JPH09188610A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition exhibiting excellent antibacterial potency against bacteria in the oral cavity, and useful for preventing and treating gingivitis and preventing periodontal diseases. SOLUTION: This composition contains an extract obtained by removing pilocarpine from the leaves of pilocarpus, a kind of rutaceous plant (e.g. pilocarpus jaborandi). The extract is obtained, pref. by carrying out extraction of the above leaves with at least one kind of solvent (e.g. water, ethanol) at 5-100wt.times the dry leaves at 10-100 deg.C for one hour to 10 days. It is preferable that the amount of the extract to be formulated in this composition be 0.0001-10wt.% (on a dry basis) based on the whole amount of this composition.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an oral composition containing a plant extract, which has an excellent antibacterial effect against oral bacteria.

[0002]

Background Art Bacteria in the oral cavity cause gingivitis and alveolar pyorrhea, and are adsorbed and proliferated on the tooth surface to form plaque, which causes caries. In order to eliminate the cause, a bactericidal agent is added to the oral composition, but the effect is not sufficiently obtained, and recently, a further effective one is required.

On the other hand, citrus family Pilocarpus
Genus plants, such as Pilocarpus
jaborandi) is an evergreen shrub that is often found in Central and South America, especially Brazil, and its leaves are mainly used as a raw material for the production of pilocarpine (perspirants, miotics). Japanese Patent Laid-Open No. 2-8
In 3310, it is described that a hairnic containing an extract obtained by extracting hot water, hydroalcohol or the like from Pilocarpus yaborangi leaves is effective in preventing dandruff, preventing hair loss and promoting hair growth. However, an extract of a plant belonging to the genus Pilocarpus of the citrus family has never been applied to an oral composition.

[0004]

DISCLOSURE OF THE INVENTION The present invention provides an oral composition which exhibits excellent antibacterial activity against oral bacteria and is useful for the prevention and treatment of gingivitis and the prevention of periodontal disease. With the goal.

[0005]

[Means for Solving the Problems] As a result of intensive studies to achieve the above-mentioned object, the present inventors have incorporated an extract of leaves of the citrus family Pilocarpus genus plant into an oral composition. As a result, excellent antibacterial activity against oral bacteria was observed, and prevention, treatment of gingivitis, prevention of periodontal disease,
They have found that a therapeutic effect can be obtained, and completed the present invention. That is, the present invention includes the following inventions.

(1) Rutaceae Pilocarpus
An oral composition comprising an extract of leaves of a genus plant. (2) An oral composition comprising an extract obtained by removing pilocarpine from an extract of a leaf of a genus Pilocarpus of the citrus family.

Pilocarpus used in the present invention
The genus plant is not particularly limited and includes, for example, Pilocarpus jaborandi, Pilocarpus
Microfilus (Pilocarpus microphyllus), Pilocarp
us pennatifolius (Pilocarpus selloanus), Pilocarpus
racemosus, preferably Pilocarpus Jaborangi
ocarpus jaborandi), Pilocarpus microfilus (P
ilocarpus microphyllus). Plant leaves
Dry leaves or fresh leaves may be used.

The extract used in the present invention is preferably extracted with at least one solvent such as water, ethanol, acetone, ethyl ether, propylene glycol, ethylene glycol, glycerin, ethyl acetate and butyl acetate. The extraction operation is not particularly limited, but for example, 5 to 100 parts by weight of the solvent is preferable to 1 part by weight of dried leaves. The temperature and time at the time of extraction at that time are preferably 10 to 100 ° C. and 1 hour to 10 days.

The obtained extract may be used as it is, or if necessary, may be subjected to processing such as concentration, drying and purification. Since pilocarpine is contained in the leaf extract of the pilocarpus genus plant, it is inferior in safety. Therefore, it is preferable to use a pilocarpine-treated product.

As a means for removing pilocarpine from the extract, column chromatography using an ion exchange resin is preferably used. As the ion exchange resin, Diaion (manufactured by Mitsubishi Chemical Co., Ltd.), Mcl gel (manufactured by Mitsubishi Chemical Co., Ltd.) and the like are used.
Ethanol, acetone, 1,3-butylene glycol, etc. can be used.

The content of the extract in the oral composition of the present invention is usually 0.00001 to 50% by weight, preferably 0.1% by dry weight, based on the total weight of the oral composition.
It is 0001 to 10% by weight. Compounding amount 0.00001
If it is less than 50% by weight, the antibacterial effect cannot be obtained, and if it exceeds 50% by weight, the antibacterial effect cannot be expected to increase and it is uneconomical. In addition,
The extract, which is an active ingredient, is an extract, the extract is pilocarpine-removed, and these have a solid content of 16%.
A concentrated product or a dried product is used.

[0012]

Preferred embodiments of the present invention will be described below. Pilocarpu
s jaborandi), Pilocarps Microfils
The dried leaves such as pus microphyllus) are extracted with 5 to 100 parts by weight of extraction solvent such as water based on 1 part by weight of the dried leaves. The temperature and time at the time of extraction at that time are 10 to 100.
The temperature is set to 1 ° C. for 1 hour to 10 days.

If necessary, the obtained extract is subjected to processing such as concentration, drying and purification, and then pilocarpine is removed by column chromatography using an ion exchange resin. As the ion exchange resin, Diaion (manufactured by Mitsubishi Chemical Co., Ltd.), Mcl gel (manufactured by Mitsubishi Chemical Co., Ltd.) or the like is used, and as the eluent, for example, water, ethanol, acetone, 1,3-
Butylene glycol or the like is used.

The active ingredient thus obtained is converted into a dry weight of 0.0001 based on the total amount of the oral composition.
The composition for oral cavity of the present invention is prepared by mixing 10 to 10% by weight. The oral composition of the present invention, as another component, if toothpaste, an abrasive such as calcium hydrogen phosphate dihydrate, a binder such as carboxymethyl cellulose, a thickener such as polyethylene glycol, lauryl A foaming agent such as sodium sulfate, a sweetening agent such as sodium saccharin, a preservative and other components are mixed with water, and the mixture is produced by a conventional method.
In addition, mouthwash such as mouthwash, and the like, appropriately contain components according to the properties of the product.

In addition, the oral composition of the present invention may contain active ingredients such as hinokitiol, vitamin E, tranexamic acid, glycyrrhizic acid or salts thereof.

[0016]

EXAMPLES The present invention will now be described with reference to examples and preparation examples, but the present invention is not limited thereto.

Preparation Example 1 Preparation of Pilocarpus Leaf Extract 3 kg of dried leaves of Pilocarpus jaborandi and 60 L of purified water were heated and gently refluxed for 4 hours, and then filtered to about 50 kg of extract (A) was obtained. The solid content at that time was 1 kg. Diameter 5 filled with 10 kg of Diaion SK-1B (manufactured by Mitsubishi Chemical Corporation).
After the same amount of 5% hydrochloric acid as the resin was passed through a 5 cm chromatographic column, the eluate was made almost neutral by passing through purified water, and then the extract (A) was passed through as an eluent. 20k of water
68 g of the extract (B) was obtained using g.

As the mixing means of the extract (A) and the extract (B) thus obtained, the extract is directly or if necessary, concentrated under reduced pressure to obtain a solid content of 16%.
It is only necessary to add a concentrated product or a dried product.

(Examples 1 to 3 and Comparative Examples 1 to 3) Antibacterial activity of each extract against various pathogenic bacteria Regarding the toothpaste obtained by the formulation of Table 1, Streptococcus mutans NI
DR 6715) and Actinomyces viscosus (Actinomyc
Each antibacterial activity against es viscosus ATCC 15987) was examined by the following test methods. As a test solution, each formulation was diluted with dimethyl sulfoxide to a concentration of 20 mg / ml. In addition, minocycline (antibiotic) is used as a reference substance to confirm proper test operation.
The antibacterial effect was also examined for a product obtained by diluting the above with distilled water to a concentration of 25 μg / ml (control example).

(Test method for antibacterial effect against Streptococcus mutans and Actinomyces viscosus) A medium having the following composition was autoclaved to 12
Heat treatment was performed at 1 ° C for 15 minutes to obtain a plate-shaped agar medium.

Composition: Brain Heart Infusion (Becton Dickinson) 9.6 g Biosate Peptone (Becton Dickinson) 5.0 g Tripticase Peptone (Becton Dickinson) 5.0 g Yeast Extract (Becton Dickinson) 5.0 g Salt Solution (mixture of A and B below) 20.0 ml Agar powder (manufactured by Nacalai Tesque) 2.5 g Hemin Solution (manufactured by Sigma) 5.0 ml Menadione (manufactured by Nacalai Tesque) 0.1 ml Purified water 480.0 ml [Solution A] Calcium chloride (dihydrate) (Katayama Chemical Co., Ltd.) 0.025 g Magnesium sulfate (anhydrous) (Katayama Chemical Co., Ltd.) 0.02 g Purified water 30 ml [Solution B] Dipotassium hydrogen phosphate (Dihydrate) (Nacalai Tesque) 0.1 g Potassium dihydrogen phosphate (monohydrate) (Nacalai Tesque) 0.1 g Sodium hydrogen carbonate (Nacalai Tesque) 1.0g Sodium chloride (Nacalai Tesque) 0.2g Purified water 50ml

Then, 50 μl of each test solution was soaked in a paper disk having a diameter of 8 mm and dried sufficiently, and then inoculated and dispersed with about 10 ⁸ (the number of bacteria) Streptococcus mutans and Actinomyces viscosus in advance. The diameter of the growth-inhibiting circle at the end of cultivation (unit: mm)
Was measured to examine the antibacterial effect of each test solution against Streptococcus mutans and Actinomyces viscosus. Table 2 shows the results. In addition, it was confirmed in advance that no growth-inhibiting circle appeared in this case by infiltrating only dimethyl sulfoxide into the paper disc and culturing in the same manner.

[0023]

[Table 1]

[0024]

[Table 2]

(Example 4) Mouthwash Extract (B) Concentrate (solid content 16%) 1.5 parts by weight Ethanol 10.0 parts by weight Polyoxyethylene hydrogenated castor oil 2.0 parts by weight Propylene glycol 5.0 Parts by weight sodium saccharin 0.2 parts by weight fragrance 0.5 parts by weight l-menthol 0.5 parts by weight water balance 100.0 parts by weight

Example 5 Gingival Massage Cream Extract (A) 10.0 parts by weight White petrolatum 12.0 parts by weight Stearyl alcohol 5.0 parts by weight Propylene glycol 4.0 parts by weight Polyethylene glycol 2000 20.0 parts by weight Polyethylene glycol 400 30.0 parts by weight Cetanol 7.0 parts by weight Perfume 0.5 parts by weight Water balance 100.0 parts by weight

(Example 6) Lozenge Extract (B) Dry solid 0.01 parts by weight Gum arabic 6.0 parts by weight Maltose 25.0 parts by weight Glucose 25.0 parts by weight Fructose 20.0 parts by weight Perfume 0. 1 part by weight Water balance 100.0 parts by weight (Example 7) Chewing gum Extract (B) Concentrate (solid content 16%) 5.0 parts by weight Mannitol 20.0 parts by weight Solbit 3.5 parts by weight Perfume 1 0.0 parts by weight Gum base balance 100.0 parts by weight

Example 8 Mouthwash Tablet Extract (B) Dry Solid 5.0 parts by weight Disodium hydrogen phosphate 15.0 parts by weight Polyethylene glycol 6000 3.0 parts by weight Citric acid 10.0 parts by weight Apple Acid 10.0 parts by weight Ethanol 6.0 parts by weight Perfume 4.0 parts by weight Sodium hydrogen carbonate balance remainder 100.0 parts by weight

[0029]

INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide an oral composition having an excellent antibacterial effect against oral bacteria.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Minoru Yasuda 12-7 Nibancho, Chiyoda-ku, Tokyo Tsumura Co., Ltd.

Claims (2)

[Claims] 1. An oral composition comprising an extract of leaves of a plant belonging to the genus Pilocarpus of the citrus family. 2. An oral composition comprising an extract obtained by removing pilocarpine from a leaf extract of a plant of the citrus family Pilocarpus genus.