Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
  • A61K8/20—Halogens; Compounds thereof
  • A61K8/21—Fluorides; Derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
  • A61K8/24—Phosphorous; Compounds thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
  • A61K8/27—Zinc; Compounds thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/676—Ascorbic acid, i.e. vitamin C
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

• the present invention relates to an opaque toothpaste composition comprising bioactive zinc salts in a chalk formulation.
• the invention also relates to a method for making said composition.
• EP-Al-O 740 932 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 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 discloses a toothpaste comprising zinc salts with glycine and a pH of from 4.5 to 8.0.
• US 5 632 972 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.
• US 4 425 325 discloses an oral composition containing biologically active zinc ions with glycine and having an adjusted pH of about 4.5 to 9.4.
• GB 1 319 247 discloses a non-liquid anticalculus dental composition
• a dental vehicle discloses a non-liquid anticalculus dental composition
• a zinc, cupric or zirconium complex of a fluorinated ⁇ - diketone discloses a non-liquid anticalculus dental composition
• a dental vehicle discloses a non-liquid anticalculus dental composition
• a zinc, cupric or zirconium complex of a fluorinated ⁇ - diketone discloses a non-liquid anticalculus dental composition
• US 4 325 939 discloses an alkali metal or ammonium zinc citrate prepared for use in dental compositions and especially in mouthwash compositions.
• compositions such as dentifrices comprising a mixture of a stannous salt such as stannous fluoride or stannous pyrophosphate and a zinc salt such as zinc citrate.
• an opaque toothpaste composition according to claim 1.
• the monofluorophosphate salt provides flurode ion to the toothpaste composition, the fluoride ion is an effective anti-caries agent.
• monofluorophosphate salts are not stable in chalk-containing toothpastes and so a stabilising agent is required. While trisodium phosphate
• TSP Tin oxide
• Zinc phosphate is not a good source of bioavailable zinc. Therefore, by incorporating a chelating agent for the zinc the levels of monofluorophosphate, and also zinc can be maintained after prolonged storage.
• the zinc salt 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.
• the log K 3 I of the chelating ligand with the zinc ion is equal to or greater than the log K 3 I of the acid anion and the zinc ion of the sparingly soluble zinc salt.
• water soluble zinc salts are preferred. Suitable zinc salts include zinc chloride, zinc sulphate and zinc fluoride. The preferred zinc salt is zinc sulphate which, in this type of formulation, provides the optimum balance as described above .
• the alkali metal is preferably potassium or sodium, most preferably sodium.
• the alkali metal phosphate is preferably a mono, di- or tri- phosphate salt, most preferably a triphosphate.
• the chelating agent for the zinc salt has a log K 3 I of from 4.0 to 6.0.
• the log K 3 I is the logarithm of the primary Stability Constant which is the binding affinity for a particular ligand with a particular metal ion, in the present invention zinc.
• the chelating agent is present at from 0.001 to 6% by weight of the composition, preferably at from 0.5 to 4.0% by weight of the composition.
• Preferred chelating agents include alkali metal salts of citric acid, alanine, glycine and serine. The most preferred are the alkali metal salts of citric acid, especially potassium citrate and most preferably tri-potassium citrate, which provides an optimal balance between being able to protect the zinc salt from hydrolysis (leading to the formation of carbon dioxide) in the chalk system and keeping it soluble and bioavailable .
• the abrasive system is present at from 10 to 70% by weight of the toothpaste composition, preferably at from 20 to 60% and most preferably at from 35 to 45% by weight of the toothpaste composition.
• the alkali metal phosphate is present at from 0.01 to 2% by weight, preferably from 0.15 to 1% and especially preferably from 0.2 to 0.5% by weight of the composition.
• the abrasive system employed in the present invention is calcium carbonate based. This does not prevent the use of non-calcium carbonate abrasives in addition, such as silicas, tungsten carbide and silicon carbide.
• the abrasive system comprises at least 50% by weight calcium carbonate, more preferably at least 75% by weight calcium carbonate and most preferably at least 95% by weight calcium carbonate. In the most preferred embodiment of the present invention the abrasive system comprises 100% by weight calcium carbonate although mixtures of calcium carbonate and additional abrasives are possible.
• Preferred calcium carbonates include fine ground natural chalk since it has a surprising stability with regard to its interactivity with zinc salts.
• fine ground natural chalk FGNC
• FGNC fine ground natural chalk
• 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.
• FGNC is meant chalk which is obtained by milling limestone or marble deposits.
• the FGNC comprises particulate matter of weight-based median particle size ranging from 1 to 15 ⁇ m and BET surface area ranging from 0.5 to 3 m 2 /g.
• composition according to the invention also preferably comprises a fluoride ion source such as an alkali metal salt of monofluorophosphate, preferably sodium monofluorophosphate .
• 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.
• the toothpaste composition 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;
• 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;
• 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 toothpaste 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;
• 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.
• a method of making an opaque toothpaste composition comprising the steps of forming a zinc-chelate solution and buffering to a pH which is equal to or higher than that of the calcium carbonate in an aqueous suspension before mixing with the suspended calcium carbonate. Further materials such as flavours may be added to the final mix.
• the following example formulation is an embodiment according to the invention. It is made by mixing first the zinc sulphate heptahydrate with glycine (and other minors) and buffering to a pH of from 8.5 to 9.5 with sodium hydroxide. The calcium carbonate, surfactant and structurants are then added to the zinc-chelate mix. The flavours are added last.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Birds (AREA)
• Epidemiology (AREA)
• Chemical & Material Sciences (AREA)
• Inorganic Chemistry (AREA)
• Oral & Maxillofacial Surgery (AREA)
• Cosmetics (AREA)

Priority Applications (1)

Applications Claiming Priority (3)

Publications (1)

Family

ID=37546780

Family Applications (1)

Country Status (4)

Families Citing this family (10)

Family Cites Families (6)

• 2007
  • 2007-07-02 EP EP07765752A patent/EP2046454A1/de not_active Ceased
  • 2007-07-02 WO PCT/EP2007/056627 patent/WO2008006725A1/en active Application Filing
  • 2007-07-02 CN CNA2007800262765A patent/CN101489628A/zh active Pending
  • 2007-07-02 BR BRPI0711979-8A patent/BRPI0711979A2/pt not_active IP Right Cessation

Non-Patent Citations (1)

Also Published As

Similar Documents

Legal Events