JP3472172B2 - Oral agent - Google Patents

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a toothpaste and other oral preparations having a caries-preventing action and a deodorizing action. [0002] In the development of dental caries, microorganisms in the oral cavity, particularly enzymes, glucosyltransferases produced by Streptococcus mutans, are involved. That is, sucrose remaining in the oral cavity among foods and drinks is converted into glucan which is water-insoluble and strongly adherent by the action of glucosyltransferase, and adheres to the surface of the tooth together with the oral microorganisms to form plaque (tooth). To form dirt). And
Microorganisms in the plaque metabolize sugars in food to make acids,
It is caries that this acid demineralizes and erodes tooth enamel. [0003] Plaque also enables the growth of microorganisms that produce ammonia and the like, and is one of the causes of unpleasant halitosis. [0004] Therefore, in order to prevent dental caries and reduce bad breath, plaque adhering to the tooth surface is not only removed by brushing, but also the growth of Streptococcus mutans in the oral cavity and the action of glucosyltransferase are inhibited. By doing so, it is desirable to suppress the production of glucan and prevent the resulting glucan from adhering to teeth as plaque. [0005] From these viewpoints, in recent years, oral preparations that have been provided with an effect of preventing caries and preventing bad breath, such as a glucosyltransferase inhibitory action, have been provided.
Glucosyltransferase inhibitors conventionally known as suitable for such applications include mutastane, crude drug tannins, ellagic acid, green tea polyphenol,
Oolong tea extracts and the like, and tannins and oolong tea extracts also have a deodorizing effect. SUMMARY OF THE INVENTION An object of the present invention is to provide an oral agent having an action of suppressing the formation of plaque causing caries and bad breath and an action of deodorizing. [0007] The oral preparation successfully provided by the present invention comprises water, an aliphatic alcohol having 1 to 4 carbon atoms, a lower aliphatic ketone, or a mixture thereof, as an extraction solvent. Characterized by containing an extract of peanut astringent skin obtained by extraction. DETAILED DESCRIPTION OF THE INVENTION Peanut astringent skin (also called thin skin or cuticle) is produced in large quantities in the process of processing peanuts into food such as peanut butter, and a part of it has been conventionally used as livestock feed. Most are just discarded. This astringent skin can be used as it is as a raw material for producing an oral agent according to the present invention. [0009] Peanut astringent skin is prepared by removing aliphatic alcohols having 1 to 4 carbon atoms such as methanol, ethanol, isopanol and butanol; polyhydric alcohols such as 1,3-butylene glycol, propylene glycol and glycerin; lower fats such as acetone and methyl ethyl ketone. When immersed in an aromatic ketone; water; or a mixture thereof at room temperature or in a heated state, a brown extract is obtained from which about 10 to 10%
A light brown extract is obtained with a yield of. [0010] This extract contains a component that exhibits a strong glucosyltransferase inhibitory action. Since it has a mild taste and odor, it can be used as it is as a glucosyltransferase inhibitory component in the oral preparation of the present invention. This extract also has the effect of preventing glucans, whose production could not be completely inhibited by the glucosyltransferase inhibitory action, from adhering to the tooth surface and growing as plaques. The synergistic action of the inhibitory action significantly reduces plaque and prevents caries. Further, since the extract has a deodorizing effect, bad breath can be effectively prevented in combination with suppression of the cause of bad breath by inhibiting plaque formation. The components in peanut astringent bark that exhibit the above-mentioned useful effects are hardly extracted by hydrocarbon solvents or ester solvents, and these solvents are not suitable as extraction solvents. The peanut astringent skin extract does not show an antibacterial effect against useful intestinal bacteria such as lactic acid bacteria. Therefore, even if this extract is sent to the gastrointestinal tract by accidental ingestion or chewing of the oral preparation, there is no possibility that the extract will adversely affect the intestinal flora. Examples of oral preparations suitable for utilizing the above-mentioned useful effects by incorporating a peanut astringent skin extract include various toothpastes, mouthwashes, troches, chewing gum, candy, gummy, oral pasta, gingiva There are massage cream, gargle, mouth freshener, etc. [0016] By blending the peanut astringent skin extract, there is no restriction on other components of the oral preparation and the method of producing the oral preparation. For example, calcium hydrogen phosphate, calcium carbonate, insoluble sodium metaphosphate, aluminosilicate, Abrasives such as silicic anhydride and resin; surfactants such as long-chain sodium alkyl sulfate, sodium lauryl sulfoacetate, lauryl diethanolamide, sucrose fatty acid ester; CMC, hydroxyethyl cellulose, alginates, carrageenan, gum arabic, polyvinyl alcohol Binders such as polyethylene glycol, sorbitol, glycerin, propylene glycol;
Sweeteners such as saccharin, stevioside, glycyrrhizic acid, thaumatin; preservatives such as dehydroacetic acid and sodium dehydroacetate; fragrances such as menthol, carvone, eugenol, anethole, peppermint oil, spearmint oil, peppermint oil, eucalyptus oil; For example, raw materials usually used for the production of oral agents can be arbitrarily selected according to the type and use of the product, and can be produced by a conventional method. The preferred addition rate of the peanut astringent skin extract to the oral preparation varies depending on the content of the active ingredient and the substance to be added. An example in which a standard peanut astringent skin extract is directly incorporated into a toothpaste is about 0.1%. 001 to 5.0
% Is an appropriate amount, and a particularly preferable compounding ratio is about 0.05.
~ 1.0% by weight. Hereinafter, the present invention will be described with reference to examples. In the examples, “parts” means parts by weight. Production Example 100 g of peanut astringent skin is placed in 1000 ml of an extraction solvent and allowed to stand at 40 ° C. for 24 hours to extract soluble components.
The obtained extract is concentrated to dryness under reduced pressure to obtain a solid extract. The above-mentioned extraction operation was carried out by changing the extraction solvent in various ways. Table 1 shows the yield of the obtained extract. Extraction solvent Extraction yield (%) Water 10.2 50% ethanol 15.5 Methanol 12.2 Ethanol 11.8 Acetone 8.9 50% Acetone 9.5 1,3-butylene glycol 10.5 Ethyl acetate 2.3 n-hexane 1.7 The obtained extract was subjected to the following tests and production of oral preparations. Test Example 1: Test of glucosyltransferase inhibitory activity 50 μl of a sample solution (solvent: 50% ethanol), 1.0 m of a 2% sucrose aqueous solution containing 0.1% of sodium azide
1, 50 μl of a crude glucosyltransferase solution (prepared from Streptococcus mutans) and 900 μl of distilled water are placed in a test tube and mixed. 37
After reacting at 5 ° C. for 5 hours, the produced glucan is dispersed in water with a stirrer, and the absorbance at a wavelength of 550 nm is measured as an index of turbidity. Separately, as a blank test, the absorbance measurement is performed in the same manner as above except that the solvent of the sample solution is used instead of the sample solution. Further, in each case, the same operation and measurement are performed without adding the crude glucosyltransferase solution. From the measurement results, the inhibition rate of glucosyltransferase activity is calculated by the following formula. Inhibition rate (%) = [1- (CD) / (AB)] × 10
0, where A: absorbance of sample solution after enzyme reaction B: absorbance of sample solution without enzyme addition C: absorbance of blank test solution after enzyme reaction D: absorbance of blank test solution without enzyme addition The above measurement is carried out by changing the concentration of the sample solution stepwise, and the concentration IC _{50 of the} sample solution at which the inhibition rate becomes 50%.
(The smaller the IC ₅₀ value, the stronger the enzyme inhibitory activity). Table 2 shows the results of the above-mentioned tests performed on the four kinds of peanut astringent skin extracts and the green tea water extract as a reference example (the ethyl acetate extract is a control example). Table 2 IC ₅₀ value (μg / ml) Water extract 14 50% methanol extract 18 Ethanol extract 21 Ethyl acetate extract> 100 (Green tea water extract 32) Test Example 2: Plaque Test of formation inhibitory action Brain Heart Infusion Broth (manufactured by Nissui Pharmaceutical Co., Ltd.) containing 2% sucrose in a test tube weighed beforehand 5.3
Add 5 ml. After heat sterilization, the sample solution (solvent: 50
% Ethanol) 0.15 ml and Streptococcus
0.5 ml of the culture solution of Mutans 6715 was added, and 37
Incubate at 20 ° C for 20 minutes. After completion of the culture, the supernatant is gently removed, and the plaque-like deposit on the tube wall of the test tube is directly washed with distilled water three times and then dried at 105 ° C. for 5 hours. Finally, the test tube is weighed to determine the dry weight w of the plaque-like deposit in the tube. Separately, as a blank test, the same operation as described above is performed using the solvent of the sample solution instead of the sample solution, and the dry weight W of the plaque-like deposit is obtained. From the measured weights w and W of the plaque-like deposits, the plaque formation inhibition rate is calculated by the following equation. Plaque formation inhibition rate (%) = (1−w / W) × 100 The above measurement was carried out by changing the concentration of the sample solution stepwise, and the concentration IC _{50 of the} sample solution at which the inhibition rate was 50% was obtained.
Table 3 shows the results of the above test conducted on four kinds of peanut astringent bark extracts obtained by interpolation and green tea water extract as a reference example (the ethyl acetate extract is a control example). Table 3 IC ₅₀ value (μg / ml) Water extract 7.0 50% methanol extract 11.2 Ethanol extract 13.5 Ethyl acetate extract> 100 (green tea water extract 14) Test Example 3: Test for deodorizing effect 20 ml of an aqueous solution of peanut astringent skin extract having a predetermined concentration was added to 900
Put in a 0.5 ml capacity bottle and add 0.5% ammonia water or 0.5%
0.5 ml of a 6% aqueous solution of trimethylamine is added. After the addition, the mixture is quickly sealed with a rubber stopper, shaken in a 37 ° C. thermostat for 10 minutes, and then left still for 5 minutes. Then, the concentration of ammonia or trimethylamine in the air in the upper space in the bottle is measured with a gas detection tube. Separately, a similar test is performed using distilled water instead of the sample solution. The measured odor gas concentration was 100 times the odor gas concentration when distilled water was used.
It is expressed as a fraction to be the odor gas residual rate. Tables 4 and 5 show the results of the above tests carried out using the water extract and the ethanol extract as the peanut astringent bark extract. For comparison, the measurement results when a green tea extract (50% ethanol extract) was used are also shown. Table 4 Odor gas residual rate (%, odor component: ammonia) Sample concentration (w / v%) Water extract Ethanol extract Green tea extract 0.5 21 28 6 0.2 51 68 24 0.0 1 69 87 49 Table 5 Odor gas residual ratio (%, odor component: trimethylamine) Sample concentration (w / v%) Water extract Ethanol extract Green tea extract 0.2 13 20 1 0.1 35 488 0.05 52 71 35 Hereinafter, examples of oral preparations containing these peanut astringent skin extracts as a caries-preventing and deodorizing component will be described. Example 1 Ethanol 20 parts Glycerin 0.2 part Chlorhexidine 5 parts 1-Carbon 0.005 parts Peanut astringent skin water extract 1 part [0037] Water was added to the above raw materials to make the total amount 100 parts, and glucosyltransferase inhibition was performed. A mouthwash having an action, a plaque formation inhibitory action and a deodorant action was produced. Example 2 45 parts of dicalcium phosphate 1 part of CMC sodium salt 1 part of glycerin 20 parts of sodium lauryl sulfate 1 part of 1-menthol 1 part of peanut astringent skin 50% ethanol extract 1 part of water 30 parts An anti-corrosion and deodorant toothpaste was manufactured. Example 3 The following materials were treated by a conventional method for producing chewing gum to produce a chewing gum having a caries-preventing action and a deodorant action. Chewing gum base 20 parts sucrose 50 parts starch syrup 20 parts softener 4 parts fragrance 1 part peanut astringent skin 50% ethanol extract 5 parts Example 4 The following ingredients are mixed, concentrated and molded by the usual method of candy production. A candy having a caries-preventing action and a deodorant action was produced. 70 parts sucrose 30 parts starch syrup 30 parts citric acid 1 part flavor 0.1 part peanut astringent skin water extract 3 parts water 15 parts Effect of the present invention Peanut astringent skin extract is the activity of glucosyltransferase causing caries It has an excellent effect of inhibiting plaque formation by inhibiting the formation of plaque, and also has a deodorizing effect. Since peanuts are a food material that may be eaten without peeling the astringent skin, there is no problem in the safety of the astringent skin extract. In addition, there is no possibility that the astringent skin extract exerts an undesirable antibacterial action on useful intestinal bacteria. The oral preparation of the present invention containing such a peanut astringent skin extract is excellent in anti-caries action and feeling of use,
Furthermore, it has excellent safety and is extremely effective as a means for preventing caries.

Continuation of the front page (56) References JP-A-7-258105 (JP, A) JP-A-8-310931 (JP, A) JP-A-10-139646 (JP, A) JP-A-4-221308 (JP) JP-A-9-2968 (JP, A) JP-A-7-242555 (JP, A) JP-A-1-301614 (JP, A) JP-A-7-17824 (JP, A) JP 59-101414 (JP, A) JP-A-3-77818 (JP, A) (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K ^7/ 00-7/50

Claims (1)

(57) [Claim 1] Water, an aliphatic alcohol having 1 to 4 carbon atoms,
An oral preparation comprising an extract of peanut astringent skin obtained by extraction using a lower aliphatic ketone or a mixture thereof as an extraction solvent.