JP2793278B2 - Crude drug patch preparation - Google Patents

Description

Description: FIELD OF THE INVENTION The present invention relates to a herbal patch containing at least one of hamamelis extract, tincture, and powder as a medicinal ingredient, and particularly to a patch formed outside the human body or on a mucous membrane. It is used for healing or alleviating inflammation.

(Prior Art) Oral preparations such as tablets and capsules, suppositories and ointments are commercially available as preparations containing Hamamelis, and these are mainly used for alleviating the symptoms of hemorrhoids.

However, long-term administration as an oral preparation may cause gastrointestinal disorders and the like. Suppositories, on the other hand, tend to be less preferred and practically difficult to use. There is also a disadvantage that the medicinal effect does not last for a long time. Ointments adhere to clothing due to stickiness or insufficient drying after rubbing, causing discomfort, and rubbing on mucous membranes is accompanied by strong pain. There are disadvantages.

(Technical problem) Hamamelis virginiana L. is obtained by drying the leaves or leaves and bark of the American witch hazel Hamamelis virginiana L. (Hammelidaceae) produced in North America. Furthermore, extract it by making it coarse powder and leaching it with a mixed solution of ethanol and water, and concentrating the liquid,
Alternatively, it is used as a crude drug in the form of a tincture prepared by leaching with a mixed solution of ethanol and water or ethanol, or a powder obtained by drying and crushing Hamamelis.

According to the recognition of the inventor, hamamelis contains hamamelitannin, saponin and the like in its components and has an astringent action, and also exhibits an anti-inflammatory effect against eczema, burns, hemorrhoids, etc., which are inflammations outside the human body. is there. However, oral preparations, suppositories and ointments have the above-mentioned problems, so that the dosage form must be carefully selected.

Patches can be mentioned as transdermal preparations that can directly expect an anti-inflammatory effect in external inflammation, do not cause side effects such as gastrointestinal disorders, and maintain the medicinal effect to some extent.

At present, there is increasing interest in medicine, not only in the medical and pharmaceutical industries, but also in the administrative and social fields, and safety and efficacy of all drugs are increasingly demanded. . Transdermal preparations must also have the prospect of meeting such demands. The drug should ideally be present in the required target organ or tissue in the required minimum amount at the required time. The extra drug is not only wasteful but also increases the side effects. Further, since the pharmacological action is manifested by the drug concentration at the point of action and the contact time, it is necessary to maintain the required minimum concentration at the required site, that is, to maintain the predetermined concentration in a steady state. However, the conventional oral medicine has a problem that the absorption rate and the blood concentration pattern have large individual differences, and therefore, in order to satisfy the above conditions, it is necessary to use a transportation method that can be controlled without being influenced by individual factors. . The patch most suitable for the above needs is a patch as a transdermal preparation.

The present invention has been made in view of the above circumstances, and an object of the present invention is to solve the above-described drawbacks or problems. Specifically, Hamamelis is used as a main component to directly treat inflammation outside the human body or mucous membrane. Demonstrates anti-inflammatory effect, does not cause problems such as discomfort after application and troublesome usage, and it can administer the necessary minimum amount to the required site regardless of individual differences, An object of the present invention is to provide a crude drug patch preparation exhibiting sustainability.

(Technical means) The object is to provide a patch for herbal medicine characterized in that at least one of hamamelis extract, tincture and powder is blended in a base for patch as an essential medicinal ingredient. Can be achieved.

Examples of the mold include a cataplasm, a plaster, and a mucosal patch. The present invention is directed to a plaster and a mucosal patch. In any case, the content of Hamamelis is preferably 0.1 to 20% by weight based on the total amount. The term "total amount" refers to the whole amount of the plaster, that is, the whole except for the support in the case of a plaster, and the whole except for the release paper in the case of a mucosal patch.

 Hereinafter, the method for producing the patch preparation of the present invention will be briefly described.

Production method of cataplasm: at least one of hamamelis extract, tincture, and powder is dissolved or dispersed in water or alcohol, kneaded into a water-soluble polymer such as sodium polyacrylate, and, if necessary, an adhesive, Fillers, humectants,
A crosslinking agent, a pH adjuster, etc. are added, kneaded and mixed, and spread into a nonwoven fabric or the like.

Production method of plaster: At least one of hamamelis extract, tincture and powder is dissolved or dispersed in a solvent such as water, alcohol or toluene, and natural and synthetic rubbers and resins of tackifier are heated. Add evenly to the melt and or dissolved in the solvent and mix uniformly, if necessary, softener,
A filler, an antioxidant and the like are added, spread on a support, dried and manufactured.

Production method of mucosal patch: Hamamelis extract, tincture,
At least one of the powders is dissolved or dispersed in water or alcohols, and added to a polymer compound (hydroxypropylcellulose, polyvinylpyrrolidone, etc.) dissolved in water, alcohols or a solvent, etc. to form a uniform liquid, If necessary, a softener, a tackifier, an antioxidant and the like are added, and the mixture is spread on a support, dried and manufactured.

As the base component for plaster agent, for example, natural rubber,
Rubber-based film-forming substances such as styrene-butadiene copolymer (SBR), styrene-isoprene-styrene copolymer elastomer (SIS), and silicone rubber, such as acrylic resin, petroleum resin, rosin, hydrogenated rosin, and ester gum Tackifiers such as concentrated glycerin, polybutene, liquid paraffin, softeners such as isopropyl myristate and the like can be mentioned. As the base component for the mucosal patch, for example, polysaccharides such as starch, for example, natural polymer compounds such as gelatin, xanthan gum, karaya gum, agar, and water-soluble compounds such as carboxyvinyl polymer, sodium polyacrylate, polyvinyl alcohol, and polyvinylpyrrolidone Examples of the hydrophilic polymer include cellulose derivatives such as methylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose phthalate, cellulose acetate phthalate, and carboxymethylethylcellulose.

The present invention is characterized in that at least one of hamamelis extract, tincture and powder is blended as an essential medicinal active ingredient, but in addition to this, other active ingredients may be blended.

Other active ingredients include methyl salicylate, glycol salicylate, salicylic acid, l-menthol, dl-menthol, d-camphor, dl-camphor, borneol, thymol, peppermint oil, eucalyptus oil, which are usually used in patches. Turpentine oil, clove oil, etc., antihistamine diphenhydramine and its salts, chlorpheniramine and its salts, etc.cortisone having anti-inflammatory action, cortisone acetate, hydrocortisone, hydrocortisone acetate, prednisone,
Corticosteroids such as prednisolone, dexamethasone, dexamethasone acetate, and betamethasone; antipruritic agents such as crotamiton; anti-inflammatory agents such as glycyrrhetinic acid, pyridoletin, and ictamol; chlorhexidine hydrochloride;
Disinfectants such as isopropylmethylphenol, acrinol, cetylpyridinium chloride, and decalinium chloride; local anesthetics such as dibucaine and dibucaine hydrochloride; vitamins such as tocopherol acetate, ergocasiferol, retinol palmitate, and pyridoxine palmitate. I can do it.

(Effects of the Invention) The crude drug patch preparation of the present invention contains at least one of hamamelis extract, tincture and powder as an essential active ingredient in a patch at a ratio of 0.1 to 20% by weight to the external inflammatory part of the human body. The following effects can be exerted by sticking on the surface.

Demonstrates anti-inflammatory effect by combining Hamamelis, bruising,
It has an effect on sprain, muscle pain, back pain, stomatitis, gingivitis, toothache, external hemorrhoids, cut hemorrhoids, pruritus, hemorrhoid pain, anal congestion, and various inflammations.

By making a patch, a certain drug delivery can be obtained from the preparation during the patching period, and it is stable and persistent, and exhibits an excellent anti-inflammatory effect locally. As a result, it alleviates various inflammations and leads to a better way.

The use of a patch does not cause discomfort such as stickiness after rubbing and adhesion to clothing due to insufficient drying like ointments, creams and liquids.

By using a patch, it has good adhesiveness to skin and mucous membranes, so that it is easy to use.

By determining the area by the number of sheets used or cutting,
One dose can be appropriately set, and the drug can be easily removed when a side effect occurs.

Therefore, according to the present invention, the excellent medicinal properties of Hamamelis can be sufficiently utilized, and at the same time, it is possible to maintain a selective and predetermined drug concentration at a predetermined site by using a patch,
It is an excellent drug that is consistent with the basic concept of the ug Delivery System (DDS). Further, by adding other active ingredients as shown from the anti-inflammatory effect of the examples, it is possible to provide an extremely useful crude drug patch preparation such that an additive and synergistic effect can be expected. Was completed.

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

Example (1) An appropriate amount of toluene was added to 8.8% of polybutene, 47.5% of petroleum resin (Quinton RU-185, manufactured by Zeon Corporation) and 31.7% of SIS (Califlex R TR-1107, manufactured by Shell Chemical Co., Ltd.) by weight ratio. After heating and dissolving, after cooling, add a solution of Hamamelis extract 4.0% in benzyl alcohol 8.0%, mix uniformly, apply and spread in a uniform thickness on a vinyl chloride film as a support. Then, toluene was distilled off to produce a plaster according to the present invention.

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

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

Example 4 50.5% of polyvinylpyrrolidone, 40% of hydroxypropylcellulose, and 0.5% of hamamelis extract were stirred and dissolved in an appropriate amount of ethanol by weight ratio, and 9.5% of propylene glycol was further added to obtain a uniform liquid, which was placed on a release paper. It was spread and dried to produce the mucosal patch according to the present invention.

Example (5) Example 4 was prepared according to the composition shown in the column of Example 5 in Table 3.
A mucosal patch was produced in the same manner as described above.

Example (6) Example 4 was prepared according to the composition shown in the column of Example 6 in Table 3.
A mucosal patch was produced in the same manner as described above.

Reference Example 1 In terms of weight ratio, sodium polyacrylate 4.0%, methoxyethylene maleic anhydride copolymer 1.0%, carboxymethyl cellulose sodium 1.0%, gelatin 2.0%, concentrated glycerin 10.0%, D-sorbitol solution 30.0%, kaolin 15.0% , 1.0% of magnesium hydroxide hydroxide and 30.0% of purified water were dissolved and kneaded at 50 ° C to prepare a plaster base comprising a water-soluble polymer, and 1.0% of Hamameris extract was added as an active ingredient to 5.0% of purified water. And a mixture was prepared while stirring at 40 ° C., and the mixture was applied to a nonwoven fabric as a support for a poultice at a uniform thickness to produce a poultice according to the present invention.

Reference Example 2 According to the composition shown in the column of Reference Example 2 in Table 2, Reference Example 1
A cataplasm was prepared in the same manner as described above.

Reference Example 3 A poultice was produced in the same manner as in Reference Example 1 using the composition shown in Reference Example 3 in Table 2.

Carrageenin Footpad Edema Inhibition Test The right instep of the rat was shaved with an electric clipper, and 0.1 ml of a 1% carrageenin solution was injected subcutaneously into the footpad as an inflammatory agent, and the test drug was immediately applied to the instep. 5 after inflammation injection
Remove only when measuring hourly foot volume (every hour) and apply again. Controls shall not have test drug applied.
The results are as shown in the figure. According to the figure, it can be confirmed that the herbal patch preparation of the present invention exerts a remarkable anti-inflammatory effect due to the combination of Hamamelis extract.

[Brief description of the drawings]

The drawing is a graph showing the test results for confirming the effect of the crude drug patch preparation according to the present invention.

──────────────────────────────────────────────────続 き Continuation of the front page (56) References JP-A-1-128934 (JP, A) JP-A-1-128933 (JP, A) JP-A 64-83024 (JP, A) JP-A 64-64 90131 (JP, A) JP-A-58-85817 (JP, A) JP-A-57-156761 (JP, A) (58) Fields investigated (Int. Cl. ⁶ , DB name) A61K 35/78

Claims (4)

(57) [Claims] (1) Whether at least one of hamamelis extract, tincture and powder is blended as an essential medicinal ingredient in a base for a plaster comprising a rubber-based film-forming substance, a mucosal agent and a softener. Or a water-soluble polymer compound,
And a crude drug patch comprising a cellulose derivative and a base for a mucosal patch which can contain at least one selected from other polysaccharides and natural polymer compounds. 2. The amount of at least one of the hamamelis extract, tincture and powder is 0.1 to 20% by weight of the total amount.
The crude drug patch preparation according to claim 1, which is: 3. The rubber-based film-forming substance is at least one selected from the group consisting of natural rubber, styrene-butadiene copolymer, styrene-isoprene-styrene copolymer elastomer, and silicone rubber. The imparting agent is at least one selected from the group consisting of acrylic resin, petroleum resin, rosin, hydrogenated rosin, and ester gum, and the softener is a group consisting of concentrated glycerin, polybutene, liquid paraffin, and isopropyl myristate. 2. The method according to claim 1, wherein the base material for the plaster is at least one selected from the group consisting of:
The crude drug patch preparation according to the above item. 4. The water-soluble polymer compound is at least one selected from the group consisting of carboxyvinyl polymer, sodium polyacrylate, polyvinyl alcohol and polyvinylpyrrolidone, and the cellulose derivative is methyl cellulose, hydroxypropyl cellulose. , Hydroxypropylmethylcellulose phthalate, cellulose acetate phthalate, one or more selected from the group consisting of carboxymethylethylcellulose, the polysaccharide is starch, the natural polymer compound is gelatin, xanthan gum, karaya gum, agar 1 selected from the group
The herbal patch preparation according to claim 1, wherein a base for mucosal patches of at least one kind is used.