Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
  • A61K8/22—Peroxides; Oxygen; Ozone
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/676—Ascorbic acid, i.e. vitamin C
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
  • A61K9/0007—Effervescent
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
  • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• • 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

• ABSTRACT The use of at least one ene-diol compound having at most 6 carbon atoms and selected from the group consisting of ascorbic acid, isoascorbic acid, dihydroxymaleic acid, dihydroxyfumaric acid, and reductic acid, or salts or derivatives thereof, and an oxidizing agent in the form of a water soluble peroxide selected from the group consisting of alkali metal percarbonate, alkaline earth peroxide, carbamide peroxide, and hydrogen peroxide in the manufacture of preparations effective against bad breath, preferably in the form of peroral dosage units.
• the present invention relates to the use of an oxidizing agent together with at least one ene-diol compound having at most 6 carbon atoms, in the manufacture of preparations which are effective against bad breath.
• the object of the present invention is to eliminate feror ex ore, bad breath, without influencing the natural micro flora of the mouth.
• Tooth breath is a great social handicap to many people and therefore there is a demand for preparations which can eliminate'it. Although frequent tooth brushing is carried out it has been shown that bad breath persists.
• mouth-washes intended to be used against bad breath are known. However, such mouth-washes do not reduce the amount of eg methyl mercaptan but only mask it.
• ascorbic acid and sodium percarbonate are used.
• ene-diol compounds besides ascorbic acid, isoascorbic acid, dihydroxymaleic acid, dihydrox yfumaric acid, or reductic acid (2,3-dihydroxy 2- cyclopenten-l-one), may be used, or salt thereof, such as the sodium, potassium or calcium salt, or derivatives thereof such as the esters of fatty acids having 2-l8 carbon atoms, such as the acetate, palmitate or stearate.
• a peroxide besides sodium percarbonate, other alkali percarbonates, alkaline earth peroxides, carbamide peroxide (carbamide crystallized with H instead of H 0), and hydrogen peroxide may be used.
• inert filling agents and lubricants known per se are used.
• Such filling agents are e.g. mannitol, sodium bicarbonate, tartaric acid and starch.
• magnesium stearate As lubricants, magnesium stearate, and paraffin may be used.
• Binding agents used in the granulation of the com pounds prior to the manufacture of e.g. tablets and the like are e.g. polyvinylpyrrolidone and gelatin.
• flavoring agents may be added. Suitable flavors are spearmint, peppermint, menthol, spiced fruits, orange, lemon, lime, etc.
• pellets or granules is chewed, whereby a reaction between the two active components, the ene-diol compound and the oxidizing agent is obtained and a destruction of the bad smelling compounds takes place.
• the amount of active oxygen produced per occasion of administration is at least 1 mg, preferably 3 mg, and the amount of the ene-diol compound is at least 10 mg.
• the administration takes place 3 to 4 times per day.
• the preparation may also be manufactured as soaking tablets, lozenges, chewing gum or in aerosol or spray form.
• Tablets may be chewed, or dissolved in water to produce a mouth wash.
• the amount of ene-diol compound should not exceed 200 mg per occasion of administration and the amount of peroxide should thus not exceed mg as active oxygen.
• EXAMPLE 1 The tablets were prepared by granulating the mannito] and the sodium percarbonate with a solution of gelatin in water.
• the sodium bicarbonate was granulated with a 50% solution of polyvinylpyrrolidone in ethanol.
• the ascorbic acid and tartaric acid were granulated with a solution of polyethylene glycol in ethanol.
• the different granulates were passed through an oscillating granulator where the granulates are mixed with flavoring agents. Finally, tablets were pressed in a common tablet punching machine.
• EXAMPLE 2 Effervescing granules were prepared and packed in dosage units, whereby each dose contained Ascorbic acid l0 mg Sodium percarbonate corresponding to active oxygen 1 mg Sodium bicarbonate 4 mg Tartaric acid 5 mg Polyvinyl pyrrolrdone 0.02 mg Flavoring agents q.s. Coloring agents q.s. Mannitol 0.03 g
• the granules were prepared in accordance with the tablets above, excluding the tableting step.
• EXAMPLE 3 Effervescing tablets were prepared containing Ascorbic acid 50 mg Sodium percarbonate corresponding to active oxygen 5 mg Tartaric acid 5 mg The preparation contained ethanol "Standard Deviation -Continued Table 2 Sodium bicarbonate 25 mg Starch 10 g Polyvinyl pyrrolidone 2.5 mg Compound m the breath MeSH n-PrOH MeSSMe Flavoring agents q. pfepurmmn Coloring agents q.s.
• a composition effective in combattmg bad breath consisting essentially of an ene-diol compound selected
• the tablets were prepared in accordance with the from the group consisting of ascorbic acid and isotablets of Example 1. ascorbic acid, said compound being present in an The reducing effect of the above preparations on bad amount of at least 10 and oxldlzmg agent m the breath has been studied in vitro. Morning saliva from form of a w Solubl?
• peroxlde Selected from i a number of tested persons was incubated at for group consisting of alkali metal percarbonates, alkaline 5 to 12 hours until great amounts of methyl mercaptan f Peroxldes f carbalmde Peroxlder wherein sflld had been formed, whereupon the saliva was divided OXd1Z mg agent Present an amount corresp ondmg into samples each containing 3 ml in 20 ml injection to acme Oxygen m an amolfm of at least 1 each flasks, which were deep-frozen in a Dewer-vessel using Case Per peroridosage coricg The different Compared preparations were 2.
• composition according to claim 1 wherein the then added in the amounts stated by opening the capcne'dlol P H ascorbic acid sule of the deep-frozen flasks, introducing the preparacomposltlon aFCOrdmg P claim 1 the tion, rapidly removing the air by sweeping with nitro ene'dlol compound ascorbl? f f f" an gen gas and closing the flasks again.
• the amount at least 10 mg and the oxidizing agent is sodium flasks were thawed and after 20 minutes at 36C a samperFarbonate Present m an amount corresponfimg to ple was taken and analyzed on a gas chromatograph.
• Example 1 A method of inhibiting bad breath by administerabove In Example 1; C, a preparation according to the in Oran at 1 st 10 m f l d invention containing in addition 0.2% of a heavy metal g per y ea ah chelo h h catalyst in the form of copper sulphate calculated on Selecteh the group cohslshhg of hscorblc acid the ene diol compound and D a known mouthwash ascorbic acid, and salts or derivatives thereof, together containing menthol as masking agent are given.
• h Oxlchzmg agent In the form Water soluble?
• Table 2 a comparison between a control sample A, and peroxlde selected from group cohslshhg of alkah the preparations B and C and in addition, E, a liquid meial percaibohates alkhhhe earth.
• perhxldes carbantibacterial iodine composition having oxidizing prophhhde perohlde ahdhydrogeh heroxlde m an amount erties is given.
• the results are given in mm peak height corresphhdmg to achve Oxygen m an hmohht of at least of the g chromatograms 1 mg., in each case*per*perkorai dtlsage unit.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Epidemiology (AREA)
• Chemical & Material Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Birds (AREA)
• Medicinal Chemistry (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Oral & Maxillofacial Surgery (AREA)
• Emergency Medicine (AREA)
• Inorganic Chemistry (AREA)
• Zoology (AREA)
• Nutrition Science (AREA)
• Physiology (AREA)
• Cosmetics (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (1)

Publications (1)

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Family Applications (1)

Country Status (13)

Cited By (26)

Families Citing this family (5)

Citations (1)

Family Cites Families (1)

• 1972
  • 1972-06-30 SE SE08597/72A patent/SE369036B/xx unknown
• 1973
  • 1973-06-12 ZA ZA733996A patent/ZA733996B/xx unknown
  • 1973-06-19 BE BE132419A patent/BE801102A/xx unknown
  • 1973-06-22 DE DE2331681A patent/DE2331681A1/de active Pending
  • 1973-06-25 AU AU57271/73A patent/AU5727173A/en not_active Expired
  • 1973-06-26 CA CA174,951A patent/CA1000204A/en not_active Expired
  • 1973-06-26 IT IT51046/73A patent/IT986224B/it active
  • 1973-06-27 GB GB3046273A patent/GB1429234A/en not_active Expired
  • 1973-06-28 DK DK357173AA patent/DK135703B/da unknown
  • 1973-06-29 NL NL7309085A patent/NL7309085A/xx unknown
  • 1973-06-29 FR FR7324041A patent/FR2190408B1/fr not_active Expired
  • 1973-06-30 JP JP48073339A patent/JPS4930544A/ja active Pending
  • 1973-07-02 US US375615A patent/US3886265A/en not_active Expired - Lifetime

Patent Citations (1)

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