RU2103990C1 - Composition for care of mouth cavity - Google Patents

Abstract

FIELD: packed compositions for care of mouth cavity, more particularly tooth pastes. SUBSTANCE: claimed composition comprises halogenated diphenyl ether such as triclosane, stabilizing terpene or aromatizing agent, polyphosphate agent, fluorine ion source, and polycarboxylate. EFFECT: prevention of formation of deposit and caries. 6 cl

Description

 The invention relates to packaged plaque-preventing oral (oral) compositions containing plaque-preventing antibacterial agent, such as 2 ′, 4, 4′-trichloro-2-hydroxydiphenyl ether (TCGE) as an effective plaque-preventing agent . Such compositions are enclosed in a container made of a polymer plastic material in contact with the oral composition, which plastic is compatible with the antibacterial agent of the composition. Although various plastics can reduce the anti-plaque effect of the mentioned antibacterial agents, nevertheless certain plastics, such as polyfluoroethylene and polyvinyl chloride, have been found to be compatible with TCGE. It was found that these plastics do not cause excessive loss preventing the formation of plaque and antibacterial activity of the oral compositions contained therein during storage at room and elevated temperatures. Even if the plastic parts of the container’s plastic are made of plastics that are not completely compatible with the antibacterial compound, compatibility can be improved by incorporating stabilizing amounts of the stabilizer of the antibacterial compound, such as terpen, for example limonene or essential oil (natural or synthetic) into the composition, which can be present in the flavoring element of the oral composition.

 Such a stabilizer is present in sufficient quantity, so that the oral composition in packaged and prepared for use form is an effective anti-plaque composition, the preparation of which is the aim of the invention. Included within the scope of the invention is a method for contacting intraoral surfaces with oral compositions containing an effective amount of an anti-plaque agent. A toothbrush is also included in the scope of the invention, containing on its bristles an effective amount of anti-plaque dentifrice.

 Plaque is believed to be the cause of negative periodontal conditions, as well as the precursor of tartar. Plaque can form on any part of the tooth, including the edges of the gums. Plaque makes teeth blunt and, in addition to promoting the formation of tartar, is considered to be the cause of gingivitis. Thus, oral compositions containing a plaque-preventing component that prevents or inhibits the development of plaque on teeth are valuable dentifrices.

 Although it was known that antimicrobial agents in oral compositions can sometimes reduce plaque in combination with other substances, nevertheless, the most diverse such antibacterial compounds have disadvantages that interfere with their use in oral compositions. For example, cationic antibacterial compounds, such as quaternary ammonium halides, tend to discolor teeth and may be inactivated by the presence of anionic substances in oral formulations (and it may often be desirable to use anionic surfactants or detergents in oral formulations).

 Essentially water-insoluble halogenated (and often hydroxylated) diphenyl ethers, such as TCHE (triclosan) and 2, 2'-dihydroxy-5,5'-dibromodiphenyl ether (DDDE) are effective in preventing plaque formation by antibacterial agents, but can be deactivated by non-ionic surfactants and many plastics, which was discovered by the applicants.

 The purpose of the invention is the introduction of antibacterial plaque-preventing agents, such as halogenated diphenyl ethers, in particular TCHE and DDDE and the like, in oral compositions, storing such compositions and removing them from packaging or containers in which the compositions do not lose in storage a noticeable degree of activity as anti-plaque agents before intended use.

 In the known triclosan-containing dentifrices extracted from the respective metering devices, the intake of triclosan occurred in quantities insufficient to significantly reduce plaque when using the agent once or twice a day in an amount of 1.5 g / time with a one-minute brushing a brush, which is considered a common rough brushing practice. To be effective, such a practice must result in at least a 25% reduction in plaque as a result of its three-week use compared with the use of a control toothpaste in the same way for three weeks.

 The most recommended antibacterial anti-plaque component present in packaged compositions is TCGE, also known as triclosan. Triclosan is described in US Pat. No. 4,022,880 as an antibacterial agent in combination with a stone formation preventing agent (producing zinc ions), as well as in the German Patent Specification (OLS) 35 22 860 in combination with a copper compound. In addition, triclosan is described in European patent applications 0161898 and 0161899 and in European patent application 0220890 as a dentifrice in a mixture with polyethylene glycol and an oil based fragrance.

 Many oral compositions or preparations are known, including pastes, gels, powders, liquids, tablets, lodgis, dentifrices in bags and sachets, liquid and tablet mouthwashes, and also dentifrices used for therapeutic purposes ( such as dentifrice compositions, for example fluoride solutions). Such products are packaged in crumpled tubes, pump dispensers, pressurized dispensers, sachets, bottles, containers and other containers. Although the deformable or crushable tubes were originally made from metals such as lead or aluminum, the bottles were made from glass. In recent years, such containers have often been made from synthetic organic polymer plastics or from laminates including such plastics. It is known that, between oral compositions and the materials into which they are packaged, an interaction occurs, for example, the reaction of toothpastes with aluminum containers, and the containers were specially treated to prevent such reactions or other materials were used to make them. However, prior to the creation of the present invention, it was not known in the prior art about the adverse effects of individual plastic packaging materials on plaque-preventing activity of halogenated diphenyl ethers used as antibacterial agents introduced into oral compositions and packaged in containers in which they are in contact with such plastics . The prior art did not suggest that it was known that such plastics could be used to make frequent containers without losing the plaque-forming activity of halogenated diphenyl ethers or losing the same activity with oral compositions packaged and in contact with “reactive” plastics that react absorb or otherwise reduce plaque-inhibiting activity of the oral composition through inhibition or elimination tion steps plastics introduction terpenes, such as limonene or other flavoring components for oral preparation.

In accordance with some of its aspects, the invention relates to an oral composition comprising an effective plaque-preventing amount of a substantially water-insoluble non-cationic antibacterial agent. The composition is packaged in a dispensing container made of a material comprising a solid polymer material, such as a synthetic organic polymer plastic in contact with the oral composition, and such a polymer material is compatible with the antibacterial affinity in the oral composition and causes excessive loss of antibacterial and anti-plaque activity oral composition when stored in a container (for example, at 20-40 ^o C for several weeks, preferably up to a year and or more). A packaged oral composition is typically a toothpaste, gel cleaner or mouthwash enclosed in a deformable dosing tube, pumping dosing device or bottle, respectively, without plastic parts adversely affecting the prevention of plaque formation the action of an antibacterial agent (which is preferably a halogenated diphenyl ether, such as triclosan), or the oral composition comprises exponentials, inhibits or prevents any such unwanted "reaction between the antibacterial agent and any plastic part of the container, which otherwise could have undesirable effects on the antiplaque activity of oral compositions.

 A product for packaging a toothpaste-preventing plaque consists of a tube for toothpaste in which a toothpaste-preventing toothpaste is shown, shown in a single amount, for example 0.8-2 g, by extruding onto a brush. The tube is opaque and made of synthetic organic polymer plastic, such as polyfluoroethylene, or coated with a material, for example, in the form of a laminate, which does not adversely affect the formation of plaque during storage. Or the tube is made or lined with plastic, for which an adverse effect on the activity of toothpaste preventing the formation of plaque was found (by a decrease in the prevention of plaque formation and the antibacterial effect of the halogenated diphenyl ether included in the toothpaste), but in this case an adverse effect on the prevention of dental formation plaque activity is eliminated or inhibited by the introduction of a stabilizer into the dentifrice, which can be tolerated , for example, limonene or another effective fragrance component. It is recommended that neither the tube for the toothpaste, nor the cap to it, nor any other part of the tube that may come into contact with the toothpaste (for example, the lining of the cap) be made of a copoly (complex) ether / poly copolymer (simple) ether or other plastic material that significantly reduces the prevention of plaque formation of the oral composition even in the presence of a stabilizer to prevent the formation of plaque component of the composition. It is also considered desirable to avoid the presence of other elastomers, such as isobutadiene, polychloropropene, butadiene rubbers and nitrile rubbers, which can react with or adsorb to TCE. It is advisable to make such parts from plastics that do not adversely affect plaque-preventing activity even in the absence of terpenes or other stabilizers in the dentifrice, but other such destabilizing plastics can still be used if the toothpaste has a stabilizer that counteracts the deactivating effect of the plastic (excluding elastomeric copoly (ester / poly (simple) ethers and other undesirable elastomers, which are recommended to be avoided t).

 The lining of the cap can also be polyfluoroethylene, as a result of which all surfaces in contact with the toothpaste during storage are compatible with the halogenated diphenyl ether, the antibacterial component of the toothpaste, and do not promote excessive losses of toothpaste activity that prevent the formation of plaque during storage. The inner side of the wall of the laminate can be not only polyfluoroethylene, but also polyethylene, and the wall can be made of polyethylene or another acceptable polymer.

 The ready-to-use infusion dispensing device contains toothpaste in a compartment bounded by a lower wall and a membrane. The weakening of the movable lever causes a downward movement of the membrane with the extrusion of the paste through the tube and neck. With the cessation of pressure on the movable lever, the elastic membrane returns to its original state and returns the tube and lever to their original positions. At the same time, the bottom is pushed up under the influence of atmospheric pressure. A variety of internal parts of the pump dispenser in contact with toothpaste are recommended to be made of plastic (s) that do not cause deactivation of the halogenated diphenyl ether used as an antibacterial and prevents plaque formation. However, if it is impossible to use plastics having the necessary physical properties required for the contacting parts and at the same time compatible with plaque-preventive agents, other plastics can be used, provided that the composite toothpaste (or gel cleanser) includes a stabilizer such as limonene or other applicable terpene, or a fragrance component. Nevertheless, it is considered better to avoid elastomeric copolymers of (ester) / poly (simple) ethers, especially for the manufacture of an inflating membrane, the plastic material of which is apparently particularly active against TCE in oral compositions of the type described.

 A bag or bag in the form of a heat-sealed unit soldered on three sides, the fourth side is formed by simple bending of the material and does not require soldering. Inside the sealed bag is an oral composition, for example a toothpaste, and the inner surface of such a bag is made of plastic that does not promote excessive loss preventing plaque formation of the antibacterial compound contained in the oral composition in the bag. As for other containers that prevent the formation of plaque in oral compositions, in this case, laminates with an inner plastic layer that do not adversely affect the antibacterial agent can be used or, if plastic still has such a negative effect, the presence of an oral composition of an acceptable stabilizer, which is also recommended as a flavoring agent.

 The opaque bottle has a sealing cap. Both the bottle and the seal in the cap are made of plastic materials that are compatible with TCHE, that is, they prevent the formation of plaque by the component of the mouthwash contained in the bottle. As with the other examples given, when using “reactive” plastic as the material of the inside of the bottle or cap seal to prevent excessive loss of plaque-preventing activity of TCE or other halogenated diphenyl ether, an acceptable stabilizer must be present in the mouthwash.

 In addition to the compositions cited as examples of filling the described packages and including gel cleansers and thick liquids instead of toothpaste, such packages may also contain dental treatments suitable for professional purposes, such as tooth hardeners, which may include fluorides and phosphates, mixtures and antibacterial agents, stain solutions for plaque indications, and other suitable oral compositions. In addition, pressurized or “aerosol” compositions containing said plaque-preventing compounds can be enclosed in pressure-resistant containers (the pressure in which is usually generated by nitrogen gas) provided that the contacting plastic parts of the container are made of a material that does not cause excessive losses preventing the formation of plaque activity of the corresponding funds contained in toothpaste or other oral composition.

 In addition to the various containers mentioned above, crushable bottles, capsules, cans, sponge-like media and various types of mechanical dispensing containers can also be used. Since some halogenated diphenyl ethers used as antibacterial agents are sensitive to the action of light, it is sometimes desirable that such containers be composed, coated or layered with a material shielding from chemical or physical radiation, many of which are known, in order to protect the oral composition and prevent plaque formation compound from exposure to deactivating radiation, such as UV radiation. In addition, it is often desirable that such containers be opaque to photochemically active radiation that deactivates the plaque-preventing component contained in an oral preparation, for example, toothpaste.

The reason for the decontamination by plastic of HCHE and other non-cationic antibacterial agents, which give oral compositions properties to prevent the formation of plaque, has not yet been elucidated. The studies cited to date have not clearly identified the mechanism responsible for the loss of such desired activity, however, the results indicate, but not conclusively, chemical reactions or physical absorption. Tests of basic mouthwash or mouthwash formulations that have been aged in dosing containers at room temperature, 38 ^° C and 49 ^° C for twelve weeks, result in "excessive" losses (more than 25% of the initial concentration of TCE) in contact with the mouthwash mouth with the walls and parts of the container made of low density polyethylene, high density polyethylene, polyethylene terephthalates, polypropylenes, nylons, polyallomers and polymethylpentenes. Similar high losses are observed when stored in containers with inner walls or parts of elastomeric copoly (ester) / poly (simple) ethers of the type previously used by Criaba for the manufacture of inflated membranes. It has been found that polyfluoroethylene, such as polytetrafluoroethylene, polyvinyl chloride, polycarbonates and polysulfones, do not absorb and does not react with excessive amounts of TCGE. However, polycarbonates and polysulfones are fragile and therefore often unsuitable for the manufacture of parts of metering containers. Polyvinyl chlorides sometimes give an off-flavor to oral compositions, except in some cases where the flavor is compatible with the flavor of the odorant used in the toothpaste. Thus, of all available polymeric materials, only polyfluoroethylene is recognized as a material for the manufacture of containers and packages, which do not significantly reduce the formation of plaque activity of the respective agents. However, as mentioned earlier, the introduction of oral plaque stabilizers to prevent the formation of plaque, such as terpenes, for example limonene, essential oils (often containing terpenes) and other fragrance components with similar stabilizing properties, can reduce the loss of activity preventing plaque formation means in contact with the container or parts of the container made of the various mentioned polymer plastics, causing large losses preventing development of tartar activity. Thus, if the oral composition contains a stabilizing amount of terpene or another acceptable “stabilizer”, polyfluoroethylene can be independent of the material used to make the dosage containers. In the case of the presence of a stabilizer in the oral composition or if polyfluoroethylene (as well as polyvinyl chloride, polycarbonate or polysulfone) is the only polymer material in contact with the oral composition, the loss of plaque-preventing storage activity is less than 25% and preferably should be less than 10% when room temperature and even at higher temperatures, for example at 20-40 ^o C, for several weeks and up to a year or more. It is believed that the most stable oral formulations are those formulations which include a stabilizing amount of terpene or other acceptable stabilizer and which only come into contact with parts of the container made of either polyfluoroethylene (or any other non-reactive plastic).

 Although terpenes and essential oils are the first among the stabilizers of this invention, other perfume components can also contribute to the stabilization of a substance that prevents the formation of plaque, either by interfering with destabilizing reactions, or by inhibiting halogenated diphenyl ether with plastic (or otherwise unknown mechanism).

 Thus, a theory has been proposed according to which components are present in the oral composition that are prone to solubilization of TCE, and its retention in the oral composition and the prevention or inhibition of its migration into plastic. On the other hand, a theory has been put forward that such a solubilizing effect can promote the migration of solubilized TCGE into plastic.

 In addition, although it is desirable that terpenes and other stabilizers are components of a perfume, this condition is optional, and stabilizers can be used only for stabilization purposes.

Although it is recommended that the packaging of this invention have internal walls in contact with the compositions made or lined with hard synthetic organic plastic, the scope of the invention also covers the use of other solid (and / or film-forming) polymeric materials, whether or not related to synthetic, organic and even plastic materials. Thus, there may be used polyethylene glycols and methoxypolyethylene type Carbowax ^®, such as Carbowax 4000 and Carbowax 600, often as lining material dispensing containers of the described compositions. Inorganic silicone polymers, such as siloxanes, as well as natural organic film-forming materials, such as gums, for example carrageenan, tragacanth, karaya are also suitable for lining dispensing containers. In addition, solid polymer products, such as cellulose, starch and their derivatives, are also useful as container materials in contact with the antibacterial and plaque-preventing components of the packaged oral compositions of the invention.

 The various oral packaged compositions of this invention that are made most frequently are toothpastes, gel-type dentifrices, and mouthwashes (often referred to as mouthwashes). The first two compositions will be called dentifrices, and the last - mouthwash. Dentifrices include three main groups of components: a carrier, a polishing agent, and a surfactant (or detergent). An antibacterial agent, for example, halogenated diphenyl ether, is usually present in a carrier, which is usually 10-80% (all figures are in terms of the final composition) of a dentifrice. The carrier contains 3-40% water, 7-77% moisturizer, such as glycerin, sorbitol, propylene glycol and mixtures thereof, as well as 0.5-10% of a gel-forming agent, such as sodium carboxymethyl cellulose, Irish moss, yotacarraginan, hydroxyethyl cellulose etc., including mixtures thereof. The polishing material of the dentifrice is usually 10-75% in gel or toothpaste and 50-99% in powder, and such polishing agent may be colloidal silica, precipitated silica, sodium aluminum silicate, insoluble sodium metaphosphate, hydrated alumina, calcined alumina, dicalcium phosphate dihydrate, anhydrous dicalcium phosphate, calcium carbonate and other known substances or mixtures thereof. Surfactants include anionic, neionic, cationic and zwitterionic surfactants, however, the use of nonionic surfactants is often avoided due to their undesirable effect on antibacterial compounds, for example, TCE, just as the use of cationic and zwitterionic surfactants is often avoided. active substances due to their tendency to stain and blacken teeth. Thus, synthetic organic anionic surfactants, which are both detergents, are recommended cleaning agents in dentifrices, of which sodium lauryl sulfate and other sodium (higher) alkyl sulfates with 10-18 carbon atoms in alkyl are preferred, although they are can be replaced with other well-known sulfated and sulfonated detergents, at least in part. Other active ingredients, such as fluoride-ion-supplying compounds, for example sodium fluoride and sodium monofluorophosphate, may be present for the purpose of tooth rejection, usually in amounts that provide 0.001-1% fluoridione, and other excipients may also be used. such as flavoring and sweetening agents in an amount of 0.1-10%. In addition, it may be desirable to use in an amount of 0.5-4% polycarboxylate, such as a copolymer of polyvinyl methyl ether with maleic anhydride (PVM / MA, Gantrez). Such a polycarboxylate has been found to significantly improve the anti-plaque effect of the antibacterial agent. The use of such a polycarboxylate in oral compositions is described in US Pat. No. 4,627,977, which is incorporated herein by reference.

 In mouth rinses, an aqueous or alcoholic oral carrier is recommended where the alcohol is ethanol or isopropanol. The carrier is usually present in the composition in an amount of 90-99.9%, of which 5-30% is alcohol, and 2-10% is propylene glycol in terms of the final product. The rest of the composition, i.e. 0.1-10%, may include perfume, a surfactant, a sweetener to prevent plaque affinity, and other special purpose adjuvants. In dentifrice and mouth rinse compositions, an effective amount of an antibacterial and plaque preventing agent is typically in the range of 0.02-0.2%, more preferably 0.03-0.1%, in a mouthwash, typically 0.25 -1%, more preferably 0.25-0.5% or 0.6%, where the amount of TCE does not exceed 0.8% in toothpastes and 0.2% in mouthwashes (at higher concentrations, numbness of the mouth is possible ), but not below the specified limits, in order to avoid inefficiency in preventing the formation of plaque and low concentrations. It is recommended that the dosed compositions contain plaque and TSHE in the specified range, and with an initial concentration of the agent within the specified range, a loss of activity of 25% may be considered acceptable, and such dosed compositions are encompassed by the scope of this invention.

 To stabilize oral compositions packaged in containers with plastic walls or parts, and such plastic is plastic that is "reactive" with respect to antibacterial compounds, the presence of 0.01-2% terpene (s) or stabilizer (s) in oral compositions is desirable ), preferably 0.05-1% and more preferably 0.1-0.5%. Such stabilizers may be present in acceptable flavors for dentifrices, administered as desired (and often their presence is desirable), and the stabilizer is present in the fragrance in an amount of at least 5% per fragrance, preferably at least 10% sea, more preferably at least 25% and most preferably at least 50%.

 Although all of the above applies primarily to dentifrices and mouth rinses, other oral compositions (e.g. chewing gums) of the invention contain similar amounts of components depending on the form of the composition (liquid compositions, such as a mouth rinse, contain less and thicker, such as toothpastes, contain more), often with the addition of specific substances that meet the purpose of such compositions. Thus, dentifrice compositions may include fluorides and phosphates, such as potassium or sodium fluoride, or sodium fluorophosphate, both in dentifrices and in mouthwashes, often in the range of 1-5%. Coloring solutions to indicate plaque may include an acceptable colorant (red is the best color for such products) often at a concentration of 0.001-0.1% on the basis for rinsing the mouth. The composition of other products can be set accordingly according to principles known to the specialist.

An antibacterial agent is a non-cationic substance, insoluble in water or practically insoluble in water (with a solubility in water at 25 ^° C. of less than 10 g / l, sometimes less than 1 or 0.1 g / l). Such substances are soluble or dispersible in a dentifrice carrier containing glycerin, sorbitol and / or propylene glycol, as well as in the final product with such an environment as a base. They are also soluble or dispersible in an aqueous-alcoholic medium for rinsing the mouth.

 In antibacterial agents, such as halogenated diphenyl ethers, bromine and / or chlorine are usually present, of which chlorine is the preferred halogen. It is recommended that such agents be substituted with 1-3 hydroxyls and 1-4 halogen atoms. More preferred is the substitution of 1 or 2 hydroxyls and 2 or 3 halogen atoms, preferably four substituents, two in each ring. Among the most recommended such compounds are 2,2'-dihydroxy-5,5'-dibromodiphenyl ether and 2 ', 4', 4-trichloro-2-hydroxydiphenyl ether (TCHE), of which the latter is most preferred. If necessary, the halogenated diphenyl ethers can be completely or partially replaced by various halogenated phenolic non-cationic, substantially water-insoluble compounds with antibacterial and plaque-preventing properties, the list of which is given on page 2-8 of S. N 07/398566, registered 25 August 1989, which is introduced into the present description by reference.

 Terpenes (in this description this term includes terpene hydrocarbons and their oxygenated derivatives) include compounds such as: d1-limonene, menthol, diterpenes, polyterpenes and their derivatives, many of which can be found in essential oils and other aromatic additives. In addition to their usefulness as stabilizers of halogenated diphenyl ethers, they also give the desired flavor to the oral compositions of the invention. Among terpenes and their derivatives, limonene is considered to best combine both properties, although other terpenes, including those that do not have aromatic properties, are also applicable, as are other emulsifiable lipophilic essential oils and flavorings containing stabilizing components.

 Various plastics, previously described as components of containers and (or) parts of the dispenser, their chemical nature and degree of polymerization are well known and do not require detailing in this description. If more details are needed, you can refer to the Modern Plastics Encyclopedia, annually produced, McGraw Grae Hill Inc., pc. New York, New York.

 As indicated in S. N 07/398566, incorporated by reference, the compositions of the invention may contain a fluoride ion source capable of delivering 25-5000 ppm of fluoridion to the oral cavity, preferably 300-2000 ppm, and more preferably 800-1500 h / million For further details on acceptable fluorides, their amounts and preparation details, see US Pat. No. 4,627,977, incorporated by reference. Fluoride is primarily necessary for curing teeth, but may also serve to stabilize the polyphosphate compound, which may be present as an anti-calculus agent. As such a polyphosphate, a mixture of sodium and potassium pyrophosphates is recommended, which is also stabilized using the Gantrez S-97. Intervals of the amounts used are given in US, S N 07/398605, registered August 25, 1989, which is introduced in this description by reference, as well as in US patent 4627977 and in US patent 4806340, also introduced by reference.

 For other details of the compositions, components, auxiliary additives, production and use, see the aforementioned patents, descriptions and applications, which are incorporated by reference.

The preparation of the described oral compositions can be carried out by any standard method for the preparation of this class of compositions. We give an example of a simplified scheme of this method. TCGE is dispersed and / or dissolved in a dentifrice carrier; terpene is present in a flavoring agent. To obtain a dentifrice, a carrier is prepared containing glycerin, sorbitol and propylene glycol, a gel-forming agent and acceptable excipients (including Gentrez ^® S-97 and triclosan), mixes the carrier and an aqueous solution of anionic detergent (sodium lauryl sulfate or a mixture of sodium lauryl sulfate and sodium metaloxyltaurate) and a polishing agent is mixed with the resulting mixture. Finally, the terpene flavoring is dissolved in ethanol, mixed and the pH adjusted. Upon receipt of the mouthwash, its various components are simply mixed with alcohol or a hydroalcoholic medium and mixed until completely dissolved. As a surface-active component of a dentifrice, a mixture of sodium lauryl sulfate (VAT) with sodium methylcoxyl teuret (in the ratio from 1: 4 to 4: 1) is recommended, and the presence of teuret can accordingly reduce the amount of VAT, which is desirable. Other oral compositions are prepared in similarly appropriate ways.

 When packaging an oral composition in dosage containers, it is advisable to avoid contacting the compositions with plastic parts from an elastomeric copolymer (ester) / poly (simple) ether, as well as contacting any such compositions not containing a stabilizer (e.g. terpene or perfumes containing it) with plastic parts made from plastics previously listed in the description as being reactive with TCE and other antibacterial and anti-plaque compounds. It is especially important to avoid manufacturing the aforementioned plastic parts in storage tanks or other containers, pipes, pumps or equipment in which the oral composition may be present for appreciable periods of time or shorter periods of time at elevated temperatures.

But even if it is possible to avoid the contact of packaged compositions containing TCGE or other halogenated diphenyl ethers as antibacterials with reactive plastics in the manufacture of the composition, it is still desirable to minimize the effect on such packaged compositions of light and heat, since, as it was found, both type of exposure accelerates the loss of plaque-preventing activity. So, the compositions of the invention are recommended to be stored and packaged in opaque containers and dispensers at 10-38 ^o C and stored at the same temperature. In this case, the packaged compositions can be stored and used in the usual way while maintaining their intended anti-plaque action. This effect has been verified by laboratory testing and dental observation of volunteers using a variety of packaged formulations and control formulations as directed. At the same time, there is a significant improvement in the prevention of plaque activity of the packaged compositions of the present invention compared to the control packaged compositions in which the package included plastic parts made of “reactive” with respect to the halogenated diphenyl ether of plastics used as an antibacterial agent, as well as in the absence of oral stabilizer composition. Such improvements are also found if packages made from "reactive" plastics (but not from elastomeric copolymers of (esters) / poly (ethers) esters) are used with oral compositions containing no terpenes and flavoring agents.

The following examples illustrate the invention, but without limiting it. Unless otherwise indicated, all percentages and ratios in the examples, description and accompanying claims, and the temperature is given in ^o C.

 Example 1

Component%
Water (deionized) - 47.85
Sorbitol (70% aqueous solution) - 20.00
Ethanol (95% aqueous solution) - 12.50
Glycerin - 10.00
Propylene glycol - 7.00
^* Gantrez S-97 (13% solution) - 1.92
Sodium hydroxide (50% aqueous solution) - 0.12
^** Teuranol - 0.20
Sodium Lauryl Sulfate - 0.25
^*** Flavoring mixture - 0.12
^**** Triclosan (Irgazan ^® DR 300, manufactured by SIBA-Geigy) - 0.05
Total - 100.00
^{* A} copolymer of polyvinyl methyl ether with maleic anhydride (GAF Corp.),
^** Sodium Methylcokyltaurate
^*** Contains at least 25% terpenes, including at least 25% limonene
^**** TCHGE (2 ', 4, 4'-trichloro-2-hydroxydiphenyl ether).

 The mouthwash (mouthwash) in this example is obtained by mixing the various components from the above list in any suitable order in accordance with the standard method, but it is recommended to first dissolve triclosan in a mixture of propylene glycol and ethanol, and then mix with an aqueous solution of sorbitol, glycerol and anionic surfactants, the latter add a flavoring mixture. The sodium hydroxide solution is used to neutralize the resulting acidic mixture to a pH of 6.84 (it is desirable to have a product with a neutral pH value or close to this value).

 The resulting mouthwash has excellent cosmetic stability, has an acceptable taste and smell, triclosan and perfume are satisfactorily dissolved, which can be partially attributed to the presence of Tauranol USHF.

If only 0.25 VAT is used as the anionic surfactant, the solubilization of the flavoring and triclosan is not entirely satisfactory. Although solubilization can be enhanced by using large amounts of VAT, its maximum limit in mouthwashes is often only 0.25%, but the mixture of Tauranol ^® WSHP and NLS is safe and acceptable in the amounts used. The described mouthwash is tested in vitro for the bioavailability of triclosan compared to a similar mouthwash, but without Tauranol WSHP in one case and with its replacement with half the amount of non-ionic surfactant (Pluronic F-127) in another case. In tests for the absorption of triclosan by measuring the absorption of triclosan with saliva-coated hydroxypatite disks and in tests for protein absorption in the “inhibition zone”, it was found that the presence of a mixture of anionic surfactants leads to a comparable bioavailability of triclosan compared to bioavailability when present in the composition VAT only, and this availability is significantly higher for formulations that do not contain a non-ionic detergent compared to formulations in which a non-ionic detergent is present (Pluro IR ^® F-127).

The mouthwash of the present example is subjected to aging at an elevated temperature (41 ^° C.) for three and five weeks, which is believed to be equivalent to real aging, for at least six months and a year at room temperature. Such aging tests are carried out in dosing containers (bottles) made of glass, polyvinyl chloride and polyethylene terephthalate (or lined with plastic). Although a chemical analysis of the mouthwash after the indicated aging periods did not show any loss of triclosan from the mouthwash in a glass bottle, the loss of triclosan from the mouthwash was noted for bottles of polyethylene terephthalate and polyvinyl chloride, but they are significantly lower than the permissible 25% (of the initial concentration), and may be below 5 or 10%.

 If dI-limonene in the amount of 0.1, 0.2 and 0.4% is used instead of the flavoring mixture, even better stabilization of triclosan in the described packaged dentifrices is achieved, a similar stabilization is observed in the presence of other terpenes from various essential oils and flavorings in similar amounts. The same good results are achieved if the container material or the lining material is polymethylpentene, polyallomer, polypropylene, low and high density polyethylene and nylon, although the same materials in the absence of a flavoring mixture (and terpenes contained in it) cause significant and excessive losses of incoming from mouthwash triclosan, especially at elevated temperatures.

 Example 2

Component%
Water (deionized) - 84.42
Ethanol (95%) - 10.00
Propylene glycol - 5.0
Sodium lauryl sulfate - 0.5
Triclosan - 0.06
Sodium saccharin - 0.02
Total - 100.0
The mouthwash of the above composition is tested for the intake of triclosan after storage for three weeks in dosing containers made or lined with various plastics. The tests are carried out at room temperature, 38 ^o C and 49 ^o C, where storage at elevated temperatures simulate longer periods of storage (up to a year or more) at room temperature. Losses of triclosan from a mouthwash during storage of more than 25% were noted for containers of polymethylpentane, polyallomer, polypropylene, high and low density polyethylene and nylon with unacceptable results (excessive losses) for containers of polypropylene, polyethylene and nylon (for nylon worst results).

If the material or the lining of the container is a material of polyvinylchloride, polycarbonate, polysulfone or polyfluoroethylene, for example polytetrafluoroethylene or Teflon ^® , essentially no loss of triclosan occurs. Loss of triclosan from mouthwashes stored in containers made or lined with the indicated polymers (polymethylpentene, etc.) can be reduced in the same way as in example 1, i.e. the introduction of mouthwash limonene, other terpenes or essential oils containing them in an amount of preferably at least 0.1% and more preferably higher, for example, 0.2% or 0.4% in terms of the final composition. In some cases, even the use of a flavoring agent that does not contain significant amounts of terpenes can have a positive effect, although it cannot be expected that this effect will be as noticeable as in the case of the presence of terpenes in the compositions.

 Example 3

Component%
Propylene glycol - 10.00
Iota Narraginan - 0.75
Sodium Fluoride - 0.33
Sorbitol (70%) - 30.00
Sodium saccharin - 0.30
Titanium Dioxide - 0.50
Sodium hydroxide (50% aqueous solution) - 0.80
Water (deionized) - 27.71
Luviform TM (35% solution) - 4.76
⁺⁺ Zeodent TM 113 - 20.00
⁺⁺⁺ Sident TM 22 - 2.00
Sodium lauryl sulfate (94% activity) - 1.60
Fragrance - 0.95
Triclosan - 0.30
Total - 100.00
⁺ Copolymer of polyvinyl methyl ether with maleic anhydride (WASF Corp.)
⁺⁺ Oxidized-polishing agent (J.M. Huber Corp.)
⁺⁺⁺ Oxide-floss thickener (Degussa Co.)
The dentifrice of the above composition is prepared in the usual way and used as a medium in tests for the stability of triclosan when exposed to a triclosan-containing agent of various plastics, used as material for containers or dispenser parts in which the dentifrice is stored or from which it is dispensed. Test plastics include Pibiflex TM 46 from Inmont and Arnitel TM modified by AKZO, used for the manufacture of membranes and bellows for the inflator. Six plastic specimens were tested, of which every three were treated with various mold release agents (to determine the effect of the mold release on the stability of triclosan in contact with plastics during storage). Lubricants for molds are silicone master TM (5% silicone oil and 95% polypropylene). Silicone Master plus silicone oil (with a predominance of silicone oil) and Armid 0 Master TM (5% oleoamide and 95% polypropylene), respectively. After storing samples for two weeks in contact with the dentifrice at various temperatures (room temperature, 38 ^o C and 49 ^o C), the dentifrice is removed from the material of the plastic container, the plastic is washed with water and immersed in methanol to dissolve triclosan, which could be Captured by plastic during storage. The methanol solution is collected and analyzed using high performance liquid chromatography. It was found that the same type of absorption of triclosan by different membrane materials actually takes place, and although variations are possible, to some extent depending on the form lubricant used, nevertheless, in almost all cases the same results were obtained. It has been found that elastomeric copolymers (ester) - ether / poly (ethers) esters absorb significant amounts of triclosan from dentifrices, and this conclusion is confirmed by the use of elastomeric copolymers (esters) / poly (ethers) for the manufacture of bellows pumping dispensers containing the described dentifrice and other dentifrices within the scope of the invention. Accordingly, it is considered undesirable to use elastomeric copolymers (ester) / poly (ethers) in contact with the dentifrices or mouth rinses of the invention, even if these agents contain flavoring agents including terpenes (which are present in perfumes of dentifrices) in amounts at least 0.1% on a dentifrice.

 When repeating tests using real pumping dispensers from Guala for dentifrices with membranes made of elastomeric copoly (ester) ether / poly (ether) esters (Arnitel TM), the loss of triclosan is also unacceptable, but when replacing elastomeric copoly (ester) ether / poly (ether) ethers with other acceptable plastics, for example polyfluoroethylene, triclosan activity is maintained at an acceptable level. It was also found that other details of such an inflating dispenser, for example polypropylene inner walls, do not absorb excessive amounts of triclosan and do not seriously reduce the formation of plaque activity of the dentifrice, apparently due to the presence of a terpenes packaged dentifrice in the perfume.

 Group tests were conducted with at least ten people who used the dentifrice of this example, dosed from tubes lined with polyethylene terephthalate and polyethylene, with toothbrushing twice a day for a month, during which the appearance of plaque on the teeth of the subjects was observed by experienced by specialists. As a result of the tests, it was found that composite dentifrices have a certain anti-plaque activity similar to that also observed in the case of mouth rinses according to examples 1 and 2, which serves as additional evidence of the absence of unacceptable decontamination of triclosan, which continues to be present in a dentifrice in effective anti-plaque and antibacterial amounts.

 Example 4

Component%
Glycerin - 7.00
Propylene glycol - 3.00
Iota-Carrageenan - 0.75
Sorbitol (70%) - 30.00
Sodium saccharin - 0.30
Titanium Dioxide - 0.50
Sodium Fluoride - 0.33
Gantrez ^® S-97 (13% solution) - 15.00
Deionized Water - 16.07
Sodium hydroxide (50% aqueous solution) - 0.80
Zeodent ^® 113 (J.M. Huber Corp.) - 20.00
Silodent ^® 15 (oxide-silicon thickener, V.R. Grace Corp.) - 3.00
Flavoring Additive - 0.95
Sodium lauryl sulfate - 2.00
Triclosan - 0.30
Total - 100.00
The toothpaste of the above composition is stored in Guala pump dispensers with bellows membranes from Arnitel. The dentifrice is also filled with tubes of laminate with an inner layer of polyethylene terephthalate in contact with the dentifrice. Dentifrices are aged at 5 ^° C, 25 ^° C and 39 ^° C for two, four and six weeks. After the indicated periods of aging, dentifrices are dosed in an amount of 1.5 g / day, and triclosan content in dosed dentifrices is determined at weekly intervals. In the case of Guala pump dispensers, the dosed dentifrices lose about 27% of triclosan, which is excessive and must be rejected. The losses are approximately constant and do not depend on temperature and storage time, which can be explained by the absorption of triclosan by the metering membrane with which triclosan contacts before dosing. This membrane is made of an elastomeric copolymer of a (complex) ether-poly (simple) ether, i.e., plastic, which should be avoided as a container material or as a part of a container or dispenser for dentifrices containing triclosan. However, when replacing the elastomeric copolymer (ester) / poly (simple) ether with any of the previously indicated acceptable plastics, such as polyethylene terephthalate for the manufacture of a modified dispenser membrane (modified to compensate for the various properties of such plastics), the stability of triclosan increases, and the dosage composition is satisfactory and effective as a plaque-preventing toothpaste.

 Gel toothpastes in such packages behave similarly in terms of the stability of triclosan during storage and dosing.

 In similar tests using tubes lined with polyethylene terephthalate, slight losses of triclosan were noted (less than 5%), which indicates that the presence of terpenes is 0.1% or more on the composition), including limonene in the flavoring agent (or the flavoring itself additives), prevents the loss of triclosan or its deactivation. When using tubes of polyfluoroethylene, triclosan is lost in small amounts even if there is no flavoring agent in the composition, which is also true when using polyvinyl chloride as a facing material in contact with a dentifrice or when packaging parts made of polysulfone or polycarbonate come into contact with the same agent . However, as indicated earlier, it is not always possible to use the last three plastics.

 If in the described tests, in which the dentifrice is dispensed from Guala dispensers, Gantrez S-97, 4.76 parts of Luviform are replaced (35%) and with a difference with respect to deionized water, there are no special differences in terms of triclosan stability for different compositions not noted.

 In the above compositions, the polishing system is a silicon-containing system, not an alumina-based system. When replacing the polishing agent with aluminum oxide, the difficulties mentioned above, in connection with some plastics, are reduced, but still remain. And in this case, the presence of terpenes in the dentifrices promotes the stability of triclosan, as in the case of the presence of terpenes in similar dentifrice compositions based on silicon polishing agents.

 Example 5

 Means for rinsing the mouth and brushing the teeth according to the specified examples can vary in composition within ± 10% or ± 25% for each component, provided that these deviations do not fall out of the previously indicated intervals in the description and that in doing so they obtain applicable and effective antibacterial and anti-plaque-forming products dosed in an effective anti-plaque-forming state of said dispensing containers made of compatible plastics. Such products can also be modified by conversion to dentifrices in the form of a gel, oral gels, paste, liquid, lozengis, capsules, tablets and sachets of the types previously mentioned in the description. Such products will behave similarly with triclosan or other halogenated diphenyl ether, or with antibacterial anti-plaque agents, remaining sufficiently stable in the presence of polyfluoroethylene, polyvinyl chloride, polycarbonate and polysulfone as packaging materials or packaging details, even if they are not present in the compositions flavors and terpenes, as well as remaining stable in the presence of polyethylene, polypropylene, polyethylene terephthalate in, polyallomers, nylons and polymethylpentenes, as package materials, or parts thereof, provided the presence in the oral composition terpene, such as limonene, or a stabilizing flavor component. As with the previously discussed mouthwashes and brushing, due to excessive absorption or other undesirable effects on triclosan from the copoly (ester) / poly (ether) ether and other elastomers, the use of such materials is recommended to be avoided.

 Example 6

Obtain dentifrices of the compositions of examples 3 and 4, which are dispensed onto bristled toothbrushes after a month of storage at 30 ^° C. in crumpled tubes of toothpaste lined with polyethylene in one case and polyethylene terephthalate in another. The amount of toothpaste on the toothbrush is in the range of 0.8-2 g, but 1-1.5 g are preferred. At a dosage of 1.5 g, the amount of active triclosan in the toothpaste on the brush is about four milligrams (with decontamination of triclosan only 10%). During storage for a longer time or at a higher temperature or if during storage the dentifrice comes in contact with a destabilizing plastic in a larger volume, the packaged compositions may contain about 3 mg of triclosan in 1.5 g per brush. So, with 1 g of toothpaste on the brush, the amounts of triclosan in it are 2.7 mg and 2 mg, respectively. When the content of triclosan in the dentifrice is 0.25-0.6%, 2.2-8 mg of triclosan can be on the toothbrush if the decontamination of triclosan reaches 10-25%, and up to 9 mg in the absence of deactivation of triclosan.

 The described dentifrices are usually used in an amount of 0.8-2 g dosed on the toothbrush with each brushing. Teeth are brushed twice a day, in the morning and in the evening for a period of four weeks, after which there is a noticeable improvement in terms of preventing the formation of plaque in comparison with a control dentifrice that does not contain triclosan. The improvement in terms of preventing plaque formation is also noticeable in comparison with the perfume-free control (lack of terpene) containing triclosan in a dentifrice packaged in tubes lined with polyethylene and polyethylene terephthalate.

 The invention is characterized by illustrative examples and embodiments, but it is not limited to them only, since it is obvious that a specialist, having before this eyes this description, will be able to use its substitutions and equivalents without departing from the invention.

Claims (5)

 1. An oral care composition packaged in a dosage container containing an insoluble non-cationic antibacterial agent containing a halogenated diphenyl ether, in particular triclosan, the dosage container has surfaces consisting of solid polyethylene or polyethylene terephthalate polymer material that is in contact and incompatible with the antibacterial agent characterized in that it further comprises a stabilizer and / or flavoring agent, a polyphosphate agent, a source of fluorine ions, ikarboksilat with the following quantitative ratio of components, wt. Triclosan 0.02 1.00
Stabilizing terpene and / or flavoring agent 0.01 2.00
Polyphosphate Agent 0.1 3.00
Fluoride ion source 0.001 1.00
Polycarboxylate 0.5 4.00
2. The composition according to claim 1, characterized in that terpen is used as a stabilizer.  3. The composition according to claim 1 or 2, characterized in that limonene is used as a stabilizer.  4. The composition according to claim 1, characterized in that as the polyphosphate agent using tetrasodium or tetrapotassium pyrophosphate or mixtures thereof. 5. A composition according to claims 1 4, characterized in that the fluoride ion source delivers a fluoride ion concentration of 5,000 million 25 ^{- 1.}  6. The composition according to PP.1 to 5, characterized in that as polycarboxylate use polyvinyl methyl ether, maleic anhydride or an acid copolymer.