JPH08268851A - Composition for oral cavity - Google Patents

Abstract

PURPOSE: To obtain a composition for oral cavities, capable of reducing the original bitter taste of an antiinflammatory medicine over a long period, good in taste, and mouth touch, and useful for treating and preventing oral cavity diseases by compounding an acidic non-steroidal antiinflammatory medicine and a perfume component. CONSTITUTION: A composition containing an acidic non-steroidal antiinflammatory medicine and used for oral cavities is compounded with one or more kinds of perfume components selected from carvone, cineol, menthone, camphor, borneol and cinnamic aldehyde in an amount of 0.01-5wt.% based on the composition. The weight ratio of the perfume component to the acidic non-steroidal antiinflammatory medicine is 0.01-10 times. The acidic non-steroidal antiinflammatory agent is preferably an arylpropionic acid antiinflammatory medicine, more preferably ibuprofen or flurbiprofen. The composition is prepared into a dentifrice such as a tooth paste, a tooth powder or a tooth liquid, a liquid mouth refrigerant such a mouth wash, a solid mouth refrigerant such as a troche, a chewing gum, a paste for oral cavities, etc., and is useful for oral cavity diseases such as gingivitis, periodontitis and dental caries halitosis.

Description

Detailed Description of the Invention

[0001]

The present invention relates to an oral composition,
More specifically, with respect to the oral composition containing an acidic non-steroidal anti-inflammatory agent as an active ingredient, the bitterness derived from the anti-inflammatory agent is improved for a long time, and treatment of periodontal disease such as gingivitis and periodontitis and The present invention relates to an oral composition having an excellent preventive effect.

[0002]

2. Description of the Related Art Acidic non-steroidal anti-inflammatory agents have a strong anti-inflammatory effect and have been tried to be applied to oral compositions in the past (Japanese Patent Laid-Open Nos. 60-61524 and 52-3.
No. 8030), and is effective for treating and preventing periodontal diseases such as gingivitis and periodontitis.

However, an oral composition containing an acidic nonsteroidal anti-inflammatory agent such as ibuprofen is
There was a problem of being bitter. Generally, a fragrance component is blended to improve the bitterness of the oral composition, but many fragrance components such as citronellal, linalool, and citral have a problem that the improvement in bitterness does not continue.

[0004]

SUMMARY OF THE INVENTION The present invention has been made by paying attention to the problems of the prior art as described above.
Long-term improvement of the bitterness of acidic non-steroidal anti-inflammatory drugs,
It is intended to provide an oral composition having a good taste.

[0005]

The oral composition of the present invention which has been able to solve the above-mentioned problems is an oral composition containing an acidic non-steroidal anti-inflammatory agent, wherein carvone, cineol, 1 selected from the group consisting of menthone, camphor, borneol and cinnamic aldehyde
It is characterized in that it is a mixture of two or more kinds.

[0006]

The present inventor has conducted various studies on the composition of an oral composition capable of improving taste for a long term when an acidic non-steroidal anti-inflammatory agent is added. As a result, it has been found that the bitterness derived from an anti-inflammatory agent can be improved by blending one or more selected from the group consisting of carvone, cineol, menthone, camphor, borneol, and cinnamic aldehyde, and the present invention. Has been completed.

The present invention will be described in more detail below.

The acid non-steroidal anti-inflammatory agent according to the present invention may be either free or pharmaceutically acceptable acid addition salt. For example, as phenylacetic acid type, diclofenac sodium, fenbufen, etc., and indole acetic acid type. Is indomethacin, acemetacin, sulindac, etc., as a propionic acid type, ibuprofen,
Flurbiprofen, pranoprofen, ketoprofen, and the like, examples of the anthranilic acid type include phenacetin, acetaminophen, and mefenamic acid.Arylpropionic acid type anti-inflammatory agents are preferable, and ibuprofen and Flurbiprofen can be mentioned. The content of these anti-inflammatory agents should be appropriately determined according to the dosage form of the liquid preparation, the type of drug, etc., but when using ibuprofen and / or flurbiprofen, the total amount thereof As a whole composition, preferably 0.01 to 5% by weight, more preferably 0.05 to
It is contained in the range of 1% by weight.

The oral composition of the present invention is at least one selected from the group consisting of carvone, menthone, cineol, camphor, borneol and cinnamic aldehyde.
One kind or two or more kinds are blended. These compounds are 0.01 to 10 times, more preferably,
Particularly preferable effects can be obtained when blended in an amount of 0.01 to 0.5 times. Further, it is preferably blended in an amount of 0.001 to 2% by weight, more preferably 0.05 to 0.5% by weight, based on the entire oral composition. If the blending amount is less than 0.01 times by weight or less than 0.001% by weight, the bitterness derived from the medicinal agent may not be reduced in the long term, and may be 10 times or 2 times.
If the content is more than 10% by weight, irritation to the oral cavity tends to be strong, and there is a problem in that the feeling of use deteriorates. Further, the above components may be blended as an essential oil or oleoresin containing the components.

In the oral composition of the present invention, carvone,
In addition to cineol, menthone, camphor, borneol, cinnamic aldehyde, l-menthol, limonene, terpinone, menthane, terpinene, eugenol, carvacrol, isoeugenol, resorcin,
Other perfume ingredients such as salicylic acid, methyl salicylate, thymol and anethole may be added.

The oral composition according to the present invention is a toothpaste such as toothpaste, powder toothpaste, liquid toothpaste, liquid mouth freshener such as mouthwash, solid mouth freshener such as troche, chewing gum,
Applicable as an oral pasta and the like, the oral composition of the present invention, if necessary, an abrasive, a viscosity adjusting agent, a sweetener, a wetting agent and the like, an appropriate component is selected and blended. To be done.

For example, in the composition for oral cavity, dibasic calcium phosphate dihydrate and anhydride, monobasic calcium phosphate, tribasic calcium phosphate, disodium phosphate, monosodium phosphate, citric acid monohydrate. And anhydrate, trisodium citrate, disodium citrate, dl-malic acid, dl-sodium malate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, alumina,
One or more of silicic acid anhydride, silica, silica gel, aluminosilicate, aluminum silicate, insoluble sodium metaphosphate, magnesium triphosphate, calcium sulfate, polymethylmethacrylate, bentonite, zirconium silicate, etc. are blended. obtain.

In the case of paste or gel such as toothpaste, composition such as ointment, carrageenan, sodium carboxymethyl cellulose, methyl cellulose, hydroxyethyl cellulose, sodium carboxymethyl hydroxyethyl cellulose, hydroxypropyl methyl cellulose as a binder, Cellulose derivatives such as hydroxypropyl cellulose, alkali metal alginates such as sodium alginate, propylene glycol alginate, xanthan gum, tragacanth gum, karaya gum, gums such as gum arabic, polyvinyl alcohol, polyvinyl acetate, sodium polyacrylate, carboxyvinyl polymer, polyvinyl Synthetic binders such as pyrrolidone, silica gel, aluminum silica gel, vinyl Gum, inorganic binder such as one including laponite or two or more can be formulated.

Furthermore, pastes, gels, ointments of toothpaste,
In the production of a liquid oral composition, as a viscous agent, one or more of sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltite, lactit and the like are used. It may be blended.

Further, the oral composition of the present invention has a carbon number of a fatty acid group such as a water-soluble salt of an alkyl sulfate ester such as sodium lauryl sulfate, higher fatty acid sodium, sodium lauryl monoglyceride sulfonate, sodium coconut monoglyceride sulfonate and the like. Is 10-18
Higher fatty acid monoglyceride sulfonate water-soluble salt, higher fatty acid sodium monoglyceride monosulfate, olein sulfonate, paraffin sulfonate, fatty acid mono or diethanolamide such as lauric acid mono or diethanolamide, stearyl monoglyceride, sucrose mono or dilaurate fatty acid Sucrose fatty acid ester having a carbon number of 12 to 18, lactose fatty acid ester, lactitol fatty acid ester, maltitol fatty acid ester, stearic acid monoglyceride, polyoxyethylene sorbitan monolaurate,
Nonionic surfactants such as polyoxyethylene hardened castor oil, sorbitan monostearate with about 60 mol of ethylene glycol added, polymers of ethylene oxide and propylene oxide, and derivatives of polyoxyethylene polyoxypropylene monolauryl ether and the like, One type or two or more types of surfactants such as betaine type double-sided surfactants can be blended.

Further, the oral composition of the present invention includes p-hydroxymethyl benzoate, p-hydroxyethyl benzoate, p-hydroxypropyl benzoate, sodium benzoate, lower fatty acid monoglyceride and the like. Preservatives, titanium dioxide, ethanol, liquid paraffin, pigments, and other components may be added, and for example, in the case of toothpaste, the above-mentioned desired components may be produced by kneading with an appropriate amount of water. Also, when other oral compositions are produced, they can be produced according to a conventional method using appropriate components that are usually used.

In the present invention, as the active ingredient, cetylpyridinium chloride, a cationic bactericidal agent such as chlorhexidine salt, dextranase, amylase, protease, mutanase, lysozyme, enzymes such as lytic enzyme (retic enzyme), Alkali metal monofluorophosphates such as sodium monofluorophosphate, potassium monofluorophosphate, sodium fluoride, fluorides such as stannous fluoride, tranexamic acid and epsilon aminocaproic acid, aluminum chlorohydroxyallantoin, dihydrocholesterol, glycyrrhizinate ,
One or more kinds of active ingredients such as glycyrrhetinic acid, glycerophosphate, chlorophyll, sodium chloride, caropeptide, water-soluble inorganic phosphate compound may be blended.

[0018]

EXAMPLES Next, the present invention will be described in more detail by showing experimental examples and examples, but the present invention is not limited to these, and changes and modifications can be made without departing from the spirit of the above and the following. All that is included in the technical scope of the present invention.

Experimental Example 1 Liquid formulations were prepared according to the conventional method according to the formulations shown in Tables 1 to 6. The bitterness test was conducted by the following method on the obtained liquid preparation and the product left at 40 ° C. for 1 month.

Bitterness test: 20 ml of the liquid preparation was rinsed for about 30 seconds, and the degree of bitterness remaining in the mouth after the vomiting was sensory-evaluated by 5 panelists in 5 levels. The evaluation criteria are as follows. The results are shown in Tables 1-6.

(Evaluation Criteria) −: No bitterness ±: Bitterness is difficult to understand ＋: Bitterness ++: Quite bitterness +++: Very bitterness

[0022]

[Table 1]

[0023]

[Table 2]

[0024]

[Table 3]

[0025]

[Table 4]

[0026]

[Table 5]

[0027]

[Table 6] As is clear from Tables 1 to 6, in Comparative Example 1, the bitterness of the medicinal agent was not reduced because the flavor component was not mixed.
In addition, as in Comparative Examples 2 to 12, citronellal, linalool, and citral are blended as fragrance ingredients.
After left at 0 ° C. for 1 month, the bitterness was not improved. On the other hand, in Examples 1 to 49, by blending carvone, cineol, menthone, camphor, borneol, and cinnamic aldehyde in a weight ratio of 0.01 times or more with respect to ibuprofen, the bitterness of the medicinal agent is improved for a long time. Has been done.

Example 50 In this example, a liquid preparation was prepared according to a conventional method according to the following formulation.

Ingredient content (%) Ibuprofen 0.2 Saccharin sodium 0.01 Ethanol 2.0 Sorbit 10.0 Polyoxyethylene hydrogenated castor oil 1.0 Glycerin 8.0 Carvone 0.05 l-Menthol 0.05 Perfume 0.05 pH adjuster Appropriate amount Purified water balance 100.0 Total liquid formulation obtained When the bitterness of No. 1 was evaluated by the above-mentioned method, good results were obtained.

Example 51 In this example, a liquid preparation was prepared according to a conventional method according to the following formulation.

Ingredient content (%) Cetylpyridinium chloride 0.05 Ibuprofen 0.1 Tranexamic acid 0.05 Sodium saccharin 0.01 Ethanol 3.0 Polyoxyethylene hydrogenated castor oil 0.5 Glycerin 8.0 Camphor 0.2 l-menthol 0.1 Perfume 0.1 pH adjuster Appropriate amount Purified water Residual total 100.0 When the bitterness of the obtained liquid preparation was evaluated by the above method, good results were obtained.

Example 52 In this example, a liquid preparation was prepared according to a conventional method according to the following formulation.

Ingredient content (%) Flurbiprofen 0.1 Cetylpyridinium chloride 0.05 Saccharin sodium 0.01 Ethanol 2.0 Sucrose fatty acid ester 0.3 Glycerin 8.0 Mentone 0.1 Limonene 0.2 Perfume 0.1 pH adjuster Appropriate amount Purified water balance 100.0 Total liquid obtained When the bitterness of the preparation was evaluated by the method described above, good results were obtained.

Example 53 In this example, a liquid preparation was prepared according to a conventional method according to the following formulation.

Ingredients Content (%) Chlorhexidine gluconate 1.0 Ibuprofen 0.1 Sodium saccharin 0.01 Glycerin 15.0 Ethanol 2.0 Polyoxyethylene hydrogenated castor oil 1.0 Dipotassium glycyrrhizinate 0.05 Carvone 0.1 l-Menthol 0.2 Perfume 0.2 Purified water Residual total 100.0 When the bitterness of the liquid preparation was evaluated by the above method, good results were obtained.

Example 54 In this example, a liquid preparation was prepared according to a conventional method according to the following formulation.

Ingredient content (%) Cetylpyridinium chloride 1.0 Ibuprofen 0.1 Saccharin sodium 0.01 Glycerin 10.0 Polyoxyethylene hydrogenated castor oil 1.0 Ethanol 2.0 Tranexamic acid 0.05 Camphor 0.1 Eugenol 0.1 Perfume 0.2 Purified water balance 100.0 Total of the obtained liquid formulation When the bitterness was evaluated by the above method, good results were obtained.

Example 55 In this example, a liquid preparation was prepared according to a conventional method according to the following formulation.

Component content (%) Cetylpyridinium chloride 0.05 Ibuprofen 0.5 Glycerin 10.0 Sodium saccharin 0.02 Polyoxyethylene hydrogenated castor oil 1.0 Ethanol 3.0 Cynamic aldehyde 0.1 l-Menthol 0.2 Perfume 0.1 pH adjuster Appropriate amount Purified water balance Total 100.0 When the bitterness of the liquid preparation was evaluated by the above method, good results were obtained.

[0040]

EFFECTS OF THE INVENTION According to the present invention, in an oral composition containing an acidic non-steroidal anti-inflammatory agent, at least one selected from the group consisting of carvone, cineol, menthone, camphor, borneol, and cinnamic aldehyde, or By blending two or more kinds, an oral composition capable of reducing the bitterness of an acidic non-steroidal anti-inflammatory agent over a long period of time was realized. The oral composition of the invention can sufficiently exhibit the anti-inflammatory effect and the alveolar bone resorption suppressing effect of the acidic non-steroidal anti-inflammatory agent,
It is useful for treating and preventing oral diseases such as gingivitis, periodontitis, caries and halitosis.

Claims (6)

[Claims] 1. An oral cavity comprising an acidic non-steroidal anti-inflammatory agent and at least one or two or more selected from the group consisting of carvone, cineol, menthone, camphor, borneol and cinnamic aldehyde. Composition. 2. The oral composition according to claim 1, wherein the acidic non-steroidal anti-inflammatory agent is an arylpropionic acid anti-inflammatory agent. 3. The arylpropionic acid anti-inflammatory agent is ibuprofen and / or flurbiprofen.
The composition for oral cavity according to. 4. The oral composition according to claim 1, wherein the content of the acidic non-steroidal anti-inflammatory agent is 0.01 to 5% by weight based on the entire oral composition. 5. The compounding amount of the group consisting of carvone, cineol, menthone, camphor, borneol and cinnamic aldehyde is 0.001-2 with respect to the entire oral composition.
The composition for oral cavity according to claim 1, wherein the composition is wt%. 6. The compounding amount of the group consisting of carvone, cineol, menthone, camphor, borneol and cinnamic aldehyde is 0.01 to 10 times by weight of the acidic nonsteroidal anti-inflammatory agent. The composition for oral cavity according to 5.