BG98625A - Composition of preparations for hygiene, prophylaxy and treatment of the oral cavity - Google Patents

Abstract

The composition has excellent antiinflammatory effect, indicates fibrosing effect in the submucuous, membrane, completely regenerates any impairments in the oral cavity without any hyperplastic manifestations in the cellular layers and the keratin, maintains the bacterial balance and is completely hermless after continuous usage. It includes, in wt.%: hydrogen peroxide 0.5-2.0, zinc chloride 0.02-0.4, tiloxapole - polymer of tertiary oxyethylated octyphenol formaldehyde 0.03-0.07, tartaric acid 0.01-0.03 ethanol 2.5-5.0, and the remainder to 100 - deionized water and certain additives for taste, flavour and stability.

Description

COMPOSITION OF HYGIENE PRODUCT *, * PREVENTION AND * TREATMENT

Of the oral cavity

Technical field

The present invention relates to a composition for preparation for oral hygiene and for the prevention of diseases of the tooth enamel and the formation of caries, for the disinfection and treatment of inflammatory processes and the repair of tissues in the oral cavity, for the prevention of plaque and tooth formation .

BACKGROUND OF THE INVENTION

Various preparations for oral hygiene and prophylaxis are known. Their active components maintain effective control of the etiologic factors that cause disease processes in the oral cavity. They also control the microflora in the mouth, inflammations, plaques and other local factors, which ultimately helps the individual maintain his or her health or improve his or her condition in dental and oral diseases.

Hydrogen peroxide is known to be an active ingredient in the hygiene, prophylaxis and treatment of diseases in the oral cavity. Under the influence of catalase and peroxidase enzymes, hydrogen peroxide decomposes and releases active oxygen, which inhibits the development of anaerobic bacteria and promotes the beneficial microflora in the mouth. In this way, it disinfects and returns to normal the tissues in the oral cavity (Wennstrom J. and Lindhe J. Effect of hydrogen peroxide on developing plaque and gingivities in man - Journal of Clinical Periodontology, 1979, No. 6, pp. 115-130).

The effect of zinc dichloride as an antibacterial agent is known. It binds to bacterial cell membranes, inhibits the metabolism of bacteria and inhibits their growth: reduces adhesion both between them and the teeth, protects the enamel of acids from the products of bacterial metabolism and nutrition (Gedalia I. and com. Effect of Zinc Chloride Mouth wash on Plaque and Zinc Levels of Surface Enamel - Clinical Preventive Dentistry Vol.10, No. 4, 1988, pp. 3-5).

The effect of the combination of citrate and sodium lauryl sulphate on the inhibition of streptococci and the reduction of plaque growth in the oral cavity, as well as on the healing of tissues in the mouth, is also known. Nitrate comes in complex with heavy metals from food and allows zinc to have a more active effect with its inhibitory effect in cellular structures (Giertsen E. and com. Plaque Inhibition by a Combination of Zinc Citrate and Sodium Lauryl Sulfate - Dental Faculty, University of Oslo, Norway, 1989, pp. 278-283).

Also known is a combination of these active ingredients in a rinsing and oral hygiene composition, which is also suitable for the treatment of periodontal disease and stomatitis at a given concentration (US patent 5104644 of 14.04.1992).

The composition contains the following active ingredients in wtL:

Hydrogen peroxide from 0.5 to 3;

Zinc dichloride above 0.02 - preferably from

0.02 to 0.8; preferably by Sodium citrate above 0,03 - 0.03 TO 0.2; Sodium lauryl sulfate over 0.04 - preferably from 0 , 04 to 0.25; Ethanol from 2 to 3.5.

The rest is deionized water and known components that give the taste and smell of the liquid.

The pH of the liquid is about 3.5 - 4, in some cases up to 5.5.

The combination of the active ingredients has an antibacterial effect, reduces plaques, regulates cellular metabolism, inhibits inflammatory initiators and helps to repair tissues, to heal bleeding tissues, and to prevent parodontosis, stomatitis, gingivitis and inflammation. Depending on the purpose of the composition, three concentrations of the active ingredients are recommended: in the lowest values for rinsing and prevention of the oral cavity; in the mean values - to reduce plaque; in the above values for the treatment of periodontal disease.

SUMMARY OF THE INVENTION

A problem with oral cavity prevention and treatment preparations is their harmlessness and the maintenance of the physiological balance of the oral microflora, since the combination of the active components leads to the destruction of bacteria associated with disease processes, but also of bacteria that are part of the normal flora of the oral cavity. This determines an altered taste in the mouth. An additional problem is the discoloration of the teeth and the secondary development of candida albicans bacteria.

The problem is solved by the present invention relating to a preparation for hygiene, prophylaxis and treatment of the oral cavity. The preparation is composed of the active com ponents of hydrogen peroxide and zinc dichloride, to which tiloxapol is a polymer of tertiary oxyethylated octylphenol formaldehyde and tartaric acid%:

fair weight ratios.

hydrogen peroxide by 0.5 to 2.0; zinc dichloride by 0.02 to 0.4; tiloxapol by 0.03 to 0.07; tartaric acid by 0.01 to 0.03; ethanol by 2.5 to 5,0; the rest up to 100 - deio lower on water and

known components for taste, odor and stabilization.

It has been unexpectedly discovered that tyloxapol, which is a known aerosol detergent in the treatment of pulmonary diseases, even infants (Miller JB Detergent Aerosol Therapy - Clinical Medicine, Oct.1967 No. 74, pp. 37-40), is proactive in preventing and treatment of diseases in the oral cavity in combination with hydrogen peroxide, zinc dichloride and tartaric acid. For the first time, its selective effect on pathogenic bacteria incl. and on candida albicans and thanks to this, maintaining the physiological balance of the microorganisms in the mouth. The combination with tartaric acid enhances this action.

The advantage of the invention is determined by the combination, and in particular by the presence therein of tyloxapol (a polymer of tertiary oxyethylated octylphenol formaldehyde), which is a non-ionic detergent, completely harmless. In combination, it reduces surface tension and prevents the formation of cellular bacterial colonies that lead to stomatitis, gingivitis and periodontal disease; inhibits bacterial enzymes and increases the permeability of bacterial membranes. The combination has a marked synergistic inhibitory effect on pathogenic bacterial growth.

The tartaric acid in the combination acts as a synergist in suppressing the inflammatory processes in the oral cavity; it also increases membrane permeability and has an antibacterial effect.

The combination as a whole - depending on the concentration, has a healing effect, which is expressed in the suppression of inflammatory processes; reduced gum bleeding; helping to maintain bacterial balance in patients injured after dental intervention; facilitates cleaning of teeth and dentures and prevents inflammation after prosthetics; reduces tartar; refreshes the oral cavity. For prolonged use it is completely harmless. This quality is due in particular to tiloxapol.

Examples of carrying out the invention

The following examples give more detailed information about the invention without limiting it.

EXAMPLE 1

The following components are mixed in an amount by weight, and it is possible to change them to

divided by ethyl alcohol - glycerin - the second column, borders: 3.5 3.0 + + 1 0.5 poloxamer 407 - 0.3 + 0.1 saccharin 0.03 + 0,005 tiloxapol 0.05 + 0.02 citric acid - 0.05 + 0.02 tartaric acid - 0.02 + 0.01 zinc dichloride - 0.03 + 0.01 flavoring composition (menthol) - 0.03 + 0,005 Na - EDTA - 0.04 + 0.01 hydrogen peroxide - 0.6 + 0.1

deionized water - up to 100 and drops of sodium hydroxide to adjust the pH of the medium to 3.5 - 4.0.

the solution of Example 1, packaged, was stored at room temperature (5 to 35 ° C) and administered for oral prophylaxis. After brushing the teeth, the oral cavity is rinsed up to 3 times daily with an amount of about 15 ml determined by a dosing cup.

EXAMPLE 2

A preparation of a preparation identical to Example 1 was prepared, increasing the amount of zinc dichloride and hydrogen peroxide as follows: zinc dichloride - 0.6 wtL + 0.05 hydrogen peroxide - 1.5 wt + 0.1.

A preparation is obtained that is suitable for the prevention and treatment of periodontal disease, gum bleeding and oral cavity injury. The solution of Example 2 was applied in the same • ♦> · ¹⁴ • · i * · »» - r «··» · • · t £ *> · «• · ··· ·· ·· ··«

- 6 way as the solution of Example 1, but not more than 20 days. After active treatment, oral prophylaxis is switched to the solution of Example 1.

EXAMPLE 3

The preparation of the preparation is accomplished by sequentially mixing the components in the order as indicated below. For receiving 1000 kg. from the preparation, the components are mixed by continuous stirring in a suitable stainless steel vessel as follows:

ethyl alcohol - 15.0 kg glycerin - 30.0 kg zinc dichloride - 0.18 kg Na-EDTA - 0.44 kg tartaric acid - 0.24 kg citric acid - 1.6 kg saccharine - 0.18 kg poloxamer 407 - 4.0 kg ethyl alcohol - 15.0 kg tyloxapol - 0.75 kg flavoring composition - 0.36 kg deionized water - 832.25 kg hydrogen peroxide 6% - 100 kg

EXAMPLE 4

In this example, the irritant effect of the preparation according to the invention on the oral mucosa of golden hamsters is evaluated. Thirty animals were tested, 15 were treated with tap water and 15 were treated with the preparation according to the invention (trade name Sure Choice).

At the beginning of the study, each animal was anaesthetized with 0.2 cc Ketamin HCl intraperitoneally. The mucosa on the left buccal side is scraped with a metal brush. Cotton swabs were soaked with detergent and tap water and placed on the left (experimental) and right (control) buccal sides for 10 minutes. The duration of treatment is 13-14 hours, 30 consecutive days.

Sections of the mucous membrane of the left and right buccal sides are fixed in 10¾ neutral formalin and included in paraffin blocks. Histological sections were stained with histological preparation with a thickness of 5 microns. They have been evaluated for: ulcers, inflammatory changes, epithelial hyperplasia and fibrosis.

Photos were also taken on the left buccal side of the animals with a Minolta x700 camera and a Kodak Gdd film. The results were processed with a computer program by the method of variational analysis at a probability level p <0.05. They state the following:

The investigated drug has a good anti-inflammatory effect, judging by the histological changes in the mechanically damaged hamster mucosa.

Compared to the control, the preparation according to the invention exhibits a fibrotic effect in the submucosa.

Under the influence of the preparation according to the invention, the oral mucosa after mechanical damage regenerates within 30 days completely without hyperplastic manifestations of the cell layers and keratin.

EXAMPLE 5

In this example, the skin sensitizing potential of the oral preparation is examined.

The study was performed on white guinea pigs in accordance with FAO requirements for skin sensitization testing (Protocol BSR 7 / LO2). The following groups of animals were studied: pre-screening - 5 animals; negative controls - 4 animals; positive controls treated with 0.1% 2,4-dinitrochlor benzene in 80% aqueous ethanol - 6 animals; experimental animals treated with the preparation according to the invention - 10 animals.

Preliminary screening was performed five times a week for 8 hours with drug administration. Reported * 4

• · · «W ··· Skin erythema and skin edema at the end of exposure and at 24 hours.

An induction study was performed and the drug was administered on the first day for 24 hours, then three times weekly for 8 hours for three weeks. Skin erythema and skin edema were reported.

The induction with the positive control was performed in the same way. After two weeks, the preparation is applied. The negative control group received an authoritative dose of the preparation without prior induction. Duration of exposure is 24 hours. Animals are examined after one week with the authorizing dose. The reading is at the 24th and the 48th hour after the appropriate permitting doses have been applied.

Examination of skin sensitization of a concentrated oral prophylaxis preparation according to the invention shows the absence of positive skin reactions after twice the authoritative doses.

The preparation does not show contact activity when testing white guinea pigs according to the FAO procedure.

Claims (4)

Patent Claims 1. Composition for preparation for hygiene, prophylaxis and treatment of oral cavity on the basis of hydrogen peroxide, zinc dichloride and ethanol, characterized in that it also contains tyloxapol - polymer of tertiary oxyethylated octylphenol formaldehyde, as well as tartaric acid in the following quantitative proportions % by weight: Wes' · hydrogen peroxide by 0.5 TO 2.0 zinc dichloride by 0.02 TO 0 , 40 tyloxapol - polymer of tertiary ethyl octylphenol formaldehyde by 0.03 TO 0 , 07 tartaric acid by 0.01 TO 0 , 03 ethanol by 2.5 to 5.0 up to 100 deionized water and flavors, odor and stability additives. Composition according to claim 1, characterized in that the hydrogen peroxide is preferably from 0.5 to 0.7% by weight and the zinc dichloride is from 0.02 to 0.04% by weight. Composition according to claim 1, characterized in that the hydrogen peroxide is preferably from 1.4 to 1.6 wt.% And the zinc dichloride from 0.55 to 0.65 wt.%. 4. Composition of preparation for hygiene, prophylaxis and treatment of the oral cavity, as given in the description and examples of implementation.