WO2018024649A1 - Composition de soins dentaires contenant de l'hydroxyapatite - Google Patents

Composition de soins dentaires contenant de l'hydroxyapatite Download PDF

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Publication number
WO2018024649A1
WO2018024649A1 PCT/EP2017/069262 EP2017069262W WO2018024649A1 WO 2018024649 A1 WO2018024649 A1 WO 2018024649A1 EP 2017069262 W EP2017069262 W EP 2017069262W WO 2018024649 A1 WO2018024649 A1 WO 2018024649A1
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WO
WIPO (PCT)
Prior art keywords
dentifrice composition
particle size
size distribution
volume
based particle
Prior art date
Application number
PCT/EP2017/069262
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German (de)
English (en)
Inventor
Joachim Enax
Adolf Klenk
Christoph Abels
Original Assignee
Dr. Kurt Wolff Gmbh & Co. Kg
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 Dr. Kurt Wolff Gmbh & Co. Kg filed Critical Dr. Kurt Wolff Gmbh & Co. Kg
Publication of WO2018024649A1 publication Critical patent/WO2018024649A1/fr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0241Containing particulates characterized by their shape and/or structure
    • A61K8/0275Containing agglomerated particulates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24Phosphorous; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/41Particular ingredients further characterized by their size
    • A61K2800/412Microsized, i.e. having sizes between 0.1 and 100 microns

Definitions

  • the different parts of a natural tooth are the tooth crown, the tooth neck and the tooth root, which are composed of several layers. Of these layers, one usually only sees the outer enamel, which surrounds the dentin and other layers. For example, to bite or grind food, the enamel is very hard. It consists of about 97 wt. Of hydroxyapatite, which has the following empirical formula: Ca 5 (P0 4 ) 3 (OH). The dentin is also considered hard tooth substance and consists of about two thirds also of hydroxyapatite. Dentin contains proteins and water in addition to hydroxyl apatite and is therefore not as hard as enamel.
  • Dental caries is considered to be a multi-factorial disease, especially of enamel and dentin, with the involvement of microorganisms.
  • a precipitate also called pellicle
  • saliva protein The rougher the tooth surface, the easier the precipitate can form or adhere to it.
  • pellicle is then formed after a time a tooth surface covering, a few microns thick film.
  • bacteria can then multiply and spread, and this film can be considered a biofilm.
  • the bacteria mentioned in today's Food commonly present low molecular weight carbohydrates produce organic acids, such as gluconic and lactic acid.
  • calcium phosphate is dissolved out of the enamel. If this process is not halted, or even vice versa, demineralization of the enamel and possibly also of the dentin may occur after some time.
  • a defect in the hard tooth tissue is called a carious lesion.
  • carious lesions on the dentin layer can be identified as having a yellow to brown colouration of the corresponding part of the tooth.
  • a Fluoride sources in the mentioned dental care products are various fluoride compounds such as sodium fluoride, stannous fluoride, amine fluorides and monofmorphosphates.
  • JM ten Cate: "The Need for Antibacterial Approaches to Improve Caries Control", Adv Dent Res 21: 8-12, August 2009, pp. 8-12, is concerned that fluoride delivery alone may not be sufficient to provide adequate caries prevention
  • bacteria also play a crucial role in caries formation, but the fluoride ion itself does not exhibit a pronounced antimicrobial effect.
  • caries prophylaxis compositions are contemplated which, in addition to fluoride, also include one or more antimicrobial substances.
  • An example Chlorhexidine (CHX) the antimicrobial agent of the oral cavity, has been studied in many studies.
  • fluorides in dental care products are also being discussed controversially, as negative side effects are feared.
  • fluorosis which is caused by an excessive fluoride intake and has symptoms such as nausea, vomiting and diarrhea.
  • Other examples are bone fmorosis, which is manifested by thickening of the outer bone layer and the associated loss of elasticity and resilience of the bones, and the molten fluorosis, which can be recognized by the appearance of whitish enamel spots on the tooth surface.
  • the ingestion of high-dose dental care products especially in children can trigger an acute fluoride intoxication, which can sometimes even be fatal.
  • WHO is unable to establish a value for a daily fluoride requirement since fluoride is not an essential trace element and thus there are no diagnostic parameters and no evidence of the existence of clinical symptoms of "fluoride deficiency".
  • an antimicrobial substance such as chlorhexidine is not uncontroversial in dental care, in particular caries prophylaxis. It has been reported that a relevant effect for caries prophylaxis is not always reproducible and occurs only in a part of the cases studied. Furthermore, the antimicrobial effect of chlorhexidine is not limited to the oral caries involved in caries formation, but also includes beneficial bacteria. In addition, a long-term treatment with chlorhexidine-containing products leads to undesirable side effects, such as tooth discoloration and taste disorders.
  • Biomimetic tooth and mouth rinsing solutions with artificial enamel may, for example, contain zinc carbonate hydroxyapatite.
  • This zinc carbonate hydroxyapatite is also known commercially as a microrepair.
  • Zinc carbonate hydroxyapatite based products may alter the initial bacterial colony reduce the surface area of the enamel surface without having antimicrobial properties that can interfere with the environmental balance of the oral cavity.
  • these products are intended to serve, among other things, for remineralization and the repair of microfine defects in enamel as well as the formation of a protective layer.
  • a dental care product which remineralises already existing, smaller carious lesions and / or repairs microfine defects in the enamel.
  • a protective layer should be applied to the tooth and / or open dentinal tubules should be closed.
  • adhesion of bacteria to the enamel should be advantageously reduced without significantly disturbing the eclogical balance in the oral cavity and / or risking tooth discoloration or taste disorder.
  • the composition according to the invention advantageously remineralises smaller carious lesions and / or repairs microfine defects in the enamel, especially in patients with Dry mouth / salivary poverty.
  • a protective layer can be applied to the tooth and further it could be found that the enamel has a favorable solubility and resistance to acid after the application of the composition according to the invention.
  • antimicrobial substances such as chlorhexidine
  • an adjuvant can be dispensed with as an adjuvant.
  • the subject of the present invention is a dentifrice composition
  • a dentifrice composition comprising Ca 5 (PO 4 ) 3 (OH) in which the Xso value of the volume-based particle size distribution Q 3 (x) is 1, 0 - 15.0 ⁇ , wherein the Xso value of the volume-based particle size distribution is measured by means of laser diffraction.
  • the dentifrice composition according to the invention may also comprise oral cosmetic and / or medical care products.
  • the Cas (P0 4 ) 3 (OH) comprised in the present dentifrice composition is preferably prepared synthetically. This means that the Ca 5 (PO 4 ) 3 (OH) used is preferably not obtained by burning out the organic constituents from animal material such as, for example, bones.
  • Cas (P0 4 ) 3 (OH) also called hydroxyapatite, is present in pure form. A pure form is according to the invention exactly then
  • the Ca 5 (P0 4) 3 (OH) containing ions (Ca, P0 4 "and OH") are each less than 1%, preferably less than 0.5%, still more preferably less than 0, 1% are substituted by one or more other ions.
  • the Ca 2+ ions are exemplified by Mg 2+ or Zn 2+ and the OH " ions are less than 1%, for example, fluoride or chloride, preferably less than 0.5%, more preferably less than 0, 1% substituted.
  • hydroxyapatite according to the invention contains no doping, such as a zinc carbonate doping.
  • composition according to the invention comprises (pure) Ca 5 (PO 4 ) 3 (OH), hydroxyapatite, as the only apatite component.
  • the X5 0 value of the volume-based particle size distribution Q 3 (x) of the Ca 5 (P0 4) 3 (OH) is from 1, 0 to 15.0 ⁇ , preferably 1, 2 to 12.0 ⁇ , more preferably 1, 5 to 10.0 ⁇ , more preferably 2.0 to 5.0 ⁇ , wherein the Xso value of the volume-based particle size distribution is measured by laser diffraction.
  • a sample of the hydroxyapatite is first sonicated in an ultrasonic homogenizer with an energy output of 96 W for 9 minutes and then for 3 minutes in a device for sample preparation.
  • the subsequent particle size distribution measurement (laser diffraction) is carried out in a particle size determination instrument at a temperature of 25 ° C + 0.3 ° C and the corresponding values are calculated according to the Mie theory.
  • the measuring instruments used are exclusively commercially available devices.
  • the Ca 5 (PO 4 ) 3 (OH) has a hexagonal crystal lattice in which the length of the a-axis is 0.930 to 0.950 nm, preferably 0.933 to 0.948 nm, particularly preferably 0.936 to 0.945 nm and the length the c-axis is 0.680 to 0.700 nm, preferably 0.682 to 0.696 nm, particularly preferably 0.685 to 0.692 nm.
  • the lengths of the a-axis and the c-axis are determined by a Rietveld evaluation of the corresponding X-ray powder diffractograms.
  • the X-ray powder diffractograms themselves are obtained by means of a measurement with a conventional powder diffractometer at the routine settings.
  • the Ca 5 (PO 4 ) 3 (OH) used according to the invention has a largely spherical crystal morphology.
  • the Ca 5 (P0 4 ) 3 (OH) has no needle-shaped crystal morphology.
  • Such a needle-like crystal morphology could entail undesirable disadvantages similar to asbestos.
  • the Cas (P0 4 ) 3 (OH) is present in aggregated form.
  • an aggregation is understood to mean an aggregation of molecules or particles into a larger dressing, the aggregate. This assembly or aggregate is governed by different forces and / or bonding modes, such as ionic bonding.
  • Nanoparticles are particles with a size of less than 100 nm. With regard to nanoparticles, it is not yet known if they can have an adverse effect on humans, for example after a possible penetration of the intestinal wall.
  • the dentifrice composition according to the invention may also comprise oral medical and / or cosmetic care products. These oral medical and / or cosmetic care products may be in any form known to those skilled in the art.
  • the dentifrice composition according to the invention is preferably in the form of a toothpaste, a mouth gel, a gum bag or a mouth rinse.
  • a toothpaste also referred to as toothpaste, can be used for mechanical tooth cleaning and is a soft or semi-solid composition for oral use, especially on the teeth.
  • a mouth gel is a gel-like composition that can be used in the treatment of discomfort / pain, for example on the oral mucosa, gums and lips or to combat dry mouth.
  • the Mundgel is usually applied to the painful area such as in the case of aphthae on the oral mucosa.
  • a mouthwash also known as mouthwash, is a liquid that can be used, among other things, for the prophylaxis of tooth decay and other disorders in the mouth.
  • the composition according to the invention is in the form of a toothpaste.
  • composition according to the invention is in the form of a mouthwash.
  • the dentifrice composition according to the invention preferably contains Ca 5 (PO 4 ) 3 (OH) in an amount of 2.5 to 15% by weight, preferably 3.5 to 13% by weight, in particular 4.5 to 11% by weight, based on the total weight of the dentifrice composition. It is known that the amount of Cas (P0 4 ) 3 (OH) can also be dependent on the form in which the dentifrice composition (toothpaste, oral gel, etc.) is present. For example, a toothpaste may contain a greater amount of Cas (P0 4 ) 3 (OH) than a mouthwash.
  • the dentifrice composition of the invention may contain one or more pharmaceutical or cosmetic adjuvants.
  • pharmaceutical or cosmetic auxiliaries are described examples game, in toothpastes, Monographs in Oral Science, Vol. 23, I st edition 2013.
  • one or more pharmaceutical or cosmetic adjuvants comprise antimicrobials, pH regulators, xylitol, abrasives, and flavoring agents.
  • Antimicrobial substances are substances that kill microorganisms, such as bacteria, or can greatly reduce their multiplication. In addition to antimicrobial substances with a non-specific defense against bacteria and fungi, there are also those that, for example, only act against targeted bacteria. Through the use of antimicrobial substances, for example, bad breath can also be combated.
  • antimicrobial substances may be contained in an amount of 0.01 to 1.0% by weight, preferably 0.05 to 0.5% by weight, in the dentifrice composition of the present invention.
  • the antimicrobials used in oral care are zinc compounds such as zinc chloride and zinc nitrate, as well as chlorhexidine, triclosan, cetylpyridinium chloride and stannous chloride.
  • the composition according to the invention contains no chlorhexidine and / or triclosan.
  • pH regulators are substances that can adjust a specific pH range, preferably a neutral range of pH 6.5 to 7.5. In the case of an acidic composition, there would be a risk of demineralization of the tooth hard substance (erosion).
  • pH regulators are sodium hydroxide (NaOH) or phosphoric acid (H 3 PO 4 ), which can be used according to the desired pH. To raise too low a pH, sodium hydroxide may be added while at too high a pH, phosphoric acid may be added.
  • the dentifrice composition according to the invention preferably contains xylitol.
  • Xylitol can minimize the number of caries bacteria and inhibit their growth.
  • xylitol can stimulate the salivation.
  • the composition of the invention may contain xylitol in an amount of 0.5 to 10% by weight, preferably 0.7 to 8% by weight, based on the total weight of the dentifrice composition.
  • the composition of the invention may contain other sugar alcohols, such as sorbitol.
  • Abrasives also known as cleaning agents or abrasives, usually remove plaque and harmful bacteria from the tooth surface during tooth cleaning, along with the toothbrush, and may also lighten the skin.
  • Abrasives may preferably be included in the dentifrice composition of the invention in an amount of up to 10% by weight, based on the total weight of the dentifrice composition.
  • abrasives are whiting, marble powder and / or silicate compounds, such as silica.
  • Flavorings may give the desired dentifrice composition of the invention.
  • aroma substances can be saliva-stimulating, whereby the moisture of the saliva can have a positive influence on the remineralization of the tooth.
  • An example of a saliva-stimulating flavorant is pellitorin, especially trans-pellitorin.
  • dentifrice compositions often contain fluoride compounds such as sodium fluoride, amine fluorides or zinc fluoride.
  • the dental care composition according to the invention contains no fluoride compound and is thus fluoride-free.
  • the dentifrice composition according to the invention is a toothpaste and contains
  • zinc salt in particular zinc chloride
  • the pH is in a neutral range of pH 6.5 to 7.5.
  • zinc salt in particular zinc PCA
  • antimicrobial substance in particular cetylpyridinium chloride
  • Flavoring agent in particular pellitorin,
  • the data in% by weight relate to the total weight of the dental care composition.
  • the pH is in a neutral range of pH 6.5 to 7.5.
  • the present invention relates to the dentifrice composition of the invention for use in the prophylaxis (prevention) and treatment of caries.
  • the dentifrice composition according to the invention By using the dentifrice composition according to the invention, the tooth hard substance, in particular the enamel, is protected from harmful bacteria for a time prior to the increased colonization.
  • the dentifrice composition according to the invention remelted so that caries, especially at an early stage, for example, by the repair of microcracks can be treated.
  • the dentifrice composition of the present invention can be used in the prevention and treatment of caries in people with xerostomia (dry mouth).
  • the hydroxylapatite is already present and does not have to be formed by remineralization.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention concerne une composition pour soins dentaires contenant de l'hydroxyapatite, de préférence synthétique, présentant une distribution granulométrique en volume particulière, et son utilisation, en particulier pour la prévention des caries.
PCT/EP2017/069262 2016-08-01 2017-07-31 Composition de soins dentaires contenant de l'hydroxyapatite WO2018024649A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102016114189.5 2016-08-01
DE102016114189.5A DE102016114189A1 (de) 2016-08-01 2016-08-01 Zahnpflegezusammensetzung mit Hydroxylapatit

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WO2018024649A1 true WO2018024649A1 (fr) 2018-02-08

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022152347A1 (fr) 2021-01-15 2022-07-21 Dr. Kurt Wolff Gmbh & Co. Kg Produit d'hygiène dentaire
DE102021111354A1 (de) 2021-05-03 2022-11-03 Dr. Kurt Wolff Gmbh & Co. Kg Mundpflegemittel

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102017009626A1 (de) 2017-10-13 2019-04-18 Dr. Kurt Wolff Gmbh & Co. Kg Oralzusammensetzung mit Zitrusextrakt und Hydroxylapatit
DE102018102365A1 (de) 2018-02-02 2019-08-08 Dr. Kurt Wolff Gmbh & Co. Kg Hydroxylapatit
RU2691960C1 (ru) * 2019-01-10 2019-06-19 Федеральное государственное бюджетное образовательное учреждение высшего образования "Кубанский государственный медицинский университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО КубГМУ Минздрава России) Гидрогель для реминерализации твердых тканей зубов
DE102019104840A1 (de) * 2019-02-26 2020-08-27 Dr. Kurt Wolff Gmbh & Co. Kg Oralgel-Zusammensetzung mit Hydroxylapatit und Calciumsalz
US20230027912A1 (en) * 2019-12-05 2023-01-26 Dr. Kurt Wolff Gmbh & Co. Kg Deep-layer remineralization of hydroxylapatite
DE102020000733A1 (de) 2020-02-04 2021-08-05 Dr. Kurt Wolff Gmbh & Co. Kg Zusammensetzung zur Oralpflege bei Tieren

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2216304C2 (ru) * 2002-05-15 2003-11-20 Общество с ограниченной ответственностью "Олимп" Способ местного лечения гиперестезии зубов при пародонтите и пародонтозе
US20080206554A1 (en) * 2005-01-04 2008-08-28 Rutgers, The State University Hydroxyapatite With Controllable Size And Morphology
DE102010063720A1 (de) * 2010-12-21 2011-06-16 Lr Health & Beauty Systems Gmbh Silberhaltige Zahnpflegezusammensetzung
WO2014162167A1 (fr) * 2013-03-30 2014-10-09 Instytut Wysokich Cisnien Polskiej Akademii Nauk Procédé de production de nanoplaques d'hydroxyapatite synthétique et nanopoudre contenant une nanoplaque d'hydroxyapatite synthétique

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2216304C2 (ru) * 2002-05-15 2003-11-20 Общество с ограниченной ответственностью "Олимп" Способ местного лечения гиперестезии зубов при пародонтите и пародонтозе
US20080206554A1 (en) * 2005-01-04 2008-08-28 Rutgers, The State University Hydroxyapatite With Controllable Size And Morphology
DE102010063720A1 (de) * 2010-12-21 2011-06-16 Lr Health & Beauty Systems Gmbh Silberhaltige Zahnpflegezusammensetzung
WO2014162167A1 (fr) * 2013-03-30 2014-10-09 Instytut Wysokich Cisnien Polskiej Akademii Nauk Procédé de production de nanoplaques d'hydroxyapatite synthétique et nanopoudre contenant une nanoplaque d'hydroxyapatite synthétique

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
"Toothpastes", vol. 23, 2013, article "Monographs in Oral Science"
DATABASE GNPD [online] MINTEL; 1 January 2016 (2016-01-01), "Sensitive Toothpaste", XP002773886, Database accession no. 3727681 *
J. M. TEN CATE: "Contemporary perspective on the use of fluoride products in caries prevention", BRITISH DENTAL JOURNAL, vol. 214, no. 4, 23 February 2013 (2013-02-23), pages 161 - 167
J. M. TEN CATE: "The Need for Antibacterial Approaches to Improve Caries Control", ADV DENT RES, vol. 21, no. 8-12, August 2009 (2009-08-01), pages 8 - 12

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022152347A1 (fr) 2021-01-15 2022-07-21 Dr. Kurt Wolff Gmbh & Co. Kg Produit d'hygiène dentaire
DE102021100811A1 (de) 2021-01-15 2022-07-21 Dr. Kurt Wolff Gmbh & Co. Kg Mundpflegemittel, insbesondere Zahnpasta
DE102021111354A1 (de) 2021-05-03 2022-11-03 Dr. Kurt Wolff Gmbh & Co. Kg Mundpflegemittel
WO2022233361A1 (fr) 2021-05-03 2022-11-10 Dr. Kurt Wolff Gmbh & Co. Kg Agent de soin buccal

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