Classifications

• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/04—Dispersions; Emulsions
  • A61K8/06—Emulsions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/04—Dispersions; Emulsions
  • A61K8/06—Emulsions
  • A61K8/062—Oil-in-water emulsions
• • 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
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
  • A61K8/345—Alcohols containing more than one hydroxy group
• • 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
  • A61K8/41—Amines
  • A61K8/416—Quaternary ammonium compounds
• • 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
  • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
  • A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
  • A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings

Definitions

• the present invention relates to a concentrated mouthrinse and methods of use and methods of making the same, wherein there is an efficient delivery of an- timicrobiais to the oral cavity thereby reducing oral bacteria, mouth malodor and further promoting oral health.
• Plaque is an organic mixture of living bacteria found in the mouth.
• the bacteria found in plaque can secrete acids, enzymes and microtoxins which can cause caries, oral malodor and periodontal diseases such as gingivitis.
• the compositions of the present invention possess a unique ability to form a concentrated and aesthetically pleasing mouthrinse.
• This invention provides a system by which, upon dilution, a relatively low concentration of a germ-killing cationic antimicrobial agent can be efficiently delivered to the oral cavity. In combination with the delivery of the antimicrobial, it has also been discovered this mechanism efficiently delivers a flavoring agent.
• the present invention relates to compositions comprising certain solvents and cationic antimicrobial agents solubilized into a concentrated solution which is aesthetically pleasing.
• This mouthrinse is diluted with water to provide a safe and effective means for reducing bacteria found in the oral cavity and further provides a signal of efficacy to users.
• the antimicrobials and flavoring agents of the present invention are delivered more efficiently while employing similar concentrations. It is therefore an object of the present invention to provide a concentrated and aesthetically pleasing mouthrinse which upon dilution delivers more effectively the antimicrobial and flavoring agents while employing concentrations of these ingredients similar to ready-to-use mouthwashes and rinses.
• a further object of the present invention is to provide a safe and effective means of preparing a mouthrinse from the concentrated solution.
• compositions of non-carbonated, concen- trated, oil-in-water emulsions suitable for use as oral mouthrinses comprising:
• safety and effective amount means an amount sufficient to reduce oral bacteria and/or enhance such reduction while providing no adverse effects to the hard and soft tissues of the oral cavity.
• substantially free of anionic surfactant means less than 0.05%, preferably less than 0.01% and most preferably less than 0.001% of an anionic surfactant.
• substantially free of non-ionic surfactant means an amount which will not substantially impair the activity of the cationic surfactant. Generally, this means the composition must contain less then about 0.5%, preferably less than 0.3% and most preferably less than 0.2% of the nonionic surfactant.
• compositions of this invention employ a cationic antimicrobial agent, a solvent or a mixture of solvents, a flavoring agent or mixture of flavoring agents and water.
• the concentrated mouthrinse is preferably clear.
• “clear” as used herein does not mean colorless, but means substantially lacking the presence of particles of sufficient size to scatter visible light as detected visually.
• the concentrated mouthrinse is mixed with a desired amount of water. This mixing allows for phase separation immediately prior to use. Without being limited by theory, it is believed that this phase separation provides an efficient delivery of a sufficient level of antimicrobial agents, while allowing for optimal taste and aesthetics.
• the amount of water added to the concentrated mouthrinse mixture must be high enough to result in the necessary phase change as described below.
• This phase change is conveniently observed by the user during dilution and provides a visual signal alerting the consumer the composition is ready for use.
• the antimicrobial of the present invention due to its inherent properties having both a hydrophobic and hydrophylic moiety, resides primarily at the oil-water interface. This phase separation, where the oily phase is dispersed within the water phase of the diluted mouthrinse remains for several hours. However, eventually the oily phase will coalesce and form a separate layer. Therefore, it is undesirable to dilute more concentrate than will be immediately used.
• the pH of the present concentrated compositions range from about 5.0 to about 8.0 with the preferred pH being from about 6.5 to about 7.0 with the most preferred pH being about 6.9.
• the essential, as well as optional components of the compositions of the present invention are described below.
• the antimicrobials used in the compositions of the present invention can be any cationic antimicrobial agents such as quaternary ammonium compounds and substituted guanidines such as chlorhexidine and the corresponding compound alexidine. Mixtures of these cationic antimicrobials may also be used in the present invention.
• Antimicrobial quaternary ammonium compounds include those in which one or two of the substitutes on the quaternary nitrogen has a carbon chain length (typicallv alkyl group) from about 8 to about 20, typically from about 10 to about 18 carbon ..:oms 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.
• 5-amino-l,3-bis(2-ethyl-hexyl)-5-methyl hexa hydropyrimidine, benzalkonium chloride, benzethonium chloride and methyl benzethonium chloride are exemplary of typical quaternary ammonium antibacterial agents.
• Other compounds are bis[4-(R-amino)-l -pyridinium] alkanes as disclosed in U.S. Pat. No. 4.206.215. June 3, 1980 to Bailey which is incorporated herein by reference.
• the pyridinium compounds are the preferred quaternary ammonium compounds, the most preferred being cetylpyridinium chloride or tetradecylpyridinium chloride.
• Quaternary ammonium antimicrobial agents are included in the present invention at levels of about 0.05% to about 10.0%, preferably from about 0.2% to 3.0%, more preferably from about 0.5% to about 3.0% and most preferably from about 0.5% to about 2.0%.
• the substituted guanidines are also suitable for use in this invention.
• Bis- biguanide compounds which are preferred for use in the present invention, are those having the generic formula: R NH NH NH NH R
• A-(X) z -N ⁇ C ⁇ H ⁇ C ⁇ NH(CH2) n ⁇ NH ⁇ C ⁇ H ⁇ C-N ⁇ (X , ) n -A wherein A and A' can be either (1) a phenyl radical which optionally is substituted by an alkyl or alkoxy group containing from 1 to about 4 carbon atoms, a nitro group, or a halogen atom; (2) an alkyl group containing from about 1 to about 12 carbon atoms; or (3) alicyclic groups containing from about 4 to about 12 carbon atoms; wherein X and X 1 each represent an alkylene radical containing from about 1 to about 3 carbon atoms; wherein Z and Z 1 each can be either 0 or 1; wherein R and R' each represent either hydrogen, an alkyl radical containing from about 1 to about 12 carbon atoms, or an aralkyl radical containing from about 7 to about 12 carbon atoms; wherein n is an integer from 2 to 12 inclusive; wherein
• the water soluble salts of the above compounds are especially preferred for use herein. Suitable water soluble salts include the chloride, the . fluoride, and especially the acetate salt.
• the preferred substituted guanidine is chlorhexidine-[ 1 ,6-di(-N ⁇ 5>-pchlorophenyl-N-diguanido)-hexane] .
• the substituted guanidine antimicrobials are generally used in the present compositions at a level of from about 0.05% to about 3.0%, preferably from about 0.5% to about 3.0% and most preferably from about 0.5% to about 2.0%.
• Solvents or Solvent System Another essential ingredient of the composition of the present invention is a solvent or solvent system such as those described in U.S. Patent 5.141.961. August 25, 1992 to Coapman, herein incorporated by reference.
• the solvent(s), which constitute the bulk of the present composition act as a carrier for the flavoring oils.
• the solvent or solvent system solubilizes the flavoring oils in the concentrate and aids in dispersing, upon dilution with added water, all oil soluble components of the concentrated formulation thereby forming a uniformly dispersed mixture.
• the solvents most preferred for use in the present invention are: propylene glycol and polyethylene glycols or mixtures thereof. Propylene glycol and polyethylene glycols being most preferred.
• Propylene glycol is well known in the art and available from any of a number of suppliers. Propylene glycol is miscible in all proportions and also has the ability to dissolve the flavoring agent of the present invention. Propylene glycol suitable for use in the present invention is obtainable from any number of sources such as Dow Chemical. Polyethylene glycols are also well known in the art and lower molecular weight species possess characteristics similar to propylene glycol. Polyethylene glycols suitable for use in the present invention are the polyethylene glycols having an average molecular weight of less than or equal to 600, such as PEG 300 "Carbowax" supplied by Union Carbide.
• Solvents comprise from about 30% to about 85%, preferably from about 35% to about 75% and most preferably from about 45% to about 60% of the concentrated form of the mouthrinse.
• Water Water is present in the concentrated composition of the present invention. Water comprises from about 10% to about 40%, preferably from about 18% to about 30% and most preferably from about 22% to about 26% of the oral compositions described herein. These amounts of water include the free water which is added, plus that amount which is introduced with other materials such as with sorbitol.
• the water, used in the present invention should preferably be deionized, distilled, free o organic impurities and bacteria and substantially free of metal ions. Flavoring Agents
• flavoring agent Another essential ingredient of the present invention is a flavoring agent or a mixture of compatible flavoring agents.
• Suitable flavoring agents include: anise, cassia, clove, dihydroanethole, estragole, menthol, peppermint, oxanone, phenyl ethyl alcohol, sweet birch, thymol, eugenol, eucalyptol, wintergreen, spearmint, cinnamic aldehyde, menthone, alpha-ionone, ethyl vanillin, limonene, isoamylacetate, benzaldehyde, ethylbutyrate and many others.
• the flavoring agents comprise from about 0.2% to about 9.0%, preferably from about 0.6% to about 4.0% and most preferably from about 2.0% to about 4.0% of the herein described composition.
• An optional ingredient useful in the present invention is a humectant or a mixture of compatible humectants.
• Humectants are well known in the art.
• suitable humectants include the polyhydric alcohols such as xylitol, glycerin and sorbitol as well as other polyhydroxy alcohols and mixtures of these humectants.
• it is feasible to use a single humectant it is preferred to incorporate a combination of humectants.
• Humectants provide from 0% to about 55%, and most preferably from about 15% to about 30% of the herein described invention.
• humectants includes glycerin and sorbitol in a ratio of about 10: 1 to about 1:4, and most preferably from about 3:1 to about 1:2.
• Other optional components include, but are not limited to: coloring agents; sweeteners, including saccharin, dextrose, levulose, cyclamate and aspartate, along with many others; buffering systems such as benzoic acid and sodium benzoate, citric acid and sodium citrate and any other buffering system compatible with the invention's herein described essential components.
• Another optional component of the present invention is ethyl alcohol. Ethyl alcohol provides several functions when combined in the compositions of the present invention.
• Ethyl alcohol can be incorporated in the present invention at a level of less than about 40%, preferably less than about 10% and most preferably in concentrations of less than 2%.
• Still another optional component of the present invention is a cooling agent such as those described in U.S. Patent 4.136.163. January 23, 1979, to Watson et al., U.S. Patent 4.230.668. October 28, 1980 to Rowsell et al. and U.S. Patent 4.032.661. to Rowsell et al. all herein incorporated by reference.
• a cooling agent such as those described in U.S. Patent 4.136.163. January 23, 1979, to Watson et al., U.S. Patent 4.230.668. October 28, 1980 to Rowsell et al. and U.S. Patent 4.032.661. to Rowsell et al. all herein incorporated by reference.
• One particularly preferred cooling agent is N-ethyl-p-menthane-3-carboxamide (WS-3 supplied by Sterling Organics), taught by the above incorporated U.S. Patent 4.136.163.
• the present invention to be effectively used as an antimicrobial mouthrinse should be prepared by the user just prior to use by adding an aqueous solution, preferably water to the concentrated oil-in-water emulsion or by adding the con ⁇ centrated oil-in-water emulsion to water.
• an aqueous solution preferably water to the concentrated oil-in-water emulsion or by adding the con ⁇ centrated oil-in-water emulsion to water.
• the oil-in-water emulsion breaks, leaving the diluted composition cloudy (or opaque). This generally occurs with the addition to the emulsion of greater than 5% v/v, preferably from about 10% and most preferably from about 20% of an aqueous solution. Therefore, after dilution, the resulting composition is not completely transparent. This transformation can be visually observed, or can be readily measured using a spectrophotometer.
• any appreciable difference in the absorbance of light as between the undiluted concentrate and the diluted concentrate signifies the interaction and diffusion of light necessary to the invention establishing the range of "cloudiness.”
• No additional agitation or mixing energy is required to cause rapid dispersion, forming a uniformly dispersed mixture of the compositions antimicrobial(s), flavoring oil(s) and other ingredients.
• the dilution of the mouthrinse concentrate requires mixing the concentrate with water in a range of ratios from about 1:1 to about 1:100, preferably from about 1:2 to about 1:50, more preferably from about 1:5 to about 1:50 and most preferably from about 1:20 to about 1:50.
• COMPOSITION USE in its method aspect involves rinsing the oral cavity with a safe and effective amount of a mouthrinse prepared by the user by diluting the herein described concentrate with a suitable amount of water.
• a safe and effective amount of a mouthrinse prepared by the user by diluting the herein described concentrate with a suitable amount of water.
• an amount of at least about 0.01 grams of the antimicrobial becomes available by diluting the concentrate as described above and is effective in eliminating or reducing the bacterial flora residing within the oral cavity.
• a concentrated mouthrinse of the present invention is prepared by combining the following ingredients as described below. Also given is the dilution factor for diluting the concentrated composition.
• the diluted composition will become cloudy signaling the user the mouthrinse is ready for use.
• the user then rinses the oral cavity with approximately 20 ml of the diluted composition and expels the mouthrinse. This use reduces or eliminates the bacteria found in the oral cavity, preventing gingivitis and oral calamity.

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• 1993
  • 1993-09-16 US US08/122,750 patent/US5405604A/en not_active Expired - Lifetime
  • 1993-10-01 AT AT93923200T patent/ATE156700T1/de not_active IP Right Cessation
  • 1993-10-01 CA CA002146635A patent/CA2146635C/en not_active Expired - Lifetime
  • 1993-10-01 AU AU52965/93A patent/AU5296593A/en not_active Abandoned
  • 1993-10-01 WO PCT/US1993/009391 patent/WO1994008558A1/en not_active Ceased
  • 1993-10-01 JP JP6510060A patent/JPH08502292A/ja active Pending
  • 1993-10-01 EP EP93923200A patent/EP0664693B1/de not_active Expired - Lifetime
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