RU2733718C1 - Composition in form of gel for oral tissues care - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to dental compositions for oral care tissues. Proposed composition in form of gel for oral care tissues contains as active ingredients aspen bark extract in amount of 0.01–0.3 wt. %, copper derivative of chlorophyll - 0.01–0.2 wt. %, dihydroquercetin 0.1–0.5 wt. % and Siberian fir extract - 0.01–0.1 wt. %, and as auxiliary substances - substances selected from the group: sodium alginate, methyl salicylate, emulsifier, flavouring agent, methylparaben, menthol, eugenol, sorbitol, hydroxyethyl cellulose, citric acid, allantoin, D-panthenol, castor oil and water, wherein as a copper chlorophyll derivative, the composition contains sodium copper chlorophyllin.

EFFECT: use of said four main active ingredients provides complex antibacterial, antiviral, anti-inflammatory, anti-haemorrhoid, cleansing, antioxidant and immunocorrective action on oral tissues; wherein the disclosed composition has a prolonged exposure by the gel form.

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Description

The invention relates to medicine, namely to therapeutic dentistry, and is intended for use as a means for caring for the oral cavity, in particular for periodontal tissues.

The periodontium is a complex of tissues surrounding and fixing the tooth, closely related morphofunctionally and genetically, which includes the cement of the tooth root, periodontium, alveolar bone with periosteum and gums (Balin V.N. Practical periodontology / V.N. Balin [et al. .]. - SPb .: Peter Press, 1995).

The prevalence of periodontal diseases in the Russian Federation tends to 100% (Dental morbidity of the population of Russia / Ed. By E. M. Kuzmina. - Moscow: MGMSU, 2009).

It is known that inflammatory periodontal diseases (gingivitis, periodontitis) in the presence of risk factors develop as a result of exposure to bacteria of the microbial biofilm (Periodontal disease. A modern view of clinical diagnostic and therapeutic aspects: textbook / O.O. Yanushevich, V.M. Grinin, VA Pochtarenko [et al.] / Under the editorship of Prof. OO Yanushevich. - M .: GEOTAR-Media, 2010).

Risk factors include inadequate oral hygiene, increased production of free radicals and inhibition of the body's natural antioxidant system (Tarasenko L.M. The role of lipid peroxidation in the pathogenesis of periodontal damage under stress / L.M. Tarasenko, O.N. Voskresensky // Pat physiological and experimental therapy. - 1986, No. 6, pp. 12-14.), as well as immunological disorders as a result of diseases of internal organs (Gorbacheva I.A.Complex approaches to the treatment of patients with combined diseases of internal organs and inflammatory lesions periodontium (author's abstract of the thesis of Doctor of Medical Sciences: 14.00.05, 14.00.21 / Gorbacheva I.A. - SPb., 2004. - 42 p.).

For the treatment of gingivitis and periodontitis, antiseptics are widely used, the most effective of which is chlorhexidine bigluconate (Clinical guidelines (treatment protocols) for the diagnosis of periodontitis, approved by the Decision of the Council of the Association of Public Associations "Dental Association of Russia" on April 23, 2013 with amendments and additions based on Resolution No. 18 of the Council of the Association of Public Associations "Dental Association of Russia" dated September 30, 2014, updated on August 02, 2018).

The disadvantages of using antiseptics are the emergence of resistant strains of microorganisms (Shumsky A.V. Lymphotropic drug and immunocorrective therapy in the complex treatment of infectious and inflammatory diseases of the oral mucosa: author of the thesis.Doctor of medical sciences / A.V. Shumsky. M, 1998), chlorhexidine bigluconate is characterized by a cytotoxic effect, primarily in relation to macrophages and lymphocytes (Ivanov, BC Periodontal disease / BC Ivanov. - M .: OOO "Medical information agency", 2001).

Herbal remedies such as chamomile, sage, calendula, St. John's wort, eucalyptus, etc., widely used for rinsing the mouth in the form of infusions, decoctions, elixirs, are devoid of these shortcomings. They have an antiseptic and anti-inflammatory effect, but they are quickly washed off with saliva (Medicinal plants in dentistry. 2nd ed., Supplemented / A.I. Marchenko, I.A. Baranyuk, E.V. Levitskaya, E.P. Sokolovskaya. - Chisinau: Shtiintsa, 1989).

An effective antibacterial, anti-inflammatory, hemostatic and wound-healing effect of a dental elixir containing an extract of aspen bark is known (Drozhzhina V.A.Natural biologically active substances in the prevention and treatment of dental and periodontal diseases: abstract of the thesis.Doctor of medical sciences: 14.00.21 / VA Drozhzhina. - SPb., 1995). However, its effect is short-term and therefore not particularly effective.

In this regard, dental compositions in the form of a gel are convenient to use. The prior art discloses dental gels with various active substances. For example, Dentoferon gel, which is described in patent RU 2490006 C1, A61K 6/00, 08/20/2013, is based on interferon. In our market, Cholisal tooth gel with a chemical composition is widely known.

Compositions in the form of a gel based on plant biologically active components are especially promising and safe. Such as a hydrophobic gel with tea tree oil, guaisulene, sage, clove and thyme oils, described in patent RU 2706010 C1, A61K 6/00, 11/13/2019, and a dental gel with a phytopeloid composition from patent RU 2699560 C1, A61K 9/00 , 09/06/2019. This gel can be chosen as the closest analogue for the present invention.

The known patent discloses a therapeutic and prophylactic agent in the form of a gel for the treatment and prevention of infectious and inflammatory diseases of the oral mucosa. The well-known dental gel contains dry extracts of goat willow bark and licorice root, an aqueous extract of sulfide-silt iodine-bromine mud, essential oil of Sage officinalis, chlorhexidine bigluconate, lidocaine hydrochloride, ascorbic acid, carbopol, sorbitol, nipagin and purified water. However, despite a number of advantages, the known composition is not completely natural of plant origin, does not have a powerful antioxidant and anti-halitosis effect due to its composition.

The objective of the present invention is to expand the arsenal of gel dental compositions by increasing the effectiveness of the proposed composition in comparison with known analogues, which would provide a powerful prevention of the onset, progression and exacerbation of inflammatory periodontal diseases, as well as the achievement of an additional anti-halitosis effect. The technical result consists in solving the problem and achieving the indicated advantages.

The problem is solved, and the technical result is achieved by applying a gel to the gums, the composition of which includes aspen bark extract as the main active components, which has an anti-inflammatory and antimicrobial effect, a copper chlorophyll derivative, which provides additional anti-inflammatory, anti-halitosis, to care for the periodontal tissues. , a cleansing effect, dihydroquercetin, which has a pronounced antioxidant effect, and fir extract, which has antibacterial, antiviral, anti-inflammatory; and immunocorrective action. The composition additionally contains auxiliary substances selected from the group: sodium alginate methyl salicylate, emulsifier, flavoring agent, preservative, menthol, eugenol, sorbitol, hydroxyethyl cellulose, citric acid, allantoin, D-panthenol, castor oil, water. In this case, the main active components are selected from the following ranges of values, mass. %: aspen bark extract - 0.01-0.3, copper chlorophyll derivative - 0.01-0.2, Siberian fir extract - 0.01-0.1, dihydroquercetin - 0.1-0.5. In a particular embodiment, the composition as a copper chlorophyll derivative contains sodium copper chlorophyllin, a water-soluble salt.

The applicant received two trademarks FITODENT (certificate No. 586139) and FITODENT (certificate No. 589149) for the claimed composition. And further in clinical examples he named his gel, which was offered to patients, Fitodent Periogel.

The preparation of copper chlorophyll derivatives is described much earlier in the inventor's certificate SU 1782603 A1, 23.12.1992, patents RU 2005464 and RU 2034556 C1, 10.05.1995. It is preferable to use a water-soluble sodium salt - sodium copper chlorophyllin. The aspen bark extract can be as described, for example, in patent RU 1814553 C1. Siberian fir extract can be any.

Additional components of the composition also have a number of beneficial properties.

Methyl salicylate is a non-steroidal anti-inflammatory drug that non-selectively inhibits cyclooxygenase, reduces the synthesis of prostaglandins, normalizes capillary permeability, normalizes microhemodynamics in periodontal tissues.

D-panthenol - provitamin B ₅ , has a wound healing and some anti-inflammatory effect.

Sodium alginate has a reparative, hemostatic, local anti-inflammatory effect, is a thickener and gelling agent.

Menthol has some antimicrobial and anti-inflammatory effects, locally causes vasoconstriction and a feeling of cold, improves tissue trophism.

Allantoin has an astringent effect, has a beneficial effect on the processes of tissue regeneration.

Eugenol has aromatic properties, antibacterial and anti-inflammatory effects.

When applied topically, castor oil has a wound healing, antifungal, antibacterial and anti-inflammatory effect.

Citric acid has an antibacterial effect, stabilizes the acidity of the gel.

Sorbitol is a sweetener, flavoring, thickening and stabilizing agent.

A preservative such as methylparaben also has antibacterial and antifungal activity.

Hydroxyethylcellulose is a thickener and gel stabilizer.

As a flavoring agent, any flavoring agent approved in the food and pharmaceutical field can be used.

Description of figures

FIG. 1 - Orthopantomogram of the patient 3. Chronic generalized periodontitis of moderate severity. Chronic granulating periodontitis.

FIG. 2 - Orthopantomogram of the patient 3. Chronic generalized periodontitis of moderate severity.

FIG. 3 - Orthopantomogram of patient A. Chronic generalized periodontitis of moderate severity.

FIG. 4 - Patient B. Chronic catarrhal gingivitis. The state of the oral cavity after professional controlled oral hygiene.

FIG. 5 - Patient B. Chronic catarrhal gingivitis. The state of the oral cavity after a week of treatment.

An example of obtaining the claimed composition in the form of a gel for the oral cavity.

A prescription amount of hydroxyethyl cellulose was dissolved in an aqueous solution of sorbitol and an aqueous solution of sodium alginate was added to it with thorough mixing. Dissolved in an emulsifier such as PEG-40 (Ricino), methyl salicylate, menthol, castor oil, flavor and eugenol. Half of the prescription amount of hot water was added to the resulting homogeneous mixture and mixed for 20 minutes. until a homogeneous mass is obtained. The previously prepared solutions were mixed. The following components were dissolved in the remaining amount of water at a temperature of 40-50 ° C: aspen bark extract, sodium copper chlorophyllin, citric acid, Siberian fir extract, dihydroquercetin, allantoin, D-panthenol, methylparaben preservative, each separately. Then all solutions were added to the total homogeneous mass. The resulting gel was thoroughly mixed, then left for 8 hours and served for packaging.

The claimed composition in the form of a gel for the oral cavity was made according to the described method, in which the components were taken in g based on 100 g of the finished product: aspen bark extract - 0.06 (in terms of absolute dry weight), methylparaben sodium salt - 0.2, flavoring - 0.05, menthol - 0.01, eugenol - 0.05, sorbitol 70% aqueous solution - 70, emulsifier (Ricino) - 2.75, methyl salicylate - 0.1, hydroxyethyl cellulose - 1.0, citric acid - 0.04, allantoin - 0.2, D-panthenol - 0.3, sodium copper chlorophyllin - 0.02,: Siberian fir extract - 0.07, sodium alginate - 0.35, dihydroquercetin - 0.3, castor oil - 2.5, water - the rest.

Method of application: after brushing your teeth, it is recommended to dry the oral mucosa with a cotton swab, apply a thin layer of gel on it using the nozzle of a dispensing tube or a clean cotton swab. It is not required to wash off the gel.

To illustrate the effect of the claimed compositions, clinical examples are given below.

Clinical example No. 1

Patient Z., 52 years old. When applying, she complains of bleeding gums, tartar and inflammation of the gums. He considers himself ill for the last 10 years, and twice a year he consults a dentist to remove tartar. History of kidney stone disease.

Objectively: The general condition is satisfactory, the face is symmetrical. Opening the mouth is not difficult. Orthognathic bite.

The presence of deposits of supra- and subgingival tartar is noted, the mucous membrane of the gingival papillae and the gingival margin is edematous and hyperemic. With light probing of the periodontal pockets, bleeding of the gums is noted. The PMA index is 57.1%.

Dental formula:

The depth of periodontal pockets (indicated is the largest among the surfaces of each tooth, mm):

Orthopantomogram: uneven bone resorption of the edges of the alveolar arches (Fig. 1).

On the basis of complaints, anamnesis, and objective research data, the patient was diagnosed with exacerbation of chronic generalized periodontitis of moderate severity.

Measures of professional controlled oral hygiene were carried out, applications to the gums of Fitodent Periogel gel with aspen bark, Siberian fir, chlorophyllin and dihydroquercetin were prescribed twice a day.

Inspection in a week. The patient notes some improvement, but complaints of bleeding gums persist.

Objectively: Facial symmetry is not broken. Opening the mouth is free. No calculus deposits were found. The mucous membrane of the gingival papillae is edematous, hyperemic, with light probing of periodontal pockets, bleeding of the gums persists. The PMA index is 31.0%.

Presumably incomplete success of treatment is associated with insufficient concentration of the main active ingredients in the gel sample.

The patient was prescribed gum applications 2 times a day of a sample of Fitodent Periogel gel with a higher concentration of aspen bark extract and dihydroquercetin.

When re-examining a week later, the patient does not present complaints, notes a significant improvement in the condition of the gums.

Objectively: the oral mucosa is pale pink, no edema of the periodontal tissues was observed? There is no bleeding of the gums when probing periodontal pockets. The PMA index is 10.7%. The success of the treatment was noted. The patient was advised to continue applying the gel for a week to consolidate the treatment result.

Clinical example No. 2

Patient I., 28 years old. Complaints about bleeding gums, bad breath.

Physical examination data: the face is symmetrical, the opening of the mouth is normal. Orthognathic bite. The mucous membrane of the gums is edematous, hyperemic, there is a pronounced bleeding of the gums when probing periodontal pockets.

Dental formula:

The depth of periodontal pockets (indicated is the largest among the surfaces of each tooth, mm):

On the orthopantomogram (Fig. 2) - uneven resorption of the interalveolar crests of the jaws, more pronounced in the upper jaw.

On the basis of complaints, anamnesis, data of objective and X-ray examination, the patient was diagnosed with chronic generalized periodontitis of moderate severity.

Professional controlled oral hygiene was performed, the patient was prescribed Fitodenpf erragel gel applications twice a day.

The next day: the patient complains of the presence of unpleasant hard grains in the gel. Probably, during the preparation of the gel, excessive amounts of dry components, namely dihydroquercetin and aspen extract, give grains in the finished gel.

Clinical case No. 3

Patient K., 64 years old. She complained of bleeding gums, inflammation and pain in the gums in the area of 16, T7 teeth and around the implants in the area of 34, 32, 42, 44.

According to the patient, she has been suffering from bronchial asthma for the last 8-9 years. Professional oral hygiene was carried out a week before the visit, the patient felt some improvement in her condition, but the main complaints persisted.

Objectively: the symmetry of the face is not broken, opening the mouth is not difficult. Palpable submandibular lymph nodes on both sides, soft-elastic consistency, mobile, not adhered to the surrounding tissues, measuring about 1.0 × 0.7 cm, painless on palpation.

Dental formula (I - implants):

No calculus deposits were found. The mucous membrane of the gingival margin, as well as in the area of the implants, is edematous and hyperemic. From periodontal pockets - scanty purulent discharge.

The depth of periodontal pockets (indicated is the largest among the surfaces of the tooth, mm):

Based on complaints, anamnesis, and objective research data, the patient was diagnosed with exacerbation of "moderate chronic generalized periodontitis, mucositis.

Prescribed applications of Fitodent Periogel gel with aspen bark, Siberian fir, chlorophyllin and dihydroquercetin twice a day.

On examination after a week: the mucous membrane of the oral cavity was pale pink, no purulent discharge from periodontal pockets was found, no tartar deposits were found. The patient notes the cessation of the manifestations of bronchial asthma against the background of the application of the gel.

It was not obvious that the claimed composition for the oral cavity, when the gel was administered to a patient suffering from chronic generalized periodontitis of moderate severity and mucositis in the area of four implants against the background of bronchial asthma, would be effective in the form of disappearance of bronchial asthma attacks. This can probably be explained by a decrease in the systemic effect on the patient's body of the inflammatory process in the cavity as a focus of chronic odontogenic infection. It was also not apparent that the gel would have an anti-halitosis effect.

Clinical example No. 4

Patient A., 42 years old, applied to the dentistry clinic with complaints of bleeding gums, the presence of bad breath. According to the patient, these phenomena have been noted over the past 3 years. He mentions that he had previously consulted a dentist, that calculus was removed, but the patient received only a short-term improvement.

Objective research data: the patient's face is symmetrical, opening the mouth is not difficult. Orthognathic bite.

Dental formula:

There are supragingival and subgingival calculus deposits.

The depth of periodontal pockets (indicated is the largest among the surfaces of the tooth, mm):

The mucous membrane of the interdental papillae and the gingival margin is edematous, hyperemic, bleeds with light probing. The PMA index is 66.6%.

On the orthopantomogram (Fig. 3) - uneven resorption of the interalveolar crests of the jaws.

On the basis of complaints, anamnesis, data of an objective clinical and X-ray examination, the diagnosis was made: Chronic generalized periodontitis of moderate severity.

Professional controlled oral hygiene was performed. Prescribed applications of Fitodent gel twice a day after brushing your teeth.

On examination after a week: the patient has no complaints. The mucous membrane of the oral cavity is pale pink. Ainamo's test was negative (no bleeding of the gums was detected with light probing of periodontal pockets). No calculus deposits were found.

The PMA index is 12.5%.

Clinical example No. 5

Patient V., 25 years old. Complaints about bleeding gums. Considers himself sick for about a year. History of chronic hyperacicidal gastritis.

With objective research: the general condition is satisfactory. Submandibular, cervical lymph nodes are not palpable. The face is symmetrical, mouth opening is free. Orthognathic bite.

Dental formula:

There is hyperemia and edema of the gingival mucosa in the area of the gingival papillae and, in part, the gingival margin. Abundant deposits of supragingival calculus. Gums bleed on light touch.

The PMA index is 37.5%. No periodontal pockets were found.

On the basis of complaints, anamnesis, and objective research data, the patient was diagnosed with chronic catarrhal gingivitis of moderate severity.

Professional controlled oral hygiene was performed. The condition of the gums after hygiene is shown in FIG. 4.

The patient is prescribed Fitodent gel applications twice a day after brushing his teeth. When viewed after a week: the oral mucosa is pale pink in color. No bleeding of the gums was detected (Fig. 5). The PMA index is 8.3%.

Thus, in case of inflammatory periodontal diseases after professional controlled oral hygiene, the use of Fitodent gel twice a day helps to reduce the intensity of the inflammatory process of the periodontal tissues.

The technical result of the claimed invention is the creation of an effective composition in the form of a Gel, which has a synergistic effect due to the properties of four main active substances - aspen bark extract, Siberian fir extract, a copper derivative of chlorophyll and dihydroquercetin, and therefore has a complex antibacterial, antiviral, anti-inflammatory, anti-halitosis, cleansing, antioxidant and immunocorrective action on the tissues of the oral cavity. In addition, in contrast to the elixir based on aspen bark extract, the claimed composition has a long-term prolonged effect due to the gel form, which has good adhesion to the oral mucosa. And unlike analog gels, it is safe, since it has a completely herbal composition, a more powerful therapeutic and prophylactic effect, and additionally has a positive effect on the patients' chronic diseases.

Claims (3)

1. Composition in the form of a gel for the care of the tissues of the oral cavity, characterized in that as the main active ingredients contains aspen bark extract in an amount of 0.01-0.3 wt. %, copper chlorophyll derivative - 0.01-0.2 wt. %, dihydroquercetin - 0.1-0.5 wt. % and Siberian fir extract - 0.01-0.1 wt. %, and as auxiliary - substances selected from the group: sodium alginate, methyl salicylate, emulsifier, flavoring, methylparaben, menthol, eugenol, sorbitol, hydroxyethylcellulose, citric acid, allantoin, D-panthenol, castor oil and water, while a copper chlorophyll derivative composition contains sodium copper chlorophyllin. 2. A composition according to claim 1, characterized in that it contains, in g per 100 g of the finished product: aspen bark extract 0.06 (in terms of absolute dry weight) sodium copper chlorophyllin 0.02 Siberian fir extract 0.07 dihydroquercetin 0.3 sodium methylparaben 0.2 flavoring 0.05 menthol 0.01 eugenol 0.05 sorbitol 70% aqueous solution 70 emulsifier 2.75 methyl salicylate 0.1 hydroxyethyl cellulose 1.0 citric acid 0.04 allantoin 0.2 D-panthenol 0.3 sodium alginate 0.35 Castor oil 2.5 water rest

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