WO2010131994A1 - Medicament destine a la prevention des maladies bucco-dentaires - Google Patents

Medicament destine a la prevention des maladies bucco-dentaires Download PDF

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Publication number
WO2010131994A1
WO2010131994A1 PCT/RU2010/000130 RU2010000130W WO2010131994A1 WO 2010131994 A1 WO2010131994 A1 WO 2010131994A1 RU 2010000130 W RU2010000130 W RU 2010000130W WO 2010131994 A1 WO2010131994 A1 WO 2010131994A1
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WO
WIPO (PCT)
Prior art keywords
weight
medicine according
magnesium
selected out
prophylaxis
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/RU2010/000130
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English (en)
Inventor
Tamazi Omarovich Manasherov
Svetlana Konstantinovna Matelo
Tat'yana Vladimirovna Kupets
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
OBSHCHESTVO S OGRANICHENNOJ OTVETSTVENNOST'YU "WDS"
Original Assignee
OBSHCHESTVO S OGRANICHENNOJ OTVETSTVENNOST'YU "WDS"
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 OBSHCHESTVO S OGRANICHENNOJ OTVETSTVENNOST'YU "WDS" filed Critical OBSHCHESTVO S OGRANICHENNOJ OTVETSTVENNOST'YU "WDS"
Priority to UAA201014577U priority Critical patent/UA75461U/uk
Priority to EP10775155A priority patent/EP2429558A4/fr
Publication of WO2010131994A1 publication Critical patent/WO2010131994A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/14—Alkali metal chlorides; Alkaline earth metal chlorides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/42—Phosphorus; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/02—Algae
    • A61K36/03—Phaeophycota or phaeophyta (brown algae), e.g. Fucus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/484—Glycyrrhiza (licorice)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9706—Algae
    • A61K8/9711—Phaeophycota or Phaeophyta [brown algae], e.g. Fucus
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9755—Gymnosperms [Coniferophyta]
    • A61K8/9761—Cupressaceae [Cypress family], e.g. juniper or cypress
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9755—Gymnosperms [Coniferophyta]
    • A61K8/9767—Pinaceae [Pine family], e.g. pine or cedar
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • 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
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9794—Liliopsida [monocotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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 invention relates to therapeutic and prophylactic formulations for oral care utilized in stomatology, particularly to medicine for dental diseases prophylaxis wherein biologically active agents of natural origin are used.
  • tooth paste sold under "Parodontax” brand. It consists of baking soda and a blend of natural ingredients, flavor, sodium fluoride. As natural ingredients it contains a blend of alcohol extracts and oils of echinacea, myrrh, chamomile, rhatany, sage (US 2002/0031481 Al, IPC 7 A61K 7/16, 2002).
  • the known formulation has considerable concentration of baking soda as abrasive, more than 40% by weight that creates hypertonic medium and may result in gingival sponginess and recession. Therefore this tooth paste cannot be viewed as a means for permanent everyday dental and gingival prophylactic care. Moreover the known formulation does not provide necessary hard teeth tissues mineralization.
  • Technical result of the invention is achieved by practical use of effective formulation containing accessible components based on biologically active agents of natural origin, which has a comprehensive effect on dental tissues and can be recommended for periodontium prophylaxis and treatment as well as caries and non-carious affections prophylaxis.
  • the main purpose of this invention was to elaborate high-efficiency formulation for prophylaxis of dental diseases of teeth and soft tissues of oral cavity in which synergist medications could heighten effect of each other attaining high therapeutic effect and results mentioned above.
  • Technical result is enhanced by medicine for dental diseases prophylaxis containing orally acceptable active and inert components.
  • Active components about 0.3% to 2.2% by weight of lipid concentrate of kelp, 0.5% to 5.0 % by weight of kelp salt, 0.5% to 4.0 % by weight of dry extract of liquorice root, 0.01% to 0.25 % by weight of one or more essential oils to enhance organoleptic properties, and 0.1% to 3.5 % by weight of anticaries mineral adjunct. Inert components content is up to 100% by weight.
  • the medicine contains about 0.5% to 1.8% by weight of lipid concentrate of kelp, 0.8% to 4.2 % by weight of kelp salt, 0.8% to 3.6 % by weight of dry extract of liquorice root, 0.03% to 0.22 % by weight of one or more essential oils.
  • essential oils used to improve organoleptic properties
  • essential oils chosen out of the group including anise, thyme, lemon, mandarin, grapefruit, orange, bergamot, nerol, sage, tea tree, manuka, eucalyptus, fir, pine, juniper.
  • Literal sources indicate to great value of biologically active agents contained in various species of kelp. There is shown particular perspective to extract lipid fractions out of laminaria of northern and far eastern seas. (Study and use of therapeutic and prophylactic medicine based on natural biologically active agents / edited by V.G. Bespalov and V.B. Nekrasova. - Spb.: Eskulap, 2000. - pp.175-176).
  • Lipid fractions are extracted in the following way regardless of seaweed species specificity: biologically active agents are ethanol extracted or highly volatile diluent extracted out of dry seaweed, then lipid concentrate and aqueous extract are skimmed.
  • Essential biologically active components of lipid concentrate chlorophyll derivatives, carotinoids (beta-carotine), mannitol, polysaccharides, fatty acids, including essential acids (polyunsaturated acids Cl 8 and C20 omega-3 and omega-6 are most prevalent fatty acids), organically associated phosphor and iodine, sulphur amino acids.
  • seaweed accumulates actively many elements and concentrates various macro-and microelements. While kelp processing there are derived inorganic salts. Biological properties of these compounds are determined by such elements as calcium, iodine, potassium, magnesium, manganese, molybdenium, copper, cobalt, ferrum, germanium, selenium, zink, etc.
  • prophylaxis intensify metabolic processes, improve trophism and blood circulation in periodontal tissues that reduces alveolar bones atrophy, contributes to nonspecific resistance increase.
  • Liquorice root extract has been used for thousands of years as a medicine. Medical opportunities are determined by chemical formulation. Liquorice root contains about 6% to 23% of triterpene saponoside glycyrrhizin, blended potassium-calcium-magnesium salt of glycyrrhizinic acid, derivatives of glycyrrhizinic acid, such as glabric acid, 18-glycyrrhetic, 18,19 - dihydroglycyrrhetic, 11-deoxyglycyrrhetic acids, liquiritic acid; up to 4% of flavonoids: liquiritin, isoliquiritin, licurazid, neoliquiritin, glabroside, uraloside, liquiritoside, glabrol, quercetin, kaempferol, apigenin,; mono- and disaccharides (up to 20%); starch (up to 34%); pectins
  • flavonoids are also active in relation to clarithromycins and amoxycillins resistant strains of Helicobacter pylori (Fukai T., Marumo A., Kaitou K., et al. Anti- Helicobacter pylori flavonoids from licorice extract. Life Sci. 2002 Aug 9;71(12):1449-63.).
  • flavonoids derived from liquorice demonstrated antimicrobial activity against methycillin resistant strains of Staphylococcus aureus with minimum inhibitory concentrations of 3.13 to 12.5 ⁇ g/ml.
  • Flavonois glabren, isolicoflavon, isolicoflavonol showed activity in relation to these strains in concentration of 1.56 to 25.0 ⁇ g/1.
  • Liquorice root extract is used not only in the form of medicine but also for preparing halva and licorice sweets in food industry which makes it attractive as a means for oral hygiene.
  • Lipid concentrate of kelp has offending scent that is negatively commented by some consumers.
  • it has been proposed to introduce one or several ether oils into tooth pastes formulation in order to mask offending scent.
  • ether oils anise, thyme, lemon, mandarin, grapefruit, bergamot, nerol, sage, tea tree, manuka, eucalyptus, fir, pine, juniper.
  • Liquorice extract also has a positive effect on tooth paste flavor.
  • Ether oils coupled with liquorice extract perform a number of antimicrobial functions.
  • Concept of remineralization is part of ideology of the formulation invented.
  • Remineralizing system is a combination of ingredients saturating enamel of healthy teeth with minerals and initial cariogenic damage centres.
  • the formulation contains anticaries mineral additive.
  • anticaries mineral adjunct content is 0.2-3.3% by weight.
  • calcium glycerophosphate and magnesium inorganic and organic salt are preferable to use as anticaries mineral adjuncts.
  • inorganic or organic magnesium salts there may be used salts incorporating magnesium chloride, magnesium sulfate, magnesium nitrate, magnesium citrate, magnesium lactate, magnesium glycerophosphate, magnesium acetate, magnesium ascorbyl phosphate.
  • This adjunct is conditioned by teeth need for these elements in cases of caries and non-carious affections.
  • Calcium and phosphor are basic building elements of teeth enamel and take part in metabolic processes through the whole human life.
  • Non-carious teeth affections are often connected with calcium metabolic imbalance and are caused by adverse influence of endogeneous character like thyroid, pancreal, germ glands abnormalities, gastrointestinal tract diseases etc.; by unfavourable external influence such as ionizing radiation, daily long (more that 6 hours) computer work; by hazard influence such as acid fumes, metal dust and their combinations; a range of negative ecological effects, which result in substantial reduction of mineral components in dental tissues and then in affection in the form of caries, erosion defects.
  • Calcium glycerophosphate is a source of active phosphorus and calcium supply to teeth and periodontium tissues and facilitates process of mineralization, improves anticaries effect of formulation, intensifies anabolic processes in tissues.
  • Magnesium (of inorganic or organic salts) is a structural component of teeth. Magnesium is incorporated in complex formulation as microelement, which is a cofactor for phosphatases ensuring incorporation of phosphates into hard teeth tissues. Under the influence of phosphates there takes place hydrolysis of glycerophosphate and its bioavailability increases correspondingly. Since the risk of teeth demineralization is substantially lower in absence of solid dental deposit it is probable that formulation does not involve fluorides.
  • Fluoride content in mouth care formulation is relevant if soft dental deposit produces organic acids during breakdown of easy-fermented carbohydrates.
  • local fluoride action cannot be traced on teeth enamel maturation (for people aging over 20) even under this condition. It is shown in loss of its efficiency in caries prophylaxis.
  • sodium monofluorphosphate potassium monofluorphosphate, calcium monofluorphosphate or magnesium monofluorphosphate in amount of 0.6-1.8 wt %.
  • abrasive - 10-38 abrasive - 10-38
  • humectant - 11-50 gelling agent - 0.5-7
  • surfactant - 0.5-3 at least one surfactant - 0.5-2
  • humectant of a tooth paste there can be used one or several agents selected out of the group including sorbitol, glycerine, polyethylene glycol, propylene glycol.
  • gelling agent of a tooth paste there can be used one or several agents selected out of the group including hydroxyethyl cellulose,xanthan gum, guar gum, carbossimethyl callulose, potassium alginate, sodium alginate, thickening silica.
  • surfactants as sodium lauryl sulfate, alkylamidobetaine, polysorbate-20, sodium lauryl sarcosinate.
  • ether oils of peppermint oil, spearmint oil, clove, skinleaf and ginger oils as well as menthol, carvone, anethol, eucalyptol, methyl salicylate
  • sweeteners such as sodium saccharinate, potassium aspartame, potassium acesulfame, stevioside, xylitol, potassium and sodium glycyrrhizate.
  • preservative there can be used one or several substances selected out of the group including methylparaben, propylparaben, and their sodium salts, phenoxyethanol, benzoic acid, sodium benzoate, potassium sorbate.
  • Tooth pastes are prepared in the following way. Weigh required glycerine quantity, then add xanthan gum. Mix till formation of homogeneous mass. Weigh required quantity of water in a measuring bin, feed it into a mixer, with further adding of stevioside, sodium benzoate, sorbitol, kelp salt, sodium monofluorphosphate (as shown in examples 4,5), magnesium chloride (as shown in examples 1,2,3). Mix to formation of transparent solution. Xanthan gum suspension in glycerine is charged into the solution obtained, and mixing continues to formation of homogeneous mass. Vacuumize the formulation and mix for 10 minutes to full deaeration of the mixture.
  • the gel prepared is placed into polymer containers for filling.
  • Mouth rinses are prepared in the following way: Weigh water required, heat it up to 80 0 C, add glycerine, sorbitol (as in examples 3,4,5), xylitol, benzoic acid, magnesium glycerophosphate (examples 1,2), magnesium sulfate (examples 2,3,4,5), calcium glycerophosphate, magnesium monofluorphosphate (examples 1,2,3) and kelp salt. Mix to formation of transparent solution and cool down to the temperature of 40 0 C. In the process of mixing add dry liquorice root extract into the solution.
  • the mouth rinse prepared is placed into polymer containers. Efficacy evaluation
  • tooth paste according to example 3 from Table 1 has shown 69.5% reduction.
  • "Parodontax" application has shown 68.3% reduction.
  • gingivitis index in formulation prepared in accordance with the invention has shown more clear-cut reduction.
  • the invention can be prepared in the form of tooth paste as well as in the form of gel or liquid (mouth rinse, mouthwash) which are also under legal protection which covers all cases of realization of medicine for dental diseases prophylaxis.

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Abstract

L'invention concerne l'utilisation pratique d'une préparation efficace contenant des composants accessibles à base d'agents biologiquement actifs d'origine naturelle. Cette préparation a un effet global sur les tissus dentaires et peut être recommandée dans la prévention et le traitement des affections du parodonte, ainsi que dans la prévention des affections carieuses et non carieuses. L'objet principal de l'invention est l'élaboration d'une préparation à haute efficacité utilisée dans la prévention des maladies des dents et des tissus mous de la cavité buccale, les médicaments synergistes contenus dans cette préparation pouvant renforcer leurs effets mutuels, ce qui permet d'obtenir des résultats et des effets thérapeutiques élevés. Le médicament selon l'invention contient des composants actifs et inertes adaptés à la voie orale. Sont utilisés comme composants actifs : environ 0,3% à 2,2% en poids de concentré lipidique de varech ; de 0,5 % à 5,0 % en poids de sel de varech ; de 0,5% à 4,0 % en poids d'extrait sec de racine de réglisse ; de 0,01% à 0,25% en poids d'au moins une huile essentielle destinée à renforcer les propriétés organoleptiques ; et de 0,1% à 3,5 % en poids d'adjuvant minéral anticaries.
PCT/RU2010/000130 2009-05-15 2010-03-23 Medicament destine a la prevention des maladies bucco-dentaires Ceased WO2010131994A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
UAA201014577U UA75461U (uk) 2009-05-15 2010-03-23 Засіб для профілактики стоматологічних захворювань
EP10775155A EP2429558A4 (fr) 2009-05-15 2010-03-23 Medicament destine a la prevention des maladies bucco-dentaires

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EA200900764 2009-05-15
EA200900764A EA013370B1 (ru) 2009-05-15 2009-05-15 Средство для профилактики стоматологических заболеваний

Publications (1)

Publication Number Publication Date
WO2010131994A1 true WO2010131994A1 (fr) 2010-11-18

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PCT/RU2010/000130 Ceased WO2010131994A1 (fr) 2009-05-15 2010-03-23 Medicament destine a la prevention des maladies bucco-dentaires

Country Status (4)

Country Link
EP (1) EP2429558A4 (fr)
EA (1) EA013370B1 (fr)
UA (1) UA75461U (fr)
WO (1) WO2010131994A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017089595A1 (fr) * 2015-11-26 2017-06-01 Fontus Health Ltd Solution comprenant de l'acide glycérophosphorique et son sel magnésium
WO2019118452A1 (fr) * 2017-12-15 2019-06-20 Colgate-Palmolive Company Nouveaux composés

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RU2016100976A (ru) 2013-06-18 2017-07-19 ЭлДжи ХАУСХОЛД ЭНД ХЕЛТ КЭР ЛТД. Композиция для ухода за полостью рта
RU2691410C1 (ru) * 2018-04-26 2019-06-13 Федеральное государственное бюджетное учреждение науки "Институт морских биологических исследований имени А.О. Ковалевского РАН" Средство для ухода за полостью рта и горла
LV15495A (lv) * 2018-11-09 2020-05-20 Gerčikovs Iļja Līdzeklis mutes dobuma kopšanai
RU2699560C1 (ru) * 2019-04-09 2019-09-06 Федеральное государственное бюджетное образовательное учреждение высшего образования "Астраханский государственный медицинский университет" Министерства здравоохранения Российской Федерации (ФГБОУ ВО Астраханский ГМУ Минздрава России) Стоматологический гель с фитопелоидной композицией
RU2706010C1 (ru) * 2019-04-17 2019-11-13 Общество с ограниченной ответственностью "АЛЬФА-ДЕНТ" Гель стоматологический

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EP2429558A1 (fr) 2012-03-21
EA013370B1 (ru) 2010-04-30

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