JPH0377829A - Crude drug plaster preparation - Google Patents

Abstract

PURPOSE:To obtain a crude drug plaster preparation exhibiting direct anti- inflammatory effect against the external inflammation of human body by using the extract, tincture and/or powder of hamamelis as an essential component of pharmacodynamically effective substance and compounding the component to a base having the form of a film or sheet. CONSTITUTION:The extract, tincture and/or powder of hamamelis is used as an essential component of pharmacodynamically effective substance and is compounded (applied or spread) to a base having film or sheet form (e.g. supporting material for poultice, supporting material for plaster or releasing paper) in an amount of 0.1-20wt.% (based on the whole plaster excluding releasing paper) to obtain the objective crude drug plaster preparation such as poultice, plaster and agent to be applied to mucous membrane. The preparation exhibits direct anti-inflammatory effect against the external inflammation of human body (e.g. eczema, scald or hemorrhoid), is free from the problems such as disagreeable feeling after application and the troublesome handling in use, capable of administering the necessary minimum amount of the drug independent of the individual difference and keeps the drug action over a log period.

Description

DETAILED DESCRIPTION OF THE INVENTION (Field of Industrial Application) The present invention relates to a herbal medicine patch containing Hamamelis as a medicinal substance, and is particularly used for treating or alleviating inflammation occurring outside the human body.

(Prior Art) As preparations containing Hamamelis, oral preparations such as tablets and capsules, suppositories and ointments are commercially available, and these have medicinal effects mainly for alleviating the symptoms of hemorrhoids.

However, if it is administered as an oral agent for a long period of time, it may cause gastrointestinal disorders. On the other hand, there is a tendency that people do not like the use of sitting-cutting, and it is actually difficult to use. Another disadvantage is that the medicinal effect does not last for a long time. Ointments tend to stick to clothing after application or are insufficiently dry, causing discomfort; application to mucous membranes is accompanied by strong pain; and the amount applied per time varies, making it difficult to administer a fixed amount. There are drawbacks such as:

(Technical issue) Hamamelis virginian
a I7,) is an American witch hazel produced in North America.
amelis virginiana L, (dried leaves or leaves and bark of the family Amelidae) It is used as a crude drug in the form of a tincture made by infusing it with ethanol or a mixture of ethanol and water, or as a powder made by drying and pulverizing Honjima.

According to the inventor's knowledge, hamamelis contains hamamelitannin, zabonin, etc., and has an astringent effect as well as an anti-inflammatory effect against external inflammation of the human body such as eczema, burns, and hemorrhoids. It is something. However, oral preparations, suppositories, and ointments have the above-mentioned problems, so the dosage form! i must choose carefully.

A patch can be used as a transdermal absorption preparation that can directly be expected to have an anti-inflammatory effect on external inflammation, does not cause side effects such as gastrointestinal disorders, and has a long-lasting medicinal effect.

Currently, interest in medicine is increasing not only in the medical and pharmaceutical industries, but also in the administrative and social aspects, and all drugs are required to be even more safe and effective. Transdermal preparations also need to have the outlook to meet these demands. Ideally, a drug should be present in the required target organ or tissue at the required minimum amount at the required time. drug on the door,
This is because excess drugs are not only wasteful but also increase side effects. Furthermore, since the pharmacological action is expressed depending on the drug concentration and contact time at the point of action, it is necessary to maintain the required minimum concentration at the required site, that is, to maintain a predetermined concentration in a steady state. However, conventional oral preparations have the problem of large individual differences in absorption rate and blood concentration pattern, so in order to meet the above conditions, it is necessary to use a delivery method that can be controlled without being influenced by individual factors. . A transdermal patch is a transdermal preparation that can meet the following needs.

The present invention has been made based on the above-mentioned circumstances, and its purpose is to solve the above-mentioned drawbacks and problems. It exerts an inflammatory effect, does not cause problems such as discomfort after application or troublesome administration, and can be administered in the minimum amount to the required area regardless of individual differences, and has a long-lasting effect. Our goal is to provide herbal medicine patch preparations that exhibit the following effects. .

(Technical means) The above object is characterized in that one or more of Hamamelis extract, tincture, and powder is blended into a film or sheet-like base as an essential component of a medicinal substance. This can be achieved through herbal medicine patch preparations.

The dosage form can be a poultice, plaster scraping, or mucosal patch, and in either case, the medicinal ingredients of Hamamelis are 0.1-20% by weight of the total amount.
is good. Note that the total amount refers to the entire amount of the precursor, that is, the entire amount excluding the respective support in the case of poultices and plasters, and the entire amount excluding the release paper in the case of mucous membrane patches.

Components of the pre-application base include polyacrylic acid, 1-lium polyacrylate, me-1-xyethylene maleic anhydride copolymer, polyvinyl alcohol 1 habolyvinylpyrrolidone, sodium alginate, sodium carboxymethyl cellulose, Gelatin, concentrated glycerin, D-sorbitol liquid, kaolin, aluminum compound, natural rubber, styrene-butadiene copolymer (SBR), Step 1
/Isobrene-styrene copolymer elastomer (S
IS ), silicone rubber, petroleum resin, rosin, hydrogenated rosin, ester gum, polybutene, liquid paraffin, isopropyl myristate, acrylic resin, starch, xanthun gum, karaya gum, methyl cellulose, carboxyvinyl polymer droxypropyl cellulose, hydroxypropyl methyl cellulose lid l/-)-, cellulose acetate phthalate, carboxymethylethylcellulose, etc. The present invention provides extracts, tinctures, and powders of Hamamelis. 1
It is characterized by containing one or more species as essential components of medicinal substances, but in addition to this, other active ingredients may also be blended.

Other active ingredients include methyl salicylate, glycol salicylate, ethyl non-glycol salicylate, salicylic acid, β-menthol, dj2-menthol, d-camphor, df2-camphor, borneol, and thymol, which are commonly used in patches. , pepper oil, eucalyptus oil,
Te1/vinyl oil, clove oil, etc., antihistamines such as diphenhydramine and its salts, chlorpheniramine and its salts, etc.

Cordecine, cortisone acetate, hydrocortisone, hydrocortisone acetate, prednisone, which have anti-inflammatory effects.
Adrenal corticosteroids such as prednisolone, dexamethacin, dexamethacin acetate, betamethacin, anti-pruritic agents such as crotamiton, anti-inflammatory agents such as glycyrrhetinic acid, pyridretin, ictamol, chlorhexidine hydrochloride, chlorhexidine gluconate,
Disinfectants such as isopropyl methylphenol, acrinol, cetylpyridinium chloride, and dequalinium chloride, local anesthetics such as dibucaine and dibucaine hydrochloride, and acetic acid!・
Vitamins such as coferol, ergocalciferol, sidinol valmitate, and pyridoxine valmidate can be added.

(Effects of the Invention) The herbal medicine patch preparation of the present invention uses one or more of the novel Hamamelis extract, tincture, and powder as an essential ingredient of the medicinal substance for the topical patch. Mix o, i ~ 20% by weight with the drug and apply it to the external inflamed area of the human body (-=
-1 produces the following effects.

■The ingredients of Hamamelis exert anti-inflammatory effect, which can reduce bruises and
It is effective against sprains, muscle pain, lower back pain, stomatitis, gingivitis, toothache, external hemorrhoids, hemorrhoids, pruritus, hemorrhoid pain, anal congestion, and various other inflammations.

■Since it is a single patch, the above effects are extremely long-lasting, and as a result, it alleviates various inflammations and leads to recovery.

■Since it is a patch, unlike ointments, creams, and liquids, it does not cause discomfort such as stickiness after application or adhesion to clothing due to insufficient drying.

■Since it is a patch, it has good adhesion to the skin and mucous membranes, making it easy to use. ■The area is determined by the number of sheets to be used or by cutting them, so
It is easy to set a single dose, and - a fixed amount can be administered.

Therefore, according to the present invention, the excellent medicinal efficacy of Hamamelis can be utilized, and at the same time, the medicinal efficacy itself is enhanced by making it into a patch, and as shown by the anti-inflammatory effect in the examples, other active ingredients can be used. By blending these ingredients, we were able to provide a highly useful crude drug patch preparation that can be expected to have additive and synergistic effects.

(Example) Examples will be described below, but the present invention is not limited thereto.

Example (1) By weight, polybutene 8.8% 1 Petroleum resin (Nippon Zeon Co., Ltd., Finton R0485) 47.5%, 5IS (
Manufactured by Shell Chemical Co., Ltd., Kaliflex RTR-1107) 3
Add an appropriate amount of toluene to 1.7% and dissolve by heating. After cooling, add 4.0% Hamamelis extract dissolved in 8.0% benzyl alcohol and mix uniformly. After spreading, dissolve in toluene. was distilled off and coated on a vinyl chloride film as a support to a thickness of -2 to produce a plaster according to the present invention.

Table 1 Example (2) A plaster agent was manufactured in the same manner as Example 1 using the composition shown in the Example 2 column of Table 1.

Example (3) A plaster was produced in the same manner as in Example 1 using the composition shown in the Example 3 column of Table 1.

Example (4) Layer ratio: 4.0% sodium polyacrylate, 1.0% methoxyethylene maleic anhydride copolymer, 1 sodium carboxymethyl cellulose. 0%, gelatin 2.
0%, concentrated glycerin 1060%, D-sorbitol solution 3
0°0%, kaolin 15.0%, aluminum compound 1
．． A plaster base consisting of a water-soluble polymer was prepared by dissolving and kneading 0% and 30.0% of purified water at 50°C, and to this was added 160% of Hamamelis aegis as an active ingredient and 5.0% of purified water.
and prepare a mixture with stirring at 40 °C,
This was applied to a nonwoven fabric as a support for a poultice to a varying thickness to produce a poultice according to the present invention.

Table 2 Example (5) A bag agent was produced in the same manner as Example 4 using the composition shown in the Example 5 column of Table 2.

Example (6) A poultice was produced in the same manner as in Example 4 using the composition shown in Example 6 in Table 2.

Example (7) Polyvinyl pyrrolidone 50.0%, hydroxypropyl cellulose 40%, Hamamelis aegis 0.5% in terms of weight ratio
was stirred and dissolved in an appropriate amount of ethanol, and 9.5% propylene glycol was further added to obtain a homogeneous liquid, which was spread on release paper and dried to produce a mucosal patch according to the present invention.

Table 3 Example (8) A mucosal patch was produced in the same manner as Example 7 using the composition shown in the Example 8 column of Table 3.

Example (9) A mucosal patch was produced in the same manner as in Example 7 using the composition shown in the Example 9 column of Table 3.

Carrageenin paw edema suppression test The fur on the right instep of rats was shaved with electric clippers, and 0.1 mβ of 1% carrageenan solution was subcutaneously injected into the paw as an inflammatory agent, and the test drug was immediately applied to the instep. . It is removed and reapplied only when measuring foot volume (hourly) for 5 hours after injection of the inflammatory agent. The test drug shall not be applied to the control. The results are as shown in the figure, and it can be confirmed from the figure that the herbal medicine patch of the present invention exhibits a remarkable anti-inflammatory effect due to the combination of Hamamelis extract.

[Brief explanation of drawings]

The figure is a graph showing the test results to confirm the effect of the medicinal patch preparation according to the present invention.

Claims (1)

[Scope of Claims] (1) One or more of Hamamelis extract, tincture, and powder is blended into a film or sheet-like base as an essential component of a medicinal substance. Herbal medicine patch preparations. (2) The herbal medicine patch preparation according to claim 1, wherein the preparation is a poultice, and a base containing Hamamelis is applied to a support for the poultice. (3) The herbal medicine patch preparation according to claim 1, wherein the preparation is a plaster, and the base containing Hamamelis is coated on a support for the plaster. (4) The crude drug patch preparation according to claim 1, wherein the preparation is a mucous membrane patch, and the base containing Hamamelis is spread on a release paper. (5) The blending amount of one or more of Hamamelis extract, tincture, and powder is 0.1 to 20% by weight of the total amount.
The crude drug patch preparation according to any one of claims 1 to 4.