JP3350678B2 - Oral aerosol products - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to oral aerosol products. More specifically, for example, nasal cavity, palate, oral cavity,
Pharynx, the active ingredient to a specific site in the oral cavity, such as tongue can act reliably directly relates to oral aerosol product never choking during use.

[0002]

2. Description of the Related Art Conventionally, active ingredients that impart a taste, a medicinal effect and the like to the oral cavity are generally used in the form of granules, liquids, solids, and the like. However, when the active ingredient is used in these forms, the active ingredient may not directly act depending on the site in the oral cavity, and it may take a long time for the effect to appear or it may be unnecessary. Since it acts on a certain part, there is much waste, and there is a possibility that a side effect may occur in other parts.

Further, in order to make the active ingredient of the liquid act directly on a desired site, it is conceivable to spray the active ingredient of the liquid onto a desired site in the oral cavity using a so-called atomizing type finger-push air pump. However, since the nozzle moves up and down when operating the air pump, it is extremely difficult to accurately spray the active ingredient only to a specific site. At the time of restoration, there is a problem that the outside air is sucked into the pump and the inside of the air pump may be contaminated by germs and the like existing in the air.

[0004]

SUMMARY OF THE INVENTION Accordingly, the present inventors
In view of the above prior art, as a result of intensive research to develop means capable of reliably causing the active ingredient to directly act on a specific site, surprisingly, the active ingredient was used in combination with a propellant having a specific composition. When the aerosol composition is used, the active ingredient can be accurately applied to a desired site in the oral cavity, and the aerosol product containing the aerosol composition allows air outside the product to enter the inside. Therefore, the present invention has finally found a completely new fact that it can be suitably used in the oral cavity since it is excellent in hygiene and has completed the present invention.

[0005]

That is, the present invention provides an oral cavity characterized by containing an aerosol composition mainly comprising a stock solution containing an active ingredient and a propellant containing oxygen and an inert gas. Related to aerosol products.

[0006]

The aerosol composition used in the oral aerosol product of the present invention mainly comprises a stock solution and a propellant, and the stock solution comprises an active ingredient and water.

[0007] The active ingredient contained in the stock solution cannot be determined unconditionally because it is appropriately selected and used according to the purpose and use of the oral aerosol product of the present invention.

[0008] The active ingredient includes, for example, a bad breath prevention effect, an anti-inflammatory effect, an analgesic effect, an antitussive effect, an expectorant effect,
Active ingredients that impart a disinfecting effect, a mucous membrane softening effect, and the like are included.

[0009] Specific examples of the above active ingredients include fennel root extract, carrot extract, radish extract, ephedra extract, cuckoo extract, cauliflower oil, kyonin, licorice, senega, sycamore, asenyaku, sodium benzoate, caffeine, noscapine, maleic acid. Chlorpheniramine, salbutamol sulfate, ormprenaline sulfate, trimethoxynol hydrochloride, chlorprenaline hydrochloride,
Antitussive expectorants such as fenoterol hydrobromide, procaterol hydrochloride, acetylcysteine, ipratropium bromide, dextromethorphan phenol phthalate, chlorhexidine hydrochloride, depotassium chloride; eucalyptus oil,
Oral fungicides such as popyon iodine, domiphen bromide, benzalkonium chloride, diphenhydramine salicylate, hydrocortisone hydrochloride, iodine, potassium iodide, peppermint water, liquid phenol, clove oil, benzethonium chloride, thymol, depotassium chloride; sodium azulene sulfonate; Sodium bicarbonate, chlorhexidine hydrochloride, acetyl kitasamycin, tetracycline hydrochloride,
Bacitracin, oxytetracycline, fradiomycin sulfate, gramicidin hydrochloride, dexamethasone, triamcinolone acetonide, depotassium chloride, domiphen chloride, cetylpyridinium chloride, chlorpheniramine maleate, lysozyme chloride, acrynol , allantoi
Anti-inflammatory agents for rhinitis , pharyngitis, tonsillitis, stomatitis, glossitis, gingivitis, etc., such as dipotassium , dipotassium glycyrrhizinate; ethyl aminobenzoate, dibucaine hydrochloride , hydrochloric acid
Dental anesthetics such as diphenhydramine, tetracaine hydrochloride, homosulfamine, benzalkonium chloride, lidocaine, thecaine, benzyl alcohol, creosote, and ether; myrrh flow extract, zinc chloride, methyl salicylate, sodium gualenate, chlorhexidine, thymol, d- polneol, dl- camphor, l
-Menthol, benzoic acid, sodium lauryl diaminoethyl glycine, sodium copper chlorophyllin, chlorhexidine gluconate, biozole, etc .; mouthwash for prevention and disinfection, expectorants such as acetylcysteine, senega, etc. It is not limited only to such an example. These active ingredients are usually used alone or in combination of two or more. The amount of the active ingredient in the stock solution varies depending on the type,
Since it cannot be determined unconditionally, it is preferable to appropriately mix them according to the purpose. If the amount of the active ingredient is too large, for example, the amount of other components such as water becomes relatively small, and the solubility of the active ingredient may be reduced or it may be difficult to absorb the active ingredient. Less than 10% (wt%, the same applies hereinafter), especially 5
% Is preferable. Further, usually, in order to sufficiently exhibit the effect of blending the active ingredient, 0.01
%, Preferably 0.1% or more.

As described above, the stock solution used in the present invention contains the above-mentioned active ingredient and water. As the water to be blended here, purified water that is usually used for a stock solution of an aerosol composition is used. The amount of the water varies depending on the type and the amount of the active ingredient, and thus cannot be unconditionally determined. Usually, it is appropriately adjusted according to the purpose and use of the aerosol product of the present invention.

In the stock solution used in the present invention, besides the above-mentioned active ingredient and water, if necessary, for example, lactose, honey, syrup, sucrose, D-sorbitol, D-mannitol, D-xylose, l-menthol , Eucalyptus oil,
Flavoring agents such as licorice extract, fragrance and peppermint water; flavoring agents such as various natural synthetic fragrances; thickeners such as glycerin, propylene glycol, carboxymethylcellulose and methylcellulose; solubilizing agents such as ethanol and ether; citric acid and hydrogen carbonate PH adjusters such as sodium;
Preservatives such as parabenzoic acid esters; tar pigments, various natural pigments, vitamins (β-carotene, riboflavin,
A dye such as sodium copper chlorophyllin) may be appropriately added.

The propellant used in the aerosol composition contains oxygen and an inert gas. The propellant is incorporated in the aerosol composition in an amount of 0.05% or more, preferably 0.3% or more. It is desirable to be adjusted so that. When the amount of the propellant is less than the above range, the aerosol composition tends to be not sufficiently ejected. In addition, in order to accurately apply the aerosol composition to a desired site in the oral cavity, it is preferable that the jet state of the aerosol composition be a thread. Therefore, in order to make such a thread-like injection, the compounding amount of the propellant is preferably 5% or less.

The inert gas contained in the propellant includes, for example, nitrogen gas, carbon dioxide gas, argon gas and the like. In view of the injection state of the composition and the miscibility with oxygen, nitrogen gas is used. Alternatively, carbon dioxide gas is preferred. Further, oxygen is contained in the propellant in an amount of 15 to 35%, preferably 20 to 25%. When the oxygen content is less than 15%, the user may feel choppy or breathless due to the low oxygen content when the aerosol composition of the present invention is injected into the oral cavity. 35%
If it exceeds 100, it tends to react with the stock solution or the active ingredient.

By mixing the stock solution and the propellant, an aerosol composition to be used in the present invention is obtained, and the aerosol composition is filled into a pressure-resistant container for aerosol by a usual method, and is used as an aerosol product for oral cavity. Is done.

The pressure-resistant container for aerosol is not particularly limited, and a commonly used one can be used.

The amount of the aerosol composition filled in the oral aerosol product thus obtained is preferably adjusted so that the internal pressure of the product is usually 5 to 8 kg / cm ² at 35 ° C. Field according internal pressure in the case of less than 5 kg / cm ² is increased relatively propellant amount is required, they tend to be difficult to impart the desired injection mode, also exceeding 8 kg / cm ² In the meantime, there is a tendency that handling becomes difficult or an appropriate injection state cannot be obtained.

The number of times the oral aerosol product is used is as follows:
There is no particular limitation, and it is preferable to appropriately adjust according to the use and symptoms.

The injection state of the oral aerosol composition includes, for example, a foam, a mist, and a thread. In order to apply the composition to a desired site in the oral cavity accurately, the thread is preferably used. preferable.

In the present invention, in order to allow a stock solution containing an active ingredient to be quantitatively ejected from an aerosol product, for example, a metering valve having a structure as shown in FIG. 1 is used. be able to.

The metering valve shown in FIG. 1 is in a steady state (stationary state).

The nozzle 1 is connected to a stem 2, and a stem rubber 4 is pressed against a mounting cap 5 by a spring 3 provided below the stem 2, so that the aerosol product is kept in a sealed state. A tank 7 made of a flexible material such as rubber is provided on the outer periphery of the guide bush 6 fixing the stem rubber 4.
The tank 7 is fixed by a housing 8.
A dip tube 9 is connected to the lower surface of the housing 8. The aerosol container (not shown) is sealed and fixed via a gasket 10 between the mounting cap 5 and the housing.

The stock solution containing the active ingredient filled in the aerosol container enters the housing 8 through the dip tube 9 and passes through the gap between the stem 2 and the tank 7 and the gap between the stem 2 and the guide bush 6. Then, the liquid enters the guide bush 6, and is then filled into the metering chamber 12 formed between the guide bush 6 and the tank 7 through the hole 11.

The valve can be operated as shown in FIG. 2 by pressing the nozzle 1 downward.

The stock solution containing the active ingredient in the aerosol container (not shown) enters the inside of the housing 8 through the dip tube 9, but since the stem 2 and the tank 7 are completely sealed, the guide The stock solution is not introduced into the bush 6.

Since the internal pressure of the aerosol container is larger than the external pressure (atmospheric pressure) of the aerosol container, when the nozzle 1 is pressed downward, the gas introduction hole 13 of the nozzle 1 and the quantification chamber 12 communicate with the communication hole 14, When communicating with the guide bush 6, the pressure of the stock solution in the aerosol container introduced through the communication hole 15 causes the tank 7 to communicate as shown in FIG.
Is deformed, and the undiluted solution in the fixed amount chamber 12
6 , a discharge hole through a conduction hole 14 and a gas introduction hole 13 sequentially.
Discharged from 16.

As described above, when the metering valve as shown in FIG. 1 is used, a fixed amount of the stock solution filled in the metering chamber 12 is jetted out through the discharge hole 16 of the nozzle 1 to the outside. be able to.

Next, the oral aerosol product of the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples.

Example 1 Antitussive expectorant An aerosol composition was obtained by uniformly mixing 60 g of a stock solution having the composition shown in Table 1 and 0.3 g of a propellant consisting of 20% oxygen and 80% nitrogen gas.

The obtained aerosol composition was placed in a pressure-resistant container for aerosol (full volume: 100 ml) at 35 ° C. and an internal pressure of 6.5 kg / kg.
cm ^2, and a metering valve having the structure shown in FIG. 1 was used as an aerosol valve, and the metering valve and the nozzle were attached to produce an oral aerosol product.

[0030]

[Table 1]

The obtained oral aerosol product was directly sprayed on the pharyngeal head of a patient in which coughing and sputum expectoration appeared severely, and could be accurately sprayed on the pharyngeal head. Therefore, when preparing the aerosol composition for the oral cavity, the preparation of the aerosol composition did not require flavoring and odor correction, and was simple to prepare. In addition, without choking the patient is at the time of injection, the state of the respiration was not the same as normal.

Although the obtained oral aerosol product was used repeatedly, the stock solution could be repeatedly sprayed by a substantially constant amount (about 0.1 ml).

Example 2 (gargle) An aerosol was prepared in the same manner as in Example 1 except that 50 g of a stock solution having the composition shown in Table 2 and 1 g of a propellant consisting of 20% oxygen and 80% carbon dioxide gas were used. The composition was obtained and filled into an aerosol pressure container at 35 ° C. so that the internal pressure was 6.5 kg / cm ² , to produce an oral aerosol product.

[0034]

[Table 2]

When the obtained oral aerosol product was directly sprayed on the throat of a patient with severe throat inflammation, it could be accurately sprayed on the throat. Also, as in Example 1, the patient was not sick at the time of injection, and his respiratory condition was not different from normal.

Example 3 (Tooth Pain) The procedure of Example 1 was repeated except that 60 g of a stock solution having the composition shown in Table 3 and 0.3 g of a propellant consisting of 20% oxygen and 80% nitrogen gas were used. An aerosol composition was obtained and filled into a pressure-resistant container for aerosol at 35 ° C. so that the internal pressure was 6.5 kg / cm ² , to produce an aerosol product for oral cavity.

[0037]

[Table 3]

When the obtained oral aerosol product was directly sprayed on the affected area after tooth extraction of a severely painful patient, it could be accurately sprayed on the affected area. In addition, when the injection was performed according to Example 1, the patient was not sick and the state of breathing was not different from normal.

Example 4 (gargle) 60 g of a stock solution having the composition shown in Table 4, 25% oxygen and 2 g
Example aerosol composition but using a propellant 1 g consisting of 75% carbon dioxide gas in the same manner as in Example 1, this such that the internal pressure at 35 ° C. to aerosol pressure vessel is 6.0 kg / cm ² Into an oral aerosol product.

[0040]

[Table 4]

When the obtained oral aerosol product was directly sprayed on the throat of a patient with severe throat inflammation, it could be accurately sprayed on the throat. In addition, injection was performed in the same manner as in Example 1, but at the time of injection, the patient was not obstructed, and the state of breathing was not different from normal.

[0042] Example 5 stock solution 50 consisting of the composition shown in (stomatitis agent) Table 5 g, 20% oxygen and secondary
For example an aerosol composition in the same manner except for using a propellant 1 g consisting of 80% oxide-carbon gas as in Example 1, which is the internal pressure at 35 ° C. to aerosol pressure vessel becomes 6.0 kg / cm ² To make an oral aerosol product.

[0043]

[Table 5]

When the obtained oral aerosol product was directly sprayed on the inflamed site in the oral cavity of the patient, it could be accurately sprayed on the inflamed site. In addition, although the injection was performed according to the first embodiment, the patient was not obstructed during the injection,
His respiratory condition was unchanged.

Experimental Examples 1-3 Using the oral aerosol products obtained in Examples 1, 2 and 5, the accuracy of reaching the affected area, breathing, taste and tightness were determined by five subjects. It was examined and evaluated based on the following evaluation criteria. Table 6 shows the results.

The experimental aerosol products obtained in Examples 1, 2 and 5 were used in Experimental Examples 1, 2 and 3, respectively.

(Evaluation Criteria) ：: Of the five subjects, four or more felt good. Δ: Out of the five subjects, two or three felt good. ×: Out of five subjects, one or less felt good.

Comparative Experimental Examples 1 to 3 In Example 1, the propellant was replaced by liquefied petroleum gas (Comparative Experimental Example 1), and in Example 2, the propellant was replaced by nitrogen gas (Comparative Experimental Example 2). Example 1 using the so-called injection type pump without using the propellant and the stock solution obtained in Example 5 (Comparative Example 3)
Experiments were performed and evaluated in the same manner as in Examples 3 to 3. Table 6 shows the results.

[0049]

[Table 6]

From the above results, it was found that the oral aerosol products according to Examples 1, 2 and 5 of the present invention used in Experimental Examples 1 to 3 were accurate in reaching the affected area, breathing, taste and tightness. It turns out that it is excellent in any point.

[0051]

EFFECTS OF THE INVENTION The oral aerosol product of the present invention can ensure that the active ingredient is allowed to directly act on a specific site, has little adverse effect on other parts, and is expected to have a rapid effect of the active ingredient. Can be used, and without waste when using,
Since it is excellent in hygiene, there is an effect that it can be suitably used in the oral cavity.

[Brief description of the drawings]

FIG. 1 is a schematic cross-sectional view of a metering valve that can be used in the oral aerosol product of the present invention in a stationary state.

FIG. 2 is a schematic sectional view showing an operation state of a metering valve which can be used for the oral aerosol product of the present invention.

──────────────────────────────────────────────────続 き Continued on the front page (58) Field surveyed (Int. Cl. ⁷ , DB name) A61M 11/00 C09K 3/30 A61K ^7/ 00-7/50 A61K 9/12

Claims (2)

(57) [Claims] 1. A stock solution containing an active ingredient and an inert gas
An aerosol product for the oral cavity, characterized by containing an aerosol composition containing, as a main component, a propellant containing 15 to 35% by weight of oxygen . 2. The oral aerosol product according to claim 1, wherein the inert gas is nitrogen gas or carbon dioxide gas.