WO2002022096A2 - Compositions destinées à être administrées par voie orale - Google Patents

Compositions destinées à être administrées par voie orale Download PDF

Info

Publication number
WO2002022096A2
WO2002022096A2 PCT/US2001/028059 US0128059W WO0222096A2 WO 2002022096 A2 WO2002022096 A2 WO 2002022096A2 US 0128059 W US0128059 W US 0128059W WO 0222096 A2 WO0222096 A2 WO 0222096A2
Authority
WO
WIPO (PCT)
Prior art keywords
polyol
carboxylic acid
oral
composition according
composition
Prior art date
Application number
PCT/US2001/028059
Other languages
English (en)
Other versions
WO2002022096A3 (fr
Inventor
Vincent Bercovici
Robert Francis Date
Kieran John Michael Madigan
Christopher David White
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 AU2001290669A priority Critical patent/AU2001290669A1/en
Publication of WO2002022096A2 publication Critical patent/WO2002022096A2/fr
Publication of WO2002022096A3 publication Critical patent/WO2002022096A3/fr

Links

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
    • 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
    • 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
    • A23G4/066—Chewing gum characterised by the composition containing organic or inorganic compounds characterised by the fat used
    • 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
    • A61K8/37—Esters of carboxylic acids
    • A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
    • 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 oral compositions, such as toothpastes and mouthwashes, which provide the function of moisturising or lubricating the oral cavity or otherwise alleviating the symptoms of 'dry mouth'. More particularly the invention relates to oral compositions comprising a polyol ester moisturising agent.
  • An undesirably dry oral mucosa (commonly known as 'dry mouth') is a frequent problem for adults, especially older adults.
  • the mucosa may dry as a result of long or short term physiological changes, such as hormonal changes or stress.
  • Environmental factors such as the weather or room conditions can also play a part, as can drugs used to treat other conditions.
  • Dry mouth can manifest itself as an uncomfortable sensation, a problem with speaking, swallowing or chewing. Further, dry oral mucosae may show a greater propensity to infection.
  • Commercial products for alleviating dry mouth are known. For example, Salutem® toothpaste, sold in Finland is specifically addressed to that purpose. It employs betaine (trimethylglycine) as a moisturiser. This use is disclosed in PCT patent application WO 98/29090.
  • the present invention relates to dentifrice compositions comprising: a) from about 0.1% to about 15% of a polyol carboxylic acid ester having a polyol moiety and at least 4 carboxylic acid moieties, wherein the polyol moiety is selected from sugars and sugar alcohols containing from about 4 to about 8 hydroxyl groups, and wherein each carboxylic acid moiety has from about 8 to about 22 carbon atoms; b) from about 0.01% to about 80% of an oral cavity benefit agent selected from surfactants, dental abrasives, fluoride ion sources and anticalculus agents; or mixtures thereof; and c) from about 0.1% to about 99.8% of an orally-acceptable carrier.
  • a polyol carboxylic acid ester having a polyol moiety and at least 4 carboxylic acid moieties, wherein the polyol moiety is selected from sugars and sugar alcohols containing from about 4 to about 8 hydroxyl groups, and wherein each carboxylic acid moiety
  • the present invention further relates to a method for moisturising the oral cavity comprising the application of a safe and effective amount of a composition to the oral mucosa.
  • the invention relates to a chewing gum comprising: a) from about 0.1% to about 15% of a polyol carboxylic acid ester having a polyol moiety and at least 4 carboxylic acid moieties, wherein the polyol moiety is selected from sugars and sugar alcohols containing from about 4 to about 8 hydroxyl groups, and wherein each carboxylic acid moiety has from about 8 to about 22 carbon atoms; b) an elastomeric chewing gum base.
  • a "safe and effective amount,” as used herein, means a sufficient amount to provide a measurable benefit in moisturisation without causing undue irritation.
  • the term "orally-acceptable carrier,” as used herein, means a suitable vehicle which can be used to apply the present compositions to the oral cavity in a safe and effective manner.
  • the compositions of the invention are preferably in the form of a toothpaste, mouthwash, liquid dentifrice, chewing gum, or oral gel, and the carrier is suitable for the chosen product form.
  • the pH of the present compositions generally range from about 3 to about 9, preferably from about 6 to about 8.
  • the essential as well as optional components of the compositions of the present invention are described in the following paragraphs.
  • compositions of the present invention comprise from about 0.1% to about 15%, preferably from about 0.5% to about 10%, and more preferably from about 1% to about 8% by weight of a polyol carboxylic acid ester having a polyol moiety and at least 4 carboxylic acid moieties.
  • polyol esters are derived from a polyol radical or moiety and one or more carboxylic acid radicals or moieties. They can also be described as polyol fatty acid esters, because the terms carboxylic acid and fatty acid are often used interchangeably by those skilled in the art.
  • a mixture of chemically distinct polyol esters may also be used and a general reference to 'polyol esters' herein is to be taken to include such mixtures provided each component conforms to the general definition, unless otherwise apparent from the context.
  • the polyol esters herein have low melting points and are mobile at typical oral cavity temperatures.
  • the polyol esters preferred for use herein have complete melting points below about 30°C, preferably below about 27.5°C, more preferably below about 25°C. Complete melting points reported herein are measured by Differential Scanning Calorimetry (DSC).
  • the preferred polyol polyesters employed in this invention comprise sugars or sugar alcohols as the polyol moiety. Accordingly, the polyol starting material must have at least four esterifiable hydroxyl groups.
  • preferred polyols are sugars, including monosaccharides and disaccharides, and sugar alcohols. Examples of monosaccharides containing four hydroxyl groups are xylose and arabinose and the sugar alcohol derived from xylose, which has five hydroxyl groups, i.e., xylitol.
  • the monosaccharide, erythrose is not suitable in the practice of this invention since it only contains three hydroxyl groups, but the sugar alcohol derived from erythrose, i.e., erythritol, contains four hydroxyl groups and accordingly can be used. Suitable five hydroxyl group- containing monosaccharides are galactose, fructose, and sorbose. Sugar alcohols containing six hydroxyl groups derived from the hydrolysis products of sucrose, as well as glucose and sorbose, e.g., sorbitol, are also suitable. Examples of disaccharide polyols which can be used include maltose, lactose, and sucrose, all of which contain eight hydroxyl groups. Preferred polyols for preparing the polyesters for use in the present invention are selected from the group consisting of erythritol, xylitol, sorbitol, glucose, and sucrose. Sucrose is especially preferred.
  • the polyol starting material having at least four hydroxyl groups is esterified on at least four of the -OH groups with a fatty acid containing from about 8 to about 22 carbon atoms.
  • fatty acids include caprylic, capric, lauric, myristic, myristoleic, palmitic, palmitoleic, stearic, oleic, ricinoleic, linoleic, linolenic, eleostearic, arachidic, arachidonic, behenic, and erucic acid.
  • the fatty acids can be derived from naturally occurring or synthetic fatty acids; they can be saturated or unsaturated, including positional and geometrical isomers. However, in order to provide the low melting polyesters preferred for use herein, at least about 50% by weight of the fatty acid incorporated into the polyester molecule should be unsaturated. Oleic and linoleic acids, and mixtures thereof, are especially preferred.
  • the polyol fatty acid polyesters useful in this invention should contain at least four fatty acid ester groups. It is not necessary that all of the hydroxyl groups of the polyol be esterified with fatty acid, but it is preferable that the polyester contain no more than two unesterified hydroxyl groups. Most preferably, substantially all of the hydroxyl groups of the polyol are esterified with fatty acid, i.e., the polyol moiety is substantially completely esterified.
  • the fatty acids esterified to the polyol molecule can be the same or mixed, but as noted above, a substantial amount of the unsaturated acid ester groups must be present to provide liquidity.
  • sucrose fatty triester would not be suitable for use herein because it does not contain the required four fatty acid ester groups.
  • a sucrose tetra-fatty acid ester would be suitable, but is not preferred because it has more than two unesterified hydroxyl groups.
  • a sucrose hexa-fatty acid ester would be preferred because it has no more than two unesterified hydroxyl groups.
  • Highly preferred compounds in which all the hydroxyl groups are esterified with fatty acids include the liquid sucrose octa- substituted fatty acid esters.
  • glucose tetraoleate the glucose tetraesters of soybean oil fatty acids (unsaturated), the mannose tetraesters of mixed soybean oil fatty acids, the galactose tetraesters of oleic acid, the arabinose tetraesters of linoleic acid, xylose tetralinoleate, galactose pentaoleate, sorbitol tetraoleate, the sorbitol hexaesters of unsaturated soybean oil fatty acids, xylitol pentaoleate, sucrose tetraoleate, sucrose pentaoletate, sucrose hexaoleate, sucrose hepatoleate, sucrose octaoleate, and mixtures thereof.
  • highly preferred polyol fatty acid esters are those wherein the fatty acids contain from about 14 to about 18 carbon atoms.
  • the polyol fatty acid polyesters suitable for use herein can be prepared by a variety of methods well known to those skilled in the art. These methods include: transesterification of the polyol with methyl, ethyl or glycerol fatty acid esters using a variety of catalysts; acylation of the polyol with a fatty acid chloride; acylation of the polyol with a fatty acid anhydride; and acylation of the polyol with a fatty acid, per se. See U.S. Patent No. 2,831,854; U.S. Patent No. 4,005,196, to Jandacek, issued January 25, 1977; U.S. Patent No. 4,005,196, to Jandacek, issued January 25, 1977. Oral cavity benefit agents
  • compositions of the invention further from about 0.01% to about 80% of an oral cavity benefit agent selected from surfactants, dental abrasives, fluoride ion sources and anticalculus agents; or mixtures thereof.
  • an oral cavity benefit agent selected from surfactants, dental abrasives, fluoride ion sources and anticalculus agents; or mixtures thereof.
  • a preferred oral cavity benefit agent for use herein is a surfactant.
  • the surfactant stabilises the polyol ester within the formulation and can assist in oral cleaning.
  • Surfactants are particularly preferred in a toothpaste and mouthwash compositions according to the invention. Suitable surfactant levels are from about 0.1% to about 15%, preferably from about 0.5 to about 10%, more preferably from about 1 to about 5%.
  • Preferred anionic surfactants useful herein include the water-soluble salts of alkyl sulphates and alkyl ether sulphates having from 10 to 18 carbon atoms in the alkyl radical and the water-soluble salts of sulphonated monoglycerides of fatty acids having from 10 to 18 carbon atoms.
  • Sodium lauryl sulphate and sodium coconut monoglyceride sulphonates are examples of anionic surfactants of this type. Mixtures of anionic surfactants can also be utilised.
  • alkali metal or ammonium salts of sarcosinates include alkali metal or ammonium salts of sarcosinates, isethionates and taurates.
  • Preferred herein are the sodium and potassium salts of the following: lauroyl sarcosinate, myristoyl sarcosinate, palmitoyl sarcosinate, stearoyl sarcosinate and oleoyl sarcosinate.
  • surfactants which can optionally be used in combination with the surfactants above include those mentioned in US-A-3,959,458; US-A-3,937,807; and US-A-4,051,234.
  • the surfactant is preferably present in the compositions of the present invention at a level of from about 0.1% to about 2.5%, preferably from about 0.3% to about 2.5% and most preferably from about 0.5% to about 2.0% by weight of the total composition.
  • Preferred cationic surfactants useful in the present invention can be broadly defined as derivatives of aliphatic quaternary ammonium compounds having one long alkyl chain containing from about 8 to 18 carbon atoms such as lauryl trimethylammonium chloride; cetyl pyridinium chloride; benzalkonium chloride; cetyl trimethylammonium bromide; di- isobutylphenoxyethyl-dimethylbenzylammonium chloride; coconut alkyltrimethyl- ammonium nitrite; cetyl pyridinium fluoride; etc.
  • Preferred compounds are the quaternary ammonium fluorides described in US-A-3,535,421, where said quaternary ammonium fluorides have detergent properties.
  • Certain cationic surfactants can also act as germicides in the compositions disclosed herein.
  • Some cationic agents such as chlorhexidine, although suitable for use in the current invention, are not preferred due to their capacity to stain the oral cavity's hard tissues. Persons skilled in the art are aware of this possibility and should incorporate cationics only with this limitation in mind.
  • Nonionic surfactants that can be used in the compositions of the present invention can be broadly defined as compounds produced by the condensation of alkylene oxide groups (hydrophilic in nature) with an organic hydrophobic compound which may be aliphatic and/or aromatic in nature.
  • suitable nonionic surfactants include the Pluronics, polyethylene oxide condensates of alkyl phenols, products derived from the condensation of ethylene oxide with the reaction product of propylene oxide and ethylene diamine, ethylene oxide condensates of aliphatic alcohols, long chain tertiary amine oxides, long chain tertiary phosphine oxides, long chain dialkyl sulphoxides and mixtures of such materials .
  • Preferred zwitterionic synthetic surfactants useful in the present invention can be broadly described as derivatives of aliphatic quaternary ammonium, phosphonium, and sulphonium compounds, in which the aliphatic radicals can be straight chain or branched, and wherein one of the aliphatic substituents contains from about 8 to 18 carbon atoms and one contains an anionic water-solubilising group, e.g., carboxy, sulphonate, sulphate, phosphate or phosphonate.
  • Preferred betaine surfactants are disclosed in US-A-5, 180,577.
  • Typical alkyl dimethyl betaines include decyl betaine or 2-(N-decyl-N,N-dimethylammonio) acetate, coco betaine, myristyl betaine, palmityl betaine, lauryl betaine, cetyl betaine, cetyl betaine, stearyl betaine, etc.
  • the amidobetaines are exemplified by cocoamidoethyl betaine, cocoamidopropyl betaine, lauramidopropyl betaine and the like.
  • the betaines of choice are preferably the cocoamidopropyl betaine and, more preferably, the lauramido propyl betaine.
  • a further preferred oral cavity benefit agent for use herein is a dental abrasive.
  • Abrasives are particularly preferred in a toothpaste and chewing gum compositions according to the invention and serve to polish the teeth and /or remove surface deposits.
  • the abrasive polishing material contemplated for use herein can be any material which does not excessively abrade dentine.
  • Suitable abrasives include insoluble phosphate polishing agents, include various calcium phosphates such as, for example, dicalcium phosphate, tricalcium phosphate, calcium pyrophosphate, beta-phase calcium pyrophosphate, dicalcium phosphate dihydrate, anhydrous calcium phosphate, insoluble sodium metaphosphate, and the like.
  • chalk-type abrasives such as calcium and magnesium carbonates, silicas including xerogels, hydrogels, aerogels and precipitates, alumina and hydrates thereof such as alpha alumina trihydrate, aluminosilicates such as calcined aluminium silicate and aluminium silicate, magnesium and zirconium silicates such as magnesium trisilicate and thermosetting polymerised resins such as particulate condensation products of urea and formaldehyde, polymethylmethacrylate, powdered polyethylene and others such as disclosed in US-A-3 ,070,510, December 25, 1962. Mixtures of abrasives can also be used.
  • the abrasive polishing materials generally have an average particle size of from about 0.1 to about 30 microns, preferably from about 5 to 15 microns.
  • Silica dental abrasives of various types offer exceptional dental cleaning and polishing performance without unduly abrading tooth enamel or dentin.
  • the silica abrasive can be precipitated silica or silica gels such as the silica xerogels described in Pader et al., US-A- 3,538,230, issued March 2, 1970 and DiGiulio, US-A-3,862,307, June 21, 1975, for example silica xerogels marketed under the tradename "Syloid" by W. R. Grace & Company, Davison Chemical Division.
  • Suitable precipitated silica materials include those marketed by the J. M.
  • Zerodent® particularly the silicas carrying the designation Zeodent® 119 or Zeodent® 118.
  • These silica abrasives are described in US-A-4,340,583, July 29, 1982 and WO 96/09809, incorporated herein by reference.
  • Suitable abrasive levels are from about 1% to about 60%, preferably from about 5% to about 35%.
  • a further preferred oral cavity benefit agent is a fluoride ion . It is common to have a compound capable of providing fluoride ions in dentifrice and other oral compositions in an amount sufficient to give a fluoride ion concentration of from about 0.0025% to about 5.0% by weight, preferably from about 0.005% to about 2.0% by weight, to provide additional anticaries effectiveness.
  • fluoride ion-yielding materials can be employed as sources of soluble fluoride in the present compositions.
  • Representative fluoride ion sources include: stannous fluoride, sodium fluoride, potassium fluoride, calcium monofluorophosphate, sodium monofluorophosphate and many others. Sodium fluoride is particularly preferred herein.
  • chelating agent is selected from tartaric acid and pharmaceutically-acceptable salts thereof, citric acid and alkali metal citrates and mixtures thereof. Chelating agents are able to complex calcium found in the cell walls of the bacteria. Chelating agents can also disrupt plaque by removing calcium from the calcium bridges which help hold this biomass intact. However, it is possible to use a chelating agent which has an affinity for calcium that is too high. This results in tooth demineraUsation and is contrary to the objects and intentions of the present invention.
  • Sodium and potassium citrate are the preferred alkali metal citrates, with sodium citrate being the most preferred. Also preferred is a citric acid/alkali metal citrate combination.
  • Preferred herein are alkali metal salts of tartaric acid. Most preferred for use herein are disodium tartrate, dipotassium tartrate, sodium potassium tartrate, sodium hydrogen tartrate and potassium hydrogen tartrate.
  • the amounts of chelating agent suitable for use in the present invention are about 0.1% to about 2.5%, preferably from about 0.5% to about 2.5% and more preferably from about 1.0% to about 2.5%.
  • the tartaric acid salt chelating agent can be used alone or in combination with other optional chelating agents. Other optional chelating agents can be used. Preferably these chelating agents have a calcium binding constant of about 101 to 10 ⁇ provide improved cleaning with reduced plaque and calculus formation.
  • chelating agents are the soluble polyphosphates, polyphosphonates, and pyrophosphates which are useful as anticalculus agents.
  • the pyrophosphate salts used in the present compositions can be any of the alkali metal pyrophosphate salts. Specific salts include tetra alkali metal pyrophosphate, dialkali metal diacid pyrophosphate, trialkali metal monoacid pyrophosphate and mixtures thereof, wherein the alkali metals are preferably sodium or potassium.
  • the salts are useful in both their hydrated and unhydrated forms.
  • An effective amount of pyrophosphate salt useful in the present composition is generally enough to provide at least 1.0% pyrophosphate ion, preferably from about 1.5% to about 6%, more preferably from about 3.5% to about 6% of such ions. It is to be appreciated that the level of pyrophosphate ions is that capable of being provided to the composition (i.e., the theoretical amount at an appropriate pH) and that pyrophosphate forms other than P2 ⁇ 7"4 (e.g., (HT ⁇ O - ⁇ )) may be present when a final product pH is established.
  • the pyrophosphate salts are described in more detail in Kirk & Oth er, Encyclopedia of Chemical Technology, Second Edition, Volume 15, Interscience Publishers (1968).
  • soluble polyphosphates such as sodium tripolyphosphate and sodium hexametaphosphate.
  • Long chain anticalculus agents of this type are described in WO 98/22079, incorporated herein by reference.
  • phytic acid compounds are also useful.
  • the hexakis phosphate ester of myo-inositol is known as phytic acid.
  • phytic acid compound means the hexakis phosphate ester of myo-inositol and the lesser substituted trikis, tetrakis and pentakis phosphate esters of myo-inositol and any physiologically acceptable derivatives and salts thereof, such as alkali metal, alkaline-earth metal, ammonium salts or mixtures thereof.
  • These phytic acid compounds may be used singly or in combination.
  • the phytic acid compounds which can be used in the present invention include phytic acid and metal salts of phytic acid in which all or some of the hydrogen atoms in the phosphate groups at the ⁇ 1- to 6-positions of phytic acid are replaced by metal substituents, for example, alkali metal salts of phytic acid such as sodium phytate, potassium phytate and lithium phytate, ammonium phytate, divalent metal salts of phytic acid such as magnesium phytate, zinc phytate and calcium phytate, aluminium phytate and phytin, and double salts thereof. Mixtures of any of these salts are also included. Particularly preferred are those soluble in water. More preferably, the phytic acid compound is selected from the group consisting of phytic acid, sodium phytate, potassium phytate, lithium phytate, ammonium phytate and mixtures thereof.
  • chelating agents suitable for use in the present invention are the anionic polymeric polycarboxylates.
  • Such materials are well known in the art, being employed in the form of their free acids or partially or preferably fully neutralised water soluble alkali metal (e.g. potassium and preferably sodium) or ammonium salts.
  • MW molecular weight
  • copolymers are available for example as Gantrez AN 139 (MW 500,000), AN 119 (MW 250,000) and preferably S-97 Pharmaceutical Grade (MW 70,000), of GAF Chemicals Corporation.
  • operative polymeric polycarboxylates include those such as the 1:1 copolymers of maleic anhydride with ethyl acrylate, hydroxyethyl methacrylate, N-vinyl-2-pyrollidone, or ethylene, the latter being available for example as Monsanto EMA No. 1103, MW 10,000 and EMA Grade 61, and 1:1 copolymers of acrylic acid with methyl or hydroxyethyl methacrylate, methyl or ethyl acrylate, isobutyl vinyl ether or N-vinyl-2- pyrrolidone.
  • Additional operative polymeric polycarboxylates are disclosed in US-A-4,138,477 to Gaffar and US-A-4,183,914 to Gaffar et al., and include copolymers of maleic anhydride with styrene, isobutylene or ethyl vinyl ether, polyacrylic, polyitaconic and polymaleic acids, and sulphoacrylic oligomers of MW as low as 1,000 available as Uniroyal ND-2.
  • the carrier for the components of the present compositions can be any vehicle suitable for use in the oral cavity.
  • Such carriers include the usual components of toothpastes, mouth rinses, lozenges, gels, chewing gums and the like and are more fully described hereinafter. Toothpastes are the preferred systems.
  • the toothpaste can be packaged as a single product or be part of a dual or multi-phase system in which different toothpaste formulations are so packaged as to be presented as a single product upon use, such as is known in the art in e.g. striped toothpastes.
  • the liquid compositions herein can also be packaged for delivery as a spray.
  • Water is usually present in the oral compositions of this invention, though in chewing gums the level may be very low. Water used should preferably be deionised and free of organic impurities. Water generally comprises from about 10% to 50%, preferably from about 20% to 40%, by weight of the toothpaste compositions herein. These amounts of water include the free water which is added plus that which is introduced with other materials such as with sorbitol. Optional components
  • the embodiments of this invention can contain a variety of optional dentifrice ingredients some of which are described below.
  • Optional ingredients include, for example, but are not limited to, humectants, flavouring agents, sweetening agents and colouring agents. These and other optional components are further described in US-A-5,004,597; US-A-4,885,155; US-A- 3,959,458 and US-A-3, 937, 807, all being incorporated herein by reference.
  • a preferred optional ingredient in the present compositions is a silicone oil.
  • Suitable classes of silicone oils include, but are not limited to, dimethicones, dimethiconols, dimethicone copolyols and aminoalkylsilicones, preferred silicone oils are selected from dimethicone copolyols and aminoalkylsilicones, more preferably from dimethicone copolyols. Highly preferred is cetyl dimethicone copolyol marketed under the trade name Abil EM90.
  • the silicone oil is useful as an antiplaque agent and helps to prevent re-soiling of teeth.
  • the silicone oil may also enhance the lubricious feel provided by the polyol ester.
  • antimicrobial agents are also useful for inclusion in the compositions of the present invention.
  • a wide variety of antimicrobial agents can be used, including stannous salts such as stannous pyrophosphate and stannous gluconate, quaternary ammonium salts, such as cetyl pyridinium chloride and tetradecylethyl pyridinium chloride, bis-biguanide salts, copper bisglycinate, nonionic antimicrobial agents and certain flavour oils such as thymol.
  • stannous salts such as stannous pyrophosphate and stannous gluconate
  • quaternary ammonium salts such as cetyl pyridinium chloride and tetradecylethyl pyridinium chloride
  • bis-biguanide salts such as copper bisglycinate
  • nonionic antimicrobial agents such as thymol.
  • sodium chlorite described in WO 99/43290.
  • Antimicrobial agents are typically included at levels of from about 0.01% to about 10%. It is preferred to keep the level of stannous and cationic antimicrobial agents to less than 5%, preferably less than 1% to avoid staining problems.
  • Preferred antimicrobial agents are non-cationic antimicrobial agent, such as those described in US5037637.
  • a particularly preferred antimicrobial agent is 2',4,4'-trichloro- 2-hydroxy-diphenyl ether (triclosan).
  • Flavouring agents can also be added to the present compositions.
  • Suitable flavouring agents include oil of wintergreen, oil of peppermint, oil of spearmint, oil of sassafras, and oil of clove.
  • Sweetening agents which can be used include aspartame, acesulphame, saccharin, dextrose, laevulose and sodium cyclamate.
  • Flavouring and sweetening agents are generally used in dentifrice at levels of from about 0.005% to about 2% by weight.
  • thickening agents are carboxyvinyl polymers, such as the Carbopol® series, carrageenan, hydroxethyl cellulose and water soluble salts of cellulose ethers such as sodium carboxymethyl cellulose and sodium carboxymethyl hydroxethyl cellulose.
  • Natural gums such as gum karaya, xanthan gun, gum arabic, and gum tragacanth can also be used.
  • Thickening agents in an amount from 0.5% to 5.0% by weight of the total composition can be used.
  • humectant material in a toothpaste to keep it from hardening.
  • Suitable humectants include glycerin, sorbitol, and other edible polyhydric alcohols at a level of from about 15% to about 70%.
  • buffering agents bicarbonates, peroxides, nitrate salts such as sodium and potassium nitrate.
  • mouthwashes comprise a water / C2 to Cg alcohol solvent, flavour, humectant, sweetener, surfactant, and colorant.
  • Mouthwashes can include ethanol at a level of from 0 to 60%, preferably from 5 to 30% by weight.
  • Oral gels are typically similarly formulated but further comprise from 1 to 30% of a gelling agent. Preferred gelling agents include carbomers and poloxamers.
  • Suitable chewing gum components are disclosed in US-A-4,083,955 and WO97/02009, both incorporated herein by reference.
  • An essential component is chewing gum base comprising an elastomer or elastomer mixture.
  • the elastomers useful in the present gum base composition include styrene-butadiene rubber (SBR) and other elastomeric materials generally known in the art.
  • Illustrative elastomers include SBR, synthetic gums or elastomers such as polyisobutylene and isobutylene-isoprene copolymers; natural gums or elastomers such as chicle, natural rubber, jelutong, balata, guttapercha, lechi caspi, sorva and mixtures thereof.
  • the elastomer or elastomer mixture is generally present in an amount of from 5% to about 30% and preferably from about 7.5% to about 25% by weight of the gum base. When the total amount of elastomer is below 3% the base composition lacks elasticity, chewing texture, and cohesiveness whereas at amounts above about 30% the formulation is hard, rubbery and maintains a tight chew.
  • the following examples further describe and demonstrate preferred embodiments within the scope of the present invention. The examples are given solely for illustration and are not to be construed as limitations of this invention.
  • Example 6 is a chewing gum formulation according to the present invention.
  • Examples 7 to 9 are representative mouthrinse formulations according to the invention.
  • compositions of the present invention can be prepared by standard techniques known to those skilled in the art.
  • compositions provide the benefits of oral lubrication or moisturisation when they are used in the normally accepted manner, such as brushing the teeth, rinsing with a mouth wash, application of a gel to the mucosa or by chewing a gum.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Polymers & Plastics (AREA)
  • Food Science & Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)

Abstract

L'invention concerne des compositions destinées à être administrées par voie orale contenant entre 0,1 % et 15 % d'un ester d'acide carboxylique de polyol comprenant une fraction polyol et au moins 4 fractions d'acide carboxylique, la fraction polyol étant choisie parmi des sucres et des alcools de sucre contenant entre environ 4 et environ 8 groupes hydroxyle, et chaque fraction d'acide carboxylique contenant entre environ 8 et environ 22 atomes de carbone. Lesdites compositions contiennent également entre environ 0,1 % et environ 15 % d'un tensioactif ainsi qu'un excipient acceptables du point de vue oral. Lesdites compositions, qui se présentent de préférence sous la forme d'une pâte dentifrice, d'un dentifrice liquide, d'un chewing-gum, d'un bain de bouche ou d'un gel oral, peuvent améliorer la sensation buccale, être bénéfiques pour l'humidification orale, et notamment soulager ou éviter la sécheresse de la bouche.
PCT/US2001/028059 2000-09-12 2001-09-07 Compositions destinées à être administrées par voie orale WO2002022096A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2001290669A AU2001290669A1 (en) 2000-09-12 2001-09-07 Oral compositions

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0022297.6 2000-09-12
GB0022297A GB0022297D0 (en) 2000-09-12 2000-09-12 Oral compositions

Publications (2)

Publication Number Publication Date
WO2002022096A2 true WO2002022096A2 (fr) 2002-03-21
WO2002022096A3 WO2002022096A3 (fr) 2002-05-10

Family

ID=9899259

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/028059 WO2002022096A2 (fr) 2000-09-12 2001-09-07 Compositions destinées à être administrées par voie orale

Country Status (3)

Country Link
AU (1) AU2001290669A1 (fr)
GB (1) GB0022297D0 (fr)
WO (1) WO2002022096A2 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090053267A1 (en) * 2007-08-20 2009-02-26 Depierro Karen Dentifrice composition containing silicone oil beads
EP1774957A3 (fr) * 2005-10-17 2012-01-25 Henkel AG & Co. KGaA Composition nettoyante pour l'hygiène buccale et dentaire contenant urée à substitution hydroxyalkyle
WO2016133977A1 (fr) * 2015-02-19 2016-08-25 The Procter & Gamble Company Compositions destinées au dépôt sur des surfaces biologiques
US9468614B2 (en) 2009-05-08 2016-10-18 3M Innovative Properties Company Oral care method and kit
WO2017027669A1 (fr) * 2015-08-12 2017-02-16 Cao Group, Inc. Procédés de croissance de couches résistant aux acides sur l'émail dentaire
US10449139B2 (en) 2010-12-23 2019-10-22 Colgate-Palmolive Company Aqueous oral care compositions

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5190747A (en) * 1989-11-06 1993-03-02 Lion Corporation Oral or detergent composition comprising a nonionic surface active agent
EP0541830A1 (fr) * 1991-11-09 1993-05-19 ISP Van Dyk Inc. Base d'absorption contenant un ester de sucrose
WO1997000618A1 (fr) * 1995-06-20 1997-01-09 Wm. Wrigley Jr. Company Chewing-gum ameliore contenant des polyesters de saccharose
US5800848A (en) * 1995-06-20 1998-09-01 The Wm. Wrigley Jr. Company Chewing gum containing sucrose polyesters
US5837300A (en) * 1989-04-11 1998-11-17 Nabisco Technology Company Physiologically compatible liquid sucrose esters as low calorie fat mimetics

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5837300A (en) * 1989-04-11 1998-11-17 Nabisco Technology Company Physiologically compatible liquid sucrose esters as low calorie fat mimetics
US5190747A (en) * 1989-11-06 1993-03-02 Lion Corporation Oral or detergent composition comprising a nonionic surface active agent
EP0541830A1 (fr) * 1991-11-09 1993-05-19 ISP Van Dyk Inc. Base d'absorption contenant un ester de sucrose
WO1997000618A1 (fr) * 1995-06-20 1997-01-09 Wm. Wrigley Jr. Company Chewing-gum ameliore contenant des polyesters de saccharose
US5800848A (en) * 1995-06-20 1998-09-01 The Wm. Wrigley Jr. Company Chewing gum containing sucrose polyesters

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1774957A3 (fr) * 2005-10-17 2012-01-25 Henkel AG & Co. KGaA Composition nettoyante pour l'hygiène buccale et dentaire contenant urée à substitution hydroxyalkyle
US20090053267A1 (en) * 2007-08-20 2009-02-26 Depierro Karen Dentifrice composition containing silicone oil beads
US9468614B2 (en) 2009-05-08 2016-10-18 3M Innovative Properties Company Oral care method and kit
EP2427184B1 (fr) * 2009-05-08 2017-08-30 3M Innovative Properties Company Procédé et kit d'hygiène buccale
US10449139B2 (en) 2010-12-23 2019-10-22 Colgate-Palmolive Company Aqueous oral care compositions
WO2016133977A1 (fr) * 2015-02-19 2016-08-25 The Procter & Gamble Company Compositions destinées au dépôt sur des surfaces biologiques
US9951295B2 (en) 2015-02-19 2018-04-24 The Procter & Gamble Company Compositions for deposition on biological surfaces
WO2017027669A1 (fr) * 2015-08-12 2017-02-16 Cao Group, Inc. Procédés de croissance de couches résistant aux acides sur l'émail dentaire

Also Published As

Publication number Publication date
GB0022297D0 (en) 2000-10-25
AU2001290669A1 (en) 2002-03-26
WO2002022096A3 (fr) 2002-05-10

Similar Documents

Publication Publication Date Title
CA2177680C (fr) Composition de dentifrice anti-tartre contenant du thymol
US20060171907A1 (en) Oral care compositions providing enhanced whitening and stain prevention
EP0652743B1 (fr) Compositions orales
CZ181099A3 (cs) Ústní směs
US5389360A (en) Oral compositions
WO1995031175A1 (fr) Compositions buccales
EP0782437B1 (fr) Compositions bucco-dentaires
AU2016344348B2 (en) Mouthwash products and methods
US20220401321A1 (en) Oral Care Compositions
HUT73785A (en) Oral composition for treating plaque and gingivitis containing a noncationic antibacterial agent and a bicarbonate salt
WO2002022096A2 (fr) Compositions destinées à être administrées par voie orale
US5496539A (en) Oral compositions
EP3534870B1 (fr) Compositions de soins buccaux
JP2001172146A (ja) 口腔用組成物
CN117320683A (zh) 口腔护理组合物
US20220133608A1 (en) Oral Care Compositions
WO1993002658A1 (fr) Compositions orales efficaces contre la plaque dentaire et la gingivite

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ CZ DE DE DK DK DM DZ EC EE EE ES FI FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PH PL PT RO RU SD SE SG SI SK SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase in:

Ref country code: JP