WO1981000513A1 - New compositions for detecting dental plaque - Google Patents

Abstract

New compositions for detecting and inhibiting dental plaque associating non-acid colourings and quaternary ammoniums or double ternary ammoniums. Application to dental hygiene and particularly to toothpastes.

Description

NEW COMPOSITIONS FOR REVELATION AND INHIBITION OF DENTAL PLATE

The present invention relates to new compositions for dental hygiene and treatment having, among other aims, that of revealing and treating dental plaque.

It should be remembered that a dental plaque denotes a film depositing on the surface of the teeth and which is interposed between the teeth and the oral environment. It is essentially made up of a layer of more or less denatured natural and salivary proteins, salivary mucin and various living or dead microorganisms. Physico-chemically, dental plaque has properties linked to its high protein content. This largely protein film therefore constitutes a barrier between the teeth and the buccal volume in which the free saliva is slightly acidic or substantially neutral (pH 5.6 to 7.6 most generally). It tends to be more acidic at rest than during the active period. However, in the absence of dental plaque, the teeth which, like the bones, are subject to demineralization, enter into an ionic exchange with saliva, an aqueous colloidal solution of mineral salts in the presence of mucin and endowed with enzymatic properties. . Dental plaque therefore completely or partially prevents these exchanges and constitutes a source of anomalies that can worsen over time. It plays above all a cariogenic role which is now well known (cf. for example: Dechaume and Brunel "Reflections on the prophylaxis of dental caries", Revue de Stomatologie, July and August 1956).

However, it is not easy for a non-specialist to measure the extent of dental plaque and therefore the dangers involved. The object of the present invention is therefore, when the user so desires, and in particular when he is washing his teeth, to allow him to see appear, thanks to a clear coloration, said dental plaque, coloration then easily eliminated by washing and / or conventional brushing generally carried out using toothpaste.

In the prior art, numerous dyes have been used to reveal dental plaque. The applicant here has himself already proposed various techniques but none provided a real solution to the double problem of detection and treatment.

However, if it was logical and within the reach of ordinary skill in the art to add, in the same composition, detector components and active treatment components, the applicant has found that remarkable exaltation and potentiation of the effects of constituents resulted from the synergy between certain families of bodies meeting a precise definition.

Apart from the elimination of plaque, it is therefore conceivable that it is either possible to use the compositions revealing dental plaque, in accordance with the invention, only, which requires subsequent elimination, or to use a unique composition including that according to the invention revealing dental plaque by coloring and the constituents of any conventional ifrice tooth. The latter solution being the simplest, we will insist on it in the examples which follow, without this limiting the scope of the invention. There is therefore addition or in certain combinations of revealing and toothpaste effects, in the case of these unique compositions.

The compositions according to the present invention therefore contain at least one body hereinafter called a developer which brings to the dental plaque a color which does not appear or appears differently on the other surfaces of the oral cavity. This staining of dental plaque can be obtained using any product which, in sufficient concentration, fixes physically, chemically and / or biologically, a layer, a film or particles, the time necessary for observation, and can then be easily removed. It is therefore important that the coloration be apparent during this observation, so that it can appear only at the time of contact between developer and dental plaque, by physical, chemical and / or biological interaction between the developers and one or more constituents of dental plaque. It will be noted in this regard, that certain coloring materials are already in use in traditional toothpaste products, but at concentrations insufficient to bring to dental plaque an appearance clearly contrasting with the neighboring surfaces, the role of these coloring agents of the prior art - priority being essentially of an order, if not aesthetic, at least commercial in the sense or understood by trademark law, that is to say as a distinctive sign without technical effect.

Furthermore, as already noted, the prior art has proposed numerous compositions revealing dental plaque including colorants in solutions of pastes often toothpaste, soluble tablets, chewing gum. But so far none has really allowed direct treatment. However, it is important to present compositions having the following properties:

- zero toxicity at the useful concentration

- good color contrast with the mucous membranes, prostheses, enamel, repairs and cracks, the coloring then being selectively fixed on the plate and its constituents

- fast coloring

- water solubility of dyes for rapid elimination after use.

- pleasant taste - good conservation

- bactericidal and inhibitory properties of plaque.

- indication of pH - reduction of surface tension

The applicant hereby has found that the combination of neutral or basic, non-toxic dyes or colored reagents, at the concentrations chosen for those skilled in the art, associated with inhibitors of dental plaque which will be defined below, gives excellent results. It is of course possible to add to these compositions now conventional constituents such as erythrbsin or iodine tincture which are dyes and can play a role in inhibiting plaque, but it has been observed, for example, that eryth throsin exerts antidextranase activity, which is troublesome due to the prophylactic role of dextranase which destroys the cariogenic dextrans of dental plaque. Iodine, on the other hand, seems to be able to play an inhibitory but weak role with respect to the compositions according to the present invention.

The applicant has found that certain ammoniums used in combination with neutral or basic colourants or reagents, give excellent results, superior to what could be expected from the simple addition of the properties of the various constituents.

It will be recalled that the technical field of the present invention being in most countries, subject to severe legislation, the latter eliminates toxic or dangerous components. To better understand the technical characteristics and advantages of the present invention, we will describe embodiments, it being understood that these are not limiting as to their mode of implementation and the applications that can be made of them. .

Example 1

A toothpaste is prepared on the basis of the following weight composition given as a percentage, with mention of the property generally considered to be the most characteristic. teristic in the context of the present invention:

• Sodium dihydroxyallantoînate 0,02 healing

. Neutral red 5 revealing

. 0.15 ammonia fluoride anticaries

. Cetylpyridinium chloride 0.50 inhibitor

. Boric acid 0.20 antiseptic

. chloroform (possibly) 2 anesthetic

. Sodium rinocleate 2 activity coadjuvant

. Nipagine (methyl parahydroxybenzoate) 0.08 preservative

. Nipasol (propyl parahydroxybenzoate) 0.07 preservative

. Glycerin (or propylene-glycol) 1 lubricant

. Aluminum hydroxide 3 abrasive agent

. Sodium saccharin 0.03 sweetener

. Mixture of silica 22 excipient

. Xylitol (or sorbitol) 20 excipient

. Essence of spearminth 0, 80 fragrance

. Menthol 0.05 perfun

. 0.50 titanium oxide whitening agent

. Laurane alcohol sulfane 2 coadjuvant. Water q.s. for 100

It will be noted that the quantity of neutral red indicated above is not limiting since satisfactory results can be obtained with contents between 0.1 and 10%. This composition can be prepared in the following manner, and this for one tonne of finished product: Ammonium fluoride and cetylpyridinium chloride are dissolved in 20 liters of purified water, which gives the solution below called solution A.

In another tank, 100 liters of purified water are dissolved and with electric stirring, the sodium rinocleatate, sodium saccharinate and sodium dihydroxyallantoinate, which gives the so-called solution B.

A sufficient quantity of purified water is introduced into a disperser with the mixture of silica, xylitol, oxy- of titanium and aluminum hydroxide. The mixture is allowed to homogenize. Solution B is then added by filtering and pumping, then boric acid, lauric alcohol sul fane and any chloroform. After a few minutes, solution A is added as well as the fragrance essences in which the preservatives have previously been dissolved. The apparatus is left to rotate until good homogeneity, then the neutral red is incorporated and it is turned until perfect homogeneity, that is to say for about thirty minutes. Then deaerated under vacuum for a quarter of an hour.

The paste thus obtained is crushed and stored in tanks for 48 hours.

This composition in accordance with the invention, like that given below, can be used as a toothpaste, the dental plaque being, in a first phase, directly colored, here essentially thanks to neutral red, the toothpaste acting in a second phase, removing the staining with all or part of the dental plaque. But in addition, neutral red indicates the pH (red at pH 6.8, yellow at 8.0) and allows the revelation and detection of plaque microorganisms. In addition, cetylpyridinium chloride associated with neutral red acts as an energetic inhibitor of plaque and dissolves mucins.

Examples 2 and 3

Example 1 is repeated, replacing cetylpyridinium chloride with chlorhexidine and neutral red (Basic Red 5 of the Color Index) with toluidine blue 0 (Basic blue 17 of the Color Index) or methyl violet (Basic Violet of color Index).

We obtain results as satisfactory as in Example 1 and in the case of methyl violet (Example 3) an enhanced action on the microorganisms of the plate. In the three examples, there are obtained revealing, inhibiting, toothpaste and, with certain dyes, indicating pH compositions. A conventional use of these various compositions in accordance with the invention in quantity and frequency equivalent to those of conventional toothpastes, did not reveal in the fifty subjects subjected to the experiment, phenomena appreciable on the various planes of the . oral toxicity, safety and tolerance.

But in all cases there has been observed, if not a total disappearance, at least a marked regression of dental plaque, at least in its least ancient forms. But in more than half of the cases, the result was completely satisfactory.

In all of the above, we have spoken of a physical chemical and / or biological reaction between developers and at least one of the constituents of dental plaque. It is obvious that the words reaction and react must be taken here in a broader sense than the classical chemical meaning, since the developers can be what are conventionally called in chemistry colored reagents, but more generally bodies which , already colored themselves or not colored, or otherwise colored will, in contact with the plate with at least one of the constituents of the plate, or thanks to its presence cause coloring at least on the surface of this plate. There is therefore generally an interaction between at least one of the developers and at least one of the constituents of dental plaque.

To the examples above we have given toothpaste compositions, but we can very well separate the roles and keep only the revealing and inhibitory part that we apply to the teeth to only involve a toothpaste. 'a posteriori, and eliminate the coloring while allowing the inhibitory action to be exerted.

Furthermore, it is obvious to those skilled in the art that, without departing from the scope of the present invention, several constituents of the various categories can be combined. It will also be noted that the fluorinated derivatives, in particular quaternary ammo-niums, are particularly active. With regard to ammoniums, the best results are obtained with quaternary ammoniums (cetylpyridinium chloride for example) or molecules having at least two ternary ammoniums (chlorhexidrine or chlorhexidrine gluconate for example).

Claims

1) Compositions for dental use comprising at least one developer of dental plaque, characterized in that at least one of the developers is non-acidic and that the compositions comprise at least one inhibitor of dental plaque. 2) Compositions according to claim 1, characterized in that at least one inhibitor is a quaternary ammonium or a double ternary ammonium. 3) Compositions according to one of the preceding claims, characterized in that one of the inhibitors is cetylpyridinium chloride. 4) Compositions according to one of the preceding claims, characterized in that one of the inhibitors is chlorhexidine. 5) Compositions according to one of the preceding claims, characterized in that one of the developers is neutral red. 6) Compositions according to one of the preceding claims, characterized in that one of the developers is toluidine blue O. 7) Compositions according to one of the preceding claims, characterized in that one of the developers is methyl violet. 8) Compositions according to one of the preceding claims, characterized in that at least one of the revealing constituents interacts with at least one of the constituents of dental plaque. 9) Compositions according to one of the preceding claims, characterized in that at least one of the revealing constituents interacts with at least one mucin. 10) Compositions according to one of the preceding claims, characterized in that at least one of the revealing constituents interacts with at least one of the microorganisms of dental plaque. 11) Compositions according to one of the preceding claims, characterized in that at least one of the constituents is a pH indicator.