RU2201202C2 - Tooth paste and filler for tooth pastes - Google Patents

Abstract

FIELD: treatment-and- prophylactic or hygienic cosmetics, particularly, tooth pastes and fillers for them. SUBSTANCE: tooth paste contains sorbitol, sodium carboxymethylcellulose or xanthane resin, polyethyleneglycol, sodium monofluorophosphate and/or sodium fluorite, sodium laurylsulfate, aromatizer, sweetener, color, biologically active additives, water and silicon- containing filler and/or chalk. Said filler is a microionized powder of silicon dioxide with abrasive properties having: filled density, not more 0.7 g/cu.cm; specific surface, no less 15 cu.m/g; moisture capacity, 0.9-1.3 cu. cm/g; and/or silicon dioxide with properties of thickening agent having: filled density, not more 0.3 g/cu.cm; specific surface, no less 80 cu.m/g; moisture capacity, 2.0-2.6 cu.cm/g. EFFECT: higher efficiency without injuries of enamel at prolonged application. 11 cl, 1 tbl, 7 n

Description

 The invention relates to the field of therapeutic and hygienic cosmetics and relates to preparations for the care of the oral cavity, namely toothpastes and fillers used to obtain them.

 Known toothpaste containing an enzyme, detergent, silica gel, glycerin, polyethylene glycol, preservative, perfume, color, saccharin and water (GB patent, 1296952, 1951).

 However, the known paste has a low bactericidal and cleansing properties.

Also known is the paste of the following composition in parts by weight:
Glycerin - 10.00
Carrageen - 0.75
70% sorbitol solution - 33.00
Propylene glycol - 0.50
Gantrez - 19.00
Water - 9.957
Sodium fluoride - 0.243
Saccharin - 0.30
Pyrophosphate - 2.00
Sodium hydroxide - 1.00
Silicon Polishing Agent (Zeodent 113) - 20.00
Silicon Thickening Agent (Sylodent 15) - 2.50
Fragrance - 0.95
Triclosan - 0.30
Sodium Lauryl Sulfate - 2.00
This paste is described in patent US 518578 And as an example of an oral composition with antibacterial, anti-raid and anticalculus action and can be indicated as the closest analogue.

 Known paste, although it has good cleansing and anti-inflammatory properties, does not provide a sufficient degree of enamel protection against abrasion during prolonged use.

 The purpose of the invention is the provision of high efficiency, safety during prolonged use.

This goal is achieved by the fact that a new paste and a new filler for its preparation are proposed. The proposed paste contains the following ingredients, indicated at a ratio in wt.%:
Sodium lauryl sulfate - 0.5 - 2
Sorbitol - 10 - 70
Sodium carboxymethyl cellulose or xanthan gum - 0.6 - 1.4
Polyethylene glycol - 1 - 5
Sweetener - 0.1 - 0.2
Dye - 0.002 - 1
Sodium Monofluorophosphate - 0.2 - 0.8
and / or sodium fluoride - 0.1 - 0.3
Fragrance (fragrance) - 0.6 - 1.2
Silicon dioxide - thickener - 2.0 - 17
and / or
Silicon dioxide and / or chalk - abrasive - 3 - 20
Water - Else
with a total silica content of 10.0 to 30.0.

 Along with the listed ingredients, various biologically active substances that provide anti-inflammatory, healing, anti-caries effects that improve metabolic processes in the periodontal tissues, such as allantoin in an amount of 0.5-2.0% triclosan in an amount of 0.05-, can be added to the paste. 0.30%, hydroxylapatite (hydroxyapatite) in an amount up to 2%, plant extracts in an amount of 0.05-6.00% and others.

 To prolong the action of active substances, gantrosis can be introduced mainly in an amount up to 0.25%.

 As a moisturizer, up to 20% glycerol is administered.

 As a sweetener, the paste may contain lactose, saccharin, sodium cyclamate, etc. Preferably, saccharin is added in an amount of 0.2%.

 As a colorant, the paste may contain, for example, titanium dioxide, preferably in an amount of 0.25% or color dye in an amount of 0.002-0.003%.

 As a fragrance, the paste may contain aromatic oils such as peppermint, lemon, eucalyptus, etc.

 In addition to the above ingredients, other targeted additives can be used, for example, soda in an amount of 3-5% in pastes with a whitening effect, in some cases a preservative. Pasta is prepared as follows.

 A solution of sodium lauryl sulfate in water is prepared (part of the prescription amount). Sorbitol and the remaining water are heated. A sweetener, sodium monofluorophosphate or sodium fluoride are introduced, as well as, if necessary, a preservative, sodium pyrophosphate, active substances. The mixture is mixed until the components are completely dissolved. Polyethylene glycol is added and, if necessary, glycerin, the resulting mixture is mixed. Then sodium carboxymethyl cellulose or xanthan gum (gum) is added and the mixture is mixed until a homogeneous gel is obtained, followed by cooling. Dye and silica and / or chalk abrasive are added and mixed for 10-15 minutes. Silicon dioxide, a thickener, is added and mixed for about 15 minutes until smooth. Perfume is introduced and stirred under vacuum for 2-5 minutes. Then sodium lauryl sulfate solution is added and stirring is carried out under vacuum for 10-15 minutes. The resulting paste has a good anti-inflammatory effect, does not irritate the mucous membrane, foam well and is harmless with prolonged use, does not erase tooth enamel.

 Improved rheological and thixotropic characteristics, the possibility of safe long-term use of the paste are provided by introducing abrasive and thickening grades of silicon dioxide (silica gels) obtained by us as a filler.

 A new filler, which is an abrasive and / or thickener, is also the subject of the present invention.

 At present, silicon compounds, including silicon dioxide in the form of a powder, are widely used as fillers for polymer, pharmaceutical, and cosmetic preparations. A review of the technical and patent literature showed that this filler should have specific properties: a loose structure with open porosity, low bulk density with low bulk density, high dispersion, moisture and oil absorption, particle sizes from about 2 to 30 microns.

 To obtain highly porous silica gel fillers, various methods are used in which the desired properties are ensured by a combination of optimal synthesis conditions and the nature of the precipitant. Methods differ in the properties of the resulting product, their reproducibility and the complexity of the hardware design.

 As a rule, silica gels are obtained by two methods, namely, through sol and through coagel. The methods include the steps of hydrolysis of the starting silicate, condensation of silicic acid, coagulation, drying.

 The most common are silica gels of the trademarks Zeodent 113, Sydent (abrasives) and Sylox 15 and Sylodent (thickeners) (US 5156835, US 5178851, US 5180578, etc.).

According to the invention, the filler with abrasive properties is an amorphous microionized silicon dioxide powder having a bulk density of 0.1-0.7 g / cm ³ , a specific surface area of at least 15 m ² / g and a moisture capacity of 0.9-3.0 cm ³ / g.

 The specified filler is obtained as follows.

(80-90) dm ^{3 of} hot demineralized water is poured into the reactor. Mixing is activated with a circulation pump and the precipitation process begins by supplying a solution of water glass and sulfuric acid. Mass concentration of SiO ₂ in a liquid glass solution (100 ± 2) g / dm ³ , density (1.1151 ± 0.05) g / cm ³ ; the density of the working solution of sulfuric acid (1.066 ± 0.005) g / cm ³ , the pH of the precipitation stage 1 is (10.5 ± 0.5).

After 10-15 minutes from the beginning of the deposition, the viscosity of the suspension begins to increase. In this mode, deposition is carried out for no more than 2 hours and 35 minutes. After this time, the supply of liquid glass stops, and the feed rate of sulfuric acid increases and the pH of the suspension is adjusted to (2.3 ± 0.7). The suspension is left to age at the reaction temperature and stirring, then pumped to the filtration. The filter cake is washed with demineralized water heated to a temperature of (50 ± 10) ^o С. Precipitated silicon dioxide is washed from sodium sulfate and sulfuric acid. The end of washing is determined by the absence of sulfate ion.

 The washed silica is dried in a chamber dryer. After that, the product is fed to a pneumatic mill for grinding by compressed air to a particle size of less than or equal to 20 microns, the proportion of which should be at least 90%.

The filler with thickening properties is a microionized amorphous silica powder having a bulk density of not more than 0.3 g / cm ³ , a specific surface area of not less than 80 m ² / g and a moisture capacity of 2.0-2.6 cm ³ / g.

 It is obtained as follows.

Prepare a solution of water glass with a density of (1.115 ± 0.05) g / cm ³ and a solution of sulfuric acid with a density of (1.066 ± 0.005) g / cm ³ . Demineralized water is poured into the reactor, and previously prepared solutions are supplied there with vigorous stirring, the precipitation pH is about 10. Precipitation is carried out for 70-80 minutes. Then, the supply of liquid glass is stopped, and the feed rate of sulfuric acid is increased, the pH is adjusted to (2.3 ± 0.7). The suspension is left to age at the deposition temperature and served for filtration. The precipitate is washed and dried. Dried silica is crushed to an average particle size of 2-30 microns.

 Depending on the purpose of the paste, fillers are used in a mixture or separately. The claimed excipients mix well with aromatic and / or medicinal substances, providing good quality pastes and gels.

 The table below shows comparative data on quality indicators of the claimed and known fillers.

 The proposed carrier, characterized by the above properties, allows you to obtain the necessary cleaning effect, retains structural and abrasive ability even under the influence of water and moisturizing substances that make up the pastes during storage for one year or more.

 The possibility of carrying out the invention can be illustrated by the following examples.

Example 1
The composition of the multifunctional toothpaste, wt.%:
Glycerin - 10
Sorbitol - 30
Sodium carboxymethyl cellulose - 1
PEG-400 - 3
Sodium Monofluorophosphate - 0.76
Saccharin - 0.2
Titanium dioxide - 0.25
Allantoin - 0.5
Triclosan - 0.28
Sodium Pyrophosphate - 2
Gantrez - 2.5
Silicon Dioxide - Abrasive - 10
Silicon Dioxide - Thickener - 10
Sodium Lauryl Sulfate - 1.45
Fragrance - 1
Water - Else
Example 2
The composition of the toothpaste, wt.%:
Sorbitol - 30
Sodium Lauryl Sulfate - 1.3
NaKMTS - 1.2
Sodium Fluoride - 0.24
Titanium dioxide - 0.25
PEG-400 - 3
Saccharin - 0.2
Preservative - 0.1
Fragrance - 0.8
Silicon Dioxide - Thickener - 10
Silicon Dioxide - Abrasive - 12
Water - Else
Example 3
The composition of the toothpaste with a whitening effect, wt.%:
Sorbitol - 30
Glycerin - 10
NaKMTS - 1
PVP K90 - 1
PEG-400 - 3
Sodium Monofluorophosphate - 0.76
Saccharin - 0.2
Titanium dioxide - 0.25
Sodium Pyrophosphate - 2
Preservative - 0.2
Silicon Dioxide - Thickener - 3
Silicon Dioxide - Abrasive - 18
Sodium Lauryl Sulfate - 1.45
Fragrance - 1
Water - Else
Example 4
The composition of the toothpaste with xylitol and urea, wt.%:
Sorbitol - 18
Xanthan gum (gum) - 0.8
Preservative - 0.2
Xylitol - 10
Urea - 0.5
Saccharin - 0.2
Sodium Monofluorophosphate - 0.76
Titanium dioxide - 0.25
Chalk - 20
Silicon Dioxide - Thickener - 10
Fragrance - 0.9
Water - Else
Example 5
The composition of the toothpaste for children in the form of a transparent gel, wt.%:
Silicon Dioxide - Thickener - 13
Silicon Dioxide - Abrasive - 5
Sorbitol - 67
Sodium carboxymethyl cellulose - 0.25
Sodium Lauryl Sulfate - 1.2
Polyethylene glycol 400 - 3
Sodium Monofluorophosphate - 0.45
Preservative - 0.2
Saccharin - 0.1
Dye - 0.003
Trisodium phosphate - 0.25
Fragrance - 0.8
Water - Else
Example 6
The composition of the toothpaste with plant extracts, wt.%:
Sorbitol - 30
Glycerin - 10
Silicon Dioxide - Abrasive - 10
Silicon Dioxide - Thickener - 9
Echinacea Extract - 3.5
Sea buckthorn extract - 1.5
Sodium Lauryl Sulfate - 1.5
Sodium carboxymethyl cellulose - 1.2
Sodium Monofluorophosphate - 0.76
Trisodium phosphate - 0.5
Calcium Glycerophosphate - 0.5
Titanium dioxide - 0.15
Saccharin - 0.2
Preservative - 0.2
Tartrazine E 102 - 0.002
Fragrance - 0.8
Water - Else
Example 7
The composition of the therapeutic and prophylactic paste, wt.%:
Sorbitol - 30
Chalk - 20
Silicon Dioxide - Thickener - 10
Sodium Lauryl Sulfate - 1.4
Xanthan Gum - 0.8
Fragrance Vrimint AJM 867 - 0.8
Sodium Monofluorophosphate - 0.76
Calcium Glycerophosphate - 0.5
Titanium dioxide - 0.25
Saccharin - 0.15
P-hydroxybenzoic acid methyl ester - 0.1
P-hydroxybenzoic acid propyl ester - 0.1
Water - Else
The proposed paste was tested in vitro and clinically by volunteers. Tests of toothpaste are made in accordance with the requirements of the "Methodological guidelines of the Ministry of Health of the USSR for experimental (pharmacological) and clinical testing of preventive and therapeutic toothpastes", 1983.

 1. Assessment of organoleptic properties.

 When studying the organoleptic properties of the paste, the evaluation of the appearance, color, taste and smell by the probants was taken into account.

 The tested paste, according to the testants, has a good taste, aroma, distribution in the mouth, foam well and satisfactorily.

 2. Test for abrasion of enamel.

 Enamel abrasion was determined by the change in the thickness of the removed human tooth before and after each brushing. A pre-polished tooth moistened with water was fixed and brushed using a mechanical rotating toothbrush for an hour. After that, the thickness of the tooth was re-measured. The difference was the amount of abrasion of the enamel. The average measurement in the experiment was 1 ± 0.1 μm.

 Under the microscope, an assessment was also made of the condition of the tooth surface. No significant scratches or cracks were found.

 3. Evaluation of the cleansing action.

 A common criterion for evaluating the cleaning properties of toothpastes is the presence of soft plaque after brushing. To quantify it, use plaque indices, the so-called hygiene indices, which are determined before and after using toothpaste.

 Clinical trials were conducted on a group of patients (28 people) with gingivitis and periodontitis using the paste from example 4.

 All subjects immediately after brushing noted an improvement in the condition of their teeth and oral cavity. The hygiene index before treatment averaged 2.9 ± 0.2, and after treatment, 1.1 ± 0.2.

 Thus, the paste according to this proposal can be recommended for systematic use for hygienic purposes, as well as a means of promoting the treatment and prevention of diseases of the oral cavity.

Claims (11)

1. Filler for toothpastes of silicon-containing compounds, characterized in that it is a microionized amorphous silicon dioxide powder with abrasive properties, having a bulk density of 0.5-0.7 g / cm ³ , a moisture capacity of 0.9-1.3 cm ³ / g, a specific surface area of at least 15 m ² / g and / or amorphous silicon dioxide with the properties of a thickener having a bulk density of not more than 0.3 g / cm ³ , a specific surface area of at least 80 m ² / g and a water capacity of 2.0-2 6 cm ³ / g  2. A filler according to claim 1, characterized in that at least 90% of the particles have a size of less than 20 microns. 3. Toothpaste containing sorbitol, sodium lauryl sulfate, a sweetener, a flavoring agent, a fluorine-containing compound, a silicon-containing carrier and water, characterized in that it additionally contains sodium carboxymethyl cellulose or xanthan gum, a dye, polyethylene glycol, as a fluorine-containing compound or sodium fluoride sodium monofluorophosphate, and as a silicon-containing carrier, the filler according to claim 1 or 2, comprising a mixture of silicon dioxide and / or chalk with abrasive properties and silicon dioxide with the properties of thickeners Itel at the following components, wt. %:
Sodium lauryl sulfate - 0.5-2.0
Sorbitol - 10-70
Sodium carboxymethyl cellulose or xanthan gum - 0.6-1.4
Polyethylene glycol - 1-5
Sweetener - 0.1-0.2
Dye - 0.002-1,000
Sodium Monofluorophosphate - 0.2-0.8
and / or sodium fluoride - 0.1-0.3
Fragrance - 0.6-1.2
Silicon dioxide - a thickener and / or - 2-17
Silica and / or chalk abrasive - 3-20
Water - Else
with a total silica content of 10-30.  4. The paste according to claim 3, characterized in that it further comprises sodium pyrophosphate and / or sodium tripolyphosphate in an amount of up to 5 wt. %  5. Paste according to any one of paragraphs. 3 and 4, characterized in that it additionally contains a gantrez in an amount of up to 2.5 wt. %  6. Paste according to any one of paragraphs. 3-5, characterized in that it further contains a preservative in an amount of up to 0.2 wt. %  7. Paste according to any one of paragraphs. 3-6, characterized in that it additionally contains glycerin in an amount of up to 20 wt. %  8. Paste according to any one of paragraphs. 3-7, characterized in that it additionally contains urea in an amount of up to 1.5 wt. % and xylitol in an amount up to 10 wt. %  9. Paste according to any one of paragraphs. 3-8, characterized in that it additionally contains biologically active additives in an amount of up to 10 wt. %  10. The paste according to claim 9, characterized in that as an active additive contains allantoin in an amount of 0.5-2.0 wt. %, or triclosan in an amount of 0.05-0.50 wt. %, or hydroxylapatite in an amount up to 2 wt. %, or polyvinylpyrrolidone up to 4 wt. %, and / or plant extract in an amount of 0.1-6.0 wt. %, and / or calcium glycerophosphate in an amount of 0.5-2.0 wt. %  11. The paste according to claim 3, characterized in that it additionally contains soda in an amount of 3-5 wt. %

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