JPH089529B2 - Oral composition - Google Patents

Description

TECHNICAL FIELD The present invention relates to an oral composition for suppressing the establishment of Streptococcus mutans in the oral cavity, preventing the formation of plaque, and preventing dental caries.

Problems to be Solved by the Related Art and Invention Conventionally, among oral bacteria, Streptococcus
Mutants are attracting attention as a causative agent of caries. That is, Streptococcus mutans produces glucosyltransferase, which synthesizes adhesive polysaccharides such as dextran and mutan from sucrose, and this polysaccharide has a certain flora involving bacteria such as Streptococcus mutans. Form plaque. On the other hand, Streptococcus mutans is said to produce acid from various sugars, and this acid accumulates in dental plaque to demineralize enamel and cause caries, thus preventing caries. Therefore, it is desired to suppress the colonization of Streptococcus mutans in the oral cavity.

For this reason, various active ingredients have been proposed in the past for suppressing the colonization of Streptococcus mutans in the oral cavity.

The present invention was also made in response to such a problem, effectively prevents the establishment of Streptococcus mutans in the oral cavity, oral composition that can prevent dental caries by suppressing the formation of plaque. The purpose is to provide things.

Means and Actions for Solving Problems The present inventors have conducted diligent studies to achieve the above-mentioned object, and as a result, found that tacanal and pralmin suppress the colonization of Streptococcus mutans in the oral cavity. .

That is, takanal (6- [2-[(5-bromo-2-
Pyridyl) aminovinyl] -1-ethyl-2-picolinium salt, in which counter ions include iodine, chlorine, orotic acid, nicotinic acid, etc.) are known as Photosensitizer No. 301, and are listed as cosmetic raw material standards. Is being done,
It is known to be effective in preventing hair nourishment, hair growth, dandruff, itch, and hair loss. Furthermore, Takata has been reported to have an activating action on pulp, a pulp extraction, a wound healing action after tooth extraction, and a gingival granulation formation action, and a report showing a promoting action on tooth growth rate. There are also clinical trial reports applied to healing. On the other hand, pralmine (2- (p-dimethylaminostyryl) -3-peptyl-4-methylthiazolinium salt, which includes chlorine as a counter ion, chlorine, orotic acid, nicotinic acid, etc.) is a photosensitizer. It is known as NK143, which is also listed in JCID, a collection of cosmetic raw materials, and is reported to exhibit strong antibacterial and antifungal effects.

However, takanal and pralmin act on Streptococcus mutans, which are conventionally known as caries-causing bacteria in the oral cavity, and there is no reported case that they have the effect of suppressing the adherence of Streptococcus mutans. It was not known to prevent dental caries by blending in an oral composition such as toothpaste, but as shown in the experimental examples described below by the present inventors, tacanal and pralmin are streptococcus. It was found for the first time that oral compositions such as dentifrice containing these as active ingredients are effective in preventing dental caries by suppressing the establishment of mutans in the oral cavity and inhibiting the formation of plaque. The present invention has been completed.

 Hereinafter, the present invention will be described in more detail.

The oral composition according to the present invention is prepared and applied as a toothpaste, a powdered toothpaste, a liquid toothpaste, a mouthwash, a gargle tablet, a gum massage cream, an oral pasta, a troche, a chewing gum, etc., and forms plaque. Takanal and / or pralmin are blended as an active ingredient for suppressing the above.

Here, the compounding amount of tacanal and pralmin is 0.0001 to 0.5% (weight%, the same applies hereinafter) of the total composition, especially 0.001.
It is preferable to be set to ˜0.05%. If the blending amount is less than 0.0001%, the effect of inhibiting Streptococcus mutans from being fixed may not be sufficiently exhibited, and if it is more than 0.5%, it is not preferable in appearance due to coloring and the like.

The present invention thus contains tacanal or pralmin as an active ingredient for the prevention of dental caries, thereby suppressing the establishment of Streptococcus mutans in the oral cavity and preventing the formation of plaque. In addition to tacanal and pralmin, other oral active ingredients for preventing dental caries include, for example, a platonin (photosensitizer 10 having an effect of suppressing oral colonization in Streptococcus mutans).
No. 1) or rumin may be added. Enzymes such as dextranase, fluorides such as sodium monofluorophosphate, stannous salts, chlorhexidines and the like can also be blended, and various other active ingredients can be appropriately selected and blended.

The other components of the present invention are selected and used according to the type of oral composition, purpose of use and the like. For example, abrasives, binders, thickeners, surfactants, sweeteners, flavors, preservatives and the like are used in the preparation of toothpaste.

Effects of the Invention The oral composition of the present invention contains tacanal and / or pralmine, thereby effectively suppressing the establishment of Streptococcus mutans in the oral cavity and preventing the formation of plaque. It is very effective for caries prevention.

 Next, the effects of the present invention will be specifically shown by experimental examples.

[Example 1] Reaction attachment method A 0.05 M phosphate buffer (pH 6.8) containing 1% sucrose, 0.01% preservative (NaN ₃ ) and heat-sterilized Streptococcus mutans strain 6715 strains was used. A predetermined amount of the drug was added, and an extracellular enzyme containing glucosyltransferase of Streptococcus mutans 6715 strain prepared in advance was added thereto and reacted at 37 ° C. for 16 hours. After the reaction, wash twice with water, then add the same amount of water as the reaction system,
After ultrasonic treatment for about 20 seconds to evenly suspend the plaque, measure the absorbance (turbidity) at a wavelength of 550 nm using a photometer, determine the amount of adhered plaque, and determine the plaque formation inhibition rate. Was calculated.

 The plaque formation inhibition rate was calculated by the following formula.

A: control plaque amount B: plaque amount when drug is added [Experimental Example 2] Adhesion of culture method A predetermined amount of a drug was added to a BHI medium containing 1% sucrose, and Streptococcus mutans 6715 strain that had been precultured was inoculated into the BHI medium, and N ₂ : CO ₂ : The cells were cultured at 37 ° C. for 16 hours in an Anaero box whose gas was replaced with H ₂ = 80: 10: 10.
After culturing, wash twice with water, then add the same amount of water as the culture solution, sonicate for about 20 seconds to uniformly suspend dental plaque, and use a photometer at a wavelength of 550 nm. The absorbance (turbidity) was measured to determine the amount of adhered plaque. The results are shown in Table 2.

As is clear from the results shown in Tables 1 and 2, it is recognized that tacanal and pralmin have an excellent effect of suppressing adhesion to Streptococcus mutans by any of the reaction adhesion method and the culture adhesion method.

 Examples will be shown below.

[Example 1] Toothpaste Aluminum hydroxide 45.0% Gelling silica 2.0 Sorbit 25.0 Sodium carboxymethyl cellulose 1.0 Sucrose monopalmitate 1.0 Sodium lauryl sulfate 1.5 Sodium saccharin 0.2 Ethanol 0.1 Sodium benzoate 0.1 Platonin 0.001 Tacanal 0.05 Perfume 1.0 Water residue Total 100.0% [Example 2] Toothpaste Precipitable silica 25.0% Sorbit 25.0 Glycerin 25.0 Polyvinylpyrrolidone 1.0 Lauroyl polyglycerin ester 1.0 Polyoxyethylene (60) sorbitan monolaurate 0.5 Saccharin sodium 0.2 Ethyl paraoxybenzoate 0.1 Chlorhexidine hydrochloride 0.1 Lumin 0.002 Puralumin 0.01 Fragrance 1.0 Water 100.0% Total [Example 3] Toothpaste Dicalcium phosphate dihydrate 20.0% Dicalcium phosphate anhydrate 20.0 Gelling silica 2.0 Sorbit 20.0 Sodium carboxymethylcellulose 1.0 Lauryl diethanolamide 1.0 Sodium lauryl sulfate 1.5 Lauroyl sarcosinate 0.3 Sodium saccharin 0.1 Ethyl paraoxybenzoate 0.1 Tacanal 0.005 Puralumin 0.005 Magnesium phosphate 1.0 Sodium monofluorophosphate 0.76 Perfume 0.8 Water residue 100.0% in total [Example 4] Pasta cetanol for oral use 10.0% Squalane 20.0 Precipitable silica (abrasiveness) 5.0 Polyoxyethylene (40) hydrogenated castor oil 0.1 Sorbitamonooleic acid ester 1.0 Glycyrrhetinic acid 0.1 Sodium saccharin 0.6 Perfume 0.6 Lumin 0.1 Purarumin 0.05 water remaining total 100.0% example 5 oral pasta Liquid paraffin 15.0% Cetyl alcohol 10.0 glycerin 20.0 sorbitan monopalmitate 0.6 polyoxyethylene Down (40) sorbitan monostearate rate 5.
0 Chlorhexidine gluconate 0.1 Fragrance 0.5 Pratonin 0.1 Takanal 0.2 Water Residual 100.0% [Example 6] Mouthwash sorbit 10.0% Ethanol 5.0 Polyoxyethylene (60) hydrogenated castor oil 0.1 Sucrose monopalmitate 0.2 Saccharin sodium 0.2 Fragrance 0.6 Platonin 0.03 Takanal 0.05 Water Residual 100.0% [Example 7] Oral troche Lactose 99.0% Chlorhexidine gluconic acid 0.05 Polyoxyethylene (60) monosterate 0.2 Platonin 0.2 Tacanal 0.2 Stevia extract 0.2 Perfume 0.01 Hydroxyethylcellulose Residual 100.0 %

Claims (2)

[Claims] 1. An oral composition for inhibiting plaque formation, which comprises tacanal and / or pralmin as an active ingredient for inhibiting plaque formation. 2. The oral composition according to claim 1, wherein the compounding amount of tacanal and / or pralmin is 0.0001 to 0.5% by weight of the total composition.