Oral care compositions, oral care products comprising stannous fluoride

Abstract

The application belongs to the technical field of oral care products, and particularly relates to a fluoride stannous fluoride-containing oral care composition and oral care product, which comprises the following components in parts by mass: a fluoride ion source of not more than 0.15 parts, a stannous salt of 0.2-0.8 parts, a nitrate of 1-10 parts, a stabilizing regulator of 2-6 parts, a buffer system of 1-5 parts, and a thickening agent of 0.1-0.5 parts; wherein the stabilizing regulator is any one or a combination of multiple of pyrophosphate, polyphosphate, poly-metaphosphate and phytate; and the buffer system is citric acid and / or soluble citrate.

Description

Technical Field

[0001] This invention belongs to the field of oral care product technology, specifically relating to an oral care composition containing stannous fluoride and an oral care product. Background Technology

[0002] Stannous fluoride (SnF2) is a widely recognized and highly effective oral care ingredient. Unlike other common fluoride ingredients such as sodium fluoride, it not only prevents cavities but also provides a range of oral health benefits.

[0003] While stannous fluoride (SnF2) is highly effective, it is extremely unstable. The "stannous" in stannous fluoride refers to divalent tin ions (Sn). 2+ This is the core active ingredient that exerts its antibacterial, anti-allergic, and anti-moth effects. However, Sn 2+ It is highly reactive and readily oxidized by oxygen in the air to form tetravalent tin ions (Sn). 4+ ); divalent tin ions (Sn) 2+ Once it becomes tetravalent tin, it loses its biological activity and can no longer inhibit bacteria or seal dentinal tubules, becoming just a regular tin salt and losing the core function of toothpaste.

[0004] Furthermore, stannous fluoride readily undergoes hydrolysis when dissolved in water, forming insoluble stannous hydroxide or basic salts. This can lead to white precipitates or crystals in toothpaste, affecting not only its appearance but also reducing the concentration of the active ingredient. Lower moisture content, to some extent, promotes the stability of stannous fluoride and prevents hydrolysis.

[0005] Existing patent CN107530240A points out that a "low-moisture composition" based on calcium pyrophosphate abrasive gives the stannous and fluoride in the composition better long-term stability and oral bioavailability. However, the limitation of its moisture content being less than 1% makes it extremely limited. Moreover, the formulation will suffer a considerable loss of fluoride at a moisture content of 10%, so it cannot be used in actual oral care products.

[0006] Therefore, overcoming the poor stability of stannous fluoride in oral care products with high moisture content is a technical problem that urgently needs to be solved in this field.

[0007] It should be noted that the information disclosed in this background section is only for understanding the background technology of the present application concept, and therefore, the above description is not considered to constitute prior art information. Summary of the Invention

[0008] This disclosure provides at least one oral care composition and oral care product containing stannous fluoride.

[0009] In a first aspect, embodiments of this disclosure provide an oral care composition comprising, by weight, the following components: no more than 0.15 parts of fluoride ion source, 0.2 to 0.8 parts of stannous salt, 1 to 10 parts of nitrate, 2 to 6 parts of stabilizer, 1 to 5 parts of buffer system, and 0.1 to 0.5 parts of thickener; wherein the stabilizer is any one or a combination of pyrophosphate, polyphosphate, polymetaphosphate, and phytate; and the buffer system is citric acid and / or soluble citrate.

[0010] In one alternative embodiment, the fluoride ion source includes any one or more combinations of sodium fluoride, sodium monofluorophosphate, stannous fluoride, ammonium fluoride, and olafluridine.

[0011] In one alternative embodiment, the stannous salt includes any one or a combination of stannous fluoride, stannous chloride, stannous sulfate, and stannous nitrate.

[0012] In one alternative embodiment, the nitrate includes any one or more combinations of zinc nitrate, potassium nitrate, sodium nitrate, copper nitrate, calcium nitrate, ammonium nitrate, and silver nitrate.

[0013] In one alternative embodiment, the thickener is carbomer.

[0014] Secondly, this disclosure also provides an oral care product, which is toothpaste with a pH value of 5.5-7.0, comprising the following components by mass: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, 30-80 parts of polyol, 0.2-1.0 parts of toothpaste thickener, 0.01-5 parts of sweetener, 10-30 parts of abrasive, 1-5 parts of surfactant, 0.5-2 parts of fragrance, and 5-20 parts of water.

[0015] Thirdly, this disclosure provides an oral care product, which is a mouthwash with a pH value of 5.5-7.0, comprising the following components by weight: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, 1-10 parts of polyol, 0.01-1 part of sweetener, 0.1-2 parts of surfactant, 0.05-0.2 parts of flavoring, and 85-95 parts of water.

[0016] Fourthly, this disclosure provides an oral care product, which is a mouth spray with a pH value of 5.5-7.0, and comprises the following components by weight: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, 1-10 parts of polyol, 0.01-1 part of sweetener, 0.1-2 parts of surfactant, 0.05-0.2 parts of fragrance, and 85-95 parts of water.

[0017] Fifthly, this disclosure provides an oral care product, which is a mousse with a pH of 5.5-7.0, comprising the following components by weight: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, 1-10 parts of polyol, 0.01-1 part of sweetener, 0.1-2 parts of surfactant, 0.05-0.2 parts of flavoring, and 85-95 parts of water.

[0018] Sixthly, this disclosure provides an oral care product, which is tooth powder with a pH value of 5.5-7.0, and comprises the following components by mass: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, and 50-80 parts of silica.

[0019] The beneficial effects of this invention are that the oral care composition and oral care product containing fluorinated stannous salt, through the setting of a six-component system of "thickener-fluoride ion source-stannous salt-nitrate-stabilizer-buffer system", on the one hand, utilizes the negative charge of the stabilizer to form a soluble complex with stannous ions, encapsulating the stannous ions in the molecular chain to isolate them from oxygen. On the other hand, the buffer system and nitrate are combined to protect the environment in which the stannous ions are located, so as to balance the negative impact of the metal ion free performance brought by the stabilizer. Thus, the stability of stannous salt in oral care products with high moisture content is achieved, and the bioavailability of stannous salt during product use is improved through the bioadhesive properties of the thickener.

[0020] Existing stannous fluoride toothpastes control the water content (≤1%) to keep the stannous fluoride in a low-water or anhydrous environment, thus preventing hydrolysis and ensuring its stability; however, oxidation can still occur. This stannous fluoride oral care composition and product, through its hexa-component system, allows stannous fluoride to be used in conventional aqueous toothpaste systems with a water content ≥10%. This not only prevents hydrolysis of the stannous fluoride but also avoids oxidation due to the hexa-component system structure. Compared to conventional low-water-content stannous fluoride toothpastes, this design better guarantees the stability and effectiveness of the stannous fluoride.

[0021] Other features and advantages of the invention will be set forth in the following description, and will be apparent in part from the description, or may be learned by practicing the invention. The objects and other advantages of the invention are realized and obtained through the structures particularly pointed out in the description and the drawings.

[0022] To make the above-mentioned objects, features and advantages of the present invention more apparent and understandable, preferred embodiments are described below in detail with reference to the accompanying drawings. Attached Figure Description

[0023] To more clearly illustrate the specific embodiments of the present invention or the technical solutions in the prior art, the drawings used in the description of the specific embodiments or the prior art will be briefly introduced below. Obviously, the drawings described below are some embodiments of the present invention. For those skilled in the art, other drawings can be obtained from these drawings without creative effort.

[0024] Figure 1 A precipitation diagram of solution 1 in scheme group 1 provided in the embodiments of this disclosure; Figure 2 The precipitation diagram is shown for solution 2 in scheme group 1 provided in the embodiments of this disclosure. Detailed Implementation

[0025] To make the objectives, technical solutions, and advantages of the embodiments of the present invention clearer, the technical solutions of the present invention will be clearly and completely described below with reference to the accompanying drawings. Obviously, the described embodiments are only some embodiments of the present invention, not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention.

[0026] As used herein, the phrases “in one embodiment,” “according to one embodiment,” “in some embodiments,” etc., generally refer to the fact that a particular feature, structure, or characteristic following the phrase can be included in at least one embodiment of this disclosure. Therefore, a particular feature, structure, or characteristic can be included in more than one embodiment of this disclosure, such that these phrases do not necessarily refer to the same embodiment. As used herein, the terms “example,” “exemplary,” etc., are used to “serve as an example, instance, or illustration.” Any implementation, aspect, or design described herein as “example” or “exemplary” is not necessarily to be construed as preferred or superior to other implementations, aspects, or designs. Rather, the use of the terms “example,” “exemplary,” etc., is intended to present concepts in a specific manner.

[0027] The following detailed description of some embodiments of the present invention is provided in conjunction with the accompanying drawings. Unless otherwise specified, the following embodiments and features can be combined with each other.

[0028] This disclosure provides an oral care composition comprising, by weight, the following components: no more than 0.15 parts of fluoride ion source, 0.2 to 0.8 parts of stannous salt, 1 to 10 parts of nitrate, 2 to 6 parts of stabilizer, 1 to 5 parts of buffer system, and 0.1 to 0.5 parts of thickener; wherein the stabilizer is any one or a combination of pyrophosphate, polyphosphate, polymetaphosphate, and phytate; and the buffer system is citric acid and / or soluble citrate.

[0029] Specifically, the citrate is a soluble citrate. Zinc citrate is commonly used in oral care products as a functional ingredient for gum care, improving the oral environment through the antibacterial effect of zinc ions. However, it is only slightly soluble in water, with a solubility of 2.6 g / L, limiting its use as a pH adjuster. The citrate used as a pH adjuster in this invention refers to sodium citrate or potassium citrate, which are highly soluble in water.

[0030] In some embodiments, specifically, the fluoride ion source includes any one or more combinations of sodium fluoride, sodium monofluorophosphate, stannous fluoride, ammonium fluoride, and olafluridine.

[0031] In some embodiments, specifically, the stannous salt includes any one or more combinations of stannous fluoride, stannous chloride, stannous sulfate, and stannous nitrate.

[0032] In some embodiments, specifically, the nitrate includes any one or more combinations of zinc nitrate, potassium nitrate, sodium nitrate, copper nitrate, calcium nitrate, ammonium nitrate, and silver nitrate.

[0033] In some embodiments, specifically, the thickener is carbomer.

[0034] Secondly, this disclosure also provides an oral care product, which is toothpaste with a pH value of 5.5-7.0, comprising the following components by mass: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, 30-80 parts of polyol, 0.2-1.0 parts of toothpaste thickener, 0.01-5 parts of sweetener, 10-30 parts of abrasive, 1-5 parts of surfactant, 0.5-2 parts of fragrance, and 5-20 parts of water.

[0035] Thirdly, this disclosure provides an oral care product, which is a mouthwash with a pH value of 5.5-7.0, comprising the following components by weight: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, 1-10 parts of polyol, 0.01-1 part of sweetener, 0.1-2 parts of surfactant, 0.05-0.2 parts of flavoring, and 85-95 parts of water.

[0036] Fourthly, this disclosure provides an oral care product, which is a mouth spray with a pH value of 5.5-7.0, and comprises the following components by weight: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, 1-10 parts of polyol, 0.01-1 part of sweetener, 0.1-2 parts of surfactant, 0.05-0.2 parts of fragrance, and 85-95 parts of water.

[0037] Fifthly, this disclosure provides an oral care product, which is a mousse with a pH of 5.5-7.0, comprising the following components by weight: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, 1-10 parts of polyol, 0.01-1 part of sweetener, 0.1-2 parts of surfactant, 0.05-0.2 parts of flavoring, and 85-95 parts of water.

[0038] The sixth invention, according to an embodiment of this disclosure, provides an oral care product, which is tooth powder with a pH value of 5.5-7.0, and comprises the following components by mass: no more than 0.15 parts of fluoride ion source, 0.2-0.8 parts of stannous salt, 1-10 parts of nitrate, 2-6 parts of stabilizer, 1-5 parts of buffer system, 0.1-0.5 parts of thickener, and 50-80 parts of silica.

[0039] Scheme Group 1: Stability test of stannous aqueous solution, the formulations of the examples are shown in Table 1 below: Table 1

[0040] Solution preparation method: Step 1: Add the fluoride ion source, nitrate, stabilizer, buffer system, pH adjuster, and other ingredients to the aqueous solution in sequence, and stir to mix thoroughly; Step 2: Add the tin oxide source to the mixed solution and stir until well mixed.

[0041] Performance Test 1: Stability Test The initial state of the solution and its properties after being placed at 50℃ for 3 months were observed. The stability test results are shown in Table 2 below: Table 2

[0042] Performance Test 2: Quantitative Test of Stannous Ions The quantitative test results of stannous ions in the aged samples (50℃ for 3 months) are shown in Table 3 below: Table 3

[0043] Specifically, as can be seen from the data of scheme group 1, both solutions 14 and 15, whether in stability testing (both exhibiting colorless and transparent liquid state) or quantitative detection of tin ions (greater than 80%), demonstrate that solutions 14 and 15 can keep tin ions in a stable state, which is the preferred scheme of the present invention.

[0044] Please see Figure 1 The stannous fluoride aqueous solution in Solution 1 does not appear as a colorless and transparent solution; instead, it is slightly turbid and cloudy, which is largely due to the instability of stannous ions. 2+ Tin is a strong reducing agent and is easily oxidized in air or when exposed to oxidizing agents, gradually transforming into tetravalent tin (Sn). 4+ Stannous crystals or their aqueous solutions can absorb oxygen from the air and undergo oxidation. Hydrolysis produces insoluble basic salt precipitates, such as basic stannous chloride or oxychloride, causing the solution to become cloudy. After an aging test at 50°C for 3 months, oxidation occurred, and a dark yellow precipitate appeared at the bottom of the stannous fluoride aqueous solution, along with dark yellow exudates on the beaker walls. However, the upper layer of solution remained colorless and transparent, indicating that stannous ions were almost completely oxidized at high temperatures, forming an insoluble precipitate, and that stannous ions are virtually inactive.

[0045] Because stannous fluoride aqueous solution is highly acidic (pH=2), direct use may lead to acid etching and demineralization of tooth enamel. Solutions 2, 3, and 4 were prepared by adjusting the pH of the stannous fluoride solution with sodium hydroxide, trisodium phosphate, and arginine, respectively. The initial samples all showed abnormalities. Please refer to [link / reference needed]. Figure 2 Sodium hydroxide and trisodium phosphate both react with stannous ions to form white precipitates. Arginine and stannous fluoride present as emulsions, which, after standing overnight, develop into white precipitates. After aging tests, the white precipitate in solution 2 further reacts to form a yellow precipitate, namely stannous ions (Sn). 2+ Further oxidation occurs. The white precipitate formed by trisodium phosphate and stannous fluoride is relatively stable, but the insoluble stannous ions greatly reduce their free activity, thus losing their stannous activity and product efficacy. Arginine itself undergoes unstable reactions such as discoloration at high temperatures; as observed in the test, the white precipitate gradually turns gray, further illustrating the instability of the product formed by the reaction of stannous fluoride and arginine. Therefore, sodium hydroxide, trisodium phosphate, and arginine are all detrimental to the stability of stannous ions and are incompatible with them.

[0046] When only nitrates are used, as in solution 6, instability is observed in both the initial and aged states, manifesting as precipitation and discoloration. This indicates that nitrates alone cannot resolve the instability of stannous fluoride. However, while solutions 8 and 9 were colorless and transparent during stability tests, their stannous content was significantly lower (below 50%) compared to the preferred solutions 14 and 15 in this experimental group. This suggests that nitrates can, to some extent, address the instability of stannous ions or contribute to improving their stability.

[0047] Sodium gluconate is a chelating agent that can react with stannous ions (Sn) in stannous fluoride. 2+ This forms a stable complex that effectively protects tin ions from hydrolysis and oxidation into inactive tetravalent tin (Sn). 4+ However, a comparison of solutions 5, 7, 15, and 16 shows that using only sodium gluconate (solution 5) or the sodium gluconate and nitrate combination (solution 7) cannot solve the stability problem of stannous fluoride. This suggests that the stability of the complex formed by gluconate chelating stannous fluoride is limited, and stannous ions are still susceptible to oxidation at high temperatures. Solution 15, as the preferred solution in this experimental group, was used to detect the stannous content (Sn). 2+ (≥80%). Compared with solution 16, sodium gluconate provides little or no help to the stability of stannous compounds, or in the case of solution 15, the effect of sodium gluconate is limited, meaning that the system formed by nitrate, stabilizer, and buffer is sufficient to address the stability of stannous compounds.

[0048] Comparison of solutions 10 and 11 with the preferred solutions 14 and 15 of this experimental group shows that, although solutions 10 and 11 pass stability tests and exhibit colorless and transparent appearance after aging tests, the tin content (Sn) is significantly lower when citrate buffer system (solution 10) and phosphate stabilizer (solution 11) are lacking. 2+ The low / % test result further illustrates the importance and beneficial effects of the buffer system and phosphate stabilizer on this invention.

[0049] In this experimental group, solutions 12 and 13 were used to verify the effect of zinc lactate on the stability of stannous metals. Solution 12 showed a white precipitate, which was analyzed to be due to the metathesis reaction between pentasodium tripolyphosphate and zinc, forming a poorly soluble zinc tripolyphosphate precipitate. This precipitate consumed the pentasodium tripolyphosphate used to stabilize stannous metals and reduced the effectiveness of the zinc salt, inevitably affecting the stability of stannous metals. When the pentasodium tripolyphosphate was removed, although solution 13 passed the stability test, its stannous metal content was low, further demonstrating the importance of the stability provided by pentasodium tripolyphosphate for stabilizing stannous metals.

[0050] Polyphosphates are polymeric dielectrics whose molecular chains carry a large number of negative charges, enabling them to react with stannous ions (Sn). 2+ This forms a soluble complex. This complexation "encapsulates" the stannous ion within the phosphate chain, creating a protective barrier that effectively blocks contact between oxygen and the stannous ion, thereby inhibiting Sn... 2+ To Sn 4+ The oxidation reaction of stannous ions is a concern. While pentasodium tripolyphosphate can chelate stannous ions and improve their stability, it also significantly alters the free properties of metal ions, drastically reducing their free concentration and thus inhibiting or changing their original stannous ion properties. Therefore, additional methods are needed to "control" the chelation performance. Solutions 14 and 15 are the preferred solutions for this experimental group. The chelating properties of pyrophosphate and the buffer environment provided by the buffer system can form a stable structure of "fluorine-stannous-nitrate-polyphosphate / pyrophosphate-citrate," which can protect stannous ions, greatly reducing their oxidation potential, and easily releasing them to ensure their free state. When stannous ions are stable and remain in a free state, their effectiveness is maximized.

[0051] Option Group 2: Application of stable oral care compositions in toothpaste. Examples of formulations are shown in Table 4 below. Table 4

[0052] Toothpaste preparation method: Step 1: Add water, humectant, and sweetener to the pot and stir to mix well; Step 2: Add the fluoride ion source, nitrate, stabilizer and buffer system to the pot in sequence, stir and mix evenly to ensure complete dissolution.

[0053] Step 3: Add the tin oxide source to the pot, stir and mix well to ensure complete dissolution.

[0054] Step 4: After mixing the abrasive and thickener evenly, add them to the pot and stir until well mixed.

[0055] Step 5: Add surfactants and flavorings to the pot and stir to mix evenly.

[0056] Step 6: Add the pH adjuster to the pot and stir until well mixed.

[0057] Performance Test 1: Stability Test Observe the initial state of the toothpaste, and its properties after being stored at 5℃, 25℃, and 45℃ for 3 months.

[0058] The stability test results are shown in Table 5 below: Table 5

[0059] Performance Test 2: Quantitative Test of Stannous Ions The quantitative test results of stannous ions in the stability samples are shown in Table 6 below: Table 6

[0060] Specifically, as can be seen from the above performance test results: When the present invention was applied to toothpaste, in Comparative Example 1, which used only stannous fluoride, the stannous fluoride hydrolyzed to form an insoluble basic salt precipitate, resulting in a decrease in the transparency of the initial sample. As the stability decreased, the oxidation reaction continued to occur, and the paste eventually turned significantly yellow, indicating that the stannous fluoride was significantly deactivated.

[0061] When sodium hydroxide (Comparative Example 2), trisodium phosphate (Comparative Example 3), and arginine (Comparative Example 4) were used to adjust the pH, various stability issues arose. For example, precipitation or crystallization led to reduced product transparency. In Comparative Example 3, after 24 hours of standing, the paste showed clearly visible white precipitates or crystals, indicating that phosphate ions combined with stannous ions to form insoluble precipitates that agglomerated, resulting in visible white particles. This confirmed the inadequacy of the proposed method. In Comparative Example 4, arginine naturally turns yellow at high temperatures; therefore, under this method, after 3 months at 45℃, the paste showed significant yellowing and a considerable change in odor, making it unsuitable for the final product.

[0062] When nitrates (Comparative Example 5), buffer systems (Comparative Example 6), and stabilizers (Comparative Example 7) were absent, the stability test results of Comparative Example 5 were relatively ideal, but its stannous content was significantly lower, with a decrease rate of over 50%. This is as described in Scheme Group 1: pyrophosphates and gluconates, which also possess chelating abilities, differ in their chelating capacity, leading to differences in stannous stability. Furthermore, when the formed chelate is too stable, it affects the free state of stannous ions, thus affecting the detection amount. Comparative Examples 6 and 7 both exhibited discoloration. The stannous content in all three comparative examples decreased by more than 50% after 3 months at 45℃, indicating a significantly high loss of stannous ions.

[0063] In Examples 1 and 2, the products remained stable at high temperatures (45°C for 3 months), without yellowing or graying. Although the stability of stannous ions decreased, it was still controlled to over 80%. This further verifies the stability of the oral care composition of the present invention. The stable structure formed by "fluorine-stannous-nitrate-polyphosphate / pyrophosphate-citrate" protects stannous ions, greatly reducing their oxidation potential, while also facilitating the release of stannous ions, ensuring their free state and thus guaranteeing product efficacy.

[0064] Scheme Group 3: Biotransmission effect of stannous ions.

[0065] Specifically, bioadhesion refers to the binding state between natural or synthetic materials and the surface of biological tissues (such as mucous membranes or skin) through physical or chemical interactions. In the field of drug and active ingredient delivery, utilizing bioadhesion is a key technology to improve its utilization.

[0066] In the oral cavity, utilizing bioadhesion to improve the utilization of active ingredients aims to address the challenge of rapid loss of drugs or active ingredients due to physiological activities such as continuous saliva rinsing, swallowing, and chewing. Bioadhesion technology can "anchor" active substances to the oral mucosa or tooth surface, thereby significantly prolonging their duration of action, promoting local absorption, and ultimately improving therapeutic efficacy.

[0067] This technology is designed for typical applications such as "oral ulcer repair" and "oral mucosal infection." It increases the retention time of active ingredients on the acquired protein membrane of the oral mucosa or tooth surface, thereby promoting local absorption and penetration through sustained and controlled release to enhance product efficacy. Alternatively, it can provide a more effective active ingredient delivery method, delivering active ingredients more efficiently and effectively to the oral mucosa and tooth enamel hard tissue surfaces.

[0068] This invention addresses the issues of tin stability and increases the content of effective tin components, while also expanding on the bioavailability of tin to maximize product efficacy.

[0069] The formulations for the examples are shown in Table 7 below: Table 7

[0070] Toothpaste preparation method: Step 1: Add water, humectant, and sweetener to the pot and stir to mix well; Step 2: Add the fluoride ion source, nitrate, stabilizer and buffer system to the pot in sequence, stir and mix evenly to ensure complete dissolution.

[0071] Step 3: Add the tin oxide source to the pot, stir and mix well to ensure complete dissolution.

[0072] Step 4: After mixing the abrasive and thickener evenly, add them to the pot and stir until well mixed.

[0073] Step 5: Add surfactants and flavorings to the pot and stir to mix evenly.

[0074] Step 6: Add the pH adjuster to the pot and stir until well mixed.

[0075] Performance Test 1: Stability Test Observe the initial state of the toothpaste, and its properties after being stored at 5℃, 25℃, and 45℃ for 3 months.

[0076] The stability test results are shown in Table 8 below: Table 8

[0077] Performance Test 2: Quantitative Test of Stannous Ions The quantitative test results of stannous ions in the stability samples are shown in Table 9 below:

[0078] Performance Test 3: Bioadhesion Test Test Method: An in vitro oral-esophageal retention (IVOR) model was used to study the mucosal adhesion of samples. The mucosa was attached to a slope, and mouthwash was poured in from top to bottom to simulate the rinsing process. Simulated saliva was then poured in to simulate the flushing process. Finally, the amount of residue on the membrane was collected, and the percentage of active ingredient content was tested to confirm mucosal adhesion. A higher percentage of residue indicates better mucosal adhesion and better retention of active ingredients.

[0079] Evaluation criteria: When the percentage of residue on the membrane is above 15%, the mucosal adhesion function is very good, and the active ingredients are well retained. When the percentage of residue on the membrane is 10-14.99% or higher, the mucosal adhesion function is very good. When the percentage of residue on the membrane is 5.01-9.99% or higher, the mucosal adhesion function is good. When the percentage of residue on the membrane is above 1.00-4.99%, the mucosal adhesion function is average. When the percentage of residue on the membrane is above 0-0.99%, the membrane adhesion function is poor, meaning it is subject to heavy rinsing.

[0080] The results of the in vitro bioadhesion test are shown in Table 10 below:

[0081] The test results above show that the introduction of the thickener carbomer did not significantly affect the stability of the products in Example A and Example B, nor the stability of the active ingredient. However, in the bioadhesion test, Example A was significantly worse than Example B, greatly improving the rinse resistance of the active ingredient in the oral cavity, ensuring its effectiveness, and enhancing its efficacy. We speculate that the possible mechanism is that the stable structure formed by "stannous fluoride-potassium nitrate-pentasodium tripolyphosphate-citrate" can prevent the stannous ions from being hydrolyzed and oxidized, while regulating the release of stannous ions to maintain their free state. Under this premise, the stable structure formed by "carbomer-stannous fluoride-potassium nitrate-pentasodium tripolyphosphate-citrate" enhances the bioavailability of stannous ions, thereby improving the clinical efficacy of the product.

[0082] The present invention provides a stable oral care composition that forms a stable regulatory composition through a "thickener-fluoride ion source-stannous salt-nitrate-stabilizer-buffer system," thereby solving the stability problem of stannous salt and improving its bioavailability.

[0083] Compared to toothpastes with low or anhydrous stannous fluoride, this hexa-component system allows stannous salts to be used in systems with high water content (≥10%), with the following advantages: a. It reduces the high-cost formulation of low-moisture or anhydrous toothpaste, resulting in significant economic benefits; b. It greatly improves the separation problem that easily occurs in low-moisture or anhydrous toothpaste. The separation problem caused by the capillary effect formed between the anhydrous paste and the tube is easy to occur, thus improving the user experience. c. Improved production efficiency: This hexa-element system is used in water-based toothpaste, i.e., conventional toothpaste processes, which can eliminate the problem of high-temperature activation of thickeners in anhydrous toothpaste, thus improving the economic benefits of tin oxide products. d. By setting up this hexa-element control system, the stability of tin in the product during its shelf life can be improved, and the hydrolysis reaction of tin can be avoided during product use, thereby improving the utilization rate of tin.

[0084] In summary, this oral care composition and product containing stannous fluoride utilizes a six-component system consisting of a thickener, a fluoride ion source, a stannous salt, a nitrate, a stabilizer, and a buffer system. On one hand, the negative charge of the stabilizer forms a soluble complex with the stannous ions, encapsulating them within the molecular chain and isolating them from oxygen. On the other hand, the buffer system and nitrate ensure the environmental conditions for the stannous ions, balancing the negative impact of the stabilizer's metal ion ionization properties. This achieves the stability of the stannous salt in oral care products with high moisture content and enhances its bioavailability during product use through the thickener's bioadhesive properties.

[0085] Existing stannous fluoride toothpastes control the water content (≤1%) to keep the stannous fluoride in a low-water or anhydrous environment, thus preventing hydrolysis and ensuring its stability; however, oxidation can still occur. This stannous fluoride oral care composition and product, through its hexa-component system, allows stannous fluoride to be used in conventional aqueous toothpaste systems with a water content ≥10%. This not only prevents hydrolysis of the stannous fluoride but also avoids oxidation due to the hexa-component system structure. Compared to conventional low-water-content stannous fluoride toothpastes, this design better guarantees the stability and effectiveness of the stannous fluoride.

[0086] Based on the above-described preferred embodiments of the present invention, and through the foregoing description, those skilled in the art can make various changes and modifications without departing from the inventive concept. The technical scope of this invention is not limited to the contents of the specification, but must be determined according to the scope of the claims.

Claims

1. An oral care composition, characterized in that, It includes the following components by mass parts: The fluoride ion source is no more than 0.15 parts, stannous salt is 0.2 to 0.8 parts, nitrate is 1 to 10 parts, stabilizer is 2 to 6 parts, buffer system is 1 to 5 parts, and thickener is 0.1 to 0.5 parts; The stabilizer is any one or a combination of pyrophosphate, polyphosphate, polymetaphosphate, and phytate. The buffer system is citric acid and / or soluble citrate.

2. The oral care composition as claimed in claim 1, characterized in that, The fluoride ion source includes any one or more combinations of sodium fluoride, sodium monofluorophosphate, stannous fluoride, ammonium fluoride, and olaf.

3. The oral care composition as claimed in claim 1, characterized in that, The stannous salt includes any one or more combinations of stannous fluoride, stannous chloride, stannous sulfate, and stannous nitrate.

4. The oral care composition as claimed in claim 1, characterized in that, The nitrates include any one or more combinations of zinc nitrate, potassium nitrate, sodium nitrate, copper nitrate, calcium nitrate, ammonium nitrate, and silver nitrate.

5. The oral care composition as claimed in claim 1, characterized in that, The thickener is carbomer.

6. An oral care product, characterized in that, The oral care product is toothpaste with a pH value of 5.5-7.0, and comprises the following components by weight: The following components are present: fluoride ion source not exceeding 0.15 parts, stannous salt 0.2-0.8 parts, nitrate 1-10 parts, stabilizer 2-6 parts, buffer system 1-5 parts, thickener 0.1-0.5 parts, polyol 30-80 parts, toothpaste thickener 0.2-1.0 parts, sweetener 0.01-5 parts, abrasive 10-30 parts, surfactant 1-5 parts, fragrance 0.5-2 parts, and water 5-20 parts.

7. An oral care product, characterized in that, This is a mouthwash with a pH of 5.5-7.0, and contains the following components by weight: The following components are present: fluoride ion source not exceeding 0.15 parts, stannous salt 0.2-0.8 parts, nitrate 1-10 parts, stabilizer 2-6 parts, buffer system 1-5 parts, thickener 0.1-0.5 parts, polyol 1-10 parts, sweetener 0.01-1 parts, surfactant 0.1-2 parts, flavoring 0.05-0.2 parts, and water 85-95 parts.

8. An oral care product, characterized in that, The oral care product is a mouth spray with a pH value of 5.5-7.0, and comprises the following components by weight: The following components are present: fluoride ion source not exceeding 0.15 parts, stannous salt 0.2-0.8 parts, nitrate 1-10 parts, stabilizer 2-6 parts, buffer system 1-5 parts, thickener 0.1-0.5 parts, polyol 1-10 parts, sweetener 0.01-1 parts, surfactant 0.1-2 parts, flavoring 0.05-0.2 parts, and water 85-95 parts.

9. An oral care product, characterized in that, The oral care product is a mousse with a pH of 5.5-7.0, and comprises the following components by weight: The following components are present: fluoride ion source not exceeding 0.15 parts, stannous salt 0.2-0.8 parts, nitrate 1-10 parts, stabilizer 2-6 parts, buffer system 1-5 parts, thickener 0.1-0.5 parts, polyol 1-10 parts, sweetener 0.01-1 parts, surfactant 0.1-2 parts, flavoring 0.05-0.2 parts, and water 85-95 parts.

10. An oral care product, characterized in that, The oral care product is tooth powder with a pH value of 5.5-7.0, and comprises the following components by weight: The fluoride ion source is no more than 0.15 parts, stannous salt is 0.2 to 0.8 parts, nitrate is 1 to 10 parts, stabilizer is 2 to 6 parts, buffer system is 1 to 5 parts, thickener is 0.1 to 0.5 parts, and silica is 50 to 80 parts.

Images