DESC:FIELD OF INVENTION:
The present invention relates to an oral care product used for preventing hypersensitivity in teeth more particularly to a mouth wash composition comprising synergistic combination of amino acid, fluoride salt and oxalate salt.
BACKGROUND: 5
Dentin Hypersensitivity is a very common clinical condition in the general population. It is described as a sharp pain arises for short period of time due to exposure of dentin in response to stimuli such as thermal, evaporative, tactile, osmotic or chemical. Dentinal tubules can be exposed due to various factors such as enamel loss or gingival recession and loss of cementum from root surfaces. The common treatment generally 10 involves use of desensitizing agents for pain relief. These Desensitizing agent act either via occluding dentinal tubule or by nerve depolarization. For examples:
US9468593B2 discloses an oral composition comprising hydroxyapatite, potassium nitrate, and calcium monohydrogen phosphate, wherein the composition has an increased ability to occlude dentinal tubules of a tooth and has an excellent inhibitory 15 effect on hypersensitivity.
US20170319455A1 discloses a method for occluding dentin tubules and remineralizing teeth with a toothpaste. The toothpaste may be applied onto a mouth tray and the teeth are contacted with the toothpaste present in the mouth tray
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wherein the toothpaste includes theobromine and at least one of a bioactive glass and hydroxyapatite.
US20200038300A1 discloses oral healthcare methods for the delivery of amorphous calcium phosphate (ACP) to an oral cavity. The prior art discloses a composition comprising amorphous calcium phosphate for use in the occlusion of dental tubules 5 and/or the deposition of remineralising agents on dental enamel.
US20220226233A1 discloses dental toothpaste formulation comprising 10% potassium nitrate and 0.5% of propolis; the propolis providing occlusion of tubules and the potassium nitrate providing depolarization of nerve membranes.
Several marketed products are also available for treatment of Dentin Hypersensitivity 10 such as Colgate’s Pro-Argin technology which comprises arginine and calcium carbonate which provides instant and long lasting relief from dentine hypersensitivity.
Listerine’s new mouth wash LISTERINE® SENSITIVITY, uses patented CRYSTAL BLOCK™ Technology comprising Dipotassium Oxalate Monohydrate which provides 24 hours’ protection for sensitive teeth by depositing stable crystals both on the surface of the 15 dentin and deep inside the tubules and blocking open tubules.
Sensodyne’s Mouth wash is an alcohol free mouth wash which contains 3% Potassium nitrate and 0.048% sodium fluoride which provide long lasting sensitivity and build soothing protection around the nerve.
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Although there are several Desensitizing agent present in market but none of these occluding/ desensitizing agents are completely effective in reducing dentinal sensitivity as effective occlusion on dentinal tubules is dependent on different variables. There is, therefore, a continuing need for tooth sensitivity treatment compositions, which have an improved affinity for dentin and effectively occlude 5 dentinal tubules.
Thus there is still a need in the art of composition that provides an increased ability to occlude dentinal tubules of a tooth, provide rapid relief from dentin sensitivity and prevents cavities. The present invention provides an oral care composition comprising synergistic combination of triple desensitizing/Occluding agents used within the 10 mouth of user to provide enhanced oral health.
Summary of the invention:
The present inventors have surprisingly found that the judicious selection of specific ingredients which provide complete protective barrier for teeth and effectively occlude exposed dentinal tubules and thereby decreasing dentinal sensitivity. The 15 present invention provides an oral care composition comprising synergistic combination of oxalate salt with amino acid and fluoride salt in a single composition. The improved oral care composition of present invention provides relief in sensitivity by blocking open tubules and forming a protective layer on the surface of exposed dentin and shielding the dentin from external stimuli. The synergistic combination of 20
5
amino acid with fluoride salt also provide anti-microbial effect and prevent dental caries.
The present invention provides a synergistic combination of oxalate salt, amino acid and fluoride salt as an oral care composition which is more effective in reducing dental hypersensitivity and dental carries as compared to existed marketed products. The 5 oral care composition achieves intrinsic blockage of dentinal tubes and at the same time provides antibacterial and anti-carries efficacy and helps in maintaining oral hygiene.
The invention further provides an oral care composition comprising, or more particularly consisting essentially of, a) from about 1-2% by volume of oxalate salt; b) 10 from about 0.5-1% by volume of amino acid or derivatives thereof c) from about 0.05-0.5% by volume of fluoride salt and one or more pharmaceutical acceptable carriers wherein oral care composition is a mouth wash.
DETAILED DESCRIPTION OF THE INVENTION
The following description of the preferred embodiment(s) is merely exemplary in 15 nature and is in no way intended to limit the disclosure, its application, or uses.
Unless otherwise specified, all percentages and amounts expressed herein and elsewhere in the specification should be understood to refer to percentages by weight
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of the entire composition. The amounts given are based on the active weight of the material.
As used herein, an “oral care composition” refers to a composition for which the intended use includes oral care, oral hygiene, and/or oral appearance, or for which the intended method of use comprises administration to the oral cavity, and refers to 5 compositions that are palatable and safe for topical administration to the oral cavity, and for providing a benefit to the teeth and/or oral cavity.
As used herein, “pharmaceutically acceptable carriers” refers to any vehicle useful in formulating the oral care compositions disclosed herein. The orally acceptable carrier is not harmful to a mammal in amounts disclosed herein when retained in the mouth 10 and do not show any pharmacological actions.
As used herein, desensitizing agent refers to any substance which are useful in preventing dentinal hypersensitivity either by occluding the dentinal tubules or by blocking the neural transmission.
The present invention provides a new and improved oral care composition that meets 15 the consumer’s requirements by providing increased desensitizing effect. It has been surprisingly discovered that synergistic combinations of oxalate salt, amino acid and fluoride salt provides superior effects as compared to existing products.
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The present invention provides an oral care composition comprising effective amount of oxalate salt, amino acid or derivatives thereof and fluoride salt.
The present invention provides an oral care composition comprises synergistic combination of:
a) from about 1-2% by volume of oxalate salt; 5
b) from about 0.5-1% by volume of amino acid or derivatives thereof;
c) from about 0.05-0.5% by volume of fluoride salt and
The composition in the present invention is useful for preventing hypersensitivity wherein combination of amino acid and fluoride salts have an anti-microbial effects and prevent dental carries. 10
In an embodiment the present invention comprises oxalate salt as a desensitizing agent selected from group consisting of sodium oxalate, lithium oxalate, Dipotassium oxalate, Potassium hydrogen oxalate, sodium hydrogen oxalate, lithium hydrogen oxalate, ammonium oxalate, Hydrogen oxalate or combination thereof wherein Dipotassium oxalate more preferably Dipotassium Oxalate Monohydrate is being 15 preferred.
In an another embodiment of the present invention comprises fluoride salt as desensitizing agent selected from group consisting of stannous fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluorosilicate,
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ammonium fluorosilicate, amine fluoride (e.g., N'-octadecyltrimethylendiamine-N,N,N'- tris(2-ethanol)-dihydrofluoride), ammonium fluoride, titanium fluoride, hexafluorosulfate or combination thereof wherein sodium fluoride is being preferred.
In an another embodiment of the present invention comprises amino acid as desensitizing agent selected from group consisting of lysine, glycine, arginine, 5 aspartic, glutamic acid or combinations thereof in free or orally acceptable salt form wherein arginine is being preferred.
In an another embodiment the present invention provides an oral care composition comprising:
a. Amino acid in free or salt form, wherein the amino acid is arginine present in 10 an amount of about 0.8%
b. Oxalate salt, wherein oxalate salt is Dipotassium Oxalate monohydrate present in an amount of about 1.4%
c. Fluoride salt, wherein fluoride salt is sodium fluoride present in an amount of about 0.2% 15
In an embodiment an oral care composition may be selected from group consisting of toothpaste or dentifrice, a mouthwash or a mouth rinse, a topical oral gel, and a denture cleanser wherein oral composition is in form of mouthwash.
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In an another embodiment the present invention provides oral mouthwash comprising:
a. L-arginine present in an amount of about 0.8% and;
b. Dipotassium Oxalate monohydrate present in an amount of about 1.4% and;
c. sodium fluoride present in an amount of about 0.2% 5
The present invention provides a mouthwash, the oral composition to the invention may be present with aqueous or alcoholic solutions containing different pharmaceutically acceptable vehicle or carriers wherein the present invention provides an alcohol free composition.
In an embodiment the mouthwash further comprises pharmaceutically acceptable 10 carriers selected from group consisting of humectant, stabilizer, flavouring agent, surfactant, preservative, foam booster, breath fresheners, cleaning agent, sweetening agent, colouring agent, alkalizer.
In an another embodiment the mouthwash further comprises humectants selected from group consisting of low molecular weight polyethylene glycols, propylene glycol, 15 glycerol, sorbitol, glycerin (glycerol), hydrogenated starch hydrolyzates or combinations thereof wherein propylene glycol is being preferred as humectant.
In an embodiment humectant is present in an amount ranging from 2-10 % more particularly about 4% w/v.
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In an another embodiment the mouthwash further comprises flavouring agent selected from group consisting of one or more flavouring agent such as but not limited to Peppermint oil, spearmint oil, eucalyptus oil, aniseed oil, fennel oil, caraway oil, menthyl acetate, cinnamic aldehyde, anethole, fresh mint, vanillin, thymol wherein fresh mint is being preferred. 5
In an embodiment the flavouring agent is present in an amount ranging from 0.5-2% more particularly about 1.5 % w/v.
In an another embodiment the mouthwash further comprises surfactant selected from group consisting of one or more but not limited to alkyl polyglucosides; sodium lauryl sulphate, block copolymers such as ethylene oxide and propylene oxide 10 copolymers e.g. Poloxamers; ethoxylated hydrogenated castor oils and/or ethoxylated sorbitan esters such as PEG-80 sorbitan laurate, fatty alcohol ethoxylates; polyethylene oxide condensates of alkyl phenols or combinations thereof wherein poloxamers and sodium lauryl sulphate is being preferred.
In an embodiment the surfactant is present in an amount ranging from 0.005-0.5% 15 w/v more particularly about 0.1% w/v.
In an another embodiment the mouthwash further comprises preservative selected from group consisting of benzoic acid, methylparaben, propylparaben, or sodium benzoate or combinations thereof wherein sodium benzoate is being preferred.
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In an embodiment the preservatives are present in an amount ranging from 0.05-0.5% w/v more particularly about 0.250% w/v.
In an another embodiment the mouthwash further comprises sweetening agents selected from group consisting of sodium saccharin, xylitol, erythritol, sucralose, aspartame wherein sucralose and sodium saccharin is being preferred. 5
In an embodiment the sweetening agents are present in an amount ranging from 0.005-20 % w/v.
In an another embodiment the mouthwash further comprises coloring agent, alkalizer, cleaning agent and breath fresheners.
In an embodiment coloring agent is sunset yellow present in an amount ranging from 10 about 0.001-0.5 % more particularly about 0.2 % w/v.
In an embodiment alkalizer is selected from phosphoric acid present in an amount ranging from about 0.1-1 % more particularly about 0.600% w/v.
In a further embodiment the mouthwash comprises purified water as a vehicle.
In an another embodiment the mouth wash has pH in range between 4 to 7. 15
In an embodiment the present invention provides an oral mouth wash comprises:
i. about 2 to 10% w/v humectant;
ii. about 0.005-0.5% w/v surfactant and;
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iii. about 0.05-0.5% preservatives and;
iv. about 0.05-2% w/v foam booster and;
v. about 0.005-20 % w/v sweetening agents and;
vi. about 0.001-0.05% w/v coloring agent and;
vii. about 0.1-0.5% w/v alkalizer and; 5
viii. about 0.5-2% w/v flavouring agent
in an another embodiment the present invention provides an oral mouth wash composition comprises:
i. Propylene glycol as humectant present in an amount of about 4% w/v and;
ii. Fresh mint as flavouring agent present in an amount about 1.50 % w/v and; 10
iii. Poloxamer and sodium lauryl sulphate as surfactant present in an amount about 0.100% w/v;
iv. Sodium benzoate as preservative present in an amount about 0.250% w/v and;
v. Sodium Methyl Cocyl Taurate as foam booster present in an amount about 15 0.1% w/v
vi. Combination of sorbitol, sucralose and sodium saccharin as sweeteners
The present invention provides process of manufacturing mouth wash comprising following steps:
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1. Preparation of aqueous phase by dissolving sodium benzoate, saccharin sodium in purified water and;
2. Addition of Dipotassium oxalate monohydrate to aqueous phase and;
3. Addition of sorbitol solution 70% to the aqueous phase obtain from step-2 and; 5
4. Preparation of sodium fluoride in separate container and adding in aqueous phase obtain from step-3 and;
5. Preparation of L-arginine in a separate container and adding in aqueous phase obtain from step-4 and;
6. Preparation and addition of surfactant phase to an aqueous phase obtain from 10 step-5 and;
7. Adding flavouring agent and propylene glycol to aqueous phase obtained from step-6 and
8. Adjusting the pH of the mouth wash obtain from step-7 and optionally adding coloring agent. 15
In an another embodiment the present invention provides process of manufacturing mouth wash comprising following steps:
A. Preparation of aqueous phase:
Sodium benzoate, saccharin sodium and sucralose was dissolved in purified water with continuous stirring till a clear solution was obtained. To this 20
14
solution add Dipotassium oxalate monohydrate with sorbitol solution to obtain clear solution. Sorbitol solution 70% was added to the solution with continuous stirring.
B. In a separate container dissolve sodium fluoride in purified water with continuous stirring to obtain a clear solution and mix this solution to above 5 aqueous phase obtained in Step-A.
C. In a separate container dissolve L-arginine was dissolved in purified water with continuous stirring till a clear solution was obtained and was added to aqueous phase obtained in Step-B.
D. Preparation of surfactant Phase: 10
In a separate container Poloxamer 407, sodium lauryl sulphate and sodium methyl cocoyl taurate was dissolved with continuous stirring to obtain surfactant phase.
E. Addition of aqueous Phase and surfactant phase:
The surfactant phase obtained in Step-D was added into the aqueous phase obtained from Step-C with continuous stirring to obtain a clear solution. 15
F. In a separate container Flavouring agent and propylene glycol was mixed well and was transferred to solution obtain from Step-E to obtain clear liquid,
G. pH adjustment:
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Phosphoric acid solution was added to clear liquid obtained from Step-F to adjust the pH of mouth wash.
H. Colour was added to the mouth wash obtained from step G and water was added to volume makeup the mouth wash
EXAMPLES: 5
The following examples and descriptions further clarify embodiments within the scope of the present invention. These examples are given solely for the purpose of illustration and are not to be construed as limitations of the present invention as many variations thereof are possible without departing from the spirit and scope.
Example 1: Mouth Wash 10
Table 1: Mouth wash composition
Ingredients
% w/v
Functions/Uses
Arginine
0.8
Active agent
Dipotassium Oxalate Monohydrate
1.400
Active agent
Sodium Fluoride
0.2
Active agent
Sorbitol Solution 70% NC
14.00
Sweetener
Propylene glycol
4.00
Humectant
Flavour Freshmint
1.50
Flavouring agent
Poloxamer
0.100
Surfactant/solubilizer
16
Sodium Benzoate
0.250
Preservative
Sodium Methyl Cocyl Taurate
0.100
Foam booster
Sodium Lauryl Sulphate
0.100
surfactant
Sucralose
0.025
Sweetening Agent
Sodium Saccharin
0.050
Sweetening Agent
Col. Sunset yellow
0.2
Colouring Agent
Phosphoric Acid
0.600
Alkalizer
Purified Water
q.s. to 100
Vehicle
Example-2 Stability Study:
The mouth wash prepared from example-1 was subjected for stability study when stored at temperature 40°C ± 2°C & RH 75% ± 5%.
Table 2: Stability study: 5
Test
Acceptance criteria
Initial Testing
01 months
Description
Light blue colour, clear liquid filled in clear PET bottle
Light blue coloured, clear liquid filled in clear PET bottle
Light blue coloured, clear liquid filled in clear PET bottle
pH
Between 4.00 to 7.00
6.02
5.376
Weight per ml
Between 0.900 gm/ml to 1.100 gm/ml
1.0522 gm/ml
1.0537 gm/ml
Microbial contamination
Total viable count
Not more than 100 cfu/ml
<10 cfu/ml
-
Total aerobic bacterial count
Not more than 10 cfu/ml
<10 cfu/ml
-
Tests for specified microorganism
Escherichia coli
Should be absent/ml
absent/ml
-
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Salmonella
Should be absent/10 ml
absent/10 ml
-
Pseudomonas aeruginosa
Should be absent/ml
absent/ml
-
Staphylococcus aureus
Should be absent/ml
absent/ml
-
Assay:
Dipotassium oxalate monohydrate 1.4% w/v
Not less than 1.26 % w/v & not more than 1.54 % w/v
(Not less than 90.00% & not more than 110.00% of label claimed)
1.3683 w/v
(97.74%)
1.373 w/v
(98.07%)
Arginine 0.8% w/v
(By HPLC)
Not less than 0.72% w/v & not more than 0.88% w/v
(Not less than 90.00% & not more than 110.00% of label claimed)
0.783 w/v
(97.82 %)
0.7834 w/v
(97.93 %)
Sodium fluoride 0.2% w/v
(By fluoride ion meter)
Not less than 0.18% w/v & not more than 0.22% w/v
(Not less than 90.00% & not more than 110.00% of label claimed)
0.2025 w/v
(101.25%)
0.1962 w/v
(98.10%)
Sodium benzoate IP
0.25% w/v (As preservative) (by HPLC)
Not less than 0.20 % w/v & not more than 0.30 % w/v
(Not less than 80.00% & not more than 120.00% of label claimed)
0.2474 w/v
(99.04%)
0.2458 w/v
(98.32%)
From Table 2 it was clear that the mouth wash prepared from example-1 was found to stable for 1 month when stored at temperature 40°C ± 2°C & RH 75% ± 5%.
Example-3: Process of manufacturing
A. Preparation of aqueous phase: 5
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Sodium benzoate, saccharin sodium and sucralose was dissolved in purified water with continuous stirring till a clear solution was obtained. To this solution add Dipotassium oxalate monohydrate with sorbitol solution to obtain clear solution. Sorbitol solution 70% was added to the solution with continuous stirring. 5
B. In a separate container dissolve sodium fluoride in purified water with continuous stirring to obtain a clear solution and mix this solution to above aqueous phase obtained in Step-A.
C. In a separate container dissolve L-arginine was dissolved in purified water with continuous stirring till a clear solution was obtained and was added to 10 aqueous phase obtained in Step-B.
D. Preparation of surfactant Phase:
In a separate container Poloxamer 407, sodium lauryl sulphate and sodium methyl cocoyl taurate was dissolved with continuous stirring to obtain surfactant phase.
E. Addition of aqueous Phase and surfactant phase: 15
The surfactant phase obtained in Step-D was added into the aqueous phase obtained from Step-C with continuous stirring to obtain a clear solution.
F. In a separate container Flavouring agent and propylene glycol was mixed well and was transferred to solution obtain from Step-E to obtain clear liquid,
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G. pH adjustment:
Phosphoric acid solution was added to clear liquid obtained from Step-F to adjust the pH of mouth wash.
H. Colour was added to the mouth wash obtained from step G and water was added to volume makeup the mouth wash. ,CLAIMS:1. An oral care composition comprising effective amount of oxalate salt, amino acid or derivatives thereof and fluoride salt.
2. An oral care composition as claimed in claim 1, wherein the composition comprises synergistic combination of: 5
a. from about 1-2% by volume of oxalate salt and;
b. from about 0.5-1% by volume of amino acid or derivatives thereof and;
c. from about 0.05-0.5% by volume of fluoride salt
3. An oral care composition as claimed in claim 2, provides an oral care composition comprising: 10
a. Amino acid in free or salt form, wherein the amino acid is arginine present in an amount of about 0.8%
b. Oxalate salt, wherein oxalate salt is Dipotassium Oxalate monohydrate present in an amount of about 1.4%
c. Fluoride salt, wherein fluoride salt is sodium fluoride present in an 15 amount of about 0.2%
4. An oral care composition as claimed in previous claim may be selected from group consisting of toothpaste or dentifrice, a mouthwash or a mouth rinse, a topical oral gel, and a denture cleanser wherein oral composition is in form of mouthwash. 20
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5. An oral care composition as claimed in previous claim is a mouth wash comprising:
a. L-Arginine present in an amount of about 0.8% and;
b. Dipotassium Oxalate monohydrate present in an amount of about 1.4% and; 5
c. sodium fluoride present in an amount of about 0.2%
6. An oral mouth wash as claimed in claim 5 further comprises one or more comprises pharmaceutically acceptable carriers selected from group consisting of humectant, stabilizer, flavouring agent, surfactant, preservative, breath fresheners, cleaning agent, sweetening agent, colouring agent, 10 alkalizer.
7. An oral mouth wash as claimed in claim 6 comprises:
a. about 2 to 10% w/v humectant;
b. about 0.005-0.5% w/v surfactant and;
c. about 0.05-0.5% preservatives and; 15
d. about 0.05-2% w/v foam booster and;
e. about 0.005-20 % w/v sweetening agents and;
f. about 0.001-0.5% coloring agent and;
g. about 0.1-1 % alkalizer and;
h. about 0.5-2% flavouring agent 20
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8. An oral mouth wash as claimed in claim 7 comprises:
a. Propylene glycol as humectant present in an amount of about 4% w/v and;
b. Fresh mint as flavouring agent present in an amount about 1.50 % w/v and; 5
c. Poloxamer and sodium lauryl sulphate as surfactant present in an amount about 0.100% w/v and;
d. Sodium benzoate as preservative present in an amount about 0.250% w/v and;
e. Sodium Methyl Cocyl Taurate as foam booster present in an amount 10 about 0.1% w/v
f. Combination of sorbitol, sucralose and sodium saccharin as sweeteners
9. An oral mouth wash as claimed in claim 1-8, the pH of mouth wash has pH range in between 4 to 7 and is alcohol free. 15
10. A process of manufacturing mouth wash comprising following steps:
a) Preparation of aqueous phase by dissolving sodium benzoate, saccharin sodium in purified water and;
b) Addition of Dipotassium oxalate monohydrate to aqueous phase and;
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c) Addition of sorbitol solution 70% to the aqueous phase obtain from step-b and;
d) Preparation of sodium fluoride in separate container and adding in aqueous phase obtain from step-c and;
e) Preparation of L-arginine in a separate container and adding in aqueous 5 phase obtain from step-d and;
f) Preparation and addition of surfactant phase to an aqueous phase obtain from step-e and;
g) Adding flavouring agent and propylene glycol to aqueous phase obtained from step-f and 10
h) Adjusting the pH of the mouth wash obtain from step-f and optionally adding coloring agent