WO1990010434A1 - Preparation dentaire - Google Patents

Preparation dentaire Download PDF

Info

Publication number
WO1990010434A1
WO1990010434A1 PCT/SE1990/000165 SE9000165W WO9010434A1 WO 1990010434 A1 WO1990010434 A1 WO 1990010434A1 SE 9000165 W SE9000165 W SE 9000165W WO 9010434 A1 WO9010434 A1 WO 9010434A1
Authority
WO
WIPO (PCT)
Prior art keywords
cupric
bisbiguanide
gluconate
acetate
salt
Prior art date
Application number
PCT/SE1990/000165
Other languages
English (en)
Inventor
Gunnar Rölla
Jan Ekstrand
Marthe Waerhaug
Original Assignee
Roella Gunnar
Jan Ekstrand
Marthe Waerhaug
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 Roella Gunnar, Jan Ekstrand, Marthe Waerhaug filed Critical Roella Gunnar
Publication of WO1990010434A1 publication Critical patent/WO1990010434A1/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/43—Guanidines

Definitions

  • the present invention refers to a dental preparation containing a water soluble, physiologically acceptable salt of an antimicrobal bisbiguanide.
  • Said dental preparation can be in the form of a mouth rinse, tooth paste, gel, tablet or chewing gum, which prevents plaque formation on the teeth. By this the development of caries and/or periodontitis, that is loosening of the teeth, can be prevented.
  • Ar is an optionally substituted aryl group and n is an f ⁇ teger from 4 to 8, especially 6.
  • n is an f ⁇ teger from 4 to 8, especially 6.
  • Chlorhexidine is difficult to dissolve in water and has to be trans ⁇ formed into a salt to attain a soluble form.
  • the salts which have been found to be appropriate to use as an antimicrobal preparation are particularly the acetate and the gluconate.
  • the gluconate salt of chlorhexidine in particular has been used extensively and is inter alia sold by ICI, Machlefield, England under the trademark "HIBITANE".
  • Chlorhexidine also arrests the development of dental diseases al eady started.
  • chlorhexidine can also be used in the form of tooth paste or gel for tooth brushing, giving the same 90/10434 . -_ .
  • DE-A1-2534887 refers to a dental preparation with inhibiting effect on the formation of plaque and caries, comprising in addition to for instance chlorhexidine a chelate forming compound.
  • the purpose of the chelate forming compound is to prevent the discoloration of the teeth which is brought about by chlorhexidine.
  • Preferred chelate forming compounds are ethylene diamino- acetic acid, kojic acid, malthol and calcium dihydrogen ethylenedi- a inotetraacetate.
  • Chlorhexidine also, when used as a mouth rinse or tooth paste, can bring about a temporary loss of taste sensation, which seems to be dependent on the concentration.
  • a combination of a bisbiguanide and a cupric salt such as cupric acetate or cupric gluconate, has a syner- gistic plaque inhibiting effect, at the same time as the formation of dis ⁇ coloration is mild and of such a character, that it can easily be brushed away by the patient by means of tooth brushing, which is not possible with discolorations which have been formed in connection with the use of chlor ⁇ hexidine solely.
  • the dental preparation of the invention comprises the salt of the bisbiguanide and the cupric salt in a proportion giving a synergistic plaque preventing effect.
  • chlorhexidine is systemically well tolerated a concentration of from about 0.2?. by weight can cause erosion of the mucous membrane. In order to prevent inconvenient side effects it is of advantage to aim at as low a concentration as possible of the active compounds in the dental preparation.
  • a solution was prepared containing 0.05% by weight chlorhexi ⁇ dine and 0.04% by weight cupric acetate.
  • a group of 15 healthy subjects took part in a double blind cross over study, wherein each subject took part in 3 studies which each lasted for three weeks. During each three week period the subjects performed no oral hygiene.
  • As a positive control the subjects rinsed with a 0.12% by weight chlorhexidine solution for three weeks and as a negative control they rinsed with physiological saline solution.
  • Plaque and gingivale indices were registered according to clinical standard methods (Loe, H. J. of Periodontology 36:610-616, 1965). 90/10434
  • MIC (minimal inhibitory concentration) tests were performed with chlor ⁇ hexidine and cupric acetate singularly and with different combinations of said salts on Streptococcus mutans and Actinomyces viscosus respectively. Percent values refers in the following to percent by weight if nothing else is stated.
  • Isolates of Streptococcus mutans serotype C and Actinomyces viscosus were cultured in Trypticase Soy Broth (TSB) supplemented with yeast extract (YE) (0.5%) in a 5% C ⁇ 2-incubator for 24 hours.
  • the cultures were harvested by centrifugation, washed and resuspended in TSB-YE of the double strength and were adjusted to the appropriate optical density upon reference to a predetermined standard curve.
  • Serial dilutions of chlorhexidine gluconate and cupric acetate were made in 0.15 M NaCl.
  • the assay mixtures consisted of a standardized inoculate of washed cells (final concentration 5xl0 5 cfu/ml) and of the same volume of the compound to be tested. To determine an optional synergistic effect different concentrations of each compound were combined and inoculated as above. All tubes were incubated for 24 hours in 5% CO2 at 37°C.
  • a dental preparation according to the invention comprising an antimicro ⁇ bal bisbiguanide in combination with a physiologically acceptable cupric salt in addition to an improved plaque inhibiting effect at a lower concentration also brings about a reduced discoloration of the teeth as well as a reduced calculus formation.
  • a solution can contain 0.5 - 5.5 mM bisbiguanide in combination with 0.55 - 10 mM cupric salt, preferably 0.5 - 2.0 mM bisbi ⁇ guanide and 2.0 - 5.0 mM cupric salt.
  • a solid preparation preferably contains 2.1 - 21 mM bisbiguanide in combination with 0.55 - 100 mM cupric salt.
  • the dental preparation according to the invention can have the form of a mouth rinse, tooth paste or gel and also have the form of a tablet or a chewing gum.
  • a mouth rinse can contain 0.05 - 0.5, preferably 0.05 - 0.2% by weight bisbiguanide as an acetate or gluconate and 0.01 - 1.0, preferably 0.04 - 0.08 % by weight cupric acetate or cuprfc gluconate.
  • a tooth paste or gel should contain 0.2 - 2 percent by weight bisbiguanide as an acetate or gluconate and 0.01 - 10 percent by weight cupric acetate or cupric gluconate.
  • a tablet or chewing gum should contain 0.2 - 2 percent by weight bisbiguanide as acetate or gluconate and 0.01 - 10 percent by weight cupric acetate or cupric gluconate.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cosmetics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Une préparation dentaire contenant un sel soluble dans l'eau, physiologiquement acceptable d'un bisbiguanide antimicrobien, de préférence de la chlorhexidine, ainsi qu'un sel cuprique soluble dans l'eau, physiologiquement acceptable, présente un effet sinergique inhibant la plaque, combiné à une décoloration et à une formation de calculs réduits. Ladite préparation dentaire peut se présenter sous la forme d'un collutoire, de pâte ou de gel dentaire, ou sous la forme d'un comprimé ou d'une gomme à mâcher.
PCT/SE1990/000165 1989-03-15 1990-03-15 Preparation dentaire WO1990010434A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE8900915-3 1989-03-15
SE8900915A SE465905B (sv) 1989-03-15 1989-03-15 Tandvaardsmedel som innehaaller ett acetat- eller glukonatsalt av en antimikrobiell bisbiguanid

Publications (1)

Publication Number Publication Date
WO1990010434A1 true WO1990010434A1 (fr) 1990-09-20

Family

ID=20375350

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/SE1990/000165 WO1990010434A1 (fr) 1989-03-15 1990-03-15 Preparation dentaire

Country Status (3)

Country Link
AU (1) AU5351590A (fr)
SE (1) SE465905B (fr)
WO (1) WO1990010434A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6500466B2 (en) * 1998-12-11 2002-12-31 Degussa Ag Chlorhexidine formulations, new chlorhexidine salts, solutions containing these and their use
WO2005084627A1 (fr) * 2004-03-01 2005-09-15 University Of Iowa Research Foundation Compositions de chlorhexidine sans alcool
DE102015218892A1 (de) 2014-10-01 2016-05-12 Wald Pharmaceuticals S.R.O. Applikationsgemisch zur Erhöhung der Wirkung von Antiseptika und/oder Desinfektionsmitteln, Applikationsmittel mit dem Gehalt des Applikationsgemischs und die Verwendung dieses Gemischs
CN113476386A (zh) * 2021-08-19 2021-10-08 杭州迅腾医疗器械有限公司 一种漱口液及其制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2534887A1 (de) * 1974-08-09 1976-02-26 Procter & Gamble Mund- und/oder zahnpflegemittel
EP0038867A1 (fr) * 1980-04-29 1981-11-04 Blendax-Werke R. Schneider GmbH & Co. Pâte dentifrice
EP0216189A2 (fr) * 1985-09-14 1987-04-01 Blendax GmbH Composition d'hygiène orale
EP0229375A1 (fr) * 1986-01-07 1987-07-22 Blendax GmbH Composition pour l'hygiène buccale

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2534887A1 (de) * 1974-08-09 1976-02-26 Procter & Gamble Mund- und/oder zahnpflegemittel
EP0038867A1 (fr) * 1980-04-29 1981-11-04 Blendax-Werke R. Schneider GmbH & Co. Pâte dentifrice
EP0216189A2 (fr) * 1985-09-14 1987-04-01 Blendax GmbH Composition d'hygiène orale
EP0229375A1 (fr) * 1986-01-07 1987-07-22 Blendax GmbH Composition pour l'hygiène buccale

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6500466B2 (en) * 1998-12-11 2002-12-31 Degussa Ag Chlorhexidine formulations, new chlorhexidine salts, solutions containing these and their use
WO2005084627A1 (fr) * 2004-03-01 2005-09-15 University Of Iowa Research Foundation Compositions de chlorhexidine sans alcool
DE102015218892A1 (de) 2014-10-01 2016-05-12 Wald Pharmaceuticals S.R.O. Applikationsgemisch zur Erhöhung der Wirkung von Antiseptika und/oder Desinfektionsmitteln, Applikationsmittel mit dem Gehalt des Applikationsgemischs und die Verwendung dieses Gemischs
US9546407B2 (en) 2014-10-01 2017-01-17 Wald Pharmaceuticals S.R.O. Mixture to increase the effectiveness of antiseptics and/or disinfectants, an agent containing the mixture, and the use of this mixture
CN113476386A (zh) * 2021-08-19 2021-10-08 杭州迅腾医疗器械有限公司 一种漱口液及其制备方法

Also Published As

Publication number Publication date
SE8900915D0 (sv) 1989-03-15
AU5351590A (en) 1990-10-09
SE465905B (sv) 1991-11-18
SE8900915L (sv) 1990-09-16

Similar Documents

Publication Publication Date Title
US5770588A (en) Non-antibacterial tetracycline compositions of the prevention and treatment of root caries
US4229430A (en) Oral composition for improving oral health
US5560906A (en) Non-alcoholic antimicrobial mouthwash for removal of dental plaque
EP0606599A1 (fr) Compositions pour soins buccaux contenant des acids de houblon
WO1992013515A1 (fr) Compositions a base de tetracyclines non antibacteriennes presentant des proprietes antiplaque
US5830489A (en) Protein preparation for the prevention and therapy of periodontitis
EP0616520B1 (fr) Compositions antimicrobiennes au phytate pour produits de soins bucco-dentaires
US4477429A (en) Oral compositions comprising N.sup.α -alkyl derivatives of arginine
US4499068A (en) Oral compositions comprising NG -alkyl derivatives of arginine
US4477428A (en) Oral compositions comprising N.sup.α,NG -diacyl derivatives of arginine
Compton et al. Inhibitory effect of benzethonium and zinc chloride mouthrinses on human dental plaque and gingivitis
US5320829A (en) Oral compositions for inhibiting plaque formation
US5827503A (en) Method and composition for treating periodontitis
WO1990010434A1 (fr) Preparation dentaire
CA1315693C (fr) Procede et composition pour l'hygiene buccale
US4886658A (en) Oral treatment method for reducing plaque with reduced staining
US20050180927A1 (en) Novel anti-bacterial compositions
WO1987005501A1 (fr) Traitement des surfaces dentaires a l'aide d'agents retardant la plaque
JPH02250815A (ja) う蝕防止剤、う蝕防止用口腔内組成物またはう蝕防止機能付き飲食物
JPH08268855A (ja) 口腔用組成物
JPH07133222A (ja) グルコシルトランスフェラ−ゼ阻害剤
AU2003213864B2 (en) Novel anti-bacterial compositions
Shern et al. Effects of daily rinses using sodium fluoride and organic fluorides on rat caries
WO1991015189A1 (fr) Procede et composition servant a prevenir les stomatites chez les utilisateurs de dentiers
JPS5812251B2 (ja) 口腔用組成物

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AU BG BR CA FI HU JP KR NO RO SU US

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): AT BE CH DE DK ES FR GB IT LU NL SE