JPH04316511A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain an oral cavity composition containing an macerating enzyme as an active ingredient and capable of effectively carrying out cleaning of artificial tooth and removal of dental plaque, removing Candida and mutans and keeping hygiene in oral cavity. CONSTITUTION:The objective oral cavity composition containing at least one kind of enzyme selected from a macerating enzyme which is an enzyme having pectinase activity, hemicellulase activity, etc., and further as necessary at least one kind of enzyme selected from protease, beta-1,3-glucanase, dextranase and mutanase as active ingredients. The composition is directly used by adding well-known diluent and other ingredients to the above-mentioned active ingredient and forming the mixture in various preparation forms or used by dissolving the obtained preparation in water when used.

Description

[Detailed description of the invention]

0001

FIELD OF THE INVENTION This invention relates to oral compositions. More specifically, the present invention relates to oral compositions for preventing oral diseases, such as denture cleaners, toothpastes, mouthwashes, and troches.

0002

[Prior art and problems] Oral pathogenic bacteria Candida
Candida albicans
Since the causal relationship between dentures and denture-induced stomatitis was pointed out, it has been known that removing stains from dentures is necessary not only for the sake of appearance, but also from the standpoint of hygiene and prevention of oral diseases. Such stains on dentures are composed of microorganisms and their products that adhere to the dentures, and are called "denture plaque." According to previous research, denture plaque is formed by Candida fungi, especially Candida albicans.

[0003] Conventional agents for removing Candida bacteria from dentures and cleaning agents include peroxide agents, acids, and bactericidal agents. In both respects, sufficient effects have not been obtained. For example, Japanese Patent Publication No. 61-52124 discloses that a denture cleaning composition containing a hydrolase β-1,3-glucanase removes and lyses Candida bacteria. Furthermore, it is stated that proteases such as papain and trypsin, cellulases, lipases, mutanase, etc. are effective enzymes for removing denture plaque (Japanese Patent Publication No. 52124/1983, Japanese Patent Application Laid-Open No. 101313/1989, Kosho 60-3532
No. 5, Japanese Patent Publication No. 63-25564), but these have not yet achieved sufficient effects. Furthermore, it is now said that denture plaque is similar to dental plaque, and it is necessary to remove Streptococcus mutans before Candida.

An object of the present invention is to provide an oral composition that can effectively clean dentures, remove denture plaque, and effectively remove Candida and Streptococcus mutans to maintain oral hygiene. There is a particular thing.

[0005]

[Means for Solving the Problems] As a result of various studies regarding the above-mentioned problems, the present inventors obtained the knowledge that maceration enzymes are effective in removing Candida and Streptococcus mutans, and based on this, the present invention was developed. I was able to complete it.

That is, the present invention provides an oral composition containing a macerating enzyme as an active ingredient. Macerating enzyme has an excellent effect on its own in removing Streptococcus, which is a major plaque constituent bacteria, and also has excellent bactericidal and removal effects against Candida albicans, and is effective in preventing the occurrence of denture-related oral inflammation. . Furthermore, the enzyme exhibits excellent effects as an active ingredient of oral compositions such as denture cleaners without exerting any harmful effects on the oral cavity and dentures.

[0007] Macerating enzyme is Rhiz
opus sp. It is a general term for crude pectinases derived from
It is an enzyme that has pectinase activity, hemicellulase activity, etc. As a commercially available product, Macerozyme (Macer
ozyme: Serva Feinbiochemi
ca Gmbh & Co), macerase (Macerase)
(manufactured by Sigma) and the like.

[0008] Some mutanase and dextranase are also effective in removing denture plaque, but only highly purified forms are effective, and they are not practical in terms of cost and stability. isn't it.

[0009] The oral composition of the present invention contains protease, β
-1,3-glucanase, dextranase or mutanase may be added. These enzymes may be added alone, or two or more of these enzymes may be added to the maceration enzyme.

[0010] In addition to the above-mentioned active ingredients, the oral composition of the present invention can be formed into various dosage forms by adding appropriate known excipients and other ingredients depending on the dosage form, and can be prepared as is or dissolved in water before use. It is preferable to use it. The dosage form of the oral composition of the present invention includes, for example, tablets, pills, granules, fine granules, powders, hard capsules, soft capsules, microcapsules,
It can be formed into coated granules, coated tablets, ointments, etc., and may also be made into liquid preparations.

Excipients or adjuvants used in the production of the above formulations include, for example, lactose, starch, corn starch, magnesium stearate, calcium stearate, dibasic calcium phosphate, sorbitol, carboxymethylcellulose, tartaric acid, citric acid, carbonic anhydride. Sodium, anhydrous sodium perborate, sodium bisulfate, avicel, sodium hexametaphosphate, hydroxypropyl cellulose, shellac, white sugar, ethyl cellulose,
Hydroxypropyl methylcellulose, diethyl phthalate, dibutyl phthalate, talc, calcium sulfate,
Charcoal, gelatin, gum arabic, methylcellulose, carboxymethylcellulose, polyvinylpyrrolidone, sodium alginate, sodium chloride, sodium bicarbonate, sucrose, mannitol, and the like are preferably used. In addition to the excipients or adjuvants mentioned above, when these preparations are dissolved in water, the aqueous solution exhibits an optimum pH of 3.5 to 7.0 for the maceration enzyme, preservatives, coloring agents,
Flavoring agents may also be added as appropriate.

[0012] The amount of maceration enzyme in the oral composition of the present invention is 0.0% based on the composition.
It is 1 to 30% by weight, preferably 0.1 to 10% by weight. In addition, when other enzymes such as protease are mixed and blended, the amount of these enzymes is 0.01% of the composition.
-30% by weight, preferably 0.1-10% by weight.

Plaque removal test: Candida albicans (C. albicans IFO1385) in a test tube.
C. Add 3 ml of heat-killed bacterial suspension of a)) and add Streptococcus sobrinus (Streptococcus s
Crude glucosyltransferase (GTF) of S. obrinus OMZ176 (S.s.) and 2 ml of 5% sucrose-containing phosphate buffer (0.05 M, pH 6.8) were added and mixed. This test tube was tilted at an elevation angle of 30° and incubated at 37° C. for 16 hours to prepare an artificial plaque. After washing the formed plaques, 0.7% test enzyme solution was gently injected and allowed to act at 37°C for 2 hours. After discarding the enzyme solution and washing, the remaining plaques were suspended in 1N NaOH and the turbidity (OD550) was measured (OD sample). A similar operation was performed using a buffer solution instead of the enzyme solution (OD control), and the removal rate of various enzymes was calculated according to the following formula. Removal rate (%) = {(OD control - O.D sample)/O.D. D control}×100 Table 1 below shows the results when denture plaque was removed using various proteases.

Table 1 ━━━━━━━━━━━━━━━━━━━━━━━━━
━━━━━━━━━━━

Concentration Removal rate (%) Fermentation
Basic
(W/V%) ────────
──

S. sC. a━━━━━━
━━━━━━━━━━━━━━━━━━━━━━━━━
━━━━━Macerozyme
0.7
60 21 protease
0.
7 10 0β-1,3
-Glucanase
0.7 0 45 dextranase
0.7 34
0 mutanase
0.7
38 30 lipase

0.7 0 0 amylase
0.7 0
0 Macerozyme
1.4
81 35 Macerozyme + Protease 0.7 + 0.7
87 65 Macerozyme + β-1,3-
Glucanase 0.7+0.7 80
81 Macerozyme + Dextranase
0.7 + 0.7 95 75 Macerozyme + Mutanase
0.7+0.7 100 97━━━━
━━━━━━━━━━━━━━━━━━━━━━━━━
━━━━━━━

[0015] Protease, lipase,
Amylase is produced by Streptococcus mutans (S
．． When used alone, it shows almost no removal effect on either Candida albicans (C.a) or Candida albicans (C.a). Mutanase and dextranase are also sufficient for S. s,C. There is no removal effect on a. On the other hand, macerozyme alone showed excellent effects, and also showed protease, β-1,3
-Exhibits excellent synergistic effects when used in combination with glucanase, dextranase, or mutanase.

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

[0017]

EXAMPLES Next, the present invention will be explained in more detail based on examples.

[Example 1] Toothpaste A toothpaste was manufactured using the following ingredients in a conventional manner.

0019
━━━━━━━
Minutes Weight% ━━━━━━━━━━━━━━━━━
━━━━━━━━━ Dicalcium phosphate 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
remainder
──────────────────────────
─ Total
100
━━━━━━━━━━━━━━━━━━━━━━━━
━━

[Example 2] Mouthwash A mouthwash was manufactured using the following ingredients in a conventional manner.

━━━━━━━━━━━━━━━━━━━
━━━━━━━
Minutes Weight% ━━━━━━━━━━━━━━━━━
━━━━━━━━━ Saccharin

0.1 ethanol
8.0
glycerin
20.0
Polyoxyethylene hydrogenated castor oil 1.0
fragrance
0.5
Macerase
2.0
water
Rest ────────
────────────────────
Total
100 ━━━━━━
━━━━━━━━━━━━━━━━━━━━

[Example 3] Troche A troche was manufactured using the following ingredients in a conventional manner.

0023] ━━━━━━━━━━━━━━━━━━━
━━━━━━━
Minutes Weight% ━━━━━━━━━━━━━━━━━
━━━━━━━━━ Glucose
75
．． 0 gum arabic
7.5
fragrance
1.0
Macerase
1.5 Dextranase 0
．． 5 Water
remainder
────────────────────
────── Total
100
━━━━━━━━━━━━━━━━━━━━
━━━━━━

[Example 4] Denture cleaning agent: Tablet A denture cleaning agent in the form of a tablet was prepared by a conventional method using the following ingredients.

0025 ━━━━━━━━━━━━━━━━━━━
━━━━━━━
Minutes Weight% ━━━━━━━━━━━━━━━━━
━━━━━━━━━ Sodium hydrogen carbonate 35.0
sodium lauryl sulfate
1.0 citric acid
3.0 Lactose
30
．． 0 Magnesium stearate
0.5 fragrance
1.5 Macerozyme
2.0 ────────────────
──────────── Total

100 ━━━━━━━━━━━━━━
━━━━━━━━━━━━

[Example 5] Denture cleaning agent: Powder A powder denture cleaning agent was produced using the following ingredients in a conventional manner.

━━━━━━━━━━━━━━━━━━━
━━━━━━━
Minutes Weight% ━━━━━━━━━━━━━━━━━
━━━━━━━━━ Potassium dihydrogen phosphate 30.0
Sodium monohydrogen phosphate
20.0 Lactose

40.0 Fragrance
1
．． 0 Macerozyme
5.0
Mutanase
4.0 ──────
──────────────────────
Total
100 ━━━━
━━━━━━━━━━━━━━━━━━━━━━

[Example 6] Denture cleaning agent: Tablet A denture cleaning agent in the form of a tablet was manufactured by a conventional method using the following ingredients.

━━━━━━━━━━━━━━━━━━━
━━━━━━━
Minutes Weight% ━━━━━━━━━━━━━━━━━
━━━━━━━━━ Sodium hydrogen carbonate 25.0
Sodium tripolyphosphate
5.0 Sodium lauryl sulfate 1.0
citric acid
29.0
lactose
30.0 Fragrance
Trace amount Macerozyme 4
．． 0 β-1,3-glucanase
6.0 ────
──────────────────────
Total
100 ━━━━
━━━━━━━━━━━━━━━━━━━━━━

[Example 7] Toothpaste A toothpaste was manufactured using the following ingredients in a conventional manner.

━━━━━━━━━━━━━━━━━━━
━━━━━━━
Minutes Weight% ━━━━━━━━━━━━━━━━━
━━━━━━━━━ Dicalcium phosphate 50.0
glycerin
20.0
sodium lauryl sulfate
2.0 Carboxymethylcellulose 1.0 Saccharin
0.1 Fragrance

0.9 Macerozyme
2.0
protease
6.0
water
Rest ──────
────────────────────
Total
100 ━━━━━━
━━━━━━━━━━━━━━━━━━━━

[0032]

Effects of the Invention The oral composition of the present invention has an excellent effect on the removal of Streptococcus and Candida bacteria, which are plaque-constituting bacteria, due to its active ingredient maceration enzyme, and is suitable for use in denture cleaning and denture plaque removal. and remove dental plaque to maintain oral hygiene and prevent oral diseases.

Claims (2)

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