TOOTHPASTE COMPOSITION
The present invention relates to an oral care composition comprising bioactive zinc salts and chalk.
EP-Al-O 740 932 (Unilever) discloses a visually-clear gel type dentifrice comprising a zinc salt which is more water soluble than zinc citrate, an amino acid which can bind zinc and a low refractive index type abrasive silica.
US 5 470 561 (Klugkist ) discloses an anti -plaque mouthwash comprising a zinc salt and triclosan . The composition may also comprise glycine and has a pH of between 4 and 8 , preferably between 5 and 7 , the preferred pH being 6 .
GBA-2 052 978 (Unilever) discloses a toothpaste comprising zinc salts with glycine and a pH of from 4.5 to 8.0.
US 5 632 972 (Williams) discloses a method for minimising damage to gingival and periodontal tissue by delivering a first component comprising zinc and a second component comprising a bicarbonate.
The present invention provides a toothpaste comprising a first phase and a second phase stored in contact with one another, the first phase comprising calcium carbonate as abrasive and an alkali-metal citrate salt, the second phase comprising a zinc salt .
The invention provides a toothpaste which does not form water insoluble zinc species, e.g. zinc hydroxide, upon
storage in a closed container such as a toothpaste tube and hence no gassing on the resulting formation of carbon dioxide. This is because the excess citrate in the first phase associates with any water-soluble zinc species which passes from the second phase to the first phase and prevents it from dissociating and reacting with calcium ions in the chalk.
Preferably, the zinc salt is sparingly soluble in water. This reduces the amount of water-soluble zinc species available for migration into the chalk phase. The most preferred zinc salt is zinc citrate.
Preferably, the molar ratio between the zinc ions and the total citrate is from 1:1 to 1:2, there being at least as much, and preferably more, citrate as zinc. Preferably, the molar ratio between the zinc and the total citrate from 1:1.3 to 1:1.7.
Preferably, zinc citrate is present at from 0.01 to 5% by weight of the toothpaste composition, preferably from 0.5 to 3.0% by weight of the composition. This ratio between the zinc and the citrate salt provides, in this type of formulation, an optimal balance between making enough zinc ions bioavailable, and capable of interacting with bacteria, without forming a deleterious amount of water-insoluble zinc species such as zinc hydroxide.
Preferably, the excess citrate is incorporated into the composition as an alkali metal citric acid salt such as potassium citrate or sodium citrate.
The toothpaste composition also comprises water. Preferably, it comprises from 5 to 50% by weight and most preferably from 15 to 35% by weight of the total composition water.
The abrasive system employed in the first phase is calcium carbonate based. This does not prevent the use of non- calcium carbonate abrasives in addition, such as silicas, perlite, tungsten carbide and silicon carbide. Further, any of these further abrasives may be employed in either phase. Preferably, the second phase comprises abrasive silica.
The first phase preferably comprises from 10 to 70% by weight of the first phase calcium carbonate, more preferably from 20% and most preferably from 35 to 60% by weight of the first phase calcium carbonate.
The second phase preferably comprises from 2 to 20% by weight of the second phase abrasive silica, more preferably from 5 to 12%.
Preferred calcium carbonates include fine ground natural chalk since it has a surprising stability with regard to its interactivity with zinc salts. The term fine ground natural chalk (FGNC) is a known term in the art and suitable examples of such are disclosed in US 2003/0072721 Al (Riley) the contents of which with regards to the definition, types and grades of FGNC are incorporated herein by reference. Nevertheless, by FGNC is meant chalk which is obtained by milling limestone or marble deposits. Preferably, the FGNC comprises particulate matter of weight-based median particle
size ranging from 1 to 15 μm and BET surface area ranging from 0.5 to 3 m2/g.
The toothpaste composition according to the invention also preferably comprises a fluoride ion source such as an alkali metal salt of monofluorophosphate, preferably sodium monofluorophosphate. Such fluoride ion source will be present at such an amount to provide free fluoride ion at from 100 to 2000 ppm, preferably from 900 to 1500 ppm.
Preferably, the toothpaste according to the invention comprises an agent selected from the group consisting of anti-caries agents, anti-tartar agents, anti-malodour agents, whitening teeth agents, anti-gingivitis agents and mixtures thereof.
In a most preferred embodiment the first phase comprises from 35 to 45% by weight of the first phase calcium carbonate, from 2 to 4% by weight of the first phase alkali- metal citrate while the second phase comprises from 6 to 10% of the second phase abrasive silica and from 1.5 to 2.5% by weight of the second phase zinc citrate trihydrate.
The toothpaste according to the invention comprise further ingredients which are common in the art, such as:
antimicrobial agents, e.g. chlorhexidine, sanguinarine extract, metronidazole, quaternary ammonium compounds, such as cetylpyridinium chloride; bis-guanides, such as chlorhexidine digluconate, hexetidine, octenidine,
alexidine; and halogenated bisphenolic compounds, such as 2,2 ' methylenebis- (4-chloro-6-bromophenol) ;
anti-inflammatory agents such as ibuprofen, flurbiprofen, aspirin, indomethacin etc.;
anti-caries agents such as sodium- and stannous fluoride, aminefluorides, sodium monofluorophosphate, sodium trimeta phosphate and casein;
plaque buffers such as urea, calcium lactate, calcium glycerophosphate and strontium polyacrylates;
vitamins such as Vitamins A, C and E;
plant extracts;
desensitising agents, e.g. potassium citrate, potassium chloride, potassium tartrate, potassium bicarbonate, potassium oxalate, potassium nitrate and strontium salts;
anti-calculus agents, e.g. alkali-metal pyrophosphates, hypophosphite-containing polymers, organic phosphonates and phosphocitrates etc. ; biomolecules, e.g. bacteriocins, antibodies, enzymes, etc.;
flavours, e.g. peppermint and spearmint oils;
proteinaceous materials such as collagen;
preservatives;
opacifying agents;
colouring agents;
pH-adjusting agents;
sweetening agents;
pharmaceutically acceptable carriers, e.g. starch, sucrose, water or water/alcohol systems etc.;
surfactants, such as anionic, nonionic, cationic and zwitterionic or amphoteric surfactants;
particulate abrasive materials such as silicas, aluminas, calcium carbonates, dicalciumphosphates, calcium pyrophosphates, hydroxyapatites, trimetaphosphates, insoluble hexametaphosphates and so on, including agglomerated particulate abrasive materials, usually in amounts between 3 and 60% by weight of the oral care composition. Preferred abrasives are chalk and silica, more preferably fine ground natural chalk.
Humectants such as glycerol, sorbitol, propyleneglycol, xylitol, lactitol etc.;
binders and thickeners such as sodium carboxymethyl- cellulose, hydroxyethyl cellulose (Natrosol®) , xanthan gum, gum arabic etc. as well as synthetic polymers such as polyacrylates and carboxyvinyl polymers such as Carbopol®;
polymeric compounds which can enhance the delivery of active ingredients such as antimicrobial agents can also be included;
buffers and salts to buffer the pH and ionic strength of the oral care composition; and
other optional ingredients that may be included are e.g. bleaching agents such as peroxy compounds e.g. potassium ' peroxydiphosphate, effervescing systems such as sodium bicarbonate/citric acid systems, colour change systems, and so on.
Liposomes may also be used to improve delivery or stability of active ingredients.
Preferably, the buffering agent is sodium hydroxide.
The two phases are preferably extruded into a toothpaste tube using devices known in the art, for example as described in WO 99/01342 (SKB) . They may be extruded such that they are dispensed side-by-side or such that one forms a stripe within the other.
In another preferred embodiment the first and second phases are coaxially arranged in and dispensed from a toothpaste tube, the second phase substantially surrounding the first phase.
Except in the operating and comparative examples, or where otherwise explicitly indicated, all numbers in this
description indicating amounts of material ought to be understood as modified by the word 'about' .
The term 'comprising' is meant not to be limiting to any subsequently stated elements but rather to encompass non- specified elements of major or minor functional importance. In other words the listed steps, elements or options need not be exhaustive. Whenever the words 'including' or 'having' are used, these terms are meant to be equivalent to 'comprising' as defined above.
Embodiments according to the invention shall now be discussed with reference to the following non-limiting examples.
EXAMPLE 1
The following example is a toothpaste made by standard processes . The two pastes are coextruded into a toothpaste tube using known processes.