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WO1995007683A1 - Compositions contenant des derives du phosphate - Google Patents

Compositions contenant des derives du phosphate Download PDF

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Publication number
WO1995007683A1
WO1995007683A1 PCT/US1994/010044 US9410044W WO9507683A1 WO 1995007683 A1 WO1995007683 A1 WO 1995007683A1 US 9410044 W US9410044 W US 9410044W WO 9507683 A1 WO9507683 A1 WO 9507683A1
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WO
WIPO (PCT)
Prior art keywords
composition
group
composition according
oral
compositions
Prior art date
Application number
PCT/US1994/010044
Other languages
English (en)
Inventor
Michael Johannes Eis
Dennis George Anthony Nelson
James Edwin Thompson
Jeffrey Charles Hayes
Dorothy Jean Stuart
Original Assignee
The Procter & Gamble Company
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by The Procter & Gamble Company filed Critical The Procter & Gamble Company
Priority to BR9407550A priority Critical patent/BR9407550A/pt
Priority to EP94927360A priority patent/EP0719128A1/fr
Priority to AU76832/94A priority patent/AU7683294A/en
Priority to JP7509236A priority patent/JPH09502718A/ja
Publication of WO1995007683A1 publication Critical patent/WO1995007683A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
    • A23G4/00—Chewing gum
    • A23G4/06—Chewing gum characterised by the composition containing organic or inorganic compounds
    • A23G4/064—Chewing gum characterised by the composition containing organic or inorganic compounds containing inorganic compounds
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L27/00—Spices; Flavouring agents or condiments; Artificial sweetening agents; Table salts; Dietetic salt substitutes; Preparation or treatment thereof
    • A23L27/70—Fixation, conservation, or encapsulation of flavouring agents
    • A23L27/75—Fixation, conservation, or encapsulation of flavouring agents the flavouring agents being bound to a host by chemical, electrical or like forces, e.g. use of precursors
    • 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
    • A61K8/55—Phosphorus compounds
    • 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

  • compositions comprising one or more phosphate derivatives, and carrier materials wherein the compositions are in a form suitable for oral or topical administration.
  • These compositions preferably contain a safe and effective amount of one or more active materials such as those which provide nutritional, therapeutic, antimicrobial, pharmaceutical, medicinal, and/or aesthetic benefit, and those commonly used in health care products.
  • a wide variety of flavor, coolant and sweetener agents are used in consumer and health care products today.
  • Aesthetic qualities of these compositions such as taste, smell, mouthfeel, and after-taste are important concerns for consumer acceptability. Products with poor flavor, a bad after-taste or other negative aesthetics may limit consumer acceptability initially or over an extended period of time, thereby limiting consumer usage and compliance with treatment regimens.
  • An additional aspect of consumer acceptability and compliance is the consumer's perception of efficacy. Consumer satisfaction with a product is likely to be increased if some type of sensory signal exists to remind the consumer that the product is working after ingestion, administration or expectoration.
  • phosphate derivatives comprising flavor, coolant, and/or sweetener components may be incorporated into oral or topical compositions to deliver pleasing aesthetics and high consumer acceptability. It has also been discovered that these compositions for oral or topical administration may be formulated to include a safe and effective amount of one or more actives. These compositions may provide sustained coolant, flavor and/or sweetener activity, depending on the particular derivative being used. These phosphate derivatives may also serve to improve the aesthetics of the compositions and provide a sensory signal to the user.
  • compositions that are aesthetically pleasing to the consumer. It is also an object of the present invention to provide compositions which provide a sensory signal to the user, and preferably contain a safe and effective amount of one or more actives.
  • compositions comprising:
  • R is selected from the group consisting of a coolant component, a sweetener component, and a flavorant component; wherein R 1 and R" are independently selected from the group consisting of R, an adherent component, M+, M++, C+, and hydrogen; wherein X, X', and X" are independently selected from the group consisting of oxygen, nitrogen, and sulfur; wherein n is an integer from 1 to 3; and
  • compositions are in a form suitable for oral or topical administration.
  • the subject invention relates to a composition comprising one or more phosphate derivatives, and carrier materials wherein the compositions are in a form suitable for oral or topical administration. These compositions also preferably contain a safe and effective amount of one or more actives.
  • active means an agent which provides an effect greater than an excipient such as agents providing nutritional, therapeutic, antimicrobial, pharmaceutical, medicinal, and/or aesthetic benefit and those commonly used in health care products.
  • suitable for oral or topical administration means any formulation that is suitable for the convenient administration of the composition whereby the composition is intentionally swallowed, chewed, ingested, retained in the oral cavity for any period of time, placed in contact with internal mucous membranes of the body, such as those of the nose, mouth, or throat whether by direct or indirect application or inhalation to the nasal passages, or applied to the surfaces of the skin for therapeutic reasons or reasons other than for cosmetic benefit.
  • a safe and effective amount means a sufficient amount of material to provide the desired benefit without undue adverse side effects (such as toxicity, irritation or allergic response) commensurate with a reasonable benefit/risk ratio when used in the manner of this invention.
  • the specific safe and effective amount will vary with such factors as the particular condition that is being treated, the severity of the condition, the duration of the treatment, the physical condition of the patient, the nature of concurrent therapy (if any), and the specific formulation and optional components employed.
  • compositions contain one or more phosphate derivatives. These compounds may be formulated by phosphorylating a least one coolant, sweetener or flavorant component. These compounds also include linking at least one coolant, sweetener or flavorant component to an adherent component via a phosphate bridge. In addition, pyrophosphate and triphosphate groupings may be substituted for the phosphate group. Coolant, flavorant, or adherent components may also be linked to phosphorous via two functional groups or attachment sites. Furthermore, the phosphate derivatives described above may be bound via Coulombic interaction with charged compounds or materials, including polymers. The present compositions may deliver the desired coolant, flavorant and/or sweetener qualities through the action of the phosphate derivative itself.
  • compositions may also provide a sustained effect through the release of the coolant, flavorant and/or sweetener component from the molecule after cleavage of the phosphate from the coolant flavorant and/or sweetener by phosphatase enzymes.
  • phosphatase enzymes include but are not limited to acid, basic, and pyrophosphatases.
  • coolant component refers to coolant compounds having a hydroxy, amino, or thiol functionality which is capable of forming an ester, amido, or thioester linkage with a phosphorus(V) atom.
  • Preferred coolant components are selected from the group consisting of menthol, 3-1- menthoxypropane-l,2-diol ("TK-10"), menthone glycerol acetal (“MGA”), and menthyl lactate.
  • TK-10 3-1- menthoxypropane-l,2-diol
  • MCA menthone glycerol acetal
  • menthyl lactate menthyl lactate.
  • menthol and “menthyl” as used herein include dextro- and levorotatory isomers of these compounds and racemic mixtures thereof.
  • flavorant component refers to flavorant compounds having a hydroxy, amino, or thiol functionality which is capable of forming either an ester, amido, or thioester linkage with a phosphorus(V) atom.
  • Preferred flavorant compounds are selected from the group consisting of methyl salicylate, eugenol, vanillin, thymol, cinnamaldehyde glycerol acetal ("CGA”), and linalool.
  • sweetener component refers to sweetener compounds having a hydroxy, amino, or thiol functionality which is capable of forming either an ester, amido, or thioester linkage with a phosphorus(V) atom.
  • Preferred sweetener components are saccharin, mannitol, sorbitol, glucose, sucrose, fructose, and neohesperidin dihydrochalcone.
  • adherent component refers to either monomers, oligomers, or polymers having hydroxy, amino, or thiol functionalities which are capable of forming either ester amido, or thioester linkages with phosphorus(V) atoms.
  • the monomers, oligomers, or polymers may also possess additional hydroxy, amino, or thiol groups which may either remain unsubstituted or be linked via ester amido, or thioester linkages to a phosphorus(V) atom which is also attached to a coolant, flavor, or active portion.
  • Preferred compounds are selected from the group consisting of C12-C18 diacyl glycerol, partially hydrolyzed vinyl acetate/ethylene copolymer, cellulose, chitin, glucose, glucosamine, silica gel, glycerol, and lower alkyl vinyl ether-maleic acids.
  • M+ and M++ refer to physiologically relevant metal cations.
  • physiologically relevant metal cations refers to metal cations that are significant to the organic or bodily processes of a human or lower animal.
  • Preferred “M+” cations are sodium and potassium.
  • Preferred "M++" cations are calcium, zinc, magnesium, manganese, copper, and stannous.
  • C+ refers to an "organic” cation.
  • An "organic” cation as used herein refers to cations that contain positively charged nitrogen, phosphorus, oxygen, or sulfur atoms. Such cations may contain more than one positively-charged site and in the case of oligomers or polymers containing nitrogen, phosphorus, oxygen, or sulfur atoms, many positively-charged centers may exist.
  • Preferred "organic" cations include ammonium, protonated amines such as protonated glucosamine, and partially or fully protonated amine-containing polymers such as protonated chitosan.
  • the phosphate derivatives of this invention are represented by the following formula:
  • R is selected from the group consisting of a coolant component, a sweetener component, and a flavorant component;
  • R' and R" are independently selected from the group consisting of R, an adherent component, M+, M++, C+, and hydrogen;
  • X, X', and X" are independently selected from the group consisting of oxygen, nitrogen, and sulfur; and n is an integer from 1 to 3.
  • R' may equal R", preferably wherein R' and R" are selected from the group consisting of calcium, zinc, and magnesium, manganese, copper and stannous.
  • Preferred phosphate derivatives have the formula:
  • R is selected from the group consisting of menthol, TK-10, MGA, menthyl lactate, methyl salicylate, saccharin, mannitol, sorbitol, glucose, sucrose, fructose, neohesperidin dihydrochalcone, eugenol, vanillin, thymol, CGA, and linalool;
  • R 1 and R" are independently selected from the group consisting of R, C12- C18 diacyl glycerol, partially hydrolyzed vinyl acetate-ethylene co-polymer, cellulose, chitin, glucosamine, silica gel, glycerol, lower alkyl vinyl ether-maleic acids, sodium, potassium, calcium, zinc, magnesium, manganese, copper and stannous, ammonium, protonated amines, partially or fully protonated amine-containing polymers, and hydrogen;
  • X, X', and X" are independently selected from the group consisting of oxygen, nitrogen, and sulfur; and n is and integer from 1 to 3.
  • R' may equal R", preferably wherein R' and R" are independently selected from the group consisting of calcium, zinc, magnesium, manganese, copper and stannous.
  • phosphate derivatives are menthyl monophosphate, eugenyl monophosphate, thymyl monophosphate, 1-menthyl diphosphate, bis 1-menthyl pyrophosphate, and 1-menthyl triphosphate.
  • the phosphate derivatives are used in the present invention at levels of from about 0.001% to about 25%, preferably from about 0.01% to about 15%, by weight of the composition.
  • Carrier Materials In formulating the compositions of this invention the phosphate derivative will be incorporated into a carrier which may be completely inert or which may contain other active ingredients.
  • carrier materials means one or more compatible substances suitable for administration to a human or lower animal.
  • compatible means that the components of the compositions are capable of being commingled with phosphate derivatives, actives, and with each other, in a manner such that there is no interaction which would substantially reduce the efficacy of the present compositions under ordinary use situations.
  • Carrier materials must also be of sufficiently high purity and sufficiently low toxicity to render them suitable for administration to the human or lower animal being treated.
  • compositions include not only foodstuffs and beverages taken into the mouth and swallowed, but also other orally ingested compositions taken into the mouth for reasons other than for sustenance.
  • Such compositions include (but are not limited to) solid oral dosage forms such as tablets, tablet coatings, caplets, hydrogels, and liquid oral dosage forms such as syrups, emulsions and suspensions.
  • Oral compositions also include those compositions which are taken into the mouth but are not necessarily swallowed, e.g. chewing gum.
  • Topical compositions include compositions applied to, or which in normal usage come in contact with, the internal membranes of the body such as those of the nose, mouth, or throat, whether by direct or indirect application. Such compositions include (but are not limited to) nasal sprays, dentifrices, oral rinses, lozenges, foams, gels, and throat sprays. Topical compositions may also be compositions applied to the external surfaces of the body for therapeutic reasons or reasons other than for cosmetic benefit. Such compositions include ointments, lotions, gels, and creams. Preferred compositions of the present invention are health care compositions such as dentifrices, oral rinses, liquid oral dosage forms and nasal sprays.
  • compositions preferably comprise from about 75% to about 99.999%, and preferably from about 85% to about 99.99%, by weight of the composition.
  • Suitable carrier materials herein, depending on intended end use are selected from the group consisting of solvents, suspending agents, solubilizing agents, diluents, surfactants, buffers, lubricants, thickeners, emulsifiers, flavoring agents, colorants, humectants, sweeteners, co-solvents, binders, disintegrating agents, flow-inducing agents, coolants, plasticizers, wetting agents, antioxidants, stabilizers, and tableting agents. Dentifrices
  • Dentifrice compositions may be of the liquid, paste, powder or gel type. These compositions will usually comprise a finely divided abrasive or polishing material, e.g. precipitated chalk, silica, magnesium silicate, calcium polymetaphosphate, aluminum hydroxide or other similar materials well known in the art. Abrasive materials are more fully described in U.S. Patent 3,070,510, Cooley et al., December 25, 1962, which is incorporated herein by reference. Toothpaste compositions additionally contain a surfactant or foaming agent. Suitable surfactants are those which are reasonably stable and foam throughout a wide pH range, including non-soap anionic, nonionic, cationic, zwitterionic and amphoteric organic synthetic detergents. These surfactants are disclosed by Gieske et al. in U.S. Patent 4,051,234, issued September 27, 1977, also incorporated herein by reference.
  • Water is also present in the dentifrice compositions. Water employed should preferably be deionized and free from organic impurities. Water generally comprises from about 10% to about 50%, and preferably from about 20% to about 40%, by weight of the compositions. These amounts of water include the free water which is added plus that which is introduced with other materials such as with sorbitol.
  • Optional ingredients in dentifrice compositions include flavoring agents, colorants, buffers, lubricants, thickeners, emulsifiers or plasticizers, and humectants.
  • Dentifrice carrier materials typically comprise from about 50% to about 94%, and preferably from about 60% to about 80%, by weight of the dentifrice compositions.
  • Oral Rinses Oral rinses usually comprise an aqueous, alcoholic, or aqueous-alcoholic solution of an antiseptic which is often colored or flavored for palatability.
  • Optional ingredients include humectants, surfactants, sweeteners, emulsifying agents, fluoride ion sources, tartar control, and anti-plaque agents.
  • Oral rinse products may also be formed by dissolving a powder or tablet containing stannous gluconate in water just prior to use.
  • Oral rinse compositions typically are based on a water/ethanol solution having a ratio of water: ethanol of from about 20:1 to about 2:1.
  • Humectants such as glycerin and sorbitol, are usually included to give a moist feel to the mouth.
  • Conventional oral rinse compositions generally comprise, by weight of the composition, from about 0% to 60% ethyl alcohol, 0% to 20% of a humectant, 0% to 2% emulsifying agents, 0% to 0.5% sweetening agents, 0% to 0.3% flavoring agents and the balance water.
  • Liquid oral dosage forms include aqueous and nonaqueous solutions, emulsions, pseudo emulsions, suspensions, and solutions and/or suspensions reconstituted from non-effervescent granules. These dosage forms also contain suitable solvents, emulsifying agents, buffering agents, suspending agents, diluents, natural and artificial sweeteners, coloring agents, and flavoring agents. Antioxidants such as butylated hydroxy anisole or butylated hydroxy toluene, and preservatives such as methyl or propyl paraben or sodium benzoate may also be included.
  • carrier and excipients that may be used to formulate oral dosage forms, are described by Roberts in U.S. Patent 3,903,297, issued September 2, 1975, which is incorporated herein by reference. Since many of the actives are generally used in the form of a water-soluble salt, they can be readily incorporated into conventional aqueous-based formulations. Water-insoluble or poorly soluble actives, generally in base form, may also be incorporated into aqueous-based orally acceptable carriers such as dispersions, suspensions, oil-in-water emulsions and the like by means of suitable dispersing, suspending or emulsifying agents, respectively, which are readily apparent to those skilled in the art of formulations.
  • aqueous-based orally acceptable carriers such as dispersions, suspensions, oil-in-water emulsions and the like by means of suitable dispersing, suspending or emulsifying agents, respectively, which are readily apparent to those skilled in the art of formulations.
  • aqueous-based orally acceptable carrier is one wherein the entire or predominant solvent content is water.
  • Typical carriers include simple aqueous solutions, syrups, dispersions and suspensions, and aqueous based emulsions such as the oil-in-water type.
  • the most preferred carrier is a suspension or solution of the phosphate derivative and active in an aqueous vehicle containing a suitable suspending or solubilizing agent.
  • suitable suspending agents include celluloses, carboxymethyl cellulose and its salts, guar gum and the like.
  • Suitable solubilizing agents include sucrose solutions, ethanol, and surfactants such as polyoxyethylene derivatives of fatty acid partial esters of sorbitol anhydrides (e.g., Polysorbate 80).
  • Suspension systems, suspension and solubilizing agents, and methods for their use are described in M. Pernarowski, "Solutions, Emulsions and Suspensions” Remington's Pharmaceutical Sciences (A. Osol, editor, 15th Edition, 1975), which is incorporated herein by reference.
  • the total water content will generally range from about 20% to about 75%, and preferably from about 20% to about 40%, by weight of the composition.
  • typical oral formulations also contain a co-solvent including but not limited to alcohol, propylene glycol, glycerin, sorbitol solution, and the like, to assist solubilization and incorporation of water-insoluble ingredients, flavoring oils and the like into the composition.
  • a co-solvent including but not limited to alcohol, propylene glycol, glycerin, sorbitol solution, and the like, to assist solubilization and incorporation of water-insoluble ingredients, flavoring oils and the like into the composition.
  • the compositions preferably contain from about 5 to about 25 volume/volume percent of the co-solvent, most preferably from about 10 to about 20 volume/volume percent of the co-solvent.
  • Carriers suitable for nasal administration provide a product which is delivered to the nasal passages.
  • Such carriers may be for example, aqueous or aerosol and are more fully described in Remington's Pharmaceutical Sciences (17th Edition, 1985), which is incorporated herein by reference.
  • product forms include (but are not limited to) nasal solutions for use as drops or as sprays, nasal suspensions, nasal ointments, nasal gels, or other vehicles suitable for nasal administration.
  • Preferred nasal dosage forms are solutions, suspensions, and gels, which normally contain sodium chloride in a major amount of water (preferably purified water).
  • Other ingredients including but not limited to: pH adjusters such as sodium hydroxide; emulsifiers or dispersing agents; buffering agents such as sodium bicarbonate; preservatives such as benzyl alcohol, parabens, benzalkonium chloride, chlorhexidine gluconate and disodium EDTA; agents for regulating isotonicity such as sodium chloride, boric acid, potassium phosphate and propylene glycol; wetting agents; thickening agents such as methylcellulose, zanthan gum, carboxymethyl cellulose, and carbomer; humectants such as sorbitol, propylene glycol, sorbitol, and glycerol; surfactants such as polyoxyethylene derivatives of fatty acid partial esters of sorbitol anhydrides; and mixtures thereof, may also be present.
  • the present composition may also be in a solid oral dosage form.
  • Tablets can be compressed, triturated, freeze dried, sugar-coated, film-coated or multiple compressed.
  • the tablets may contain suitable binders, lubricants, diluents, disintegrating agents, coloring agents, flavoring agents, preservatives and flow- inducing agents.
  • carrier materials suitable for the preparation of unit dosage forms for oral administration are well-known in the art. Their selection will depend on secondary considerations like taste, cost, and shelf stability, which are not critical for the purposes of the present invention, and can be made without difficulty by a person skilled in the art.
  • lozenges and chewing gums include lozenges and chewing gums.
  • Lozenge compositions comprise a lozenge carrier (i.e. a candy base).
  • Candy bases are disclosed in U. S. Patent 4,472,373, Ryan, issued September 18, 1984, and in U.S. Patent 4,083,955, Grabenstetter et al., issued April 11, 1978.
  • Chewing gum compositions comprise a chewing gum carrier such as those which are disclosed in these same patents, both of which are incorporated herein by reference.
  • Chewing gum carriers may comprise, for example, a gum base, flavoring agents, and sweetening agents.
  • Other Carriers may comprise, for example, a gum base, flavoring agents, and sweetening agents.
  • compositions may be formulated with a wide variety of carrier materials in addition to those already disclosed.
  • substances which can serve as carrier materials are sugars such as lactose, glucose, and sucrose; starches such as comstarch and potato starch; cellulose and its derivatives such as sodium carboxymethylcellulose, ethylcellulose, cellulose acetate; powdered tragacanth; malt; gelatin; talc; stearic acid; magnesium stearate; dicalcium phosphate; calcium sulfate; mineral oil and vegetable oils such as peanut oil, cottonseed oil, sesame oil, olive oil, corn oil, and oil of theobroma; silicones such as siloxanes, silicon oils, fluids, gums and greases, and 1 or 2 part Room Temperature Vulcanizable; polyols such as propylene glycol, glycerin, sorbitol, mannitol, polyethylene oxide, and polyethylene glycol; agar; karaya gum; al
  • Coolant materials may also be included as carrier materials in the invention compositions.
  • Preferred coolants in the present compositions are the paramenthane carboxyamide agents such as N-ethyl-p-menthane-3-carboxamide, (known commercially as “WS-3"), and 3-l-menthoxypropane-l,2-diol (known commercially as "TK-10"), and mixtures thereof. These coolants are described in PCT Patent Application Publication WO 92-17164, to Upson et al., published October 15, 1992. TK-10 is also described in U.S. Patent 4,459,425 to Amano et al., issued July 10, 1984; and WS-3 and other parmenthane carboxyamides agents are described in U.S.
  • Suitable binders include starch, gelatin, natural sugars, corn sweeteners, natural and synthetic gums such as acacia sodium alginate, carboxymethylcellulose, microcrystalline cellulose, polyethylene glycol and waxes.
  • Lubricants may include, for example, starch, methylcellulose, agar, bentonite, guar gum, etc.
  • Wetting agents such as sodium lauryl sulfate, as well as coloring agents, flavoring agents, sweetening agents, excipients, tableting agents, stabilizers, antioxidants, and preservatives can also be present. Active:
  • compositions may also contain a safe and effective amount of one or more actives.
  • actives that are useful in these compositions include (but are not limited to) antimicrobial agents such as iodine, sulfonamides, mercurials, bisbiguanides, or phenolics; antibiotics such as tetracycline, neomycin, kanamycin, metronidazole, or clindamycin; anti-inflammatory agents such as aspirin, acetaminophen, naproxen, ibuprofen, flurbiprofen, indomethacin, eugenol, or hydrocortisone; immune-suppressive or stimulatory agents such as methotrexate or levamasole; dentinal desensitizing agents such as potassium nitrate, strontium chloride or sodium fluoride; odor masking agents such as peppermint oil or chlorophyll; immune reagents such as immunoglobulins or soluble antigens;
  • an antimicrobial and an anti-inflammatory agent may be combined in a single delivery system to provide combined effectiveness.
  • Preferred actives are nutritional, therapeutic, medicinal, pharmaceutical, and those commonly used in health care products.
  • compositions which comprise one or more actives are dental care preparations such as dentifrices and oral rinses, and cough/cold preparations in liquid oral dosage forms.
  • Actives commonly utilized in cough/cold preparations include but are not limited to decongestants such as pseudoephedrine hydrochloride, phenylpropanolamine hydrochloride, and ephedrine hydrochloride; antitussives such as dextromethorphan, chlophedianol, carbetapentane, noscapine, codeine, hydrocodone, hydromorphone; analgesics such as acetaminophen and ibuprofen; expectorants or mucolytics such as glyceryl guaiacolate, guaiacolate, terpin hydrate, ammonium chloride, N-acetylcysteine and ambroxol; antihistamines such as chlo ⁇ heniramine maleate,
  • Oral forms of cough/cold preparations comprise a safe and effective amount of one or more active components.
  • Solid oral dosage forms preferably contain from about 5% to about 95%, more preferably from about 10% to about 95%, and most preferably from about 25% to about 95%, of the active components.
  • Liquid oral dosage forms preferably contain from about 1% to about 50%, more preferably from about 1% to about 25%, and most preferably from about 3% to about 10%, of the active components.
  • Dental care preparations typically comprise a soluble fluoride ion source as one of the actives. The soluble fluoride ion source is used in an amount sufficient to provide from about 10 to about 5000 ppm of the fluoride ion.
  • Preferred fluorides are sodium fluoride, stannous fluoride, inidium fluoride, and sodium monofluorophosphate.
  • Various polymers and mixtures thereof are also useful in dental care preparations. These polymers may be synthetic anionic polymeric polycarboxylates and their complexes and/or carboxyvinyl polymers. Polymers useful in the present compositions are disclosed in U.S.
  • Pyrophosphate salts are pharmaceutical actives that may also be included in dental care preparations. Any of the alkali metal pyrophosphate salts may be used in either their hydrated or unhydrated forms. Specific salts include tetra alkali metal pyrophosphate, dialkali metal diacid pyrophosphate, trialkali metal monoacid pyrophospate and mixtures thereof, wherein the alkali metals are preferably sodium or potassium. Pyrophosphate salts are described in more detail in Kirk & Othmer, Encyclopedia of Chemical Technology, Second Edition, Volume 15, Interscience Publishers (1968), incorporated herein by reference in its entirety.
  • the amount of pyrophosphate salt useful is any effective amount and is generally enough to provide at least 1.0% P2 ⁇ y4 preferably from about 1.5% to about 6%, and more preferably from about 0.5% to about 6%, to the compositions. It is to be appreciated that the level of P2 ⁇ 7" is that capable of being provided to the composition (i.e., the theoretical amount at an appropriate pH) and that other pyrophosphate forms (e.g., HP2O7"- ) may be present when a final product is established.
  • Anti-plaque and anti-gingivitis pharmaceutical actives may also be included in the dental preparations. These actives include quaternary ammonium compounds or bis-biguanides such as chlorhexidine and stannous ion in the form of a combination of stannous fluoride and stannous gluconate. Oral compositions comprising stannous ion are described fully in U.S. Patent 5,004,597 to Majeti et al., issued April 2, 1991, inco ⁇ orated herein by reference in its entirety. Disinfectant agents like triclosan and antiseptic agents like thymol may also be included in the dental preparations.
  • compositions for relieving gastrointestinal distress may include antacid agents, acid secretion prevention agents, other pharmaceutical actives and mixtures thereof.
  • Antacid agents include aluminum carbonate, aluminum hydroxide, aluminum phosphate, aluminum hydroxy-carbonate, dihydroxy aluminum sodium carbonate, aluminum magnesium glycinate, dihydroxy aluminum amino acetate, dihydroxy aluminum aminoacetic acid, calcium carbonate, calcium phosphate, aluminum magnesium hydrated sulfates, magnesium aluminate, magnesium alumino silicates, magnesium carbonate, magnesium glycinate, magnesium hydroxide, magnesium oxide, magnesium trisilicate, sucralfate, sodium bicarbonate, and mixtures thereof.
  • Acid secretion prevention agents include cimetidine, ranitidine, famotidine, omeprazole, and mixtures thereof.
  • compositions include antiflatulent agents such as simethicone and bismuth-containing agents such as, bismuth subsalicylate, bismuth aluminate, bismuth citrate, bismuth subcitrate, bismuth nitrate, bismuth subcarbonate, bismuth subgalate, and mixtures thereof.
  • the pharmaceutical actives comprise from about 1% to about 99%, and preferably from about 25% to about 60% by weight of the composition.
  • the one or more actives are used in the present compositions at levels of from about 0.001% to about 99%, and preferably from about 0.01% to about 90%, by weight of the compositions.
  • a toothpaste composition according to the present invention is prepared having the following components:
  • Example II Oral Mouth Rinse Composition An oral mouth rinse composition according to the present invention is prepared having the following components:
  • a liquid oral dosage form composition according to the present invention is prepared having the following components:
  • Add flavor. Mix together sucrose solution with propylene glycol solution. Mix together this solution and potassium sorbate solution. Lastly, add flavor solution. Adjust water level for proper batch size. Adjust pH to about 6.5-8.5. Mix for 30-35 minutes.
  • a chewable tablet composition according to the present invention is prepared having the following components:

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  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne des compositions se présentant sous une forme appropriée pour être administrées oralement ou localement, et qui comprennent un ou plusieurs dérivés du phosphate, des matériaux-supports et de préférence une quantité sûre et efficace d'un ou plusieurs matériaux actifs.
PCT/US1994/010044 1993-09-17 1994-09-07 Compositions contenant des derives du phosphate WO1995007683A1 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
BR9407550A BR9407550A (pt) 1993-09-17 1994-09-07 Composiçao contendo derivados de fosfato
EP94927360A EP0719128A1 (fr) 1993-09-17 1994-09-07 Compositions contenant des derives du phosphate
AU76832/94A AU7683294A (en) 1993-09-17 1994-09-07 Composition containing phosphate derivatives
JP7509236A JPH09502718A (ja) 1993-09-17 1994-09-07 リン酸誘導体を含有した組成物

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US12348493A 1993-09-17 1993-09-17
US08/123,484 1993-09-17

Publications (1)

Publication Number Publication Date
WO1995007683A1 true WO1995007683A1 (fr) 1995-03-23

Family

ID=22408932

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1994/010044 WO1995007683A1 (fr) 1993-09-17 1994-09-07 Compositions contenant des derives du phosphate

Country Status (7)

Country Link
EP (1) EP0719128A1 (fr)
JP (1) JPH09502718A (fr)
CN (1) CN1130863A (fr)
AU (1) AU7683294A (fr)
BR (1) BR9407550A (fr)
CA (1) CA2170489A1 (fr)
WO (1) WO1995007683A1 (fr)

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996015768A1 (fr) * 1994-11-18 1996-05-30 The Procter & Gamble Company Composes a usage oral
US6042812A (en) * 1996-11-26 2000-03-28 The Procter & Gamble Company Flavor systems for oral care products
WO2001039606A1 (fr) * 1999-11-12 2001-06-07 The Procter & Gamble Company Compositions de gomme a macher
WO2001056399A1 (fr) * 2000-02-04 2001-08-09 The Procter & Gamble Company Compositions de chewing-gum
EP1378503A1 (fr) * 2002-07-01 2004-01-07 Symrise GmbH & Co. KG Lactate de menthyle compacte
US6916463B2 (en) 2002-09-24 2005-07-12 The Procter & Gamble Company Oral products having an aesthetic layer
US6926916B1 (en) * 1999-11-12 2005-08-09 The Procter & Gamble Company Chewing gum compositions
WO2006020686A1 (fr) * 2004-08-11 2006-02-23 Cadbury Adams Usa Llc Compositions de rechauffement et systemes de liberation associes
SG127675A1 (en) * 2000-12-12 2006-12-29 Takasago Perfumery Co Ltd Warming composition
JP2008001726A (ja) * 1997-04-16 2008-01-10 Cima Labs Inc 迅速溶解性の頑丈な投与形態物
US7588793B1 (en) 1998-06-05 2009-09-15 Cadbury Adams Usa, Llc Enhanced flavoring compositions containing N-ethyl-p-menthane-3-carboxamide and method of making and using same
US8846007B2 (en) 2005-12-23 2014-09-30 Intercontinental Great Brands Llc Compositions providing a heating sensation for oral or dermal delivery
EP2346475B1 (fr) 2008-11-20 2017-03-15 The Procter & Gamble Company Compositions pour soin personnel fournissant une sensation de refroidissement améliorée

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005314254A (ja) * 2004-04-28 2005-11-10 Pola Chem Ind Inc 医薬部外品に好適な皮膚外用剤
US20120045401A1 (en) * 2009-05-18 2012-02-23 Colgate-Palmolive Company Oral composition

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BE678243A (fr) * 1965-03-24 1966-09-01
LU68497A1 (fr) * 1972-09-27 1973-12-07
DE2330384A1 (de) * 1973-06-14 1975-01-09 Michael Dr Babor Kosmetische praeparate
EP0387024A1 (fr) * 1989-03-09 1990-09-12 The Procter & Gamble Company Compositions antitartres
EP0512599A2 (fr) * 1991-05-09 1992-11-11 Unilever N.V. Contrôle du dépôt de tartre à l'aide de composés polyhydroxy phosphorylés
US5244651A (en) * 1991-09-04 1993-09-14 Kao Corporation Method of desensitizing hypersensitive dentin
JPH0631559A (ja) * 1992-07-21 1994-02-08 Toyota Motor Corp ねじ締め制御装置

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BE678243A (fr) * 1965-03-24 1966-09-01
LU68497A1 (fr) * 1972-09-27 1973-12-07
DE2330384A1 (de) * 1973-06-14 1975-01-09 Michael Dr Babor Kosmetische praeparate
EP0387024A1 (fr) * 1989-03-09 1990-09-12 The Procter & Gamble Company Compositions antitartres
EP0512599A2 (fr) * 1991-05-09 1992-11-11 Unilever N.V. Contrôle du dépôt de tartre à l'aide de composés polyhydroxy phosphorylés
US5244651A (en) * 1991-09-04 1993-09-14 Kao Corporation Method of desensitizing hypersensitive dentin
JPH0631559A (ja) * 1992-07-21 1994-02-08 Toyota Motor Corp ねじ締め制御装置

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Week 7136, Derwent World Patents Index; AN 71-58875S *

Cited By (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5628986A (en) * 1994-11-18 1997-05-13 The Procter & Gamble Company Oral compositions
WO1996015768A1 (fr) * 1994-11-18 1996-05-30 The Procter & Gamble Company Composes a usage oral
US6042812A (en) * 1996-11-26 2000-03-28 The Procter & Gamble Company Flavor systems for oral care products
JP2012162558A (ja) * 1997-04-16 2012-08-30 Cima Labs Inc 迅速溶解性の頑丈な投与形態物
JP2008001726A (ja) * 1997-04-16 2008-01-10 Cima Labs Inc 迅速溶解性の頑丈な投与形態物
US7588793B1 (en) 1998-06-05 2009-09-15 Cadbury Adams Usa, Llc Enhanced flavoring compositions containing N-ethyl-p-menthane-3-carboxamide and method of making and using same
WO2001039606A1 (fr) * 1999-11-12 2001-06-07 The Procter & Gamble Company Compositions de gomme a macher
US6926916B1 (en) * 1999-11-12 2005-08-09 The Procter & Gamble Company Chewing gum compositions
WO2001056399A1 (fr) * 2000-02-04 2001-08-09 The Procter & Gamble Company Compositions de chewing-gum
SG127675A1 (en) * 2000-12-12 2006-12-29 Takasago Perfumery Co Ltd Warming composition
EP1378503A1 (fr) * 2002-07-01 2004-01-07 Symrise GmbH & Co. KG Lactate de menthyle compacte
US6916463B2 (en) 2002-09-24 2005-07-12 The Procter & Gamble Company Oral products having an aesthetic layer
WO2006020754A1 (fr) * 2004-08-11 2006-02-23 Cadbury Adams Usa Llc Compositions d'agent sensoriel et systemes de delivrance pour celles-ci
AU2005272922B2 (en) * 2004-08-11 2009-07-09 Intercontinental Great Brands Llc Warming compositions and delivery systems therefor
WO2006020686A1 (fr) * 2004-08-11 2006-02-23 Cadbury Adams Usa Llc Compositions de rechauffement et systemes de liberation associes
AU2009222555B2 (en) * 2004-08-11 2010-11-11 Intercontinental Great Brands Llc Warming compositions and delivery systems therefor
US8097271B2 (en) 2004-08-11 2012-01-17 Kraft Foods Global Brands Llc Warming compositions and delivery systems therefor
US8101208B2 (en) 2004-08-11 2012-01-24 Kraft Foods Global Brands Llc Sensate compositions and delivery systems therefor
US8846007B2 (en) 2005-12-23 2014-09-30 Intercontinental Great Brands Llc Compositions providing a heating sensation for oral or dermal delivery
EP2346475B1 (fr) 2008-11-20 2017-03-15 The Procter & Gamble Company Compositions pour soin personnel fournissant une sensation de refroidissement améliorée

Also Published As

Publication number Publication date
CN1130863A (zh) 1996-09-11
BR9407550A (pt) 1996-12-31
EP0719128A1 (fr) 1996-07-03
JPH09502718A (ja) 1997-03-18
AU7683294A (en) 1995-04-03
CA2170489A1 (fr) 1995-03-23

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