CN112076112A - Oral care composition comprising stabilized stannous ions - Google Patents
Oral care composition comprising stabilized stannous ions Download PDFInfo
- Publication number
- CN112076112A CN112076112A CN201910506957.6A CN201910506957A CN112076112A CN 112076112 A CN112076112 A CN 112076112A CN 201910506957 A CN201910506957 A CN 201910506957A CN 112076112 A CN112076112 A CN 112076112A
- Authority
- CN
- China
- Prior art keywords
- stannous
- hyaluronic acid
- oral care
- care composition
- ion source
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
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- 150000002500 ions Chemical class 0.000 title claims abstract description 38
- 229920002674 hyaluronan Polymers 0.000 claims abstract description 81
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- TXUICONDJPYNPY-UHFFFAOYSA-N (1,10,13-trimethyl-3-oxo-4,5,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl) heptanoate Chemical compound C1CC2CC(=O)C=C(C)C2(C)C2C1C1CCC(OC(=O)CCCCCC)C1(C)CC2 TXUICONDJPYNPY-UHFFFAOYSA-N 0.000 claims description 8
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- 235000013343 vitamin Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 210000004127 vitreous body Anatomy 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
- A61K8/735—Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Oral & Maxillofacial Surgery (AREA)
- Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Cosmetics (AREA)
Abstract
The present invention relates to an oral care composition comprising stable stannous ions, characterized in that it comprises: a stannous ion source, hyaluronic acid, and, an orally acceptable carrier; and the mass ratio of the stannous ion source to the hyaluronic acid is 1:10-10: 1. In the oral care composition of the present invention, the hyaluronic acid in a specific ratio can greatly improve the stability of the stannous ion source in the composition.
Description
Technical Field
The present invention relates to the field of oral care technology, in particular to an oral care composition comprising stable stannous ions.
Background
Stannous ions have a long history of use in oral care products. Early stannous ions are added to oral care compositions in the form of stannous fluoride to provide fluoride ions; then, stannous ions are gradually found to have the effects of resisting bacteria, resisting allergy, preventing demineralization and the like.
For example, chinese patent publication No. CN 104853715 a discloses an aqueous oral care composition comprising a water soluble stannous ion source, wherein the composition comprises at least 50 wt% water, and wherein the stannous ion source is selected from the group consisting of stannous chloride, stannous pyrophosphate, stannous formate, stannous acetate, stannous gluconate, stannous lactate, stannous tartrate, stannous oxalate, stannous malonate, stannous citrate, stannous glyoxylate, and mixtures thereof. The oral care composition has greatly improved robustness against microbial challenges. That is, to give the oral care composition robustness against microbial challenges.
As another example, chinese patent publication No. CN 104069013 a discloses an oral composition comprising a stannous ion source, a polyvalent cation source, and a mineral surface active agent that provides enhanced therapeutic efficacy derived from stannous fluoride and/or other stannous salts, including antimicrobial efficacy, inhibition of halitosis, inhibition of dental plaque growth and metabolism, reduction of gingivitis, slowing of periodontal disease progression, reduction of dentinal hypersensitivity, and reduction of crown and root caries.
As another example, chinese patent publication No. CN 106074192 a discloses an oral care composition comprising a polyphenol compound, a stannous ion source, and a soluble alkaline earth metal ion source, wherein the alkaline earth metal ion source is a non-antioxidant. In the oral care composition, stannous ions reduce oxidation of the polyphenolic compounds in the composition.
The above are all effective examples of the use of stannous ions. However, stannous ions added to oral care compositions are easily oxidized, especially in aqueous environments, to stannous oxide or to stannic oxide precipitates, which not only affects the bioavailability of the stannous ions, but also the stability of the composition itself.
Hyaluronic acid is an acidic mucopolysaccharide, which was first isolated from bovine vitreous humor by Meyer et al, university of Columbia, 1934, and is also widely distributed in various parts of the human body.
Disclosure of Invention
The technical problem to be solved by the present invention is to provide an oral care composition comprising stable stannous ions. In the oral care composition, the hyaluronic acid in a specific ratio can greatly improve the stability of the stannous ion source in the composition.
In order to solve the technical problems, the invention adopts the following technical scheme:
an oral care composition comprising stabilized stannous ions comprising
A stannous ion source,
hyaluronic acid and, in addition,
an orally acceptable carrier; and is
The mass ratio of the stannous ion source to the hyaluronic acid is 1:10-10: 1.
Preferably, the mass ratio of the stannous ion source to the hyaluronic acid is 1:1-10: 1; more preferably, the mass ratio of the stannous ion source to hyaluronic acid is 1:3-10: 1.
As a further improvement of the technical scheme, the addition amount of the stannous ion source in the oral care composition is 0.05% -3%; preferably, the stannous ion source is added in an amount of 0.1% to 3% in the oral care composition; more preferably, the stannous ion source is added in an amount of 0.5% to 3% in the oral care composition; most preferably, the stannous ion source is added in an amount of 1% to 3% in the oral care composition.
As a further improvement of the technical proposal, the addition amount of the hyaluronic acid in the oral care composition is 0.05-5%; preferably, the hyaluronic acid is added in an amount of 0.1-5% in the oral care composition; more preferably, the hyaluronic acid is added in an amount of 0.5-5% in the oral care composition; most preferably, the hyaluronic acid is added in an amount of 1-5% in the oral care composition.
As a further improvement of the technical scheme, the stannous ion source is selected from one or more of stannous fluoride, stannous chloride, stannous acetate, stannous gluconate, stannous sulfate, stannous lactate and stannous tartrate;
preferably, the stannous ion source is selected from stannous fluoride or stannous chloride.
As a further improvement of the technical proposal, the molecular formula of the hyaluronic acid is (C)14H21NO11) n, having the formula:
preferably, the hyaluronic acid comprises an acid form of hyaluronic acid or a salt form of hyaluronic acid; the salt form of hyaluronic acid includes, for example, sodium hyaluronate and the like.
Preferably, the hyaluronic acid is selected from low molecular weight hyaluronic acid, medium molecular weight hyaluronic acid or high molecular weight hyaluronic acid.
Preferably, the low molecular weight hyaluronic acid has a molecular weight in the range of 10kDa to 1000kDa, preferably 200kDa to 400 kDa; the molecular weight range of the medium molecular weight hyaluronic acid is 1000KDa-1800 KDa; the molecular weight range of the high molecular weight hyaluronic acid is more than 1800KDa, and is preferably 1900KDa-2400 KDa.
As a further improvement in the technical solution, the oral care composition comprises a toothpaste, gel, mouthwash or tooth powder.
Any range recited herein is intended to include the endpoints and any number between the endpoints and any subrange subsumed therein or defined therein.
The starting materials of the present invention are commercially available, unless otherwise specified, and the equipment used in the present invention may be any equipment conventionally used in the art or may be any equipment known in the art.
Compared with the prior art, the invention has the following beneficial effects:
the oral care composition contains stannous ions, and the stability of the stannous ion source in the composition can be greatly improved by adding hyaluronic acid in a specific ratio.
Detailed Description
In order to more clearly illustrate the invention, the invention is further described below in connection with preferred embodiments. It is to be understood by persons skilled in the art that the following detailed description is illustrative and not restrictive, and is not to be taken as limiting the scope of the invention.
As one aspect of the invention, the invention is an oral care composition comprising stabilized stannous ions comprising
A stannous ion source,
hyaluronic acid and, in addition,
an orally acceptable carrier; and is
The mass ratio of the stannous ion source to the hyaluronic acid is 1:10-10: 1.
In certain embodiments of the invention, the mass ratio of the stannous ion source to hyaluronic acid is 1:9-10:1, 1:8-10:1, 1:5-10:1, 1:3-10:1, 1:1-10:1, 1:10-9:1, 1:10-8:1, 1:10-5:1, 1:10-3:1, 1:10-1:1, 1: 9-9:1, 1:8-8:1, 1:7-7:1, 1:5-5:1, 1:3-3: 1;
in certain preferred embodiments of the invention, the mass ratio of the stannous ion source to hyaluronic acid is 1:3 to 10: 1.
It has been surprisingly discovered that the stability of stannous ions can be significantly improved by adding hyaluronic acid in the specific ratio described above to an oral care composition containing a stannous ion source.
In certain embodiments of the invention, the stannous ion source is added to the oral care composition in an amount of 0.01% to 3%, preferably in an amount of 0.05% to 3%, more preferably in an amount of 0.1% to 3%, 0.2% to 3%, 0.5% to 3%, 1% to 3%, 2% to 3%, 0.01% to 2.5%, 0.05% to 2.5%, 0.1% to 2.5%, 0.2% to 2%, 0.5% to 1.5%, 0.5% to 1%.
In certain embodiments of the invention, the hyaluronic acid is added to the oral care composition in an amount of 0.01% to 3%, preferably in an amount of 0.05% to 3%, more preferably in an amount of 0.1% to 3%, 0.2% to 3%, 0.5% to 3%, 1% to 3%, 2% to 3%, 0.01% to 2.5%, 0.05% to 2.5%, 0.1% to 2.5%, 0.2% to 2%, 0.5% to 1.5%, 0.5% to 1%.
In certain embodiments of the present invention, the stannous ion source is selected from one or more of stannous fluoride, stannous chloride, stannous acetate, stannous gluconate, stannous sulfate, stannous lactate and stannous tartrate.
In certain preferred embodiments of the present invention, the stannous ion source is selected from stannous fluoride or stannous chloride.
The hyaluronic acid is also called uronic acid and hyaluronic acid (Hyaluronan) and is widely distributed in each part of a human body; is a high-grade polymer polysaccharide composed of units of D-glucuronic acid and N-acetylglucosamine, wherein the D-glucuronic acid and the N-acetylglucosamine are connected by beta-1, 3-glycosidic bonds, the disaccharide units are connected by beta-1, 4-glycosidic bonds, and the disaccharide units can reach as much as 25000.
In certain embodiments of the invention, the hyaluronic acid formula is (C)14H21NO11) n, having the formula:
in certain embodiments of the invention, the hyaluronic acid comprises an acid form of hyaluronic acid or a salt form of hyaluronic acid. The salt form of hyaluronic acid includes, for example, sodium hyaluronate and the like.
In certain preferred embodiments of the invention, the hyaluronic acid is selected from low molecular weight hyaluronic acid, medium molecular weight hyaluronic acid or high molecular weight hyaluronic acid.
In certain preferred embodiments of the invention, the low molecular weight hyaluronic acid has a molecular weight in the range of 10kDa to 1000kDa, preferably 200kDa to 400 kDa; the molecular weight range of the medium molecular weight hyaluronic acid is 1000KDa-1800 KDa; the molecular weight range of the high molecular weight hyaluronic acid is more than 1900KDa, and is preferably 1800KDa-2400 KDa.
In certain embodiments of the present invention, the oral care composition comprises a toothpaste, gel, mouthwash, or tooth powder.
In the present invention, the "orally acceptable carrier" refers to any vehicle suitable for formulating the oral care compositions disclosed herein; (ii) is not harmful to the mammal when the orally acceptable carrier is retained in the mouth in the amounts disclosed herein without swallowing for a period of time sufficient to allow effective contact with the tooth surface as required by the present invention; overall, an orally acceptable carrier is not harmful if not intentionally swallowed; suitable orally acceptable carriers include, for example, one or more of the following: water, thickeners, buffers, humectants, surfactants, abrasives, sweeteners, flavoring agents, visual aids (e.g., colors, dyes, or mixtures thereof), anti-caries agents, antibacterial agents, whitening agents, desensitizing agents, vitamins, preservatives, enzymes, mixtures thereof, and the like.
In certain preferred embodiments of the present invention, adjuvants such as humectants, thickeners, and/or surfactants are included in the oral care composition.
"humectants" are ingredients that prevent the oral care composition from becoming dehydrated and hardened. Exemplary humectants include, but are not limited to, glycerin, propylene glycol, sorbitol, and the like. The humectant is typically present in the oral care composition in an amount of 10 to 80% by mass.
A "thickener" is a substance that increases the viscosity of a solution or liquid/solid mixture, but does not substantially change its properties. The purpose of the thickener is to provide skeleton, flow and stability to the product. Exemplary thickening agents include, but are not limited to, one or more of hydroxyethylcellulose, carboxymethylcellulose and salts thereof (e.g., sodium carboxymethylcellulose), carrageenan (carrageenan), carboxyvinyl polymers, xanthan gum (xanthan g μm), carrageenan, gelatin, pullulan, sodium alginate, and the like. In certain embodiments, the thickening agent comprises one or more of xanthan gum, carrageenan, or sodium carboxymethyl cellulose. The proportion by weight of thickener in the oral care composition is typically from 0.2 to 2%.
The "surfactant" serves the purpose of emulsifying the flavor and lathering in the oral care composition and may, to some extent, assist in the sufficient and complete dispersion of the hydroxyapatite-polycarboxyl compound complex. Exemplary surfactants include, but are not limited to, anionic surfactants such as sodium dodecyl sulfate; amphoteric surfactants, such as betaine; amino acid surfactants such as sodium sarcosinate lauryl alcohol and nonionic surfactants. The proportion of surfactant by weight in the oral care composition is typically from 0.5 to 2.5%.
According to certain preferred embodiments of the present application, the oral care composition may further comprise active ingredients such as antibacterial agents, anticaries agents, anti-sensitivity agents, and/or whitening agents.
By "antibacterial agent" is meant a chemical substance that is capable of maintaining the growth or reproduction of certain microorganisms in an oral care composition below a necessary level over a period of time. Exemplary antimicrobial agents include, but are not limited to: tetrahydrocurcumin, cetylpyridinium chloride, triclosan, and the like.
"anticaries agent" means a substance having an inhibitory effect on caries, for example, a substance which enhances the anticaries ability of teeth by decreasing the solubility of enamel hydroxyapatite, or a substance which controls plaque, inhibiting bacterial growth. Exemplary anticaries agents include, but are not limited to, phosphorus-containing agents (calcium phosphate, magnesium glycerophosphate, calcium lactate phosphate, sodium caseinate, etc.), or arginine and its derivatives. Preferably, in certain embodiments, the anticaries agent comprises a fluoride ion source.
An "anti-sensitivity agent" refers to a substance that prevents or treats dentinal hypersensitivity by inhibiting nerve impulses or being capable of closing or decreasing the permeability of dentinal tubules. Exemplary anti-sensitivity agents include, but are not limited to: potassium ion sources such as dipotassium glycyrrhizinate, potassium fluoride, potassium nitrate, potassium chloride and the like.
The "whitening agent" refers to a substance having a whitening effect on teeth. Exemplary whitening agents include, but are not limited to: a peroxide bleaching agent.
Examples 1-4, comparative example 1:
an oral care composition containing stable stannous ions comprises the following raw materials in the following table 1 weight ratio, wherein the total amount is calculated by 100 parts.
Table 1:
after the compositions of examples 1 to 4 and comparative example 1 were left at room temperature for 7 days, the content of stannous fluoride remaining in the solution of the compositions was measured, and the data are shown in table 2 below.
Table 2:
as can be seen from table 1 and table 2 above, in the composition containing stannous ions, when hyaluronic acid is not added, the stability of the stannous ions is very low, and after the composition is placed for 7 days, the mass ratio of the remaining stannous ion source is less than 30%; when the mass ratio of the stannous ion source to the hyaluronic acid is less than or equal to 1:1, the stability of the stannous ion is obviously improved, and after the stannous ion source is placed for 7 days, the mass ratio of the remaining stannous ion source is more than 50%; when the mass ratio of the stannous ion source to the hyaluronic acid is less than or equal to 1:3, the stability of the stannous ion is remarkably improved, and after the stannous ion source is placed for 7 days, the mass ratio of the remaining stannous ion source is more than 65%; when the mass ratio of the stannous ion source to the hyaluronic acid is less than or equal to 1:5, the stability of the stannous ion is remarkably improved, and after the stannous ion source is placed for 7 days, the mass ratio of the remaining stannous ion source is more than 75%; however, after the mass ratio of the stannous ion source to the hyaluronic acid is less than or equal to 1:5, even if the addition amount of the hyaluronic acid is increased, the stability improvement ratio of the stannous ion source to the hyaluronic acid does not tend to be improved continuously and obviously.
In the invention, the detection method of the stannous ions adopts a detection method of chemical industry standard HG/T2526-2007 stannous ions.
Examples 5-8, comparative example 2:
an oral care composition containing stable stannous ions comprises the following raw materials in a weight ratio of table 3, wherein the total weight is 100 parts.
Table 3:
after the compositions of examples 5 to 8 and comparative example 2 were left at room temperature for 7 days, the remaining stannous fluoride content in the solution of the compositions was measured, and the data are shown in the following table 4:
as can be seen from table 3 and table 4 above, in the composition containing stannous ions, when hyaluronic acid is not added, the stability of the stannous ions is very low, and after the composition is placed for 7 days, the mass ratio of the remaining stannous ion source is less than 30%; when the mass ratio of the stannous ion source to the hyaluronic acid is less than or equal to 10:1, the stability of the stannous ion is obviously improved, and after the stannous ion source is placed for 7 days, the mass ratio of the remaining stannous ion source is more than 45%; when the mass ratio of the stannous ion source to the hyaluronic acid is less than or equal to 3:1, the stability of the stannous ion is remarkably improved, and after the stannous ion source is placed for 7 days, the mass ratio of the remaining stannous ion source is more than 55%; when the mass ratio of the stannous ion source to the hyaluronic acid is less than or equal to 1:1, the stability of the stannous ion is remarkably improved, and after the stannous ion source is placed for 7 days, the mass ratio of the remaining stannous ion source is more than 75%.
Example 9, comparative example 3:
an oral care composition containing stable stannous ions comprises the following raw materials in the proportion of table 5, and the total amount is prepared into toothpaste according to 100 parts.
Table 5:
the remaining stannous fluoride content of the composition solutions was measured after aging the composition products of example 9 and comparative example 3 at 40 c for 30 days, and the data are shown in table 6 below:
table 6:
as can be seen from table 5 and table 6 above, in the formula of the toothpaste containing stannous ions, when hyaluronic acid is not added, the stability of the stannous ions is very low, and after aging for 30 days at 40 ℃, the mass ratio of the remaining stannous ion source is less than 30%; when the mass ratio of the stannous ion source to the hyaluronic acid is 1:1, the stability of the stannous ion is remarkably improved, and after aging for 30 days at 40 ℃, the mass ratio of the remaining stannous ion source is still larger than 75%.
As described above, when hyaluronic acid is added to an oral care composition containing stannous ions at a specific ratio, the stability of the stannous ion source in the composition can be greatly improved.
It should be understood that the above-described embodiments of the present invention are merely examples for clearly illustrating the present invention, and are not intended to limit the embodiments of the present invention. Other variations and modifications will be apparent to persons skilled in the art in light of the above description. Not all embodiments are exhaustive. All obvious changes and modifications which are obvious to the technical scheme of the invention are covered by the protection scope of the invention.
Claims (10)
1. An oral care composition comprising stabilized stannous ions, comprising:
a stannous ion source,
hyaluronic acid and, in addition,
an orally acceptable carrier; and is
The mass ratio of the stannous ion source to the hyaluronic acid is 1:10-10: 1.
2. The oral care composition comprising stabilized stannous ions according to claim 1, characterized in that: the mass ratio of the stannous ion source to the hyaluronic acid is 1:1-10: 1; preferably, the mass ratio of the stannous ion source to the hyaluronic acid is 1:3-10: 1.
3. The oral care composition comprising stabilized stannous ions according to claim 1, characterized in that: the stannous ion source is added in the oral care composition in an amount of 0.05% -3%; preferably, the stannous ion source is added in an amount of 0.1% to 3% in the oral care composition; more preferably, the stannous ion source is added in an amount of 0.5% to 3% in the oral care composition; most preferably, the stannous ion source is added in an amount of 1% to 3% in the oral care composition.
4. The oral care composition comprising stabilized stannous ions according to claim 1, characterized in that: the hyaluronic acid is added in the oral care composition in an amount of 0.05-5%; preferably, the hyaluronic acid is added in an amount of 0.1-5% in the oral care composition; more preferably, the hyaluronic acid is added in an amount of 0.5-5% in the oral care composition; most preferably, the hyaluronic acid is added in an amount of 1-5% in the oral care composition.
5. The oral care composition comprising stabilized stannous ions according to claim 1, characterized in that: the stannous ion source is selected from one or more of stannous fluoride, stannous chloride, stannous acetate, stannous gluconate, stannous sulfate, stannous lactate and stannous tartrate.
6. The oral care composition comprising stabilized stannous ions according to claim 5, characterized in that: the stannous ion source is selected from stannous fluoride or stannous chloride or a combination of two of the stannous fluoride and the stannous chloride.
7. The oral care composition comprising stabilized stannous ions according to claim 1, characterized in that: the molecular formula of the hyaluronic acid is (C)14H21NO11) n, having the formula:
8. the oral care composition comprising stabilized stannous ions according to claim 7, characterized in that: the hyaluronic acid comprises an acid form of hyaluronic acid or a salt form of hyaluronic acid; the salt form of hyaluronic acid comprises sodium hyaluronate.
9. The oral care composition comprising stabilized stannous ions according to claim 1, characterized in that: the hyaluronic acid is selected from low molecular weight hyaluronic acid, medium molecular weight hyaluronic acid or high molecular weight hyaluronic acid;
preferably, the low molecular weight hyaluronic acid has a molecular weight in the range of 10kDa to 1000kDa, preferably 200kDa to 400 kDa; the molecular weight range of the medium molecular weight hyaluronic acid is 1000KDa-1800 KDa; the molecular weight range of the high molecular weight hyaluronic acid is more than 1800KDa, and is preferably 1900KDa-2400 KDa.
10. The oral care composition comprising stabilized stannous ions according to claim 1, characterized in that: the oral care composition comprises a toothpaste, gel, mouthwash or tooth powder.
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