Oral compositions comprising silica and chondroitin sulfate and uses thereof

Abstract

The present application provides an oral composition comprising the following components: (a) at least one silica particle; and (b) at least one chondroitin sulfate, the mass ratio of component (a) to component (b) being greater than 1; the molecular weight of the component (b) is 8kDa or above, and the composition can enable the sealing rate of dentinal tubules to reach 50% or above or even 90% or above after acting on teeth for a short time, so that the effect of rapidly relieving and repairing tooth sensitivity is achieved.

Description

Technical Field

[0001] The present application relates to the field of oral technology, and in particular to an oral composition comprising silicon dioxide and chondroitin sulfate and uses thereof. Background Art

[0002] Tooth sensitivity is a pain point for a considerable number of consumers. The reason is that the loss of enamel leads to the exposure of dentinal tubules, which allows irritating foods to directly stimulate the dental nerves through the dentinal tubules (e.g., 2-3 μm). Dentin is a material with a low degree of mineralization, composed of minerals (hydroxyapatite) and organic content (collagen). The dentin layer is also porous, with circular tubules extending outward from the root of the tooth and allowing nutrients to be transferred to different parts of the tooth. When these tubules are exposed to external stimuli (such as heat, cold or polysaccharides), it is speculated that the fluid pressure in the tubules changes (due to expansion / contraction) and causes the pain associated with sensitive teeth.

[0003] In order to alleviate tooth sensitivity, the oral care industry has developed a variety of repair technologies based on the mechanism of closing the dentinal tubules, such as desensitizing toothpaste containing potassium nitrate. Potassium nitrate is a nerve blocker, and the potassium ions in it interfere with the ability of teeth to send pain signals to the brain. However, it is recommended not to use potassium nitrate toothpaste continuously for more than two weeks. For example, mineral deposited toothpaste containing fluoride and calcium; particle deposited toothpaste containing hydroxyapatite, etc. Some silica particles are air-milled to achieve the appropriate particle size distribution required for loading into the tubules.

[0004] However, it is difficult for the existing technology to completely seal the exposed dentinal tubules after a short-term action on the teeth (such as one or two brushings), so there is still a certain gap between the effectiveness of quickly relieving tooth sensitivity and consumers' expectations. Summary of the invention

[0005] In view of the technical problems existing in the prior art, the present application provides an oral composition and its use. After cleaning the teeth, the composition can seal most of the dentinal tubules, thereby achieving the effect of quickly alleviating tooth sensitivity.

[0006] The specific technical solutions of this application are as follows:

[0007] 1. An oral composition comprising the following components:

[0008] (a) at least one silicon dioxide; and

[0009] (b) at least one chondroitin sulfate,

[0010] The mass ratio of the component (a) to the component (b) is greater than 1;

[0011] The molecular weight of the component (b) is above 8 kDa.

[0012] 2. The composition according to item 1, wherein the component (a) is ≥ 10%, preferably 10-50%, by mass percentage in the composition.

[0013] 3. The composition according to item 1 or 2, wherein the molecular weight of component (b) is 8k-40kDa.

[0014] 4. The composition according to any one of items 1 to 3, wherein the component (b) is ≥ 0.8% by mass in the composition.

[0015] 5. The composition according to any one of items 1 to 3, wherein the component (b) accounts for 0.8-5% by mass in the composition.

[0016] 6. The composition according to claim 1, wherein the mass ratio of the component (a) to the component (b) is 5-30:1.

[0017] 7. The composition according to any one of items 1 to 6, further comprising one or more orally acceptable carriers.

[0018] 8. Use of the composition according to any one of items 1 to 7 for preparing a product for sealing dentinal tubules.

[0019] 9. Use of the composition according to any one of items 1 to 7 for preparing a product for preventing / alleviating tooth sensitivity.

[0020] 10. The use according to item 8 or 9, wherein the product is a dentifrice product.

[0021] Effects of the Invention

[0022] The composition described in the present application can effectively seal the dentin tubules after cleaning the teeth;

[0023] Furthermore, the composition described in the present application can achieve a closure rate of dentinal tubules of more than 50% or even more than 90% after a short-term effect on teeth, thereby achieving the effect of quickly alleviating and repairing tooth sensitivity. BRIEF DESCRIPTION OF THE DRAWINGS

[0024] Figure 1 is a schematic diagram of brushing teeth using a toothbrush device.

[0025] Figure 2A Schematic diagram of dentinal tubules in a control area of ​​teeth brushed with the toothpaste sample of Example 1.

[0026] Figure 2BSchematic diagram of dentinal tubules in the brushing area of ​​teeth brushed with the toothpaste sample of Example 1.

[0027] Figure 3A Schematic diagram of dentinal tubules in a control area of ​​teeth brushed with the toothpaste sample of Example 3.

[0028] Figure 3B Schematic diagram of dentinal tubules in the brushing area of ​​teeth brushed with the toothpaste sample of Example 3. DETAILED DESCRIPTION

[0029] The present application is described in detail below in conjunction with the described embodiments. Although specific embodiments of the present application are shown, it should be understood that the present application can be implemented in various forms and should not be limited by the embodiments set forth herein. On the contrary, these embodiments are provided to enable a more thorough understanding of the present application and to enable the scope of the present application to be fully communicated to those skilled in the art.

[0030] It should be noted that certain words are used in the specification and claims to refer to specific components. Those skilled in the art should understand that technicians may use different nouns to refer to the same component. This specification and claims do not use the difference in nouns as a way to distinguish components, but use the functional differences of components as the criterion for distinction. As mentioned throughout the specification and claims, "including" or "comprising" are open-ended terms and should be interpreted as "including but not limited to". The subsequent description of the specification is a preferred embodiment of the present application, but the description is based on the general principles of the specification and is not intended to limit the scope of the present application. The scope of protection of the present application shall be determined by the attached claims.

[0031] The present application provides an oral composition comprising the following components:

[0032] (a) at least one type of silica particles; and

[0033] (b) at least one chondroitin sulfate,

[0034] The mass ratio of the component (a) to the component (b) is greater than 1;

[0035] The molecular weight of the component (b) is above 8 kDa.

[0036] In some embodiments, the component (a) is ≥ 10% by mass in the composition, preferably 10-50%.

[0037] For example, the component (a) can be 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, etc., in terms of mass percentage in the composition.

[0038] In some embodiments, the component (b) is ≥ 0.8% by mass in the composition, preferably 0.8-5%.

[0039] For example, in terms of mass percentage in the composition, the component (b) can be 0.8%, 0.9%, 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, 5.5%, 6%, etc.

[0040] In some embodiments, the mass ratio of the component (a) to the component (b) is 5-30:1.

[0041] For example, the mass ratio (m) of the component (a) to the component (b) is 二氧化硅 :m 硫酸软骨素 ) can be 2:1, 3:1, 4:1, 5:1, 6:1, 7:1, 8:1, 9:1, 10:1, 11:1, 12:1, 13:1, 14:1, 15:1, 16:1, 17:1, 18:1, 19:1, 20:1, 21:1, 22:1, 23:1, 24:1, 25:1, 26:1, 27:1, 28:1, 29:1, 30:1, 31:1, 35:1, 40:1, etc.

[0042] In some embodiments, the molecular weight of the component (b) is 8k-40kDa, preferably 10k-30kDa.

[0043] For example, the molecular weight of the component (b) may be 8 kDa, 9 kDa, 10 kDa, 15 kDa, 20 kDa, 25 kDa, 30 kDa, 35 kDa, 40 kDa, etc.

[0044] In the present application, the molecular weight of the component (b) refers to the weight average molecular weight of chondroitin sulfate.

[0045] The weight average molecular weight is the statistical average molecular weight by mass, which is the molecular weight averaged over a unit weight and can be measured by conventional measurement methods in the art, such as high performance liquid chromatography (HPLC), gel permeation chromatography (GPC), light scattering, and the like.

[0046] In the present application, the silica suitable for achieving the effect of preventing / alleviating tooth sensitivity is at least hydrophilic.

[0047] In the present application, the component (a) can be selected from silicon dioxide particles suitable for oral cavity.

[0048] In some specific embodiments, the median particle size (D50) of the silica particles is 6-280 μm, for example, 6 μm, 7 μm, 8 μm, 9 μm, 10 μm, 11 μm, 12 μm, 13 μm, 14 μm, 15 μm, 16 μm, 10 μm, 20 μm, 30 μm, 40 μm, 50 μm, 60 μm, 70 μm, 80 μm, 90 μm, 100 μm, 110 μm, 120 μm, 130 μm, 140 μm, 150 μm, 160 μm, 100 μm, 200 μm, 300 μm, 400 μm, 500 μm, 600 μm, 700 μm, 800 μm, 8 0μm, 90μm, 100μm, 110μm, 120μm, 130μm, 140μm, 150μm, 160μm, 170μm, 180μm, 1 90μm, 200μm, 210μm, 220μm, 230μm, 240μm, 250μm, 260μm, 270μm, 275μm, 280μm.

[0049] The median particle size refers to the particle size corresponding to when the cumulative particle size distribution percentage of a sample reaches 50%, and can be measured by conventional measurement methods in the art, such as laser method, sieving method, sedimentation method, etc.

[0050] The composition described in the present application can effectively seal the dentinal tubules after acting on the teeth, thereby achieving the effect of quickly alleviating tooth sensitivity.

[0051] In some embodiments, the composition further comprises one or more orally acceptable carriers.

[0052] In some embodiments, the composition may further include fluoride ions, a pH adjuster, a thickener, an abrasive, a wetting agent, a foaming agent, and the like.

[0053] As the fluoride ion, as the anti-caries agent, for example, sodium fluoride, potassium fluoride, sodium monofluorophosphate, etc. can be mentioned.

[0054] Examples of pH adjusters include organic acids or bases derived from nature or obtained by microbial fermentation or chemical synthesis, such as tartaric acid, lactic acid, hydrochloric acid, calcium hydroxide, potassium hydroxide, sodium bicarbonate, and the like.

[0055] As the thickener, the particles are exemplified, for example, xanthan gum, gum arabic, carrageenan, carboxymethyl cellulose, hydroxypropyl cellulose, starch, modified starch and the like.

[0056] Examples of the abrasive include calcium carbonate, calcium pyrophosphate, abrasive precipitated silica, abrasive silica gel and other silica, calcium silicate, aluminum silicate, aluminum oxide, aluminum hydroxide, alumina, zeolite, titanium oxide, and zirconium silicate.

[0057] Examples of the wetting agent include glycerin, polyethylene glycol, sorbitol, xylitol, ethylene glycol, 1,3-butylene glycol, and propylene glycol;

[0058] As the bubbling agent, there can be mentioned, for example, sodium lauryl sulfate, lauroyl sarcosine, etc.;

[0059] Flavors, flavoring agents, sweeteners, coloring agents, etc. may also be added.

[0060] The composition described in the present application can make the closure rate of dentinal tubules above 50% or even above 90% after brushing for 3 minutes, indicating that the dentinal tubules can be greatly improved in a relatively short period of time, thereby achieving the effect of quickly alleviating and repairing tooth sensitivity.

[0061] The present application provides use of the above-mentioned composition in preparing a product for sealing dentinal tubules.

[0062] Dentin is a hard tissue that constitutes the main body of teeth. It is located in the inner layer of enamel and cementum, and is also the side wall of the pulp cavity and root canal. It is light yellow in color, contains about 30% organic matter and water, 70% inorganic matter, and has a lower hardness than enamel. If observed under a microscope, it can be seen that there are many regularly arranged thin tubes in the dentin, called dentinal tubules, which contain nerve fibers. When the dentin is exposed, it can sense external stimuli such as cold, heat, acid, and sweet, causing pain. Therefore, sealing the dentinal tubules can isolate external stimuli such as cold, heat, acid, and sweet, and prevent / relieve tooth sensitivity.

[0063] The present application provides use of the above-mentioned composition in preparing a product for preventing / alleviating tooth sensitivity.

[0064] Regarding the product for sealing the dentinal tubules, the present application does not impose any restriction on its type, as long as it has the function of sealing the dentinal tubules.

[0065] In some embodiments, the product is a tooth cleaning product, including toothpaste, tooth powder or tooth gel.

[0066] The present application provides the use of at least one silicon dioxide and at least one chondroitin sulfate in preparing a product for sealing dentin tubules, wherein the mass ratio of the silicon dioxide to the chondroitin sulfate is greater than 1, and the molecular weight of the chondroitin sulfate is greater than 8 kDa.

[0067] In some embodiments, the molecular weight of the chondroitin sulfate is 8k-40kDa.

[0068] In some embodiments, the molecular weight of the chondroitin sulfate is 10k-30kDa.

[0069] In some embodiments, the concentration of silica in the product for sealing dentin tubules is ≥ 10%.

[0070] In some embodiments, the concentration of silica in the product for sealing dentin tubules is 10-50 wt %.

[0071] In some embodiments, the chondroitin sulfate is present in a concentration of ≥ 0.8% in the product for sealing dentin tubules.

[0072] In some embodiments, the concentration of chondroitin sulfate in the product for sealing dentinal tubules is 0.8-5 wt %.

[0073] In some embodiments, the mass ratio of the silicon dioxide to the chondroitin sulfate is 5-30:1.

[0074] The present application provides the use of silicon dioxide and chondroitin sulfate in preparing a product for preventing / alleviating tooth sensitivity.

[0075] The description and definition of silicon dioxide and chondroitin sulfate are as described above.

[0076] Example

[0077] The present application provides a general and / or specific description of the materials and test methods used in the experiments. In the following examples, unless otherwise specified, % represents wt%, i.e., weight percentage. The reagents or instruments used without indicating the manufacturer are all conventional reagent products that can be obtained commercially. The materials and equipment used in the embodiments, comparative examples, and experimental examples are shown in Tables 1 and 2.

[0078] Table 1

[0079]

[0080]

[0081] Table 2

[0082] name model factory Ion sputtering instrument ETD-2000 Boyuan Micro-Nano Scanning electron microscopy EM-30 Beijing OPTON Optical Technology Co., Ltd. Toothbrush L8 Shanghai Toothpaste Factory Paste Making Machine ESCO Labor AG-EL3-pm ESCO-Labor AG Light Curing Machine LY-A180 Foshan Nanhai Liangya Dental Equipment Co., Ltd.

[0083] Example 1-11 Preparation method of toothpaste sample

[0084] Premixing of grinding phase: Put the silicon dioxide particles into the powder bin, stir and shake to form the grinding phase for later use;

[0085] Premixing of aqueous phase: Add chondroitin sulfate to pre-measured deionized water and stir until completely dissolved to form an aqueous phase for later use;

[0086] Premixing of hydrophilic colloid: Add carrageenan and xanthan gum to glycerin in sequence, stir and disperse evenly to form a hydrophilic colloid phase for later use;

[0087] Premixing of flavors: Add BIO-201 bioglycolipid into the flavors according to the formula, stir and disperse to form a flavor phase for later use;

[0088] Paste preparation process: add sorbitol to the water phase, stir and homogenize until mixed evenly; add the grinding phase, evacuate the vacuum, and stir and homogenize until mixed evenly; add the hydrophilic colloid phase, evacuate the vacuum, and stir and homogenize until mixed evenly; add the flavor phase, evacuate the vacuum, and stir and homogenize until mixed evenly; after degassing, inspect and verify that the internal control standards are met before discharging to obtain a toothpaste sample, wherein the contents of various ingredients are shown in Table 3.

[0089] Comparative Examples 1-6

[0090] The preparation was carried out in the same manner as in Example 1-11, except that the contents of the components were different. The contents of the various components are shown in Table 3.

[0091] Table 1

[0092]

[0093]

[0094]

[0095] Experimental example

[0096] (1) Pretreatment of cattle teeth:

[0097] Take the prepared bovine tooth slices, place them in a pre-sterilized beaker, add deionized water to cover them, soak for 10 minutes, pour out the deionized water, and repeat the operation 3 times;

[0098] Prepare a 10% phosphoric acid solution as a tooth treatment solution;

[0099] The bovine teeth were immersed in the tooth treatment solution for 15 min, then taken out, rinsed with deionized water, and then immersed in deionized water for 10 min before being taken out;

[0100] The tooth samples were placed in an environment of 25°C and 5% relative humidity (RH) for drying for 6 h;

[0101] A protective layer of light-curable resin was applied on the surface of half of the bovine tooth and cured using a light-curing machine to maintain the original morphology of the exposed tubules in this part as a comparison area.

[0102] (2) Toothbrushing test method

[0103] Take 80g of the toothpaste samples of the embodiment and the comparative example, add 40g of oral simulated fluid (modified SBF simulated body fluid, m-SBF) and 40g of deionized water, stir and disperse evenly to form toothpaste slurry for standby use; place the toothbrush in deionized water and soak it for 30min for standby use;

[0104] like Figure 1As shown in the figure (wherein 1 is an acrylic plate, 2 is a bovine tooth slice sample, 3 is a toothbrush machine holder, 4 is a standard toothbrush, 5 is a brush cup, 6 is a toothpaste slurry liquid surface, and 7 is a firmly fixed acrylic plate), the tooth sample is fixed on the acrylic plate 1, and then the acrylic plate 1 is placed in the toothbrush machine, and the toothbrush 4 is fixed on the toothbrush machine;

[0105] Inject toothpaste slurry into the brush cup 5 of the toothbrush machine, and adjust the height of the brush cup to ensure that the slurry can completely immerse the teeth and the toothbrush head;

[0106] Start the toothbrushing process and set the time to 3 minutes. After brushing, take out the teeth, rinse them with deionized water, and let them air dry naturally;

[0107] Finally, the photocurable resin protective layer of the tooth contrast area was removed, and the tooth samples were gold-sprayed using an ion sputtering instrument. The number and distribution of dentinal tubules were then observed using a scanning electron microscope, and the closure rate of dentinal tubules was calculated based on the following formula;

[0108] Dentin tubule closure rate = abs (1-total area of ​​dentinal tubules in the brushing area / total area of ​​dentinal tubules in the control area) * 100%, where *abs represents absolute value. The results are shown in Table 4;

[0109] In addition, the dentinal tubules after brushing with the toothpaste samples of Example 1 and Example 3 were photographed using a scanning electron microscope and compared with the control area. The results are as follows: Figure 2A-2B and as shown in 3A-3B.

[0110] Table 4 Closure rate of small holes

[0111] Case Dentin tubule closure rate Example-1 90％ Example-2 95％ Example-3 95％ Example-4 100％ Example-5 100％ Example-6 95％ Example-7 90％ Example-8 50％ Example-9 55％ Example-10 55％ Example-11 50％ Comparative Example-1 2％ Comparative Example-2 3％ Comparative Example-3 30％ Comparative Example-4 20％ Comparative Example-5 6％ Comparative Example-6 4％

[0112] from Figure 2A-2B , 3A-3B and Table 4 show that, by using the composition described in the present application, the closure rate can reach more than 50%, or even more than 90% after brushing for 3 minutes, which can greatly improve the closure rate of dentinal tubules in the short term, thereby achieving the effect of quickly alleviating and repairing tooth sensitivity.

[0113] The above is only the preferred embodiment of the present application, and does not limit the present application in other forms. Any technician familiar with the profession may use the above disclosed technical content to change or modify it into an equivalent embodiment with equivalent changes. However, any simple modification, equivalent change and modification made to the above embodiment based on the technical essence of the present application without departing from the technical solution of the present application still falls within the protection scope of the technical solution of the present application.

Claims

1. An oral composition comprising the following components: (a) at least one type of silica particles; and (b) at least one chondroitin sulfate, The mass ratio of the component (a) to the component (b) is greater than 1; The molecular weight of the component (b) is above 8 kDa.

2. The composition according to claim 1, wherein Calculated by mass percentage in the composition, the component (a) is ≥ 10%, preferably 10-50%.

3. The composition according to claim 1 or 2, wherein The molecular weight of the component (b) is 8k-40kDa.

4. The composition according to any one of claims 1 to 3, wherein Calculated by mass percentage in the composition, the component (b) is ≥ 0.8%.

5. The composition according to any one of claims 1 to 3, wherein Calculated by mass percentage in the composition, the component (b) is 0.8-5%.

6. The composition according to claim 1, wherein The mass ratio of the component (a) to the component (b) is 5-30:

1.

7. The composition of any one of claims 1-6, further comprising one or more orally acceptable carriers.

8. Use of the composition according to any one of claims 1 to 7 in preparing a product for sealing dentinal tubules.

9. Use of the composition according to any one of claims 1 to 7 in preparing a product for preventing / alleviating tooth sensitivity.

10. The use according to claim 8 or 9, wherein the product is a tooth cleaning product.

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