient and it cannot be used as an adhesive.
%. If it is less than 25%, the adhesive strength is insufficient, while if it exceeds 65%, the adhesive becomes hard and loses its effectiveness as an adhesive. It is preferable that the softener is present in an amount of 0.1 to 40%; less than 0.1% has no effect, while more than 40% results in insufficient cohesive force. When the base material is used as an emulsion, the solid content may be within the range of the above-mentioned mixing ratio.When producing a plaster, the solvent method, hot melt method, emulsion method, etc. Existing methods can be used as appropriate, but depending on the characteristics of the obtained plaster,
It is free to change the order of addition of the medicinal ingredients and base materials as appropriate in consideration of the simplicity of the process procedure, or to apply heating, ultrasonic treatment, etc. for the purpose of promoting melting of the medicinal ingredients.

The paste obtained in this way is spread on a support and a release paper is pasted thereon.

The support used in the present invention is preferably made of a flexible material that can easily follow the movements of the human body, and various nonwoven fabrics,
Woven cloth, flannel or polyethylene film on these materials,
A laminated film of ethylene vinyl acetate film, polyurethane film, etc., or a single or composite film of vinyl chloride film, polyethylene film, polyurethane film, etc. can be used. The obtained plaster may be processed into an appropriate shape in consideration of the indication, the applicable site, etc. For example, holes may be formed in the support in consideration of the dispersion of sweated water.

Examples will be described below, but the present invention is not limited to the following examples, and it is within the technical scope of the present invention to make appropriate design changes in accordance with the spirit of the above and below.

In all Examples, the total amount was too large and was spread evenly over 1 m2 of the support.

[Example] Example 1 Styrene-isoprene-styrene block copolymer (Califlex TR1107: manufactured by Ciel Chemical Co., Ltd.) 30 g liquid paraffin 5.5 g alicyclic saturated hydrocarbon resin (Alcon P-100: manufactured by Arakawa Chemical Co., Ltd.) 45g of polyisobutylene (10g of dibutylhydroxytoluene) and 5g of dibutylhydroxytoluene were melt-kneaded at a temperature of about 150°C, followed by 1.0g of diphenhydramine.
Dibucaine 0.581-menthol 3.0g was mixed to prepare a medicinal paste. The antipruritic plaster was obtained by uniformly applying this plaster onto a release paper at a warm temperature and, after cooling, supporting the front surface with a vinyl chloride film.

Examples 2 to 4 below were produced in the same manner as Example 1.

Example 2 Lidocaine 2.0g Glycol salicylate (anti-inflammatory analgesic) 1.0g Chlorpheniramine maleate 1.0g Tocopherol acetate (peripheral vascular circulation promotion effect) 0.5g Styrene-isoprene-styrene block copolymer 25g Liquid paraffin 2 .0g alicyclic saturated hydrocarbon resin (Alcon p-ioo) 50g polyisobutylene ttg oleyl alcohol (emulsifier) 1.0'g dibutylhydroxytoluene 1.5g propylene glycol 5
．． Og Example 3 Chlorpheniramine 2.0g Hydrocortisone acetate 0.5g Chlorhexidine gluconate 0.58 Styrene-isoprene-styrene block copolymer 40g Alicyclic saturated hydrocarbon resin (Alcon P-100) 55g Dibutylhydroxytoluene 2g Example 4 Chlorpheniramine 1.5 g Tocopherol acetate 1.5 g Glycol salicylate 2.0 g Styrene-isoprene-styrene block copolymer 43 g Alicyclic saturated hydrocarbon resin (Alcon P-100) 50 g Dibutylhydroxytoluene 2.0 g [Effects of the Invention] Since the present invention is configured as described above, the medicinal ingredients do not precipitate as crystals, the medicinal efficacy is sufficiently expressed and its sustainability is excellent, and it can be used easily and conveniently. An antipruritic plaster is obtained.

[Brief explanation of drawings]

FIGS. 1 and 2 are diagrams showing the advanced inhibition rate of histamine-induced vascular permeability in each drug sample. Figure 1

Claims (1)

[Claims] An antipruritic plaster characterized by containing diphenhydramine or chlorpheniramine maleate.