TW528602B - Composition for use in oral cavity comprising fluorine ion providing compound, calcium ion providing compound and sugar alcohol - Google Patents

Abstract

The present invention relates to a composition for the oral cavity, which comprises a compound serving as a fluorine ion supplier, a compound serving as a calcium ion supplier, and a sugaralcohol in which xylitol is contained in a proportion of not less than 1/2 by weight. This composition is capable of blocking the potential precipitation of calcium fluoride between calcium ion and fluorine ion even when anionic surfactant is present, and has a highly excellent effect of accelerating re-calcification of the teeth.

Description

528602 is a composition that promotes A7 and B7. Technical Field The present invention relates to an oral composition; in particular, it is a composition for oral I recalcification and excellent stability.

Technical background The main component of W dentin is hydroxyapatite (Cai () (P〇4) 6 (〇Hy. ^ In the oral cavity, the dissolution of phosphate ions and calcium ions, etc., produces 2 acting ash)) and becomes The crystallization of Calcium Phosphate and Hydroxyapatite is in a state of equilibrium (recalcification). Here, generally, the acids produced by the bacteria on the shoulders of the teeth will promote their deliming effect. In other words, Dental caries is caused by bacteria such as ^ MQQocous mutans that make up tartar, and decomposes sucrose and other substances, and produces organic acids mainly composed of lactic acid, which will lower the pH =, so that = and other substances will be dissolved and caused. In the early days, although white spots will be produced on the pearl of the Ming Dynasty, at present, it has also been lost because fluoride and calcium ions can promote recalcification, which will make the white spots disappear and make enamel. It becomes transparent again. However, when * fluoride and # 5 ions coexist, all fluoride precipitates will be generated, which will reduce the effect of recalcification. To solve this problem, there is a solution of fluoride ion solution and calcium ion solution. save The 2 doses of oral hygiene products used in different containers, which are appropriately mixed only when used, are provided (Japanese Patent Application Laid-Open No. 5 2 -6 1 2 3 6 and Japanese Patent Application Laid-Open No. 5 8-2 1 9 1 No. 0 7), and an oral composition in which calcium fluoride is dispersed into a gelatinous form with a sugar phosphate or the like to promote recalcification thereof (Japanese Patent Application Laid-Open No. 3-724-15). The technologies disclosed in No. 52-6 No. 1236 and 58-2 19 No. 107 'The manufacturing steps are extremely complicated, and it must be painful to use. 2 liquid mixing, please read (Please read the precautions on the back before filling this page)

-4-: ¾¾ • 部 屮 Rong i?. ^ R ^ n < .T. Consumer 1 Hezhu $ 卬 f 528602 A7 、 --- ^ _____________ B7 V. Description of the invention (2) From the viewpoint of convenience It can be a problem. The technology of JP-A-3_72415 'is not easy to disperse fluorination in a high concentration into a colloidal form, and anionic surfactants such as sulphuric acid used for brushing m @ 帛, n_aminoaminobismuth, etc. When present, there will be a problem that the dispersion effect of the aforementioned sugar phosphate is low. Therefore, an object of the present invention is to provide a composition for oral cavity, which can inhibit refluoridation of teeth by suppressing the fluorination and sinking effects caused by fluoride ions and the auditory body. Disclosure of the present invention The inventors of the present case have discovered that if a sugar alcohol containing xylitol is added in addition to a fluoride ion-supplying compound and a calcium ion-supplying compound, the precipitation of calcium fluoride will be completely unexpected. The present invention has been accomplished by suppressing the formation of an oral composition having an excellent tooth recalcification promoting effect while suppressing its production. The present invention provides a composition for oral cavity, which is characterized by including a fluoride ion-supplying compound, a calcium ion-supplying compound and a sugar alcohol, and more than 1/2 (weight ratio) of the sugar alcohol is xylitol. Best mode for carrying out the present invention The fluorine ion donating compound used in the present invention may be an inorganic compound or an organic compound. Specifically, it may be sodium fluoride, potassium fluoride, tin fluoride, sodium fluoride silicate, sodium monofluorophosphate, aluminum fluoride, silver fluoride, hexylamine hydrofluoride, decanolamine hydrofluoride, Octadecylamine hydrofluoride and the like. Among them, from the perspectives of safety, dissolution and flavor, sodium fluoride is particularly good. The content of fluoride ion-supplying compounds in the oral cavity composition, if converted into fluorine, _____ _5_ This paper is of appropriate size (CNS) A4 size (—public (please read the precautions of the back fi and then fill out this page)

528602 A7 B7 This paper scales against the fifteenth, description of the invention (3 is preferably 0.002-1% by weight, particularly preferably 0.01-0.2% by weight. When the blending amount is between 0.02 and 21% by weight, it is not only It will not adversely affect the flavor and physical properties of the oral composition, and will also promote its recalcification effect. The dance ion donating compound used in the present invention can be an inorganic or organic mouthwash. Specific Examples include: calcium chloride, calcium bromide, calcium nitrate, calcium lactate, calcium gluconate, calcium acetate, etc. Among them, taking into consideration factors such as safety, synthesis, and flavor, calcium lactate is used as Particularly preferred. The amount of calcium ion-supplying compound in the oral composition is preferably 0.001-0.5% by weight when converted to calcium, and particularly preferred is 0% by weight of 0 muscle. When the amount is between 0 and 0.5 When it is between% by weight, it will not cause any adverse effects on the flavor and physical properties of the oral composition, and it can further promote its recalcification. Handle = content relative to the fluoride ion-supplying compound (converted to fluorine), Its 〆 ', the content of the compound (converted to calcium (That is, the weight ratio of Ca / F) is less than ^ ^, especially between coffee and -1/3. When the ratio is between 1/2 and: ', it can suppress the formation of air sacrifice and promote it more. At the same time as the formation of re-lime re-sinking, it also has the ability to promote, maltthorn-π 田 摩 么 (examples have been saccharitol, isomalt ^ 0-alcohol, and maltotriol, glucosyl malt _ ^ sugar Tetraol, j 4 f Toxicity, Isomalt, Glycerol, Fresh Alcohol, Arabitol: Ribitol, Xylitol, Sorbitol, Glycolol, Maltosan, ° ° Also good Gan · The temple sugar alcohol is D type or L penalty, horse stable, mixture. Among them, xylene-alcohol-earth bacteria _ η shot "to make scaly fur in tartar and inhibit the reduction of scale ρΗ 値, " When suppressing calcium fluoride 'cnsYm gauge (read the precautions on the back before filling in this page)

浐 ir ^-^ hJ · elimination of mixed bamboo shirts y 528602 Ⅴ. Description of the invention (4 The effect of precipitation is also very good. Therefore, the content of xylitol in sugar alcohol is too high. In Mao Ming, the ratio (weight ratio) is preferably 2/3 or more. In addition, all sugar alcohols (solid form or more) are particularly preferred in the blending amount, preferably 12, wt%, particularly preferred = the original compound. The oral composition of the present invention may be 0% by weight. It may be in a paste or liquid form. In the case of water, it may be in powder form or 90% by weight in water. It is not particularly limited in ^, but 1- When water is used, the sugar alcohol is relatively preferably 25% by weight or more, and the & water < content ratio is better than 35-300 tongues. 0 / For water, the content ratio is 25%. Precipitation and formation of sugar alcohol phase can also improve mouth ☆. People, not only can inhibit calcium fluoride < wettability. The composition for heart and oral cavity of the present invention can make the generation of fluoride ions and dance ions, especially i The presence of xylitol) can stabilize the composition of the present invention. / State, so the composition of the present invention may contain a lambda. Rt, which is used as a horse oral composition, for example, sulfonium sulfate vinegar such as sodium lauryl sulphate, laurel tincture in a sub-surfactant: ::. Especially when the shade is lt When the content of sodium I (weight ratio) is more than 1/2, the effect of the present invention will not be impaired. In addition, the ethylene diamine tetraacetic acid (ribidine A) and N · (2-hydroxyl) are not included in the present invention. Ethyl) -imine diacetic acid and other calcium ion blocking agents (chelating agents) are preferred for promoting the recalcification of the teeth. On the other hand, the oral composition of the present invention may be added with grinding Agent, but it is preferred to use 2 hard abrasives as the abrasive, rather than substantially adding each abrasive. Generally speaking, when using abrasive silica and fluorine to supply compounds by hand

(Please read the notes on the back before filling in this page)

528602 A7 B7 OCHoCHo · (1) 1. Description of the invention (5: When the prepared abrasive is used to brush the teeth, the teeth will have a frictional touch, and the toothbrushing agent of the present invention is exhausted: it also contains abrasive stone stone It has the excellent effect of not feeling friction as described above with fluoride ion: compound. Abrasive silica used in the present invention absorbs 2 amounts of non-cutting acid or containing cutting acid (measured according to JISK5101 method) Winners, the same below) is preferably 80-200 ml / g, average particle size is 2_2G microns. The blending amount of these abrasive stones in the toothbrush preparation is preferably stomach 5-30 weight 10-20% by weight .When the blending amount is between 5-30% by weight, it can be sufficient: the grinding effect is exerted. In addition, if the present invention uses 2-15% by weight of oil absorption '200-400ml / 100g of cohesive silica, Because it can keep good shape retention, it is also the better one. In the present invention, if further adding morning acid vinegar or a salt thereof having a carbon number of 10-20, preferably 12-16, & In addition to promoting the recalcification of the teeth, it can also give the teeth a smooth feel. This phosphate mono-fermentation refers to the following formula (1) Shown:

II

Bu P-OH

I

OH (wherein R1 is a carbon number, a linear or branched alkyl or alkenyl group of 6-20; f Table 0-4 < number.) And its salts may be sodium, potassium, calcium, Magnesium salts, etc. Among them, the calcium salt or the magnesium salt may be a salt composed of a calcium plasma and a molecular phosphate monoester of i or a salt composed of two molecular phosphorus-bismuth monoester bridges. Phosphate monoester salts can be easily mixed with monobasic phosphate from steel hydroxide, hydroxide conversion, etc. (Read the precautions and precautions of back-xenon before filling this page)

-8- 528602 A7 B7 i 浐. ^-/. Jh J > /)! MM ^. 印 f 5. Invention description (6 2 generated. Therefore, when adding acid monohydrate, you can deploy嶙 and lice sodium oxide, etc., after cooking, it is recognized as "Early ® Day", and "Man V", which generates phosphate monoesters in toothbrushing agents. ^ In the present invention, carbon numbers of 10-20 may be additionally added. , Preferably a straight bond of 12-16, to further alleviate the frictional feeling after brushing the teeth. The complex acid can be divided into lauric acid, yuna a ^ κ # palm bismuth, stearic acid, oleic acid, linoleic acid Etc. And here ... the salt can be sodium salt, unsalted salt, unsalted salt, magnesium sleep, etc. A few acid salts: It is easily composed of hydroxide, hydroxide, and money. You and 'in adding In the case of acidification, it is possible to mix chitoic acid and steel hydroxide, etc., and then to generate carboxylic acid salt in the toothbrushing agent. The composition of the present invention can be added with glycerin, as long as the effect of the present invention is not impaired. Polyethylene glycol: wetting agents such as alcohol, binding agents such as kinetocellulose, saccharin, sweetener, coloring agent, preservatives such as paraben benzoate, benzoic acid, etc. benzeth〇n_ _ Γι, isopropylmethyl isocyanate and other fungicides, anti-inflammatory agents, and fragrances, etc. However, the addition of carbon dioxide, hydrogen phosphate, and pyrophosphoric acid is an addition of abrasives, because it will fluoride fluoride and hinder recalcification. The effect is not a good choice. The oral composition of the present invention can be prepared by stirring or kneading the aforementioned ingredients according to common methods. The oral composition of the present invention can be used as tooth powder, moisturizing brushing agent, toothpaste, liquid Use for toothbrushing and mouthwash.

Several examples are given below to illustrate the present invention in more detail, but the scope of the present invention is not limited to the following examples. X -9 This paper is suitable for China National Standards (CNS) M specifications (2 丨 0X 297). (Please read the back ¾. Note r item before filling this page j 丨 order 528602 Α7 Β7 —--- --- V. Description of the invention (7 Example i-2, Comparative Examples 1-5, with the formula shown in the table below, prepare oral compositions (perform the following tests: and) '亚 4 7 teeth of 7 cattle It is divided into two, and the table is the same as the eight powers of S. She only studied her research history ... The other side of the change was covered with oil-bearing mamcure for the following tests. v > / ττ 、,,, and HEC% sticky milk I, immersed in Youchong (pH 4.5) and 37 »C for 5 days, so as to deliming. Here, it has been divided into 2 The inside of the cow's teeth was treated as a recalcification treatment group, while the other was a control group (only the decalcification treatment group and the recalcification treatment group were subjected to the following recalcification treatment. That is, a 5-minute mouthwash treatment After that, rinse with water, artificial saliva; (PH7.0, 20mMHEPES buffer solution + 15% solution from plus 2 + 0.99ΓηΜΡΟΛ solution from K2HP04) immersed for about 8 hours. After cooking with After washing, the M mouthwash was treated for 5 minutes, and then washed again with water and recalcified for about 16 hours. This was a series of treatments, such as dehydration and drying. Then After the calcification treatment group and the control group were embedded with polyacetate resin, they were cut off and made into abrasive slices with a thickness of about 100 micrometers, and soft radiographs were taken. Compare and observe the recalcification treatment group. The soft X-ray film of the group was subjected to pattern analysis at the same time to calculate the recalcification rate. The results are shown in Table 2. On the other hand, the oral composition (mouthwash) shown in Table 丨 was stored in the room after preparation. Observe solubility at 'i-day under temperature'. Judgment of solubility is represented by 0 if it is transparent; .χ if it is mixed. The results are also shown in Table 1. In addition, the laser scattering Observation can be confirmed. Examples and 2 -10 copies of this paper rule] China National Standard (CNS) Μ specifications T2Η) X 297 clear (楚 Please read the back & note Ψ item before filling This page j

528602 A7 B7 ,, 1 'Λ [Part A 卬 5. In the description of the invention (8), there are colloidal particles considered to be calcium fluoride, but not in the comparative example. Table 1 Formulation ratio (weight ° / 〇) Example 1 Example 2 Comparative example 1 Comparative example 2 Comparative example 3 Comparative example 4 —- — Comparative example 5 Sodium fluoride 0.21 0.21 0.21 0.21 0.21----- ^ lactic acid 0.1 0.1 0.1 0.1-0.1-Xylitol 25 15--25-Sorbitol-15-----Glucose 1 sodium phosphate---10---Sodium lauryl sulfate 0.1 0.1 0.1 0.1 0.1 0.1-Spice 0.05 0.05 0.05 0.05 0.05 0.05-Pure water 74.54 69.54 99.54 89.54 99.64 84.54-Artificial saliva *------100 Total 100 100 100 100 100 100 100 100 Solubility 0 0 XX 0 〇〇Recalcification rate (%) 70 65 22 25 33 19 17 * The composition of artificial saliva: 20 mM HEPES buffer + 15 mM caC: 12 + 0.9 mM K2H | > 〇4 (pH 7.0) From the above table, it is known that it contains sodium fluoride and calcium lactate Examples of sugar alcohols 1-2, compared with Comparative Examples 1-5, did have a higher recalcification rate. Examples 3-5 and Comparative Example 6 The composition of each example was formulated according to the formula shown in Table 2, where > Example 4 is made of -11-This paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X 297 mm) '' ---_ 528602 A7 _________ B7 ----- 5. Description of the invention (9) Tooth powder, while other examples and comparative examples are made into toothpaste. Each of the five subjects was ordered to use these compositions for one month (these subjects had white spots above the anterior teeth of their upper jaw that were thought to be caused by the action of lime). As a result, in Example 3, the white spots tended to shrink, especially

In the ^ I section I ii?. ^-XJ ', i < T- 消 抡 合 竹 # 卬' H Examples 3 and 4, the effect is particularly great. No other changes were seen. Table 2 On the one hand, Comparative Examples 16 and 16 are fully formulated (weight%) Example 3 Example 4 Example 5 Example 6 Sodium fluoride 0.21 0.21 Steel monofluorofluoride--0.7 0.7 Lactic acid # 5 0.1 0.05-Chloride -〇.1 Xylitol 25 40 20 Sorbitol 5 21.84-4 Glycerol---26 Carrageenan 0.5-0.5 0.5 Xanthan gum 0.3 0.2 0.5 Carboxymethylcellulose sodium 0.3-0.7 0.7 Anhydrous crushed acid 26 30 22 22 Polyethylene glycol 600 5 5 Ί 7 Methyl parahydroxybenzoate 0.1 0.1 〇.1 0.1 -12- $ Paper size Shizhou Chinese National Standard (CNS) A4 specification (210X297 mm) (翱 Read the back first (Notes for TSL • Matters need to be completed on this page)

528602 A7 B7 Jk il in the fifth part of the invention description (10 sodium lauryl sulfate 1.4 1.6 1.2 1.2 spices 1 1 1 1 appropriate amount of pure water--appropriate amount total 100 100 100 100 Ca content / F content (wt%) 1 / 7.3 1 / 14.6 1 / 2.6 0 Number of teeth white spots reduced 4/5 3/5 2/5 0/5 Example 6-9, Comparative Example 7 Add the ingredients shown in Table 3 to pure water and stir Then, the toothbrushing agent was prepared and the following tests were performed. Using the various toothbrushing agents obtained above, each pair of 10 reviewers' required that they brush their teeth for 5 minutes in the morning and night respectively5 and asked the reviewers to follow The evaluation criteria are used to evaluate the tactile sensation of the teeth after brushing. The average evaluation of 10 persons is shown in Table 3. The evaluation criteria of the tooth sensation: 2: smooth feel 1: slightly smooth feel 0: no one can say One feeling -1: Slight frictional feeling 2: 2: Frictional feeling (read the precautions and notes of vg before reading this page)

、 1T consumption fc A 卬 13- This paper size is applicable to China National Standard (CNS) A4 specification (210X 297 mm) 528602

B. Description of the invention (11) Table 3 Formulation ratio (% by weight) Example 6 Example 7 Example 8 Example 9 Comparative Example 7 Sodium fluoride * '0.21 0.21 0.21 0.21 0.21 Calcium lactate ** 0.1 0.1 0.1 0.1-Xylitol 25 25 25 25 25 Sorbitol 5 5 5 5 5 Carrageenan 0.5----Xanthan gum 0.3 0.5 0.5 0.5 0.5 Sodium carboxymethyl cellulose 0.3 0.4 0.4 0.4 0.4 Abrasive silica 18 18 18 18 18 Thickening Crushed stone 8 8 8 8 8 Polyethylene glycol 600 5 5 5 5 5 Sodium lauryl sulfate 1.4 1.4 1.4 1.4 1.4 Methyl parahydroxybenzoate 0.1 0.1 0.1 0.1 0.1 Cinnamic acid-0.4---Lauric acid- -0.2--Calcium stearate--1 48% sodium hydroxide solution-0.1 0.05--Fragrance 1 1 1 1 1 Pure water 35.09 34.79 35.04 34.29 35.39 Total 100 100 100 100 100 Touch of teeth after brushing 0.3 1.5 1.1 0.8 -1.7 (Read the first page of the back and the precautions before filling out this page) -14- The paper size is suitable for National Standards (CNS) Λ4 specifications (210X 297 mm) A7 B7 528602 V. Description of the invention (π * : Sodium fluoride 〇.21% = Gas conversion amount 0 095% I Milk fat conversion amount 〇013〇 / From Table 3, Example 6 〇, t ,, the agent phase is light, and the teeth are stretched into _ 〈brushing agent, compared to Example 7 for toothbrushing acid suppression: //, ㈣ ~ are indeed better, especially those containing a specific chain length of mm salt _, The effect is more significant. Industrial applicability The oral group of the present invention is extremely excellent in personal fruit, and it is also very good in making the recalcification promotion effect of = :: qu. When used as a toothbrushing agent, Its feeling of use and hobby -------- # gI (Please read the note on the back • Note 4 $ · Matters before filling out this page) .I order department

Jk i ·· 消 fc 合 竹 卬 15- This paper has the right size] Chinese National Standard (CNS) A4 size (210X 297 mm) I Announce the date of this application i, 〇 'Case No. 87111638 Category h', 1 < (Notes to the above by the Bureau) Supplement fj A4 C4 Chinese Manual Correction Page (June 90) Ode-ί member clearly stated whether the original substance will be changed after three revisions, printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economic Affairs % 1 Patent Specification 52 edits 2 I. The name of the hairpin New Chinese Oral composition containing fluoride ion supplying compound, calcium ion supplying compound and sugar alcohol English COMPOSITION FOR USE IN ORAL CAVITY COMPRISING FLUORINE ION PROVIDING COMPOUND. CALCIUM ION PROVIDING COMPOUND AND SUGAR ALCOHOL I. Inventor I. Name creation Nationality 1. Oshio Noji 2 · Masaya Toshiro 3. Yukiko Ueki 4. Yamazaki Moto 5 Miyuki Okashima 6 Hiroki Ueda 7. Both Maeda Akira said the place of residence and the place of residence 2606 Kao Co., Ltd., Kabe Co., Ltd. in Kagami-gun, Fagaga-gun, Gokugi County, Japan Japanese name III. Applicant's residence and residence (office) Name of representative No. 10 Goto, Nihonbashi, Kababa-cho, Chuo-ku, Tokyo, Japan-Goto Takuya -1-The size of the linen paper is applicable to Chinese National Standards (CNS) A4 specifications (2 〖〇X 297 ychu）

Claims (1)

• ~ Oral compositions. It is characterized by containing a fluoride ion-supplying compound ^ calcium ion-supplying compound and a sugar alcohol, in which more than 1/2 of the sugar alcohol (weight I ratio) is xylitol, and the fluorine-ion-supplying compound The content (converted into fluorine) is 0.002-1% by weight, the content of calcium ion-supplying compounds (calculated as calcium) is 0.001-0.5% by weight, and the content of sugar alcohol is 12.99% by weight; The content (converted to fluorine) and the content (calculated to calcium) of the calcium ion-supplying compound (Ca / F, weight ratio) are 1/2 or less. According to the application, it is called the oral composition of item 1 of the patent scope, in which the ratio (calculated as calcium) of the calcium ion-supplying compound (Ca / F) to the content of the ion-supplying compound (converted to fluorine) , Weight ratio) is ⑼. The oral composition according to item 1 or 2 of the patent application does not contain # 5 ion blocking agent. The oral composition according to claim 1 or 2 further comprises water. The oral composition according to item 4 of the application #patent scope, wherein the content ratio of sugar alcohol to water is 25% by weight or more. 6. The composition for oral cavity according to item 1 or 2 of the scope of patent application, which further contains abrasive silica and is substantially free of calcium-based abrasives. 7. The oral composition according to item 1 or 2 of the scope of patent application, which further contains a phosphate monoester having a carbon number of 10-20 or a salt thereof. 8. The oral composition according to item 1 or 2 of the scope of patent application, which further contains a carboxylic acid having a carbon number of 10-20 or a salt thereof. 9. The composition for oral cavity according to item i or 2 of the scope of the patent application, wherein the gas ion supplying compound is sodium fluoride and the calcium ion supplying compound is lactic acid # 5. 10. The oral composition according to item i or 2 of the patent scope of the application, which uses 528602 8 8 8 8 A BCD. 6. Application of patent scope of oral composition for promoting recalcification of teeth. 11. The oral composition according to item 1 or 2 of the scope of patent application, which is a toothbrushing agent. This paper size applies to China National Standard (CNS) A4 (210X 297 mm)