Description:
TITLE OF THE INVENTION

Safe cleansing composition for oral care

FIELD OF THE INVENTION

The present invention relates generally to a safe and effective cleansing composition for dental use, more particularly to a non-perborate composition that is stable and has effective cleansing properties for use in oral care formulations.

OBJECTIVE OF THE INVENTION

It is an objective of the present invention to provide a safe dental care
composition that providing oral care hygiene and that aids in effective
cleansing action.

It is one another objective of the present invention to provide an alternative composition that to the perborate based oral care composition wherein the use of perborate is being regulated in such formulations.

It is yet another objective of the present invention to provide a non-perborate based dental care composition that provides effective cleansing action and aid in effective oral care hygiene.

BACKGROUND OF THE INVENTION

Oral care products are defined as products used for care of the teeth
and the mouth. Various products are available based on their special clinical indications including toothpastes, mouthwashes, tooth-whitening products, and denture care materials. To-date oral hygiene compositions majorly fall into two main categories: dentifrices, and mouthwashes or rinses. Dentifrices are generally known to contain an insoluble dentally acceptable abrasive which is utilized to physically cleanse the surface of the teeth. These dentifrices are generally provided in the form of solid or pasty preparations which can be readily applied to a toothbrush, for example, powders, pastes or viscous gels. The most important component of dentures comprises of abrasives, bleaching agents, fluorides, surfactants and xylitol.

The global oral care market size was valued at USD 33.7 billion in
2021 and is expected to expand at a compound annual growth rate (CAGR) of 6.4% from 2022 to 2030. The growing prevalence of dental caries both among adults and children is expected to fuel the market growth. According to the World Health Organization (WHO), over 530 million children population suffer from tooth decay of primary teeth.

Bleaching agents in the oral care formulation is an important component and white teeth are still being considered cosmetically desirable. However, due to the presence of chromogenic (colour-causing) substances in our day-to day edibles including beverages, tobacco, and salivary fluid, in addition to other factors antibiotics such as tetracycline, teeth become almost invariably discoloured in the absence of any intervention. The structure of a tooth comprising the enamel, dentin and the acquired pellicle are responsible for the stained appearance.

Bleaching agents in the dental or oral care compositions provide the
necessary action for whitening of the stained teeth. Most commonly used
bleaching agents include peroxides and perborate, more particularly the
common bleaching agent is sodium perborate. Functionally, the generation of active oxygen in aqueous solutions is the basis for the use of sodium perborate as bleaching component. The crystalline reagent is available as a hydrate with the general formula NaBO3 • n H2O (n: 1 or 4).

Sodium perborate is soluble in water and releases hydrogen peroxide. Unlike percarbonate, perborate is not just an addition compound of peroxide, but contains true peroxygen bonds. In dilute solution, an equilibrium exists that still contains peroxoborate anions. These peroxoborate species are able to deliver the hydroperoxide anion at a lower pH than when H2O2 is used. Sodium perborate monohydrate and tetrahydrate contain theoretically about 34% and 22% hydrogen peroxide, respectively.

In aqueous solutions at room temperature, an equilibrium between
sodium perborate and hydrogen peroxide/sodium metaborate is instantly
established.

[NaBO2(OH)2 x 3 H2O]2 ⇆ 2NaBO2 + 2H2O2 + 6 H2O

(Sodium perborate tetrahydrate) ⇆ (Sodium metaborate) + (Hydrogen
peroxide) + (Water)

At low concentrations (about ≤ 2 g/l) the equilibrium is largely on the side of the hydrolysis products whereas at higher concentrations (about ≥ 12g/l) the undissociated molecule is present in aqueous solutions. Via
degradation to (active) oxygen and water the hydrogen peroxide can be
removed from the equilibrium leading to an irreversible shift of the
equilibrium (equation above) to the degradation products sodium metaborate and water:

Further the European Commission on scientific committee on
consumer safety provided report on toxicology studies of perborate more
particularly boric acid, sodium borate, or sodium perborate in concentration of 100 – 500 mg/kg bw in humans. The skin irritation test concluded that in some studies with the monohydrate after prolonged exposure very mild irritating effects were observed which were not completely reversible in some cases. Solutions of 10% sodium perborate tetrahydrate are mildly irritating.

Furthermore, in all studies according to standard protocols, sodium
perborate showed severe eye irritating effects, when applied as solid substance to the eyes (Bagley et al., 1994; ICI, 1986 a, b; Interox, 1987c; Momma et al., 1986). Moderate corneal opacity, severe iritis and conjunctival effects which consisted of severe redness, moderate chemosis and severe discharge were recorded. The effects were not completely reversible. It is also noted that the irritating potential of sodium perborate tetrahydrate seems to be lower than for the monohydrate, being consistent with its higher water content.

It has also been notified that In the European Union, sodium perborate, like most borates, was classified as "carcinogenic, mutagenic, or
toxic for reproduction" (CMR), category 1B of Regulation (EC) 790/2009, as a result of being included in Part 3 of Annex VI of the regulation 1272/2008 on Classification, Labelling and Packaging (CLP) of substances and mixtures. As a result, their use has been automatically banned in cosmetic products in the EU, in any concentration, starting 1 December 2010. That extends to the use of perborates for tooth whitening.

Further, prior art indicates that the alternative to sodium perborate as a
bleaching agent such as hydrogen peroxide and sodium percarbonate are not as effective as sodium perborate and there is a need for an effective non-perborate based toothpaste composition.

However, difficulty occurs in formulating a cleansing composition,
wherein the composition provides effective cleansing of plaque and bleaching agents that are not sodium perborate based and that is as effective as the existing bleaching agents. The present invention provides means and methods to achieve this composition that provides a non-perborate based oral care composition that is suitable for formulating, safe and effective and can be suitable for use in oral hygiene.

SUMMARY OF THE INVENTION

The following presents a simplified summary of one or more
embodiments in order to provide a basic understanding of such embodiments. This summary is not an extensive overview of all contemplated embodiments and is intended to neither identify key or critical elements of all embodiments nor delineate the scope of any or all embodiments. Its sole purpose is to present some concepts of one or more embodiments in a simplified form as a prelude to the more detailed description that is presented later.

In accordance with one aspect of the present invention provides means and methods for a non-perborate based oral care composition trisodium
phosphate. In one embodiment, the present invention comprises sodium
benzoate as the preservative and Sulfamic Acid, citric acid and Sodium
carbonate as the effervescence agent. The non-perborate composition of the present invention is stable and provides improved cleansing activity compared to perborate-based compositions. The oral care composition of the present invention is a safer alternative to perborate based dental compositions and is used in all means of oral delivery for maintain dental hygiene.

The foregoing has outlined rather broadly the features and technical
advantages of the present invention so that those skilled in the art may better understand the detailed description of the invention that follows. Additional features and advantages of the invention will be described hereinafter that form the subject of the claims of the invention. Those skilled in the art should appreciate that they may readily use the conception and the specific embodiment disclosed as a basis for modifying or designing other structures for carrying out the same purposes of the present invention. Those skilled in the art should also realize that such equivalent constructions do not depart from the spirit and scope of the invention in its broadest form.

DETAIL DESCRIPTION OF THE INVENTION

Before undertaking the detailed description of the invention below it
may be advantageous to set forth definitions of certain words and phrases used throughout this patent document: the terms “include” and “comprise ” as well as derivatives thereof mean inclusion without limitation; the term “or ” is inclusive meaning and/or; the phrases “associated with” and “associated therewith ” as well as derivatives thereof may mean to include be included within interconnect with contain be contained within connect to or with couple to or with be communicable with cooperate with interleave juxtapose be proximate to be bound to or with have a property of or the like. Definitions for certain words and phrases are provided throughout this patent document those of ordinary skill in the art should understand that in many if not most instances such definitions apply to prior as well as future uses of such defined words and phrases.

Certain terms are used throughout the description and claims to refer
to particular system components. As one skilled in the art will
appreciate consumer electronic equipment manufacturers may refer to a
component by different names. This document does not intend to distinguish between components that differ in name but not function.

In the following description, numerous specific details are set forth in
order to provide a thorough understanding of embodiments of the present
invention. It will be apparent to someone skilled in the art that embodiments of the present invention may be practised without some of these details.

If the specification states a component or feature “may”, “can”,
“could”, or “might”, be included or have a characteristic, that particular
component or feature is not required to be included or have the characteristic.

As used in the description herein and throughout the claims that
follow, the meaning of “a”, “an”, and “the”, includes plural references unless the context clearly dictates otherwise. Also, as used in the description herein, the meaning of “in” includes “in” and “on” unless the context clearly dictates otherwise.

In some embodiments, the numbers expressing quantities or
dimensions of items, and so forth, used to describe and claim certain
embodiments of the invention are to be understood as being modified in some instances by the term “about”. Accordingly, in some embodiments, the numerical parameters set forth in the written description and attached claims are approximations that can vary depending upon the desired properties sought to be obtained by a particular embodiment. In some embodiment, the numerical parameters should be construed in light of the number of reported significant digits and by applying ordinary rounding techniques.

Notwithstanding that the numerical ranges and parameters setting forth the broad scope of some embodiments of the invention are approximations, the numerical values set forth in the specific examples are reported as precisely as practicable. The numerical values presented in some embodiments of the invention may contain certain errors necessarily resulting from the standard deviation found in their respective testing measures.

The recitation of ranges of values herein is merely intended to serve as
a shorthand method of referring individually to each separate value falling
within the range. Unless otherwise indicated herein, each individual value is incorporated into the specification as if it were individually recited herein.

Various terms as used herein should be given the broadest definition
persons in the pertinent art have given that term as reflected in printed
publications and issued patents at the time of filing.

Applicants have recognized that there is a need for an oral care
composition that provides safe and effective dental care that does not have any toxic substances and that is stable and effective to the perborate based available oral care composition.

In one embodiment, the present invention relates to a safe and effective
non perborate based oral care composition comprising Trisodium
Phosphate, Sodium Benzoate, Sulfamic Acid, Citric Acid, Sodium Carbonate, Polyvinylpyrrolidone, Isopropyl Alcohol, Sodium Lauryl Sulphate, TAED & EDTA.

In one embodiment, the present invention comprises trisodium
Phosphate as the cleaning agent. The Trisodium Phosphate of the present invention acts as the cleaning agent and provides the effective antibacterial activity. Trisodium Phosphate removes attached bacteria from oral surfaces by means of its surfactant properties and high alkalinity with pH about 12.0. Furthermore, Trisodium Phosphate kills bacteria by disrupting the cell membrane and causing leakage of cellular material and thus preventing bacterial infection and removing plaques to provide an oral cleansing activity.

In one embodiment, the Trisodium Phosphate is present between 15 –
22% of the total composition. In yet another embodiment Sodium Benzoate is used as an preservative in the oral care composition. Sodium benzoate added in the oral care composition provides stability to the active ingredients and ads safety to the oral care composition until the life of the product.

In one embodiment, the sodium benzoate is used between 0.25%-0.75% of the total composition.

In one embodiment, the present oral care composition comprises one
or more effervescent agent. In one embodiment, Sulfamic acid, citric acid,
Sodium Carbonate are used as the effervescent agents. These agents release CO2 when in contact with water and immediately activate the active ingredient in the formulation.

In yet another embodiment, the total composition of the effervescent
agent is added in the range of 63%-75% of the total composition.
In one embodiment, the oral care composition of the present invention
comprises one or more lubricants. The lubricant of the present invention is selected from SLS (Sodium Lauryl Sulphate), TAED
Tetraacetylethylenediamine and/or Ethylenediaminetetraacetic acid (EDTA).The said lubricants in the oral care composition provides appropriate disbursement of the active ingredients.

In one embodiment, the composition of the lubricant in the present invention range about 1.5% to 2.5 % of the total composition.

In yet another embodiment, present invention further comprises any flavouring agents. The flavouring agents added in the present oCmposition adds enhanced palatability of the oral care composition and masks the taste of the other chemicals that ae involved in the cleansing action. The commonly used flavouring agents include but not limited to mint, peppermint, saccharin, xylitol and mixtures thereof. The said flavouring agents are added in the composition in range of approx. 0.5 %.

In one optional embodiment, the present invention further comprises of isopropyl alcohol as the solvent and Polyvinylpyrrolidone as the binder.

In one embodiment, the present invention relates to the use of said safe composition, wherein the composition is administered as such as toothpaste (dentifrice), prophylactic paste, tooth powder, tooth polish, tooth gel, chewing gum, candy, lozenge, mouthwash, mouth sprays and/or gel for local delivery in the gum pockets or the like. In yet another embodiment, the present composition is used a tablet for denture apparatus cleansing.

In one embodiment, the non-perborate composition of the present invention is safe and effective and has comparable antimicrobial and oral cleansing activity. The present composition is specifically formulated to provide enhanced oral and or dental care composition that is safe and approved by regulatory authorities.

Examples
The present invention may be better understood through to the following examples. These examples are included to describe exemplary embodiments only and should not be interpreted to encompass the entire breadth of the invention.

Example 1: Preparation of dental care composition
The dental care composition as disclosed in the invention was 10 prepared by following process with Isopropyl Alcohol as the solvent. All the ingredients of the composition was taken in a container to which Isopropyl Alcohol was added and mixed thoroughly, post all other ingredients were added one by one and thoroughly mixed using a stirrer. All the concentrations of various agents were adjusted to get the oral care composition. Details of the 15 composition is given in below Table 1.

S. No Ingredients Quantity in percentage s (%)

1 Sulphamic Acid USP 15%
2 Trisodium Phosphate 18.2%
3 Sodium Carbonate IP 49.1%
4 PVPK-30 0.45%
5 Sodium Lauryl Sulphate IP 2.03%
6 Mint Flavour IH 1.56%
7 TAED 0.35%
8 EDTA 4.4% Page 12 of 18
9 Sodium Benzoate 0.4%
10 Citric acid 9%
11 Colouring agent 0.001%

Example 2: Anti-microbial activity of composition of the present
invention

To assess anti-microbial property of dental care composition as disclosed in examples, first the sample was incubated with a prescribed inoculum of various microorganisms including Bacteria and Fungi at a particular temperature and the samples were withdrawn at particular time intervals and checked the organism present in the sample.

In this experiment, first inoculum was prepared by transferring bacteria (Staphylococcus aureus ATCC6538, E.coli ATCC8739, Pseudomonas aeruginosa ATCC 9027, Bacillus subtilis ATCC6633) and Salmonella for 24 hours on SCDA.

Yeast (Candida albicans ATCC 10231) 22.5±2.5 ℃ was transferred to sabouraud dextrose agar (SDA) and incubated at 22.5 ± 2.5 ℃ for 24 hours on SDA.

After incubation, all the cultures were washed with 10 ml sterile solution having pH of 7.2. Post which, the culture was scrapped with a sterile loop, transfer the washed solution into a clean sterile tube and vortex before use. From the washed solution, 10 fold serial dilution was carried out using sterile saline solution.

20 ml of the dental care composition as disclosed in example 1 was prepared. The bacteriological were diluted and were prepared with microbiological count in test tubes as listed in the table 2.

Table 2: Initial Microbial load

S. No Name of Organism Suspension ID Counts CFU/ml
1 E.coli ATCC8739 E.C 110-01 82X105
2 Staphylococcus aureus ATCC6538 S.A. 110-01 30X105
3 Pseudomonas aeruginosa ATCC 9027 P.A. 110-01 56X105
4 Salmonella S.I. 110-01 60X105
5 Candida Albicans ATCC 10231 C.A. 110-01 26X105
6 Bacillus Subtilus ATCC 6633 B.S. 110-01 78X1

The test tubes were then added and mixed with the prepared sample and were mixed thoroughly for even distribution of surviving cells and incubated for 15 mins, 30 mins, 45 mins and 60 mins. To maintain control in this experiment, standardized inoculum was inoculated in normal saline solution. The results of the anti-microbial studies are tabulated in Table 3.

Table 3: Results of anti-microbial studies

S. No Name of Organism Initial Counts CFU/ml % reduction after 15 mins % reduction after 30 mins % reduction after 45 mins % reduction after 60 mins
1 E.coli ATCC8739 82X105 99.999 99.999 99.999 99.999
2. Staphylococcus aureus 30X105 99.992 99.999 99.999 99.999 Page 14 of 18 ATCC6538
3. Pseudomonas aeruginosa ATCC 9027 56X105 99.994 99.999 99.999 99.999
4. Salmonella 60X105 99.995 99.999 99.999 99.999
5. Candida Albicans ATCC 10231 26X105 99.998 99.999 99.999 99.999
6.Bacillus Subtilus ATCC 6633 78X105 99.991 99.999 99.999 99.999

Example 3: Stability studies of the oral care composition of the
present invention.

Example 3: Stability studies of the oral care composition of the present invention.
The stability of the composition as prepared in example 1 has been tested in various temperature and Relative humidity for a period of 120 hours, 1 month 2 month, 3 months, 4 months, 5months, 6 months and 9 months. The pH, Hardness and DT (Disintegration Time) of the composition was reported as in Table 4. The product is found stable after 6 months at 40+20C/75+5%RH & after 6 months at R.T

Table 4: results of stability studies

Conditions time pH DT (in min) Hardness (in Kg) Assay as % Trisodium phosphate
Initial ----- 9.96 3 min. 10 sec. 10 – 12 kg 97.32%
50+2 C 120 hours 9.85 5 min. 40 sec. 15 – 16 kg 97.20%
40°C / 75% RH
1 month 10.18 6 min. 30 sec. 17 – 18 kg 101.01%
2 month 10.07 6 min. 15 sec. 16 – 18 kg 101.15%
3 month 10.06 8 min *** 15 – 18 kg 93.0%
4 month 10.09 7 min 40 sec.*** 15 – 18 kg 91.15%
5 month 10.22 6 min 30 sec. 13 – 15 kg 92.36%
6 month 10.03 6 min 38 sec. 15 – 17 kg 93.60%
25°C / 70% RH
3 month 10.03 6 min 17 – 18 kg 93.56%
6 month 10.23 5 min. 15 sec. 12 – 13 kg 93.40%
9 month
Specification LT 9.5 to 10.5 NMT 10 min NLT 8 kg LT NLT 90 %

Dated this the 29th day of June 2023

Attorney for the Applicant
Priyadarsini Shanmugam / Chenthoori Pughazendhi
Registration No. IN/PA-1677
, C , Claims: CLAIMS
We Claim:

1. A non-perborate based oral care composition comprising:
a) a cleaning agent,
b) a preservative,
c) one or more effervescent agent,
d) a binder and
d) one or more lubricant,

2. The non-perborate based oral care composition comprising according to claim 1, wherein the cleaning agent is Trisodium Phosphate within the range of 15% to 22%.

3. The non-perborate based oral care composition comprising according to claim 1, wherein the preservative is Sodium Benzoate within the range of 0.25% to 0.75%.

4. The non-perborate based oral care composition comprising according to claim 1, wherein the one or more effervescent agent selected from Sulfamic Acid, Citric Acid, Sodium carbonate within the range of 63% to 75%.

5. The non-perborate based oral care composition comprising according to claim 1, wherein the binder is P.V.P.K-30 within the range of 0.3% to 0.50%.

6. The non-perborate based oral care composition comprising according to claim 1, wherein the one or more lubricant is selected from Sodium Lauryl Sulphate, (TAED) Tetraacetylethylenediamine, (EDTA) Ethylenediaminetetraacetic acid, in the range of 1.5% to 2.5 %.

7. The non-perborate based oral care composition comprising according to claim 1, optionally comprises, fragrant, enzymes and/or colouring agents.

8. The non-perborate based oral care composition comprises 15% Sulphamic Acid, 18.2% Trisodium Phosphate, 49.1% Sodium Carbonate IP, 0.45% PVPK-30, 2.03% Sodium Lauryl Sulphate IP, 1,56% Mint Flavour IH, 0.35% TAED, 4.4% EDTA, 0.4% Sodium Benzoate and 9% Citric acid.

Dated this the 29th day of June 2023

Attorney for the Applicant

Priyadarsini Shanmugam / Chenthoori Pughazendhi
Registration No. IN/PA-1677