Field of the invention

The present invention relates to a dental care composition having anti-inflammatory activity. The invention further relates to preparation of the said composition and its application enabling chemo-mechanical removal of dental caries.

Background of the Invention:

Loss of tooth due to dental caries is major problem especially in children. Caries caused by bacterial inflammatory activity starts from plaque layer formed on tooth surface. If left untreated it gradually leads to degeneration of the tooth structure.

In periodontal disease, the root surface is exposed to the oral environment and bacterial plaque. Exposure to crevicular fluid as well as to enzymes and metabolites produced by subgingival plaque bacteria induces physical and chemical alterations on root cementum. These leads to dental calculus formation results from calcification of microbial plaque on tooth surface covered with endotoxin, proteins. Many chemical agents and mechanical systems are used for removal of cemental collagen matrix to provide biologically acceptable surface for new connective tissue attachment. Over recent years the dental profession has shifted towards practicing preventive dentistry and adopting more conservative and tooth-preserving procedures. Excavation of carious tooth structure is very important for controlling the progression of lesion, removal of necrotic tissue and to allow proper support for the filling (Yazici AR, Ozgunaltay G, Dayanga? B. A scanning electron microscopic study of different caries removal techniques on human dentin. Oper Dent 2002; 27:360-366). In mechanical removal the amount of caries to be removed is still a challenge to successfully treat the lesion as there are no criteria to guide the caries excavation. However inherent fundamental drawbacks of the mechanical approach are unpleasantness to patients, need for local anesthesia, and potential adverse effects to the pulp due to heat and pressure. This method is uncomfortable for the patient and treatment time is prolonged. The Chemo-mechanical caries removal technique involves' the application of chemical agents to cause a selective softening of infected dentine and facilitate removal by gentle excavation.

Prior art:

The advances in restorative dentistry have facilitated a change from the need for a standard cavity design to the recent minimally invasive techniques. The chemo mechanical removal system is developed with idea of removing infected dentine, preventing removal of sound dentin and intended to cause less discomfort for patients. The first solution used for chemo mechanical removal of caries was Caridex which required 10-20 ml of solution. Later this was replaced by a preparation of two liquid components (US patent No: 6,409,994 B1). The first component comprised active chlorine, a second component amine or substituted, gelling agent carboxymethyl cellulose and a dye agent erythrocin that interacts on carious material.

According US patent no: 6,413,502 B1 the preparation for treatment of dental caries has two components in which one contains three amino acids with different charges, 3% carboxy methyl cellulose or any other polysaccharide and coloring agent 0.04% Erythrosin. This preparation was required in fewer amounts compared to earlier one. Further according to another method of preparation (US Patent No: 6,582,681) the above gel which had sodium hypochlorite as active component had to be mixed with other component to reduce the aggressiveness of the hypochlorite on healthy tissue. The mixture of two liquids has to be applied on dental caries and removed later by means of excavating dental instruments.

The prior art also includes the method of preparation of a gel by product name Papacarie® contains (Bussadori S, Castro L, Galvao A. Papain gel: a new chemo mechanical caries removal agent. J Clin Pediatr Dent.2005; 30:115-19.) papain, chloramines and toludiene blue which acts on collagen present in carious tissue by softening the infected tissue later can be removed by excavating dental instruments. Papacarie is known to be less aggressive and reduces exposure of pulp (Motta LJ, Martins MD, Porta KP and Bussadori SK. Aesthetic restoration of deciduous anterior teeth after removal of carious tissue with Papacarie®. Indian J Dent Res, 2009; 20:11 7-20) making it good option for caries removal. The main agents in all these existing gels used in chemo mechanical caries removal consists of a mixture of sodium hypochlorite and three amino acids (lysine, leucine and glutamic acid) in a gel preparation. It softens the carious dentine which is then hand excavated and claims that it will not affect the underneath healthy affected dentine. These preparations are two components of liquid . The liquids are mixed just before the treatment and then applied on carious cavity and after 5-8 minutes the dentist removes the softened carious substance by a sharp spoon excavator. The mixture cannot be stored and reused.

In comparison to prior art, the composition of the present invention does not contain sodium hypochlorite and has a unique endoprotein from papaya extract, chloramines and dye. In addition the composition contains specific combination of essential oils from plant sources, which has anti-inflammatory and mild anesthetic effect. The composition also contains explicit gelling agent in accurate percentage to give exact consistency to the gel so that when applied there is no spill over.

The components used in the composition are extracts from papaya, chloramines, essential oil from plant source and coloring dyes, out of which the active components like endoprotein and essential oils, are from natural sources. According to the invention, the composition does not have hypochlorite but instead contains chloramines which act as anti-microbial agent and are less aggressive on healthy gum tissue. Coupleed with the above advantages, the composition maintains the dissolving effect on denatured collagen along with anti microbial activity. The Softened infected caries can be removed by using excavating dental instruments. Coloring agents may be added to the composition to facilitate the visibility of existing caries on the tooth cavity.

Surprisingly it has been found that composition of present invention provides aroma and anti-inflammatory activity which is not found in any of the prior art compositions.
Summary of the invention

The present provides a dental care composition having anti-inflammatory activity, comprising essentially of endoprotein enriched papaya extract, chloramines, essential oils, coloring agents, gelling agent and sterile water.The invention also provides a process for the said composition and its application to remove dental caries.

Description of Drawings:

Figure 1 shows the materials used for evaluation of the composition

Figure 2(a) and 2(b) show application of the composition of example 1 and caries removal using Manipal Spoon excavator respectively.

Figure 3 shows a caries-free tooth surface

Detailed Description of the Invention:

Accordingly,, the present invention provides a dental care composition having anti inflammatory activity, the said composition comprising of:
W/W (%)

Endoproteins enrichedPapaya extract 5.0-35

Chloramines 0.8-1.2
Sodium Chloride 0.20 - 0.30
coloring agents 0.04 - 0.06
Gelling agent 0.8-1.2
Essential oil 0.08-0.12
sterile water qs

Preferably, the composition of the invention may be in the form of a gel or an ointment. The composition may also be formulated in other delivery forms as known in the art.

One of the preferred components of the composition of the invention is papaya extract; and preferably, a papaya extract enriched in Papain enzyme is used in the composition.

Chloramine which is another ingredient of the composition and the preferred chloramines may be N-chlorophenyl sulphonamide.

The essential oil used in the composition is derived from plant-source selected from a group consisting of eucalyptus, clove or lemongrass oil.

Any coloring agent may be used in the composition, preferably, selected from a group consisting of toluidine blue, methylene blue or erythrocin.

The invention also provides a method for the preparation of the dental care composition under sterile conditions comprising steps of:

(a) mixing endoprotein containing papaya extract and sodium chloride in sterile water and stirring to dissolve,

(b) adding coloring agents, stirring to obtain uniform color distribution,

(c) adding further gelling agent, stirred to form a gel, followed by addition of essential oil and stirring,

(d) storing overnight the mixture of step (c) at room temperature to obtain required Carie-care composition.

The invention also provides a method for the evaluation of composition, the said method comprising steps of:

(a) selecting and mounting the extracted teeth having carious surface,

(b) applying Carie-care composition on the carious surface and left for 30-60 seconds,

(c) removing the softened carious dentin of decayed teeth by using spoon excavator

The composition of the invention which is also called Carie-Care is in the form of single composition i.e a single unit that includes all the ingredients as opposed to prior art wherein the ingredients were split or divided and later had to be combined when in use. The composition of the invention can be stored at 4°C for more than 6 months. Carie-Care is applied directly onto the tooth having caries by means of a disposable applicator tip; and soon the gel composition changes color in the affected area. After 1 minute the gel along with dissolved caries may be removed by means of an Excavator.

The following examples describe the preparation of the composition of the present invention and should not be construed to limit the scope of the invention.
Example 1:

Preparation of the Composition - Carie-Care:

5-35% of endoprotein containing extracts from papaya, 0.2-0.3% of NaCl and 0.8-1.2% of Chloramines is mixed with sterile water. The contents are stirred on a magnetic stirrer till the contents dissolves and volume suitably adjusted. 0.04-0.06% of coloring agents are added and stirred till the color distribution is uniform. 0.8-1.2% Gelling agent is added and stirred till it dissolves for 30-40 mins for gel formation. Essential oil 0.08-0.12% from plant sources like eucalyptus, clove or lemongrass was added for aroma and anti-inflammatory action and further stirred for some more time and stored at room temperature over night. All the steps are performed under sterile conditions.

Example 2:

Evaluation of composition in extracted teeth:

Ten freshly extracted human permanent teeth with dentinal caries were used in this in vitro study. The carious lesions were examined and categorized according to area of involvement as minimally cavitated (<2.5mm2) and extensively cavitated (>2.5 mm2). The materials used were composition of example 1, spoon excavator, tweezer, airotor and cotton pellets. These materials are depicted in figure 1.

1) The selected teeth were mounted on dental stone.

2) A cotton pellet was used to applying the composition of example 1 on the carious surface for a period of 30-60 seconds.

3) Once applied for the above mentioned time, the decayed portion of teeth was
softened by the invented dental care composition.

4) The softened carious dentin was gently removed using a spoon excavator. Figure 2(a) and 2(b) show application of the composition of example 1 and caries removal using Manipal Spoon excavator respectively. Figure 3 shows a caries-free tooth surface

Examples 3:

Effect of Carie-Care gel on types of lesion

1) Carie-Care effectively softened the carious portion of all the 10 teeth.
2) Time taken for softening caries varied which is given in tablel
3) However, airotor was needed for opening up of small cavitated lesions to facilitate the placement of the gel.

Advantages

Carie-care composition of the present invention provides anti-inflammatory activity.

Carie-care composition of the present invention provides aroma.

Carie-care composition of the present invention is a Single unit for application.

WE CLAIM:

1. A dental care composition having anti inflammatory activity comprising essentially of:
W/W (%)

Papaya extract enriched in endoproteins 5.0-35
Chloramines 0.8-1.2
Sodium Chloride 0.20 - 0.30
coloring agents 0.04 - 0.06
Gelling agent ,0.8-1.2
Essential oil 0.08-0.12
sterile water qs

2. The composition of Claim 1, wherein endoprotein of papaya extract comprises of Papain enzyme.

3. The composition of Claim 1, wherein Chloramine is N-chlorophenyl sulphonamide.

4. The composition of Claim 1, wherein essential oil is derived from plant-source selected from a group consisting of eucalyptus, clove or lemongrass oil.

5. The composition of Claim 1, wherein coloring agent is selected from a group consisting of toluidine blue, methylene blue or erythrocin.

6. A method for the preparation of a dental care composition of Claim 1 under
sterile conditions comprising steps of:

(a) mixing endoprotein enriched papaya extract and sodium chloride in sterile water and stirring to dissolve,

(b) adding coloring agents, stirring to obtain uniform color distribution,

(c) adding further gelling agent, stirred to form a gel, followed by addition of
essential oil and stirring,

(d) storing overnight the mixture of step (c) at room temperature to obtain
required composition.

7. A method for the evaluation of Carie-care composition of claim 1, the said
method comprising steps of:

(a) selecting and mounting the extracted teeth having carious surface,

(b) applying Carie-care composition on the carious surface and leaving for 30-60 seconds,

(c) removing the softened carious dentin of decayed teeth by using spoon
excavator.