JP2005060324A - General-purpose external antipruritic agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a general-purpose external antipruritic agent capable of corresponding to all pruritus-generating factors accompanying skin inflammation and capable of being combinedly used with a steroid external preparation used as treatment by medical specialists. <P>SOLUTION: The general-purpose external antipruritic agent comprises nearly 1-2 wt.% antihistamic agent as an antipruritic agent and nearly ≥85 wt.% purified water. <P>COPYRIGHT: (C)2005,JPO&NCIPI

Description

  The present invention relates to a general-purpose external antipruritic agent.

In the field of dermatology, “itch” remains a great enemy for both doctors and patients. “Scratching” ensures that skin lesions are exacerbated. In addition, some patients suffer from “self-injury” that creates “scratches” that are much deeper on the skin due to “ugliness”, and there is also a tragedy that adds infection. Even if you do not go there, dry skin shows an increase in the number of skin resident bacteria.
For example, if dry skin that was not red until yesterday suddenly turned red the next day, staphylococcus aureus is growing when the skin surface is cultured. This can be expressed as “pathogenicity of non-pathogenic resident bacteria”.

In this case, many antipruritic agents for external use have been devised in the past, but unfortunately there are no antipruritic agents made from the dermatopathological and bacteriological standpoints.
In the past, “external preparations” include cocaine, local anesthetic nupercaine, or potassium soap emulsified with alcohol and water and added with camphor, diphenhydramine hydrochloride (water-soluble), methylephedrine, and the like. In addition, the antifungal effect of the insecticide crotamiton is also known.
In recent years, diphenhydramine has also become basic (oil-based) which does not break emulsification with an anionic active agent, and d-cloferamine maleate has also been added. Crotamiton is also formulated.
Anti-histamines and anti-allergic agents are used internally in medical institutions, and "external use" mainly focuses on the treatment of inflammation with steroids. In particular, external use of anti-pruritic agents has no lesion on the epidermis. Other than gin machines, skin pruritus, insect bites, etc., it is generally not possible to use any skin disease.

  The components of an external antipruritic agent currently on the market are as follows. Diphenhydramine, diphenhydramine maleate, diphenhydramine hydrochloride, chlorferamine maleate (antihistamine), corticosteroids (pharmaceuticals), crotamiton (skin irritation, steroid solubilizer, and denies the possibility of affecting the transesterification of topical steroids Not possible), dibucaine, lidocaine (local anesthetic, long-term anxiety, effective for insect bites), ethyl aminobenzoate (possibility of allergy), mint component, ammonia water, salicylic acid (irritant, temporary use of insect bites) ), Dl camphor, L-menthol (safe for concentration).

Each of these components can be kept safe depending on the concentration, base, and usage.
However, based on the idea that has been taken one step further, in addition to high safety and antipruritic effect for skin with constantly lesions, it suppresses pruritus for a long period of time in order to enhance the therapeutic effect of dermatology, and worsens by scratching It is not a general-purpose external antidiarrheal agent that prevents patients and contributes to comfortable treatment of patients.

  The present invention relates to histopathologically, skin surface defects, wrinkles extending deeper than the dermal papilla layer, and pruritic skin diseases other than ulcers (atopic dermatitis, dry skin, urticaria, senile pruritus). It is intended for the prevention of pruritus in pruritus such as stress pruritus, pregnancy pruritus, pruritus associated with dialysis, pruritus caused by living diseases such as diabetes, pruritus from initial stage to prurigo-type reaction, etc.

  In particular, since dry skin is accompanied by defects in the surface of each layer, the acid film on the skin surface inevitably also forms dysfunction, and the growth of skin resident bacteria is seen. Easily edema of the basal layer of the epidermis, not so strong around the subdermal papillary vascular plexus, but lymphocyte infiltration is seen, affecting stratum corneum formation. In other words, refractory dry skin causes pathogenization of skin resident bacteria, exhibits eczema-type reaction, soaks in a vicious circle that becomes dry skin due to keratinization, and curettage due to itching is an adverse factor in all the processes Acts and always involves the pathogenesis of skin resident bacteria.

Therefore, the present invention is intended to provide a general-purpose external antipruritic agent that can cope with all pruritus-causing factors associated with skin inflammation and can be used together with a steroid external preparation used as a treatment by a specialist. To do.
As the condition,
(1) Do not rash (do not cause allergies).
(2) No irritation.
(3) To act to enhance the effect of dermatological medicine without disturbing it.
(4) The patient can be aware of the antipruritic effect.
(5) Safe for skin lesions that are sensitive to inflammation.
Is mentioned.

The present invention provides a general-purpose external antidiarrheal agent containing approximately 1 to 2% by weight of an antihistamine as an antidiarrheal agent and approximately 85% by weight or more of purified water as described in claim 1. Is.
Further, the present invention provides a general-purpose external antipruritic agent according to claim 1, wherein the antihistamine is a diphenhydramine base or diphenhydramine hydrochloride as described in claim 2. .

In addition, the present invention, as described in claim 3, contains 1 to 3 kinds of emulsifiers having a large skin permeability in the general-purpose external antipruritic agent according to claim 1 or 2, containing approximately 1.5% by weight. The present invention provides a general-purpose external antipruritic agent.
Further, the present invention is the versatile external antipruritic agent according to claim 3, wherein the emulsifier is ceteth 23, sorbet tetraoleate, sorbitan stearate, polyoxyethylene cetyl ether, as described in claim 4. The present invention provides a general-purpose external antipruritic agent comprising any one of polyoxyethylene sorbitol tetraolenic acid.

Further, according to the present invention, as described in claim 5, in the general-purpose external antipruritic agent according to any one of claims 1 to 4, a solvent comprising approximately 4% by weight of isopropyl propionate or isopropyl myristate is added. The present invention provides a general-purpose external antipruritic agent to be contained.
Further, according to the present invention, as described in claim 6, in the general-purpose external antipruritic agent according to any one of claims 1 to 5, a moisturizing agent comprising approximately 5% by weight of propylene glycol is contained. A general-purpose external antipruritic agent is provided.

Further, according to the present invention, as described in claim 7, in the general-purpose external antidiarrheal according to any one of claims 1 to 6, the herbal medicine component such as Tea Tree Oil (manufactured by Southern Cross Co.) is almost zero. The present invention provides a general-purpose external antipruritic agent containing 5% by weight.
Further, as described in claim 8, the present invention contains approximately 1 to 2% by weight of antihistamine as an antidiarrheal agent, and contains approximately 35% by weight or more of ethanol and approximately 35% by weight or more of purified water. The present invention provides a general-purpose external antipruritic agent.

Moreover, the present invention provides a general-purpose external antipruritic agent comprising approximately 5% by weight of isopropyl adipate in the general-purpose external antipruritic agent according to claim 8, as described in claim 9. To do.
In addition, the present invention provides a general-purpose external antipruritic agent according to claim 8 or 9, wherein the general-purpose external antidiarrheal agent comprises approximately 10% by weight of jojoba oil. It is to provide.

  Further, according to the present invention, as described in claim 11, in the general-purpose external antipruritic agent according to any one of claims 1 to 10, approximately 0.2 to 1% by weight of menthol and / or approximately 0.4. The present invention provides a general-purpose external antipruritic agent containing dl-camphor in an amount of% by weight. .

  According to the general-purpose external antipruritic agent according to the present invention, the antipruritic agent has a constitution containing approximately 1 to 2% by weight of antihistamine as an antidiarrheal agent and approximately 85% by weight or more of purified water. The agent's solvent is mainly purified water, and the irritation is reduced. At the same time, the application of antipruritic agent can be made as small and thin as possible, so it does not cause irritation and allergies, and does not cause irritation and is sensitive to inflammation. Unlike the case where an ointment or cream is applied, the steroid is diluted by the primer and reduces the concentration effect even if it is used for the primer of the steroid that is the main agent of treatment. In addition, there is no fear of ester transfer of the steroid, and it is possible to perform double coating in parallel with the steroid.

In the present invention, the emulsifier contained in the general-purpose external antipruritic agent in an amount of about 1.5% by weight is ceteth-23, sorbes tetraoleate 60, sorbitan stearate, polyoxyethylene cetyl ether, polyoxyethylene tetraoleenate. By having a constitution composed of any of sorbitol, it is possible to obtain a very safe antipruritic agent having a large skin permeability.
Further, the present invention provides a general antistatic agent for external use according to any one of the above, comprising a composition comprising approximately 4% by weight of a solvent composed of isopropyl propionate or isopropyl myristate, Can be effectively emulsified.

Moreover, this invention can contain the moisturizing agent which consists of about 5 weight% propylene glycol in the general purpose external antipruritic agent described in any of the above.
In addition, the present invention is a general-purpose external antipruritic agent according to any one of the above, by having a composition containing approximately 0.5% by weight of a herbal component such as Tea Tree Oil (manufactured by Southern Cross). It can add bactericidal, antibacterial and antioxidant effects to antipruritic agents.

    In addition, as herbal ingredients, vitamin C (persimmon, tea, seri, pine needles), carotenoids (carrots), flavonoids (Coganebana, Neubara, Daidai, Green tea, licorice), tannins (geno shochu, pomegranate, clove, keihi), caffeic acid derivatives (mugwort, perilla, weevil), lignans (sesame oil, ginseng), saponins (soybean, mishimashiko), etc. Plants and herbal medicines containing them can be used in combination.

  In addition, the present invention contains a composition containing approximately 1 to 2% by weight of an antihistamine as an antidiarrheal agent, and contains approximately 35% by weight or more of ethanol and approximately 35% by weight or more of purified water. As an alcohol solvent type antipruritic agent, there is no surface defect (carp column) and it is suitable for severe pruritus such as gin machine, cutaneous pruritus, insect bite, etc. However, even if there is a papule, it can be used if the patient desires it and does not complain of discomfort.

In addition, the present invention has a constitution in which the above-mentioned general-purpose external antipruritic agent contains approximately 5% by weight of isopropyl adipate, so that it dissolves in both alcohol and oil and suppresses irritation of the antidiarrheal agent. be able to.
In addition, the present invention has a constitution in which approximately 10% by weight of jojoba oil is contained in the above-mentioned general-purpose external antipruritic agent, thereby maintaining the concentration of the contained components, and protecting the skin and stabilizing the bactericidal properties. Can be planned.
In addition, the present invention is a general-purpose external antipruritic agent that has a constitution in which approximately 0.2 to 1% by weight of menthol and / or approximately 0.4% by weight of dl-camphor is contained. It has the effect of improving the antipruritic effect by paralysis after excitement.

  A preferred embodiment of the present invention is as follows.

1) Emulsion Type Setes-23 0.5% (Emulsifier)
SORBES TETRAOLEATE 60 0.5% (Emulsifier)
Sorbitan stearate 0.5% (emulsifier)
Pharmacopoeia Setanol 1% (viscosity agent)
Isopropyl propionate 4% (emulsifier)
L-Menthol 0.2% (Excitement / paralysis agent)
dl-Camphor 0.4% (excitement / paralysis agent)
Diphenhydramine base 2.0% (antipruritic agent)
Methylparaben 0.1% (preservative)
Propylene glycol 5% (penetration / humectant)
Tea Tree Oil (Southern Cross) 0.5%
Purified water 85.3%

2) Emulsion Type Setes-23 0.5%
Solveste tetraoleate 60 0.5%
Sorbitan stearate 0.5%
Pharmacopoeia Setanol 1%
Isopropyl propionate 4%
L-Menthol 0.2%
d1-Camphor 0.4%
Diphenhydramine base 2.0%
Methylparaben 0.1%
Propylene glycol 5%
Tea Tree Oil (Southern Cross) 0.5%
Purified water 85.28-85.253%
Hidden Gluconate 20% solution 0.02-0.05%
(General disinfectant with less irritation)

3) Alcohol solvent type
Polyoxyethylene lauryl ether 5% (surfactant)
Diphenhydramine base 1.0%
Ethanol 40% (bactericidal / antibacterial agent)
Menthol 1%
d-Camphor 0.4%
Diisobutyl adipate 5% (Irritation inhibitor)
Jojoba oil 10% (tree nut oil)
Purified water 37.7%

4) Infant type ceteth-23 0.5%
Solveste tetraoleate 60 0.5%
Sorbitan stearate 0.5%
Pharmacopoeia Setanol 1%
Isopropyl propionate 4%
d-Chlorferamine maleate 1%
Diphenhydramine base 1%
Methylparaben 0.1%
Propylene glycol 5%
Tea Tree Oil (Southern Cross) 0.5%
Purified water 85.4%

5) Infant type ceteth-23 0.5%
Solveste tetraoleate 60 0.5%
Sorbitan stearate 0.5%
Pharmacopoeia Setanol 1%
Isopropyl propionate 4%
d-Chlorferamine maleate 1% (antipruritic agent)
Diphenhydramine base 1%
Methylparaben 0.1%
Propylene glycol 5%
Tea Tree Oil (Southern Cross) 0.5%
Purified water 85.38-85.35%
Hibiten Gluconate 20% solution 0.2-0.05%

The results of a clinical test of the antipruritic agent of the present invention thus obtained are shown.
The test subject is
B. Atopic dermatitis 0 to 60 years old 30 random extractions 30 eczema 0 to 60 years old 30 random extractions 30 urticaria 15 to 75 years random extraction 30 cases 2 Acute / chronic urticaria 15 years old Up to 75 years old Random extraction 30 cases Eczema pruritus Senile / pregnancy 15 cases each Total 30 cases Antipruritic drugs are in principle using 1) emulsion type (Example 1) to react sensitive skin reaction The emulsion type (Example 2) of 2) was used only for the object shown.
The results are shown in Table 1.

In Table 1, three cases which had no effect at all were very effective when the alcohol solvent type (Example 3) of 3) was applied, and reported a use effect of up to about 3 hours. There were no worsening cases.

Claims (11)

A general-purpose external antipruritic agent containing approximately 1 to 2% by weight of an antihistamine as an antidiarrheal agent and approximately 85% by weight or more of purified water. The general-purpose external antipruritic agent according to claim 1, wherein the antihistamine is a diphenhydramine base or diphenhydramine hydrochloride. 3. The general-purpose external antipruritic agent according to claim 1 or 2, wherein 1 to 3 kinds of emulsifiers having high skin permeability are contained in an amount of about 1.5% by weight. The general-purpose external antipruritic agent according to claim 3, wherein the emulsifier is any one of ceteth-23, tetraoleic acid sorbes 60, sorbitan stearate, polyoxyethylene cetyl ether, and tetraoxylenic acid polyoxyethylene sorbite. Anti-tarnish agent for external use. 5. The general-purpose external antipruritic agent according to any one of claims 1 to 4, wherein the general-purpose external antidiarrheal agent comprises approximately 4% by weight of a solvent composed of isopropyl propionate or isopropyl myristate. 6. A general-purpose external antipruritic agent according to any one of claims 1 to 5, comprising a moisturizing agent comprising approximately 5% by weight of propylene glycol. The general-purpose external antidiarrheal agent according to any one of claims 1 to 6, wherein the general-purpose external antidiarrheal agent contains approximately 0.5% by weight of a crude drug component such as Tea Tree Oil (manufactured by Southern Cross). A general-purpose external antidiarrheal agent containing approximately 1 to 2% by weight of an antihistamine as an antidiarrheal agent and containing approximately 35% by weight or more of ethanol and approximately 35% by weight or more of purified water. 9. A general-purpose external antipruritic agent according to claim 8, comprising approximately 5% by weight of isopropyl adipate. The general-purpose external anti-tarnish agent according to claim 8 or 9, wherein the general-purpose external anti-tarnish agent contains approximately 10% by weight of jojoba oil. The general-purpose external anti-tarnish agent according to any one of claims 1 to 10, wherein the general-purpose external anti-stop agent contains approximately 0.2 to 1% by weight of menthol and / or approximately 0.4% by weight of dl-camphor. Glaze.