JP2949896B2 - Oral composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to oral compositions.
More specifically, the present invention relates to an oral composition for preventing oral diseases such as denture cleaning agents, toothpastes, mouthwashes, and troches.

[0002]

BACKGROUND OF THE INVENTION Candida, an oral pathogen
Since the causal relationship between Albicans (Candida albicans) and denture stomatitis was pointed out, it was necessary to remove denture stains not only from the appearance but also from the viewpoint of hygiene and prevention of oral diseases. Are known. Such denture stains consist of microorganisms that adhere to the denture and their products,
It is called "denture plaque". According to previous studies, denture plaques are formed by Candida fungi, especially Candida albicans.

[0003] Conventionally, there are peroxides, acid agents, bactericides and the like as a remover and a remover for Candida bacteria from dentures, but they have a cleaning effect, corrosiveness to dentures, and an effect of removing microorganisms from dentures. In each case, no sufficient effect has been obtained. For example, Japanese Patent Publication No. Sho 61-52124 discloses that a denture cleaning composition containing the hydrolase β-1,3-glucanase removes and lyses Candida. It is also described that proteases such as papain and trypsin, cellulases, lipases, mutanases and the like are effective enzymes for removing denture plaque (Japanese Patent Publication Nos. 61-52124, 63-101313, and 63-113313, Kosho 60-3532
No. 5, JP-B-63-25564), but these have not yet been able to obtain a sufficient effect. At present, denture plaque is also said to be similar to dental plaque, and it is necessary to remove mutans bacteria first, rather than Candida bacteria.

[0004] An object of the present invention is to provide an oral composition capable of effectively cleaning dentures and removing denture plaque, and effectively removing Candida and mutans bacteria to maintain oral hygiene. It is in.

[0005]

Means for Solving the Problems The present inventors have conducted various studies on the above-mentioned problems, and as a result, have found that the macerating enzyme is effective for removing Candida and mutans bacteria. Was completed.

[0006] That is, the present invention provides an oral composition containing a macerating enzyme as an active ingredient. The macerating enzyme has an excellent action to remove Streptococcus sp., Which is a major plaque-constituting bacterium, and also has an excellent bactericidal action and removal action against Candida albicans, and is effective in preventing the development of denture stomatitis . In addition, the enzyme has an excellent effect as an active ingredient of an oral composition such as a denture cleanser without having any harmful effect on the oral cavity and the denture.

[0007] The macerating enzyme is Rhizopus.
It is a generic term for crude pectinase derived from sp. Commercially available products include Macerozyme: Serva Fein
biochemica Gmbh & Co), Macerase: Si
gma).

[0008] Although mutanase and dextranase are also effective in removing denture plaque, only highly purified ones exhibit an effect, and are practical in view of cost and stability. is not.

The oral composition of the present invention contains, as active ingredients, protease and β in addition to the macerating enzyme.
-1,3-Glucanase, dextranase or mutanase may be incorporated. These enzymes may be added alone, or two or more of these enzymes may be added to the macerating enzyme.

The oral composition of the present invention is formed into various dosage forms by adding known excipients and other components according to the dosage form, in addition to the above-mentioned active ingredients, and dissolving it as it is or in water at the time of use. It is preferable to use them. Examples of the dosage form of the oral composition of the present invention include tablets, pills, granules, fine granules, powders, hard capsules, soft capsules, microcapsules, coated granules, coated tablets, ointments and the like. It can be molded and may be a liquid.

[0011] Excipients or auxiliaries used in the manufacture of the above-mentioned preparations include, for example, lactose, starch, corn starch, magnesium stearate, calcium stearate, dibasic calcium phosphate, sorbitol, carboxymethyl cellulose, tartaric acid, citric acid, carbonic anhydride Sodium, anhydrous sodium perborate, sodium bisulfate, Avicel, sodium hexametaphosphate, hydroxypropylcellulose, cerac, sucrose, ethylcellulose,
Hydroxypropyl methylcellulose, diethyl phthalate, dibutyl phthalate, talc, calcium sulfate,
Carbonized coal, gelatin, gum arabic, methylcellulose, carboxymethylcellulose, polyvinylpyrrolidone, sodium alginate, sodium chloride, sodium bicarbonate, sucrose, mannitol and the like are preferably used. In addition to the above-mentioned excipients or auxiliaries, when these preparations are dissolved in water, the aqueous solution shows an optimal pH of 3.5 to 7.0 for the macerating enzyme, and preservatives, coloring agents, fragrances, etc. You may add suitably.

The amount of the macerating enzyme in the oral composition of the present invention is 0.0
It is 1 to 30% by weight, preferably 0.1 to 10% by weight. When other enzymes such as protease are mixed and compounded, the amount of these enzymes to be added is 0.0 with respect to the composition.
It is 1 to 30% by weight, preferably 0.1 to 10% by weight.

Plaque removal test: 3 ml of a heat-killed suspension of C. albicans IFO1385 (Ca) was placed in a test tube, and the Streptococcus sobrinas (St.
reptococcus sobrinus OMZ176 (Ss)) and 2 ml of 5% sucrose phosphate buffer (0.05 M, pH 6.8). The test tube was inclined at an elevation angle of 30 ° and incubated at 37 ° C. for 16 hours to prepare an artificial plaque. After washing the formed plaque, 0.7% of the test enzyme solution was gently injected and allowed to act at 37 ° C. for 2 hours. After washing away the enzyme solution, the remaining plaque was suspended in 1N NaOH and the turbidity (OD 550) was measured (OD sample). The same operation was performed using a buffer solution instead of the enzyme solution (OD).
Control) and the removal rates of various enzymes were calculated according to the following equations. Removal rate (%) = {(OD control−OD sample) / OD control} × 100 Table 1 below shows the results when denture plaque was removed by various proteases.

Table 1 ━━━━━━━━━━━━━━━━━━━━━━━━━━━━━━━━━━━━ Concentration removal rate (%) Enzyme (W / V%) Ｓ S.s C.a ━━━━━━━━━━━━━━━━━━━━━━━━━━━━━ ━━━━━━━ Macerozyme 0.7 6021 protease 0.7 100 β-1,3-glucanase 0.7 0.45 dextranase 0.7 340 mutanase 0.7 38 30 lipase 0.70 0 amylase 0.7 0.7 macellozyme 1.4 81 35 macerozyme + protease 0.7 + 0.7 8765 macerozyme + β-1,3-glucanase 0.7 + 0.7 80 81 macerozyme + dextranase 0.7 + 0.7 95 75 75 Macerozyme + mutanase 0.7 + 0.7 100 97 ━━━━━━━━━━━━ ━━━━━━━━━━━━━━━━━━━━━━━━

[0015] Proteases, lipases and amylases
Neither Streptococcus mutans (S.s) nor Candida albicans (C.a.) shows almost no removal effect by itself. Mutanase and dextranase also have no sufficient removal effect on Ss and Ca. On the other hand, macerozyme shows an excellent effect by itself, and further shows an excellent synergistic effect when used in combination with protease, β-1,3-glucanase, dextranase or mutanase.

The composition for oral cavity of the present invention can be in the form of toothpaste, toothpaste, liquid dentifrice, mouthwash, pasta, denture cleaner, troche, chewing gum and the like.

[0017]

Next, the present invention will be described more specifically based on examples.

[Example 1] Toothpaste A toothpaste was produced by a conventional method using the following components.

━━━━━━━━━━━━━━━━━━━━━━━━━━ Component weight% ━━━━━━━━━━━━━━━━━第二 Calcium diphosphate 50.0 Sorbitol 15.0 Glycerin 10.0 Sodium lauryl sulfate 1.5 Carrageenan 1.0 Saccharin 0.1 Macerozyme 1.0 Fragrance 1.0 Water balance ─── １００ Total 100 ━━━━━━━━━━━━━━━━━━━━━━━━━ ━

[Example 2] Mouthwash A mouthwash was produced by a conventional method using the following components.

━━━━━━━━━━━━━━━━━━━━━━━━━━ component weight% ━━━━━━━━━━━━━━━━━ ━━━━━━━━━ Saccharin 0.1 Ethanol 8.0 Glycerin 20.0 Polyoxyethylene hydrogenated castor oil 1.0 Fragrance 0.5 Macerase 2.0 Water balance ────────── １００ Total 100 ━━━━━━━━━━━━━━━━━━━━━━━━━━

Example 3 Lozenges Lozenges were prepared by a conventional method using the following components.

━━━━━━━━━━━━━━━━━━━━━━━━━━ component weight% ━━━━━━━━━━━━━━━━━グ ル コ ー ス Glucose 75.0 Gum arabic 7.5 Fragrance 1.0 Macerase 1.5 Dextranase 0.5 Water balance ──────────────── １００ Total 100 ━━━━━━━━━━━━━━━━━━━━━━━━━━

Example 4 Denture Cleanser: Tablet A denture cleanser for tablets was produced by a conventional method using the following components.

━━━━━━━━━━━━━━━━━━━━━━━━━━ Component weight% ━━━━━━━━━━━━━━━━━ナ ト リ ウ ム Sodium bicarbonate 35.0 Sodium lauryl sulfate 1.0 Citric acid 3.0 Lactose 30.0 Magnesium stearate 0.5 Fragrance 1.5 Macerozyme 2.0 ────── １００ Total 100 ━━━━━━━━━━━━━━━━━━━━━━━━━━

Example 5 Denture Cleanser: Powder A powder denture cleanser was manufactured by a conventional method using the following components.

━━━━━━━━━━━━━━━━━━━━━━━━━━ Component weight% ━━━━━━━━━━━━━━━━━カ リ ウ ム Potassium dihydrogen phosphate 30.0 Sodium monohydrogen phosphate 20.0 Lactose 40.0 Fragrance 1.0 Macerozyme 5.0 Mutanase 4.0 ───────── １００ Total 100 ━━━━━━━━━━━━━━━━━━━━━━━━━━

Example 6 Denture Cleanser: Tablet A denture cleanser for tablets was produced by a conventional method using the following components.

━━━━━━━━━━━━━━━━━━━━━━━━━━ Component weight% ━━━━━━━━━━━━━━━━━ナ ト リ ウ ム Sodium bicarbonate 25.0 Sodium tripolyphosphate 5.0 Sodium lauryl sulfate 1.0 Citric acid 29.0 Lactose 30.0 Fragrance Trace amount of macerozyme 4.0 β-1,3-glucanase 6 0.0 ────────────────────────── Total 100 ━━━━━━━━━━━━━━━━━━━━ ━━━━━━

Example 7 Toothpaste A toothpaste was produced by a conventional method using the following components.

━━━━━━━━━━━━━━━━━━━━━━━━━━ Component weight% ━━━━━━━━━━━━━━━━━第二 Calcium diphosphate 50.0 Glycerin 20.0 Sodium lauryl sulfate 2.0 Carboxymethylcellulose 1.0 Saccharin 0.1 Flavor 0.9 Macerozyme 2.0 Protease 6.0 Water balance ── １００ Total 100 ━━━━━━━━━━━━━━━━━━━━━━━━ ━━

[0032]

EFFECT OF THE INVENTION The oral composition of the present invention has an excellent effect of removing the plaque-constituting bacteria Streptococcus spp. And Candida spp. By using the macerating enzyme as its active ingredient, Remove dental plaque and maintain oral hygiene and prevent oral diseases.

Claims (2)

(57) [Claims] An oral composition containing a macerating enzyme as an active ingredient. 2. The composition for oral cavity according to claim 1, further comprising at least one enzyme selected from protease, β-1,3-glucanase, dextranase and mutanase.