Anti-inflammatory dental care agents

Details Anti-inflammatory dental care agents Anti-inflammatory dental care agents

2001-04-06

2002-12-10

Rose, Shep K. (Department: 1614)

Drug, bio-affecting and body treating compositions

Dentifrices

Reexamination Certificate

active

06491899

ABSTRACT:

FIELD OF THE INVENTION
This invention relates to dental care and cleaning preparations which counteract inflammation of the gums (gingivitis) through a special combination of active ingredients.
BACKGROUND OF THE INVENTION
Dental care preparations are primarily intended to remove food residues, discoloration and firmly adhering bacterial films from the surface of the teeth. In addition, attempts have been made to counteract diseases of the teeth and gums such as, for example, caries, gingivitis and parodontosis by incorporating special additives, for example fluorine compounds or antimicrobial agents, in dental care preparations.
A particularly stubborn disease which, unless successfully treated, can lead to the loosening and loss of teeth is periodontitis which, in its initial stages, is manifested in inflammation and bleeding of the gums (gingivitis). It is caused by bacteria which colonise the dental pockets and which are difficult to control by mechanical cleaning of the teeth with a toothbrush.
Attempts have been made to counteract inflammation of the gums by addition of antibacterial agents to toothpastes and mouthwashes. In most cases, however, conclusive results cannot be obtained in this way. Although certain non-cationic bactericidal agents, particularly from the group of chlorinated diphenylethers, have proved to be particularly effective, these compounds are not able on their own effectively to combat persistent inflammation of the gums.
A process for treating the periodontal tissue with a pharmaceutical composition containing a vitamin A derivative is known from U.S. Pat. No. 5,188,817. Toothpastes containing vitamin A have also been commercially available for some time (Aronal®).
It has now been found that the anti-inflammatory properties of, in particular, toothpastes already containing an antibacterial component can be significantly improved by addition of a combination of a panthenol or pantothenate and a retinol or retinol derivative.
SUMMARY OF THE INVENTION
Accordingly, the present invention relates to a dental care preparation with anti-inflammatory properties containing polishing components, fluorine compounds, humectants, binders, a water-insoluble non-cationic bactericidal component and water, characterized in that it contains a combination of panthenol or a salt of pantothenic acid and retinol or a retinol derivative to improve it anti-inflammatory properties.
DETAILED DESCRIPTION OF THE INVENTION
Dental care preparations in the context of the present invention are tooth powders, toothpastes, liquid tooth creams and tooth gels. Tooth. pastes and liquid tooth cleaning preparations are particularly suitable.
Suitable polishing components are, in principle, any of the known toothpaste abrasives, more particularly those which do not contain any calcium ions. Accordingly, particularly suitable polishing components are silicas, aluminium hydroxide, aluminium oxide, sodium aluminium silicates, organic polymers and mixtures of these abrasives.
However, calcium-containing polishing components such as, for example, chalk, calcium pyrophosphate or dicalcium phosphate dihydrate may be present in quantities of up to 5% by weight.
The total content of polishing components is preferably in the range from 5 to 50% by weight, based on the dental care preparation.
Toothpastes and liquid dental cleaning preparations which contain silicas as polishing component are particularly preferred. Suitable silicas are, for example, silica gels, silica hydrogels and precipitated silicas. Silica gels are obtained by reacting sodium silicate solutions with strong aqueous mineral acids to form a hydrosol, ageing to form the hydrogel, washing and drying. If drying is carried out under moderate conditions to a water content of 15 to 35% by weight, the so-called silica hydrogels known, for example, from U.S. Pat. No. 4,153,680 are obtained. Drying to water contents below 15% by weight results in irreversible shrinkage of the previously loose structure of the hydrogel to the dense structural of the so-called xerogel. Silica xerogels are described, for example, in U.S. Pat. No. 3,538,230.
A second particularly suitable group of silica polishing agents are the precipitated silicas. Precipitated silicas are obtained by precipitation of silica from dilute alkali metal silicate solutions by addition of strong acids under conditions which preclude aggregation to the sol and gel. Suitable processes for the production of precipitated silicas are described, for example, in DE-OS 25 22 486 and in DE-OS 31 14 493. A particularly suitable precipitated silica is that produced in accordance with DE-OS 31 14 493 which has a BET surface of 15 to 110 m
2
/g, a particle size of 0.5 to 20 &mgr;m (at least 80% by weight of the primary particles should be below 5 &mgr;m in size) and a viscosity in the form of a 30% glycerin/water (1:1) dispersion of 30 to 60 Pa.s (20° C.) and which is used in a quantity of 10 to 20% by weight, based on the toothpaste. In addition, particularly suitable precipitated silicas of this type have rounded corners and edges and are commercially obtainable under the name of Sident® 12 DS (DEGUSSA).
Other precipitated silicas of this type are Sident 8 (DEGUSSA) and Sorbosil AC 39 (Crosfield Chemicals). These silicas are distinguished by a weaker thickening effect and a slightly larger mean particle size of 8 to 14 &mgr;m for a specific BET surface of 40 to 75 m
2
/g and are particularly suitable for liquid tooth creams. These should have a viscosity (25° C., shear rate D =10 s
−1
) of 10 to 100 Pa.s.
By contrast, toothpastes which have a far higher viscosity of more than 100 Pa.s (25° C., D=10 s
−1
) require a sufficiently high percentage content of silicas with a particle size of less than 5 &mgr;m, preferably at least 3% by weight of a silica with a particle size of 1 to 3 &mgr;m. Accordingly, besides the precipitated silicas mentioned, even finer so-called thickening silicas with a BET surface of 150 to 250 m
2
/g, for example the commercial products Sipernat 22 LS or Sipernat 320 DS, are preferably added to such toothpastes.
Another polishing component which may be present in a quantity of about 1 to 5% by weight is, for example, aluminium oxide in the form of lightly calcined alumina containing &ggr;- and &agr;-aluminium oxide. A suitable aluminium oxide such as this is commercially obtainable under the name of “Poliertonerde P10 feinst” (Giulini Chemie).
The dental care preparations according to the invention may contain sodium fluoride, zinc fluoride, tin(II) fluoride, amine fluoride or sodium monofluorophosphate, for example, as fluorine compounds. A quantity of 0.01 to 0.2% by weight fluorine in the form of the compounds mentioned should preferably be present.
Glycerin, sorbitol, xylitol, propylene glycol, polyethylene glycol or mixtures thereof may be used as humectants. The dental care preparations according to the invention preferably contain a mixture of glycerin, sorbitol and polyethylene glycol in a ratio by weight of 10:(8-12):(0.1-1) as humectant.
Suitable binders and consistency factors are, for example, natural and synthetic water-soluble polymers such as, for example, carrageen, tragacanth, guar, cellulose and nonionic derivatives thereof such as, for example, hydroxyethyl cellulose or methyl hydroxypropyl cellulose. Agar agar, xanthan gum, pectins, water-soluble carboxyvinyl polymers (for example Carbopol® types), polyvinyl alcohol, polyvinyl pyrrolidone and relatively high molecular weight polyethylene glycols (with molecular weights of 10
3
to 10
6
D) are also suitable as binders and thickeners.
Suitable non-cationic bactericidal components are, for example, phenols, resorcinols, bisphenols, salicylanilides and halogenated derivatives thereof, halogenated carbanilides and p-hydroxybenzoic acid esters. Particularly preferred antimicrobial components are halogenated diphenylethers, for example 2,4-dichloro-2′hydroxydiphenyl ether, 4,4′-dichloro-2′-hydroxydiphenyl ether, 2,4,4′-tribromo-2′-hydroxydiphenyl et

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