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CN118415890A - Oral care compositions comprising stannous and zinc ion sources and methods of improving structural stability of the compositions - Google Patents

Oral care compositions comprising stannous and zinc ion sources and methods of improving structural stability of the compositions Download PDF

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Publication number
CN118415890A
CN118415890A CN202410339446.0A CN202410339446A CN118415890A CN 118415890 A CN118415890 A CN 118415890A CN 202410339446 A CN202410339446 A CN 202410339446A CN 118415890 A CN118415890 A CN 118415890A
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Prior art keywords
stannous
zinc
oral care
ion source
care composition
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Inventor
陈晓斌
高琳
李可瑶
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Hawley and Hazel Chemical Co Zhongshan Ltd
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Hawley and Hazel Chemical Co Zhongshan Ltd
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Priority to CN202410339446.0A priority Critical patent/CN118415890A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24Phosphorous; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/27Zinc; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/58Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/48Thickener, Thickening system

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  • 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)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

An oral care composition comprising a stannous ion source and a zinc ion source, comprising 1) a stannous ion source; 2) A zinc ion source; 3) A thickener; 4) Tetrapotassium pyrophosphate; 5) An orally acceptable carrier; wherein the thickener is xanthan gum. The addition of tetrapotassium pyrophosphate to an oral care composition comprising a stannous ion source and a zinc ion source, and the use of xanthan gum as a thickening agent, can improve the stability of the composition structure and improve the activity of the composition in inhibiting plaque growth.

Description

Oral care compositions comprising stannous and zinc ion sources and methods of improving structural stability of the compositions
Technical Field
The invention relates to the technical field of oral care, in particular to an oral care composition containing a stannous ion source and a zinc ion source and a method for improving structural stability of the composition and improving the efficacy of the composition in inhibiting dental plaque growth.
Background
Stannous ions have a long history of use in oral care products because of their excellent clinical manifestations of inhibiting microbial and dental plaque growth, inhibiting bad breath, inhibiting gingivitis, etc. However, the addition of a stannous ion source to the oral care composition may affect the rheology of the composition formulation.
For example, chinese patent application CN113244118a mentions that oral care compositions comprising stannous chloride, especially in combination with a thickening agent such as carboxymethyl cellulose, have poor rheology. To improve the rheology of the composition, this application discloses an oral care composition comprising a stannous ion source and a thickener, wherein the thickener comprises at least 3 compounds selected from the group consisting of linear sulfated polysaccharides (e.g., carrageenan), natural gels, and hydroxyethylcellulose as a nonionic cellulose derivative.
Zinc is also a commonly used active substance in oral care products and has the effects of resisting microorganisms, strengthening tooth enamel, promoting cell repair and the like. However, compositions of zinc ion sources in combination with carrageenan suffer from water splitting.
There is therefore a need to develop a new composition which is stable and which gives better benefits in terms of the structure which the composition contains both a stannous ion source and a zinc ion source.
Disclosure of Invention
The first technical problem to be solved by the present invention is to provide an oral care composition comprising a stannous ion source and a zinc ion source. The oral care composition is structurally stable.
A second technical problem to be solved by the present invention is to provide a method of improving the structural stability of an oral care composition comprising a stannous ion source and a zinc ion source.
The present invention addresses the third technical problem by providing the use of an oral care composition comprising a stannous ion source and a zinc ion source for inhibiting the growth of dental plaque.
In order to solve the first technical problem, the invention adopts the following technical scheme:
an oral care composition comprising a stannous ion source and a zinc ion source, comprising:
1) A stannous ion source;
2) A zinc ion source;
3) A thickener;
4) Tetrapotassium pyrophosphate;
5) An orally acceptable carrier;
wherein the thickener is xanthan gum.
As one embodiment, the xanthan gum is present in the oral care composition in an amount of 0.3 to 0.8% by mass.
As one embodiment, the stannous ion source comprises one or more of stannous fluoride, stannous chloride, stannous pyrophosphate, stannous phosphate, stannous bromide, stannous iodide, stannous oxide, stannous sulfide, stannous metaphosphate, stannous acetate, stannous tartrate, stannous citrate, stannous malate, stannous malonate, stannous gluconate, stannous oxalate.
As an embodiment, the stannous ion source is present in the oral care composition in a mass ratio of 0.05% -0.8%, preferably 0.1-0.5%.
As one embodiment, the zinc ion source comprises one or more of zinc citrate, zinc chloride, zinc lactate, zinc nitrate, zinc acetate, zinc gluconate, zinc sulfate, zinc pyrophosphate and zinc phosphate.
As an embodiment, the zinc ion source is present in the oral care composition at a mass ratio of 0.1 to 2.0%, preferably 0.2 to 2.0%.
As one embodiment, the tetrapotassium pyrophosphate comprises 0.2 to 4.0% by mass of the oral care composition.
As one embodiment, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate is in the range of 1:0.41 to 1:1.09.
In order to solve the second technical problem, the invention adopts the following technical scheme:
A method of improving the structural stability of an oral care composition comprising a stannous ion source and a zinc ion source comprising the steps of:
Xanthan gum and tetrapotassium pyrophosphate are added to an oral care composition comprising a stannous ion source and a zinc ion source.
In order to solve the third technical problem, the invention adopts the following technical proposal
There is provided the use of an oral care composition comprising a source of stannous ions and a source of zinc ions to inhibit the growth of dental plaque, the oral care composition having added tetrapotassium pyrophosphate and xanthan gum as a thickening agent.
Any range recited in the invention includes any numerical value between the endpoints and any sub-range of any numerical value between the endpoints or any numerical value between the endpoints.
Unless otherwise indicated, all starting materials herein are commercially available, and the equipment used in the present invention may be conventional in the art or may be conventional in the art.
Compared with the prior art, the invention has the following beneficial effects:
the addition of tetrapotassium pyrophosphate to an oral care composition comprising a stannous ion source and a zinc ion source, and the use of xanthan gum as a thickening agent, can improve the stability of the composition structure and improve the activity of the composition in inhibiting plaque growth.
Detailed Description
In order to more clearly illustrate the present invention, the present invention will be further described with reference to preferred embodiments. It is to be understood by persons skilled in the art that the following detailed description is illustrative and not restrictive, and that this invention is not limited to the details given herein.
All percentages and ratios used herein are by weight of the total composition unless otherwise specified. Unless otherwise indicated, all percentages, ratios, and levels of ingredients referred to herein are based on the actual level of the ingredient and do not include solvents, fillers, or other materials that may be combined with the ingredients in commercially available products.
The term "comprising" herein means that other steps and ingredients may be added that do not affect the end result.
The term "preferably" and its variants herein refer to embodiments of the invention that are capable of providing particular benefits under particular circumstances. However, other embodiments may be preferred under the same or other circumstances. Furthermore, the detailed description of one or more preferred embodiments does not represent additional embodiments, but rather is intended to exclude additional embodiments from the scope of the present invention.
The specific conditions are not noted in the embodiment of the invention, and the method is carried out according to the conventional conditions or the conditions suggested by manufacturers; the reagents or apparatus used were conventional products commercially available without the manufacturer's attention.
As one aspect of the present invention, an oral care composition comprising a stannous ion source and a zinc ion source comprises:
1) A stannous ion source;
2) A zinc ion source;
3) A thickener;
4) Tetrapotassium pyrophosphate;
5) An orally acceptable carrier;
wherein the thickener is xanthan gum.
The present application unexpectedly found that the problem of composition structural instability is very likely to occur in oral care compositions comprising a stannous ion source and a zinc ion source, which can be significantly ameliorated by the addition of tetrapotassium pyrophosphate and xanthan gum as a thickening agent.
Stannous ion source
In an embodiment of the present invention, a stannous ion source is included in the oral care composition.
The stannous ion source is derived from one or more of stannous fluoride, stannous chloride, stannous pyrophosphate, stannous phosphate, stannous bromide, stannous iodide, stannous oxide, stannous sulfide, stannous metaphosphate, stannous acetate, stannous tartrate, stannous citrate, stannous malate, stannous malonate, stannous gluconate and stannous oxalate.
In certain embodiments of the invention, the stannous ion source comprises a stannous ion mass ratio of 0.05-0.8% in the composition, such as but not limited to 0.08-0.8%,0.1-0.8%,0.15-0.8%,0.2-0.8%,0.3-0.8%,0.4-0.8%,0.5-0.8%,0.6-0.8%,0.05-0.6%,0.08-0.6%,0.1-0.6%,0.15-0.6%,0.2-0.6%,0.3-0.6%,0.4-0.6%,0.5-0.6%,0.05-0.5%,0.08-0.5%,0.1-0.5%,0.15-0.5%,0.2-0.5%,0.3-0.5%,0.4-0.5%,0.05-0.4%,0.08-0.4%,0.1-0.4%,0.15-0.4%,0.2-0.4%,0.3-0.4%,0.05-0.3%,0.08-0.3%,0.1-0.3%,0.15-0.3%,0.2-0.3%,0.05-0.2%,0.08-0.2%,0.1-0.2%,0.15-0.2%.
Zinc ion source
The oral care compositions of the present invention include a zinc ion source therein;
in certain embodiments of the present invention, the zinc ion source comprises one or more of zinc citrate, zinc chloride, zinc lactate, zinc nitrate, zinc acetate, zinc gluconate, zinc sulfate, zinc pyrophosphate, and zinc phosphate.
In certain preferred embodiments of the present invention, the zinc citrate is zinc citrate trihydrate.
In certain embodiments of the invention, the zinc ion source is present in the composition at a mass ratio of 0.1-2%, such as, but not limited to 0.1-1.5%,0.1-1.0%,0.1-0.8%,0.1-0.5%,0.1-0.3%,0.2-2.0%,0.2-1.5%,0.2-1.0%,0.2-0.8%,0.2-0.5%,0.5-2.0%,0.5-1.5%,0.5-1.0%,0.5-0.8%,0.8-2%,0.8-1.5%,0.8-1.0%,1.0-2%,1.0-1.8%,1.0-1.5%,1.0-1.2%,1.2-2%,1.2-1.8%,1.2-1.5%,1.5-2%,1.5-1.8%.
Xanthan gum
A thickener is a substance that increases the viscosity of a solution or liquid/solid mixture without substantially changing its properties. The purpose of the thickener is to provide the product with a skeleton, flowability and stability.
The present invention has unexpectedly found that the addition of tetrapotassium pyrophosphate and xanthan gum as a thickening agent in an oral care composition comprising both a stannous ion source and a zinc ion source can significantly improve the aforementioned composition's problem of structural instability.
In certain embodiments of the present invention, the xanthan gum is present in the oral care composition at a mass ratio of 0.3 to 0.8%, such as but not limited to 0.3-0.8%,0.3-0.7%,0.3-0.6%,0.3-0.5%,0.3-0.4%,0.4-0.8%,0.4-0.7%,0.4-0.6%,0.4-0.5%,0.5-0.8%,0.5-0.7%,0.5-0.6%,0.6-0.8%,0.6-0.7%.
Tetrapotassium pyrophosphate
The present invention has unexpectedly found that the addition of tetrapotassium pyrophosphate and xanthan gum as a thickener in an oral care composition comprising both a stannous ion source and a zinc ion source can significantly improve the aforementioned composition's problem of structural instability.
In certain embodiments of the invention, the tetrapotassium pyrophosphate comprises 0.2 to 4.0% by mass of the oral care composition, such as but not limited to 0.5-4.0%,1-4.0%,1.5-4.0%,2-4.0%,2.5-4.0%,3-4.0%,0.2-3.0%,0.5-3.0%,1-3.0%,1.5-3.0%,2-3.0%,2.5-3.0%,0.2-2.5%,0.5-2.5%,1-2.5%,1.5-2.5%,2-2.5%,0.2-2%,0.5-2%,1-2%,1.5-2%,0.2-1.5%,0.5-1.5%,1-1.5%,0.2-1%,0.5-1%,0.2-0.5%.
Ratio of sum of molar amounts of zinc element and tin element to molar amount of pyrophosphate
In certain embodiments of the invention, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate ranges from 1:0.41 to 1:1.09, such as, but not limited to, from 1:0.41 to 1.0, from 1:0.41 to 0.75, from 1:0.6 to 1.09, from 1:0.6 to 1.0, from 1:0.6 to 0.8, from 1:0.8 to 1.09, and from 1:0.8 to 1.0.
Orally acceptable carrier
In the present invention, the "orally acceptable carrier" refers to any vehicle suitable for formulating the disclosed oral care liquid compositions; an orally acceptable carrier is not harmful to a mammal when retained in the mouth in the amounts disclosed herein without swallowing for a period of time sufficient to allow effective contact with the tooth surfaces as required by the present invention; generally, an orally acceptable carrier is not harmful even if inadvertently swallowed; suitable orally acceptable carriers include, for example, one or more of water, pH adjusting agents, humectants, sweeteners, flavoring agents, visual aids (e.g., pigments, dyes or mixtures thereof), anticaries agents, antibacterial agents, whitening agents, desensitizing agents, vitamins, preservatives, enzymes, mixtures thereof, and the like.
As another aspect of the present invention, there is provided a method of improving the structural stability of an oral care composition comprising a stannous ion source and a zinc ion source, comprising the steps of:
the thickeners xanthan gum and tetrapotassium pyrophosphate are added to an oral care composition comprising a stannous ion source and a zinc ion source.
As a further aspect of the invention there is provided the use of an oral care composition comprising a source of stannous ions and a source of zinc ions to inhibit the growth of dental plaque, the oral care composition incorporating tetrapotassium pyrophosphate and xanthan gum as a thickening agent.
The present invention has unexpectedly found that in an oral care composition comprising a stannous ion source and a zinc ion source, the oral care composition can significantly inhibit plaque growth by adding tetrapotassium pyrophosphate and using xanthan gum as a thickening agent.
Method for evaluating structural stability of oral care composition
The structural stability of the oral care composition refers to physical appearance of a toothpaste body structure, and comprises a water division phenomenon of the toothpaste body and a phenomenon that whether the toothpaste body is difficult to extrude.
In certain embodiments of the invention, "gamma" represents no water division and "/" represents water division, wherein:
1-the paste is slightly water-separated
2-Represents moderate water division of paste
3-Represents that the paste has serious water diversion, but is in an acceptable range
4-Represents that the paste is extremely severely dehydrated and unacceptable
In certain embodiments of the invention, "gamma" indicates no difficult extrusion of the paste, and "/" indicates difficult extrusion, wherein
1-Can be extruded relatively smoothly from a tube container
2-From tube containers, extrusion is slightly difficult
3-More difficult to extrude from tube containers
4-Inability to extrude paste from tube container
Evaluation method for plaque inhibition effect of oral care composition in vitro
The artificial oral cavity biomembrane dynamic model is a better dental plaque research in-vitro model which is currently accepted, can simulate the oral environment of a human body, observe the dynamic process of bacteria forming biomembrane, and is an effective research method for bacterial plaque growth and control. The experiment comprises the following specific steps:
1) Collecting 3 human stimulated saliva, centrifuging to obtain supernatant, and sterilizing by ultraviolet irradiation for 60 min;
2) Placing the autoclaved hydroxyapatite sheet (Hydroxyapatite, HAP) into saliva, soaking overnight to form an acquired membrane;
3) The above 3 people were collected for stimulating saliva (subjects should have no oral hygiene activity for 24 hours prior to collection),
4) Sucking the mixed liquid of the stimulating saliva into the artificial oral cavity, and fully soaking the HAP tablet in the solution. Placing the bacterial plaque in a water bath kettle at 42.5 ℃ and enabling a culture medium to flow in a pulse mode to culture the bacterial plaque;
5) Evenly mixing toothpaste and deionized water in a ratio of 1:2 to prepare toothpaste slurry to obtain a sample solution;
6) After 8 hours of plaque growth, the medium in the flow chamber was pumped out. Pumping the sample solution into a flow chamber at a maximum flow rate;
7) After the whole flow chamber is filled with the sample solution, soaking is timed for 1min, and the sample solution is pumped out completely;
8) Pumping the culture medium solution into a flow chamber, continuously culturing for 16 hours, and terminating the experiment;
9) The experimental result is treated by an OD method, namely, the HAP sheet is taken out by tweezers, dipped and washed in distilled water for 5 times, then placed in a sterile test tube filled with 2mL of physiological saline, and fully and uniformly vibrated by a vortex oscillator;
10 300. Mu.L of the suspension in the previous step was aspirated into 96-well cell culture plates, the OD630 value was measured with an enzyme-labeled instrument (Tecan, INFINITE M, 200) at a wavelength of 630 nm and the average value was calculated, the OD630 value indicated the bacterial concentration, and the smaller the OD630, the better the antibacterial effect.
DETAILED DESCRIPTION OF EMBODIMENT (S) OF INVENTION
Example 1, comparative examples 1 to 5
The oral care compositions of example 1 and comparative examples 1-5 were prepared according to the formulation of table 1 below, all data in parts by weight, totaling 100 parts. In the invention, the oral care composition is prepared according to the formula and is mixed uniformly.
Table 1:
As can be seen from table 1, example 1 and comparative examples 1-5 each added 2% zinc citrate, 0.1% stannous fluoride and 2.5% tetrapotassium pyrophosphate, except that different thickeners were added, wherein:
example 1 xanthan gum as thickener;
comparative example 1 carrageenan was used as a thickener;
Comparative example 2a cellulose gum was used as a thickener;
Comparative example 3a combination of carrageenan and cellulose gum was used as a thickener;
Comparative example 4a combination of carrageenan and xanthan gum was used as thickener;
comparative example 5 a combination of cellulose gum and xanthan gum was used as a thickener.
After the preparation of the above example 1 and comparative examples 1 to 5 was completed, the composition was aged at 40℃for 3 months, and the paste structure was observed, and the results are shown in Table 2.
Table 2:
Example 1 Comparative example 1 Comparative example 2 Comparative example 3 Comparative example 4 Comparative example 5
Dividing water 4 2 3 3
Paste is difficult to extrude 4 4 3
As can be seen from Table 2, example 1 had no problems such as water division and difficult extrusion of paste, while comparative example 1 and comparative example 4 had different degrees of water division, comparative example 5 had different degrees of difficult extrusion of paste, and comparative example 2 and comparative example 3 had both water division and difficult extrusion of paste. It can be seen that in an oral care composition comprising a stannous ion source and a zinc ion source, the oral care composition can be structurally stable only with xanthan gum and only xanthan gum as the thickener.
Comparative examples 6 to 9
Comparative examples 6-9 oral care compositions were prepared according to the formulation of table 3, with the data of example 1 being presented in table 3, all by weight, totaling 100 parts for comparison purposes.
Table 3:
Example 1 Comparative example 6 Comparative example 7 Comparative example 8 Comparative example 9
Sorbitol 50 50 50 50 50
Zinc citrate 2 2 2 2 2
Xanthan gum 0.6 0.6 0.6 0.6 0.6
Tetra sodium pyrophosphate / 2.5 / / /
Sodium tripolyphosphate / / 2.5 / /
Potassium tripolyphosphate / / / 2.5 /
Tetrapotassium pyrophosphate 2.5 / / / /
Silica dioxide 22 22 22 22 22
Stannous fluoride 0.1 0.1 0.1 0.1 0.1
Saccharin sodium salt 0.25 0.25 0.25 0.25 0.25
Sodium lauryl sulfate 2.2 2.2 2.2 2.2 2.2
Essence 1.2 1.2 1.2 1.2 1.2
Deionized water Added to 100% Added to 100% Added to 100% Added to 100% Added to 100%
As can be seen from table 3, example 1 and comparative examples 6 to 9 each use xanthan gum as thickener, except that different phosphates were added, wherein:
Example 1 was supplemented with 2.5% tetrapotassium pyrophosphate;
comparative example 6 was added with 2.5% tetrasodium pyrophosphate;
comparative example 7 was added with 2.5% sodium tripolyphosphate;
Comparative example 8 was added with 2.5% potassium tripolyphosphate;
Comparative example 9 does not add phosphate.
After the preparation of the above comparative examples 6 to 9 was completed, the composition was aged at 40℃for 3 months, and the paste structure was observed, and the results are shown in Table 4:
Table 4:
Example 1 Comparative example 6 Comparative example 7 Comparative example 8 Comparative example 9
Dividing water 2 2 3 4
Paste is difficult to extrude 2 3 3 4
As can be seen from Table 4, example 1 had no problems such as water separation and difficult paste extrusion, while comparative examples 6 to 9 all had water separation and difficult paste extrusion to different extents. It can be seen that in oral care compositions comprising a stannous ion source and a zinc ion source, the paste structure is stabilized only by the addition of the phosphate tetrapotassium pyrophosphate.
Examples 2 to 3, comparative examples 10 to 11
Oral care compositions of examples 2-3 and comparative examples 10-11 were prepared according to the formulation of Table 5, with example 1 listed in Table 5 for comparison purposes, where the data are all parts by weight and total 100 parts.
Table 5:
As can be seen from Table 5, examples 2 to 3 and comparative examples 10 to 11 each use xanthan gum as a thickener and add tetrapotassium pyrophosphate, except that the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate is different, wherein:
the ratio of example 1 to example 1 was 1:0.68;
The ratio of example 2 to example 2 was 1:0.41;
The ratio of example 3 to example 1:1.09;
the ratio of the two of comparative example 9 was 1:0.33;
The ratio of the two comparative examples 10 was 1:1.5.
After the preparation of the above comparative examples 2 to 3 and comparative examples 10 to 11 was completed, the compositions were aged at 40℃for 3 months, and the paste structures were observed, and the results are shown in Table 6.
Table 6:
Example 1 Example 2 Example 3 Comparative example 10 Comparative example 11
Dividing water 4 2
Paste is difficult to extrude 3
As can be seen from Table 6, examples 1 to 3 all had no water separation and paste hardly extruded, and comparative example 10 had no paste hardly extruded but water separation was severe, and comparative example 11 had both water separation and paste hardly extruded. That is, the paste structure of the oral care composition is stable when the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of potassium pyrophosphate is in the range of 1:0.41-1:1.09 under the condition that the thickening agents are all xanthan gum.
Examples 4 to 5, comparative examples 12 to 15
Oral care compositions of examples 4-5 and comparative examples 12-15 were prepared according to the formulation of Table 7, where the data are all parts by weight, totaling 100 parts.
Table 7:
as can be seen from table 7, examples 4 to 5 and comparative examples 12 to 15 each added 0.2% zinc citrate and 0.05% stannous fluoride, and all used xanthan gum as a thickener, except that the types and amounts of pyrophosphates added were different, wherein:
example 4 was added with 0.48% of tetrapotassium pyrophosphate, and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:1.07;
Example 5 was added with 0.2% tetrapotassium pyrophosphate, and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:0.45;
comparative example 12 was added with 0.6% tetrapotassium pyrophosphate, and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:1.34;
Comparative example 13 was added with 0.4% tetrapotassium pyrophosphate, and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:0.23;
comparative example 14 was added with 0.39% tetrasodium pyrophosphate, and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:1.08;
comparative example 15 was added with 0.4% of tetrapotassium pyrophosphate, and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:0.48;
After the preparation of examples 4 to 5 and comparative examples 12 to 15 described above was completed, the composition was aged at 40℃for 3 months, and the paste structure was observed, and the results are shown in Table 8.
Table 8:
Example 4 Example 5 Comparative example 12 Comparative example 13 Comparative example 14 Comparative example 15
Dividing water 1 3 2 1
Paste is difficult to extrude 3 1 2
As can be seen from table 8:
Examples 4-5 all have no water diversion and paste extrusion difficulty;
Comparative example 13 has no paste extrusion problem but has water separation phenomenon;
Comparative example 12, comparative example 14 and comparative example 15 all had various degrees of water separation and paste difficult extrusion.
Namely, when tetrapotassium pyrophosphate is added to the oral care composition and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate is in the range of 1:0.41 to 1:1.09, the composition is structurally stable, whereas when tetrasodium pyrophosphate is added to the oral care composition, even if the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate is in the range of 1:0.41 to 1:
within 1.09, the oral care composition still has problems of water separation and difficult paste extrusion.
Examples 6 to 7
The oral care compositions of examples 6-7 were prepared according to the formulation of Table 9, where the data are all parts by weight and total 100 parts.
Table 9:
Example 6 Example 7 Comparative example 16 Comparative example 17
Sorbitol 50 50 50 50
Zinc citrate 1 1 1 1
Xanthan gum 0.3 0.8 0.2 0.9
Tetrapotassium pyrophosphate 2.5 2.5 2.5 2.5
Silica dioxide 22 22 22 22
Stannous fluoride 0.5 0.5 0.5 0.5
Saccharin sodium salt 0.25 0.25 0.25 0.25
Sodium lauryl sulfate 2.2 2.2 2.2 2.2
Essence 1.2 1.2 1.2 1.2
Deionized water Added to 100% Added to 100% Added to 100% Added to 100%
As can be seen from table 9, examples 6 to 7 each added 1% zinc citrate, 0.5% stannous fluoride and 2.5% tetrapotassium pyrophosphate, and each used xanthan gum as a thickener, except that the added xanthan gum was at different concentrations, wherein:
Example 6 added 0.3% xanthan gum;
example 7 added 0.8% xanthan gum;
After the preparation of examples 6 to 7 and comparative examples 12 to 15 described above was completed, the composition was aged at 40℃for 3 months, and the paste structure was observed, and the results are shown in Table 10.
Table 10:
Example 6 Example 7 Comparative example 16 Comparative example 17
Dividing water 2
Paste is difficult to extrude 2
As can be seen from Table 10, examples 6 to 7 all had no water separation and paste hardly extruded, whereas comparative example 16 had no paste hardly extruded, but the paste was water-separated, and comparative example 17 had no water separation but the paste hardly extruded, i.e., the paste structure of the composition remained stable only when the addition amount of xanthan gum was in the range of 0.3 to 0.8%.
Examples 8 to 11
The oral care compositions of examples 8-11 were prepared according to the formulation of Table 11, where the data are all parts by weight and total 100 parts.
Table 11:
As can be seen from table 11, examples 8-11 used a combination of different zinc ion sources and stannous ion sources, wherein:
example 8 comprises 2% zinc citrate and 0.1% stannous chloride, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate being 1:0.91;
example 9 comprises 2% zinc gluconate and 0.1% stannous chloride, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate being 1:0.74;
Example 10 comprises 1% zinc citrate and 0.1% stannous chloride, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate being 1:0.78;
Example 11 contains 1% zinc chloride and 0.1% stannous chloride, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate being 1:0.46;
The paste structures of the compositions of examples 8 to 11 were observed by aging at 40℃for 3 months, and the results are shown in Table 12.
Table 12:
Example 8 Example 9 Example 10 Example 11
Dividing water
Paste is difficult to extrude
As can be seen from Table 12, examples 8-11 all had no water distribution and paste extrusion difficulties, i.e., the composition structure was stable when different zinc ion sources and different stannous ion sources were selected.
Comparative example 18
Comparative example 18 oral care compositions were prepared according to the formulation of table 13, and for ease of comparison, the compositions of examples 1-3, comparative examples 1-2, comparative example 10 and comparative example 11 are shown in table 13, where the data are in parts by weight and total 100 parts.
Table 13:
As can be seen from Table 13, examples 1-3, comparative examples 1-2, comparative examples 10-11 and comparative example 16 each had 2% zinc citrate and 0.1% stannous fluoride added thereto, except that:
example 1 added 0.6% xanthan gum and 2.5% tetrapotassium pyrophosphate, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:0.68;
example 2 was added with 0.6% xanthan gum and 1.5% tetrapotassium pyrophosphate, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate being 1:0.41;
Example 3 added 0.6% xanthan gum and 4% tetrapotassium pyrophosphate, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:1.09;
Comparative example 1 was added with 0.6% carrageenan and 2.5% tetrapotassium pyrophosphate, and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:0.68;
comparative example 2 to which 0.6% of cellulose gum and 2.5% of tetrapotassium pyrophosphate were added, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:0.68;
comparative example 10 to which 0.6% xanthan gum and 1.2% tetrapotassium pyrophosphate were added, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:0.36;
Comparative example 11 to which 0.6% xanthan gum and 4.2% tetrapotassium pyrophosphate were added, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:1.15;
Comparative example 18 with comparative example 2 with 0.6% xanthan gum and 2% tetrasodium pyrophosphate added, the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate was 1:0.68, which is equivalent to example 1;
table 13 after the preparation of examples and comparative examples was completed, the plaque-inhibiting effect of the above examples and comparative examples was evaluated by the oral care composition in vitro plaque-inhibiting effect evaluation method, and the results are shown in table 14.
Table 14:
Example 1 Example 2 Example 3 Comparative example 1 Comparative example 2 Comparative example 10 Comparative example 11 Comparative example 18
OD630 0.531 0.561 0.557 0.675 0.701 0.82 0.736 0.684
As can be seen from Table 14, examples 1-3 have smaller OD 630 values than the other comparative examples, i.e., oral care compositions comprising a stannous ion source and a zinc ion source have better efficacy in inhibiting dental plaque growth when tetrapotassium pyrophosphate is added, xanthan gum is the thickener, and the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate is in the range of 1:0.41 to 1:1.09.
In the description of the present specification, descriptions of the terms "one embodiment," "some embodiments," "examples," "particular examples," or "some examples," etc., mean that a particular feature, material, or characteristic described in connection with the embodiment or example is included in at least one embodiment or example of the embodiments of the present specification. In this specification, schematic representations of the above terms are not necessarily directed to the same embodiment or example.
Furthermore, the various embodiments or examples described in this specification and the features of the various embodiments or examples may be combined and combined by those skilled in the art without contradiction. The above description is merely an embodiment of the present specification and is not intended to limit the present specification. Various modifications and changes may be made to the embodiments herein by those skilled in the art. Any modification, equivalent replacement, improvement, or the like, which is made within the spirit and principle of the embodiments of the present specification, should be included in the scope of the claims of the embodiments of the present specification.

Claims (10)

1. An oral care composition comprising a stannous ion source and a zinc ion source, comprising:
1) A stannous ion source;
2) A zinc ion source;
3) A thickener;
4) Tetrapotassium pyrophosphate;
5) An orally acceptable carrier;
wherein the thickener is xanthan gum.
2. The oral care composition according to claim 1, wherein the mass ratio of the xanthan gum in the oral care composition is 0.3-0.8%.
3. The oral care composition of claim 1 wherein the stannous ion source comprises one or more of stannous fluoride, stannous chloride, stannous pyrophosphate, stannous phosphate, stannous bromide, stannous iodide, stannous oxide, stannous sulfide, stannous metaphosphate, stannous acetate, stannous tartrate, stannous citrate, stannous malate, stannous malonate, stannous gluconate, stannous oxalate.
4. The oral care composition according to claim 1, wherein the stannous ion source is present in the oral care composition in an amount of from 0.05% to 0.8%, preferably from 0.1% to 0.5% by mass.
5. The oral care composition of claim 1 wherein the zinc ion source comprises one or more of zinc citrate, zinc chloride, zinc lactate, zinc nitrate, zinc acetate, zinc gluconate, zinc sulfate, zinc pyrophosphate, and zinc phosphate.
6. The oral care composition according to claim 1, wherein the zinc ion source is present in the oral care composition in an amount of from 0.1 to 2.0%, preferably from 0.2 to 2.0% by mass.
7. The oral care composition according to claim 1, wherein the tetrapotassium pyrophosphate comprises 0.2 to 4.0% by mass of the oral care composition.
8. The oral care composition of claim 1 wherein the ratio of the sum of the molar amounts of zinc element and tin element to the molar amount of pyrophosphate is in the range of 1:0.41 to 1:1.09.
9. A method of improving the structural stability of an oral care composition comprising a stannous ion source and a zinc ion source comprising the steps of:
Xanthan gum and tetrapotassium pyrophosphate are added to an oral care composition comprising a stannous ion source and a zinc ion source.
10. Use of an oral care composition comprising a stannous ion source and a zinc ion source for inhibiting the growth of dental plaque, wherein tetrapotassium pyrophosphate is added to the oral care composition and xanthan gum is used as a thickening agent.
CN202410339446.0A 2024-03-22 2024-03-22 Oral care compositions comprising stannous and zinc ion sources and methods of improving structural stability of the compositions Pending CN118415890A (en)

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