JP2000297044A - Transdermal patch for external use for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject transdermal patch for external use that has excellent sustainability and antipruritic effect by using at least one selected from an extract of a plant, Artemisia princeps, an antihistaminic agent and antipruritic agent. SOLUTION: This transdermal patch agent includes (A) an Artemisia princeps extract, (B) antihistamine agent and antipruritic agent. In a preferred embodiment, additionally, (C) at least one kind of plant extract selected from root of Sanguisorba officinalis, leaves of Juniperus communis, leaves of Japan cedar, Lotus root, root of Panax notoginseng, Lycium barbarum, madder and Sophora angustifolia and (D) a microbicide. The Artemisia princeps extract is prepared from leaves, stems and the like in the Artemisia princeps plant body. They are extracted through the known methods and the extract can be used directly as it is, in the form of the concentrate thereof, or after evaporation to the dryness, in any forms. The formulation of these extracts is some 0.001-10 wt.%, preferably in an amount of 0.01-5 wt.%, more preferably 0.05-1 wt.%.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

FIELD OF THE INVENTION The present invention is useful as a composition for external use on the skin, and more particularly, as a cosmetic, pharmaceutical or quasi-drug excellent in prevention and suppression of itching, wound healing, prevention of skin roughening and improvement of skin roughening. A highly moisturizing skin patch for external use.

[0002]

2. Description of the Related Art Itching is caused by irritation to the upper layer of the skin, and histamine is well known as a stimulating chemical substance. Histamine is released into the tissue by degranulation from mast cells and causes itching (Edited by Jun Kubota et al .: Modern dermatology 3C, edited by Yasumasa Ishibashi et al .:
Itchy skin disease). Itchy diseases include atopic pruritus and dry pruritus such as senile pruritus, but such skin disorders can cause mental distress to patients,
Scratching also exacerbates the symptoms. Conventionally, various external preparations have been proposed to prevent or treat such skin diseases. Of these, those containing a crude drug as a main component have attracted attention because of their mild action on the skin (for example, JP-A-1-319424), but the effect is not sufficient. Also, a patch is known which is effective for senile xerosis, cutaneous keratosis, atopic symptoms and the like by incorporating an antipruritic component, a bactericidal component or a moisturizing component into a base (Japanese Patent Application Laid-Open No. Hei 9 (1999)).
-110680 gazette). However, these external preparations are not sufficient in terms of the persistence of the effect.

[0003]

OBJECTS AND SUMMARY OF THE INVENTION An object of the present invention is to provide an external skin patch having an antipruritic effect with excellent durability.

[0004] In view of the above circumstances, the present inventors have paid attention to mugwort extract when examining an antipruritic topical agent having excellent durability in actual clinical settings. The present inventors have found that a long-lasting moisturizing effect and an antipruritic effect can be obtained by adding the compound to a patch, thereby completing the present invention.

[0005] The present invention provides an external skin patch comprising a mugwort extract and at least one drug component selected from antihistamines and antipruritics.
In the present invention, in addition to this, it is preferable to blend at least one plant extract selected from Jiyu, pine needles, cedar leaves, lotus root, radish, dermis, Akane root and Clara, Further, a bactericide may be blended. The patch of the present invention maintains moisture retention and antipruritic properties.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION (Mugwort extract) The mugwort extract used in the present invention is not particularly limited. As an extraction raw material, any of mugwort leaves, stems and the like can be used, and any of the extract itself extracted by a known method, a concentrate thereof, and a dried product are used.

The extraction comprises water or a solvent of intermediate polarity,
The reaction can be carried out with a monohydric or polyhydric lower alcohol or a mixed solvent thereof. Examples of the solvent having an intermediate polarity include ethyl ether, chloroform, ethyl acetate, acetone and the like. Examples of the monohydric lower alcohol include alcohols having 1 to 4 carbon atoms such as methanol, ethanol, propanol, and butanol, and examples of the polyvalent lower alcohol include propylene glycol,
Examples thereof include glycols such as 1,3-butylene glycol and dihydric or trihydric lower alcohols such as glycerin. These may be used alone or as a mixture of two or more. Among them, water or ethanol is particularly preferable from the viewpoint of extraction efficiency.

[0008] The extraction conditions are not particularly limited.
For example, a method of immersing in an extraction solvent of about 1 to 30 times the volume of the raw mugwort at room temperature or under heating (50 to 80 ° C.) for an appropriate time (1 to 8 hours) for one to several times can be mentioned. In addition, removal of solids by filtration or centrifugation,
Purification can be performed by a known method, such as decolorization with activated carbon or resin treatment with a synthetic polymer adsorbent. However, the anti-itch, antipruritic effect of the extract is strongly expressed even with the unpurified extract, so the color, smell,
As long as there is no inconvenience in terms of stability or the like, a high degree of purification is usually unnecessary.

[0009] The amount of the extracted extract is determined by the dosage form,
Depends on the desired anti-itch effect, etc.
Usually, the total amount of the composition is 0.
001 to 10% by weight, preferably 0.01 to 5% by weight,
More preferably, it is about 0.05 to 1% by weight.

If the amount is less than this, the moisturizing feeling is not maintained and the anti-itch effect is not sufficient. On the other hand, when the amount exceeds this range, the effect does not increase in proportion to the amount, and when used for a long time, a skin sensitizing effect occurs, which is not preferable. Furthermore, the smell and coloring peculiar to the plant extract are generated, which may impair the commercial value.

(Drug component) The antihistamine, antipruritic and bactericide to be incorporated in the patch of the present invention are not particularly limited, but the following are preferably incorporated. Examples of the antihistamine include diphenhydramine hydrochloride, diphenhydramine salicylate, diphenhydramine, chlorpheniramine maleate, diphenylimidazole, and the like, and preferably diphenhydramine hydrochloride and diphenhydramine salicylate. Antipruritic agents include crotamiton.

[0012] Examples of the fungicide include thymol, isopropanol, benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, chlorhexidine hydrochloride, isopropylmethylphenol, salicylic acid, and povidone-iodine, and thymol is particularly preferred.
The content of these fungicides is 0.01 to the total amount of the composition.
It is 5% by weight, preferably 0.1 to 3% by weight. These active ingredients may be used alone or in combination of two or more. Of these, diphenhydramine hydrochloride and crotamiton are particularly preferred because of their excellent synergistic effect with mugwort extract. The compounding amount of these medicinal ingredients is 0.01 to 5% by weight, preferably 0.1 to 3% by weight based on the total amount of the composition.

(Plant Extract) The composition for external use of the present invention includes:
In addition, Jiyu, Morimatsuba, Sugiha, Lotus root, Three Ginseng, Jigoku skin,
It is preferable to mix at least one plant extract selected from Akane root and Clara. These plant extracts are produced by a known method. For example, extraction is performed as follows. 100 g of dried crude drug minced powder (in the case of a mixed extract, mix equal amounts of each crude drug minced powder)
Heat to reflux in 300 ml of 3% aqueous ethanol for 3 hours and filter through a glass filter. This process is repeated once more, the obtained filtrates are combined, and concentrated to dryness to obtain the desired product.
The amount of these plant extracts is 0.0001 in terms of solid content.
３3% by weight. If the amount is less than 0.0001% by weight, the moisturizing feeling will not be maintained.

(Preparation of Patch) The patch of the present invention is generally referred to as a poultice, and is used to support a gel-like plaster containing a water-soluble polymer gel-forming agent such as gelatin, a filler such as kaolin and water and a non-woven fabric or the like. A typical example is a form applied to the body and covered with a liner such as a plastic film.
In the water-containing gel-like plaster, in addition to water, a polyhydric alcohol such as glycerin, propylene glycol, 1,3-butylene glycol, sorbitol, polyethylene glycol, propylene glycol mannitol can be used as a wetting agent.

Examples of the gel-forming agent include polyacrylic acid / a salt thereof, gelatin, casein, carrageenan, methylcellulose, carboxymethylcellulose, polyvinyl alcohol, hydroxypropylcellulose, sodium alginate, xanthan gum, polyvinyl alcohol and pullulan. As a filler, kaolin, bentonite, zinc oxide, titanium oxide, talc,
Silicic anhydride and the like can be mentioned.

The gel-like plaster may further contain a crosslinking agent, a surfactant, a pH adjuster, and the like, if necessary.
Examples of the crosslinking agent include glycinal, hydrous aluminum silicate, aluminum hydroxide, and alumina / magnesium hydroxide. Examples of the surfactant include polyoxyethylene hydrogenated castor oil, propylene glycol fatty acid ester, polyoxyethylene sulbitan fatty acid ester, glycerin fatty acid ester, sorbitan fatty acid ester, polyethylene glycol fatty acid ester, and polyoxyethylene monostearate.

As the pH adjuster, lactic acid, tartaric acid, citric acid, gluconic acid, malic acid, maleic acid, etc. can be used. The amounts of these components are as follows:
20% by weight, 10 to 70% by weight of water, 10 to 50% by weight of wetting agent, 0.005 to 5% by weight of crosslinking agent, 0.1 to 10% of surfactant
A range of 5% by weight and a pH adjuster of 1 to 10% by weight is preferable. Further, in addition to the above components, additives usually used in external preparations can be appropriately compounded. For example, humectants such as sodium hyaluronate, sodium chondroitin, urea, maltitol, sodium lactate, placenta,
Peppermint oil, lavender, camomile, eucalyptus, rosemary, orange, rose, cucumber, sage,
Fragrance ingredients such as oils / extracts and menthol, such as extracts of lime, lemon, bergamot, saffron, etc.
Preservatives such as vitamins such as tocopherol and paraoxybenzoic acid esters are included.

The support is not particularly limited, but may be a nonwoven fabric such as polyester, polypropylene, or rayon, a woven fabric, a knitted fabric, or a film of an elastomer such as polyethylene, polypropylene, or polyurethane that can be applied to the skin without causing discomfort. It is selected from a sheet or the like. The skin patch of the present invention is applied once or twice a day to a dermatologically irritated part such as senile pruritus, dry pruritus, or atopic sensation. Prevent
Improvement of symptoms such as skin swelling and inflammation and suppression of itch are maintained, and their effects are maintained. Furthermore, the skin diseased part is covered and protected by the patch, and can be avoided from external stimuli.

[0019]

Next, the present invention will be described in more detail with reference to Examples and Comparative Examples. It goes without saying that the present invention is not limited to these embodiments. Unless otherwise specified, [%] in Examples means [% by weight].

Examples 1 to 3 The components shown in Table 1 below were uniformly kneaded using a humidifying mixer according to a conventional method.
Immediately apply the obtained gel-like plaster on the nonwoven fabric in an amount of 10
It was rolled to 00 g / m ² and covered with a polyester film to prepare a skin patch. [Comparative Examples 1 and 2] A plaster was prepared in the same manner as in the Example, except that the extract was prepared by removing the extract components and the antihistamine and the antipruritic except for the antipruritic agent.

[0021]

[Table 1] Formulation of skin patch

[Results] The patch samples (10 cm × 14 cm) obtained in Examples and Comparative Examples were used in patients with subjective symptoms as follows, and the progress was confirmed. 20 patients with atopic dermatitis in their 10s and 60s were affixed to the affected skin at bedtime for 5-8 hours at bedtime, and the changes in their symptoms were evaluated and evaluated on a 10-point scale. Is 1). Table 2 shows the results. By adding the mugwort extract component, the improvement was superior to the case of the drug component alone.

[0023]

[Table 2] Improvement of subjective symptoms 度 Improvement of symptoms (average value) Symptom Before use After 2 weeks After 4 weeks ───────────────────────────────── Example 1 Itching 10 2. 2 2.2 Drying (Roughness) 10 6.0 3.2〃2 Itching 10 2.2 1.8 Drying (Roughness) 10 3.6 2.2〃3 Itching 10 1.8 1.4 Drying ( 10 3.0 1.6 〃 4 Itching 10 1.8 1.4 Dry (scratch) 10 4.0 2.6 ──────────────────比較 Comparative Example 1 Itching 10 2.0 2.0 Drying (Roughness) 10 4.8 3.0 〃 2 Itching 10 7.6 6.4 Drying ( Roughness) 10 6.4 3.8 ━━━━━━━━ ━━━━━━━━━━━━━━━━━━━━━━━━

[0024]

EFFECT OF THE INVENTION The skin outline patch of the present invention has a moisturizing effect and exhibits a long-lasting antipruritic effect.

 ──────────────────────────────────────────────────続 き Continued on the front page F term (reference) 4C076 AA72 AA81 BB31 CC18 DD27 DD28 DD29 DD37A DD38 DD43 DD45R DD46 DD49A DD52A EE09A EE23A EE32A EE42 EE53 EE58A FF31 4C083 AA111 AA112 AB242 AB372 AC442 AC432AC302 AC302 AD092 AD272 AD432 CC03 DD22 DD27 EE12 EE13 4C088 AB03 AB14 AB18 AB29 AB39 AB48 AB51 AB59 AC04 AC05 AC11 AC13 BA08 BA09 BA10 MA02 MA08 MA32 MA63 NA12 ZA89

Claims (4)

[Claims] An external skin patch comprising a mugwort extract and at least one drug component selected from an antihistamine and an antipruritic. 2. The skin according to claim 1, further comprising at least one plant extract selected from the group consisting of Jiuyu, Juniper, Sugiha, Lotus root, Three ginseng, dermis, Akane root and Clara. External patch. 3. The external patch for skin according to claim 1, further comprising a bactericide. 4. The external patch for skin according to claim 1, wherein the patch has a moisturizing property and an antipruritic property.