DESC:FIELD OF INVENTION
The present invention relates to the field of oral care products, and more particularly to a mouthwash for maintaining oral hygiene and prevent dryness of mouth.

BACKGROUND:
Maintaining good oral health is a necessary to keep the gums and teeth healthy, as 5 mouth is habitat for billions of bacteria. Sometimes these bacteria build up plaque, causing tooth decay (cavities) and gingivitis, which can lead to periodontal (gum) disease. Thus practicing a good oral hygiene such as regular brushing and flossing with regular dental checkup is essential in keeping your teeth free from decay, plaque buildup and infections. Regular brushing and flossing alone is not sufficient and 10 dentist recommended use of oral products such as mouth rinses or washes to prevent dental plaque, infections and prevent the growth of bacteria and dental caries.
However, regular or overuse of alcohol-based mouthwashes can causes drying of mouth and reduces salivary flow causing dental caries, periodontal infections, cavities, dental plaque, mouth ulcers and bread breath, this condition is also known 15 as Xerostomia. The treatment for dry mouth generally involved methods to increase saliva production. Several prior art compositions tried to solve the problem by means of different approaches such as:
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US8173711B2 discloses composition capable of relieving or preventing xerostomia comprising an oxidized coenzyme Q and/or a reduced coenzyme Q as active ingredients.
US20110300241A1 discloses an oral care composition for promoting salivary flow comprises all-natural ingredients, including, for example, green tea polyphenols and 5 jaborandi extract.
CA3169206A1 discloses an oral rinse composition for alleviating xerostomia comprising a polyethylene glycol derivative as an active ingredient. The polyethylene glycol derivative allows covalent bonding of the composition to the oral mucosa without irritation to increase the oral moisturizing capacity, but also allows easy 10 manufacture and packaging by having a granule formulation, as well as being advantageous for storage and use.
Although there are several prior arts which tried to manage the dry mouth however the prior art focuses only on increasing or stimulating saliva secretion but does not focuses on other dental problem such as tooth decay, gum disease, cavities and other 15 periodontal diseases.
Therefore, there is unmet need of an improved oral product which effectively inhibit the formation of plaque, caries and prevent the decay of teeth, reduces inflammation
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and bleeding and also useful in managing or alleviating the symptoms associated with over use of alcohol based mouth wash such as dry mouth or Xerostomia.
The present invention not only helps in alleviating the dental problems such as oral plaque, gingivitis or other mouth infections but also treat or prevent xerostomia. The present invention provides a synergistic combination of one or more oral care agents 5 and a moisturizer wherein moisturizer protect and lubricate the oral mucosa and provide an additional advantage protection against dental disease and provide a favorable environment for tissue protection and repair.
SUMMARY OF THE INVENTION:
The present invention disclosed a dental composition comprising synergistic 10 combination of one or more oral care agents and a moisturizer wherein the oral care agents prevents or eliminates gingivitis, periodontitis, mouth ulcer, plaque and a moisturizer which coats and hydrates the oral mucosa and provide additional lubrication and provide relief from dry mouth.
The disclosed moisturizers also provide additional benefits i.e. it inhibits plaque 15 growth with anti-inflammatory, antioxidant and bacteriostatic properties.
The present invention provides an improved oral care composition comprising one or more oral care agents selected from chlorhexidine gluconate, fluoride and Zinc salts and moisturizers is hyaluronic acid wherein synergistic combinations of chlorhexidine
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gluconate, fluoride and Zinc salts wherein chlorhexidine gluconate act as antiseptic agent which reduces the growth of bacteria in the mouth and can be used to treat gingivitis; Fluoride salts helps in preventing cavities and protect the teeth from acid demineralization and Zinc chloride act as mild antiseptic which control plaque, reduce malodor and inhibit calculus formation and Hyaluronic acid (HA) provides oral comfort 5 and provide oral lubrication and hydrates the oral mucosa and provide relief from dry mouth. With its novel features, the oral care composition of the present invention comprises synergistic combinations of chlorhexidine gluconate, sodium fluoride, zinc chloride and Hyaluronic acid (HA) effective at preventing or controlling the dental problems 10 and also treat problem associated with post rinse drying.
The present invention thus generally relates to oral care composition for maintaining oral hygiene and prevent dry mouth and provides method of preparation thereof.
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, “Xerostomia” also called “Dry mouth” is a condition of dryness in mouth occurs due to reduced or absent of saliva flow.
As used herein, "oral diseases" refers to diseases and disorders affecting the oral cavity or associated medical conditions. Oral diseases include, but are not limited to, 15 dental caries; and periodontal diseases. (e.g., gingivitis, adult periodontitis, early- onset periodontitis etc.) As used herein, the term "gingivitis" refers to inflammation of gingival tissue without loss of connective tissue.
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As used herein, the term "periodontitis" refers to inflammation and loss of connective tissue of the supporting or surrounding structure of teeth with loss of attachment.
The present invention provides an oral care product comprising synergistic combination comprising therapeutic effective amount of one or more oral care agents and a moisturizer. 5
The oral care composition as envisaged herein may preferably be a mouth wash, a tooth paste or tooth gel, a mouth spray, a powder, dental cream. In a preferred embodiment oral care composition is mouth wash.
The oral care composition comprising one or more oral care agents and a moisturizer wherein one or more oral care agents is selected from Chlorhexidine Gluconate, 10 fluoride salt and zinc salt and moisturizer is Hyaluronic acid.
In an another embodiment, the oral care composition is a mouthwash comprising an effective amount of one or more oral care agents and a moisturizer wherein one or more oral care agents is selected from Chlorhexidine Gluconate, fluoride salt and zinc salt and moisturizer is Hyaluronic acid. 15
In an embodiment fluoride salt is selected from group consisting of stannous fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate, amine fluoride (e.g., N'-octadecyltrimethylendiamine-N,N,N'- tris(2-ethanol)-dihydrofluoride), ammonium
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fluoride, titanium fluoride, hexafluorosulfate or combination thereof wherein sodium fluoride is being preferred.
In an another embodiment zinc salt is selected from group consisting of zinc nitrate, zinc chloride, zinc sulfate, zinc phosphate, zinc molybdate, zinc chromate, zinc ricinoleate or combinations thereof wherein zinc chloride is being preferred. 5
In an another embodiment the present invention provides a mouth wash comprising synergistic combinations of:
a. an effective amount of Chlorhexidine Gluconate and;
b. an effective amount of zinc chloride and;
c. an effective amount of sodium fluoride and; 10
d. an effective amount of Hyaluronic acid
In an another embodiment the Chlorhexidine Gluconate is present in an amount ranging from 0.05 to 1% w/v.
In one embodiment zinc chloride is present in an amount ranging from 0.05 to 2% w/v. 15
In in another embodiment sodium fluoride is present in an amount ranging from 0.05 to 5% w/v.
In an another embodiment Hyaluronic acid is present in an amount ranging from 0.05 to 1% w/v.
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The present invention provides mouth wash comprising:
a. about 0.2% w/v Chlorhexidine Gluonate and;
b. about 0.09% w/v Zinc chloride and;
c. about 0.05% w/v Sodium fluoride and;
d. about 0.1% w/v Hyaluronic acid 5
The mouthwash of the invention may further comprise additives like flavouring agent, cooling agent, sweetener, anti-staining agent, humectant, surfactant, solubilizer, preservative, wetting agent, coloring agent and vehicle.
In an another embodiment the mouth wash comprises flavouring agent selected from group consisting of spearmint, peppermint, wintergreen, sassafras, clove, sage, 10 eucalyptus, marjoram, cinnamon, lemon, lime, grapefruit, orange, menthol, carvone, and anethole or combinations thereof more preferably spearmint and menthol wherein menthol also provide cooling effects to user after application.
In an another embodiment the mouth wash further comprises saccharin, sodium saccharate, xylitol, stevioside, extract of stevia, revaudioside, p-methoxy cinnamic 15 aldehyde, neohesverisyl hydroxy carcon, perillartine, thaumatin, glycyrrhizin, monoglucoside glycyrrhizinate, hernandulcin, trehalose, aspartame and sorbitol or combinations thereof more preferably aspartame and sorbitol wherein sorbitol have additional role as a Moisturizing agent.
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In an embodiment aspartame also impart sweetness to the mouth wash.
In an another embodiment the present invention further comprises Anti-staining agent which prevents the staining of teeth caused by the regular use of chlorhexidine wherein anti-staining agent is citric acid.
In an embodiment the mouth wash further comprises propylene glycol or 5 polyethylene glycol as wetting agent.
In an another embodiment the mouth wash further comprises humectant. The humectant serves to give mouthwash a moist feel to the mouth. Certain humectants can also impart desirable sweetness of flavor to toothpaste and mouthwash compositions. Suitable humectants for use in compositions of the present invention 10 include edible polyhydric alcohols such as glycerin, sorbitol, xylitol, polyethylene glycol, and propylene glycol more preferably glycerin.
In an another embodiment the mouth wash further comprises preservative that prevent microbial growth in the compositions. Suitable preservatives include, but are not limited to, methylparaben, propylparaben, benzoates, and alcohols such as 15 ethanol or combinations thereof wherein mouth wash comprises combinations of methyl paraben and propyl paraben most preferably Sodium Methyl Paraben and Sodium Propyl Paraben.
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In an another embodiment the mouth was further comprises surfactant selected from sodium alkyl sulfate, sodium lauroyl sarcosinate, cocoamidopropyl betaine, polysorbate 20, lauryl trimethylammonium chloride, cetyl pyridinium chloride, cetyl trimethylammonium bromide, di-isobutylphenoxyethyldimethylbenzylammonium chloride, coconut alkyltrimethylammonium nitrite, cetyl pyridinium fluoride or 5 combinations thereof wherein surfactant is polysorbate 20.
In an another embodiment the mouth wash further comprises one or more solubilizer selected from but not limited to Caprylyl/Capryl Glucoside; sodium Cocoyl Glutamate; Glyceryl Caprylate; Citric Acid; Polyglyceryl-6 Oleate; Polyoxyl 35 castor oil (cremophor), Polyglyceryl-10 Caprylate, Poloxamer, sodium surfactin or combinations 10 thereof.
The mouthwash of present invention typically involves application of the composition to the oral cavity, for a recommended time period before being expectorated. Preferred application times are from 10 to 60 seconds.
In an another embodiment the mouth wash comprises: 15
i. Chlorhexidine Gluconate present in an amount ranging from 0.05 to 1% w/v and;
ii. zinc chloride present in an amount ranging from 0.05 to 2% w/v.
iii. sodium fluoride present in an amount ranging from 0.05 to 5% w/v.
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iv. preservative present in an amount ranging from 0.005 to 5 % w/v
v. humectant present in an amount ranging from 5 to 10% w/v and;
vi. solubilizer present in an amount ranging from 0.5 to 10% w/v and;
vii. surfactant present in an amount ranging from 2 to 10% w/v
In an another embodiment the present invention provides process of manufacturing 5 mouth comprising following process:
a. Preparation of aqueous phase by dissolving poloxamer in water with continuous stirring until a clear solution is obtained and;
b. Addition of Zinc chloride and sodium fluoride one by one into aqueous phase with continuous stirring and; 10
c. Addition of sorbitol solution and glycerin to the solution obtained from step-b with continuous stirring and;
d. Preparation of preservative phase by adding sodium methyl paraben and sodium propyl paraben one by one into solution obtained in step-c until a clear solution is obtained and; 15
e. Add aspartame into above solution with continuous stirring and transfer into main manufacturing vessel;
f. Addition of Chlorhexidine gluconate solution in main manufacturing vessel with continuous stirring and;
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g. Preparation and addition of Hyaluronic acid phase by slowly dissolving hyaluronic acid into separate container with continuous stirring and then transfer it in main manufacturing vessel with continuous stirring;
h. pH is adjusted to the mouth wash obtained in step g with citric acid solution and 5
i. optionally adding colouring agent and makeup the volume with purified water.
The following examples are provided to more specifically recite the elements and preparation of the mouthwash formulation of the present invention. They are for illustrative purposes only, and it is recognized that many variations may be formulated 10 to change or alter the composition to a degree. It is understood however that such alterations will still be considered to fall within the spirit and scope of the invention as recited by the claims that follow.
This invention is further defined by reference to the following examples. Although the examples are not intended to limit the scope of the present invention, they should be 15 considered in the light of the description detailed above.
EXAMPLE-I:
Mouthwash compositions having the ingredients shown in table 1 below were prepared.
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Table 1: Composition details of mouth wash:
Ingredients
Percent (w/v)
Function
Chlorhexidine gluconate
0.20
Active agent
Sodium Fluoride
0.05
Active agent
Zinc Chloride
0.09
Active agent
Hyaluronic Acid
0.1
Active agent
Menthol IP
0.1
Flavouring agent
Aspartame (Powder Form)
0.02
Sweetener
Citric Acid monohydrate
0.1
anti-staining agent
Glycerin
8.00
humectant
Sodium Methyl Paraben
0.1
preservative
Sodium Propyl Paraben
0.01
preservative
Sorbitol Solution 70%
12.00
humectant
cremophor
1.00
solubilizer
Polysorbate 20 (Tween-20)
3.85
surfactant
Spearmint
0.300
Flavouring agent
Col. Fast Green FCF
0.001
Coloring agent
Purified Water
As required
vehicle
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EXAMPLE-II STABILITY STUDY:
The formulation prepared by example-1 of were subjected to stability study for physiochemical test at temperature 40°C ± 2° C & RH 75% ± 5%
Table 2: Stability study of mouth wash
Test
Acceptance criteria
Initial testing
1 month
3 month
6 month
Description
Light greenish blue color solution filled in transparent PET bottle
Light greenish blue color solution filled in transparent PET bottle
Light greenish blue color solution filled in transparent PET bottle
Light greenish blue color solution filled in transparent PET bottle
Light greenish blue color solution filled in transparent PET bottle
pH
Between 4.00 to 6.00
4.68
4.949
4.818
4.831
Weight/ml
Between 1.00 to 1.10 gm/ml
1.053
1.0554
1.0563
1.0536
4-chloroaniline (by HPLC)
Not more than 0.3 % w/w
0.079%
0.096%
0.120%
0.146%
Microbial contamination
As below
Total viable count
As below
Total aerobic bacterial count
Not more than 100 cfu/gm
Not more than 10 cfu/gm
-
-
-
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Total combined yeast & mould count
Not more than 10 cfu/gm
Not more than 10 cfu/gm
-
-
-
Test for specified microorganism
As below
Escherichia coli
Should be absent/gm
Absent/gm
-
-
-
salmonella
Should be absent/10 gm
Absent/10 gm
-
-
-
shigella
Should be absent/10 gm
Absent/10 gm
-
-
-
Staphylococcus aureus
Should be absent/gm
Absent/gm
-
-
-
Pseudomonas aeruginosa
Should be absent/gm
Absent/gm
-
-
-
Assay
Shelf Life limit
Chlorhexidine gluconate sol. IP Eq. to chlorhexidine Gluconate………… 0.20% w/v (by HPLC)
Not more than 0.19% w/v & not more than 0.21% w/v (not less than 95% & not more than 105% of the label claim)
0.2005 % w/v
100.25%
0.1982% w/v
99.10%
0.2010 % w/v
100.50 %
0.1978% w/v
98.90%
The mouth wash of the present invention was found to be stable when stored at temperature 40°C ± 2° C & RH 75% ± 5% for 6 months. ,CLAIMS:We claim:
1. An oral care composition comprising therapeutic effective amount of one or more oral care agents is selected from Chlorhexidine Gluconate, fluoride salt and zinc salt, and moisturizer agent.
2. An oral care composition as claimed in claim 1 wherein Chlorhexidine gluconate is present in the amount of ranging from 0.05 to 1% w/v, fluoride salt is present in the amount of 0.05 to 5% w/v and zinc salt present in the range of 0.05 to 2% w/v.
3. An oral care composition as claimed in claim 1 wherein the moisturizer agent is Hyaluronic acid and wherein Hyaluronic acid is present in the range of 0.05 to 1% w/v.
4. An oral mouth wash as claimed in claim 1 comprises:
i. Chlorhexidine Gluconate present in an amount ranging from 0.05 to 1% w/v and;
ii. zinc chloride present in an amount ranging from 0.05 to 2% w/v and;
iii. sodium fluoride present in an amount ranging from 0.05 to 5% w/v
5. An oral mouth wash composition as claimed in claim 3 wherein composition comprises:
a. about 0.2% w/v Chlorhexidine Gluonate and;
b. about 0.09% w/v Zinc chloride and;
c. about 0.05% w/v Sodium fluoride and;
d. about 0.1% w/v Hyaluronic acid
6. An oral mouth wash composition as claimed in claim 1-5 further comprises one or more excipients selected from flavouring agent, cooling agent, solubilizer, surfactant, sweetener, anti-staining agent, humectant, preservative, wetting agent, coloring agent and vehicle.
7. A process of manufacturing mouth was comprising following steps:
a. Preparation of aqueous phase by dissolving poloxamer in water with continuous stirring until a clear solution is obtained and;
b. Addition of Zinc chloride and sodium fluoride one by one into aqueous phase with continuous stirring and;
c. Addition of sorbitol solution and glycerin to the solution obtained from step-b with continuous stirring and;
d. Preparation of preservative phase by adding sodium methyl paraben and sodium propyl paraben one by one into solution obtained in step-c until a clear solution is obtained and;
e. Add aspartame into above solution with continuous stirring and transfer into main manufacturing vessel;
f. Addition of Chlorhexidine gluconate solution in main manufacturing vessel with continuous stirring and;
g. Preparation and addition of Hyaluronic acid phase by slowly dissolving hyaluronic acid into separate container with continuous stirring and then transfer it in main manufacturing vessel with continuous stirring;
h. pH is adjusted to the mouth wash obtained in step g with citric acid solution and
i. optionally adding colouring agent and makeup the volume with purified water.