DE102004041333A1 - Tooth gel, useful for non-therapeutic treatment and bleaching of teeth, comprises peroxy compound (measured as hydrogen peroxide) and additionally trialkyl siloxy silicates (e.g. trimethylsiloxysilicate) - Google Patents

Abstract

Tooth gel (A) (with a pH of 4.5-6.5) comprises 5.5-7.5 wt.% of peroxy compound (I) (measured as hydrogen peroxide) and additionally 0.1-2 wt.% of trialkyl siloxy silicates (II).

Description

The The invention relates to a dental gel containing a peroxy compound, as well as a use of such a dental gel.

The Use of peroxy compounds, in particular of peroxides such as Hydrogen peroxide, as a bleaching agent for teeth has long been known. About that In addition, peroxy compounds are used for the treatment of dental diseases used. It is in the oral cavity through the interaction of hydrogen peroxide with tissues and salivary enzymes more elemental Oxygen in the form of small bubbles educated. Does the oxygen with chromophore substances in contact, which are located on the tooth surface or in the enamel are stored, so these substances are by the oxygen oxidized so that the Discolored substances become.

It However, it has proved difficult to esthetically or gel-formulate for dental purposes provide. This is especially due to the chemical behavior attributed to hydrogen peroxide, the decomposes on contact with water. However, water is in most make a necessary component of such a gel or such Paste.

Aqueous hydrogen peroxide-containing tooth gels are known from the prior art, which are cosmetically and chemically stable. EP 0 288 420 discloses an aqueous hydrogen peroxide dental gel containing a grafting agent based on a polyoxyethylene-polyoxypropylene block copolymer, a humectant, a nonionic surfactant and a flavoring agent, wherein the toothed gel should have a pH of between 4.6 and 6.0 ,

The Tooth gels are applied to the tooth surfaces. So that these at the point of application for a sufficiently long time to act on the tooth surface and penetrate the enamel, however, is sufficient Adhesion of the dental gel to the tooth surface required. It is off known in the art, the tooth gel by means of so-called Aufbißschienen or to fix plastic films on the surface of the teeth to be treated. This is however for Tooth gel, which the user himself, d. h, without the involvement of a dentist wants to apply, associated with great effort and also little otherwise comfortable. Although other known tooth gels do not require separate carrier like rails or foils, but are too tough to handle them in a simple way and manner, for example by means of a brush to apply. Otherwise are too sticky and therefore too tough Dental gels poorly dosed from a tube or similar storage container.

When Furthermore, the use of flavorings in tooth gels, which contain a peroxy compound proved. If the flavoring in contact with the peroxy compound, so does the flavor with the peroxy compound and loses its aroma properties.

task The invention is to the disadvantages of the prior art remove. It is intended in particular a stable, a peroxy compound containing dental gel, the improved properties and as a result has a higher flavor stability and at home Area comparatively easy to apply.

These The object is solved by the features of claims 1 and 22. Advantageous embodiments The inventions result from the features of claims 2 to 21 and 23.

According to the invention this is achieved by the tooth gel a trialkylsiloxysilicate, especially preferably contains a Trimethylsiloxysilicat. The content of the trialkylsiloxysilicate hanging in the gel of the intended duration of use and the other ingredients of the dental gel. In particular, the trialkylsiloxysilicate with further film images, for example combined with polyvinylpyrrolidone become.

To proviso According to a preferred embodiment of the invention, a dental gel is provided, from 5.5 to 7.5% by weight, calculated as hydrogen peroxide, of one pharmaceutically acceptable Contains peroxy compound, has a pH of 4.5 to 6.5, and further 0.1 to 2 wt .-% a trialkylsiloxysilicate.

information in weight percent (wt.%) here and in the following, Unless otherwise indicated, on the weight of the dental gel.

Preferably contains the dental gel 0.1 to 1% by weight of a trialkylsiloxysilicate, especially preferably 0.3% by weight of a trialkylsiloxysilicate. As already explained, is the trialkylsiloxysilicate preferably trimethylsiloxysilicate.

trimethylsiloxysilicate is a co-hydrolysis product of tetraalkoxysilane and trimethylethoxysilane. This product forms a three-dimensional network of polysilicic acid units, which are terminated with Trimethylsiliylgruppen, which may be a contains low levels of ethoxy and hydroxy functions. The mean molecular weight of the trimethylethoxysilane may be from the ratio of tetraalkoxysilane units be determined to the trimethylethoxysilane units. Preferably is this ratio is 0.5 to 1.0, more preferably 0.66. An example of a trimethylethoxysilane with a relationship of 0.66 is Wacker-Belsil TMS 803 from Wacker-Chemie GmbH, Munich, DE.

trimethylsiloxysilicate is a waterproof additive used as a film former and fixative can be. In a preferred embodiment, this is trimethylethoxysilane with a further film former, particularly preferably with polyvinylpyrrolidone combined. The proportion of polyvinylpyrrolidone in the dental gel should be 0.5 to 3 wt .-% amount. Polyvinylpyrrolidone is, for example, below the name PVP Luviskol 30 from BASF AG, Ludwigshafen, DE available.

The tooth gel according to the invention contains an effective amount of a pharmaceutically acceptable peroxy compound which 5.5 to 7.5 wt .-%, calculated as hydrogen peroxide.

wobei m_{Peroxyverbindung} der Anteil der Peroxyverbindung an dem Gewicht des Zahngels darstellt; M_{Peroxyverbindung} das Molekulargewicht der Peroxyverbindung darstellt;

der Anteil von Wasserstoffperoxid an dem Gewicht des Zahngels, wenn statt der Peroxyverbindung Wasserstoffperoxid in dem Zahngel verwendet werden würde;

das Molekulargewicht von Wasserstoffperoxid darstellt; und A die Anzahl der Peroxid-Ionen in der Peroxyverbindung darstellt.By the term "calculated as hydrogen peroxide" is meant that the number (A) of peroxide ions in the peroxygen compound is determined and each of these peroxide ions is considered as hydrogen peroxide to calculate the proportion of the peroxy compound on the dental gel. In the calculation, the peroxide ion is considered to be O 2- / 2, but it does not matter that the peroxide ion is actually present as an ion in the peroxy compound. This calculation of the proportion of a peroxygen compound can be carried out by multiplying the molecular weight of the peroxygen compound to be actually used in the dental gel by the desired amount of hydrogen peroxide on the weight of the dental gel, which must be between 5.5 and 7.5 is divided by the product of the molecular weight of hydrogen peroxide (34.01 g / mol) and the number of peroxide ions in the peroxy compound:

where m _{peroxy compound represents} the proportion of the peroxy compound to the weight of the dental gel; M _{peroxy compound represents} the molecular weight of the peroxy compound;

the amount of hydrogen peroxide on the weight of the dental gel, if instead of the peroxy compound hydrogen peroxide would be used in the dental gel;

represents the molecular weight of hydrogen peroxide; and A represents the number of peroxide ions in the peroxy compound.

entspricht, so muß der Gewichtsanteil von Natriumperoxid (m_{Peroxyverbindung}) an dem Zahngel 16,04 Gew.-% betragen. Demzufolge kann der Gewichtsanteil an Natriumperoxid in dem Zahngel 12,61 Gew.-% (entspricht 5,5 Gew.-% Wasserstoffpero xid) bis 17,19 Gew.-% (entspricht 7,5 Gew.-% Wasserstoffperoxid) betragen.If, for example, sodium peroxide (Na ₂ O ₂ , molecular weight 77.97 g / mol, A = 1) is to be used as the peroxy compound in a weight fraction which contains 7% by weight of hydrogen peroxide

corresponds to, the proportion by weight of sodium peroxide (m _{peroxy compound} ) on the dental gel must be 16.04 wt .-%. Accordingly, the proportion by weight of sodium peroxide in the dental gel may be 12.61% by weight (corresponding to 5.5% by weight of hydrogen peroxide) to 17.19% by weight (corresponding to 7.5% by weight of hydrogen peroxide).

entspricht, so muß der Gewichtsanteil von Natriumcarbonat-Peroxyhydrat (m_{Peroxyverbindung}) an dem Zahngel 18,47 Gew.-% betragen. Demzufolge kann der Gewichtsanteil von Natriumcarbonat-Peroxyhydrat in dem Zahngel 16,93 Gew.-% (entspricht 5,5 Gew.-% Wasserstoffperoxid) bis 23,08 Gew.-% (entspricht 7,5 Gew.-% Wasserstoffperoxid) betragen.If, for example sodium carbonate peroxyhydrate (2Na ₂ CO _3. 3H ₂ O _2, molecular weight 314, 01 g / mol, A = 3) are used as peroxy compound in a proportion by weight, of 6 wt .-% of hydrogen peroxide

corresponds to, the weight proportion of sodium carbonate peroxyhydrate (m _{peroxy compound} ) to the toothed gel must be 18.47 wt .-%. Accordingly, the weight ratio of sodium carbonate peroxyhydrate in the dental gel may be 16.93% by weight (corresponding to 5.5% by weight of hydrogen peroxide) to 23.08% by weight (corresponding to 7.5% by weight of hydrogen peroxide).

entspricht, so muß der Gewichtsanteil von Carbamidperoxid (m_{Peroxyverbindung}) an dem Zahngel 15, 21 Gew.-% betragen. Demzufolge kann der Gewichtsanteil von Carbamidperoxid in dem Zahngel 15,21 Gew.-% (entspricht 5,5 Gew.-% Wasserstoffperoxid) bis 20,75 Gew.-% (entspricht 7,5 Gew.-% Wasserstoffperoxid) betragen.If, on the other hand, carbamide peroxide (H ₂ N-CO-NH ₂ .H ₂ O ₂ , molecular weight 94.08 g / mol, A = 1) is to be used as the peroxy compound in a weight fraction which contains 5.5% by weight of hydrogen peroxide

corresponds to, the proportion by weight of carbamide peroxide (m _{peroxy compound} ) on the toothed gel must be 15, 21 wt .-%. Accordingly, the proportion by weight of carbamide peroxide in the dental gel may be 15.21% by weight (corresponding to 5.5 Wt .-% hydrogen peroxide) to 20.75 wt .-% (corresponding to 7.5 wt .-% hydrogen peroxide).

Becomes used as peroxygen hydrogen peroxide is one such Calculation, of course not mandatory. In this case, the tooth gel contains 5.5 to 7.5 Wt .-% hydrogen peroxide.

The Peroxy compound is preferably hydrogen peroxide, peroxides, Peroxycarbonates or mixtures of these Verbindun conditions selected. Stronger Preferably, the peroxy compound is hydrogen peroxide, carbamide peroxide, Sodium carbonate peroxyhydrate or mixtures of these selected. Most preferably, the peroxy compound is hydrogen peroxide.

hydrogen peroxide is usually as a 30 to 35% aqueous solution available. Becomes a 30 to 35% aqueous solution used to formulate the dental gel, its proportion is so selected that the effective amount of hydrogen peroxide between 5.5 to 7.5% by weight is. Preferably, the amount of hydrogen peroxide is chosen so that the effective Amount of hydrogen peroxide 7 wt .-% is.

Of the pH value of the dental gel according to the invention is between 4.5 and 6.5, preferably between 5 and 6. The pH can be accurately adjusted with a pH adjusting agent become. It is essential that the selected Means the stability and effectiveness of the peroxygen compound is not adversely affected. One suitable means for this is, for example, triethanolamine. Furthermore, the tooth gel according to the invention contain a pH buffer. Suitable buffers are phosphate buffers. Prefers For example, sodium and potassium phosphates are used as buffers. A special preferred buffer is pentakalium triphosphate.

The tooth gel according to the invention may contain one or more of the following additives: emulsion stabilizers, Emulsifiers, sweeteners, Humectants, antioxidants, buffers and adjusting agents of the pH. Likewise further additives may be included in the tooth gel. It is essential that the additives the stability and do not adversely affect the effectiveness of the peroxy compound and, just like all other components of the dental gel, pharmaceutical compatible are.

• – 5,5 bis 7,5 Gew.-% einer Peroxyverbindung, berechnet als Wasserstoffperoxid;
• – 0,1 bis 2 Gew.-% zumindest eines Trialkylsiloxysilicats;
• – 0,5 bis 3 Gew.-% zumindest eines Filmbildners, der kein Trialkylsiloxysilicat ist;
• – 0,1 bis 2 Gew.-% zumindest eines Aromastoffes;
• – bis zu 1 Gew.-% zumindest eines Süßstoffes;
• – 20 bis 40 Gew.-% zumindest eines Feuchthaltemittels;
• – 0,1 bis 3 Gew.-% zumindest eines Antioxidationsmittels;
• – bis zu 3 Gew.-% eines Puffers;
• – 0,5 bis 3 Gew.-% zumindest eines Mittels zur Einstellung des pH-Wertes;
• – 1,5 bis 3 Gew.-% zumindest eines Emulsionsstabilisators;
• – 1 bis 5 Gew.-% zumindest eines Emulgators;
• – 5 bis 60 Gew.-% Wasser; und
• – 15 bis 30 Gew.-% zumindest eines Alkohols.

In a preferred embodiment, the tooth gel contains

• From 5.5% to 7.5% by weight of a peroxy compound, calculated as hydrogen peroxide;
• 0.1 to 2% by weight of at least one trialkylsiloxysilicate;
• From 0.5% to 3% by weight of at least one film former which is not a trialkylsiloxysilicate;
• 0.1 to 2% by weight of at least one flavoring agent;
• - up to 1% by weight of at least one sweetener;
• 20 to 40% by weight of at least one humectant;
• 0.1 to 3% by weight of at least one antioxidant;
• Up to 3% by weight of a buffer;
• - 0.5 to 3 wt .-% of at least one means for adjusting the pH;
• 1.5 to 3% by weight of at least one emulsion stabilizer;
• From 1 to 5% by weight of at least one emulsifier;
• 5 to 60% by weight of water; and
• - 15 to 30 wt .-% of at least one alcohol.

The Shares are to be chosen in this way that yourself total 100 wt .-% result.

Of the Alcohol is preferably ethanol.

suitable Flavorings are, for example, spearmint, peppermint, sage, Eucalyptus and menthol. Preferably, as a flavoring spearmint, particularly preferably spray-dried Mint used.

When Sweetener is Sodium saccharin used. Alternatively, aspartame or xylitol can be used become.

Suitable humectants are glycerol, polyethylene glycols or mixtures of glycerine and at least one polyethylene glycol. Polyethylene glycols are water-soluble linear polymers formed by an addition reaction of ethylene oxide. The general formula for polyethylene glycol is H- (OCH ₂ CH ₂ ) _n -OH where n represents the average number of repeating units.

preferred Humectants are PEG 2M and PEG 12, where 12 is the number for the average number of repeat units.

When Antioxidant is preferably butylhydroxytoluene used. Butylhydroxytoluene stabilizes the peroxy compound, so that this on exposure to heat not liquefied.

suitable Emulsion stabilizers are carbomers. A carbomer is a crosslinked one Acrylic acid polymer with a high molecular weight. It acts as a gelling agent. A suitable one Carbomer is Carbopol 980 F.

suitable Emulsifiers are polysorbates. A preferred polysorbate is polysorbate 20th

The tooth gel according to the invention is a stable formulation that has sufficient adhesion the tooth surface allows without carrier foils made of plastic or bite rails needed become. Allows the application with a brush. Adhesiveness or stickiness of the Tooth gel on the surface becomes determined by the addition of trialkylsiloxysilicate, wherein the starch and Duration of adhesion by the amount of trialkylsiloxysilicate that in the Tooth gel formulation is determined. The tooth gel can easily come out of one Tube are dosed.

The The invention will be described in greater detail below by means of an example.

• – 20 Gew.-% 35%iges wässeriges Wasserstoffperoxid;
• – 0,3 Gew.-% Trimethylsiloxysilicat;
• – 1,5 Gew.-% Polyvinylpyrrolidon PVP Luviskol K 30;
• – 0,5 Gew.-% sprühgetrocknete Minze;
• – 0,15 Gew.-% Natriumsaccharin;
• – 10 Gew.-% 86,5%ig wässeriges Glycerin;
• – 10 Gew.-% PEG 12;
• – 0,15 Gew.-% Butylhydroxytoluol;
• – 1 Gew.-% Triethanolamin;
• – 10 Gew.-% PEG 2M
• – 1,8 Gew.-% Carbopol 980 F;
• – 0,5 Gew.-% Pentakaliumtriphosphat;
• – 3 Gew.-% Polysorbat 20 TEGO SML 20;
• – 23,6 Gew.-% entionisiertes Wasser; und
• – 17,5 Gew.-% Ethanol.

A formulation with the following composition was prepared:

• 20% by weight of 35% aqueous hydrogen peroxide;
• - 0.3 wt .-% trimethylsiloxysilicate;
• 1.5% by weight of polyvinylpyrrolidone PVP Luviskol K 30;
• 0.5 wt.% Spray-dried mint;
• 0.15% by weight of sodium saccharin;
• 10% by weight of 86.5% aqueous glycerol;
• 10% by weight of PEG 12;
• 0.15% by weight of butylhydroxytoluene;
• 1% by weight of triethanolamine;
• - 10 wt .-% PEG 2M
• 1.8% by weight Carbopol 980 F;
• 0.5% by weight of pentakalium triphosphate;
• 3% by weight polysorbate 20 TEGO SML 20;
• 23.6% by weight of deionized water; and
• 17.5% by weight of ethanol.

The Formulation was prepared as follows: First, a mixture of the deionized water, Carbopol 980 F and ethanol, with polysorbate 20 denatured was made. Glycerol (glycerol DAB 10), PEG 12 and PEG 2M. The resulting mixture was then mixed with triethanolamine. Subsequently, it was spray-dried Mint, sodium saccharin, Luviskol K 30 and pentakalium triphosphate and butylhydroxytoluene (Vulkanox BHT). To the thus obtained Gel then became the 35% hydrogen peroxide and the trimethylsiloxy silicate added.

It became a stable, stiff, transparent gel with excellent storage stability. The pH was 5.3. The gel was applied with a brush the tooth surfaces Apply and stuck there more than 15 min without loss of mass. On contact the tooth gel with the lip settled partially detach the tooth gel. After the treatment time, the gel could be completely removed by rinsing with water become. The gel had a high chemical and cosmetic stability. Testing showed that the Content of active hydrogen peroxide (originally 7% by weight) after 30 months Residence time in a light-protected Packaging 6.5% by weight. Furthermore, excellent flavor stability was noted.

The Tooth gel was applied to the surfaces of human teeth (14 Days, twice a day, 15 min each) a significant bleaching effect. There was an average whitening of the tooth surface and Enamel achieved by 2 to 4 color grades according to the VITAPAN color scale.

Claims (23)

Tooth gel containing 5.5 to 7.5 wt .-%, calculated as hydrogen peroxide, of a peroxy compound and having a pH of 4.5 to 6.5, characterized in that it further comprises 0.1 to 2 wt .-% of a trialkylsiloxysilicate. Tooth gel according to claim 1, characterized that it Contains 0.2 to 1 wt .-% of a trialkylsiloxysilicate. Tooth gel according to claim 1 or claim 2, characterized characterized in that it Contains 0.3 wt .-% of a trialkylsiloxysilicate. Tooth gel according to one of the preceding claims, characterized characterized in that Trialkylsiloxysilicate is trimethylsiloxysilicate. Tooth gel according to one of the preceding claims, characterized characterized in that Peroxy compound of hydrogen peroxide, peroxides, peroxycarbonates or mixtures of these selected is. Tooth gel according to one of the preceding claims, characterized characterized in that Peroxy compound of hydrogen peroxide, carbamide peroxide, sodium carbonate peroxyhydrate or Mixtures of this is selected. Tooth gel according to one of the preceding claims, characterized characterized in that it furthermore film formers, emulsion stabilizers, emulsifiers, sweeteners, Humectants, antioxidants, buffers and / or agents for adjusting the pH. Tooth gel according to one of the preceding claims, characterized characterized in that it - 5.5 to 7.5% by weight of a peroxy compound, calculated as hydrogen peroxide; - 0.1 to 2% by weight of at least one trialkylsiloxysilicate; - 0.5 to 3 wt .-% of at least one film former, the no trialkylsiloxysilicate is; - 0.1 up to 2% by weight of at least one flavoring agent; - up to 1 wt .-% at least a sweetener; - 20 to 40 wt .-% of at least one humectant; - 0.1 to 3% by weight of at least one antioxidant; up to 3% by weight a buffer; - 0.5 up to 3% by weight of at least one pH adjusting agent; - 1.5 to 3% by weight of at least one emulsion stabilizer; - 1 to 5% by weight of at least one emulsifier; 5 to 60% by weight of water; and - 15 to 30 wt .-% of at least one alcohol contains. Tooth gel according to claim 7 or claim 8, characterized characterized in that it contains as a film former polyvinylpyrrolidone. Tooth gel according to one of claims 7 to 9, characterized that it as a flavoring contains mint. Tooth gel according to one of claims 7 to 10, characterized that it as sweetener sodium saccharin contains. Tooth gel according to one of claims 7 to 11, characterized that it as humectant glycerol, at least one polyethylene glycol or mixtures of glycerin and at least one polyethylene glycol contains. Tooth gel according to one of claims 7 to 12, characterized that it contains as antioxidant butylhydroxytoluene. Tooth gel according to one of claims 7 to 13, characterized that it as buffer contains pentakalium thiophosphate. Tooth gel according to one of claims 7 to 14, characterized that it contains triethanolamine as the pH adjusting agent. Tooth gel according to one of claims 7 to 15, characterized that it as emulsion stabilizer contains a carbomer. Tooth gel according to one of claims 7 to 16, characterized that it as emulsifier contains a polysorbate. Tooth gel according to one of the preceding claims, characterized characterized in that it 20% by weight 35% aqueous hydrogen peroxide; - 0.3 % By weight of trimethylsiloxysilicate; 1.5% by weight of polyvinylpyrrolidone; 0.5% by weight spray-dried Mint; - 0.15 Wt% sodium saccharin; - 10 Wt% glycerin 86.5%; - 20 % By weight of polyethylene glycols; 0.15% by weight of butylhydroxytoluene; - 1% by weight triethanolamine; - 1.8 Wt .-% carbomer; - 0.5 Wt% pentapotassium triphosphate; 3% by weight of a polysorbate; - 23.6% by weight Water; and - 17.5 % By weight of an alcohol contains. Tooth gel according to one of claims 12 to 18, characterized that the Polyethylene glycols PEG 12 and PEG 2M are. Tooth gel according to claim 19, characterized that PEG 12 and PEG 2M are contained in equal amounts in the dental gel. Tooth gel according to one of claims 17 to 21, characterized that this Polysorbate is polysorbate 20. Use of a dental gel according to one of the preceding claims for the non-therapeutic treatment of teeth. Use according to claim 22, characterized that this Dental gel used for bleaching teeth becomes.