RU2248787C2 - Compositions for dental care - Google Patents

Abstract

FIELD: medicine, stomatology.

SUBSTANCE: the present innovation deals with taking care of one's mouth cavity. The suggested composition contains a silicone polymer, silicone resin, nonvolatile liquid polysiloxane and, also, an active substance for taking care of mouth cavity, a volatile solvent of either organic or silicone origin at its boiling point being 200 C, or lower at the pressure of 1 atm. This composition provides prolonged release of active substance.

EFFECT: higher prophylactic and therapeutic action.

18 cl, 8 ex, 8 tbl

Description

Technical field

The present invention relates to oral care compositions that contain a silicone polymer, silicone resin and liquid silicone, and to the use of such compositions for the care and surface treatment of hard and soft tissues of the oral cavity. In more detail, the present invention relates to silicone compositions for caring for the oral cavity, which form a substantial film on the surface of the teeth or gums when processing these surfaces and which are easily removed by brushing, rinsing or eating at the end of the treatment. In accordance with a first aspect of the present invention, the compositions may also contain an active substance for caring for the oral cavity and, in essence, can provide a delayed release of the active substance in the tissue of the oral cavity. The compositions of the present invention are particularly effective for the release of active oral care substances that either improve the appearance of the teeth or have therapeutic and / or prophylactic benefits.

State of the art

Many consumers are well aware of the preventive, therapeutic, and cosmetic benefits of maintaining a high level of oral hygiene. Indicated benefits include reducing tooth decay and plaque, reducing gum disease, and calculus formation; hypersensitivity treatment; giving freshness to breath; teeth whitening and stain removal; remineralization of teeth and the like. A huge variety of oral care products are currently available that, in a short time, help maintain oral hygiene by delivering various oral care substances or active substances to soft and hard oral tissues. In general, such products exist in the form in which they are used by the consumer alone, either at home or outside the house and / or used by the dentist / hygienist in their usual professional practice of caring for oral hygiene. Representative examples of such products, especially those that are used by the consumer on their own, include toothpastes containing, for example, anti-caries active substances and / or antibacterial substances that prevent the formation of plaque; mouthwashes containing active substances that give freshness to breathing and / or antibacterial substances; and chewing gums containing tooth whitening actives.

Most often, oral hygiene is carried out by the consumer independently and usually, as is customary in the West, this happens once or twice a day. However, there are a large number of processes that lead to a deterioration of the tissues of the oral cavity and in which effective treatment, either prophylactic or therapeutic, in general, is possible only under constant supervision, which is impractical or with long-term treatment. Currently, traditional varieties of goods usually do not give long, prolonged or delayed therapeutic, prophylactic and / or cosmetic therapeutic effects. Instead, the drugs act only for a relatively short period of time in which the teeth remain cleaned and the oral cavity is washed, and after applying the product, the level of active substances on the hard and soft tissues of the oral cavity decreases rapidly. Thus, until now, the only way to achieve a sustained release of active substances in the case of traditional products was to periodically use the product or use specific delivery devices, such as mouthpieces. Therefore, it would be desirable to have an oral care product that contains one or more active substances that are substantial within the oral cavity, and that the oral care product has a pleasant taste for acceptable aesthetic perception for long-term use in the oral cavity. It is also desirable to have a substantial oral care product in which the active substances are released over an extended period of time and thus are able to provide a prolonged effect. Finally, it would be desirable that the oral care product can be easily removed at the end of the treatment period without damaging the soft and hard tissues of the oral cavity when the product is removed, and that the oral care product is suitable for use by the user at home without the need for a professional help. In addition, such compositions could be particularly effective in underdeveloped countries where prophylactic oral hygiene by a specialist is generally less affordable.

Several attempts have been made previously to increase the substantivity of the active ingredients of oral care products. These attempts include the use of water-soluble films formed by polymers to release various active substances, for example, a bleaching agent (US Pat. No. 5,425,953, PCT / CN97 / 00); bactericidal pharmacological substance (US patent 5438076); a cationic bactericidal substance that prevents the formation of plaque (European patent 0864315); fluoride ions (US patent 5989535) and so on. However, due to the fact that the above systems are water-soluble, they are readily soluble in saliva and, therefore, their duration is relatively low and they cannot provide a sustained release of the active substance. In addition, their water-soluble nature prevents their use together with active substances for caring for the oral cavity, which can be unstable in water-based films, for example, with sodium percarbonate. The second approach, which has been described in this area to improve the substantivity of active substances in the oral cavity, relates to the use of substances that can be absorbed into the tissue. For example, US Pat. No. 3,956,480 describes compositions in which a cationic bactericide and an anionic polymer are absorbed on the hydroxyapatite surface of the teeth; European patent EP0736544 describes the use of antibodies for the adhesion of specific proteins in the oral cavity, for example, in film structures; US Pat. No. 1,027,877 and US Pat. No. 5,139,768 disclose compositions comprising hydrophobic polymers, for example cellulose polymers or carbonyloxycarbonyl polymers to achieve substantivity; and WO 93/24103 describes an antimicrobial agent on an inert oxide synthetic microparticle substrate that is adsorbed by tooth enamel. However, these methods are limited to substances that have a preferred affinity for hard tissues of the oral cavity, and, in addition, they can be limited by the type of active substances for caring for the oral cavity, which can be introduced into their composition. A higher level of duration of action was achieved through the use of hard protective coatings on the teeth. For example, US Pat. No. 5,401,528 describes the polymerization of organically modified silicic acid polycondensation products to form a coating on teeth; similarly, US Pat. No. 5,888,491 describes the use of polymers grafted onto polysiloxane chains to form a highly substantive coating on hard tissues in the oral cavity. However, these dense coating systems are often unsuitable for home use, give an unpleasant aftertaste, and the coating itself may be exposed to harmful bacteria that cause plaque.

Silicones are widely used in various fields of dentistry, including as denture adhesive compositions (WO 93/14737); nonsubstantial neutral films (US 5032387) and polymeric means for taking casts (European patent 822233). In addition, it has long been known that polysiloxanes can be used in oral care compositions to provide a smooth, very thin, water-repellent coating of teeth on which they form a hydrophobic surface and are thus able to prevent tooth decay and stains (GB 686429) WO 93/23009 and WO 95/03776). It has also been shown that as long as the polysiloxane coating remains on the teeth, it is able to act as a source of sustained release of fat-soluble active substances, for example antibacterial agents (US patent 5422098). However, polysiloxanes themselves stick to teeth only for a short period of time, so attempts have been made to increase substantivity by modifying silicone oil, for example, using quaternized tertiary cyclic amines (US patent 789851); quaternary ammonium groups (US patent 4161518) and aminoalkyl groups in combination with lipophilic active substances (European patent 0528457). The initial study was then continued in WO 96/19190, WO 96/19191, WO 96/19192 and WO 96/19563, which describe alkyl, alkoxy and aminoalkyl-dimethicone copolyols for dentifrice or acrylate dentures, containing a large number of various active substances for teeth. These compositions combine efficacy and substantivity, performance and good cleaning performance. In addition, US Pat. No. 5,057,307, US 5,057,309 and US 5,733,529 describe gels containing a nonionic surfactant, a coating material that is not soluble in this surfactant, preferably polysiloxane polymers with viscosities of up to 50 million centipoise, thickeners, preferably simple cellulose ethers, and oral care actives such as tin divorce. Finally, applications pending PCT / US99 / 15890 and PCT / US99 / 15891 describe oral care compositions containing an organosiloxane polymer in combination with a volatile carrier capable of solubilizing the polymer and an active oral care agent to prepare compositions that harden on the surface of the oral cavity. Although the prior art compositions and descriptions provide useful information about the use of polysiloxanes in oral compositions, existing approaches still have limitations. There is no composition that provides a combination of substantive and sustained release substances or active substances for oral care, in combination with a product that is a non-drying composition that is easily applied to all surfaces of the oral cavity, which does not cause discomfort on the surfaces of the cavity a mouth that can be used for self-treatment / at home and which is easy to remove.

Adhesive silicone systems are well known, including systems that contain mixtures of silicone resins and silicone polymers in combination with a hardener (e.g., catalyzed condensation reactions, heating, and the like) and which are commonly referred to as sensitive adhesives. Such systems in this area are described in US Pat. Nos. 4,016,328, US 3,929,704, US 2,814,601, US 2,736,721 and Canada 2,085,696. Such systems alone are not suitable for home oral care due to the harsh hardening conditions required. However, attempts to modify these systems to use their substantivity in personal care products have been described in this area. Applications on this topic include WO 93/17660, WO 98/16196, WO 97/17058 and WO 97/17059, which describe the use of silicone polymer / resin mixtures and volatile solvents in cosmetic compositions; WO 92/08439, US patents 4906459, US 4902499, WO 92/10161 and WO 92/10162, which describe the use of mixtures of silicone polymer / resin / liquid silicone in combination with surfactants as hair care products; WO 00/06100, WO 00/06107, which describe the use of silicone polymers in compositions for shaping hair; and UK patents 2289686 and US 5523017, which describe a system of transparent silicone emulsions for use in personal care products. Although prior art data indicate useful advantages for using silicone compositions in personal care products, there is insufficient information on how to combine silicone resins, polymers and liquid silicone to produce non-volatile, non-hardening compositions that are substantial on the surface of the cavity and are readily removable and which may also optionally be used to delay the release of various oral care actives.

It has been unexpectedly found that if the silicone polymer is combined with a silicone resin and a non-volatile liquid polydimethylsiloxane, a composition is formed that can be easily applied to all surfaces of the oral cavity and which remains substantial on these surfaces. In addition, when oral care active substances are added to these compositions, the compositions can be used to delay the release of various oral care active substances into the oral cavity throughout their use. In addition, since the composition does not contain volatile solvents, it remains liquid on the teeth, and therefore is extremely effective for releasing therapeutic agents into the space between the teeth, under the gums and certain periodontal cavities and, moreover, retains the preferred aesthetic qualities for the consumer, since the product does not form a hard coating on the surface of the teeth. Finally, since the film remains liquid, it is easily removed during normal brushing and, thus, it is ideal for independent use by the consumer. The invention can be improved by optionally preparing a composition in the form of a water-in-silicone emulsion, where water-soluble oral care actives can be dispersed in the aqueous phase.

Without the intention of adhering to any theory, it is likely that the resin / polymer mixture forms a hydrophobic surface on hard and soft tissues of the oral cavity, which is able to prevent the development of plaque and / or slow release of active substances for caring for the oral cavity. In addition, the introduction of a low viscosity liquid into this composition is likely to facilitate the rapid wetting of the surface by the composition, which facilitates the distribution of the composition on the surface of the oral cavity and also facilitates the production process. Finally, it is likely that if such a system is a water-in-silicone emulsion, then after some time the aqueous phase increases its weight as a result of the osmosis of water from saliva into the internal aqueous phase. This, apparently, leads to an increase in the substantivity of the composition with respect to the surfaces of the oral cavity.

The aim of the present invention is to provide a substantive coating of teeth that has an acceptable taste in the mouth and which can be prophylactically or therapeutically treat the surface of the oral cavity, including by delayed release of active substances for caring for the oral cavity. In addition, the object of the present invention is a substantive film for application to oral tissue, which does not dry for a long time and, thus, is easily removed, so that such a film can be easily used by the consumer on his own.

These and other objects of the present invention will become apparent in light of the following description.

SUMMARY OF THE INVENTION

In accordance with a first aspect, the present invention relates to a non-volatile composition comprising:

i) from about 0.5% to about 60% by weight of a silicone polymer;

ii) from about 0.1% to about 30% by weight of silicone resin;

iii) from about 0.1% to about 95% by weight of non-volatile liquid polydimethylsiloxane, whose viscosity is from about 1 cSt to about 1000 cSt; and

iv) from about 0.01% to about 50% by weight of an active substance for caring for the oral cavity selected from substances that change the color of teeth, anti-tartar agents, anti-plaque agents, sources of fluoride ions, antimicrobial agents, nutrients, antioxidants, N-2 antagonists, analgesics, antiviral agents, pharmacological substances absorbed by the mucosa, and mixtures thereof.

In accordance with a second aspect, the present invention relates to the use of a volatile silicone composition for caring for the oral cavity, for applying to the surface of hard or soft tissues of the oral cavity, where the composition contains:

i) from about 0.5% to about 60% by weight of a silicone polymer;

ii) from about 0.1% to about 30% by weight of silicone resin;

iii) from about 0.1% to about 95% by weight of non-volatile liquid polydimethylsiloxane, whose viscosity is from about 1 cSt to about 1000 cSt.

In accordance with a third aspect, the present invention relates to a non-volatile composition, which contains:

i) from about 0.1% to about 30% by weight of a methyl-substituted polyorganosiloxane resin with a viscosity of more than 500,000 cSt;

ii) M: Q polyorganosiloxane polymer, where the ratio of M: Q is in the range from 0.6 to 0.7;

iii) a non-volatile liquid polydimethylsiloxane which has a viscosity of from about 5 cSt to about 400 cSt; and where the mass ratio of the polyorganosiloxane polymer and polyorganosiloxane resin is in the range of from about 1: 1 to about 7: 1, where the mass ratio of liquid polydimethylsiloxane and polyorganosiloxane resin is in the range of from about 2: 1 to about 8: 1 and where the viscosity of the final composition is in the range from about 1 Pa · s to about 1000 Pa · s.

DETAILED DESCRIPTION OF THE INVENTION

Unless otherwise indicated, all percentages and ratios used here are mass based on the total composition and all measurements were carried out at 25 ° C. Unless otherwise specified, all percentages, ratios, and levels of ingredients indicated herein are based on the actual amount of ingredients and do not include solvents, excipients, or other substances in combination with which the ingredient may be in commercially available products.

Unless otherwise indicated, all publications cited here are incorporated by reference in full.

As used herein, the term “active substance for oral care” refers to any composition that can be used prophylactically, therapeutically or cosmetically, either directly in the oral cavity, or which is absorbed in the oral cavity and exerts its primary beneficial effect elsewhere.

As used herein, the term “treatment” refers to the application of a substance in the oral cavity, where this substance may or may not contain an active oral care substance that has prophylactic, therapeutic or cosmetic value.

The term “oral cavity” as used herein refers to the cavity from the lips to the larynx. “Hard tissues” include tissues such as teeth, periodontal and the like, and “soft tissues” include tissues such as gums, tongue, cheek surfaces and the like. Within the scope of this application, hard and soft tissues of the oral cavity should also be considered and include any devices that are used in this regard, for example dentures, partial dentures, braces, and so on.

As used herein, the term “substantive” means that a sufficient amount of the composition is retained in the oral cavity, and thus, it can be perceived by the user visually or by touch after a certain period of time. The expected substantiality of the compositions in vivo in this case can be measured by in vitro methods. The method consists in using the standard Erweka pharmaceutical grinding device, model ZT3-2, modified for applying the gel. Briefly, a 50 μm film of the composition mixture is obtained on a glass slide using a device that reduces the cross section of the layer. The slide with the composition applied was continuously removed and immersed in the test solution (artificial saliva, 35 ° C) for a long time; film weight was recorded at regular intervals. Substantive compositions were defined as compositions that retain at least 10%, preferably 20%, and more preferably 50% of their initial wet weight after 2 hours of treatment with the solution, preferably after 4 hours and more preferably after 6 hours.

As used herein, the term “safe and effective amount” means an amount of a compound, component, or composition sufficient to significantly increase the beneficial effect, but low enough to avoid serious side effects, that is, an amount that provides an acceptable risk to benefit ratio within an area related to a medical condition.

By the term “non-volatile” as used herein, it is meant that a substance under ambient conditions has a very low vaporization point or does not have it at all, which is well known in the art. A non-volatile substance will also typically have a boiling point at a pressure of one atmosphere equal to at least 200 ° C, preferably 275 ° C, and more preferably at least 300 ° C. In addition, this term means that the compositions contain less than 10%, preferably less than 5%, and more preferably less than 2% by weight of volatile material. As defined here, a volatile substance is any substance with a boiling point in one atmosphere below 200 ° C.

Viscosity was measured using standard methods using a Brookfield viscometer at room temperature, which are well known to those skilled in the art. The viscosity of the final products was measured at 25 ° C using a Brookfield viscometer (model DV-II) and a Spindle D at 10 rpm. Three readings were recorded with an interval of 1 minute, taking the average as an indicator of the viscosity of the sample.

The active and other ingredients used herein may be categorized or described depending on their cosmetic and / or therapeutic efficacy or on their intended mode of action. However, it should be understood that the active and other ingredients used herein may in some cases produce more than one cosmetic and / or therapeutic effect or have more than one mode of action. Therefore, the classification given here is intended to be convenient and not to limit the ingredient to a specific indicated use or list of uses.

A general reference for silicones, including sections describing liquid silicones, resins and polymers, and the preparation of silicones, can be found in Encyclopaedia of Polymer Science and Engineering, Volume 15, Second Edition, pp. 204-308, John Wiley & Sons Inc. 1989 and Chemistry and Technology of Silicones, Walter Noll, Academic Press Inc. (Harcourt Brue Javanovich, Publishers, New York), 1968, pp. 282-287 and 409-426, which are incorporated herein by reference.

Elements of these compositions are described below in more detail.

Silicone polymers

The compositions used in the present invention include from about 0.5% to about 60%, preferably from about 2% to about 50%, more preferably from about 10% to about 40%, and most preferably from about 15% to about 25% by weight of silicone polymer.

The silicone polymers referred to herein are highly crosslinked polymeric siloxane systems. Cross-linking was introduced by the inclusion of trifunctional and tetrafunctional silanes, and monofunctional or difunctional, or both silanes in the production of silicone polymer. As is well known in the art, the crosslink density, which is necessary in order to obtain a silicone polymer, will vary depending on the specific silane units incorporated into the silicone polymer. In general, silicone materials that have a significant level of trifunctional and tetrafunctional siloxane monomer units (and therefore a significant crosslink density), and therefore form a rigid or solid film upon drying, are considered silicone polymers. The ratio of oxygen atoms and silicon atoms is an indicator of the crosslink density of a particular silicone material. Silicone materials that have a ratio of oxygen atoms to silicon atoms of at least about 1: 1 will form silicone polymers in this case. Preferably, the ratio of oxygen atoms: silicon is at least about 1.2: 1.0. Typical silanes used in the manufacture of silicone polymers are monomethyl, dimethyl, monophenyl, diphenyl, methylphenyl, monovinyl, and methyl vinylchlorosilanes and tetrachlorosilanes. Preferred polymers are silicone polymers substituted with methyl, ethyl or phenyl. Commercially available silicone polymers can usually be supplied in uncured form, either in powder form or in the form of a volatile substance with a low density, or, preferably, in the form of a non-volatile liquid silicone. In this case, it is preferable to use silicone polymers, which are supplied in powder form or in the form of a polymer mixture with non-volatile liquid silicone.

Silicone polymers can easily be identified in accordance with the abbreviated nomenclature system, well known to those skilled in the art as the “MDTQ” nomenclature. In this system, silicones are described by the presence of various siloxane monomer units that form silicone. Briefly, the symbol M denotes a monofunctional unit ((CH ₃ ) ₃ SiO) _0.5 ; D represents a difunctional unit (CH ₃ ) ₂ SiO; T represents a trifunctional unit ((CH) ₃ SiO) _1,5 ; and Q is a quadro- or tetrafunctional SiO ₂ unit. It should be noted that small amounts of up to about 5% silanol or alkoxy functional groups may also be present in the polymer structure as a result of processing. The bar on the link symbols, for example M ', D', T ', Q', denotes substituents with the exception of methyl, and in each case must be specifically specified. Typical alternating substituents include groups such as vinyl, phenyl, amino, hydroxyl and so on. The molar ratio of the various units, either as indicators of the lower index of the symbols, showing the total number of each type of unit in the silicone or as their average value, or as a specifically indicated ratio in combination with the molecular weight, completes the description of the silicone material according to the MDTQ system. High relative amounts of T, Q, T ', Q' and D, D ', M, M' in the silicone polymer indicate a high crosslink density. As previously described, however, the full level of crosslinking can also indicate the ratio of oxygen to silicone.

Silicone polymers that are preferably used here are MQ, MT, MTQ, and MDTQ; such MQ polymers are described in US Pat. No. 5,330,747 to Krysik on July 19, 1994. Accordingly, methyl is the preferred silicone substituent. Particularly preferred are MQ polymers in which the M: Q ratio is from about 0.4 to about 0.8, preferably from about 0.6 to about 0.7. Preferred silicone polymers are solid at about 25 ° C and their average molecular weight is from about 1000 to about 10,000. Preferred polymers are soluble in organic solvents such as toluene, xylene, isoparaffins, cyclosiloxanes and mixtures thereof. Organosiloxane polymers such as these are commercially available, for example SR 1000 and GE 1170-002, GE SS4230 and SS4267 from General Electric Company and Wacker 803 and 804 are available from Wacker Silicones Corporation of Adrian, Michigan, US.

Silicone resins

Compositions for use in the present invention contain from about 0.1% to about 30%, preferably from about 1% to about 20%, more preferably from about 1% to about 10%, and most preferably from about 2% to about 7%, weight of silicone resin.

“Silicone resins” refers to high molecular weight polydiorganosiloxanes having a viscosity at 25 ° C. of from about 500,000 cSt to about 50,000,000 cSt. The viscosity of the compound can be measured by the methods described in the Dow Corning Corpoarete Test Method CTM004, July 20, 1970 using a glass capillary viscometer. In addition to silicone resins, polydiorganosiloxanes with an average molecular weight of more than 500,000 are considered in this case.

Suitable silicone resins are described by Petrarch and others, including US Pat. No. 4,152,416 and Noll, Walter Chemistry and Technology of Silicones of the New York Academic Press 1968. Also described are silicone resins of various General Electric Silicone Rubber Product Data Sheets. All of these described links are hereby incorporated by reference.

Polysiloxane resins most suitable for use in this case include resins represented by the general formula (I):

where each R is independently substituted or unsubstituted with an aliphatic group (eg, alkyl or alkenyl), aryl, alkoxy, alkylaryl, alkoxy, alkylamino (eg, alkyl or alkenylamino), hydroxy or hydrogen, or combinations thereof; and x is an integer sufficient for the resin to have the desired viscosity.

The polysiloxane resin used in this case may be linear or cyclic. Examples of linear polysiloxanes are compounds of formula (I) above. A branched chain may also be used. Cyclic polysiloxanes include polysiloxanes represented by the formula (II):

where R is as described above, and n is an integer high enough for the resin to have the desired viscosity.

The substituents of the siloxane chain R can have any structure in which the polysiloxanes formed are hydrophobic, do not cause irritation, are not toxic, or otherwise harmful when applied to human teeth, can precipitate on human teeth, be compatible with other components of the composition and chemically stable under normal use and storage conditions.

Preferred alkyl and alkenyl substituents include C1-C5 alkyls and alkenyls, more preferably C1-C4, most preferably C1-C2. The aliphatic parts of other groups containing alkyl, alkenyl or alkynyl (such as alkoxy, alkylaryl and alkamino) may be straight or branched chains and preferably have from 1 to 5 carbon atoms, more preferably from 1 to 4 carbon atoms, even more preferably from 1 to 3 carbon atoms and most preferably from 1 to 2 carbon atoms. As discussed above, R substituents may also contain functional amino groups, for example, alkino groups, which may be primary, secondary, tertiary amines or quaternary ammonium. They include mono, di, trialkylamino and alkoxy amino groups in which the aliphatic part of the chain is preferably as described above. Substituents R may also be substituted with other groups, such as halogens (e.g., chlorine, fluorine and bromine), halogenated aliphatic or aryl groups, and hydroxy groups (e.g., aliphatic groups substituted with hydroxy groups). Suitable halogenated R groups may include, for example, trihalogenated (preferably fluorine) alkyl groups such as R1-C (F) ₃ , where R1 is C1-C3 alkyl. Preferred are methylorganosiloxane resins substituted with methyl, or polyorganosiloxane resins substituted with methyl.

Substituents containing aryl include alicyclic and heterocyclic five- and six-membered aryl rings, and substituents containing fused five- or six-membered rings. Aryl rings themselves may be substituted or unsubstituted. Substituents include aliphatic substituents and may also include alkoxy substituents, acyl substituents, ketones, halogens (e.g., chlorine, fluorine and bromine), amines, and so on. Examples of groups containing aryl include substituted or unsubstituted alkyl or alkenyl substituents, for example allyl phenyl, methyl phenyl, ethyl phenyl, vinyl phenyls such as styrenyl, and phenylalkines (e.g. phenyl C2-C4 alkynes). Heterocyclic aryl groups include substituents derived from furan, imidazole, pyrrole, pyridien and so on. Condensed aryl ring substituents include, for example, naphthalene, coumarin and purine.

Specific examples of preferred siloxane resins include polydimethylsiloxane, methyl vinyl siloxane copolymer, poly (dimethyl siloxane), diphenyl, methyl vinyl siloxane copolymer and mixtures thereof. The safety of polydimethylsiloxanes or the use in these diverse products is well described. See, Rowe et al., Journal of Industrial Hygiene, 30: 332-352 (1948). See also Calandra et al., “ACS Polymer Preprints”, 17: 1-4 (1976) and Kennedy et al., J. Toxicol. & Environmental Health, 1: 909-920 (1976). The most preferred siloxane resin is SE30 from General Electric.

For the compositions used here, it is highly preferred that the weight ratio of the silicone polymer to the high molecular weight silicone resin is in the range of from about 0.1: 1 to about 9: 1, preferably from about 1: 1 to about 7: 1, and most preferably from about 1: 1 to about 5: 1.

Liquid silicones

The compositions used here also contain from about 0.1% to about 95%, preferably from about 5% to about 90%, more preferably from about 10% to about 85% by weight of non-volatile liquid polysiloxane with a viscosity at 25 ° C of from about 1 cSt to about 1000 cSt, preferably from about 2 cSt to about 500 cSt, and more preferably from about 5 cSt to about 400 cSt.

As with resins, the liquid polysiloxanes used here can be linear or cyclic. They can be replaced by a wide variety of substituents. Any substituent already described above in the case of siloxane resins can also be considered effective as a substitute for liquid polysiloxanes. Preferred alkyl and alkenyl substituents include C1-C5 alkyls and alkenyls, more preferably C1-C4, most preferably C1-C2, and preferred aryl substituents are alicyclic and heterocyclic five- and six-membered aryl rings. Most preferred substituents include methyl, ethyl and phenyl substituents. Methyl is the most preferred substituent.

Suitable liquid polysiloxanes include linear polysiloxane polymers such as dimethicone and other analogs of polysiloxane substances with a low viscosity, preferably of 200 cSt or less at 25 ° C, and cyclomethicone and other cyclic siloxanes having, for example, a viscosity at 25 ° C. equal to 200 cSt or less. Examples of suitable commercial substances include Dow Corning DC200 Series and Wacker Silicones AK Series Fluids.

In the case of the composition used here, it is preferable that the mass ratio between the low viscosity liquid polysiloxane and the high viscosity polysiloxane resin is in the range from about 0.1: 1 to about 20: 1, preferably from about 1: 1 to about 10: 1 and more preferably from about 2: 1 to 8: 1, and most preferably from about 2: 1 to about 5: 1.

Oral Care

According to a first aspect of the invention, the compositions comprise from about 0.01% to about 50%, preferably from about 0.01% to about 20%, more preferably from about 0.01% to about 10%, by weight of the active substance for caring for an oral cavity selected from substances that change the color of teeth, agents that prevent the formation of tartar and prevent the formation of plaque, sources of fluoride ions, antimicrobials, nutrients, antioxidants, N-2 antagonists, analgesics, antiviral substances, pharmacological substances c, absorbed by the mucous membrane, and mixtures thereof. Active substances for caring for the oral cavity, preferably, contain an active substance with a concentration at which, when used directly, the benefit for the consumer is provided without compromising the treated surface of the mouth.

Oral care compositions or substances of the present invention may include a large amount of the active substances previously described in the art. The following list does not limit the active substances for caring for the oral cavity that can be used according to the present invention:

1. Substances that change the color of teeth. Along with other active oral care agents useful in the present invention, tooth discoloration agents can be considered. These substances are used to change color to meet consumer needs. These substances can be particles that, when applied to the surface of the teeth, change this surface based on absorption and / or reflection of light. Such particles give a visible effect when a film containing such particles is applied to the surface of a tooth or teeth. This effect can continue until the film is destroyed or removed, revealing, for example, a spotty or unusual tooth surface.

The most useful particles of the present invention include pigments and dyes, which are commonly used in the cosmetic field. There are no particular restrictions on the pigments and / or dyes used in the compositions of the present invention, except for limiting the effect that they have on the surface of the teeth when illuminated. Pigments and dyes include inorganic white pigments, inorganic color pigments, pearlescent additives, filler powders and the like; see Japanese Published Kokai Patent Application No. 9 [1997] -100215, published April 15, 1997, incorporated herein by reference. Representative examples are selected from the group consisting of talc, mica, magnesium carbonate, calcium carbonate, magnesium silicate, aluminum carbonate, silica, titanium dioxide, zinc oxide, red iron oxide, brown iron oxide, yellow iron oxide, black iron oxide, ammonium ferrocyanide , purple manganese, ultramarine, nylon powder, polyethylene powder, methacrylate powder, polystyrene powder, silk powder, crystalline cellulose, starch, titanium mica, titanium mica with iron oxide, bismuth oxychloride and mixtures thereof. Most preferred are examples selected from the group consisting of titanium dioxide, bismuth oxychloride, zinc oxide and mixtures thereof. Pigments that are generally known to be safe, are listed in CTFA Cosmetic Ingredient Handbook, 3 ^rd Edition, Cosmetic and Fragrances Association Inc., Washington DC (1982), incorporated herein by reference.

Pigments are commonly used as opacifiers and dyes. These pigments can be used in the form of processed particles or in the form of unprocessed pigments themselves. Typical pigment concentrations are selected depending on the particular action desired by the user. For example, for teeth that are partially damaged or stained, pigments are usually used in an amount sufficient to lighten the teeth. On the one hand, if individual teeth or stains on the teeth are lighter than other teeth, pigments can be used that make them darker. The content of pigments and dyes is usually in the range from about 0.05% to about 20%, preferably from about 0.1% to about 15%, and most preferably from about 0.25% to about 10% by weight of the composition. Most preferably, the pigment-containing composition used herein further comprises an additional active oral care agent.

The compositions used herein may also contain substances that remove or whiten internal or external stains on the surface or inside the teeth. Such substances are selected from the group consisting of peroxides, metal chlorites, perborates, percarbonates, peroxyacids, persulfates and mixtures thereof. Suitable peroxide compounds include hydroperoxide, urea peroxide, calcium peroxide, carbamide peroxide, and mixtures thereof. Urea peroxide is most preferred. Suitable metal chlorites include calcium chlorite, barium chlorite, magnesium chlorite, lithium chlorite, sodium chlorite and potassium chlorite. Additional bleaching agents may be hypochlorite and chlorine dioxide. A preferred chlorite is sodium chlorite. A preferred percarbonate is sodium percarbonate. Preferred persulfates are oxones. The content of these substances depends on the free oxygen or chlorine, respectively, which the molecule provides for bleaching spots. Their content, commonly used in the compositions of the present invention, is from about 0.1% to about 35%, preferably from about 1% to about 25%, and most preferably from about 5% to about 10% of the composition.

2. Substances that prevent the formation of tartar. Substances that prevent the formation of tartar, which are known for use in dental products, include phosphate. Phosphates includes pyrophosphates, polyphosphates, polyphosphonates and mixtures thereof. Pyrophosphates are the most well-known substances used in dentifrices, but polyphosphates are also considered frequently used in the compositions of the present invention. The pyrophosphate salts used in the compositions of the present invention include pyrophosphate salts of alkaline metals, pyrophosphate salts of tetra-alkali metals, and mixtures thereof. Disodium dihydropyrophosphate (Na ₂ H ₂ P ₂ O ₇ ), tetrasodium pyrophosphate (Na ₄ P ₂ O ₇ ) and tetracal pyrophosphate (K ₄ P ₂ O ₇ ) and mixtures thereof in their unhydrated as well as hydrated forms are preferred classes. Although any of the above pyrophosphate salts may be used, a tetrasodium pyrophosphate salt is preferred. Sodium polyphosphate and triethanolamine polyphosphates, for example, are preferred.

Pyrophosphate salts are described in more detail and Kirk Othermer, Encyclopeadia of Chemical Technology, 3 ^rd Edition, Volume 17, Wiley Interscience Publishers (1982). Additional anti-calculus agents include pyrophosphates or polyphosphates described in US Pat. No. 4,590,066 issued to Parran and Sakkab on May 20, 1986; polyacrylates and other polycarboxylates, for example, those described in US Pat. No. 3,429,963 issued to Shedlovsky on February 25, 1969, and in US Pat. No. 4,304,766 to Chang on December 8, 1981; and US Pat. No. 4,661,341 to Benedict and Sunberg on April 28, 1987; polyepoxysuccinates, for example, those described in US Pat. No. 4,846,650 to Bendict, Bush and Sunberg, July 11, 1989; ethylenediaminetetraacetic acid described in UK patent 490384 of February 15, 1937; nitrilotriacetic acid and related compounds described in US Pat. No. 3,678,154 to Widder and Briner on July 18, 1972; polyphosphonates described in US Pat. No. 3,737,533 to Francis on June 5, 1973; US Pat. No. 3,988,443 to Ploger, Schmidt-Dunker and Gloxhuber, October 26, 1976, and US Pat. sodium tripolyphosphate; diphosphonates such as ethane-1-hydroxy-1, 1-diphosphonate, 1-azacycloheptane-1, 1-diphosphonate and linear alkyl diphosphonates; linear carboxylic acids; and sodium zinc citrate and other soluble zinc salts.

Preferred polyphosphates are those polyphosphates that have a chain length of three or more, especially which have a chain length of about four or more phosphate molecules, including, but not limited to, tetrapolyphosphate and hexametaphosphate. Polyphosphates, which are larger than tetrapolyphosphate, usually exist as amorphous, transparent substances. Preferred according to this invention are linear "transparent" polyphosphates with the formula:

XO (XRO ₃ ) _n X

where X is sodium, potassium or hydrogen, and n is a whole number from about 6 to about 125. Most preferred is ground sodium polyphosphate with an average chain length of from about 10 to about 30, preferably from about 15 to 25, more preferably from about 21 to about 23. Such polyphosphates are produced by FMC Corporation and they are commercially known as Sodaphos (n≈6), Hexaphos (n≈13) and Glass H (n≈21). Hexaphos and Glass H are preferred, while Glass H is the most preferred polyphosphate. These polyphosphates can be used alone or in the form of combinations thereof.

Agents that can be used in place of or in combination with the pyrophosphate salt include known substances such as synthetic anionic polymers, including polyacrylates and copolymers of maleic anhydride or acid and methyl vinyl ether (e.g., Gantxez), as described, for example, in US Pat. No. 4,627,977 Gaffer et al .; as well as, for example, polyaminopropanesulfonic acid (AMPS), zinc citrate trihydrate, polyphosphates (e.g. tripolyphosphate; hexametaphosphate), diphosphonates (e.g. EHDP; ANP), polypeptides (such as polyaspartic and polyglutamic acids) and mixtures thereof.

3. Substances that prevent the formation of plaque. Substances that prevent the formation of plaque are any substances that inhibit the formation of bacterial plaque on the surfaces of the oral cavity. Examples include xylitol and other antimicrobial agents.

4. Source of fluoride ions. Sources of fluoride ions are well known as anticaries agents for use in oral compositions. Fluoride ions are contained in a large number of oral care compositions for these purposes, especially in toothpastes. Patents disclosing such toothpastes include US Pat. No. 3,538,230, November 3, 1970, issued by Pader et al .; U.S. Patent 3,689,637, September 5, 1972, Pader; U.S. Patent 3,711,604, Jan. 16, 1973, Colodney et al .; US patent 3911104, October 7, 1975, Harrison; US patent 3935306, January 26, 1976, Roberts et al .; and U.S. Patent 4,040,858, August 9, 1977, Wasson.

The use of fluoride ions for tooth enamel is useful for protecting teeth from decay. As sources of soluble fluorides in the composition of this invention can be used a wide variety of substances, sources of fluoride ions. Examples of suitable fluoride ion producing substances are contained in US Pat. No. 3,535,421, October 20, 1970, issued by Briner et al., And US Pat. No. 3,678,154, July 18, 1972, issued by Widder et al. Preferred sources of fluoride ions for use in this case include sodium fluoride, potassium fluoride, tin fluoride, ammonium fluoride, and a mixture thereof. Sodium fluoride is particularly preferred. Preferably, the composition provides from about 50 ppm to about 10,000 ppm, more preferably from about 100 ppm to about 3,000 ppm of fluoride ions in compositions that interact with tooth surfaces, in cases when they are used in conjunction with the delivery system of the present invention.

5. Antimicrobial agents. Antimicrobial agents may also be present in the oral care compositions or substances of this invention. Such agents may include, but are not limited to, 5-chloro-2- (2,4-dichlorophenoxy) -phenol, commonly referred to as triclosan, and described in the Merck Index, 11 ^th Edition, (1989), pp. 529 (article number 9573), in US patent 3506720 and in European patent application 0251591, Beecham Group, Plc, published January 7, 1988; phthalic acid and its salts, including, but not limited to, described in US Pat. No. 4,994,262, published February 19, 1991, preferably potassium magnesium phthalate, chlorhexidine (Merck Index, No. 2090); alexidine (Merck Index, No. 222); hexetidine (Merck Index, No. 4624); sanguinarine (Merck Index, No. 8320); benzalkonium chloride (Merck Index, No. 1066); salicylanilide (Merck Index, No. 8299); domifenbromide (Merck Index, No. 3411); cetylpyridinium chloride (CPC) (Merck Index, No. 2024); tetradecylpyridinium chloride (TPC); N-tetradecyl-4-ethylpyridinium chloride (TDEPC); octenfin; delmopinol; octapinol; and other piperidine derivatives; nitsin preparations; zinc / tin (II) ion agents; antibiotics such as augmentin, amoxicillin, tetracycline, doxycycline, minocycline and metronidazole; and their analogues and salts; base oils, including thymol, geraniol, carvacrol, citral, hinokithiol, eucalyptol, catechol (in particular 4-allylcatechol) and mixtures thereof; methyl salicylate; hydrogen peroxide; metal salts of chlorite and mixtures of all the substances mentioned above.

6. Nutrients. Nutrients can improve the condition of the oral cavity and can be included in the composition or substance for caring for the oral cavity of the present invention. Nutrients include minerals, vitamins, oral nutritional supplements, enteral nutritional supplements, herbal supplements, natural extracts, and mixtures thereof.

Minerals that may be included in the compositions of the present invention include calcium, phosphorus, fluorine, zinc, magnesium, potassium, and mixtures thereof. These minerals are described in Drug Facts and Comparisons (USP), Wolters Kluer Company, St. Louis, Mo., © 1997, pp. 10-17.

Vitamins can be included with minerals or used separately. Vitamins include vitamins C and D, thiamine, riboflavin, calcium pantothenate, niacin, folic acid, nicotinamide, pyridoxine, cyanocobalamin, para-aminobenzoic acid, bioflavonoids, and mixtures thereof. These vitamins are described in Drug Facts and Comparisons (USP), Wolters Kluer Company, St. Louis, Mo., © 1997, pp. 3-10.

Oral nutritional supplements include amino acids, lipotropic substances, fish oil, coenzyme Q10, and mixtures thereof, as described in Drug Facts and Comparisons (USP), Wolters Kluer Company, St. Louis, Mo., © 1997, pp. 54-54e. Amino acids include, but are not limited to, L-tryptophan, L-lysine, methionine, threonine, levocarnitine or L-carninite and mixtures thereof. Lipotropic substances include, but are not limited to, choline, inositol, betaine, linoleic acid, linolenic acid, and mixtures thereof. Fish oil contains a large amount of omega-3 (N-3) polyunsaturated fatty acids, eicosapentaenoic acid and docosahexaenoic acid.

Enteral nutritional supplements include, but are not limited to, protein products, glucose polymers, corn oil, safflower oil, medium chain triglycerides as described in Drug Facts and Comparisons (US Medicines Regulatory Book), Wolters Kluer Company, St. Louis, Mo., © 1997, pp. 55-57.

7. Antioxidants. Antioxidants are commonly known as useful additives in compositions, such as the compositions of the present invention. Antioxidants are described in manuals such as Cadenas and Packer, The Handbook of Antioxidants, © 1996 by Marel Dekker, Inc. Antioxidants that may be included in the oral compositions of the present invention include, but are not limited to, vitamin E, ascorbic acid, uric acid, carotenoids, vitamin A, flavanoids and polyphenols, herbal antioxidants, melatonin, aminoindoles lipoic acids and mixtures thereof.

8. Antagonists of N-2. Histamine-2 (H-2) receptor antagonists (H-2 antagonists) can be used in the oral compositions of the present invention. As used herein, selective H-2 antagonists are compounds that block H-2 receptors but do not have significant activity in blocking histamine-1 (H-1) receptors. Selective antagonists of N-2 stimulate the contraction of the smooth muscles of various organs, such as the intestines and bronchi; this effect can be suppressed by low concentrations of mepiramine, a typical antihistamine. Pharmacological receptors that are involved in mepiramine-sensitive histamine responses have been identified as H-1 receptors (Ash, A.S. F & Scbild H. O, Brit J Pharmacol Chem 1966, Vol 27, p. 427). Histamine also stimulates gastric acid secretion (Loew ER & Chickering O, Proc Soc Exp Biol Med, 1941, Vol 48, p. 65), increases heart rate (Trendelenburg U J. Pharmacol I960, Vol 130, p. 450) and inhibits contraction uterus in rats (Dews PB & Graham JDP, Brit J. Pharmacol Chem, 1946, Vol 1, p278); these actions cannot be blocked by mepiramine and similar drugs. H-2 antagonism is useful in oral care compositions or in substances that block receptors that are involved in mepiramine-insensitive non-H-1 (H-2) histamine responses and do not block receptors that are involved in mepiramine-sensitive histamine responses .

Selective H-2 antagonists are those compounds that are considered H-2 antagonists based on their properties in classical preclinical screening tests for the function of the H-2 antagonist.

Selective H-2 antagonists are identified as compounds that exhibit the function of competitive or non-competitive inhibitors of histamine-induced effects in these screening models that are specifically dependent on the function of the H-2 receptor, but do not have significant histamine antagonists in these models, depending on the function of the receptor H-1. Specifically, they include compounds that can be classified as described by Black JW, Duncan WAM, Durant CJ, Ganelline CR & Parsons EM, “Definitions and Antagonism of Histamine H2-Receptors”, Nature 1972, vol 236, pp. 385 -390, as H-2 antagonists, if assessed as described by Black in the study of guinea pigs in an experiment with spontaneous beating of the right atrium in vitro and in the study of gastric acid secretion in rats in vivo, but without significant antagonistic activity against H -1 compared with antagonistic activity against H-2, if the wire be estimate as described in Black, or in the study in guinea pigs in vitro contraction of the ileum, or in the investigation of stomach muscle contraction in vivo in rats. Preferably, the selective H-2 antagonists do not have significant activity against H-1 at moderate dose levels in the above H-1 studies. Typically, a moderate dose level is the lowest dose level at which 90% inhibition of histamine occurs, preferably 99% inhibition of histamine, which is achieved in the above H-2 studies.

Selective H-2 antagonists include compounds possessing the above criteria, which are described in US Pat. Nos. 5,294,433 and 5,364,616 to Singer et al., Issued March 15, 1994 and November 15, 1994, respectively, and referred to by Procter & Gamble in which selective H-2 antagonists selected from the group consisting of cimetidine, ethintidine, ranitidine, ICIA-5165, thiotidine, ORP-17578, lupitididine, donetidine, famotidine, roxatidiine, pifatidine, lamtidine, BL-6548, BMY-25271, zaltidine, nizatidine, mifentin23 , SKF-94482, BL-6341A, ICI -162846, ramoksotidin, Wy-45727, SR-58042, BMY-25405, lokstidin, DA-4634, bisfentidin, sufoti in, ebrotidin, HE-30-256, D-16637, FRG-8813, FRG-8701, impromidin, L-643728 and HB-408.4. Particularly preferred is cimetidien (SKF-92334), N-cyano-N'-methyl-N ″ - (2 - (((5-methyl-1H-imidazol-4-yl) methyl) thio) ethyl) guanidine:

Cimetidine is also described in Merck Indes, 11 ^th editions (1989), p. 354 (article no. 2279) and Physicians' Desk Reference, 46 ^th edition (1992), p. 2228. Related preferred H-2 antagonists include burimamide and methiamide.

9. Analgesics. Anesthetic or desensitizing agents may also be present in the oral care compositions or substances of the present invention. Such agents may include, but are not limited to, strontium chloride, calcium nitrate, wild herbs such as tannin, hoof, cubebin, galanga, scutellaria, Liangmianzhen (Latin name Radix Zanthoxyli), Chinese angelica root and so on. Analgesics also include anti-inflammatory drugs. Such agents may include, but are not limited to, non-steroidal anti-inflammatory drugs (NSAIDs) such as ketorolac, flurbinprofen, ibuprofen, naproxen, indomethacin, aspirin, ketoprofen, piroxicam and meclofenamic acid. The use of NSAIDs, such as ketorolac, is claimed in US Patent 5,626,838, issued May 6, 1997. They describe methods for the prevention and / or treatment of primary and repeated squamous carcinomas of the oral cavity or oral pharynx by topical application of an effective amount to the oral cavity or oral pharynx. NSAIDs.

10. Antiviral agents. Antiviral actives effective for the present composition include any known actives that are commonly used to treat viral infections. Such antiviral actives are described in Drug Facts and Comparisons (US Medicines Regulatory Collection), Wolters Kluer Company, St. Louis, Mo, © 1997, pp. 402 (a) -407 (z), incorporated herein by reference in full. Representative examples include the antiviral actives described in US Pat. No. 5,747,070, issued May 5, 1998 to Satyanarayana Majeti, incorporated herein by reference in its entirety. This patent describes the use of divalent tin salts for controlling viruses. Stannous salts and other antiviral actives are described in detail in Kirk and Othmer Encyclopaedia of Chemical Technology, 3 ^rd Edition, vol 23, Wiley Interscience Publishers (1982), pp. 42-71, incorporated herein by reference in full. Salts of stannous tin that can be used in the present invention may include organic tin (II) carboxylates and inorganic tin (II) halides. Although tin fluoride can be used, it is usually used only in combination with another tin halide, or with one or more tin (II) carboxylates, or with other therapeutic agents.

11. Pharmacological compounds absorbed by the mucosa.

Antitussive drugs are active substances that are especially useful for stopping uncontrolled coughing attacks. Antitussive agents effective in the present invention include, but are not limited to, groups containing codeine, dextromethorphan, dextrorphan, diphenhydramine, hydrocodone, noscapine, oxycodone, pentoxiverin, folcodine, and mixtures thereof. Among these antitussive agents, dextromethorphan is preferred. Such dextromethorphan-containing compositions may include a safe and effective amount of other antitussive / cooling actives. Particularly effective active substances are active substances that can be absorbed by mucous membranes, as described by JGHardman, The Pharmacologic Basis of Therapeutics, Ninth Edition, McGraw-Hill, New York, 1995. Other active substances that are absorbed on the mucous membrane include antihistamines facilities; non-sedative antihistamines; decongestants; expectorant; mucolytics, analgesics, antipyretic anti-inflammatory drugs, local anesthetics and mixtures thereof. Essentially, such active substances can also be included in the compositions of the present invention.

Other ingredients

In addition to these, oral care products may contain various non-essential, optional components suitable to make these compositions more suitable for use. Such conventional, optional ingredients are well known to those skilled in the art, for example, preservatives such as benzyl alcohol, methylparaben, propylparaben and imidazolinedinyl urea; cationic surfactants such as cetyltrimethylammonium chloride, lauryltrimethylammonium chloride, tricylmethylammonium chloride and di (partially hydrogenated fat) dimethylammonium chloride; thickeners and viscosity modifiers such as long chain fatty acid diethanolamide (e.g. PEG 3 lauramide), ethylene oxide and propylene oxide block polymers such as Pluronic F88, which offers BASF Wyandotte, sodium chloride, sodium sulfate, polyvinyl alcohol and ethyl alcohol; pH adjusting agents and buffering agents such as citric acid, succinic acid, phosphoric acid, sodium hydroxide, sodium carbonate and so on; sweeteners; flavors such as peppermint oil, sassafras oil, clove oil from flower buds, peppermint oil, menthol, anethole, thymol, methyl salicylate, eucalyptorl, cassia, 1-methyl acetate, sage, eugenol, parsley oil, oxanone, butterfish, alpha irizon, curly peppermint oil, marjoram, lemon, orange, propenyl guaethol, cinnamon and mixtures thereof; aromatic substances; dyes; and complexing compounds such as disodium ethylene diamine tetraacetate. Such agents are typically used individually with a content of from about 0.001% to about 10%, preferably from about 0.5% to about 5.0%, by weight of the composition.

The compositions used herein contain less than 10%, preferably less than 5%, and more preferably less than 2% by weight of volatile solvents. As described herein, volatile solvents refer to any substances of organic or silin origin that have a boiling point at 200 ° C. or lower at a pressure of one atmosphere.

In addition, the compositions used herein are intended for use without the need for curing, either hot curing or cold curing. This means that the compositions of the present invention are used alone and without any additional curing agents.

In accordance with a third aspect, the present invention relates to compositions having a viscosity of from about 1 Pa · s to about 1000 Pa · s. For all aspects of this invention, it is preferred that the compositions have a viscosity of from about 2 Pa · s to about 500 Pa · s, preferably from about 5 Pa · s to about 300 Pa · s, and more preferably from about 10 Pa · s to about 250 Pass.

Rheology Modifiers

The compositions of the present invention may optionally contain rheology modifiers that inhibit the deposition and separation of components or control deposition in a manner that facilitates dispersion and can control the properties of the rheological flow. Suitable rheology modifiers include organo-modified alumina, silicas, cellulose polymers such as hydroxypropyl methyl cellulose, xanthan gum, carbomers, inorganic clay polymers, polycarboxylates, EO / PO block copolymers (poloaxomers) thickening alumina and mixtures thereof. Preferred organophilic clays include Quaternium-18 hectorite or Stearalkonium hectorite such as Bentone 27 and 38 from Rheox, organoclay dispersions such as Bentone ISD Gel; or organomodified clay bentonites, such as Bentone 34 from Rheox or Claytone Series from Southern Clay Products; and mixtures thereof. Preferred silicas may be colloidal silicas such as Aerosil series from Degussa or Cab-o-Sil series from Cabot Corporation, silica gels such as Sylodent or Sylox series silica gels from WR Grace & Co, or precipitated silicas such as Zeothix 265 from JM Huber Corporation. Rheology modifiers are preferably presented in a composition with a content of from about 0.1% to about 15%, preferably from about 0.5% to about 10%, and most preferably from about 1% to about 3% by weight of the composition.

Carriers

The compositions used can be in various forms, for example, in the form of single-phase silicone systems, an emulsion system, such as a water-in-silicone emulsion or an oil-in-silicone emulsion, or dispersion. The advantage of introducing an additional phase into the compositions of the present invention is that the additional phase can be used to solubilize additional ingredients, for example, oral care actives that are not normally soluble in the silicone system. It is highly preferred that the compositions used herein are water-in-silicone emulsions or “water-in-silicone” dispersions, wherein the internal aqueous phase contains from about 5% to about 95%, preferably from about 25% to about 75%, more preferably from about 30% to about 60% by weight of the final composition. Moreover, it is preferable that such systems contain from about 0.001% to about 90%, preferably from about 5% to about 75%, even more preferably from about 10% to about 60% by weight of water. Moreover, it is preferable that if the composition is an emulsion or dispersion of “water in silicone”, then the internal aqueous phase contains rheology modifiers.

Getting songs

The compositions of the present invention are prepared by standard methods well known to those skilled in the art. If the composition contains more than one phase, then usually the various phases are obtained separately with any order of addition of substances of one phase. Then the two phases are combined with vigorous stirring to obtain a polyphase system, for example an emulsion or dispersion. Any ingredients in the composition with high volatility, or ingredients sensitive to hydrolysis at high temperatures, are usually added after mixing the various phases with gentle stirring.

Mode of application

The second aspect of the present invention relates to the use of a non-volatile silicone composition for caring for the oral cavity with the formation of a hydrophobic layer on the surfaces of hard and soft tissues of the oral cavity, where the composition includes:

i) from about 0.5% to about 60% by weight of a silicone polymer;

ii) from about 0.1% to about 30% by weight of silicone resin;

iii) from about 0.1% to about 95% by weight of non-volatile liquid polysiloxane, which has a viscosity of from about 1 cSt to about 1000 cSt.

The compositions of the present invention are applied to the surface of the oral cavity either using an applicator or using a finger. Compositions can either be applied to one or more specific areas of the oral cavity, or freely applied to the entire surface of the oral cavity. Due to the wetting properties, compositions applied once will quickly spread and cover a wide area. As a result, the compositions can be used to cover hard-to-reach areas of the oral cavity, such as spaces between teeth, sublingual spaces and the like. Moreover, due to the substantiality of these compositions, they will remain on the surfaces of the oral cavity for at least 2 hours, preferably 4 hours, more preferably 6 hours and most preferably 8 hours. The compositions can then be easily removed from the oral cavity by conventional hygiene procedures, such as brushing, without damaging the tissues of the oral cavity.

EXAMPLES

The following examples further illustrate preferred embodiments within the scope of the present invention. These examples are given solely for the purpose of illustration and are not intended to limit the present invention, since a large number of different variants of the present invention are possible without going beyond its scope and essence. Unless otherwise specified, all ingredients are expressed in mass percent of the composition.

Example 1:

Using a top-loading mixer, silicone resin was slowly added to pre-weighed liquid silicone. Once evenly mixed, slowly added to the polymer with stirring until the composition became visually transparent.

Example 2:

Ingredient % wt./wt. Silicone polymer (TMS 803, Wacker Chemicals) ³ 32.00 A mixture of silicone resin / liquid silicone (CF1251; GE Silicone) ¹ 53.33 Liquid Silicone (DC200 350 cSt; Dow Corning) ² 14.67 Total 100.00

Using a top-loading mixer, silicone polymer was slowly added to the pre-weighed mixture of liquid silicone / silicone resin until the mixture became uniformly mixed and visually transparent.

Example 3:

Ingredient % wt./wt. Silicone polymer (SR1000; GE Silicone) ¹ 35.00 A mixture of silicone resin / liquid silicone (CF1251; GE Triclosan) ¹ 64.70 Triclosan 0.30

Total 100.00

Using a top-loading mixer, silicone polymer was slowly added to the pre-weighed mixture of liquid silicone / silicone resin until the mixture became uniformly mixed and visually transparent.

Example 4:

Ingredient % wt./wt. Silicone polymer (SR 1000; GE Silicone) 19.82 A mixture of silicone resin / liquid silicone (SF1236; GE Silicone) 33.31 Liquid Silicone (DC200 100 cSt; Dow Corning) ² 8.47 Water 28.30 Xylitol 10.00 Methyl / Propyl Parabens 0.10 Total 100.00

Using a top-loading mixer, liquid silicone was added to a pre-weighed mixture of liquid silicone / silicone resin until the mixture became uniformly mixed and visually transparent. Xylitol and parabens were separately dissolved in water, added to a pre-prepared silicone mixture with vigorous stirring.

Example 5:

Using a top-loading mixer, liquid silicone was added to the liquid silicone / silicone resin mixture. The silicone polymer (with triclosan pre-dispersed therein) was slowly added to the pre-weighed liquid silicone / silicone resin mixture until the mixture became uniformly mixed and visually transparent. Xylitol and parabens were separately dissolved in water, added to a pre-prepared silicone mixture with vigorous stirring.

Example 6:

Ingredient % wt./wt. Silicone polymer (SR1000; GE Silicone) ¹ 10.00 A mixture of silicone resin / liquid silicone (SF1236; GE Silicone) ¹ 33.31 Liquid Silicone (DC200 350 cSt; Dow Corning) ² 7.99 Triclosan 0.30 Water 30.00 Xylitol 10.00 Glycerol 8.00 Xanthan gum (Ketrol 1000) ⁴ 0.30 Methyl / Propyl Parabens 0.10 Total 100.00

Using a top-loading mixer, liquid silicone was added to the liquid silicone / silicone resin mixture. A silicone polymer (with triclosan previously dispersed therein) was slowly added to the pre-weighed mixture of liquid silicone / silicone resin until the mixture became uniformly mixed and visually transparent. Xylitol and parabens were separately dissolved in water and added to a pre-prepared silicone mixture with vigorous stirring. Xanthan gum was previously dispersed in glycerol and added to the mixture with vigorous stirring.

Example 7

Ingredient % wt./wt. Silicone polymer (SR1000; GE Silicone) ¹ 10.00 A mixture of silicone resin / liquid silicone (SF1236; GE Silicone) ¹ 33.31 Liquid Silicone (DC200 350 cSt; Dow Corning) ² 7.89 Triclosan 0.30 Water 30.00 Xylitol 10.00 Glycerol 8.00 Xanthan gum (Ketrol 1000) ⁴ 0.30 Pemoulin TR2 (BF Goodrich) ⁵ 0.10 Methyl / Propyl Parabens 0.10 Total 100.00

Using a top-loading mixer, liquid silicone was added to the liquid silicone / silicone resin mixture. The silicone polymer (with triclosan pre-dispersed therein) was slowly added to the pre-weighed liquid silicone / silicone resin mixture until the mixture became uniformly mixed and visually transparent. Separately dispersed pemulen in water with vigorous stirring. Xylitol and parabens were dissolved in a water / pemulene mixture and added to a pre-prepared silicone mixture with vigorous stirring. Xanthan gum was previously dispersed in glycerol and added to the mixture with vigorous stirring.

Example 8:

Ingredient % wt./wt. Silicone Polymer (TMS 803; Wacker Silicone) ³ 10.00 A mixture of silicone resin / liquid silicone (DC Q2 1403; Dow Corning) ¹ 38.46 Triclosan 0.30 Water 32.64 Xylitol 10.00 Glycerol 8.00 Xanthan gum (Ketrol 1000) ⁴ 0.30 Pemoulin TR2 (BF Goodrich) ⁵ 0.10 Methyl / Propyl Parabens 0.10 Total 100.00

Using a top-loading mixer, a silicone polymer was added to the silicone resin / liquid silicone mixture (with triclosan pre-dispersed therein) until the mixture became uniformly mixed and visually transparent. Separately, pemulen was dispersed in water with vigorous stirring. Xylitol and parabens were dissolved in a water / pemulene mixture and added to a pre-prepared silicone mixture with vigorous stirring. Xanthan gum was previously dispersed in glycerol and added to the mixture with vigorous stirring.

¹ .GE Silicones 260 Hudson River Road, Waterford, New York 12188, USA.

² .dow Corning 62, Rue General De Gaulle, 1310 La Hulpe, Brussels, Belgium.

³ .Wacker-Chemie GmbH, Silicones Division, Haans-Seidel-Plate 4, D-81737 Munchen, Germany.

⁴ .Keico Dorset House, Regent Park, Kingston Road, Leatherhead, Surrey KT22 7PL, UK.

⁵ .BF Goodrich Rue de Verdunstraat, 742, B-1130, Brussels Belgium.

Claims (18)

1. Non-volatile composition for caring for the oral cavity, which includes i) from 0.5 to 60% by weight of silicone (organosilicon) polymer; ii) from 0.1 to 30% by weight of silicone resin; iii) from 0.1 to 95% by weight of non-volatile liquid polysiloxane, whose viscosity is from 1 to 1000 cSt; iv) 0.01 to 50% by weight of an active substance for caring for an oral cavity selected from substances that change the color of teeth, anti-tartar agents, anti-plaque agents, sources of fluoride ions, antimicrobial agents, nutrients , antioxidants, N-2 antagonists, analgesics, antiviral agents, pharmacological substances absorbed by the mucous membrane, and mixtures thereof; and v) less than 10% of a volatile solvent, of organic or silicone origin, which has a boiling point of 200 ° C or lower at a pressure of 1 atm. 2. The composition according to claim 1, where the silicone polymer is selected from MQ polymers, where the ratio M: Q is in the range from about 0.4 to 0.8, preferably from about 0.6 to 0.7. 3. The composition according to claims 1 and 2, which comprises from 2 to 50%, preferably from 10 to 40% and most preferably from 15 to 25% by weight of the silicone polymer. 4. The composition according to any one of claims 1 to 3, which includes from 1 to 20%, preferably from 1 to 10%, more preferably from 2 to 7% by weight of silicone resin. 5. The composition according to any one of claims 1 to 4, where the liquid polysiloxane has a viscosity of from about 2 to about 500 cSt, preferably from about 5 to about 400 cSt. 6. The composition according to any one of claims 1 to 5, which comprises from about 5 to about 90%, more preferably from about 10 to about 85%, by weight of the liquid polysiloxane. 7. The composition according to any one of claims 1 to 6, where the liquid polysiloxane is a liquid polydimethylsiloxane. 8. The composition according to any one of claims 1 to 7, where the mass ratio of silicone polymer and silicone resin is in the range from 0.1: 1 to 9: 1, preferably from 1: 1 to 7: 1, and more preferably from 1: 1 up to 5: 1. 9. The composition according to any one of claims 1 to 8, where the mass ratio of liquid polysiloxane and high molecular weight silicone resin is in the range from about 0.1: 1 to about 20: 1, preferably from about 1: 1 to about 10: 1, more preferably from about 2: 1 to about 8: 1; and most preferably from about 2: 1 to about 5: 1. 10. The composition according to any one of claims 1 to 9, where the active substance for caring for the oral cavity is selected from substances that change the color of teeth, agents that prevent the formation of tartar, agents that prevent the formation of plaque, sources of fluoride ions, antimicrobial substances and their mixtures. 11. The composition according to any one of claims 1 to 10, where the active substance for caring for the oral cavity is selected from peroxide, polyphosphates, xylitol, triclosan, tin fluoride, soluble salts of zinc, potassium nitrate and mixtures thereof; preferably from peroxide, polyphosphates, xylitol, triclosan and mixtures thereof. 12. The composition according to any one of claims 1 to 11, which contains from 0.01 to 20%, preferably from 0.01 to 10% by weight of the active substance for caring for the oral cavity. 13. The composition according to any one of claims 1 to 11, which is an emulsion of “water in silicone” and where the emulsion contains from 5 to 95%, preferably from 25 to 75%, more preferably from 30 to 60% by weight of the composition. 14. The composition according to item 13, where the internal aqueous phase contains rheology modifiers selected from polymers of cellulose, xanthan gum, carbomers, inorganic clay polymers, polycarboxylates, EO / PO block copolymers (poloxomers) thickeners based on silicon dioxide and mixtures thereof. 15. The composition according to item 13 or 14, which contains from 0.001 to 90%, preferably from 5 to 75%, most preferably from 10 to 60% by weight of water. 16. The use of a non-volatile silicone composition containing i) from about 0.5 to about 60% by weight of the silicone polymer; ii) from about 0.1 to about 30% by weight of silicone resin; iii) from about 0.1 to about 95% by weight of non-volatile liquid polysiloxane, which has a viscosity of from about 1 to about 1000 cSt as a carrier for the active substance for the care and treatment of surfaces of hard and soft tissues of the oral cavity. 17. The use according to clause 16, where the composition also includes an active substance for caring for the oral cavity, selected from substances that change the color of teeth, anti-calculus agents, anti-plaque agents, sources of fluoride ions, antimicrobial agents, nutrients, antioxidants, N-2 antagonists, analgesics, antiviral substances, pharmacological substances absorbed by the mucous membrane, and mixtures thereof. 18. Non-volatile composition for caring for the oral cavity, which includes i) from 0.1 to 30% by weight of methyl-substituted polyorganosiloxane resin with a viscosity of more than 500,000 cSt; ii) M: Q polyorganosiloxane polymer, where the ratio of M: Q is in the range from 0.6 to 0.7; iii) a non-volatile liquid polydimethylsiloxane which has a viscosity of 5 to 400 cSt; and where the mass ratio of the polyorganosiloxane polymer and polyorganosiloxane resin is in the range from 1: 1 to 7: 1 and the mass ratio of liquid polydimethylsiloxane and polyorganosiloxane resin is in the range from 2: 1 to 8: 1 and where the viscosity of the final composition is in the range from 1 to 1000 Pa s