JP5852910B2 - Oral preparation in container - Google Patents

Description

  The present invention relates to a containerized oral preparation.

About 70% of the causes of tooth loss are periodontal disease, and it is useful to use oral preparations containing active ingredients such as bactericides and anti-inflammatory agents in order to prevent periodontal disease. It is said. The root cause of periodontal disease is a pathogenic bacterium that exists in the narrow part of the bottom of the periodontal pocket.
Therefore, in order to prevent the onset of periodontal disease, it is important for the self-care to infiltrate and retain the preparation to the depth of the periodontal pocket to kill pathogenic bacteria.

  In order to allow the preparation to penetrate into the back of the periodontal pocket, the tooth neck is cleaned with a liquid toothpaste containing an active ingredient or a liquid composition containing an active ingredient is contained in the mouth. As a result, the active ingredient is diluted, and there is a problem that the active ingredient is less likely to stay in the periodontal pocket.

Conventionally, various preparations and instruments have been proposed for the purpose of preventing or improving periodontal disease.
For example, a gradual stick-shaped preparation for interdental insertion, which is formed in a stick shape that can be inserted into the interdental area and has adhesion to the gingiva and / or tooth surface, has been proposed (for example, Patent Document 1). Since the invention of Patent Document 1 adheres to the interdental surface or tooth surface and releases the active ingredient gradually, the effect can be maintained for an arbitrary time.
Or (A) 1 or more types chosen from fats and oils, wax, and higher hydrocarbon, (B) Polyoxyethylene alkyl ether, (C) Cellulose derivative, (D) Calcium compound, (E) Cephem antibiotic A sustained-release preparation for treating periodontal disease has been proposed (for example, Patent Document 2). According to the invention of Patent Document 2, after being applied to the affected area, cephem antibiotics are continuously released to improve the persistence of the drug effect.

 Further, a barrel having a nozzle mounting portion at the tip, a plunger having a gasket capable of liquid-tightly sliding the inner wall of the barrel at the tip, a plunger inserted from the rear end of the barrel, and a detachable to the nozzle mounting portion There has been proposed a drug injector comprising a nozzle, a base end side mounting portion provided with means for mounting to the nozzle mounting portion, and a discharge portion that is bent at a predetermined angle from the mounting portion. (For example, Patent Document 3). According to the invention of Patent Document 3, a medicine can be infiltrated into the bottom of the periodontal pocket.

JP 2001-163768 A JP 2000-302621 A JP 2000-107298 A

However, since the techniques of Patent Documents 1 and 2 increase the viscosity of the composition and improve the adhesion to the affected area and the vicinity of the affected area, the composition is less likely to enter the periodontal pocket (low penetration). There was a problem. In addition, there is a problem that not all of the composition dissolved in saliva or the like necessarily enters the periodontal pocket, but a part of it flows out.
In addition, a composition having a reduced viscosity can easily enter into a narrow gap such as a periodontal pocket, but it can be easily washed away by saliva and the like, and the drug effect cannot be sustained (low retention).
The technique of Patent Document 3 is premised on a medical treatment by a doctor, and the operation is complicated for the purpose of self-care.
Then, this invention aims at the oral preparation in a container which can infiltrate an oral preparation into a periodontal pocket effectively by simple operation.

The containerized oral preparation of the present invention is a containerized oral preparation in which the oral preparation is accommodated in a dispensing container, and the oral preparation is 20 rpm, 25 ° C. using a B-type viscometer. Viscosity measured at 0.3 to 20 Pa · s, and the dispensing container is provided at a container main body in which the oral preparation is stored and at one end of the container main body, and the oral preparation And an inner diameter of the tip of the nozzle body is 0.2 to 3 mm.
It is preferable that a ratio represented by [viscosity of the oral preparation (Pa · s)] / [inner diameter (mm) of the tip of the nozzle body] is 0.15 to 40, The length is preferably 5 to 20 cm, and the maximum width is preferably 1 to 6 cm. The container body has flexibility, and the container body may be pressed to pour out the oral preparation. The container body may have plasticity.
The container body is preferably provided with a check valve in the vicinity of the tip, and the back end of the nozzle body is formed with a backflow prevention portion in which two flat portions having flexibility are opposed to each other. The prevention part is preferably opened when the container body is pressed to pour out the oral preparation and closed when the container body is released.

  According to the present invention, the oral preparation can be effectively infiltrated into the periodontal pocket by a simple operation.

It is a top view of the extraction container concerning one embodiment of the present invention. It is a top view of the nozzle body of FIG. It is sectional drawing of the non-return valve of FIG. It is a top view of the extraction container concerning one embodiment of the present invention. It is a top view of the extraction container concerning one embodiment of the present invention. It is a top view of the nozzle body concerning one Embodiment of this invention. It is a top view of the nozzle body concerning one Embodiment of this invention. It is a top view of the nozzle body concerning one Embodiment of this invention. (A) It is a front view of the nozzle body of FIG. (B) It is the elements on larger scale of the nozzle body of FIG. (C) It is C1-C1 sectional drawing of FIG.9 (b). (A) It is a front view explaining the usage method of the nozzle body of FIG. (B) It is a partial enlarged view explaining the usage method of the nozzle body of FIG. (C) It is C2-C2 sectional drawing of FIG.10 (b). (A) It is a front view explaining the usage method of the nozzle body of FIG. (B) It is a partial enlarged view explaining the usage method of the nozzle body of FIG. (C) It is C3-C3 sectional drawing of FIG.11 (b). It is a top view of the extraction | pouring part used for the Example.

(Intraoral preparation in a container)
The containerized oral preparation of the present invention is a preparation in which the oral preparation is stored in a dispensing container, and is applied to a periodontal pocket for the purpose of preventing or improving periodontal disease, for example. .

<Pouring container>
An embodiment of the dispensing container of the present invention will be described below with reference to the drawings.
A dispensing container 1 shown in FIG. 1 includes a container body 2 and a nozzle body 3 provided at one end of the container body 2.

The container body 2 includes a hollow cylindrical body portion 20, a shoulder portion 22 that closes one open end of the body portion 20, a cylindrical mouth and neck portion 26 that protrudes from the shoulder portion 22, and the other of the body portion 20. It is what is called a tube container provided with the bottom part 24 where the inner sides of the open ends are attached to each other and bonded together.
In the present embodiment, the check valve 4 is provided inside the shoulder portion 22, the mouth neck portion 26 of the check valve 4 protrudes from the shoulder portion 22, and the nozzle body 3 is attached to the protruding mouth neck portion 26. ing.

 The length L1 of the container body 2, that is, the length from the end of the bottom 24 to the base end (nozzle base end) 35 of the nozzle body 3 is not particularly limited, but is preferably 5 to 20 cm, for example, 7 to 15 cm. Is more preferable. If the length L1 is less than 5 cm, it may be too small to fit in the hand and it may be difficult to accurately apply the oral preparation to the application target. When the length L1 is more than 20 cm, the operability such as positioning of the nozzle body 3 in the oral cavity decreases, and it may be difficult to accurately apply the oral preparation to the application target.

  Although the width W1 which is the maximum width of the container main body 2 is not specifically limited, For example, 1-6 cm is preferable and 2-4 cm is more preferable. When the width W1 is 1 to 6 cm, the container main body 2 can easily fit in the hand, the operation of the nozzle body 3 in the oral cavity is facilitated, and the oral preparation can be accurately applied to the application target.

 The material of the trunk portion 20 is not particularly limited as long as it has flexibility. For example, a single-layer film made of a polyolefin such as polypropylene or polyethylene, a polyester such as polyethylene terephthalate, a resin such as polyamide, or a single layer thereof. The multilayer film which laminated | stacked the layer film etc. are mentioned. The multilayer film may include a metal thin film such as aluminum or a vapor deposition film. If the trunk | drum 20 is formed with such a single layer film or a multilayer film, the formulation for oral cavity will be poured out by pressing the trunk | drum 20, and the trunk | drum 20 will be released by releasing the press of the trunk | drum 20. Since the shape is restored (restorability), all of the oral preparation in the container body 2 can be poured out.

The trunk portion 20 presses a region centered on the midpoint between the boundary with the shoulder portion 22 and the end portion of the bottom portion 24 with a plunger, and when the plunger comes into contact with the tube, the stress ( Hereinafter, it may be called trunk | drum hardness), and it is preferable that it is 1-35N, and it is more preferable that it is 2-10N. When the body hardness is less than 1N, the body 20 may become too soft and it may be difficult to hold the dispensing container 1, and when it exceeds 35N, when pouring the oral preparation, The body part 20 will be strongly pressed, and there is a risk that it will be difficult to control the amount of the intraoral preparation dispensed.
The trunk hardness is a value measured using a SUN RHEO METER CR-500DX (manufactured by San Kagaku Co., Ltd.) at a descending speed of 300 mm / min of a plunger (a cylindrical shape having a diameter of 10 mm).
The body hardness can be adjusted by a combination of the material and thickness of the film constituting the body 20 and the width W1 of the body 20.

 The thickness of the film which comprises the trunk | drum 20 is not specifically limited, It can determine in consideration of a material etc.

 The material of the shoulder portion 22 is not particularly limited, and examples thereof include resins such as polyolefin and polyester.

 The nozzle body 3 includes a substantially cylindrical pouring part 30 in which a flow path for pouring the oral preparation is formed, and a cylindrical connection part 32 fitted to the outer peripheral surface of the mouth-and-neck part 26. The pouring part 30 and the connection part 32 are integrally molded. The extraction part 30 extends in the communication direction F1 between the container body 2 and the nozzle body 3, and the extraction direction of the oral preparation is substantially the same as the communication direction F1. The nozzle body 3 has a tapered shape that gradually decreases in diameter from the extraction portion base end 33 that is a boundary with the connection portion 32 toward the nozzle tip 31, and this tapered shape has an inner diameter with respect to the length direction of the nozzle body 3. A taper that decreases linearly (linear taper).

 The length l1 of the nozzle body 3, that is, the length from the nozzle tip 31 to the nozzle base 35 (FIG. 2) is not particularly limited, but is preferably 20 to 60 mm, and more preferably 30 to 50 m. When the length l1 is less than 20 mm, the nozzle tip 31 does not easily reach the tooth neck of the back tooth, and there is a possibility that it is difficult to apply the oral preparation to the application target. When the length l1 is more than 60 mm, the operability of the nozzle body 3 in the oral cavity is lowered, and it may be difficult to accurately apply the oral preparation to the application target.

 The length l2 of the extraction portion 30, that is, the length from the nozzle tip 31 to the extraction portion base end 33 (FIG. 2) is not particularly limited, but is preferably 15 mm or more and less than 60 mm, and more preferably 25 mm or more and less than 50 mm. preferable. If the length l2 is less than 15 mm, the nozzle tip 31 is unlikely to reach the back neck of the tooth, and there is a risk that it is difficult to apply the oral preparation to the application target. When the length l2 is 60 mm or more, the operability of the nozzle body 3 in the oral cavity is lowered, and the oral preparation is applied to the subject to be applied (especially all the cervical parts on the maxilla, mandible, tongue side and buccal side). It may be difficult to apply accurately. In addition, if the length l2 is 15 mm or more and less than 60 mm, it is easy to adjust the nozzle hardness described later.

  The inner diameter (tip inner diameter) r1 (FIG. 2) of the nozzle tip 31 of the nozzle body 3, that is, the opening diameter of the nozzle body 3 is 0.2 to 3 mm, preferably 0.3 to 2 mm. When the tip inner diameter r1 is less than 0.2 mm, the body part 20 is strongly pressed when pouring the oral preparation, and it is difficult to control the amount of the oral preparation to be dispensed. The operation of the dispensing container 1 becomes complicated due to the small amount. When the tip inner diameter is more than 3 mm, liquid dripping occurs from the nozzle tip 31 and the handling is complicated.

 Even if the inner diameter (base end inner diameter) r2 of the extraction base end 33 of the nozzle body 3 is too small or too large, the desired nozzle hardness may not be obtained. Therefore, the inner diameter of the extraction portion base end 33 can be determined in consideration of the material of the nozzle body 3 and the like. For example, the base end inner diameter r2 is 1 to 10 mm.

  The material of the nozzle body 3 is not particularly limited, and examples thereof include resins such as polyolefin, polyester, vinyl chloride, silicon elastomer, urethane, and polystyrene. Among them, relatively soft polyolefin, vinyl chloride, silicon elastomer, urethane, and the like can be given. preferable.

The nozzle body 3 presses a region centering on the midpoint between the nozzle tip 31 and the extraction portion base end 33 with a plunger, and stress (nozzle when the plunger is lowered by 1 mm after contacting the nozzle body 3) (Hardness) is preferably 1 to 80N, and more preferably 3 to 50N. If the nozzle hardness is less than 1N, the nozzle body 3 bends due to its own weight or the nozzle tip 31 swings, which may make it difficult to apply the oral preparation to the application target. When the nozzle hardness is more than 80N, for example, when the nozzle tip 31 is moved according to the boundary between the teeth and the gums, the dispensing part 30 does not sufficiently bend and the oral preparation is accurately applied to the application target. There is a risk of pain when it is difficult to apply or when the nozzle tip 31 hits the gingiva.
The trunk hardness is a value measured using a SUN RHEO METER CR-500DX (manufactured by San Kagaku Co., Ltd.) at a descending speed of 300 mm / min of the plunger (ground surface 1 × 7 mm).
The nozzle hardness can be adjusted by a combination of the material and thickness of the nozzle body 3, the length l1 of the nozzle body 3, the length l2 of the extraction portion 30, and the shape of the extraction portion 30.

As shown in FIG. 3, the check valve 4 has a substantially cylindrical cylinder portion 40 in which a first check valve opening 43 and a second check valve opening 45 are formed on both sides in the communication direction F1. And a mouth-and-neck part 26 extending from the periphery of the first check valve opening 43, and a spherical valve body 50 that is housed in the cylinder part 40 and movable in the communication direction F1.
In the cylinder part 40, a convex part 42 is formed in the vicinity of the periphery of the first check valve opening part 43, and a convex line extending in the circumferential direction of the inner peripheral surface on the second check valve opening part 45 side. 44 is formed.

The material of the cylinder part 40 is not specifically limited, Resin, such as polyolefin and polyester, Metals, such as aluminum, etc. are mentioned.
The material of the mouth / neck part 26 is the same as the material of the cylinder part 40, and the material of the valve body 50 is the same as the material of the cylinder part 40.

(Oral composition)
The composition for oral cavity has a viscosity of 0.3 to 20 Pa · s, preferably 0.5 to 5 Pa · s. If the viscosity is less than 0.3 Pa · s, dripping may occur from the nozzle tip 31 and the handling may become complicated. If the viscosity is more than 20 Pa · s, the oral preparation is removed from the dispensing container 1. It is difficult to dispense and the operation is complicated, and it is difficult for the oral preparation to penetrate into a narrow part such as a periodontal pocket.
In addition, the ratio represented by [viscosity of oral preparation (Pa · s)] / [inner diameter r1 (mm) at the tip of the nozzle body] (hereinafter also referred to as viscosity / inner diameter ratio) is 0. 15-40 are preferable, 0.4-30 are more preferable, and 0.7-8 are still more preferable. If the viscosity / inner diameter ratio is within the above range, the state of the oral preparation poured out from the dispensing container 1 can be more easily controlled, and the oral preparation can be easily applied to a narrow part such as a periodontal pocket. .
The viscosity of the oral preparation was measured under the following measurement conditions using a BH rotary viscometer (product name: TVB-10) manufactured by Toki Sangyo Co., Ltd.
Rotor: No. 4. Number of rotations: 20 rpm, measurement temperature: 25 ° C., measurement time: 180 seconds later

  The composition of the oral preparation is not particularly limited as long as the viscosity can be adjusted to 0.3 to 20 Pa · s. Active ingredients such as bactericides and anti-inflammatory agents, thickeners, binders, chelating agents, A combination of surfactants, sweeteners, preservatives, pigments, fragrances and the like can be mentioned.

Active ingredients include, for example, cationic fungicides such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, fungicides such as hinokitiol, isopropylmethylphenol, triclosan, sodium fluoride, potassium fluoride, stannous fluoride , Strontium fluoride, fluoride having remineralization effect such as sodium monofluorophosphate, tranexamic acid, epsilon-aminocaproic acid, allantochlorohydroxyaluminum, hinokitiol, ascorbic acid, dl-tocopherol acetate, dihydrocholesterol, α-bisabolol , Azulene, dipotassium glycyrrhizinate, glycyrrhetinic acid, copper chlorophyllin sodium, chlorophyll and other anti-inflammatory agents, copper gluconate and other copper compounds, aluminum lactate, Lithium, hypersensitivity suppression components such as potassium nitrate, Japanese angelica root soft extract, Phellodendron bark extract, camomile, clove, rosemary, scutellaria root extract, etc. safflower and the like. Among these, when an oral preparation is used as a periodontal pocket cleaning agent, a cationic bactericidal agent (hereinafter sometimes referred to as “component (C)”) is preferable from the viewpoint of bactericidal power.
These active ingredients can be used individually by 1 type or in combination of 2 or more types as appropriate.
The content of the active ingredient in the oral preparation can be determined within a range that does not impair the effects of the present invention in consideration of the type of the active ingredient.

Examples of the thickening agent include glycerin, sorbit, propylene glycol, polyethylene glycol having a molecular weight of 200 to 6000, ethylene glycol, polyhydric alcohol such as reduced starch saccharified product, and the like. These thickeners can be used singly or in appropriate combination of two or more.
Although content of the viscous agent in an intraoral formulation is not specifically limited, For example, you may be 5-50 mass%.

As binder, water-soluble polymer containing nitrogen such as hydroxyethyl cellulose dimethyl diallylammonium chloride, dimethyl diallylammonium chloride polymer, polyvinylpyrrolidone, carboxyvinyl polymer, sodium polyacrylate, xanthan gum, sodium alginate, propylene glycol alginate Examples include organic binders such as esters, sodium carboxymethyl cellulose, hydroxyethyl cellulose, guar gum, gelatin, and Avicel, and inorganic binders such as montmorillonite, kaolin, and bentonite. Among them, carboxyvinyl polymer (hereinafter referred to as (A) component) And a water-soluble polymer containing nitrogen (hereinafter sometimes referred to as component (B)) is preferably used in combination.
The content of the binder in the oral preparation is not particularly limited, but is, for example, 5% by mass or less.
In this paper, “water-soluble” means that the solubility in water (20 ° C.) is 0.1 g / 100 g or more of water. The “polymer” has a weight average molecular weight of 1000 or more, and the “weight average molecular weight” is the weight average molecular weight measured by the light scattering method using the K value defined in the United States Pharmacopeia (USP). It is converted.

When the component (A) and the component (B) are used in combination, as the component (A), the viscosity of a 0.5% by mass aqueous solution (hereinafter referred to as “.0”) measured at 20 rpm and 25 ° C. using a B-type viscometer. The viscosity may be 5% by mass), but is preferably 20 Pa · s or less, more preferably 2 to 20 Pa · s, and still more preferably 5 to 16 Pa · s. Examples of such component (A) include Carbopol 941, 981, ETD2050, 2984 (trade name, manufactured by Lubrizol Corporation), HV501, 501E (trade name, manufactured by Sumitomo Seika Co., Ltd.), and the like.
These (A) components can be used individually by 1 type or in combination of 2 or more types.

Examples of the component (B) include hydroxyethyl cellulose dimethyl diallylammonium chloride, dimethyl diallylammonium chloride polymer, polyvinyl pyrrolidone and the like. Among them, polyvinyl pyrrolidone is preferable from the viewpoint of further improving the retention.
As polyvinylpyrrolidone, Rubiscol K-30, 90 (trade name, manufactured by BASF Japan Ltd.) and the like are commercially available.

In the oral preparation using both the (A) component and the (B) component having a 0.5 mass% viscosity of 20 Pa · s, the yield value increases when it comes into contact with moisture in the oral cavity. For this reason, the intraoral formulation containing the component (A) and the component (B) has a high penetration property when applied to an application target and a high retention property after application.
In addition, a yield value can be measured at 37 degreeC with sensor C35 / 4 degree, 0-20 Pa (30 second) using viscoelasticity measuring apparatus RheoStress RS50 (made by HAAKE).

 When the component (A) and the component (B) are used in combination, the mass ratio ((A) / (B)) of the component (A) to the component (B) is 0.2 to 5, preferably 0.8. 4-3. If it is less than 0.2, sufficient retention may not be obtained, and if it exceeds 5, infiltration and retention may be impaired.

Examples of the surfactant include anionic surfactants such as sodium lauryl sulfate, sodium lauroyl sarcosine, polyoxyethylene alkyl sulfate, N-lauroyl taurate, α-olefin sulfonate, N-acyl glutamate, 2- Amphoteric surfactants such as alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, polyoxyethylene hydrogenated castor oil, alkylglycoside, alkylol amide, polyoxyethylene sorbitan monostearate, polyoxyethylene polyoxypropylene Nonionic surfactants such as glycol, polyoxyethylene alkyl ether, decaglyceryl laurate and the like can be mentioned.
The content of the surfactant in the oral preparation can be determined in consideration of the type of the surfactant and the like, for example, 0.1 to 5% by mass.

Examples of sweeteners include saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, and perilartin. Examples of preservatives include parabens (paraoxybenzoate) such as butylparaben and ethylparaben. And sodium benzoate. These sweeteners can be used singly or in appropriate combination of two or more.
The content of the sweetener in the oral preparation can be determined within a range that does not impair the effects of the present invention in consideration of the type of sweetener.

As fragrances, natural fragrances, and fragrances obtained by processing these natural fragrances (front reservoir cut, rear reservoir cut, fractional distillation, liquid extraction, essence, powder fragrance, etc.), synthetic fragrances, natural fragrances and / or Well-known fragrance | flavors, such as the mixing | blending fragrance | flavor which combined the synthetic fragrance | flavor, are mentioned. These fragrance | flavors can be used individually by 1 type or in combination of 2 or more types as appropriate.
Content of the fragrance | flavor in an intraoral formulation can be determined according to the kind of fragrance | flavor, for example, 0.000001-1 mass% is preferable. Moreover, when using the fragrance | flavor formulation which melt | dissolved the said fragrance | flavor in the fragrance | flavor solvent, 0.1-2.0 mass% of content of the fragrance | flavor formulation in an intraoral formulation is preferable, for example.

The dispersion medium for the oral preparation is not particularly limited as long as it is water, and examples thereof include tap water, well water, purified water treated by distillation, ion exchange, filtration, or a combination thereof.
The water content (water content) in the oral preparation is 30 to 85% by mass, preferably 40 to 75% by mass. When the amount is less than 30% by mass, the penetration property is insufficient, and when it exceeds 85% by mass, the retention property is insufficient.

(Production method)
A method for producing the containerized intraoral preparation of this embodiment will be described.
First, according to a conventional method, an arbitrary component is dispersed or dissolved in water to obtain an oral preparation.

After mounting the check valve 4 on a member (shoulder member) constituting the shoulder portion 22 so that the mouth-and-neck portion 26 protrudes from the shoulder portion 22, one opening end of the tubular film is formed by the shoulder member. Is closed to form the shoulder 22. The formation method of the shoulder part 22 is not specifically limited, For example, the method of heat-welding a shoulder part member and a cylindrical film is mentioned.
Next, after filling the oral preparation from the other open end of the film, the open end is closed to form the bottom 24. The formation method of the bottom part 24 is not specifically limited, For example, the method of attaching | bonding the inner sides of a cylindrical film and heat-bonding, or adhere | attaching with an adhesive agent is mentioned.
And the oral cavity formulation can be obtained by mounting | wearing the mouth neck part 26 with the nozzle body 3. FIG. In addition, the nozzle body 3 may be adhere | attached on the mouth neck part 26, and may be mounted | worn so that attachment or detachment is possible.

(how to use)
A method for using the containerized intraoral preparation of this embodiment will be described.
The torso 20 is grasped with fingers, the nozzle tip 31 is brought into contact with the boundary between the teeth and gums, and the torso 20 is pressed with the grasped fingers to dispense the oral preparation from the nozzle tip 31. When the body part 20 is pressed, the valve body 50 is pushed by the oral preparation in the body part 20 and moves toward the mouth-neck part 26 and comes into contact with the convex part 42 to be in the state of reference numeral 50a. At this time, since the valve body 50 a does not block the first check valve opening 43, a flow path through which the oral preparation flows in the mouth and neck portion 26 is secured in the check valve 4. .

While pouring the oral preparation, the nozzle tip 31 is moved according to the boundary between the teeth and the gums, thereby applying the oral preparation over a wide range.
Since the oral preparation applied to the boundary between the tooth and the gingiva has fluidity, it penetrates to the bottom of the periodontal pocket.
The body part 20 is restored when the pressure is released, and the oral preparation in the mouth-and-neck part 26 and the nozzle body 3 tries to return to the body part 20. At this time, the valve body 50a moves to the second check valve opening 45 side and abuts on the protrusion 44 to close the second check valve opening 45. In this way, the check valve 4 prevents saliva and the like in the mouth from entering the trunk portion 20.

 According to the present embodiment, since the oral preparation having a viscosity of 0.3 to 20 Pa · s is stored in the pouring container having an inner diameter of the nozzle tip of 0.2 to 3 mm, it is narrow by a simple operation. The oral preparation can be effectively infiltrated into a proper periodontal pocket.

(Other embodiments)
The present invention is not limited to the embodiment described above.
In the above-described embodiment, the container body is a tube container. However, the present invention is not limited to this, and for example, a substantially cylindrical syringe 120 and a plunger 122, such as a dispensing container 100 shown in FIG. It may be a syringe-type container main body 102 composed of Or the container main body 202 of the planar view substantially ellipse shape blow-molded with the flexible material like the extraction container 200 shown in FIG. 5 may be sufficient.

 In the above-mentioned embodiment, although the extraction | pouring part is substantially cylindrical shape, this invention is not limited to this, A rectangular tube shape may be sufficient as an extraction | pouring part. In the case where the dispensing portion has a rectangular tube shape, the inner diameter of the nozzle tip is the diameter of a circle that is inscribed by the outline of the inner diameter of the nozzle tip.

In the above-described embodiment, the shape of the extraction portion is a linear taper, but the present invention is not limited to this. For example, even if the extraction portion base end to the nozzle tip end have substantially the same inner diameter. Good.
Further, for example, as in the nozzle body 103 illustrated in FIG. 6, a nozzle body that includes a pouring portion 130 that gradually decreases in diameter from the pouring portion base end 133 toward the nozzle tip 131 and that has an outer peripheral surface that is a concave curved surface. It is done.
Alternatively, as in the nozzle body 203 shown in FIG. 7, there is one that includes a pouring portion 230 that gradually decreases in diameter from the pouring portion base end 233 toward the nozzle tip 231 and whose outer peripheral surface is a bulging surface.
Among these, the nozzle body 103 shown in FIG. 6 is preferable as the nozzle body.

 Further, the nozzle body is preferably one having a backflow preventing portion formed at the tip of the nozzle. As the backflow prevention unit, a so-called double lead type can be mentioned. The extraction | pouring part in which such a backflow prevention part was formed is demonstrated using FIGS. 8 is a plan view of the nozzle body 303, FIG. 9A is a front view of the nozzle body 303 as viewed from the nozzle tip, and FIG. 9B is a partially enlarged view of FIG. 9 (c) is a cross-sectional view taken along the line C1-C1 of FIG. 9 (b).

 The pouring part 330 of the nozzle body 303 shown in FIG. 8 has a shape that gradually narrows from the pouring part base end 333 toward the nozzle tip 331 and then widens in a plan view, and is a part that gradually widens toward the nozzle tip 331. Is a backflow prevention unit 340. As shown in FIG. 9, the backflow prevention unit 340 is formed by a flat portion 341 and a flat portion 342 that are opposed to each other and their inner surfaces are butted against each other, and is configured by a flexible resin. is there. The nozzle body 303 has the nozzle tip 331 in a closed state in a state (normal state) in which the flat portion 341 and the flat portion 342 are abutted by the mating portion 344.

 Next, the usage method of the extraction container provided with the nozzle body 303 is demonstrated using FIGS. 10A is a front view of the nozzle body 303 viewed from the nozzle tip, FIG. 10B is a partially enlarged view of the nozzle body 303, and FIG. 10C is a view of FIG. It is C2-C2 sectional drawing. FIG. 11A is a front view of the nozzle body 303 viewed from the nozzle tip, FIG. 11B is a partially enlarged view of the nozzle body 303, and FIG. 11C is FIG. It is C3-C3 sectional drawing.

First, when the body part of the dispensing container is pressed, as shown in FIG. 10, the planar part 341 and the planar part 342 are separated from each other to form an opening 346, and the oral preparation is dispensed. When the body part is further pressed, the opening 346 is expanded as shown in FIG. 11, and a larger amount of the oral preparation is poured out.
When the pressure on the trunk is released after dispensing an arbitrary amount of the oral preparation, the flat surface portion 341 and the flat surface portion 342 are brought into contact with each other as shown in FIG. 9, and the nozzle tip 331 is closed.
By forming such a backflow prevention unit 340, it is possible to prevent saliva and the like attached to the nozzle tip 331 from flowing back into the nozzle body 303.
The “inner diameter at the tip” of the nozzle body 303 is the opening diameter when the opening 346 is made into a true circle in front view. The inner diameter of the nozzle body 303 at the base end of the backflow prevention unit 340 (that is, the position where the width of the nozzle body 303 is the narrowest in plan view) is preferably 0.2 to 3 mm.

 In the above-mentioned embodiment, although the extraction | pouring part is made into the shape (straight shape) which extends in a communication direction and the extraction direction and communication direction of an intraoral formulation are substantially the same, this invention is limited to this. Instead, the pouring part may be bent. However, the shape of the pouring part is preferably a shape in which the pouring direction and the communication direction of the oral preparation are substantially the same. Usually, when applying an oral preparation to the oral cavity, the dispensing container is operated while looking at a mirror or relying on the comfort of the nozzle tip. If the dispensing part has a straight shape, the oral preparation can be applied easily and accurately to the application target even if the nozzle body is inserted into the oral cavity at any angle.

In the above-described embodiment, the check valve is provided in the shoulder, but the present invention is not limited to this, and the check valve may not be provided.
In the above-described embodiment, the check valve includes a spherical valve body. However, the present invention is not limited to this, and any conventionally known check valve may be used.

In the above-described embodiment, the material of the body portion is flexible and has resilience. However, the present invention is not limited to this, and the material of the body portion is the presence or absence of a check valve, the backflow. It can be decided in consideration of the presence or absence of the prevention part. For example, when the pouring container does not include the check valve and the backflow prevention part, the body part may be made of a flexible and plastic material. By adopting a plastic material, it is possible to prevent saliva or the like attached to the nozzle tip from flowing into the container body.
Examples of the material having flexibility and plasticity include a film of a single metal layer such as aluminum.

  EXAMPLES Hereinafter, although an Example is shown and this invention is demonstrated in detail, this invention is not limited by the following description.

(Raw materials used)
The raw materials used for the oral preparation of each example are as follows.
<(A) component>
A-1: Carboxyvinyl polymer (trade name; Carbopol 981, viscosity of 0.5 mass% aqueous solution; 6 Pa · s, manufactured by Lubrizol Corporation)
A-2: Carboxyvinyl polymer (trade name; Carbopol ETD2050, viscosity of 0.5 mass% aqueous solution; 15 Pa · s, manufactured by Lubrizol Corporation)
<(B) component>
B-1: Polyvinylpyrrolidone (trade name; Rubiscol K-90, manufactured by BASF Japan Ltd.)

<(C) component>
C-1: Cetylpyridinium chloride (Wako Pure Chemical Industries, Ltd.)
C-2: Benzalkonium chloride (manufactured by Kanto Chemical Co., Inc.)
C-3: Benzethonium chloride (manufactured by Kanto Chemical Co., Inc.)

<Others>
For other ingredients, standard products of quasi-drug raw material standards were used.

(Manufacture examples 1-7) Manufacture of composition A-G for oral cavity According to the composition of Table 1, each component was added to water, it stirred, and the oral preparation of each case was manufactured.

(Examples 1-9, Examples 12-41)
According to the specifications of Tables 2 to 5, a dispensing container similar to the dispensing container 1 shown in FIG. 1 was produced. A laminate tube was used to form the container body. In this laminated tube, a laminated film having the following specifications is formed into a cylindrical shape having a “laminate tube diameter” in a cylindrical table. Moreover, a nozzle body is a nozzle body provided with the extraction part of the straight shape (extraction part shape "A") shown to Fig.12 (a).
In the dispensing container, the oral preparations of each example shown in Tables 2 to 5 were accommodated to prepare oral preparations in containers. About the obtained oral preparation in a container, dripping, ease of extruding the preparation, operability in the oral cavity, ease of holding the container, ease of dispensing control, and ease of application to the tooth neck The results are evaluated and the results are shown in the table.
Laminate film: low density polyethylene 72 μm / ethylene / acrylic acid copolymer resin 90 μm / aluminum 10 μm / ethylene / acrylic acid copolymer resin 35 μm / linear low density polyethylene 50 μm, thickness 257 μm, manufactured by Dai Nippon Printing Co., Ltd.

(Example 10)
A containerized oral preparation was obtained in the same manner as in Example 1 except that the dispensing part was as shown in FIG. About the obtained oral preparation in a container, dripping, ease of extruding the preparation, operability in the oral cavity, ease of holding the container, ease of dispensing control, and ease of application to the tooth neck The results are evaluated and the results are shown in the table.
The pouring container used in this example includes a pouring portion 430 bent at θ1 = 135 ° between the pouring portion base end 433 and the nozzle tip 431, and the shape of the pouring portion is shown in the table. Was described as “B”.

(Example 11)
A containerized oral preparation was obtained in the same manner as in Example 1 except that the dispensing part was as shown in FIG. About the obtained oral preparation in a container, dripping, ease of extruding the preparation, operability in the oral cavity, ease of holding the container, ease of dispensing control, and ease of application to the tooth neck The results are evaluated and the results are shown in the table.
The pouring container used in this example includes a pouring part 530 bent at θ2 = 90 ° between the pouring part base end 533 and the nozzle tip 531. Was described as “C”.

(Comparative Examples 1-4)
A containerized oral preparation was obtained in the same manner as in Example 1 except that the specifications in Table 6 were followed. The resulting oral preparation in a container was evaluated for dripping, ease of extrusion of the preparation, operability in the oral cavity, ease of holding the container, and ease of application to the cervical region. Is shown in the table.

(Evaluation method)
<Evaluation method of dripping>
About the oral preparation in a container of each case, the answer was obtained in four stages regarding the state of dripping from the nozzle tip when applied to the entire cervical region including the upper and lower jaws. Nozzle dripping 4 points, “almost no” 3 points, “I do n’t care” 2 points, “Yes” 1 point, from the average score of 10 people according to the following criteria The dripping from the tip was evaluated.
◎: 3.5 points or more ○ to ◎: 3.0 points or more and less than 3.5 points ○: 2.5 points or more and less than 3.0 points △ to ○: 2.0 points or more and less than 2.5 points △: 1 .5 point or more and less than 2.0 point x: 1.0 point or more and less than 1.5 point

<Evaluation method for ease of extrusion of formulation>
About the oral preparation in a container of each example, the answer was obtained in four steps about the ease of extrusion from a container when it applied to the cervical part of the whole oral cavity including the upper jaw and the lower jaw. 4 points for “very good”, 3 points for “good”, 2 points for “slightly good”, and 1 point for “bad”. did.
◎: 3.5 points or more ○ to ◎: 3.0 points or more and less than 3.5 points ○: 2.5 points or more and less than 3.0 points △ to ○: 2.0 points or more and less than 2.5 points △: 1 .5 point or more and less than 2.0 point x: 1.0 point or more and less than 1.5 point

<Evaluation method of operability in the oral cavity>
About the oral preparation in a container of each case, when it applied to the cervical part of the whole oral cavity including an upper jaw and a lower jaw, the reply was obtained in four steps about the ease of movement in an oral cavity. 4 points for “very good”, 3 points for “good”, 2 points for “slightly good”, 1 point for “bad”, and ease of movement in the oral cavity based on the following criteria from the average score of 10 people evaluated.
◎: 3.5 points or more ○ to ◎: 3.0 points or more and less than 3.5 points ○: 2.5 points or more and less than 3.0 points △ to ○: 2.0 points or more and less than 2.5 points △: 1 .5 point or more and less than 2.0 point x: 1.0 point or more and less than 1.5 point

<Evaluation method for ease of holding containers>
For each oral preparation in a container of each case, an answer was obtained in four stages regarding the ease of holding the container when applied to the entire cervical region including the upper and lower jaws. 4 points for “very good”, 3 points for “good”, 2 points for “slightly good”, and 1 point for “bad”. .
◎: 3.5 points or more ○ to ◎: 3.0 points or more and less than 3.5 points ○: 2.5 points or more and less than 3.0 points △ to ○: 2.0 points or more and less than 2.5 points △: 1 .5 point or more and less than 2.0 point x: 1.0 point or more and less than 1.5 point

<Evaluation method for ease of dispensing control>
About the oral preparation in a container of each case, it is 1 cm / sec. On paper. The content was poured into a 15 cm straight line at a speed of 5 mm, and the dispensing state was evaluated according to the following evaluation criteria. This operation was repeated 10 times, and the average score was classified into the following criteria to evaluate the ease of dispensing control.
≪Evaluation criteria≫
5 points: Can be poured out uniformly with a certain width.
4 points: Can be poured out with a substantially constant width, and there is almost no unevenness.
3 points: Can be poured out with a substantially constant width, but slightly uneven.
2 points: The width of the dispensed intraoral preparation is wide and narrow, and it is clearly uneven.
1 point: Oral preparations are intermittently dispensed, or oral preparations flow and spread, and cannot be dispensed constantly.
≪Judgment criteria≫
◎: 4.5 points or more ○ to ◎: 3.5 points or more and less than 4.5 points ○: 3 points or more and less than 3.5 points △: 2 points or more and less than 3 points ×: 2 points or less

<Evaluation method of ease of application to tooth neck>
Regarding the oral preparations in containers in each case, answers were obtained in four stages regarding the ease of application when applied to the entire neck of the oral cavity including the upper and lower jaws. Apply 4 points for “very good”, 3 points for “good”, 2 points for “slightly good”, and 1 point for “bad”. Ease was evaluated.
◎: 3.5 points or more ○ to ◎: 3.0 points or more and less than 3.5 points ○: 2.5 points or more and less than 3.0 points △ to ○: 2.0 points or more and less than 2.5 points △: 1 .5 point or more and less than 2.0 point x: 1.0 point or more and less than 1.5 point

As shown in Tables 2 to 5, in Examples 1-41 to which the present invention was applied, the evaluation of dripping was “O” or more, the evaluation of ease of extruding the formulation was “O” or more, and to the cervical region The evaluation of the ease of coating was “Δ to ○” or more, and the evaluation of the ease of dispensing control was “◯” or more.
In addition, in Examples 1 to 41 having a viscosity / inner diameter ratio of 0.15 to 40, the ease of dispensing control was “◯” or more. Examples 35 and 37 having a viscosity / inner diameter ratio of 0.4 to 30 are dispensed compared to Example 36 having a viscosity / inner diameter ratio of less than 0.4 and Example 41 having a viscosity / inner diameter ratio of more than 30. Ease of control was better. Examples 2 and 39 having a viscosity / inner diameter ratio of 0.7 to 8 were dispensed compared to Example 38 having a viscosity / inner diameter ratio of less than 0.7 and Example 40 having a viscosity / inner diameter ratio of more than 8. The ease of control was even better.
As shown in Table 6, in Comparative Example 1 in which the viscosity of the oral preparation is 0.1 Pa · s, and in Comparative Example 4 in which the tip inner diameter r1 is 3.5 mm, evaluation of dripping and tooth neck The evaluation of the ease of application to was “x”. Further, in Comparative Example 2 in which the viscosity of the oral preparation is 30 Pa · s and in Comparative Example 3 in which the tip inner diameter r1 is 0.1 mm, the evaluation of the extrudability of the preparation is “x”, and the tooth neck part is evaluated. The evaluation of the ease of coating was “Δ”.
From these results, it was found that the oral preparation in a container to which the present invention was applied can effectively infiltrate the oral preparation into the periodontal pocket by a simple operation.

DESCRIPTION OF SYMBOLS 1,100,200 Outlet container 2,102,202 Container main body 3,103,203,303 Nozzle body 4 Check valve 31,131,231,331,431,531 Nozzle tip 340 Backflow prevention part 341,342 Plane part F1 direction of communication

Claims (11)

In the oral preparation containing a container in which the oral preparation is stored in a dispensing container,
The oral preparation contains a binder, and the viscosity measured at 20 rpm and 25 ° C. using a B-type viscometer is 0.3 to 20 Pa · s,
The dispensing container includes a container body that stores the oral preparation, and a nozzle body that is provided at one end of the container body and that dispenses the oral preparation, and has an inner diameter at the tip of the nozzle body. There Ri 0.2~3mm der, be a ratio represented by [the inner diameter (mm) of the tip of the nozzle body] [the viscosity of the oral formulation (Pa · s)] / is from 0.15 to 40 An oral preparation in a container , wherein the nozzle body is used in contact with the boundary between teeth and gums . The container-containing intraoral preparation according to claim 1 , wherein the container body has a length of 5 to 20 cm and a maximum width of 1 to 6 cm. The container body has flexibility,
The container-containing oral preparation according to claim 1 or 2 , wherein the container body is pressed to pour out the preparation for oral use. The container-containing intraoral preparation according to claim 3 , wherein the container body has plasticity. The container-containing oral preparation according to any one of claims 1 to 3 , wherein the container body is provided with a check valve in the vicinity of the tip. At the tip of the nozzle body, there is formed a backflow prevention portion in which two flat portions having flexibility are opposed to each other,
The said backflow prevention part opens, when the said container main body is pressed and the formulation for oral cavity is poured out, and it will be closed if the press of the said container main body is cancelled | released, The one of Claims 1-3 characterized by the above-mentioned. Oral preparation for oral cavity as described in 2.   The body hardness which is a stress when the body portion of the container body is pressed by a plunger and lowered by 5 mm after the plunger comes into contact with the container body is 1 to 35N. The oral preparation in a container according to claim 1.   The nozzle hardness which is a stress when the nozzle body is pressed by a plunger and lowered by 1 mm after the plunger contacts the nozzle body is 1 to 80 N according to any one of claims 1 to 7. The containerized oral preparation as described.   The container-filled oral cavity according to any one of claims 1 to 8, wherein the nozzle body has substantially the same dispensing direction of the oral preparation and a communication direction of the container body and the nozzle body. Internal preparation.   The binder is a water-soluble polymer containing nitrogen, carboxyvinyl polymer, sodium polyacrylate, xanthan gum, sodium alginate, propylene glycol alginate, sodium carboxymethylcellulose, hydroxyethylcellulose, guar gum, gelatin, Avicel, montmorillonite, kaolin The containerized oral preparation according to any one of claims 1 to 9, which is at least one binder selected from the group consisting of bentonite.   The container-containing oral preparation according to any one of claims 1 to 10, wherein the binder includes a water-soluble polymer containing nitrogen and a carboxyvinyl polymer.

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