GB1565672A - Toothpaste compostion - Google Patents

Description

(54) NOVEL TOOTHPASTE COMPOSITION (71) I, JEAN JACQUES GOUPIL of 30 Avenue du President Wilson 94230 Cachan, France, of French Nationality, do hereby declare the invention, for which I pray that a patent may be granted to me and the method by which it is to be performed, to be particularly described in and by the following statement: The significant role played by dental plaque in buccodental health is well known. Dental plaque or bacterial plaque is an adherent coating derived from the saliva, rich in polysaccharides and mucoproteins, which rapidly forms a deposit on the gingival edge of the teeth constituting a veritable culture center where infection and caries-generating microorganisms proliferate.

The thickness of this coating increases and the character of the bacteria is modified with ageing.

The initial aerobic germs are gradually replaced by a strictly anaerobic flora, which increases the pathogenic power of the dental plaque on the gum.

In fact the presence of microorganisms which are living and developing in the absence of oxygen, such as Actinomyces viscosus, Naeslundi, Fusospirochetes vibrions and Veillonella is considered to be responsible for acute or chronic infections of the periodontium.

As a rule the saliva acts a natural antiseptic owing to its antibodies and enzymes and to the fact that it contains traces of dissolved oxygen as well as an oxidase and a peroxidase. But this is insufficient and the saliva alone can not usually play a prophylactic and curative role in the infections and inflammatory states of the bucco-lingual and bucco-gingival mucosa.

It is known that oxygen, present in the saliva in insufficient quantities, is a biogenetic element which is essential to the life of the cell and that it possesses an antimicrobial action.

The aim of the present invention therefore is to reinforce the natural functions of the saliva by effecting a local oxygenation of the buccal cavity by means of an influx of oxygen produced on the tissues themselves, in order to obtain a tonic action, increasing the tissues' defensive response and an antimicrobal and deodorising action on the anaerobic flora of the dental plaque and, if necessary, on the lesions in the periodontium.

The invention has as its object useful compositions for prophylaxis and the treatment of bucco-dental infections, characterised in that they are capable of liberating nascent oxygen upon contact with the gums in the buccal cavity.

Chemical compounds which are capable of liberating oxygen and are compatible with the desired internal usage are the superoxygenated salts such as peroxy salts and peroxides. But these compounds are usually unstable and often incompatible with the chemical nature of the excipients (presence of water, humidity, organic matters).

According to the present invention, the idea was conceived of effecting a tooth-paste, in which a superoxygenated product is introduced, such as a stable peroxide or peroxy salt, which is insoluble in water, in a suitable excipient, as well as a product capable of liberating the oxygen produced by the superoxygenated product through contact with the latter at the moment of its utilisation, but the two components being kept isolated from each other during storage, for example by separate packaging in appropriate wrapping. The two products only come into contact at the moment of utilisation when, owing to the mechanical brushing action and to the salivary medium, the oxygen produced from the superoxygenated product is liberated upon contact with the gums.

Accordingly the present invention provides a toothpaste composition capable of liberating nascent oxygen upon contact with the gums, which comprises two active parts which are each separately coated in a pharmaceutically acceptable excipient and separately wrapped, the first active part comprising a stable superoxygenated compound which is insoluble in water together with a toothpaste carrier or diluent, the superoxygenated compound being present in an amount of from 5 to 10% by weight based on the weight of the first active part and the second active part comprising a pharmaceutically acceptable mineral or organic acid or acid salt together with a toothpaste carrier or diluent, the mineral or organic acid or acid salt being present in an amount of from 7.5 to 10% by weight based on the weight of the second active part.

The superoxygenated products which are stable and compatible with the excipients of a toothpaste are peroxy salts or peroxides which are insoluble in water and do not liberate their oxygen at ambient temperature until they are in the presence of appropriate products such as acids or acidic salts. Magnesium peroxide may be quoted as an example. This product is readily available in the commercial world, contains 50% active matter, is non-toxic and is perfectly suitable for putting the invention into operation.

The compounds liable to release oxygen produced from peroxides and peroxy salts may be pharmaceutically acceptable acids or acidic salts compatible with the desired internal usage, that is to say those which are non-toxic. Acids which are currently used in pharmacy and in the food industry such as phosphoric acid, tartaric acid, citric acid, and malic acid are examples of such compounds.

The acidity of the acidic part of the composition must generally be between pH=2 and pH=3. In these conditions the pH of the saliva which is usually 6.7 is advantageously reduced to a pH of from 3 to 4, during the brushing of the teeth with the composition of the present invention.

The excipient of the superoxygenated part may be the same as the excipient of the acidic part, providing that the excipients are not decomposable by the acids either during storage or at the moment of utilisation. This provision excludes the use of calcium and magnesium carbonates, metallic oxides and hydroxides. Typical powdery excipients which are compatible with the present invention are: Calcium phosphates; e.g. hydrated dicalcium phosphate, tricalcium phosphate, calcium pyrophosphate.

Insoluble sodium metaphosphate.

Precipitated colloidal silica.

Binding agents which may be used in the ex cipient of the tooth-paste of the present invention are for example chosen from: sodium carboxymethylcellulose sodium alginate sodium carraghenate bentonites natural hydrocolloids (various gums) carboxyvinylic polymers.

It is however necessary to specify that the binding agents of the acid part should be compatible with the pH thereof and its viscosity should be stabilised in relation to the medium used.

The following products may be used as humectants: Glycerol Sorbitol (70So) Propylene glycol.

Preferred wetting agents are: Sodium laurylsuiphate.

Sodium laurylsarcosinate.

Sodium laurylsulphoacetate.

The following preservatives may be used in the invention: Derivatives of benzoic acid, e.g.

the chlorinated derivatives Derivatives of sorbic acid.

The pastes containing the peroxide or peroxy salt are prepared separately from those containing the acid compound. The proportion of peroxide or peroxy salt in the oxygentaed part of the composition of the present invention is 5 to 10% by weight based on the weight of that part. The proportion of acidic compound in the acid part of the composition of the present invention is 7.5 to 10% by weight based on the weight of that part.

The invention is described in detail in the following examples, given as an illustration not a limitation to the invention.

Paste containing peroxide or peroxy salt The peroxide used is magnesium peroxide Mug32 at 50% active matter and its proportion in the oxygentaed part of the composition of the present invention from 5 to 10% in weight.

The choice of constituents in the oxygenated part and of their proportions is illustrated in the two following formulae: Formula Formula No.1 No.2 Constituents % in weight in weight MgO2 50% 5 10 Carraghenate Na 1.5 1.5 Benzoate Na 2.5 2.5 Pure precip. silica. 25 20 Laurylsulphate. Na 2 2 Saccharinate Na 0.040 0.040 Methyl Paraoxybenzoate 0.15 0.15 Sorbitol 70% 25 25 Flavouring 0.8 0.8 Water, to 100 100 Paste containing the acid compound The acid used is citric acid and the proportion thereof in the acid part of the composition in the excipient of the present invention is from 7.5 to 10% by weight based on the weight of that part.

The choice of constituents in the acid part and of their proportions is illustrated in the two following formulae: Formula Formula No. 1 No.2 Constituents % in weight in weight Anhydrous citric acid 7.5 10 Carraghenate of Na 1.5 1.5 Carboxymethylcellulose 0.3 0.3 Pyrogenic silica 0.1 0.3 Insol.Na Metaphosphate 15 15 Precipitated pure silica 15 20 Na Laurylsulphate 2 2 Na Saccharinate 0.04 0.04 Methyl paraoxybenzoate 0.15 0.15 Sorbitol at 70% 25 25 Flavouring 0.8 0.8 Water, to 100 100 The process for the preparation of the above formulae is the same for the different formulae and takes place in a mixer at a temperature not exceeding 60"C.

Subject to not exceeding the temperature of 600C for the paste containing the superoxygenated compound, the method of operation is the same for the two formulae.

The binding agent is dissolved under turbogitation in a part of the mixture of water and sorbitol, in which the main water-solubles have already been incorporated. Then the constituents are gradually added, mixing the rest of the liquid phase to the powdery substances in the proportions set out above. The magnesium peroxide in one case and the acid in the other are added at the end of fabrication, before introducing the wetting agent and the sweetener. Close mixing takes place under a vacuum, so that a perfect homogenisation and deaeration are obtained. Preservation takes place in a cool place and in well sealed vats, before packaging in an appropriate wrapping, each of the two pastes being isolated. The preferred relative proportions of each of the two pastes constituting the utilised unit are in the weight ratio 1:1 and correspond to a weight of about 0.500g each.

The following table gives the ranges of the relative proportions in weights of acid and peroxide which are present per unit used.

The composition of the tooth-paste having thus been prepared, the active constituent of each paste can only react upon the other once in contact, during brushing and due to its mechanical action. During storage, the oxygen generator is stable.

Acid content Acid content Acid of acidic of acidic paste at 7.5% paste at 10% Citric acid 0.0375 g 0.0500 g Tartaric acid 0.0405 g 0.0540 g Malic acid 0.0360 g 0.0480 g Phosphoric acid - 0.0300 g 0.0400 g Density 1.7

Peroxide Peroxide content content Peroxide of per- of per oxide oxide paste at paste at 5% 10% 0% Magnesium per- 0.025 g 0.050 g oxide This control of the release of oxygen until in contact with the gums is effected by a simple and quick method allowing the concentration of oxygen liberated in the saliva to be tested 'in vivo' both qualitatively and quantitatively.

1. Principle The majority of peroxy salts, peroxides, either in a neutral medium or in an acidic medium, liberate the iodine of potassium iodide.

In the case of magnesium peroxide, after an acid attack and in the presence of the saliva, hydrogen peroxide is produced according to the reaction MgO2 + H2 SO4 = H2 2 + MgSO4, which, upon contact with the mucousa, readily liberates its oxygen, which can be shown by potassium iodide in the presence of dilute sulphuric acid (H2 2 + 2KI + 2H2 S04 = 12 + 2K2 S04 + 2H2 0). The quantity of displaced iodine is proportional to the quantity of dissolved oxygen and permits the quantity to be determined.

2. Technique Since saliva contains traces of dissolved oxygen as well as oxidase and peroxidase, the operation is effected in relation to a sample constituted by the result of brushing the teeth for two minutes with one gram of paste containing peroxide which is then centrifuged and filtered. The operation is similarly effected by mixing the quantities of oxygenating paste and acid in the previously determined proportions, necessary to spread one gram of mixture on a previously moistened tooth-brush.

As in the first case, brushing takes place for two minutes, and sample is centrifuged and filtered.

In two test tubes, the following are simultaneously incorporated: Sample Tube Experimental Tube a) Filtrate MgO2 5 ml Filtrate MgO2 + Acid 5 ml b) NH2 S04 XX drops NH2 S04 XX drops c) Sol. KI 20% III Sol. KI 20% III drops drops After stirring, the iodine is liberated in proportion to the concentration of oxygen.

The speed and intensity of the reaction, which is maximal at the end of half an hour, permits a very clear visual appreciation (brown colour) of the quantity of oxygen dissolved in the saliva after two minutes brushing, in relation to the sample. This rapid method only constitutes a test and that the classical analytic techniques maintain their entire value.

The tooth-paste compositions according to the present invention are extremely useful in prophylaxis and in the treatment of buccodental infections.

The release of oxygen on the gum tissues themselves acts on the anaerobic flora in the dental plaque and gives to the tooth-paste composition the following properties: bucco-dental antisepsis, deodorisation of the breath (particularly useful for heavy smokers), tonic action on the tissues, contribution to prophylaxis and treatment and for the care of infectious and inflammatory states of the periodontium and the bucco-lingual mucosa, such as gingivitis, stomatitis, pyorrhea, recession of the gums and prophylaxis of caries.

WHAT I CLAIM IS: 1. A toothpaste composition capable of liberating nascent oxygen upon contact with the gums which comprises two active parts which are each separately coated in a pharmaceutically acceptable excipient and separately wrapped, the first active part comprising a stable superoxygenated compound which is insoluble in water together with a toothpaste carrier or diluent, the superoxygenated compound being present in an amount of from 5 to 10% by weight based on the weight of the first active part and the second active part comprising a pharmaceutically acceptable mineral or organic acid or acid salt together with a toothpaste carrier or diluent, the mineral or organic acid or acid salt being present in an amount of from 7.5 to 10% by weight based on the weight of the second active part.

2. A toothpaste composition as claimed in Claim 1 wherein the stable superoxygenated compound insoluble in water is chosen from metallic peroxides and peroxy salts which do not liberate nascent oxygen at ambient tempersture except in the presence of an acid.

3. A toothpaste composition as claimed in Claim 1 or Claim 2, wherein the superoxygenated compound is magnesium peroxide.

4. A toothpaste composition as claimed in any of Claims 1 to 3 wherein the pharmaceutically acceptable acid is selected from phosphoric, citric, malic and tartaric acids.

5. A composition as claimed in any of Claims 1 to 4 which is capable of bringing the pH of the saliva from pH 6.7 to a pH of from 3 to4.

6. A toothpaste as claimed in any of Claims 1 to 5 wherein the active part comprising a pharmaceutically acceptable mineral or organic acid or salt has a pH of from 2 to 3.

7. A toothpaste composition as claimed in Claim 1 substantially as herein described.

**WARNING** end of DESC field may overlap start of CLMS **.

Claims (7)

1. **WARNING** start of CLMS field may overlap end of DESC **.

   Sample Tube Experimental Tube a) Filtrate MgO2 5 ml Filtrate MgO2 + Acid

   5 ml b) NH2 S04 XX drops NH2 S04 XX drops c) Sol. KI 20% III Sol. KI 20% III drops drops After stirring, the iodine is liberated in proportion to the concentration of oxygen.

   The speed and intensity of the reaction, which is maximal at the end of half an hour, permits a very clear visual appreciation (brown colour) of the quantity of oxygen dissolved in the saliva after two minutes brushing, in relation to the sample. This rapid method only constitutes a test and that the classical analytic techniques maintain their entire value.

   The tooth-paste compositions according to the present invention are extremely useful in prophylaxis and in the treatment of buccodental infections.

   The release of oxygen on the gum tissues themselves acts on the anaerobic flora in the dental plaque and gives to the tooth-paste composition the following properties: bucco-dental antisepsis, deodorisation of the breath (particularly useful for heavy smokers), tonic action on the tissues, contribution to prophylaxis and treatment and for the care of infectious and inflammatory states of the periodontium and the bucco-lingual mucosa, such as gingivitis, stomatitis, pyorrhea, recession of the gums and prophylaxis of caries.

   WHAT I CLAIM IS: 1. A toothpaste composition capable of liberating nascent oxygen upon contact with the gums which comprises two active parts which are each separately coated in a pharmaceutically acceptable excipient and separately wrapped, the first active part comprising a stable superoxygenated compound which is insoluble in water together with a toothpaste carrier or diluent, the superoxygenated compound being present in an amount of from 5 to 10% by weight based on the weight of the first active part and the second active part comprising a pharmaceutically acceptable mineral or organic acid or acid salt together with a toothpaste carrier or diluent, the mineral or organic acid or acid salt being present in an amount of from 7.5 to 10% by weight based on the weight of the second active part.
2. 2. A toothpaste composition as claimed in Claim 1 wherein the stable superoxygenated compound insoluble in water is chosen from metallic peroxides and peroxy salts which do not liberate nascent oxygen at ambient tempersture except in the presence of an acid.
3. 3. A toothpaste composition as claimed in Claim 1 or Claim 2, wherein the superoxygenated compound is magnesium peroxide.
4. 4. A toothpaste composition as claimed in any of Claims 1 to 3 wherein the pharmaceutically acceptable acid is selected from phosphoric, citric, malic and tartaric acids.
5. 5. A composition as claimed in any of Claims 1 to 4 which is capable of bringing the pH of the saliva from pH 6.7 to a pH of from 3 to4.
6. 6. A toothpaste as claimed in any of Claims

   1 to 5 wherein the active part comprising a pharmaceutically acceptable mineral or organic acid or salt has a pH of from 2 to 3.
7. 7. A toothpaste composition as claimed in Claim 1 substantially as herein described.