COMPOSITION FOR THE TREATMENT AND/OR PREVENTION OF THE ORAL DISEASES

Abstract

The group of inventions relates to healthcare, concerns dentistry. The group of inventions includes a composition for the treatment and/or prevention of the oral diseases comprising an effective amount of aqueous and lipophilic extracts of aspen bark and at least one or more auxiliary compounds for the treatment and/or prevention, also includes a method of treatment and the use of a composition for the manufacture of a product for the treatment and/or prevention of the oral diseases. The group of inventions is characterized by high efficiency in the treatment and/or prevention of various the oral diseases, provides high-quality hygienic cleaning of the surface of the teeth and oral cavity. The use of a group of inventions makes it possible to reduce the likelihood of the occurrence and/or elimination of inflammation, as well as ulcers and erosions of the oral cavity in situations that contribute to their formation.

Claims

1. A composition for the treatment or prevention of oral diseases comprising an effective amount of aqueous and lipophilic extracts of aspen bark and at least one or more auxiliary substances for the treatment prevention.

2. The composition according to claim 1, wherein one or more of the following substances are used as an auxiliary substance: a thickener, a binding agent, an abrasive agent, a wetting agent, a foaming agent, a flavor, a sweetener, a stabilizer, a preservative.

3. The composition according to claim 1, further comprising anti-carious additives.

4. The composition according to claim 1, wherein the quantitative ratio of aqueous and lipophilic extracts of aspen bark is 1:1-100:1 by weight.

5. The composition according to claim 1, wherein the quantitative ratio of aqueous and lipophilic extracts of aspen bark is 1:10-100:1 by weight.

6. The composition according to claim 1, wherein the quantitative ratio of aqueous and lipophilic extracts of aspen bark is 1:1, 2:1, 5:1, 10:1, 20:1, 30:1, 40:1, 50:1, 60:1, 70:1, 80:1, 90:1 or 100:1 by weight.

7. The composition according to claim 1, wherein therapeutic or preventive action is aimed at acute and chronic forms of stomatitis, periodontal diseases, for example, gingivitis, periodontitis or parodontosis, dental caries, pulpitis.

8. The composition according to claim 1, comprising a therapeutic or preventive action aimed at burning hot food, injuring an oral cavity with a sharp object, chemical burn.

9. The composition according to claim 1, wherein the composition comprises: TABLE-US-00008 Component % wt. Glycerin 15 Xylitol 25 Calcium glycerophosphate 0.1 Hydroxyethylcellulose 1.5 Water extract of aspen bark 1 CO.sub.2 extract of aspen bark 0.5 Polysorbate-20 2 Methylparaben 0.3 O-cumene-5-ol 0.02 Flavoring agent 0.6 Water Up to 100

10. The composition according to claim 1, wherein the composition comprises: TABLE-US-00009 Component % wt. Glycerin 30 Xylitol 5 Calcium glycerophosphate 2 Hydroxyethylcellulose 3 Water extract of aspen bark 5 CO.sub.2 extract of aspen bark 0.05 PEG-40 hydrogenated castor oil 0.6 Methylparaben 0.1 O-cumene-5-ol 0.1 Flavoring agent 0.05 Water Up to 100

11. The composition according to claim 1, wherein the composition comprises: TABLE-US-00010 Component %, wt. Sorbitol 40 Xylitol 8 Silicon dioxide (abrasive) 5 Sodium Fluoride 0.3 Xanthan gum 0.8 Water extract of aspen bark 2 CO.sub.2 extract of aspen bark 0.2 Alkylamidobetaine 0.6 Sodium lauroylsarcosinate 0.5 Sodium Benzoate 0.8 Potassium Sorbate 0.2 Sodium saccharin 0.05 O-cumene-5-ol 0.05 Flavoring agent 0.6 Water Up to 100

12. The composition according to claim 1, wherein the composition comprise: TABLE-US-00011 Component % wt. Sorbitol 20 Xylitol 15 Silicon dioxide (abrasive) 15 Sodium Fluoride 0.1 Xanthan gum 1.2 Water extract of aspen bark 3 CO.sub.2 extract of aspen bark 0.1 Alkylamidobetaine 0.8 Sodium lauroylsarcosinate 0.2 Sodium Benzoate 0.5 Potassium Sorbate 0.4 Sodium saccharin 0.2 O-cumene-5-ol 0.08 Flavoring agent 1.2 Water Up to 100

13. The composition according to claim 1, wherein the aqueous extract of aspen bark comprises no more than 95% by weight of water and volatile substances.

14. The composition according to claim 1, wherein the lipophilic extract of aspen bark comprises no more than 60% by weight of water and volatile substances.

15. A use of the composition according to claim 1 for the manufacture of a product for the treatment or prevention of the oral diseases.

16. The use according to claim 15, wherein the product is a toothpaste, mouthwash or non-abrasive gel.

17. The composition The use of the composition according to claim 1 for the treatment or prevention of oral diseases.

18. A method for the treatment or prevention of oral diseases, which comprises applying a composition according to 1 to a surface of teeth in an oral cavity and keeping the composition in the oral cavity for between 5 seconds and 5 minutes of time.

19. The method according to claim 18, wherein the composition is kept in the oral cavity for between 30 seconds and 5 minutes.

Description

BRIEF DESCRIPTION OF THE DRAWINGS

[0060] FIG. 1. shows the cultivation of S. mutans with the studied samples of toothpastes.

EXAMPLES

Example 1. Preparation of Toothpaste

[0061] Compositions in the form of toothpaste are prepared as follows.

[0062] The required amount of water is weighed in a measuring dispenser, then the water is loaded into a mixer, if necessary, heated to a temperature of 50-60° C. Thickener, wetting agents, sweetener, preservatives, anti-caries additives are added to the water. The mixture is mixed until a homogeneous gel is obtained, if necessary, homogenized and vacuumed. An abrasive filler is added to the resulting gel, mixed until a homogeneous mass is obtained, if necessary, homogenized and vacuumed. If necessary, the resulting mass is cooled to a temperature of 30-40° C., and surfactants, an aqueous extract of aspen bark, stabilizers, and a mixture of fragrance with CO.sub.2 extract of aspen bark are added. Mix, homogenize and vacuum if necessary. The manufactured toothpaste is pumped into storage tanks and packed into tubes on filling machines.

Example 2. Preparation of Non-Abrasive Gel

[0063] Compositions in the form of a non-abrasive gel are prepared as follows.

[0064] The required amount of water is weighed in a measuring dispenser, then the water is loaded into a mixer, if necessary, heated to a temperature of 50-60° C. Thickener, wetting agents, sweetener, preservatives, anti-caries additives are added to the water. The mixture is mixed until a homogeneous gel is obtained, if necessary, homogenized and vacuumed. If necessary, the resulting mass is cooled to a temperature of 30-40° C., and surfactants, an aqueous extract of aspen bark, stabilizers, and a mixture of fragrance with CO.sub.2 extract of aspen bark are added. Mix, homogenize and vacuum if necessary. The manufactured gel is pumped into storage tanks and packed into tubes on filling machines.

[0065] The compositions according to the invention can be prepared using standard techniques.

Example 3. Examples of Compositions According to the Invention

[0066] Below are examples of specific formulations of compositions according to the present invention. These examples are illustrative in nature and are not restrictive. It is clear to the specialist that compositions with the properties of the invention can be implemented in other formulations that meet the characteristics of the invention.

[0067] 1. Non-Abrasive Gel:

TABLE-US-00001 Example Example Component 1, wt. % 2, wt. % Glycerin 15 30 Xylitol 25 5 Calcium glycerophosphate 0.1 2 Hydroxyethylcellulose 1.5 3 Water extract of aspen bark 1 5 CO.sub.2 extract of aspen bark 0.5 0.05 Polysorbate-20 2 — PEG-40 hydrogenated castor oil — 0.6 Methylparaben 0.3 0.1 O-cumene-5-ol 0.02 0.1 Flavoring agent 0.6 0.05 Water Up to 100 Up to 100

[0068] 2. Toothpaste:

TABLE-US-00002 Example 3, Example 4, Component wt. % wt. % Sorbitol 40 20 Xylitol 8 15 Silicon dioxide (abrasive) 5 15 Sodium Fluoride 0.3 0.1 Xanthan gum 0.8 1.2 Water extract of aspen bark 2 3 CO.sub.2 extract of aspen bark 0.2 0.1 Alkylamidobetaine 0.6 0.8 Sodium lauroylsarcosinate 0.5 0.2 Sodium Benzoate 0.8 0.5 Potassium Sorbate 0.2 0.4 Sodium saccharin 0.05 0.2 O-cumene-5-ol 0.05 0.08 Flavoring agent 0.6 1.2 Water Up to 100 Up to 100

[0069] The water extract of aspen used in the preparation of compositions is characterized by a mass fraction of water and volatile substances—86.6%; a mass fraction of tannins—2.0%.

[0070] Lipophilic (fat-soluble) CO.sub.2 extract comprises 4.35% water and volatile substances, 4.0% tannins.

[0071] The mixture of extracts is characterized by the presence in its formulation of phenolic glycosides (salicin, salicortin, tremuloicin), tannins, organic acids (oleic, linoleic, palmitic, capric, lauric, arachin, begenic), triterpenoids, pectin, glycine betaine, flavonoids, wax, sterols, carotenoids, polysaccharides, anthocyanins, glycolipids, phospholipids.

Example 4. Antibacterial Activity of the Compositions

[0072] A comparative analysis of the antibacterial (Streptococcus mutans) action of toothpastes 1 and 2 was carried out using an automated system for monitoring the growth of microorganisms.

[0073] In the experimental part, a bioreactor “RTS-1” (BioSan, Latvia) was used, with a mixing system—“reverse-spinner”. The system is designed for cultivating microorganisms and evaluating their growth in real time. The results were interpreted by measuring the optical density (OD) at a wavelength of λ=850 nm.

[0074] For the cultivation of S. mutans, a liquid nutrient medium—Todd Hewitt Broth (M313)—was used. For the cultivation of microorganisms in the bioreactor, 50 ml tubes with a membrane filter (TubeSpin SW) were used.

[0075] Test samples: [0076] Control sample—suspension of S. mutans; [0077] Sample of toothpaste 1; [0078] Sample of toothpaste 2.

TABLE-US-00003 TABLE 1 Experimental samples of toothpastes. Sample 1, Sample 2, Component wt. % wt. % Sorbitol 15 15 Glycerin 15 15 Xylitol 8 8 Silicon dioxide 15 15 Xanthan gum 1.1 1.1 Water extract of aspen bark 1 1 CO.sub.2 extract of aspen bark — 0.3 Alkylamidobetaine 0.8 0.8 Sodium lauroylsarcosinate 0.4 0.4 Sodium Benzoate 0.4 0.4 Sodium saccharin 0.3 0.3 Sodium Fluoride 0.2 0.2 Ortho-cumene-5-ol 0.05 0.05 Flavoring agent 0.8 0.8 Water Up to 100 Up to 100

[0079] For each experiment, a bacterial suspension in the amount of 5 ml was prepared separately in sterile test tubes with a volume of 15 ml. The optical density of the resulting suspension was measured using a DEB-1B densitometer (BioSan, Latvia). The concentration of the test sample was 0.1 g/1 ml.

[0080] When cultivating a clinical S. mutans isolate, in a control sample, the adaptive phase lasted up to 8 hours. This phase corresponds to the period of physiological adaptation, including the induction of enzymes, synthesis and assembly of ribosomes. The initial stationary period lasted up to 4 hours, 4-6 hours—the period of initial cell growth, 6-8 hours-the period of accelerated development. The exponential phase was marked by a classical jump in the optical density at the interval of 8-16 hours, after which a period of growth delay with a sharp transition to stationary equilibrium is traced. The peak optical density index at the end of true logarithmic development (indicator a) is 4.51±0.3 mcf (16 hours), the total indicator for the entire period of culture development (indicator (3) is 5.25±0.3 mcf (16 hours). The stationary phase, characterized by the equilibrium between cell growth and division and the process of cell death, was short (18-24 hours), followed by a gradual transition of the culture into the dying phase. The average optical density in stationary equilibrium is 5.28±0.3 mcf.

[0081] Cultivation of the bacterial population of S. mutans with the addition of the studied samples of pastes 1 and 2 (refer to FIG. 1) showed the following:

[0082] Sample 2—the adaptive phase is significantly prolonged compared to the control sample: up to 6 hours—the initial stationary period; up to 8 hours—the period of initial cell growth; up to 14 hours—the period of accelerated cell development. The period of accelerated cell development is characterized by the beginning of cell division, an increase in the total mass of the population and a constant increase in the growth rate of the culture, but exponential signs of growth were noted only after 15 hours of the experiment. The duration of logarithmic cell development was shortened compared to the control sample, and the rate of generation of new populations, therefore, the change in the optical density index was an order of magnitude lower. The indicator a is 4.15±0.3 mcf (22 hours), the indicator βis 4.25±0.3 mcf (24 hours). The stationary equilibrium phase was longer than in the control sample, with an average optical density of 4.25±0.3 mcf (24 hours).

[0083] Sample 1—according to the results of cultivation of the bacterial population with this sample, the adaptive phase lasted up to 10 hours. The transition of culture into exponential development was almost instantaneous, without a pronounced acceleration of growth. The indicator a is 4.54±0.3 mcf (20 hours), the indicator 0 is 4.25±0.3 mcf (22 hours). There is a stationary equilibrium phase with an average optical density of 4.55±0.3 mcf (22-32 h).

TABLE-US-00004 TABLE 2 Indicators of key points of the curve The average indicator in the stationary Indicator Indicator phase Reduction, Sample α (mcf) β (mcf) (mcf) % Control 4.51 ± 0.3 5.25 ± 0.3 5.28 ± 0.3 — Toothpaste 1 4.54 ± 0.3 4.65 ± 0.3 4.55 ± 0.3 13 Toothpaste 2 4.15 ± 0.3 4.25 ± 0.3 4.25 ± 0.3 19

[0084] Thus, the study of samples of toothpastes 1 and 2 with aspen bark extracts with an automated assessment of the growth curves of the microbial population of S. mutans showed the presence of antibacterial activity (bacteriostatic), and sample 2 (comprising an additional 0.3% CO.sub.2 of aspen bark extract) showed the best dynamics of this activity with the leading cariesogenic species for the child's body—S. mutans.

Example 5. The Effectiveness of Toothpaste in Patients Undergoing Orthodontic Treatment

[0085] Patients undergoing long-term orthodontic treatment were selected as a model for studying the effectiveness of toothpastes as a special case of the claimed composition.

[0086] This group of patients, due to the accelerated formation of plaque and its altered distribution architectonics in the oral cavity, is characterized by an increased intensity of the carious process and a pronounced severity of symptoms of periodontal diseases (severe forms of gingivitis).

[0087] 65 patients aged 13-15 years were examined. All the subjects were trained in the rules of oral hygiene, all were carried out professional hygiene. Subsequent hygiene was carried out by the subjects independently using orthodontic toothbrushes and brushes. Teeth brushing was carried out three times a day.

[0088] The subjects were divided into 3 groups:

[0089] The first group carried out oral hygiene using a toothpaste comprising an aqueous and lipophilic extract of aspen bark, (the composition of the paste corresponds to sample 4, disclosed in Example 3);

[0090] The second group carried out oral hygiene using a toothpaste comprising only an aqueous extract of aspen bark, (the composition of the paste corresponds to sample 1, disclosed in Example 4);

[0091] The third group (control) carried out oral hygiene using a toothpaste that does not comprise aspen extracts, attention was not focused on the specific composition of the paste.

[0092] At the first examination of patients, the hygiene efficiency index (O'Leary), the index of the state of periodontal tissues (PMA) was determined, which allows assessing the severity of gingivitis, the rate of salivation, the viscosity of saliva, the buffer capacity of oral fluid.

[0093] It was found that all patients who are being treated with non-removable orthodontic equipment have unsatisfactory indicators of oral hygiene. On average, the hygiene index for the three groups was 87.96±1.33%. The saliva viscosity in all patients is lower than the age norm, the buffer capacity is shifted to the acidic region, the salivation rate is lower than the reference values.

[0094] These indicators were determined in patients after three months.

[0095] Below are the data on the results of the study for each group.

TABLE-US-00005 TABLE 3 Results of the study of patients of the first group Before the start After 3 Degree of Index of the study months reduction, % O'Leary, % 89.56 ± 3.67  38.23 ± 3.81 57.31 PMA, % 78.45 ± 3.07  29.32 ± 3.12 62.63 Salivation rate, 0.28 ± 0.03  0.29 ± 0.05 — ml/min Saliva viscosity, cPs 1.98 ± 0.08  1.32 ± 0.05 — Buffering capacity 6.45 ± 0.03  7.10 ± 0.04 — of oral fluid

TABLE-US-00006 TABLE 4 Results of the study of patients of the second group Before the start After 3 Degree of Index of the study months reduction, % O'Leary, % 86.78 ± 3.18  42.64 ± 4.10  50.86 PMA, % 74.32 ± 3.20  38.65 ± 3.65  47.99 Salivation rate, ml/ 0.28 ± 0.03 0.29 ± 0.03 — min Saliva viscosity, cPs 1.98 ± 0.08 1.40 ± 0.05 — Buffering capacity 6.40 ± 0.03 7.05 ± 0.04 — of oral fluid

TABLE-US-00007 TABLE 5 Results of the study of patients of the third group Before the start After 3 Degree of Index of the study months reduction, % O'Leary, % 88.18 ± 3.53  61.65 ± 3.24 30.10 PMA, % 70.25 ± 3.27  67.33 ± 4.76  4.16 Salivation rate, ml/ 0.28 ± 0.03  0.29 ± 0.03 — min Saliva viscosity, cPs 1.98 ± 0.08  1.89 ± 0.05 — Buffering capacity 6.45 ± 0.03  6.53 ± 0.03 — of oral fluid

[0096] The conducted studies have shown the following. During the study period, there was no significant change in the rate of salivation for patients of all groups. In the subjects of the first and second groups, the hygiene index significantly decreased, which corresponds to a decrease in the amount of plaque and dental calculus. A slight decrease in the O'Leary index is also observed in patients of the control group. The subjects of the first and second groups also have a significant improvement in the condition of the gums at the teeth. In patients of the first and second groups, a decrease in the viscosity of saliva was also observed, which leads to a more complete cleaning of the surfaces of the teeth and oral cavity, and contributes to an increase in its remineralizing potential. The use of a paste comprising extracts of aspen bark leads to a shift in the pH of saliva to a more neutral area.

[0097] At the same time, based on the data in tables 3 and 4, it can be seen that the composition, characterized by the presence of two aspen extracts: lipophilic and aqueous, demonstrates excellent properties not only in comparison with the control compositions, but also in comparison with a paste comprising only an aqueous extract of aspen bark.

[0098] In general, a method for the prevention and treatment of oral diseases using the composition of the present invention consists in applying it to the surface of the teeth and finding the composition in the oral cavity and on the surface of the teeth for 5 seconds to 5 minutes of time. Preferably from 30 seconds to 4 minutes. Preferably from 1 minute to 4 minutes. In this case, a brush can be additionally used.

[0099] Thus, the composition proposed in the scope of the present invention can be used in healthcare, providing effective prevention and/or treatment of the oral diseases.