JP2013095687A - Intraoral adhesive preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an intraoral adhesive preparation having a sufficient sorption effect on the oral mucosa, and sufficient safety even in the case of accidental ingestion.SOLUTION: There is provided an intraoral adhesive preparation 1 of a film shape, for attaching on a mucosa in the oral cavity to absorb the active ingredient into the body through the mucosa, which comprises a medicinal ingredient layer 2 comprising a round shape film and a cover layer 3 covering the surface except a contacting surface 10 of the medicinal ingredient layer 2 and contacting the mucosa of a user, and having a U-shaped cross section, and forms a disc shape as a whole, and whose holding part for making the intraoral adhesive preparation easily held is provided with a projection set at almost the center of the non-contacting surface of the opposite side surface to the contacting surface.

Description

  The present invention relates to an intraoral patch, and more particularly to an intraoral patch that can be applied to a mucosal surface at any location in the oral cavity and can absorb various drugs into the body through the mucous membrane. .

Various drugs have been developed that absorb medicinal ingredients from the mucous membrane in the oral cavity when performing various treatments.
However, if a medicine composed of an ointment or gel is simply applied to the oral cavity, the applied medicine will be washed away due to the action of saliva or the like. For example, when a drug for periodontal disease is applied to the affected area, there is a problem that an amount showing a sufficient medicinal effect is not absorbed by the affected area. When a drug for systemic diseases is applied, absorption from the mucous membrane is not absorbed. There is a problem that the advantage is not fully exhibited although it is more advantageous in terms of absorbency than absorption from the above.
Therefore, various oral patches in the form of films and sheets, not ointments and gels, have been proposed.
For example, Patent Document 1 proposes an edible intraoral patch characterized by laminating a drug layer on a support made of an edible polymer substance. Patent Document 2 proposes an oral mucosal patch preparation in which a drug layer made of an edible film is sandwiched between two support layers made of an edible film. Patent Document 3 proposes an intraoral patch comprising a support having a spunlace nonwoven fabric and a plaster composition having adhesiveness to teeth or gums.

JP 58-174307 A

JP 2010-138123 A

JP 2010-168370 A

However, the oral patch according to the above-mentioned proposal is still insufficient. Specifically, the intraoral patch described in Patent Document 1 has a problem that the drug layer is dissolved by dissolving the support and the effect of being stuck in the oral cavity for a long time hardly occurs. It was. In the intraoral patch described in Patent Document 2, one of the two supports is affixed to the mucous membrane, and one is exposed to the oral cavity. The exposed support is first dissolved and the drug layer is formed. There was a problem that it was exposed to the oral cavity and dissolved before being absorbed through the mucous membrane. The intraoral patch described in Patent Document 3 has a problem that the plaster composition dissolves from the gap between the support and the mucous membrane, and also has a problem in terms of safety because it swallows the spunlace nonwoven fabric. It was.
In short, the conventionally proposed oral patches still do not satisfy the absorption effect in the oral mucosa and the safety in case of accidental ingestion, and satisfy all these performances. It is the present situation that development of is demanded.

  Accordingly, an object of the present invention is to provide an intraoral patch having a sufficient absorption effect in the oral mucosa and having sufficient safety even if it is accidentally swallowed.

As a result of intensive studies to solve the above-mentioned problems, the present inventors have included an edible film in an edible film attached to the mucous membrane in the oral cavity, and the surface of the edible film has poor solubility than the edible film. The inventors have found that the above problems can be solved by coating with a film, and have completed the present invention.
That is, this invention achieves the said objective by providing the following invention.
1. An intraoral patch that is applied to the mucous membrane in the oral cavity in the form of a film and the active ingredient is absorbed into the body through the mucosa,
A film-shaped drug ingredient layer that contains an edible water-soluble base and a drug, and is attached to the oral mucosa of the user,
Covers the surface other than the contact surface that contacts the user's mucous membrane in the medicinal component layer, is less water-soluble than the water-soluble base, or expresses stickiness in the oral cavity than the water-soluble base An oral patch comprising a coating layer containing an edible coating base that does not.
2. 2. The intraoral patch according to 1, wherein a grasping part that facilitates clamping of the intraoral patch is provided.
3. The intraoral patch according to 2, wherein the gripping part is formed by providing a protrusion at substantially the center of a non-contact surface that is the surface opposite to the contact surface.
4). The intraoral patch according to 2, wherein the gripping part is formed by providing a protrusion on a part of the periphery of the coating layer.
5. 2. The intraoral patch according to 1, wherein a mark portion for performing various treatments is provided in the central portion of the coating layer.
6). 6. The intraoral patch according to 5, wherein the mark portion is formed by coloring a non-contact surface that is a surface opposite to the contact surface.
7). The water-soluble base is a base selected from the group consisting of pullulan, polyvinyl alcohol (PVA), hydroxypropylcellulose (HPC), polyvinylpyrrolidone (PVP), gelatin, starch, and mixtures thereof;
2. The intraoral patch according to 1, wherein the coating base is a base selected from the group consisting of ethyl cellulose, hydroxypropyl methylcellulose acetate succinate, hypromellose phthalate, kanten and mixtures thereof.

  The intraoral patch of the present invention has a sufficient absorption effect on the mucous membrane of the oral cavity and has sufficient safety even if it is accidentally swallowed.

FIG. 1 is a diagram schematically showing one embodiment of an intraoral patch of the present invention, in which (a) is a perspective view and (b) is a thickness direction sectional view (b-b line sectional view). . 2A and 2B are diagrams showing another embodiment, in which FIG. 2A is a bottom view showing a contact surface, and FIG. 2B is a sectional view in the thickness direction (corresponding to FIG. 1B). FIG. 3 is a cross-sectional view in the thickness direction showing another embodiment (corresponding to FIG. 1B).

1 Intraoral patch, 2 drug component layer, 3 coating layer, 4 gripping part

Hereinafter, the intraoral patch of the present invention will be described in detail with reference to the drawings.
The intraoral patch 1 of this embodiment shown in FIG. 1 is a film that is attached to the mucous membrane in the oral cavity, and the active ingredient is absorbed into the body through the mucous membrane.
More specifically, the intraoral patch 1 of the present embodiment is composed of a circular film, and a drug component layer 2 (see FIG. 1 (b)) to be affixed to the user's oral mucosa, and the drug component layer 2 It covers a surface other than the contact surface 10 that contacts the user's mucous membrane, and is composed of a coating layer 3 having a U-shaped cross section, and has a disk shape as a whole.

  In addition, the intraoral patch 1 of the present embodiment is provided with a grip portion 4 that can be easily held using a gripping tool such as tweezers. The grip portion 4 is formed by projecting substantially the center of the surface of the coating layer 3 and providing a projection. The grip 4 can also be used as a mark when it is necessary to perform various treatments (for example, injection) at the stage of treatment.

The thickness of the drug component layer 2 is preferably 20 to 300 μm, more preferably 40 to 200 μm. The size of the medicinal component layer 2 is arbitrary depending on the type of medicinal component and the use of the intraoral patch, but a diameter of 0.5 to 1.5 cm is applied to the oral cavity. It is preferable from the viewpoint of a balance between feeling of use and efficacy.
The thickness of the coating layer 3 is preferably 50 to 400 μm, and more preferably 100 to 300 μm.
Moreover, it is preferable from a viewpoint of the usability | use_condition at the time of sticking in an intraoral area that the magnitude | size of the whole intraoral patch shall be 1-3 cm in diameter, and thickness shall be 70-700 micrometers.

<Formation material for drug component layer>
The drug component layer is formed of an edible film made of an edible water-soluble base and a drug. The edible film can be constituted by appropriately adding necessary additives to the water-soluble base.

The water-soluble base preferably has a 2% by weight aqueous solution having a viscosity at 20 ° C. of 2 to 100 mPa · s, more preferably 3 to 50 mPa · s. If the viscosity of the water-soluble base is less than 2 mPa · s, the film becomes brittle, and if it exceeds 100 mPa · s, the viscosity of the film solution becomes too high, and handling during production deteriorates, so it is preferably within the above range. .
As such a water-soluble base, those shown below can be used.
Polyvinylpyrrolidone, polyvinyl alcohol, polyacrylic acid, carboxymethylcellulose, starch, xanthan gum, karaya gum, methylcellulose, hydroxypropylcellulose (HPC), cellulose acetate phthalate (also known as cellulose acetate phthalate, CAP), carboxymethylethylcellulose (CMEC), hydroxy Ethylcellulose, hydroxypropylmethylcellulose (HPMC), carboxyvinyl polymer (trade name: Carbopol, manufactured by BF Goodrich), tragacanth, gum arabic, locust bean gum, guar gum, dextrin, dextran, amylose, potassium carboxymethylcellulose, carboxymethylcellulose sodium , Carboxymethylcellulose calcium, pullula , Chitosan, sodium carboxymethyl starch, plantago seed coat, galactomannan, Eudragit, casein, sodium alginate, alkyl alginate, gelatin, cellulose acetate, hydroxyethyl methylcellulose, water-insoluble methacrylic acid copolymer, ethyl methacrylate / methacrylic acid trimethyl Ammonium ethyl copolymer, dimethylaminoethyl methacrylate / methyl methacrylate copolymer, acrylic acid, methyl methacrylate copolymer, polyethylene glycol and the like.

  In addition, among the water-soluble bases described above, those that exhibit adhesiveness by the action of saliva when introduced into the oral cavity and exhibit high adhesion to the oral mucosa are preferred, specifically pullulan, A base selected from the group consisting of polyvinyl alcohol (PVA), hydroxypropyl cellulose (HPC), polyvinyl pyrrolidone (PVP), gelatin, starch and mixtures thereof is particularly preferably used.

Moreover, an emulsifier and a plasticizer can be mentioned as said additive.
The above emulsifier is a component for improving dispersibility of drugs and the like in the solution, and preventing the repellency from appearing on the substrate film that is the object to be coated when applying the edible film forming solution in the manufacturing process. And surfactants such as polyoxyethylene sorbitan oleate, sucrose fatty acid ester, polyglycerin fatty acid ester, soybean-derived lecithin, and the like, each of which can be used alone or in combination of two or more. it can. "Surf Hope" (trade name of sucrose fatty acid ester, manufactured by Mitsubishi Chemical Foods), "M-7D" (commercial product of polyglycerin fatty acid ester, manufactured by Mitsubishi Chemical Foods), "Sun lecithin A-1" Commercial products such as a commercial product of soybean-derived lecithin (manufactured by Taiyo Kagaku Co., Ltd.) and polysorbate 80HM (manufactured by NOF Corporation) can also be used.
The amount of the emulsifier used is preferably 0.1 to 10 parts by weight, more preferably 1 to 5 parts by weight with respect to 100 parts by weight of the water-soluble base.

The plasticizer is a component for imparting flexibility to the edible film, and examples thereof include glycerin, sorbitol, polyglycerin, and the like, and each can be used alone or in admixture of two or more. Commercial products can also be used.
The amount of the plasticizer used is preferably 5 to 50 parts by weight, more preferably 10 to 30 parts by weight, based on 100 parts by weight of the water-soluble base.

  In addition, the edible film may contain other additives, for example, a gelation accelerator such as potassium phosphate, malt reducing sugar syrup, sucrose, lactose, fructose, or saccharin as long as the desired effect of the present invention is not inhibited. Sweeteners such as aspartame, aspartame L-phenylalanine compound, sucralose, thaumatin, acesulfame potassium, stevia, peppermint, peppermint oil, cherry flavor, orange oil, fennel oil, ethyl maltol, l-menthol and other fragrances, benzoic acid, Preservatives such as sodium benzoate, benzyl benzoate, ethyl paraoxybenzoate, butyl paraoxybenzoate, propyl paraoxybenzoate, opacifiers such as titanium oxide, colorants such as iron sesquioxide, yellow iron sesquioxide; biguanite series Drugs, paeoniflorin, donepezil, ibupro Various medicinal components such as phen, butyl scopolamine bromide, chondroitin group, and isosorbite can also be used.

In addition, the intraoral patch of the present invention can also be colored on the base layer in order to impart a psychological healing effect to the patient. Coloring agents that can be used in this case include asenyakutannin powder, yellow ferric oxide, turmeric extract, brown iron oxide, carbon black, caramel, carmine, carotene solution, β-carotene, licorice extract, gold foil, silver foil, Platinum foil, black iron oxide, light silicic acid anhydride, titanium oxide, iron sesquioxide, edible blue No. 1, edible yellow No. 4, edible yellow No. 4 aluminum rake, edible yellow No. 5, edible yellow No. 5 aluminum rake, edible red No. 2, Edible Red No. 3, No. Edible Red No. 102, Talc, Copper Chlorophyllin Sodium, Copper Chlorophyll, Green Tea Extract, Octyldodecyl myristate, Medicinal Charcoal, Riboflavin, Riboflavin Butyrate, Riboflavin, Green Tea Powder, Rose Oil Etc. can be used.
In addition, addition of a fragrance or a sweetener is also effective in reducing the burden on treatment for the patient.

As the drug used in the present invention, a drug according to the following drug classification can be used. Specific examples thereof are listed in the following component column.
(Drug classification)
Antibacterial drugs, antiviral drugs, antifungal drugs, antiparasitic drugs, vaccination drugs, antiseptics, antineoplastic drugs, immunosuppressive drugs, corticosteroids, nonsteroidal anti-inflammatory drugs, antirheumatic drugs, anti-inflammatory enzymes, anti Histamine, Antiallergic, Diabetes, Hyperlipidemia, Gout and Hyperuricemia, Female Hormone, Male Hormone, Other Hormone, Thyroid Disease, Bone / Calcium Metabolism, Vitamin Formulation, Nutrient, Hematopoietic, Hemostatic, Antithrombotic, Antihypertensive, Angina, Antiarrhythmic, Heart failure / Pressor, Vasodilator, Diuretic, Bronchodilator, Respiratory, Antitussives, expectorants, gastrointestinal function regulators, peptic ulcer drugs, bowel disease drugs, laxatives, biliary tract disease drugs, liver disease drugs, pancreatic disease drugs, antipsychotic drugs, sleeping pills / anti-anxiety drugs, anti Antiepileptic drugs, migraine treatment drugs, antiemetics and antipruritic drugs A therapeutic agent for Parkinson's disease, cerebral circulation and metabolism improving drug, an anti-dementia drugs, autonomic agents, muscle relaxants, narcotics and similar drugs, anesthetic, antidote, herbal medicine, contrast agent, various nutrients, trace elements, such as (components)
Antibacterial agent: Antifungal agent such as cetylpyridinium chloride, protamine, l-menthol, etc .: Antiviral agent such as amphotericin B, miconazole, etc. Anti-inflammatory agent such as acyclovir, oseltamivir phosphate, etc. Anti-allergic drugs such as acetylsalicylic acid: steroids such as ketotifen fumarate, ozagrel hydrochloride, hormone drugs: antitussive expectorants such as prednisolone and estradiol: anesthetics such as noscapine, guaifenesin, tipepidine hibenzate bone, calcium such as lidocaine, tetracaine, dibucaine Metabolic drugs: anti-rheumatic drugs such as alfacalcidol and alendronate sodium: anti-thrombotic drugs such as methotrexate and infliximab: antibacterial drugs such as voglibose and pioglitazone hydrochloride: warfari Antihypertensive agents such as potassium, ticlopidine hydrochloride, etc .: Antigens such as atenolol, nifedipine, captolyl, losartan potassium, etc. Anti-arrhythmic agents such as amyl nitrite, trimetazidine hydrochloride, heart failure drugs such as procainamide hydrochloride, verapamil hydrochloride, vasopressors: digitoxin, hydrochloric acid Vasodilators such as dopamine: Diuretics such as isoxsuprine hydrochloride and trazoline hydrochloride: Bronchodilators such as furosemide: Peptic ulcers such as ephedrine hydrochloride and ipratropium bromide: Psychotropic drugs such as omeprazole and famotidine: Sleeping drugs such as chlorpromazine hydrochloride and fluvoxamine maleate・ Anxiolytic drugs: Parkinson's disease drugs such as barbital and triazolam: Levodopa, selegiline hydrochloride, bromocriptine mesylate and other cerebral circulation / metabolism improving drugs, anti-dementia drugs (dementia drugs): donepezil hydrochloride, etc. The mixing ratio of the agent, depending on each drug may be adjusted to satisfy the minimum effective concentration in the formulation has a known in each drug.

<Formation material of coating layer>
The coating layer is made of an edible film that contains an edible coating base that is less water-soluble than the water-soluble base or does not exhibit adhesiveness in the oral cavity than the water-soluble base. . That is, the following coating base is used in place of the water-soluble base, or the coating base is used as a main base, and the edible film is used for the above-described drug component layer except that the drug component is not contained. The same composition can be used.

The coating base used for the coating layer is a resin that is less soluble in water than the water-soluble base, or that does not exhibit adhesiveness in the oral cavity than the water-soluble base. These are relative ones that vary depending on what is used as the water-soluble base, and the difference in kinematic viscosity at 20 ° C. between 2% aqueous solution and the water-soluble resin (dynamic viscosity of the water-soluble base-coating the kinematic viscosity of use base agent) ^can be preferably used those which are 4mm ² / s~4000mm 2 / s.
Examples of coating bases that exhibit such tackiness include ethyl cellulose (EC), hypromellose phthalate (HPMCP), hydroxypropyl methylcellulose acetate succinate, shellac, kanten, carrageenan, and zein. In this case, they can be used alone or as a mixture. That is, the coating base is a group selected from the group consisting of ethyl cellulose (EC), hypromellose phthalate (HPMCP), hydroxypropyl methylcellulose acetate succinate, shellac, kanten, carrageenan, zein and mixtures thereof. Preferably, it is a base selected from the group consisting of ethyl cellulose, hydroxypropyl methylcellulose acetate succinate, hypromellose phthalate, citrus and mixtures thereof.

  The edible film forming the coating layer is formed by adding an additive to the coating base. As the additive used in this case, the additive used in the above-described drug component layer is used by blending at the above-mentioned blending ratio except that the ratio with respect to the water-soluble base is the ratio with respect to the coating base. An edible film can be formed.

<Production method>
The intraoral patch of this embodiment prepares an edible film that forms each layer by casting a solution for forming a medicinal component layer and a solution for forming a coating layer on a plastic base film in the same manner as a normal edible film. Then, the edible film for each layer obtained can be cut into a predetermined size using a normal cutter, and the edible film for forming both layers can be bonded and thermocompression bonded. Moreover, it can also manufacture by superimposing the edible film formation solution for both layer formation on a predetermined shape, and coating.
The drug component layer forming solution and the coating layer forming solution can be obtained by dissolving the water-soluble base, the coating base and additives, and the drug described above in a solvent.
As the solvent that can be used at this time, the following can be used.
Water, ethanol, acetic acid, acetone, anisole, 1-butanol, 2-butanol, n-butyl acetate, t-butyl methyl ether, cumene, dimethyl sulfoxide, ethyl acetate, diethyl ether, ethyl formate, formic acid, heptane, isobutyl acetate, Isopropyl acetate, methyl acetate, 3-methyl-1-butanol, methyl ethyl ketone, methyl isobutyl ketone, 2-methyl-1-propanol, pentane, 1-pentanol, 1-propanol, 2-propanol, propyl acetate, tetrahydrofuran, acetonitrile, Chlorobenzene, chloroform, cyclohexane, 1,2-dichloroethene, dichloromethane, 1,2-dimethoxyethane, N, N-dimethylacetamide, N, N-dimethylformamide, 1,4-dioxane, 2-ethane Xylethanol, ethylene glycol, formamide, hexane, methanol, 2-methoxyethanol, methylbutylketone, methylcyclohexane, N-methylpyrrolidone, nitromethane, pyridine, sulfolane, tetralin, toluene, 1,1,2-trichloroethene, xylene, 1,1-diethoxypropane, dimethoxymethane, 2,2-dimethoxypropane, isooctane, isopropyl ether, methyl isopropyl ketone, methyl tetrahydrofuran, petroleum ether, trichloroacetic acid, trifluoroacetic acid, methylene chloride, etc. can be used. In that case, it can be used alone or in combination. Among these solvents, ethanol, water, ethyl acetate or a combination of these solvents (for example, ethanol-water mixture, ethanol-ethyl acetate mixture) can be most preferably used.

<Usage and effect>
The intraoral patch of the present embodiment has a different sticking time depending on what is contained as a medicinal component. However, when used, for example, when used by a dentist, the grasping part 4 is grasped with tweezers and the like, and is applied to the affected part. The intraoral patch 1 is brought into contact with the intraoral mucosa so that the contact surface 10 comes into contact, and is used by maintaining the state of being stuck for a predetermined time during which the drug component is absorbed through the mucous membrane. it can.
The oral patch of the present embodiment is one that absorbs moisture in the oral cavity and swells both in the drug component layer and the coating layer, and expresses adhesiveness. The drug component layer is not exposed and the drug component does not melt into the oral cavity. Therefore, the drug component can be absorbed into the body through the mucous membrane as designed by the drug.
In addition, since all of the intraoral patches of the present embodiment are made of edible films, there is no particular danger for infants, children, and elderly people, and they are safe even if they are swallowed.

In the following, other embodiments will be described. In the following description, portions that are formed in the same manner as in the above-described embodiment will not be described, and portions that are different from the above-described embodiment will be mainly described. For the points that are not particularly described, the description in the above-described embodiment is applied as appropriate.
<Second Embodiment>
In the intraoral patch 101 of the embodiment shown in FIG. 2, the medicinal component layer 102 is composed of a central circular portion and a donut-shaped portion positioned on the outer periphery of the periphery, and the adhesiveness is increased between the two portions. A doughnut-shaped adhesive layer 106 is interposed. Further, the grip portion 104 is provided on the periphery of the coating layer 103. The center portion of the covering layer 103 is colored and provided with a mark portion 105.
The adhesive layer 106 is formed of an edible film in the same manner as the drug component layer 102 and the covering layer 103, and can be formed by the same manufacturing method and the same composition as the drug component layer except that it does not contain a drug component. it can. The adhesive layer 106 can sufficiently adhere to the oral mucosa by strengthening the adhesive force of the drug component layer because the adhesive force of the water-soluble base that does not contain the drug component is sufficiently exerted.
As the colorant for forming the mark portion 105, the above-mentioned colorants can be used without any particular limitation, and printing is performed without any particular limitation on the method used when printing the colorant on an ordinary edible film. Can be formed.

<Third Embodiment>
In the intraoral patch 201 of the embodiment shown in FIG. 3, the mark portion 205 is provided not on the surface of the coating layer but on the surface of the drug component layer 202, and the grip portion 204 is provided on the periphery of the coating layer 203. .
By providing the mark portion 205 at the center of the surface of the medicinal component layer 202, it is possible to determine which portion the medicinal component layer is in contact with when performing various treatments after applying and removing the oral patch for a predetermined time. The practitioner can easily confirm it.

In addition, this invention is not restrict | limited to the above-mentioned embodiment, A various change is possible in the range which does not deviate from the meaning of this invention.
For example, in the above-described embodiment, the circular shape is shown and described. However, the shape is not limited to this, and various shapes such as a rectangular shape, a triangular shape, and a star shape can be used.
In the embodiment shown in FIG. 3, the mark portion may be formed of edible ink that can be transferred, and the mark may be transferred to the mucous membrane.

Hereinafter, the present invention will be described more specifically with reference to Examples and Comparative Examples, but the present invention is not limited thereto.

[Example 1]
30 parts by weight of a raw material for a drug component layer having the following composition 1 was dissolved in 70 parts by weight of 70 wt% ethanol to obtain a solution for forming a drug component layer.
Separately, 30 parts by weight of a raw material for forming a coating layer having the following composition 2 was dissolved in 70 parts by weight of purified water to obtain a coating layer forming solution.
Both obtained solutions were sequentially applied onto a PET film as a base film and dried to obtain films for forming each layer. The covering layer film was partially pulled outward to form a predetermined number of protruding portions for forming the gripping portions at predetermined locations. Subsequently, both films were cut into a predetermined shape, and both layers were attached to obtain the intraoral patch of the present invention shown in FIG. Regarding the size of the obtained anesthetic, the diameter of the drug component layer was 10 mm, the total diameter was 25 mm, the thickness of the drug component layer was 100 μm, and the total thickness was 200 μm.
<Composition 1>
Propylene glycol 9 parts by weight Polyacrylic acid 15 parts by weight Shin-Etsu Chemical "TC-5E" * 1 26 parts by weight Lidocaine 50 parts by weight * 1 Hydroxypropyl methylcellulose <Composition 2>
Polysorbate 80 (trade name, manufactured by NOF Corporation) 2 parts by weight Ethylcellulose 80 parts by weight Medium chain fatty acid Triglyceride 18 parts by weight

[Example 2]
An oral patch of the present invention was obtained in the same manner as in Example 1 except that the raw material composition for forming each layer was changed to the composition shown below.
<Composition 1>
Propylene glycol 9 parts by weight Polyacrylic acid 15 parts by weight Nippon Soda [HPC-SSL] * 2 26 parts by weight Lidocaine 50 parts by weight * 2 Hydroxypropylcellulose <Composition 2>
Polysorbate 80 (trade name, manufactured by NOF Corporation) 2 parts by weight ethyl cellulose 80 parts by weight Medium chain fatty acid triglyceride 18 parts by weight [Example 3]
An oral patch of the present invention was obtained in the same manner as in Example 1 except that the raw material composition for forming each layer was changed to the composition shown below.
<Composition 1>
Propylene glycol 9 parts by weight Polyacrylic acid 15 parts by weight Polyvinylpyrrolidone “K-90” 26 parts by weight Lidocaine 50 parts by weight <Composition 2>
Polysorbate 80 (trade name, manufactured by NOF Corporation) 2 parts by weight Ethylcellulose 80 parts by weight Medium chain fatty acid Triglyceride 18 parts by weight

[Test example]
For each obtained oral patch, the anesthetic effect as a drug effect was confirmed according to the following test method. The results are shown in Table 1.
The effect of each oral patch obtained was confirmed in the following manner.
As a result, as is apparent from the results shown in Table 1, the intraoral patch of the present invention is 90 seconds or 120 seconds after pasting, as in the case where an anesthetic is injected with a normal syringe at about 180 seconds at the latest. Excellent anesthetic effect. Moreover, as an impression of each monitor, since it was in the form of a film, there was no pain as injecting and anesthesia could be performed. The effect was concentrated near the center, and the patient's discomfort was light compared to anesthesia by normal injection. Therefore, the chewing action could be performed without a sense of incongruity 30 minutes after the corresponding application after the treatment was completed. Moreover, as a sensitivity evaluation, there was almost no sense of incongruity during pasting and it was excellent in usability.
<Test method>
The effect of each oral patch obtained was confirmed in the following manner. Each patch was affixed to the gums using tweezers for 2 minutes.
A film-like anesthetic with a lidocaine content of 50% by weight of 10 mm × 10 mm, a thickness of 460 μm, and a weight of 50 mg was applied to 6 monitors, and after applying, 30 seconds, 60 seconds, 90 seconds, 120 seconds, The anesthetic effect after 180 seconds gives a stimulus to the affixed part, and if the stimulus is felt at that time, “no effect” is assumed, and if no stimulus is felt, “effect appears” or “effect lasts” Judged.
The results are shown in Table 1.

Claims (7)

It is an intraoral patch for sticking to the mucous membrane in the oral cavity in the form of a film to absorb the active ingredient into the body through the mucosa,
A film-shaped drug ingredient layer that contains an edible water-soluble base and a drug, and is attached to the oral mucosa of the user,
Covers the surface other than the contact surface that contacts the user's mucous membrane in the medicinal component layer, is less water-soluble than the water-soluble base, or expresses stickiness in the oral cavity than the water-soluble base An intraoral patch comprising a coating layer comprising an edible coating base that does not. The intraoral patch according to claim 1, further comprising a grasping portion that facilitates clamping of the intraoral patch. The intraoral patch according to claim 2, wherein the grip portion is formed by providing a protrusion at substantially the center of a non-contact surface that is a surface opposite to the contact surface. The intraoral patch according to claim 2, wherein the grasping part is formed by providing a protrusion on a part of the periphery of the coating layer. The intraoral patch according to claim 1, wherein a mark portion for performing various treatments is provided in the central portion of the coating layer. The intraoral patch according to claim 5, wherein the mark portion is formed by coloring a non-contact surface that is a surface opposite to the contact surface. The water-soluble base is a base selected from the group consisting of pullulan, polyvinyl alcohol (PVA), hydroxypropylcellulose (HPC), polyvinylpyrrolidone (PVP), gelatin, starch, and mixtures thereof;
2. The intraoral patch according to claim 1, wherein the coating base is a base selected from the group consisting of ethyl cellulose, hydroxypropyl methyl cellulose acetate succinate, hypromellose phthalate, epilepsy and a mixture thereof.