DE1956016A1 - Preparation for dental and oral care - Google Patents

Description

BLENDAX - PLANTS
R. Schneider & Co.
Patent department

65 M a i η ζ

Dental and oral care preparation

The invention relates to a preparation for dental and oral care, the not only caries prophylactic and possibly remineralizing Has properties, but also on that Gums and the. Oral mucosa has a tissue-strengthening and vascular effect, stimulating blood circulation and thus counteracts bleeding gums.

The use of numerous fluorine compounds in dental care products serves to prevent caries and has undeniable successes brought. It is also known that inorganic and also organic phosphates remineralizing the tooth enamel works. Optimal results in terms of caries prophylaxis are obtained from the applicant according to a proposal Combination of fluorine compounds with mixtures of inorganic and organic phosphates achieved. Even the caries-inhibiting one The effectiveness of vitamins of the K complex, in particular of vitamin K_, has already been described by H. Schreiber, Medical Klinik 48/21, 747-8 (1953). Vitamin K, engages in the metabolism where there is the D-glyceraldehyde-3-phosphate dehydrogenase inhibits and thereby interrupts the breakdown of carbohydrates. Pantothenic acid and its derivatives, especially panthenol, have an anti-inflammatory effect through absorption in the mucous membranes regulating and just like rutin and its derivatives, which, after resorption in the tissue, condense the capillaries against blood leakage, counteracting the bleeding of the gums and exert a tissue-strengthening effect on the gums and the lining of the mouth.

It has now been found that a practically generally applicable Preparation for dental and oral care, which in addition to caries prophylactic and possibly remineralizing properties also have an excellent effect against bleeding gums as well as on the gums and the oral mucosa

109820/2066

Tissue-strengthening and vascular-effective, blood circulation-promoting Influence is obtained when one of such a preparation combinations of fluorine compounds and possibly Vitamins of the K complex and pantothenic acid and their derivatives, in particular PanthenoL, and / or rutin and its Derivatives, as well as, if appropriate, preferably water-soluble adding inorganic and / or organic phosphates.

In the context of the invention, practically all of them have been in dental care products so far fluorine compounds used, for example alkali fluorides such as ammonium fluoride, sodium fluoride, Potassium fluoride, lithium fluoride, tin fluoride, zinc fluoride, Zirconium fluoride, indium fluoride, copper fluoride, Nickel fluoride, palladium fluoride, complex-bound fluorine compounds such as alkali monofluorophosphates, alkali hexafluorophosphates, alkali fluorozirconates, tin fluorozirconate, fluorosilicates, Fluoroborates, fluorostannites, fluorogermanates, in particular Tin fluorogermanate, organic fluorine compounds such as amine hydrofluorides, alkanolamine hydrofluorides, quaternary ammonium fluorides and water-soluble addition products of amino acids with hydrogen fluoride or fluorides, It can also Mixtures of these and other fluorine compounds are used. Alkali monofluorophosphates such as Lithium, ammonium, sodium and potassium monofluorophosphate, preferably in an amount of 0.05 to 5.0% by weight of the total composition .

Vitamins of the K complex, which may be contained in the preparations according to the invention for dental and oral care, are 2-methyl-3-phythy 1-1,4-naphthoquinone (Vit. Κ _χ ), S-difarnesyl ^ -methyl-l ^ -naphthoquinone (Vit, K_), 2-methyl-1,4-naphthoquinone (Vit. K ₃ ), 2-methylnaphthalene _{-1,4-diol (Vit. K 4} ) and its esters, 4-araino-2- iaethyl-l-naphthol hydrochloride (Vit. K ₅ ), 2-methyl-1,4-naphthylenediamine (Vit. Kg), 4-amino-3-methyl-l-naphthol (Vit. K-) and their derivatives. Preference is given to using vitamin K ₃ , the anticarious effect of which, as already stated above, is known per se,

109820/2066

especially in the form of its sodium bisulfite, in amounts of 0.1 oil to about 5.0% by weight of the total composition.

Pantothenic acid and its derivatives, in particular panthenol, are expediently in an amount of 0 _? o 5 to 5, ο% by weight of the total composition. The proportion of rutin and its derivatives, in particular the sodium salt of rutin-sulfuric acid ester, is preferably about 0.1 to 5, ο% by weight of the total composition.

Optionally, in the dental and oral care products according to the invention preferably water-soluble inorganic and / or organic phosphates in amounts of about 0.01 to 10.0% by weight be included. Such phosphates are, for example, the various alkali and ammonium orthophosphates, water-soluble Alkali metaphosphates, water-soluble alkali polyphosphates, phosphates of polyhydric alcohols and sugar phosphates and their alkali and alkaline earth salts.

The preparations for dental and oral care can be used in any form of application, for example as pastes, solutions, Ointments, emulsions, powders, tablets, coated tablets or chewing gum. The pH value depends on the type and amount the active ingredients used.

Contain the preparations according to the invention for dental and oral care the other basic and auxiliary materials customary in such preparations. Toothpastes and tooth powders are usually used Polish added. Such polishing agents are, for example, insoluble alkali metal metaphosphates, calcium carbonates, calcium phosphates such as dicalcium phosphate or its dihydrate, tricalcium phosphate and calcium pyrophosphate, magnesium phosphates, Magnesium carbonate, aluminum oxide or its trihydrate, kaolin, Silicon dioxide, various silicates such as magnesium silicate and aluminum silicate, zirconates such as aluminum zirconate and

10982Ö / 2066

in particular powdered plastics, for example polystyrene, Polymethyl methacrylate, polyamides, polycarbonates, polyesters, urea-formaldehyde resins, melamine-formaldehyde resins and phenol-formaldehyde resins and mixtures of the substances listed with one another and with other known polishing agents.

Toothpastes usually contain binders and thickeners. Examples of such are polyacrylic acid and its Alkali salts, polyvinylpyrrolidone, carboxymethyl cellulose and their salts, pectin and alginic acid and its derivatives called.

In addition to glycerol and sorbitol, humectants are in particular various other polyalcohols, for example propanediol and / or butanediol.

Dentifrices and oral care products appropriately contain preservatives, in particular p-hydroxybenzoic acid esters and hexachlorophene, and surface-active substances, for example Alkylarylsulfonates, olefin sulfonates, fatty acid monoglyceride sulfates, higher alkyl sulfoacetates, higher fatty acid esters of dihydroxyalkanesulfonates such as 1,2-dihydroxypropanesulfonate, Fatty acid protein condensates, N-acylaminoalkanecarboxylic acids, in particular N-lauric isarcoside, and its alkali salts; nonionic Surface-active compounds such as alkylene oxide, especially ethylene oxide, condensation products, esters Fatty acids and sugars, amine oxides; cationic surfactants; amphoteric substances such as betaines, sulfobetaines, sulfatobetaines and long-chain ones N-alkylaminocarboxylic acids and compatible mixtures of the surface-active substances listed.

Finally, the preparation according to the invention for dental and oral care can also contain customary flavors and aromas such as Saccharin, sodium cyclamate, menthol, peppermint, wintergreen or eucalyptus oil, lower alcohols, optionally coloring and / or optical brighteners, complexing agents as well as other active ingredients, for example astringents and optionally also contain enzymes such as proteases, amylases and / or dextranases.

1098 20/20 66 -5-

The tooth and oral care products according to the invention are produced in the customary manner by mixing the starting materials and introducing the same into a carrier material,

Sodium monofluorophosphate 0.75% by weight

Vitamin K- (as sodium bisulfite) 0.25 "

Panthenol 0.2o "

Rutin (as the sodium salt of

Sulfuric acid ester) 0, lo "

Hexachlorophene 0.3o "

ethyl p-hydroxybenzoate 0.2o "

Glycerine, 86% 25, oo "'

Dicalcium phosphate dihydrate. 4θ, οο "

Aromas and flavors l, 2o "

N-lauroyl sarcoside, sodium salt l, oo "

Carboxymethyl cellulose 1.5 "

Water 29.5o "

§§I§Ei§i _ ?. l toothpaste

Sodium monofluorophosphate l, oo Weight% Vitamin K ₃ (as sodium bisulfite) O, 2o Il Panthenol 0.2o Il Rutin (as the sodium salt of Sulfuric acid ester) 0.2o Il Sodium dihydrogen phosphate 2, oo Il methyl p-hydroxybenzoate 0.3o Il Flavors and aromas l, lo Il Silicon dioxide (Aerosil ^R ) l, oo η Fatty alcohol sulfate, sodium salt l, 5o ti Sorbitol, 70% 20, oo η Glycerin, 8 6% strength ΙΟ, οο Il Dicalcium phosphate dihydrate 35, oo π Polyamide powder 5, oo ■ ι Carboxymethyl cellulose l, 5o π water 21, oo η

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-6-

Gel-shaped toothpaste

Sodium fluoride O, 5o Wt% Panthenol 0.2o Il Rutin (as the sodium base of Sulfuric acid ester) 0.15 Il Carbopol ^iR) 940 l, 5o η NaOH, 5% 8, oo Il Silica gel l, oo Il Sodium lauryl sulfate 3, oo ti Aromas and flavors l, 5o Il Hexachlorophene 0.15 η methyl p-hydroxybenzoate O, Io Il Ethanol l, 5o Il Sorbitol, 70% 10, OO ir water 72, 4o Il Example 4; Mouthwash

Sodium monofluorophosphate 1.3% by weight

Rutin (as the sodium salt of

Sulfuric acid ester) 0.2o "

Disodium Glycerophosphate 2.5o "

Potassium dihydrogen phosphate 1.2o "

Disodium hydrogen phosphate 1,3o "

Aromas and flavors lj-3o "

Cetylpyridinium chloride O, 2o "

Glycerine, 86% 8, oo "

Ethanol, 90% 40, oo "

Water 44, oo "

109 82Ö / 2066

ORIGINAi INSPECTED

Sodium monofluorophosphate 1.5% by weight

Vitamin K ₃ (-sodium bisulfite) O, 2o "

Panthenol O.2o "

Aromas and flavors l, lo "

Fatty alcohol sulfate, sodium salt l, 5o "

Sodium alginate I, 5o "

Polyethylene glycol (MW approx. 600) 1.5 o "

Carboxymethyl cellulose Ι, οο "

Calcium pyrophosphate 5.5ο "

insoluble Sodium metaphosphate 8.00 "

Dicalcium phosphate dihydrate 78.00 "

Sodium hexafluorophosphate (NaPF,) 0.8% by weight

Rutin (-sodium salt of

Sulfuric acid ester) 0.3o "

(R)
Syloid ^v 63 (silicon dioxide with

a particle size of 10 microns

and a surface area of 830 m / g) 15.00 "

Syloid ^(R) 244 (silicon dioxide with

a particle size of 3 microns

and a surface of 300 m ² / g) 5.00 "

Hydroxypropyl cellulose l, 2o "

Sorbitol, 70% '28.00 "

Glycerine, 86% 10.00 "

Aroma-u, flavorings l, 5o "

N-lauroyl sarcoside, sodium salt 1.90 "

Dye solution, green 0.3o "

p-Hydroxybeneoic acid methyl ester 0, lo "

p-Hydroxybenzoic acid propyl ester 0, lo "

Allantoin 0.8o "

Water 35.00 "

-8- 10982Ö "/ 2066

-Ir

Ethanolamine hydrofluoride panthenol

Bioprase ^ SP

(Protease from Bacillus subtilis) hexachlorophene bromochlorophene ethyl p-hydroxybenzoate, N-lauroyl sarcoside, sodium salt Lauryl dimethylamine oxide carboxymethyl cellulose sorbitol, 7O% Glycerine, 86% aroma and flavoring substances insoluble. Potassium metaphosphate

Polymethyl methacrylate (mean particle size about 1.5 microns)

Calcium pyrophosphate (mainly present in the ß-phase)

water

1 , OO Weight 0 »45 Il O , 55 π O , Io Il 0 , Io π 0 , Io Il 0 , 9o Il O , 80 η 1 , 5o Il 15th , 00 η IO , 00 II 1 , 5o H 7th , 00 Il 18th , 00 η. 15th , 00 π 28, oo

In a chewing gum mass of the usual composition were additionally

0.85 parts by weight of sodium monofluorophosphate, 0.25 "vitamin K ₃ (sodium bisulfite),

0.25 "panthenol,

0.3o "rutin (-sodium salt of sulfuric acid ester),

2, Io "sodium dihydrogen phosphate,

l, oo "dipotassium hydrogen phosphate and

2.5o "fructose-1,6-diphosphate

incorporated per 100 parts by weight of the total composition, intimately mixed, the mass rolled and cut into strips. A chewing gum is obtained which not only has caries prophylactic properties, but also affects the gums and the oral mucosa is a blood circulation-enhancing, tissue-strengthening Exerts influence and counteracts bleeding gums.

1Q982Ö72066

Claims (5)

Claims 1.) Preparation for dental and oral care with a content of fluorine compounds and possibly vitamins of the K complex, characterized in that it is additionally Rutin or its derivatives and / or pantothenic acid or its derivatives and, if appropriate, preferably water-soluble Contains phosphates. 2.) Preparation for dental and oral care according to claim 1, characterized in that it contains _{vitamin K 3 as a vitamin of the K complex.} 3.) preparation for dental and oral care according to claim 1 and / or 2, characterized in that it is panthenol contains. 4.) Preparation for dental and oral care according to one of the preceding Claims, characterized in that it contains an alkali monofluorophosphate as the fluorine compound. 5.) / Preparation for dental and oral care according to one of the preceding claims, characterized in that it is in the form of a toothpaste and O, o5 to 5, ο wt .-% of an alkali monofluorophosphate, O, oil to 5, ο wt. -% vitamin K ₃ in the form of sodium bisulfite, O, oil up to 5, ο wt .-% rutin in the form of the sodium salt of its sulfuric acid ester, 0, o5 to 5, o wt, -% panthenol and optionally 0, o5 to 10, o Contains wt .-% of one or more water-soluble phosphates. 10982 (^ / 2066