JPS61200905A - Composition for oral cavity application - Google Patents

Abstract

PURPOSE:To provide an oral composition consisting of a combination of a chlorhexidine salt with phytic acid or its compound, effective to remarkably promote the adsorption of the chlorhexidine salt to the tooth and prevent the formation of plaque and accordingly prevent dental caries. CONSTITUTION:The objective oral composition for the chemical plaque control is obtained by combining (A) a chlorhexidine salt known as a disinfectant with (B) phytic acid or its compound (e.g. sodium phytate, ester of phytic acid and an alcohol, etc.). The amount of the component A in the composition is preferably >=0.01%, and the ratio of B/A is >=1. It can be used in the form of tooth powder, toothpaste, gargle, troche, aerosol, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to oral compositions. More specifically, the present invention relates to an oral cavity composition in which adsorption of chlorhexidine salts, which are bactericidal agents, to tooth surfaces is promoted. For example, it relates to additives for compositions contained in the oral cavity, such as dentifrices, mouthwashes, and troches.

[Conventional technology]

Plaque is formed when oral bacteria such as Streptococcus nitans adsorbs to the tooth surface and proliferates, and it is well known that it causes tooth decay, but it also causes gingivitis and It has become clear that it is also a cause of alveolar leakage.Therefore, removal of plaque and prevention of plaque adhesion (plaque control) are important for oral hygiene.The most commonly used methods for plaque control are:
Brushing is the mechanical removal of plaque with a toothbrush. However, advanced brushing techniques are required to completely remove the teeth by brushing. Most people don't brush their teeth enough, so plaque is not removed enough, and the incidence of tooth decay, gingivitis, and pyorrhea has not decreased despite brushing. Probably.

Therefore, chemical plaque control methods are being researched to supplement or replace brushing. Among these, chlorhexidine salts are compounds that have been clinically recognized as effective and safe.

Chlorhexidine is a compound having the following structure (3HOHOHOH) and is water-insoluble. Therefore, in order to make it water-soluble, it is generally used as a salt such as hydrochloride or glucone monosalt. Chlorhexidine salts have a bactericidal effect and are relatively easily adsorbed to the oral mucosa and tooth surfaces.

It is known that it is sustainedly released into the oral cavity over a long period of time. It is believed that this tightening prevents the inside of the oral cavity 1 from adhering to the tooth surface and, in turn, prevents the formation of dental plaque. At present, there does not seem to be any research on promoting the adhesion of chlorine salts to the tooth surface.

[Problem that the invention seeks to solve]

The oral composition of the present invention promotes the adsorption of chlorhexidine salts onto the tooth surface, and as a result, it can be expected to be more effective than conventional oral compositions in preventing plaque formation and, ultimately, tooth decay. It is something.

[Means for solving problems]

The present inventors conducted intensive research with the aim of further increasing the effect of chlorhexidine salts remaining in the oral cavity, particularly promoting adsorption to the tooth surface and preventing plaque formation. The present inventors have discovered that adsorption of chlorhexidine salts to teeth is significantly promoted by combining acids or their compounds, and have completed the present invention.

That is, the present invention is an oral composition that contains chlorhexidine salts and phytic acid or a compound thereof as additives.

As mentioned above, when phytic acid or its compound is combined with chlorhexidine salts, adsorption of chlorhexidine hydrochloride to teeth is promoted, but this mechanism is not yet well understood.

Phytic acid has the following structural formula: OH O P-OH OH and is a natural product widely found in grain seeds. Industrially, it is a highly safe compound extracted from rice bran and used as a food improver.

Phytic acid exhibits strong acidity, so when used as a component of an oral composition, it is better to use one that has been neutralized with a base or one that has been esterified. A phytic acid compound means such a neutralized product or an esterified product. Examples of these compounds include sodium phytate, potassium phytate, lithium phytate, magnecum phytate, calcium phytate, ammonium phytate, ethanolamine neutralized products of phytic acid, and esters of phytic acid and alcohol. be able to.

Chlorhexidine salts are ICD, 001wz in the composition.
If the content is 0.01% or more, it has a bactericidal effect, but in order to expect a sufficiently satisfactory bactericidal effect, the content should be 0.01% or more. There is no particular upper limit to the content of chlorhexidine salts from the perspective of bactericidal effect alone, but it is important to note that chlorhexidine salts have a bitter taste and that too much of these salts are present in leftovers (containing them may stain teeth). Considering that,
It is preferable that the composition contains 1% or less. The content of phytic acid or its compound, which is an adhesion promoter of chlorhexidine salts to the tooth surface, should be at least the same as the content of chlorhexidine, or be in excess. If the content of phytic acid or its compound is too small compared to that of chlorhexidine, the effect of phytic acid on promoting the adhesion of chlorhexidine to teeth will be reduced.

When carrying out the present invention, in addition to being used as powder toothpaste, toothpaste, rinse agent, troche, etc., it can also be sprayed into the oral cavity as an aerosol. It can also be used as a tooth coating agent, or by impregnating dental floss or toothpicks.

In addition, in these implementations, raw materials commonly used for the respective preparations can be used, except for the lorhexidine salts and the phytic acid compound, which are safe for the present invention.

〔Example〕

The present invention will be described below with reference to Examples, but the present invention is not limited to these Examples.

Experiment of adhesion of monochlorhexidine compound to the tooth surface The tooth surface is called enamel, and its composition is inorganic.
li 97'34s, 1% organic matter, 2% moisture,
The main component of S-free negative is L-droxiapatite (0ato(P
It is a calcium phosphate called O4)4(OH)2). Therefore, in this experiment, we used hydroxyapatite powder (Blo-Ge1HTP) as a model of tooth enamel.
, Bio-Rad Laboratories) was immersed in human saliva at 37°C for 10 minutes and then washed with water. The reason for immersing it in saliva is to make the surface of hydroxyapatite adsorb salivary mucoproteins, etc., so that the condition is the same as that of actual tooth enamel wet with saliva.

0.3 lI of this saliva-treated hydroxyapatite powder
Weigh accurately into a centrifuge tube, add accurately a water bath solution of chlorhexidine hydrochloride (Hibiten hydrochloride, Sumitomo Chemical Co., Ltd.) with a concentration of 100 ppm, mix and stir, and then add 12 N& 9. Leave it in a water bath at 57°C containing 0.01% (w/v) for 1 hour.
The heart was separated at 0.00 rpm for 10 minutes, and the concentration of chlorhexidine hydrochloride in the supernatant was determined by high performance liquid chromatography. High performance liquid chromatography was carried out using LLGHRO30RB RP-8 (15mX 4
．． 6 Wφ] with a separation column l, 0,005M n
- Sodium pentanesulfonate solution (methanol, A/
: Water=7:3*PH=5.53 was used as eluent. The flow rate is 1. (114), chlorhexidine hydrochloride was detected by absorbance measurement at 260 nm, and quantified using a calibration curve prepared using a standard chlorhexidine hydrochloride.

In addition, using the same procedure, saliva-treated apatite powder was
0, 0.0!5, 0.1, 04% (w
/v) in a water bath containing 12Na4 phytate, and the amount of chlorhexidine hydrochloride was determined. The results are shown in the first factor.

The chlorhexidine hydrochloride adsorption rate was calculated using the following formula.

Co-0 A (%) = -XIQO O.

A: Chlorhexidine adsorption rate Co: Chlorhexidine hydrochloride concentration (100 ppia
) C: Concentration of chlorhexidine hydrochloride in the supernatant after adsorption and centrifugation As shown in No. 10, surprisingly, when the sodium phytate concentration exceeds 0.03% (w/v), chlorhexidine hydrochloride It can be seen that the salt is almost completely adsorbed to the hydroxyapatite powder.

[Example 1 of toothpaste] The following components were degassed, kneaded and stirred to produce a toothpaste.

Aluminum hydroxide 40.0 U1% silicon anhydride m2.0 Sodium carboxymethyl cellulose 1.2 Glycerin 10.0 N Rubit solution (70
%) 14.0 Saccharin Sodium
0.2 Glucon Factory Chlorhexidine AFI (20
%) O,OS phytin yabu 12 sodium salt
0.1 Sodium lauryl sulfate 1.
5 Weight% Methylparaben 0.0
5 Flavor 0.8 Total 100% by weight [Example 2 of toothpaste] The following components were deaerated and kneaded and stirred to produce a toothpaste.

Anhydrous (ai' 50.0 weight II% carboxymethyl cellulose sodium 0.
5 Glycerin 10.0 Norbit solution (70%) SO,O Sodium saccharin 0.3 chloride Musidine hydrochloride 0.0
2 Fuichin i! ! ! 12 Arginine salt 0.1 Sodium lauryl sulfate 1.5 Methylparaben 0.05 Fragrance 0.
8 Sodium monofluorophosphate 0.7 Purified water
Appropriate amount needle 100% by weight [Example of a rinsing agent] The following components were deaerated and kneaded to produce a liquid rinsing agent.

Ethanol 3.0 11% scent
Materials 0.05 Glycerin 10.0 Sodium benzoate 0.5 Polyoxyethylene polypropylene glycol 1.0
Satucalin sodium 0.01 Food coloring Trace amount of gluconate Chlorhexidine #fi (zo%) 0
．． 1 Phytin #112 Potassium solution 0.1 Purified water Appropriate amount

[Brief explanation of drawings]

Figure 1 shows the effect of phytate in an example of the present invention. It is a graph showing S and experimental results for the results.

Claims (1)

[Scope of Claims] 1. An oral composition comprising chlorhexidine salts and phytic acid or a compound thereof. 2. Chlorhexidine salt content is 0.01% to 1%
The oral composition according to claim 1. 3. Claim 1 in which the content of phytic acid or its compound is at least the same amount as the content of chlorhexidine salts
Oral composition according to item 1 or 2.