JPS62273910A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:The titled composition having low side effects, containing vitamin C or a stabilized derivative thereof, vitamin E or a derivative thereof, lysozyme chloride and other proteolytic enzyme and lecithin or hydrogenated lecithin in specific concentration ranges. CONSTITUTION:A composition for oral cavity containing 0.1-10wt% one or more of vitamin C and a stabilized derivative (e.g. ascorbic acid monostearate, etc.), 0.1-10wt% one or more of vitamin E and a derivative (e.g. acetic acid dl-alpha-tocopherol, etc.) thereof, 0.1-5wt% one or more of lysozyme chloride and other proteolytic enzyme (e.g. anti-inflammatory enzyme agent, etc.) and 0.2-20wt% lecithin and hydrogenated lecithin. A composition wherein the vitamin C or the vitamin C and the vitamin E are included in matrix of the lecithin and the lysozyme chloride is added to the matrix is preferable as the composition.

Description

Detailed Description of the Invention 3. Detailed Description of the Invention [Field of Industrial Application] The present invention relates to an oral composition, and more particularly, it relates to an oral composition containing vitamin C or its stabilized derivative and vitamin E or its stabilized derivative. An oral composition containing a derivative, lysozyme chloride or other proteolytic enzyme, and lecithin or hydrogenated lecithin in a specific concentration range, for preventing, treating periodontitis,
The present invention relates to an oral composition that has an excellent effect on removing bad breath and has few side effects.

[Conventional technology]

First, periodontitis, which is the target of the composition of the present invention, will be described. Periodontitis is inflammation that occurs in the tissues surrounding teeth. This periodontitis begins to appear in childhood around the age of 3, and
It is 95% for school children around the age of 95, and 95-1 for adults.
Increase to 00%.

The cause is chronic inflammation that occurs and persists as a reaction directly under the mucous membrane around the teeth to the accumulation of plaque and tartar, small trauma caused by brushing or toothpicks, and persistent stimulation of harmful substances produced by oral bacteria. The first change is dilation of capillaries with increased permeability of the capillaries and an increase in blood flow. As a result, edema occurs in the intercellular space between the gingival sulcus epithelium and the attached epithelium, and the intercellular space expands.Next, blood congestion occurs in the capillaries, and white blood cells, lymphocytes, tissue cells (which have phagocytosis and immune communication functions) are produced. ), proliferation of immune-producing cells such as mast cells and plasma cells is observed. In addition, collagen fibers collapse and degenerate. On the other hand, repairs such as benthic formation of collagen fibers and neovascularization due to the appearance of fibroblasts are occurring in the same lesion. To summarize the mechanism of onset, it begins with inflammation caused by plaque, tartar, small trauma caused by brushing, etc., and substances produced by oral bacteria, which then leads to a decrease in the tissue's resistance to external stimuli, which in turn becomes a vicious cycle that worsens the inflammation. Perpetuates inflammation. As a result of this persistent inflammation, periodontitis is a situation in which negative reactions such as tissue destruction and degeneration and positive reactions such as repair phenomena occur simultaneously using the gingiva as a reaction site.

Conventional oral preparations for periodontitis include impregnators, antibiotic preparations, adrenal hormone preparations, other oral tablets, and dentifrices, as well as specialized therapeutic agents in the field of dental treatment.

Conventionally used for the prevention and treatment of periodontitis include povidone-iodine, domiphene bromide, sodium guaiazulene sulfonate, dequalinium chloride, cetylpyridinium chloride, chlorohydrochloride,
Examples include rhexidine. Sodium guaiazulene sulfonate has anti-inflammatory and weak anti-allergic effects, and others are for sterilization purposes.

In addition, the medicinal ingredients of dentifrice include fluorine compounds as a facial preventive agent, glycyrrhizin as an anti-inflammatory agent, hinokitiol as a bactericidal and anti-inflammatory agent, allantoin to promote wound healing, and another mechanism of action to reduce bleeding associated with inflammation. Epsilon aminocaproic acid, which has a hemostatic effect to prevent
Tranexamic acid is also included. In addition, recently it has become known that vitamin E is added to promote peripheral blood flow and inhibit inflammation, and lysozyme is added to enhance anti-inflammatory effects, bacteriolysis, hemostasis, and phagocytosis of white blood cells. There is. On the other hand, sodium copper chlorophyllin is added for deodorizing purposes, and sodium chloride as an astringent is also being reconsidered. However, even when these are actually combined, the effects are insufficient in various aspects such as anti-inflammatory action and improvement of subjective symptoms such as continuous removal of bad breath. The reason for this is thought to be that, considering the changes in the tissue stages of periodontitis mentioned above, the effects of each compounded drug act only on one aspect of the U-texture change.

[Problem that the invention seeks to solve]

The first way to prevent periodontitis is by brushing the teeth, but in reality, the incidence of periodontitis reaches 95-100% in adults, and it is difficult to prevent or treat it using conventional techniques. It shows that. In fact, many people suffer from stubborn bad breath and uncomfortable gums for a long time. Therefore, it is expected that a highly effective preventive and therapeutic agent will be developed that can eliminate unpleasant subjective symptoms such as bad breath in a short period of time, provide a comfortable condition, have no side effects, and enable long-term treatment.

[Means for solving problems]

In order to resolve the insufficient effects of such conventional oral compositions, the present inventors have elucidated periodontitis based on microscopic histological findings, and developed an effective and highly safe composition that can be repeatedly applied over a long period of time. As a result of repeated studies on preventive and therapeutic agents for periodontitis, we found that they contain vitamin C or its stabilized derivatives, vitamin E or its derivatives, and lecithin or hydrogenated lecithin in specific concentration ranges, and that they contain vitamin C or its stabilized derivatives, vitamin E or its derivatives, and lecithin or hydrogenated lecithin. A composition containing lysozyme chloride or other proteolytic enzymes added at an appropriate concentration provides prevention and treatment for periodontitis that is unimaginably more effective and safer than conventional products. We have discovered the fact that it has an effect and have completed the present invention.

That is, the present invention provides one of vitamin C or its stabilized derivatives.
0.1 to 10% by weight of one or more kinds of vitamin E or two or more kinds, and 0.1 to 10% by weight of one or more kinds of vitamin E or its derivatives;
One or two of lysozyme chloride or other proteolytic enzymes
The present invention relates to an oral composition characterized in that it contains 0.1 to 5% by weight of lecithin or more, and 0.2 to 20% by weight of lecithin or hydrogenated lecithin.

The stabilized derivatives of vitamin C used in the oral composition of the present invention include vitamin C fatty acid esters such as ascorbic acid monostearate, ascorbic acid isopalmitate, and ascorbic acid dipalmitate, ascorbic acid sulfate ester salts, and ascorbic acid phosphate. Examples include vitamin C inorganic acid ester salts such as ester salts.

In order to produce the oral composition of the present invention, ascorbic acid is used for the troche, but for other dosage forms, it is preferable to use a stabilized derivative thereof rather than ascorbic acid because it is more stable after formulation.

Further, vitamin E or its derivatives used in the present invention include natural vitamin E1 di-α-tocopherol acetate, nicotine 1ldl-α-tocopherol, amber fidl
-α-Tocopherol natka.

In carrying out the present invention, when vitamin C or a stabilized derivative thereof, or vitamin C or a stabilized derivative thereof and vitamin E or a derivative thereof are incorporated in a matrix of lecithin or hydrogenated lecithin, absorption is achieved. is good, and excellent effects can be obtained.

Proteolytic enzymes used in the present invention include lysozyme chloride and other anti-inflammatory enzymes.

The oral composition of the present invention contains vitamin C or a stabilized derivative thereof, vitamin E or a derivative thereof, lysozyme chloride and/or other anti-inflammatory enzymes, and lecithin or hydrogenated lecithin as essential components. The form of the base is not particularly limited, and various forms of the oral composition such as dentifrice, gingival massage agent, troche, and chewing gum are possible.

[For production]

Although the exact mechanism of action of the oral composition of the present invention is not known, vitamins C and E are essential factors for repairing DNA damaged by generator enzymes produced during inflammation. It is thought to form the basis of the defense function for living organisms. Other benefits of vitamin C include promoting collagen production, promoting detoxification, and improving immune function. Vitamin E has anti-inflammatory effects, especially the effect of blocking leukotrienes that advance inflammation, and is important for the stability of biological membranes.
Suppresses cell destruction, which is the basis of tissue damage caused by inflammation.

The present invention mainly applies, in addition to the action of vitamin C1E, the action of lysozyme chloride and/or other anti-inflammatory enzymes to enhance the biological defense response to the prevention and treatment of periodontitis. It seems that the addition of lecithin promotes absorption, resulting in effects that cannot be obtained with conventional products.

Up to now, there have been 3 applications of vitamin C in oral materials.
A dentifrice in which -0-glucosyl-ascorbic acid and sodium ascorbate are used and lysozyme chloride is blended with vitamin E and/or its derivatives is already in use.

However, vitamin C and/or its stabilized derivatives, vitamin E and/or its derivatives, lysozyme chloride and/or
There is no example in which a drug or other anti-inflammatory enzyme agent is contained in the same preparation, lecithin or hydrogenated lecithin is combined, and the combination is made to act simultaneously to prevent or treat periodontitis.

〔Example〕

EXAMPLES Hereinafter, the present invention will be explained in more detail with reference to Examples, but the present invention is not limited to these Examples.

Note that the percentages in the examples are based on weight.

Example 1 A gingival pine surge agent having the composition shown below was obtained.

Vitamin E 3.5% hydrogenated lecithin 2.1% ascorbic acid dipalmitate 0.9% triglyceride
7.0% methylparaben
o, oi% citrate buffer (pH 4,0)
10% polyglycerin fatty acid ester 3%
Lysozyme chloride (potency) 0.5% water 71.
94% Example 2 A dentifrice having the composition shown below was obtained.

Vitamin E 3.5% hydrogenated lecithin 2.1% ascorbic acid dipalmitate 0.9% triglyceride
7.0% methylparaben
0.01% citrate buffer (pH 4,0)
10% polyglycerin fatty acid ester 3
%・-Lysozyme chloride (potency) 0.5% Calcium carbonate 39% Water
32.94% Example 3 A lozenge having the following composition was obtained.

Vitamin E 100 mg/1 tablet Ascorbic acid 100 mg/1 tablet Lysozyme chloride 30 mg/1 tablet (potency) Hydrogenated lecithin 100 mg/1 tablet Example 4 A chewing gum having the following composition was obtained.

Vitamin 2 100 mg/1 piece Ascorbic acid 100 mg/1 piece Lysozyme chloride
30 mg/1 piece (potency) hydrogenated lecithin
50 mg/1 piece [Effect of the invention] A clinical test was conducted on the oral compositions obtained in Examples 1 and 2.

That is, either the gingival tract surge agent obtained in Example 1 (hereinafter referred to as Agent A) or the dentifrice obtained in Example 2 (hereinafter referred to as Agent B) was administered to 30 target patients after sufficient tartar removal.
After a week, a 1.8 cm long piece was placed on a toothbrush twice a day, morning and evening, and the patient was allowed to brush for 3 minutes using his usual method. The period of use was 4 weeks, and patients were asked to visit the hospital every week to observe their subjective and objective symptoms. The observation site was limited to the anterior labial gingiva of the upper and lower jaws. Observation items include the following eight objective symptoms: redness, swelling, bleeding, drainage, bad breath, plaque deposits, periodontal pockets, and tooth movement.
Medical examinations and records were recorded for 1, 2, 3, and 4 weeks after administration (before administration), and 1, 2, and 3.4 weeks after administration.

Regarding subjective symptoms, the patient's impressions were interviewed and recorded at the end of treatment (4 weeks later) regarding two points: 1) overall subjective symptoms, and 2) range of use. Furthermore, the clinical results were comprehensively evaluated by adding the observation results of intraoral color photographs before and after use to the above-mentioned objective symptoms.

As a result, among the 8 symptoms, after 4 weeks, for swelling, 90.0% of agent A and 72.7% of agent B, 81.4% on average, and for redness, 81.8% of agent A and 72.7% of agent B. %, average 77.
3%, and for bleeding, agent A was 63.6% and agent B was 59. .

%, average 61.3%, A for inhibition of plaque deposition
The improvement rate was 59.0% for agent B and 77.0% for agent B, with an average improvement rate of 68.0%. That is, a remarkable trend of improvement was observed in the four symptoms of redness, swelling, bleeding, and plaque deposition. Furthermore, these symptoms tended to improve as the days of administration progressed. However, no significant changes were observed in other symptoms. A questionnaire was used to examine patients' impressions 4 weeks after using the main drug (A and B drugs). The result A
The improvement rate in subjective symptoms for both Agent B was 72-77%. During the period of regular use, not a single case of side effects, both subjective and objective, was observed.

The above results revealed that the oral composition of the present invention exhibits excellent effects.

Claims (1)

[Scope of Claims] 1. 0.1 to 10% by weight of one or more types of vitamin C or its stabilized derivatives, and 0.1 to 10% by weight of one or more types of vitamin E or its derivatives. and one or more of lysozyme chloride or other proteolytic enzymes 0.1
~5% by weight and lecithin or hydrogenated lecithin 0.2~
20% by weight of an oral cavity composition. 2. Vitamin C or a stabilized derivative thereof, or vitamin C or a stabilized derivative thereof and vitamin E or a derivative thereof, are included in a matrix of lecithin or hydrogenated lecithin, and lysozyme chloride or other proteolytic 2. The oral composition according to claim 1, which contains one or more enzymes.