FORM 2
THE PATENTS ACT
COMPLETE SPECIFICATION (SECTION 10)
CHITOSAN BASED MEDICATED TOOTHPASTES"
The following specification describes the nature of the invention and the manner in which it is performed:

FIELD OF THE INVENTION:
Present invention relates to chitosan based medicated dentifrice compositions. Particularly present invention relates to chitosan based medicated toothpaste compositions.
OBJECTIVE OF THE INVENTION:
The object of the present invention is to provide chitosan based medicated dentifrice composition wherein chitosan is used as base.
Yet another object of the present invention is to provide chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base.
Yet another object of the present invention is to provide a process of preparing chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base.
Yet another object of the present invention is to provide a process of preparing chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base with one or more additional agents effective in oral care.
Yet another object of the present invention is to provide a process of preparing chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base with one or more additional agents effective in oral care.
BACKGROUND OF THE INVENTION:
The present invention relates to chitosan based medicated dentifrice composition wherein chitosan is used as base.
Oral hygiene is of utmost importance as it- contributes in aesthetic expectations of individual; and of society. Negligence, carelessness and unawareness of some people towards maintaining good oral hygiene and increased popularity of fast food, cold drinks


and tobacco-chewing which again contributes in disturbing oral hygiene lead to development of gum and dental diseases.
Unbalanced diet, or lack of diet containing natural abrasives like fruits, cereals, leafy vegetable, fibers etc ; which polishes the surfaces of teeth, gums and the oral cavity leads to development of bad breath, plaque and local as well as systemic infections. The strong positive association that exists between poor oral hygiene and gingival and periodontal diseases; makes poor hygiene the primary etiologic agent.
To get rid of oral hygiene problems variety of products like medicated and non-medicated toothpastes are available. However their usefulness is limited by varied reasons like multiple frequency of dosing, limited therapeutic effectiveness, fails to fulfill aesthetic expectations of people and lack of availability of toothpaste having all essential ingredients in single formulation.
Chitosan an abundant natural polymer is obtained by alkaline N-deacetylation of chitin. The physical and chemical properties of chitosan, such as inter and intra molecular hydrogen bonding and cationic charge in acidic medium, makes this polymer attractive for development of novel oral hygiene products. Chitosan being a binding agent, bio-adhesive, biocompatible and nontoxic polymer also possessing medicinal activities like Antifungal, antibacterial, antiprotozoal, anticancer, antiplaque, antitartar, haemostatic, wound healing, potentiating anti-inflammatory response, inhibits the growth of cariogenic bacteria, immunopotentiation, antihypertensive, serum cholesterol lowering, absorption enhancer, increases salivary secretion (antixerostomial), and formation of bone substitute materials.
Considering the limitations of presently available products and the promising properties of chitosan suitable to address oral care problems, present invention was directed-to design and develop chitosan based polyherbal and polymineral medicated toothpaste with enhanced performance in oral care as chitosan potentiate the effectiveness of active ingredients of toothpaste.

DETAILED DESCRIPTION OF THE INVENTION;
In one aspect the present invention relates to chitosan based medicated dentifrice compositions wherein chitosan is used as base.
In one embodiment the present invention provides chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base.
In yet another embodiment the present invention provides a process of preparing chitosan composition based medicated toothpaste wherein chitosan is used as toothpaste base.
In yet another embodiment the present invention provides a process of preparing chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base with one. or more additional agents effective in oral care.
In yet another embodiment the present invention provides a process of preparing chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base with one or more additional agents effective in oral care.
In yet another preferred embodiment the present invention provides a chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base which further comprises of one or more abrasives, one or more binding agents, one or more surfactants, one or more humectants, one or more sweeteners, one or more foaming agents, one or more antifoaming agents.
Examples of abrasives includes but are not limited to silicas including gels and precipitates, insoluble sodium polymetaphosphate, hydrated alumina, calcium carbonate, dicalcium orthophosphate dihydrate, calcium pyrophosphate, tricalcium phosphate, calcium polymetaphosphate, and resinous abrasive materials such as particulate condensation products of urea and formaldehyde and the like.

Examples of surfactants or foaming agents includes but are not limited to sodium lauryl sulfate, sodium coconut monoglyceride sulfonates, sarcosinates, such as sodium lauryl sarcosinate, taurates, sodium lauryl sulfoacetate, sodium lauryl isethionate, sodium laureth carboxylate, and sodium dodecyl benzenesulfonate or mixtures thereof and the like.
Examples of humectants includes but are not limited to edible polyhydric alcohols such as glycerin, sorbitol, xylitol, butylene glycol, polyethylene glycol, and propylene glycol, especially sorbitol and glycerin and the like.
Examples of antifoaming agents includes but are not limited to silicon dioxide, magnesium aluminometasilicate, cellulose, diatomaceous earth, montmorillonite, bentonite, titanium dioxide, amorphous silicon dioxide, calcium carbonate, talc (SiO2+MgO), attapulgite (silicon, aluminium and iron oxides clay) and kaolin (aluminum silicate) and the like.
Examples of flavoring and sweetening agents includes but are not limited to stevia rebaudiana extract, oil of wintergreen, oil of peppermint, oil of spearmint, clove bud oil, menthol, anethole, methyl salicylate, eucalyptol, cassia, 1-menthyl acetate, sage, eugenol, parsley oil, oxanone, alpha-irisone, marjoram, lemon, orange, propenyl guaethol, cinnamon, vanillin, thymol, linalool, cinnamaldehyde glycerol acetal known as CGA, and mixtures thereof and the like.
Additional Other Active Agents:
The present invention may also include other agents, such as antimicrobial agents. Included among such agents are water insoluble non-cationic antimicrobial agents such as halogenated diphenyl ethers, phenolic compounds including phenol and its homologs, mono and poly-alkyl and aromatic halophenols, resorcinol and its derivatives, bisphenolic compounds and halogenated salicylanilides, benzoic esters, and halogenated carbanilides. The water soluble antimicrobials include quaternary ammonium salts and bis-biquanide salts, among others. Triclosan monophosphate is an additional water soluble


antimicrobial agent. The quaternary ammonium agents include those in which one or two of the substitutes on the quaternary nitrogen has a carbon chain length (typically alkyl group) from about 8 to about 20, typically from about 10 to about 18 carbon atoms while the remaining substitutes (typically alkyl or benzyl group) have a lower number of carbon atoms, such as from about 1 to about 7 carbon atoms, typically methyl or ethyl groups. Dodecyl trimethyl ammonium bromide, tetradecylpyridinium chloride, domiphen bromide, N-tetradecyl-4-ethyl pyridinium chloride, dodecyl dimethyl (2-phenoxyethyl) ammonium bromide, benzyl dimethylstearyl ammonium chloride, cetyl pyridinium chloride, quaternized 5-amino-l,3-bis(2-ethyl-hexyl)-5-mefhyl hexa hydropyrimidine, benzalkonium chloride, benzethonium chloride and methyl benzethonium chloride are exemplary of typical quaternary ammonium antibacterial agents.
The present invention may preferably include Glycerrhiza glabra extract, Pterocarpus marsupium extract and sodium chloride.
The concentration of chitosan according to present invention is present in range of 0.1% to 9% w/w of the composition, preferably in range of 0.2% to 7 % w/w of the composition, still preferably 0.5 to 3% w/w.
In a still preferred embodiment the chitosan based medicated toothpaste comprises of precipitated calcium carbonate 30 %, dicalcium phosphate 26 %, chitosan 5 % gel 15%>, glycerin %, sodium lauryl sulphate 2 %, silicon dioxide 0.4 %, stevia rebaudiana extract 0.1 % , glycerrhiza glabra extract 1 %, eugenol 0.5 %.
In a still preferred embodiment the chitosan based medicated toothpaste comprises of precipitated calcium carbonate 30 %, dicalcium phosphate 21 %, chitosan 5 % gel 15 %, glycerin 25 %, sodium lauryl sulphate 2 %, silicon dioxide 0.4 %, stevia rebaudiana extract 0.1 %, glycerrhiza glabra extract 1 %, pterocarpus marsupium extract 5 %, eugenol 0.5 %.

In a still preferred embodiment the chitosan based medicated toothpaste comprises of precipitated calcium carbonate 30 %, dicalcium phosphate 25 %, chitosan 5 % gel 15 %, glycerin 25 %, sodium lauryl sulphate 2 %, silicon dioxide 0.4 %, stevia rebaudiana extract 0.1 %, glycerrhiza glabra extract 1 %, sodium chloride 1 % eugenol 0.5 %.
In a yet another preferred embodiment a process of preparing chitosan based medicated toothpaste wherein
1. Preparing mixture of Glycerin and 5 % Chitosan gel
2. Adding remaining solid substances with continuous titration. ' 3. Adding Eugenol and mixing thoroughly
4. Filling obtained toothpaste into the tubes.
While the present invention has been described in terms of its specific embodiments, certain modifications and equivalents will be apparent to those skilled in the art and are included within the scope of the present invention. Examples are provided to illustrate particular aspects of the disclosure and do not limit the scope of the present invention as defined by the claims.
Example 1 Table 1

No Ingredients NormalA(%) AstringentB(%) SaltC(%) PlaceboD(%)
1 Precipitated calcium carbonate 30 30 30 30
2 Dicalcium phosphate 26 21 25 27.5
3 Chitosan 5 % gel 15 15 15 -
4 Gum tragacanth mucilage - - - 15
5 Glycerin 25 25 25 25
6 Sodium lauryl sulphate 2 2 2 2
7 Silicon dioxide 0.4 0.4 0.4 0.4
8. Stevia rebaudiana extract 0.1 0.1 . 0.1 0.1
9 Glycerrhiza glabra extract 1 1 1 -
10 Pterocarpus marsuphtm extract - 5 - -
11 Sodium chloride - - 1 -
12 Eugenol. 0.5 0.5 0.5 -

A - Normal - Toothpaste containing chitosan
B - Astringent -Toothpaste containing Pterocarpus marsupium extract as astringent.
C - Salt- Toothpaste containing Sodium chloride as osmotic cleaner
D - Placebo- Toothpaste without chitosan.
Chitosan based toothpaste was prepares by using composition as shown in table 1 mixture of Glycerin and 5 % Chitosan gel was taken in to glass mortar and remaining solid substances were added with continuous titration. In the end Eugenol was added as flavor and mixed thoroughly and final formulation was filled into the tubes.
Table 2 Ingredients and their roles:

No Ingredients Uses
1 Precipitated calcium carbonate Abrasive, calcium source.
2 Dicalcium phosphate Abrasive, calcium and phosphate source.
3 Chitosan 5 % gel 1 .Non-medicated uses- Binding agent, mucoadhesive, biocompatible, biodegradable, non-toxic polymer. 2.Medicated uses- Antifungal, antibacterial, antiprotozoal, anticancer, antiplaque, antitartar, haemostatic, wound healing, potentiating anti-inflammatory response, inhibits the growth of cariogenic bacteria, immunopotentiation, antihypertensive, serum cholesterol lowering, absorption enhancer, increases salivary secretion (antixerostomial), and formation of bone substitute materials.
4 Gum tragacanth mucilage Binding agent.
5 Glycerin Humectant, sweetener.
6 Sodium lauryl sulphate Foaming agent
7 Silicon dioxide Antifoaming agent.
8 Stevia rebaudiana extract Sweetener.
9 Glycerrhiza glabra extract Penetration enhancer, increases saliva secretion, Antifungal, antibacterial, anticandidal, antihalitosis, antixerostomia, antisore, antipyretic, antitussive, wound healing, cancer of esophagus, antitumor, emollient, rejuvenation.
10 Pterocarpus marsupium extract Analgesic, antipyretic, anti-inflammatory, antisore, haemostatic, wound healing, leucorrhoea.

11 Sodium chloride Osmotic cleaner of oral mucosa.
12 Eugenol. Local anesthetic, antibacterial, antifungal, antihistamine, antioxidant, antimutagenic, antiseptic, antiviral, antiasthmatic, antihalitosis, blood purifier, blood thinner (anti-platelet agent), anticancer, carminative, anticavities, anticolic, antitussive, counterirritant, antidiabetic, expectorant, food preservative, antigout, antihiccups, antihypertensive, antiinflammatory, insecticidal, insulin mimetic, parasiticidal, lipid-lowering, in mouth and throat inflammation, as mouthwash, in nausea or vomiting, analgesic, in neurodegeneration, anticandidal, spasmolytic, in oral cavities, oral edema, pediculocide, smooth muscle relaxant (clove oil), in tooth or gum pain.
Evaluation of Toothpastes:
The formulated toothpastes were evaluated as per U. S. Government Tooth Paste Specifications.
W. Sounder and I.'C. Schoonover, of the National Bureau of Standards have worked out a set of specifications toothpaste to be purchased by the US Govt, and these specifications were published in the "Journal of the American Dental Association."
"Concerning material and workmanship, the tooth paste shall be free from material other than those specified and shall be uniform in composition."
"The tooth paste shall, when used in the normal manner, assist in the removal of the usual daily accumulations of debris and deposits from the exposed surfaces of the teeth without injury to the teeth, mucous membrane of the mouth or body in general."
The results obtained are presented in table 3.
Table 3:

No. Text Limit ObservationsOfallA,B,C,Dformulations Inference
1. Mucosal Irritation Test Should not produce any irritation No irritation observed Complies.
2. Flow Property at 1.0°C Continuous Continuous Flow Complies.

observed
3. Flow Property at 20°C (orifices down) Minimum length of 10 mm More than 15 mm Complies.
4. Attachment Test at 20°C (orifices down) NLT 15 seconds More than 20 seconds Complies.
5. Stability Test at 50°C for 72 hours. Should not segregate, ferment or deteriorate. No change in consistency. Complies.
6. Amount of Abrasives More than 40 % More than 50 % Complies.
7. Amount of soap NMT 20 % 1-3% Complies.
8. Sieve Test material transfer from US std no. J 00 sieve. 100% 100% Complies.
9. Sieve Test material transfer from U.S. Std No. 200 sieve. 98% 99-100 % Complies.
10. pH Test 4.9- 10.1 6.0- 8.0 Complies.
11. Glass Scratch Test Should not produce any scratch on glass. No scratch observed Complies.
12. Test for container Use chemical resistant collapsible tubes having screw cap. Used chemical resistant collapsible tubes having screw cap. Complies.
14. Orifice area NLT 13 and NMT 36 sq. mm 15-30 sq. mm Complies.
15. Flavors and sweetener when used in proper amount. Distinct and pleasant Distinct and pleasant Complies.


Clinical testing:
The formulated toothpastes were evaluated in human volunteers for their performance; the results obtained are depicted in table 4.
Table 4

Sr.No Parameters tested Normal Astringent Salt Placebo
1 Good Consistency Yes Yes Yes Yes
2 Appreciable Taste Yes Yes Yes Yes
3 Fresh Mouth Feel Yes Yes Yes No
4 Adequate Foaming Yes Yes Yes Yes
5 Removes Debris / Stains Yes Yes Yes No
6. Removes Plaque Yes Yes Yes No
7. Mucosal Irritation No No No No
8. Medicinal Effect Yes Yes Yes No
9. Any Adverse Effect No No No No
10. Better Than Regular Toothpaste Yes Yes Yes No
From above evaluation of chitosan based medicated toothpaste it can be concluded that the medicated toothpaste containing chitosan are superior to non-chitosan containing toothpastes.

CLAIMS:
1. Chitosan based medicated toothpaste composition wherein chitosan is present as toothpaste base.
2. Chitosan based medicated toothpaste composition according claim 1 wherein composition further comprises of one or more additional agents effective in oral care.
3. Chitosan based medicated toothpaste composition claim 1 wherein composition further comprises of one or more abrasives, one or more binding agents, one or more surfactants, one or more humectants, one or more sweeteners, one or more foaming agents and one or more antifoaming agents.
4. Chitosan based medicated toothpaste composition according claim 1 chitosan is present in the range of 0.5 To 3 % w/w of composition.
5. Chitosan based medicated toothpaste composition comprising chitosan, abrasive, binding agent, surfactant, humectant, sweetener, more foaming agent, antifoaming agent.
6. Chitosan based medicated toothpaste composition according claim chitosan is present in the range of 0.5 To 3 % w/w of composition,
7. Chitosan based medicated toothpaste composition according claim 5 wherein composition further comprises of one or more additional agents effective in oral care.
8. Chitosan based medicated toothpaste comprising precipitated calcium carbonate 30 %, dicalcium phosphate 2,1 %, chitosan 5 % gel 15 %, glycerin 25 %, sodium lauryl sulphate 2 %, silicon dioxide 0.4 %, stevia rebaudiana extract 0.1 %, glycerrhiza glabra extract 1 %, pterocarpus marsupium extract 5 %, eugenol 0.5 %.
9. Chitosan based medicated toothpaste comprising precipitated calcium carbonate 30 %, dicalcium phosphate 25 %, chitosan 5 % gel 15 %, glycerin 25 %, sodium lauryl sulphate 2 %, silicon dioxide 0.4 %, stevia rebaudiana extract 0.1 %, glycerrhiza glabra extract \.%, sodium chloride 1 % eugenol 0.5 %.

10. Process of preparing chitosan based medicated toothpaste comprising following steps;
a) preparing mixture of glycerin and 5 % chitosan gel.
b) adding remaining solid substances with continuous titration.
c) adding eugenol and mixing.
d) filling obtained toothpaste in to the tubes.

ABSTRACT
Present invention discloses chitosan based medicated dentifrice compositions and process of preparing the same. Preferably present invention discloses chitosan based medicated toothpaste compositions with one or more additional agents effective in oral care. Preferably present invention provides a chitosan based medicated toothpaste composition wherein chitosan is used as toothpaste base which further comprises of one or more abrasives, one or more binding agents, one or more surfactants, one or more humectants, one or more sweeteners, one or more foaming agents and one or more antifoaming agents.