JPH04300816A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain a composition for the oral cavity, capable of synergistically enhancing preventive action on hemorrhage, inhibitory action on edema, etc., in chronic inflammation, excellent in preventive and treating effects on diseases such as gingivitis and periodontitis in the oral cavity and good in safety and usability. CONSTITUTION:A composition for the oral cavity is obtained by blending (A) epsilon-aminocaproic acid expressed by formula I with (B) one or more compounds selected from lysine expressed by formula II (R1 is H, Phe-Ala or Ala-Phe; Phe is phenylalanine; Ala is alanine; R2 is OH or CH2Cl; R3 is H or formula III) or arginine expressed by formula IV (R1 is H, D-Phe-Pro, Glu-Gly, Ile- Glu-Gly, Pro-Phe or Ala-Phe; Pro is proline; Glu is glutamic acid; Gly is glycine; lie is isoleucine) or derivatives thereof as essential ingredients at (30:1)-(1:30) weight ratio of the ingredients (A) : (B). The total amount of the blended ingredients (A) and (B) based on the total amount of the composition for the oral cavity is 0.001-10wt.%, especially 0.01-5wt.%. The aforementioned composition has the above-mentioned effects.

Description

[Detailed description of the invention]

0001

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to oral compositions, particularly oral compositions used for the prevention and treatment of periodontal diseases.

0002

[Prior Art] Generally, periodontal diseases such as gingivitis and periodontitis are said to be chronic inflammation caused by chronic stimulation of periodontal pathogens or metabolites produced by them. Yes, it's not clear yet. For these periodontal diseases, oral compositions containing anti-inflammatory agents such as allantoin and glycyrrhizic acid, anti-plasmin agents such as ε-aminocaproic acid and tranexamic acid, hinokitiol, and sodium chloride have been used.

0003

[Problems to be Solved by the Invention] Problems with the Prior Art However, (1) None of these had sufficient effects. ■Due to its relationship with other ingredients, it could not be effective. ■There was a problem with its stability. (2) There were problems such as poor usability of the blended system, and it was not always satisfactory.

OBJECTS OF THE INVENTION The present invention was made in view of the problems of the prior art, and its purpose is to provide an oral composition that is excellent in preventive and therapeutic effects on periodontal diseases, and is also safe and easy to use. Our goal is to provide the following.

[0005] In order to achieve the above object, the present inventors have conducted extensive research to obtain substances that have excellent effects on periodontal diseases, and have found that ε-aminocaproic acid, lysine, lysine derivatives, and arginine By blending one or more selected from arginine derivatives, bleeding prevention during chronic inflammation, edema suppression, etc. are synergistically enhanced, resulting in extremely high effectiveness.

[0006] Although it is known that ε-aminocaproic acid, lysine, arginine and their derivatives exhibit protease inhibitory effects, there have been no reports on the effects of a combination of these on periodontal diseases, and their application to oral compositions has not been reported. is also unknown.

The present inventors have completed the present invention based on the above findings.

[0008]

[Means for Solving the Problems] That is, the present invention provides ε-
This is an oral composition characterized in that it contains aminocaproic acid and one or more selected from lysine, lysine derivatives, arginine, and arginine derivatives.

The configuration of the present invention will be explained in detail below.

The ε-aminocaproic acid, lysine, lysine derivatives, arginine, and arginine derivatives used in the present invention are each represented by the following general formulas. i.e.

001
1] ε-aminocaproic acid

[Chemical I]

[0012] Lysine and its derivatives

[Chemical II]

[0013] Arginine and its derivatives

[Chemical III]

In the present invention, ε-aminocaproic acid and lysine, lysine derivatives, arginine, and arginine derivatives are preferably blended in a weight ratio of 30:1 to 1:30. When the amount is significantly outside this range, the effects of the present invention cannot be sufficiently obtained. Further, the total amount of ε-aminocaproic acid, lysine, lysine derivative, arginine, and arginine derivative is preferably 0.001 to 10% by weight based on the total amount of the oral composition, and more preferably 0.01 to 5% by weight. If it is less than 0.001% by weight, the effects of the present invention cannot be sufficiently obtained, and if it exceeds 10% by weight, it is unreasonable in terms of formulation or cost.

[0015] In addition to the above-mentioned essential ingredients, the oral composition of the present invention may optionally contain abrasives such as dibasic calcium phosphate and silica, and humectants such as glycerin, sorbitol, and propylene glycol, depending on the form of the composition. , thickeners such as carboxymethylcellulose, methylcellulose, hydroxyethylcellulose, carrageenan, sodium polyacrylate, surfactants such as sodium lauryl sulfate, sucrose fatty acid ester, lauroyl sarcosinate,
Higher alcohols, oils such as wax, lower alcohols,
Ingredients normally used in oral compositions, such as fragrances, pigments, preservatives, antioxidants, and water, can be blended. Furthermore, the oral composition of the present invention may be in any form, and may be used in toothpastes, toothpastes, moist toothpastes, powdered toothpastes, water toothpastes, etc., oral pasta, mouthwashes, mouth fresheners, chewing gum, etc. can.

[0016]

Effects of the Invention The oral composition of the present invention contains ε-aminocaproic acid, lysine, lysine derivatives, arginine, and arginine derivatives, so it has a synergistic effect on preventing bleeding during chronic inflammation, suppressing edema, etc. Therefore, it has excellent preventive and therapeutic effects on oral diseases. Furthermore, oral diseases can be effectively prevented and treated while maintaining good safety and usability.

[0017]

EXAMPLES Next, the present invention will be explained in more detail with reference to Examples. Note that the present invention is not limited to this. Prior to Examples, the test methods and evaluation methods used in the present invention will be explained.

[0018] Practical use test (Subject) A 30-year-old patient complaining of swollen and bleeding gums.
~100 boys and 100 girls aged 54

0019
Test method> Brushing for 3 minutes 3 times a day for 14 days using the toothpastes of Examples 1 to 4 and Comparative Examples 1 to 3 with the compositions shown in Table 1.
I went there today. During this period, the use of other oral compositions was prohibited, and no particular instructions on brushing were given.

[0020]

[Table 1]

<Evaluation> The effects on gum swelling and bleeding were evaluated on the following four levels. Significant effect: Significant improvement in gum swelling and bleeding Effectiveness:
Slightly effective at improving gum swelling and bleeding: Ineffective at improving gum swelling and bleeding:
No change before and after use

The above-mentioned lysine and its derivatives, arginine and its derivatives are shown in Table 2.

[0023]

[Table 2]

The results are shown in Table 3.

[0025]

[Table 3]

[0026] As is clear from Table 3, the oral composition of the present invention exhibited superior synergistic effects in preventing and treating gum swelling and bleeding, compared to the composition containing each component alone. .

Example 5 Toothpaste
Weight% (1) Silicic anhydride

20.0(2) Sorbit

50.0 (3) Carrageenan
0.5(
4) ε-Aminocaproic acid
3.0(
5) Lysine derivative *1
0.
1(6) Carboxymethyl

1.0 Sodium cellulose (7) Sodium lauryl sulfate
1.8(
8) Saccharin sodium
0.08
(9) Methyl paraoxybenzoate
0.2(1
0) Fragrance

0.9 (11) Purified water

remainder

[Production method] According to the conventional method *1 In chemical formula II, R1=H, R2=CH2Cl,
R3=H. As a result of actual use tests of the toothpaste of the present invention, it showed an excellent improvement effect on periodontal diseases.

Example 6 Pasta for oral cavity

Weight% (1) Vaseline

10.0(2) Propylene glycol
7.0(3) Stearyl alcohol
10.0(4)ε-aminocaproic acid
0.1(5) Lysine derivative *2

1.5(6) Arginine derivative *1
1.5(7) Polyethylene glycol 1500
30.0(8) Hinokitiol

0.1(9) Polyethylene glycol 400
remainder

[Manufacturing method] Lysine derivative according to conventional method *2 In Chemical II, R1=P
he-Ala, R2=OH, R3=H. Arginine derivative *1 R in chemical formula III
1=Phe-Ala, R2=OH, R3=H. As a result of a practical use test of the oral pasta of the present invention, it showed an excellent improvement effect on periodontal diseases.

Example 7 Mouthwash

Weight% (1) Ethyl alcohol

10.0(2) Saccharin sodium

0.05 (3) Fragrance

0.8(4) Polyoxyethylene (20 moles)
1.0 Sorbitan laurate (5) ε-aminocaproic acid

0.001(6) Arginine derivative *1

0.01 (7) Purified water

As a result of actual use tests of the mouthwash of the present invention, it showed an excellent improvement effect on periodontal diseases.

[Production method] According to the conventional method *1 In chemical formula III, R1=Phe-Ala,
Those with R2=OH and R3=H.

Example 8 Mouth freshener (spray type) Weight % (
1) Ethyl alcohol
40.0
(2) Saccharin sodium
0.1
(3) Sorbit

10.0(4) Fragrance

1.0 (5) Polyoxyethylene (
20 moles)
0.7 Hydrogenated castor oil (6) Chlorhexidine hydrochloride
0.0
5(7)ε-Aminocaproic acid
0.
5(8) Arginine derivative *2
0.
2(9) Purified water

remainder

[Manufacturing method] According to the conventional method *2 In chemical III, R1=H, R2=CH2
Cl, those with R3=H. As a result of actual use tests of the mouth freshener of the present invention, it showed an excellent improvement effect on periodontal diseases.

Example 9 Chewing gum

Weight% (1) Gum base

25.0(2) Calcium carbonate

2.0(3) Fragrance

1.0(4) Copper chlorophyll
0.05(5)ε-aminocaproic acid
0.01(6) Lysine

0.01 (7)
sorbit powder
remainder

[
Manufacturing method: The chewing gum of the present invention was tested using a conventional method, and as a result, it showed an excellent improvement effect on periodontal diseases.

Example 10
toothpaste
Weight% (1) Silicic anhydride

20.0(2) Sorbit
50.0(3
) carrageenan

0.5(4)ε-aminocaproic acid

1.0(5) Lysine derivative *1

0.2(6) Arginine derivative *1

0.2(7) Carboxymethyl

1.0 Sodium cellulose (8) Sodium lauryl sulfate
1.
8(9) Saccharin sodium

0.08(10) Methyl paraoxybenzoate

0.2 (11) Fragrance

0.9 (12) Purified water

remainder

[Manufacturing method]
Lysine derivative according to conventional method *1 In chemical formula II, R1=H, R
2=CH2Cl, R3=H. Arginine derivative *1 In formula III, R1=Phe-Ala, R2=OH, R3=H. As a result of actual use tests of the toothpaste of the present invention, it showed an excellent improvement effect on periodontal diseases.

Claims (1)

[Claims] 1. An oral composition comprising ε-aminocaproic acid and one or more selected from lysine, lysine derivatives, arginine, and arginine derivatives.