Systems for delivering a cosmetic and/or therapeutic active to oral surfaces

The present invention relates to an oral care active ingredient delivery system for oral surfaces, an oral care product and the use of polybutene in the preparation of the delivery system.

Dental products are known for the application of various cosmetic and / or therapeutic active ingredients to the teeth and in the oral cavity. Examples of such products include: brushing agents such as dentifrices for delivering anti-caries actives such as fluoride; effervescent dentifrice tablets requiring soaking artificial teeth for a period of time to remove plaque and plaque; and mouthwashes containing breath freshening agents or antibacterial actives. However, such conventional oral care products typically do not retain the active ingredients in the oral cavity long enough to optimally enhance or prolong the action of the active ingredients providing therapeutic, prophylactic and / or cosmetic benefits.

The use of a dental strip has been found to be a convenient and inexpensive way of providing cosmetic and therapeutic benefits to the teeth and mucosal surfaces of the oral cavity. For example, dental whitening strips are known in which a whitening composition is applied to the strip and then applied to the teeth to ensure prolonged contact of the teeth with an oral care active, see e.g. WO 99/62472 to Wolf. However, in such applications, elastomeric polymers are often used as the second adhesive layer. Such adhesives provide a sustained release of the active ingredient, but may lead to the formation of a thick, sticky residue in the mouth after the strip is removed from the teeth.

In order to provide compositions that provide increased stability without causing build up of an undesirable layer of adhesive on the teeth and oral mucosa, the use of a low molecular weight polybutene applied by an integral carrier in one form of a strip of material has been disclosed.

Polybutene is known to be a component of denture adhesives and as a rubber backing. For example, US Patent No. 5,880,172 (Rajaiah et al.) Discloses a peelable denture adhesive that is easy to remove and includes polybutene as an optional component. In addition, U.S. Patent No. 5,496,541 (Cutler) relates to a tooth cleaning chewing gum and discloses the use of polybutene as an optional gum base. However, in such applications, high molecular weight non-flowable polybutene is often used in order to achieve the expected benefits thereafter.

The invention relates to an oral care active ingredient delivery system to oral surfaces comprising:

a) an integral carrier and b) a composition, characterized in that it comprises (i) a polybutene with a molecular weight of 300-3000; and (ii) a unit dose of one or more cosmetic or therapeutic active ingredients selected from the group consisting of anti-tartar agents, fluoride ion sources, stannous ion sources, bleaching agents, antimicrobial and anti-plaque agents, anti-inflammatory agents, nutrients, antioxidants , antivirals, antifungal agents, painkillers and anesthetics, H-2 antagonists, baking soda, flavoring and sensory agents, pigments and colorants, and mixtures thereof;

wherein the composition is combined with an integral carrier for the sustained release of said therapeutic or cosmetic actives onto oral surfaces.

Preferably, the delivery system comprises polybutene with a molecular weight of 750-1500.

A delivery system is preferred in which the cosmetic or therapeutic actives are selected from the group consisting of triclosan, baking soda, sodium fluoride, potassium nitrate, sodium nitrate, nystatin, grapefruit seed extract, stannous fluoride, tetrasodium pyrophosphate, monofluorophosphate, tetrachlorotetrabromofluorescein, polytetrabromofluorescein. carbamide peroxide and cetylpyridinium chloride.

Preferably, the delivery system comprises a first layer in the form of a strip of material that constitutes an integral carrier, and a second layer comprising a composition, releasably connected to the first layer, wherein the amount of the composition is less than 0.2 g / cm 2.² first layer.

PL 204 658 B1

A delivery system in which the integral carrier is in the form of a flexible strip of material with sufficient flexibility to form a curved shape on the oral surface is preferred, the strip of material conforming to the oral surface without being permanently deformed when the delivery system is placed on the oral surface. thereafter, the flexible strip of material having a first side and a second side, the composition being applied to the other side of the flexible strip of material.

A more preferred delivery system is in which the flexible strip of material further has a plurality of pockets.

Particularly preferred is a delivery system in which the flexible strip of material has a width of 0.5-4 cm, a length of 2-12 cm, and a thickness of less than 1 mm.

The invention also relates to an oral care product which comprises: a) a packaging, and

b) one or more delivery systems according to the invention, positioned within the package for delivering one or more cosmetic or therapeutic actives to surfaces in the oral cavity.

The invention further relates to the use of a polybutene with a molecular weight of 300-3000 in the manufacture of a delivery system for the sustained release of therapeutic and cosmetic actives on oral surfaces, the delivery system comprising an integral carrier and a composition comprising polybutene and one or more cosmetic or therapeutic substances. separated in a manner that is separably linked to the carrier.

In a preferred embodiment, the active ingredient is a whitening agent, preferably carbamide peroxide.

The invention also relates to the use of a 300-3000 molecular weight polybutene for the production of a delivery system for the inhibition and prophylaxis of gingivitis, caries, discoloration, fungal and bacterial growth and plaque build-up in the oral cavity by providing a composition containing polybutene and a therapeutic active ingredient on surfaces in the oral cavity.

In a preferred embodiment, the integral carrier is a flexible strip of material.

According to the invention, the low molecular weight polybutene and the cosmetic or therapeutic active ingredient are used in conjunction with the delivery system, in particular in the form of a dental strip, which provides a protective coating on the teeth. Low molecular weight polybutene is a flowing liquid that is extremely durable when applied to the teeth, but not sticky to the soft tissue of the mouth. The polybutene coating inhibits and prevents tooth discoloration and is useful for delivering an active ingredient for treating the oral cavity. After the strip is removed from the teeth, undesirable sticky residue or deposits of the composition do not form on the teeth and oral mucosa.

The systems of the invention serve to deliver the cosmetic or therapeutic active ingredient to the teeth and the oral cavity by means of an integral carrier. In one embodiment, the delivery system comprises: a first layer of strip material; a second layer comprising a polybutene of about 300-3000 molecular weight releasably connected to the strip material; and a cosmetic or therapeutic active ingredient bound to the second layer. The system of the invention provides therapeutic and cosmetic oral benefits by direct application of an integral carrier to the teeth. The integral carrier may be sized such that it overlaps the soft tissue of the mouth when applied. This provides a system useful for delivering cosmetic and therapeutic active ingredients both directly to the gingival tissue and to the teeth.

The cosmetic and therapeutic active ingredients incorporated in the second layer of the delivery system may be selected from the group consisting of the substances mentioned above, ingredients other than polybutene for tooth cleanliness, pigments, dyes, lakes and coloring agents, and mixtures thereof. Optionally, a viscosity modifier may be added to the second layer if desired.

The systems of the invention deliver therapeutic and cosmetic active ingredients to the oral cavity or to the teeth by applying a composition containing a polybutene with a molecular weight of about 300-3000 and one or more therapeutic or cosmetic active ingredients to the teeth or hard surfaces of the oral cavity. The use of the system according to the invention makes it possible to inhibit and prevent gingivitis, caries, discoloration, fungal and bacterial growth and plaque build-up in the oral cavity.

PL 204 658 B1

The systems of the invention provide for the delivery of cosmetic and therapeutic active ingredients to the teeth and the oral cavity using an integral carrier including: a first layer of carrier material; a second layer comprising a polybutene with a molecular weight of about 300-3000 and releasably connected to this support material; and a cosmetic or therapeutic active ingredient combined with the second layer.

As used herein, the term "teeth" includes natural teeth, dentures, dental plates, fillings, onlays, crowns, bridges, dental implants and the like, and any other hard surface dental prosthesis permanently or temporarily fixed in the oral cavity.

The term "safe and effective amount" as used herein means an amount of an agent (e.g., an anticalculus agent) that is high enough to significantly improve the condition being treated, but low enough to avoid serious side effects (with a reasonable benefit-risk ratio), within the range recognized. medical / dental knowledge. A safe and effective amount of the agent (e.g. of an anti-tartar agent) may vary depending upon the particular condition being treated, the age and physical condition of the patient being treated, the severity of the condition, duration of treatment, the nature of concurrent therapy, the particular form of source used, and the particular vehicle in which the agent is used.

The term "non-self-contained" is used to describe a composition that exhibits a lack of integrity and strength. Where appropriate, this means that the composition cannot be detached as one solid piece from the tooth, even after several hours of use in the mouth. The artwork cannot be cut and formed into specific shapes, such as a sheet or cone, to maintain the original dimensions.

The term "mucoadhesion" or "bioadhesion" refers to the phenomenon where a natural or synthetic substance applied to moist mucosal epithelium sticks to the mucosal layer, usually creating a new interface. (CRC Critical Review in Ther. Drug Carrier, Vol. 5, 1st Edition, p. 21 (1988)). In general, mucoadhesion can be achieved by physical and / or chemical means. This mechanism is described in the Journal of Controlled Release, vol.2, pp. 257 (1982) and Journal of Controlled Release, vol. 18 (1992), p. 249. The above publications are incorporated in their entirety as references.

"Tartar" and "salivary calculus" are used interchangeably herein to denote biological membranes in the form of mineralized plaque.

Dosage unit form refers to physically discrete units suitable as unitary dosages for humans and other mammals, each containing a predetermined amount of active ingredient calculated to achieve the desired therapeutic effect.

The term "viscosity" as used herein refers to the kinematic viscosity as measured by a standardized method of measuring Kinematic Viscosity of Transparent and Opaque Liquids (the Calculation of Dynamic Viscosity), ASTM D-445. As stated, viscosity is measured at 99 ° C (210 ° F), unless otherwise stated. The sample is placed in a U-shaped 'Cannon-Fenske' viscometer (for transparent liquids) and immersed in a constant temperature bath. The flow time between the two marks on the tube is measured and the viscosity is determined by a simple calculation taking into account the flow time and a standardized factor provided by the tube manufacturer.

As used herein, "molecular weight" refers to the number average value as determined by gel permeation chromatography. The number average molecular weight, or arithmetic average, is a function of the number of molecules in a given polymer weight. It is represented by the formula:

Σ ^NM = Σ «Μ, Σ N ~ where Ν ,, denotes the number of molecules of a given molecular weight M, an = Ν / ΣΝ denotes a number fraction of the molecular weight Mi.

Percentages and ratios throughout this specification are by weight and are based on the total weight of the composition, unless otherwise stated.

The invention will be better understood on reading the following description of the preferred embodiments, taken in conjunction with the accompanying drawing in which like reference numerals identify like elements. In one embodiment of the invention, the integral carrier is a strip of material. Without intending to limit the invention, this embodiment will be described in more detail below.

Fig. 1 is a perspective view of a substantially flat material strip with rounded corners;

PL 204 658 B1

Fig. 2 is a perspective view of the embodiment of the invention of the strip of Fig. 1, to which a second layer composition containing a polybutene having a molecular weight of about 300-3000 and a cosmetic or therapeutic active ingredient for the treatment of teeth and gingiva has been detachably bonded. ;

Fig. 3 is a cross-sectional view taken along section lines 3 - 3 in Fig. 2 of an example of a strip of material having a thickness less than the second layer overlapping it;

Fig. 4 is a cross-sectional view of an alternative embodiment of the invention, with shallow pockets in the strip of material that serve as reservoirs for an additional amount of the second layer applied to the strip;

Fig. 5 is a top view cross-sectional view of an alternative embodiment of applying the second layer composition to adjacent teeth with a matching material strip adhered to the teeth with the second layer composition between the teeth and the material strip;

Figure 6 is a cross-sectional view of a tooth taken along section lines 6-6 in Figure 5 with a strip of material fitted to the teeth and adhered to them with an oral care substance between the teeth and the strip of material;

Fig. 7 is a cross-sectional top view, similar to Fig. 5, of a strip of material fitted to the tooth and adjacent soft tissue and adhered to both sides of the tooth by means of a second layer composition between the teeth and the strip of material;

Fig. 8 is a cross-sectional view of a tooth in elevation taken along section lines 8-8 in Fig. 7 with a strip of material fitting both the tooth and adjacent soft tissue and adhered to both sides of the tooth with the second layer composition between the teeth and the strip of material;

Fig. 9 is a perspective view of an alternative embodiment of the invention comprising a strip of material coated with the second layer composition of Fig. 2 for treating teeth and adjacent soft tissue, including a release liner;

Fig. 10 is a cross-sectional view of an alternative embodiment of the invention, along section lines 10-10 in Fig. 9, with a release liner attached to the strip of material by the composition of the second layer on the strip of material.

I. The first layer

The first layer according to the invention is an integral carrier, in one embodiment a strip of material, in the system for delivering cosmetic and therapeutic active ingredients to the oral cavity.

With reference to the drawing, especially Figs. 1 and 2, there is shown a first embodiment of the invention, generally designated 10, which is a delivery system for cosmetic and therapeutic active ingredients to the teeth and the oral cavity. Delivery system 10 includes a strip of material 12 that is substantially flat and preferably has rounded sides.

On this strip of material 12 is separably applied the composition 14 of the second layer.

The composition of the second layer 14 is homogeneous and can be uniformly and continuously applied to the strip of material 12 as shown in Fig. 3. However, the second layer composition 14 may alternatively be in the form of a laminate or split layers of components, an amorphous mixture of components, discrete stripes or dots, or may form a different arrangement of different components or a combination of these structures comprising a continuous coating of the second layer composition 14 along the longitudinal axis of the strip of material portion 12. .

As shown in Fig. 4 in an alternate embodiment, shallow pockets 18 may be formed in the strip of material 12. When the second layer composition 14 forms a coating on the strip of material 12, an additional second layer composition 14, if present, fills the shallow pockets 18 forming a layer. additional reservoirs of second layer composition 14.

Figures 5 and 6 show the delivery system 24 of the invention applied to a tooth surface and a plurality of adjacent teeth. A series of adjacent teeth 22 are embedded in adjacent soft tissue 20. Adjacent soft tissue is defined herein as the soft tissue surfaces surrounding the tooth structure, including: tooth papilla, gingiva free, gingival sulcus, interdental gingiva, gingival structure on the lingual and buccal surfaces including the gingival junction and the palette.

In Figures 5 and 6, the delivery system 24 is represented by a strip of material 12 and a second layer composition 14, with the second layer composition 14 disposed on the side of the strip of material 12 facing the tooth 22. The second layer composition 14 may be pre-applied to the strip.

The material 12 or may be applied to the strip of material 12 by the user prior to application to the teeth. In an alternative embodiment, the second layer composition may be applied directly to the teeth 22 by the user and then covered with the strip of material 12. In any event, the strip of material 12 is thick and flexible / stiff to conform to the contour of the tooth 22 surface and adjacent soft tissue 20. Preferably, the strip of material has sufficient flexibility to follow the contour of the oral surface, the surface covering most of the adjacent teeth. The strip of material also easily conforms to the tooth surfaces and interdental spaces, without being permanently deformed during application. The delivery system can be applied without significant pressure.

Figures 7 and 8 show the delivery system 24 of the invention applied to the anterior and posterior surfaces of a series of adjacent teeth 22 as well as adjacent soft tissue 20. The delivery system 24 comprises a strip of material 12 and a second layer composition 14, wherein the second layer composition 14 is is located on the side of backing strip 12 facing tooth 22.

Figures 9 and 10 show a variant release liner 27. The release liner 27 is attached to the strip of material 12 by the second layer composition 14. The second layer composition 14 is on the side of the strip of material 12 facing the release liner 27.

The first layer of the delivery system according to the invention is a strip of material. Such first layer materials are described in more detail in U.S. Patent Nos. 6,136,297, 6,096,328, 5,894,017, 5,891,453, and 5,879,691 (Sagel et al., The Procter & Gamble Company) and U.S. Patent Nos. 5,989,569 and 6,045,811 to Dirksing et al. The Procter & Gamble Company).

The strip serves as a barrier to oral care substances. It prevents the second layer from leaching and / or eroding, e.g. by the user's tongue, lips and saliva. This allows the active ingredient in the second layer to act on the hard surfaces of the mouth for an extended period, ranging from several minutes to several hours.

The strip material can be polymers, natural and synthetic woven materials, non-woven material, foil, paper, rubber, and combinations thereof. The strip material can be a single layer of material or a laminate of two or more layers. Regardless of the number of layers, the strip of material is substantially water-insoluble. The strip may also be water impermeable. In one embodiment, the material is any type of polymer or combination of polymers that meet the flexural rigidity requirements and are compatible with oral care substances. Suitable polymers include, but are not limited to, polyethylene, ethylene / vinyl acetate copolymer, polyesters, ethylene / vinyl alcohol copolymer, and combinations of these polymers. Examples of polyesters include Mylar® and fluoroplastics Teflon®, both manufactured by DuPont. In one embodiment, the material is polyethylene. Typically, the thickness of the strip of material is less than about 1 mm, in one embodiment less than about 0.05 mm, and in still another embodiment about 0.001-0.03 mm. The thickness of the polyethylene strip of material is preferably less than about 0.1 mm, in one embodiment about 0.005-0.02 mm.

The strip of material may be of any shape and size sufficient to cover the desired oral surface. In one embodiment, the strip has rounded corners to avoid irritation of the soft tissue of the mouth. The term "rounded corners" means that there are no sharp angles or points. In one embodiment, the length of the strip material is about 2-12 cm, in another embodiment, about 4-9 cm. The width of the strip material will depend on the oral surface to be covered. The width of the strip is typically about 0.5-4 cm, in one embodiment about 1-2 cm. In yet another embodiment, it can be worn as a patch on one or more teeth to treat a local condition.

The strip of material may include shallow pockets. When the cosmetic or therapeutic active ingredient is applied to such a strip of material, additional amounts of the cosmetic or therapeutic active ingredient fill the shallow pockets, thereby forming reservoirs of additional cosmetic or therapeutic active ingredient. Additionally, the shallow pockets make it easier to texturize the delivery system. In one embodiment, the foil preferably has a plurality of deliberately spaced shallow pockets. Generally, the shallow pockets are approximately 0.4 mm wide and 0.1 mm deep. When shallow pockets are present on the backing strip and the thickness of the oral care substances applied is different, the overall thickness of the delivery system is generally less than about 1 mm. Preferably, the total thickness is less than about 0.5 mm.

PL 204 658 B1

Bending stiffness is a material property that is a function of the combination of strip length and width and the material's modulus of elasticity. This test is a method of measuring the stiffness of polyolefin films and sheets. It measures the bending resistance of a specimen by using a tensioning device attached to the end of a horizontal beam. The opposite end of the beam presses against the sample strip to force a portion of the strip into a vertical groove in the horizontal platform on which the sample rests. A microammeter attached to the tensioning device is calibrated in grams of deformation force. The stiffness of the sample is read directly from the microammeter and expressed in grams per centimeter of width of the sample strip. The flexural stiffness of the strip of material is less than about 5 N / m as measured by a Handle-O-Meter, model No. 211-300, available from Thwing-Albert Instrument Co., Philadelphia, PA, in accordance with ASTM Test Method D2923-95. In one embodiment, the strip has a flexural stiffness less than about 3 N / m, in another embodiment less than about 2 N / m, and in yet another embodiment about 0.1-1 N / m. Typically, the flexural stiffness of the strip of material is substantially constant and does not change during normal use. For example, the strip of material does not need to be wetted in order to achieve the low bending stiffness within the above-mentioned ranges.

The relatively low stiffness allows the strip of material to cover the contours of the mouth with very little force. This means that the conformation to the oral surface of the wearer is maintained by the fact that the strip of material has very little residual force bringing it back to its original shape just prior to application to the oral surface, i.e. the strip is substantially flat. The elasticity of the strip of material allows it to be in contact with soft tissue for an extended period of time without causing irritation. The strip of material does not require continuous pressure to be held against the oral surface.

The strip of material is held in place on the oral surface by the adhesive bond provided by the polybutene. The viscosity and general stickiness of polybutene to dry surfaces will cause the strip to stick to the oral surface without significant slippage due to the frictional forces exerted by lips, teeth, tongue and other surfaces in the mouth rubbing against the strip of material while talking, drinking, etc. . However, this adhesion to the oral surface is low enough that the user can easily remove the strip of material by simply peeling off the strip of material with the fingers.

The delivery system is easily removable from the oral surfaces without the use of an instrument, solvent, or chemical, and without excessive abrasion.

II. Second layer

Polybutene

Polybutene is a sticky copolymer of isobutylene and butene monomers. As used herein, the term "polybutene" refers to both the hydrogenated (CAS No. 68937-10-0) and the non-hydrogenated (CAS No. 9003-29-6) forms of the polymer. Polybutene is a viscous, colorless, non-drying, liquid polymer. The polybutenes range from a liquid liquid to an almost semi-solid. Polybutenes are clear, odorless, chemically durable, resistant to oxidation by light and heat, non-toxic and harmless.

The second layer according to the invention comprises a low molecular weight polybutene of about 300-3000, in another embodiment about 500-2200, and in still another embodiment about 750-1500. The viscosity of the polybutene is from about 30 mm.²/ s at 38 ° C to about 4500 mm²/ s at 99 ° C, in another embodiment from about 200 mm²/ s at 38 ° C to approx. 3500 mm²/ s at 99 ° C, and in yet another embodiment from about 75 mm²/ s at 99 ° C to about 700 mm²/ s at 99 ° C. The polybutene comprises about 0.01-100 wt.%. % of the second layer, in another embodiment from about 1-100 wt%, and in yet another embodiment from about 50-100 wt%.

The polybutene used in the invention has no elastomeric properties. Elastomers are amorphous polymers that exhibit the ability to stretch and contract to their original shape. Such elastomeric polymers must exhibit a moderate degree of cross-linking to prevent the polymer chains from slipping one after the other, and the chains must be irregular in shape to prevent the formation of crystalline regions in the polymer chains. Synthetic elastomers are described in detail in Kirk-Othmer, Encyclopedia of Chemical Technology, 4th Edition, Vol. 8, Wiley-Interscience Publishers (1996), pp. 934-955. The polybutene used in the invention is not cross-linked and does not exhibit rubbery or elastic properties. When subjected to a tensile or bending force, the polybutene useful in the invention does not return to its original shape when the force is removed.

Low molecular weight polybutene (MW = 300-3000), which is a pourable liquid known for its adhesive properties, is essentially non-mucoadhesive. This means that the polybutene,

While showing excellent adhesion to hard surfaces of the mouth, it will not adhere significantly to mucosa or moist, soft tissue in the mouth. In fact, polybutene is extremely durable when applied to teeth, denture, plaque, dental implant or other hard surfaces in the mouth, so it can be applied and applied to artificial teeth once a day. The polybutene is retained to a great extent, even after thorough brushing on hard surfaces. Consequently, polybutene, when applied to the surface of the teeth, is long-lasting and is rinse-resistant, which enables a sustained release of cosmetic and therapeutic active ingredients. Importantly, the compositions used according to the invention are not self-supporting before, during or after application to the teeth.

When applied to the teeth, the polybutene has a very smooth, clean texture, perceived by the user as a desirable clean sensation. The polybutene acts as a hard surface lubricant and reduces the friction that occurs when the tongue slides over those surfaces.

Suitable polybutenes for use in the invention include, but are not limited to: Indopol L-14, molecular weight ("MW") = 370; Indopol L-50, MW = 455; Indopol L-65, MW = 435; Indopol L100, MW = 510, H-15, MW = 600; H-25, MW = 670; H-35, MW = 725; H-40, MW = 750; H-50, MW = 815; H-100, MW = 940; H-300, MW = 1330; H-1500, MW = 2145; H-1900, MW = 2270; Panalane L-14E, MW = 370; Panalane H-300E, MW = 1330; all trade names of BP Amoco Chemicals (Chicago, IL). Other suitable grades of polybutene include Parapol 450, MW = 420; Parapol 700, MW = 700; Parapol 950, MW = 950; Parapol 1300, MW = 1300; and Parapol 2500, MW = 2700; all trademarks of ExxonMobil Corporation.

Cosmetic and / or therapeutic active substances

As already mentioned, the system according to the invention serves the delivery of cosmetic and therapeutic active substances to the teeth and the oral cavity, using polybutene together with an integral carrier. In one embodiment, the delivery system comprises: a first layer of a strip of material; and a second layer comprising a polybutene having a molecular weight of about 300-3000, releasably associated with the strip material, and a cosmetic or therapeutic active agent associated with the second layer. The second layer composition according to the invention may contain one or more cosmetic and / or therapeutic actives in unit dosage form which, by targeted application, enhances the benefits desired by the user. Examples of oral conditions that are affected by such actives include, but are not limited to, whitening, bleaching, bleaching, stain removal, other changes in the appearance and structure of teeth, and the treatment and prevention of plaque, tartar, cavities, inflammation, and / or bleeding gums, gingivitis, fungal infections such as yeast, mucosa cuts, lesions, ulcers, aphthous ulcers, herpes on the lip, dental abscesses and removal of oral malodor resulting from the above conditions and other causes such as microbial proliferation.

Suitable cosmetic and / or therapeutic actives include any ingredient that is generally considered safe for use in the oral cavity and that provides for changes in the overall appearance and / or health of the oral cavity. When a cosmetic and / or therapeutic active ingredient is present, its amount in the compositions used according to the invention is usually, unless otherwise stated, about 0.001-90%, in one embodiment about 0.01-50%, in another embodiment about 0.1 - 30 wt.% second layer composition. When the cosmetic and therapeutic actives are in particulate form, a suitable particle size for use in the invention is from about 0.01 to 1000 µm, in one embodiment from about 0.1 to 500 µm, in another embodiment from about 1 to 100 µm. The following is a non-limiting list of cosmetic and / or therapeutic active ingredients that can be used in the present invention.

Compositions used in the systems of the invention may contain at least one anti-tartar (i.e. anti-salivary) agent present in an amount of about 0.001-50 wt.%. of the second layer composition, in another embodiment about 0.01-25%, and in yet another embodiment about 0.1-15%. The anti-tartar agent should be substantially compatible with the other ingredients used in the invention. The anticalculus agent may be selected from the group consisting of polyphosphates (including pyrophosphates) and their salts; poly (aminopropanesulfonic acid) (AMPS) and its salts; polyolefin sulfonates and their salts; polyvinylphosphates and their salts; polyolefinophosphates and their salts; diphosphonates and their salts; phosphonoalkane carboxylic acid and its salts; polyphosphonates and their salts; polyvinylphosphonates and their salts; polyolefinophosphonates and their salts; polypeptides; and mixtures thereof. In one embodiment, the salts are alkali metal salts. Usually polyphosphates

The compounds are used in the form of their fully or partially neutralized water-soluble salts with alkali metals such as potassium, sodium, ammonium salts and mixtures thereof. Inorganic polyphosphate salts include alkali metal (e.g. sodium) tripolyphosphates, tetrapolyphosphates, e.g. sodium) and mixtures thereof. Polyphosphates larger than tetrapolyphosphates usually occur as glassy amorphous materials. In one embodiment, the polyphosphates are those manufactured by FMC Corporation, commercially known as Sodaphos (n-6), Hexaphos (n-13), and Glass H (n-21, sodium hexametaphosphate), and mixtures thereof. Pyrophosphate salts useful in the invention include alkali metal pyrophosphates, di-, tri-, and mono-potassium or sodium pyrophosphates, di (alkali metal) pyrophosphates, tetra (alkali metal) pyrophosphates, and mixtures thereof. In one embodiment, the pyrophosphate is selected from the group consisting of trisodium pyrophosphate, disodium dihydrogen pyrophosphate (Na₂H.₂P.₂ABOUT₇), dipotassium pyrophosphate, tetrasodium pyrophosphate (Na₄P.₂ABOUT₇), tetrapotassium pyrophosphate (K.₄P.₂ABOUT₇) and mixtures thereof. Polyolefin sulfonates include compounds in which the olefinic group contains 2 or more carbon atoms, and their salts. Polyolefinophosphonates include compounds in which the olefinic group contains 2 or more carbon atoms. Polyvinylphosphonates include polyvinylphosphonic acid. Diphosphonates and their salts include azocycloalkane-2,2-diphosphonic acids and their salts, azocycloalkane-2,2-diphosphonic acid ions and their salts, azacyclohexane-2,2-diphosphonic acid, azacyclopentane-2,2-diphosphonic acid, N-methylazacyclo-pentane-2,3-diphosphonic acid, EHDP (ethane-1-hydroxy-1,1, -diphosphonic acid), AHP (azacycloheptane-2,2-diphosphonic acid), ethane-1-amino-1,1 -diphosphonate, dichloromethane diphosphonate etc. The phosphonoalkane carboxylic acids or their alkali metal salts include PPTA (phosphonopropane tricarboxylic acid), PBTA (phosphonobutane-1,2,4-tricarboxylic acid), each in the acid form or with alkali metals. Polyolefinophosphates include compounds in which the olefinic group contains 2 or more carbon atoms. The polypeptides include poly (aspartic acid) and poly (glutamic acid).

Fluoride ion sources are known for use in oral care compositions as dental anticaries agents and may optionally be included in compositions and kits in accordance with the invention. The use of fluoride ions on tooth enamel in the case of natural teeth serves to protect the teeth against decay. A wide variety of fluoride ion releasing materials can be used as sources of soluble fluoride in the compositions of the invention. Examples of suitable fluoride ion releasing materials can be found in US Patent Nos. 3,535,421 (Briner et al.) And US Patent Nos. 3,678,154 (Widder et al.). The preferred sources of fluoride for use in the compositions of the invention include sodium fluoride, potassium fluoride, stannous fluoride, monofluorophosphate (MFP), and ammonium fluoride. In one embodiment, sodium fluoride is a source of fluoride ion. According to the invention, the fluoride ion content of the total composition is from 5 to 10,000 ppm, in one embodiment from 100 to 3,000 ppm.

Compositions used in the systems of the invention may contain a stannous source. The stannous ions can be provided by stannous fluoride and / or other stannous salts. Stannous fluoride has been found to help reduce gingivitis, plaque and sensitivity, and improve breathing. The stannous ions provided in the oral composition will benefit the person applying the composition. While efficacy may include benefits other than reduction of gingivitis, efficacy is defined as a significant reduction in in situ metabolism of plaque. Formulations providing such efficacy typically contain a concentration of stannous ions provided by stannous fluoride and / or other stannous salts in the range of about 3,000-15,000 ppm of stannous ions in the total composition. Below about 3,000 ppm of stannous ions, their efficacy is insufficient. The stannous ion is present in an amount of about 4,000-12,000 ppm, in another embodiment about 5,000-10,000 ppm. Other stannous salts include organic stannous carboxylates such as stannous acetate, stannous gluconate, stannous oxalate, stannous malonate, stannous citrate, stannous salt of ethylene glycol, stannous formate, stannous sulphate, stannous lactate, stannous tartrate, etc. Other sources of stannous ions include stannous halides such as stannous chlorides, stannous bromide, stannous iodide and stannous chloride dihydrate. In one embodiment, the stannous ion source is stannous fluoride, in another embodiment, stannous chloride dihydrate. The stannous salt combinations may be present in an amount of about 0.01-11 wt%. composition. The stannous salts may typically be present in an amount of about 0.1-7%, in one embodiment about 1-5%, and in yet another embodiment about 1.5-3% by weight. the second layer of the composition.

Antimicrobials may also be present in the compositions used in the invention. Such agents include, but are not limited to: 5-chloro-2- (2,4-dichlorophenoxy) phenol,

Commonly referred to as triclosan and described in The Merck Index, 11th edition (1989), pp. 1529 (entry No. 9573), in U.S. Patent No. 3506720 and European Patent Application No. 0251591 (Beecham Group, PLC); 8-hydroxyquinoline and its salts; copper (II) compounds, including but not limited to copper (II) chloride, copper (II) sulfate, copper (II) acetate, copper (II) fluoride and copper (II) hydroxide; phthalic acid and salts thereof, such as, but not limited to, the compounds described in US Patent No. 4,994,262, preferably magnesium monopotassium phthalate; chlorhexidine; alexidine; hexetidine; sanguinarine; benzalkonium chloride; salicylanilide; domiphen bromide; cetylpyridinium chloride (CPC); tetradecylpyridinium chloride (TPC); N-tetradecyl-4-ethylpyridinium chloride (TDEPC); octenidine; iodine; sulfonamides; bisbiguanides; phenolic compounds; delmopinol, octapinol and other piperidine derivatives; nicin preparations; zinc / stannous agents; nystatin; grapefruit extracts; apple extracts; thyme oil; thymol; antibiotics such as augmentin, amoxicillin, tetracycline, doxycycline, minocycline, metronidazole, neomycin, kanamycin, and clindamycin; analogs and salts of the above compounds; essential oils including thymol, geraniol, carvacrol, citral, hinokithiol, eucalyptol, catechin (especially 4-allyl catechin) and mixtures thereof; methyl salicylate; hydrogen peroxide; metal chlorites; and mixtures of all of the above ingredients.

The compositions used according to the invention may contain an anti-plaque agent such as stannous salts, copper salts, strontium salts, magnesium salts or dimethicone copolyol. The dimethicone copolyol is selected from C12 - C20 alkyl dimethicone copolyols and mixtures thereof. In one embodiment, the dimethicone copolyol is cetyl dimethicone copolyol available under the tradename Abil EM90. The dimethicone copolyol is generally used in an amount of about 0.001-25%, in one embodiment about 0.01-5%, and in another embodiment about 0.1-1.5% by weight. second layer composition.

The second layer composition according to the invention may contain anti-inflammatory agents. Such agents may include, but are not limited to, non-steroidal anti-inflammatory agents, oxicams, salicylates, propionic acid derivatives, acetic acid derivatives, and fenamates. Such NSAIDs include, but are not limited to, ketorolac, flurbiprofen, ibuprofen, naproxen, indomethacin, diclofenac, etodolac, indomethacin, sulindac, tolmetin, ketoprofen, fenoprofen, piroxicam, nabumetone, aspirin, diflofenazbutic acid, meflophenabutamic acid, meflophenabutic acid, and mefenfenambutic acid. acetaminophen. The use of NSAIDs such as ketorolac is claimed in US Patent No. 5,626,838. It discloses methods of preventing or treating primary and recurrent platelets of the oral cavity or oropharynx by topically administering an effective amount of NSAIDs to the oral cavity or oropharynx. Suitable steroidal anti-inflammatory drugs include corticosteroids such as fluocinolone and hydrocortisone.

Nutrients can improve the condition of the oral cavity and can be included in the compositions used according to the invention. Nutrients include minerals, vitamins, oral nutritional supplements, enteral nutrient supplements, and mixtures thereof. Suitable minerals include calcium, phosphorus, zinc, manganese, potassium, and mixtures thereof. Vitamins can be combined with minerals or used independently. Suitable vitamins include vitamin C and D, thiamine, riboflavin, calcium pantothenate, niacin, folic acid, nicotinamide, pyridoxine, cyanocobalamin, para-aminobenzoic acid, bioflavonoids, and mixtures thereof. Oral nutritional supplements include amino acids, lipotropic agents, fish oil, and mixtures thereof. Amino acids include, but are not limited to, L-tryptophan, L-lysine, methionine, threonine, levocarnitine or L-carnitine, and mixtures thereof. Lipotropic agents include, but are not limited to, choline, inositol, betaine, linoleic acid, linolenic acid, and mixtures thereof. Fish oil is rich in Omega-3 (N-3) polyunsaturated fatty acids, eicosapentaenoic acid and docosahexaenoic acid. Enteric nutritional supplements include, but are not limited to, protein products, glucose polymers, corn oil, safflower oil, medium chain triglycerides. Minerals, vitamins, oral nutritional supplements, and intestinal nutritional supplements are described in more detail in Drug Facts and Comparisons, Wolters Kluer Company, St. Louis, Mo.,^© 1997, pp. 3 - 17 and 54 - 57.

According to the invention, the whitening agent may be included as a cosmetic and / or therapeutic active ingredient in the second layer composition according to the invention. Such substances are selected from the group consisting of peroxides, metal chlorites, perborates, percarbonates, peroxyacids, persulfates, and combinations thereof. Suitable peroxide compounds include hydrogen peroxide, urea peroxide, calcium peroxide, carbamide peroxide, and mixtures thereof. In one embodiment, the peroxide compound is carbamide peroxide. Suitable metal chlorites include chlorite

Calcium, barium chlorite, magnesium chlorite, lithium chlorite, sodium chlorite and potassium chlorite. Additional whitening agents may be hypochlorite and chlorine dioxide. In one embodiment, the chlorite is sodium chlorite. In another embodiment, the percarbonate is sodium percarbonate. In one embodiment, the persulfates are oxones. The amount of such substances depends on the available oxygen or chlorine, respectively, that the molecule is able to provide for whitening the discoloration. Such an amount in the described compositions is about 0.01-40%, in one embodiment about 0.1-20%, in another embodiment about 0.5-10% of the composition, and in still another embodiment about 4-7 wt%. second layer composition.

Antioxidants have been found to be useful in oral care compositions. Antioxidants are described in publications such as Cadenas and Packer, The Handbook of Antioxidants,^© 1996, Marcel Dekker, Inc. Antioxidants that can be used in accordance with the invention include, but are not limited to, vitamin E, ascorbic acid, uric acid, carotenoids, vitamin A, flavonoids and polyphenols, herbal antioxidants, melatonin, aminoindoles, lipoic acids, and mixtures thereof.

Antiviral actives useful in the second layer compositions of the invention include any known actives routinely used in the treatment of viral infections. Such antiviral actives include, but are not limited to: phosphonomuric acid; cytosine derivatives; purine analogs such as adenosine, guanosine and inosine analogs; pyrimidine bases such as cytidine and thymidine; amantadine; Rimantadine Hydrochloride; ribavirin; zanamivir; oseltamivir phosphate; trifluridine; heterocyclic dyes; acyclovir; famciclovir; valaciclovir, cidofovir; ganciclovir; Levimisole; idoxuridine; lipophilic β-ketones; and thiosemicarbazones. Such antiviral agents are described in Drug Facts and Comparisons, Wolters Kluwer Company, St. Louis, Mo.,^© 2001, pp. 1400-1423 (b), and in KirkOthmer, Encyclopedia of Chemical Technology, 4th Edition, Vol. 3, Wiley-Interscience Publishers (1992), pp. 576-607. Specific examples include the antiviral actives disclosed herein. U.S. Patent No. 5,747,070 (Majeti). The specification also discloses the use of stannous salts to combat viruses. The stannous salts are described in more detail above. While stannous fluoride can be used as an antiviral agent, it is typically only used in combination with another stannous halide or with one or more stannous carboxylates or other therapeutic agent.

The antifungal compounds may also be included in the second layer composition according to the invention. Antifungal compounds are agents that destroy fungi or inhibit their growth. Antifungal agents useful in the invention include drugs for systemic mycoses or drugs for mucocutaneous infections. Useful antifungal agents include, but are not limited to, nystatin; miconazole; econazole nitrate; clotrimazole and flucytosine. In one embodiment, the antifungal agent is nystatin.

Analgesic or desensitizing agents may also be present in the second layer composition of the inventive system. Analgesics are agents that relieve pain by centrally acting to raise the pain threshold without disturbing consciousness or affecting other sensory modalities. Such agents may include, but are not limited to, strontium chloride, potassium nitrate, sodium nitrate, sodium fluoride, acetanilide, phenacetin, acertophan, thiorphan, spiradolin, aspirin, codeine, thebaine, levorfenol, hydromorphone, oxymorphone, fenazocin, fentanyl, buprenorphine, butaphanol, nalbuphine, pentazocine, natural herbs such as galls, asarum, cubebin, galanga, scutelleria, liangmianzhen, baizhi etc. Local anesthetics or analgesics such as acetaminophen, sodium salicylate, trolamine salicylate, lidocaine and benzocaine may also be present. Such analgesics are described in detail in Kirk-Othmer, Encyclopedia of Chemical Technology, 4th Edition, Vol. 2, Wiley-Interscience Publishers (1992), pp. 729-737.

Histamine-2 (H-2 or H2) receptor antagonist compounds (H-2 antagonists) may also be used in compositions useful in the systems of the invention. Selective H-2 antagonists herein are compounds that block H-2 receptors but have no significant activity in blocking histamine-1 receptors (H-1 or H1). Selective H-2 antagonists stimulate smooth muscle contraction in various organs such as the gut and bronchi; this effect can be suppressed by low concentrations of mepyramine, a typical antihistamine. H-2 antagonists useful in such compositions are those which block receptors involved in mepyramine insensitive, non-H-1 (H2) histamine responses, and do not block receptors involved in mepyramine sensitive histamine responses. Selective H-2 antagonists are compounds meeting the above criteria as disclosed in the patents

PL 204 658 B1

US 5,294,433 and 5,364,616 (Singer et al., Entitled The Procter & Gamble), wherein the selective H-2 antagonist is selected from the group consisting of cimetidine, ethintidine, ranitidine, ICIA-5165, thiotidine, ORF-17578, lupitidine, donethidine, famotidine, roxatidine, piphatidine, lamtidine, BL-6548, BMY-25271, zaltydine, nizatidine, mifentidine, BMY-52368 (SKF-94482), BL-6341A, ICI-162846, ramixotidine, Wy-45727, SR-58042, BMY-25405 , Locstidine, DA-4634, Bispentidine, Sufotidine, Ebrotidine, HE-30-256, D-16637, FRG-8813, FRG-8701, Impromidin, L-643728, and HB-408. Related preferred H-2 antagonists are burimamide and methiamide.

The compositions used in the systems of the invention may also contain one or more ingredients imparting the desired flavor and / or sensory properties to the compositions (heating or cooling agents). Suitable ingredients are menthol, menthyl lactate, wintergreen oil, peppermint oil, spearmint oil, cis-3-hexene-1-ol, camphor, clove oil, eucalyptus oil, anethole, methyl salicylate, eucalyptol, cassia oil, 1- acetate. 8-menthyl, eugenol, oxanone, α-irisone, propenyl guaetol, cinnamon, thymol, linalool, benzyl aldehyde, cinnamaldehyde glyceryl acetal known as CGA, and mixtures thereof, as well as cooling agents. A coolant can be a wide variety of compounds. These include substances such as carboxamides, menthol, ketals, diols and mixtures thereof. Preferred cooling agents in the composition used in the invention are paramentane carboxamide agents such as N-ethyl-p-menthane-3-carboxamide, commercially known as "WS-3",

N, 2,3-trimethyl-2-isopropylbutanamide, known as "WS-23", and mixtures thereof. Additional preferred cooling agents are selected from the group consisting of menthol, 3-1-menthoxypropane-1,2-diol, known as TK-10, manufactured by Takasago, menthone glyceryl acetal, known as MGA, manufactured by Haarmann and Reimer, and menthyl lactate, known as Frescolat®, manufactured by Haarmann and Reimer. The term menthol and menthyl as used herein includes the right- and left-handed isomers of these compounds and their racemic mixtures. TK-10 is described in US Patent No. 4,459,425 (Amano et al.), And WS-3 and other agents are described in US Patent No. 4,136,163 (Watson et al.).

Pigments may be added to the compositions used in the systems of the invention to more accurately indicate the locations where the composition is currently in contact. Additionally, such substances may be useful for modifying the color of the dentition to the satisfaction of the user. These substances contain particles which, when applied to the tooth surface, modify the surface with respect to absorption and / or reflection of light. Certain particles provide a favorable appearance when a film containing such particles is applied to the surface of the dentition. Pigments, dyes, colorants, and lakes can also be added to modify the appearance of the composition to result in a more user-friendly product. The appropriate amount of pigment is selected to achieve the effect desired by the user. For example, in the case of dentition which is particularly dark or discolored, it is usual to use pigments in an amount sufficient to lighten the teeth. On the other hand, when a particular tooth or the stains on the teeth are lighter than other teeth, pigments that darken the dentition can be useful. The amount of pigments and colorants may be approximately

0.001-20%, in one embodiment about 0.01-15%, and in another embodiment about 0.1-10%, based on the total weight of the composition.

Pigments and colorants include inorganic white pigments, inorganic color pigments, pearlescent agents, filler powders and the like; see Japanese Published Patent Application Kokai No. 9 [1997] - 100215. Specific examples are selected from the group consisting of talc, mica, magnesium carbonate, calcium carbonate, magnesium silicate, magnesium aluminum silicate, silica, titanium dioxide, zinc oxide, iron red, brown iron oxide, iron yellow, iron black, ferric ammonium ferrocyanide, violet manganese, ultramarine, nylon powder, polyethylene powder, methacrylate powder, polystyrene powder, natural silk powder, crystalline cellulose, starch, titanium mica, titanated mica with iron oxide, bismuth oxychloride, and mixtures thereof. In one embodiment, the pigments and colorants are selected from the group consisting of titanium dioxide, bismuth oxychloride, zinc oxide, Opatint D&C Red 27, CI 16185: 1 Acid 27 Lake E123, CI14720: 1 Carmosoisine Aluminum Lake E122, Red 7 Lake, or Red. 30 Lake and mixtures thereof.

Additional active ingredients useful in the invention may include, but are not limited to, insulin, steroids, herbal and other herbal remedies, and anti-cancer agents. Additionally, anti-gingivitis or gum care products can be used. Alternatively, ingredients other than polybutene can be added to give the teeth a clean impression. Such ingredients may include, for example, baking soda or Glass-H. It was further found that

Combinations of the aforementioned agents may be useful in achieving optimal results with certain forms of therapy. For example, the antimicrobial agent and the anti-inflammatory agent may be combined in a single composition to provide combined efficacy.

The second layer composition used in the invention may further comprise a viscosity modifier to inhibit settling and separation of ingredients or to control settling in a manner that facilitates redispersing, which further can regulate flow. The viscosity modifier is particularly useful in retaining oral care actives that are particulate suspended in the polybutene ingredients used in the invention. A suitable viscosity modifier may be mineral oil, clays modified with organic compounds, petroleum jelly, silicas and mixtures thereof. In one embodiment, the viscosity modifier is silica. When a viscosity modifier is used, it is used in the polybutene component of the invention in an amount of about 0.001-30%, in one embodiment about 0.01-10%, and in another embodiment about 0.1-3% of the second layer composition.

The second layer composition may optionally additionally contain one or more flavorings. Such flavorings may be selected from synthetic flavoring liquids and / or oils derived from leaves, flowers, fruits and similar parts of plants, and mixtures of these substances. Examples of liquid flavorings are vanillin, sage, marjoram, parsley oil, spearmint oil, cinnamon oil, wintergreen oil (methyl salicylate), peppermint oil, clove oil, bay oil, anise oil, and eucalyptus oil. Artificial, natural or synthetic fruit flavorings such as citrus oils, including lemon, orange, banana, grape, lime, apricot, and grapefruit oils, and fruit essences including apple, strawberry, cherry, orange, pineapple and pineapple essences are also useful. the like; flavorings derived from beans and nuts, such as coffee, cocoa, cola, peanuts, almonds, etc. Additionally, a flavoring agent adsorbed on a hydrophilic matrix may be used, eg "spray dried" flavorings. In addition, encapsulated flavorings can be used. The amount of flavor used is normally dictated by preferences with respect to factors such as flavor type and flavor strength desired. Flavorings may be used in an amount up to about 4%, in one embodiment about 0.05-3.0%, in another embodiment about 0.8-2.5% by weight. entire composition.

Compositions used in the systems of the invention may further contain sweetening agents. Suitable sweeteners include natural and artificial water-soluble, water-insoluble and intense sweeteners. The sweetening agent can be dextrose, sucrose, maltose, dextrin, dried invert sugar, mannose, xylose, ribose, glucose, fructose, levulose, galactose, corn syrup, high fructose corn syrup, corn syrup solids, partially hydrolyzed starch, aspartame, sugar alcohols such as sorbitol, mannitol, xylitol, maltitol, isomalt, and hydrogenated starch hydrolyzate, or combinations thereof. Natural or artificial intense sweeteners such as dipeptide-based intense sweeteners, monelin, thaumaoccous danielli and L-aspartyl-L-phenylalanine methyl ester and soluble saccharin salts can also be included as sweeteners. The amount of sweetener will vary depending upon the type of sweetener selected and the level of sweetness desired. Sweetening agents and flavoring agents are typically used in the oral care compositions in an amount of about 0.005 - 5 wt.%. composition.

Oral care media

It may be desirable to add one or more oral care carriers to the second layer composition.

Water may be incorporated into the composition of the second layer, preferably it should be low ion and free of organic impurities.

The second layer composition may optionally additionally contain one or more flavorings. Such flavorings may be selected from synthetic flavoring liquids and / or oils derived from leaves, flowers, fruits and similar parts of plants, and mixtures of these substances. Examples of liquid flavorings are vanillin, sage, marjoram, parsley oil, spearmint oil, cinnamon oil, wintergreen oil (methyl salicylate), peppermint oil, clove oil, bay oil, anise oil, and eucalyptus oil. Artificial, natural or synthetic fruit flavorings are also useful, such as citrus oils including lemon, orange, banana, grape, lime, apricot and grapefruit oils, and fruit essences including apple, strawberry essence,

Cherry, orange, pineapple and the like; flavorings derived from beans and nuts such as coffee, cocoa, cola, peanuts, almonds, etc. Additionally, a hydrophilic matrix adsorbed flavor may be used, eg "spray dried" flavorings. In addition, encapsulated flavorings can be used. The amount of flavor used is normally dictated by preferences with respect to factors such as flavor type and flavor strength desired. Flavorings may be used in an amount up to about 4%, in one embodiment about 0.05-3.0%, in another embodiment about 0.8-2.5% by weight. entire composition.

Compositions used in the systems of the invention may further contain sweetening agents. Suitable sweeteners include natural and artificial water-soluble, water-insoluble and intense flavors. The sweetening agent can be dextrose, sucrose, maltose, dextrin, dried invert sugar, mannose, xylose, ribose, glucose, fructose, levulose, galactose, corn syrup, high fructose corn syrup, corn syrup solids, partially hydrolyzed starch, aspartame, sugar alcohols such as sorbitol, mannitol, xylitol, maltitol, isomalt, and hydrogenated starch hydrolyzate, or combinations thereof. Natural or artificial intense sweeteners such as dipeptide-based intense sweeteners, monelin, thaumaoccous danielli and L-aspartyl-L-phenylalanine methyl ester and soluble saccharin salts can also be included as sweeteners. The amount of sweetener will vary depending upon the type of sweetener selected and the level of sweetness desired. Sweetening agents and flavoring agents are typically used in the oral care compositions in an amount of about 0.005 - 5 wt.%. composition.

Compositions used in the systems of the invention may contain surfactants, also commonly referred to as foaming agents. Suitable surfactants are those which are reasonably stable and foam over a wide pH range. Surfactants are used in an amount of about 0.001-12%, in one embodiment about 0.01-8%, and in another embodiment about 0.1-6% by weight. an oral care carrier as an ingredient of an oral care composition. The surfactant can be anionic, non-ionic, amphoteric, zwitterionic, cationic or mixtures thereof. Useful anionic surfactants include water-soluble alkyl sulfate salts having 8-20 carbon atoms in the alkyl group (e.g., sodium alkyl sulfate) and water-soluble salts of sulfonated fatty acid monoglycerides containing 8-20 carbon atoms. Sodium lauryl sulfate and sodium coconut monoglyceride sulfonate are examples of anionic surfactants of this type. Other suitable anionic surfactants are sarcosinates such as sodium lauryl sarcosinate, taurates, sodium lauryl sulfoacetate, sodium lauroyl isethionate, sodium laureth carboxylate and sodium dodecyl benzene sulfonate. Mixtures of anionic surfactants can also be used. Many suitable anionic surfactants are disclosed in US Patent No. 3,959,458 (Agricola et al.). Nonionic surfactants that can be used in the compositions described can generally be defined as those produced by the condensation of alkylene oxide groups (hydrophilic in nature) with organic hydrophobic compounds which may be aliphatic or alkyl aromatic in nature. Examples of suitable nonionic surfactants are poloxamers (sold under the trade name Pluronic), polyoxyethylene sorbitan esters (sold under the trade name Tween), ethoxylated fatty alcohols, polyethylene oxide and alkylphenol condensates, ethylene oxide condensates and propylene oxide and ethylene diamine reaction products , condensates of ethylene oxide and aliphatic alcohols, long-chain tertiary amine oxides, long chain tertiary phosphine oxides, long chain dialkyl sulfoxides, and mixtures of such materials. The amphoteric surfactants useful in the compositions described herein can be broadly defined as derivatives of secondary and tertiary aliphatic amines, in which the aliphatic group may be straight-chained or branched, and in which one of the aliphatic substituents contains about 8-18 carbon atoms, the other contains an anionic group giving them water solubility such as, for example, a carboxyl, sulfonate, sulfate, phosphate or phosphonate group. Other suitable amphoteric surfactants are betaines, in particular coconut oil acid amidopropyl betaine. Mixtures of amphoteric surfactants can also be used. Many of these suitable nonionic and amphoteric surfactants are disclosed in US Patent No. 4,051,234 (Gieske et al.).

PL 204 658 B1

Additional oral care carriers suitable for use in the second layer composition include: abrasive polishes such as silica gels and precipitated silicas; aluminum oxides and phosphates; alkali metal bicarbonates such as sodium bicarbonate; buffering agents such as monosodium phosphate, sodium hydroxide, potassium hydroxide, sodium carbonate, and imidazole; acid compounds; thickeners; humectants and xylitol.

III. Separating spacer

The release liner may be made of any material having an affinity for the second layer composition that is less than that of the second layer composition for each other and for the first layer strip material. The release liner may comprise a sheet of rigid material such as polyethylene, paper, polyester, or other material which is then coated with a non-sticky material. The release liner may be trimmed to be substantially the same size and shape as the strip of material, or the release liner may be trimmed to be larger than the strip of material to provide a readily accessible means of separating material from the strip. The release liner can be made of a brittle material that breaks when the strip is bent, or a plurality of pieces of material or a cut piece of material. Alternatively, the release liner may be in the form of two overlapping pieces, such as in a conventional adhesive bandage design. A description of materials useful as resolving agents can be found in Kirk-Othmer, Encyclopedia of Chemical Technology, 4th Edition, Vol. 21, pp. 207-218.

The method of manufacturing a delivery system according to the invention is described below.

In the delivery system described above, the second layer composition is conveniently prepared as follows: Combine the polybutene and cosmetic or therapeutic actives in a mixer and mix by any known means, e.g., with a spatula or mixer. If necessary, warm the composition to facilitate mixing. Continue mixing the composition until homogenous. When a cosmetic or therapeutic active ingredient is added in the form of solid particles, the addition of a viscosity modifier such as silica may be useful to keep the particles dispersed and suspended in the composition. Flavorings or sweeteners and other oral care carriers may also be added to the second layer composition by mixing as required.

Integral carrier material, such as a strip, can be produced by a variety of known methods for producing a film. In one embodiment, the polyethylene strip is made by a blow or pour process. Other methods including extrusion or methods that do not affect the flexural rigidity of the strip material are also useful. Additionally, the second layer composition can be applied to the strip during strip manufacture. The second layer composition may also be a laminate on the strip.

When the integral carrier is a strip of material, the second layer composition can be applied to the strip of material, or it can be applied by the user to the strip of material or applied by the user to the teeth, and the strip of material is placed over the coated teeth. The amount of the second layer composition applied to the strip of material or to the teeth will depend on the size and capacity of the piece of material, the concentration of the active ingredient, and the benefits desired. Typically less than 1 g of substance is required, preferably about 0.05-0.5 g, more preferably about 0.1-0.4 g of substance are used. The amount of composition per square cm (cm²) of the material is less than about 1 g / cm², preferably less than about 0.2 g / cm², more preferably 0.005-0.1 g / cm², even more preferably about 0.01-0.04 g / cm².

The optimal time and frequency of use will depend on the cosmetic or therapeutic effect required, the severity of the condition being treated, the health of the user, and other factors. For example, the strap can be worn at a time for a period of from about 5 minutes to 12 hours, more preferably about 5-120 minutes, and may be used about 1-7 times daily. The duration and frequency of application will depend on a number of factors, e.g. the severity of the condition, age and health of the user, etc. In addition, the duration of treatment to achieve the desired benefits, e.g. teeth whitening, may be from about 1 day to 6 months, more preferably about 1-28 days, and most preferably about 7-28 days. Due to the high degree of durability of polybutene on the teeth, the polybutene can remain adhered to the teeth for an extended period of time after removal of the strip.

There is no need to prepare the oral cavity before using the described composition. The surfaces in the mouth do not need to be drained or excessively wetted with saliva or water before

Application of the composition. However, it is believed that the adhesion to the tooth surfaces will be better when the surfaces are dry when the composition is applied.

The above-described delivery systems can be combined into a kit that includes one or more strips and instructions for use.

The following examples further illustrate and describe embodiments of the invention wherein both primary and additional ingredients are combined.

In the examples below, the second layer composition is prepared as follows: The polybutene is combined with the cosmetic or therapeutic active in a mixer and mixed thoroughly with a mechanical mixer. The composition is mixed until uniform. When the cosmetic or therapeutic active ingredient is in particulate form, a viscosity modifier such as silica may be added to the mixture in the same manner and mixed until uniform. The following values ​​are percentages by weight based on the total composition of the second layer.

Examples 1-6

<td>Ingredient</td><td colspan="6">Example</td>

<td></td><td> 1</td><td> 2</td><td> 3</td><td> 4</td><td> 5</td><td> 6</td>

<td>Polybutene¹</td><td> 87%</td><td> 99,7%</td><td> 99,742%</td><td> 99,56%</td><td> 99,84%</td><td> 75,00%</td>

<td>Glass-H</td><td></td><td> 13%</td><td></td><td></td><td></td><td> 25,00%</td>

<td>Triclozan</td><td></td><td> 0,3%</td><td></td><td></td><td></td><td></td>

<td>Timol</td><td></td><td></td><td> 0,064%</td><td></td><td></td><td></td>

<td>Eucalyptol</td><td></td><td></td><td> 0,092%</td><td></td><td></td><td></td>

<td>Menthol</td><td></td><td></td><td> 0,060%</td><td> 0,12%</td><td></td><td></td>

<td>Methyl salicylate</td><td></td><td></td><td> 0,042%</td><td></td><td></td><td></td>

<td>Menthyl lactate</td><td></td><td></td><td></td><td> 0,17%</td><td></td><td></td>

<td>Peppermint flavor</td><td></td><td></td><td></td><td> 0,15%</td><td></td><td></td>

<td>8-hydroxyquinoline salts</td><td></td><td></td><td></td><td></td><td> 0,10%</td><td></td>

<td>CuCfe ^ hfeO</td><td></td><td></td><td></td><td></td><td> 0,06%</td><td></td>

¹ Indopol H-300, MW = 1330, tradename BP Amoco Chemicals (Chicago, IL).

Examples 7 - 12

<td rowspan="2">Ingredient</td><td colspan="6">Example</td>

<td> 7</td><td> 8</td><td> 9</td><td> 10</td><td> 11</td><td> 12</td>

<td>Polybutene²</td><td> 90%</td><td> 80%</td><td> 99,955%</td><td> 99,757%</td><td> 99,97%</td><td> 99,1%</td>

<td>CPC</td><td></td><td></td><td> 0,045%</td><td></td><td></td><td> 0,09%</td>

<td>Apple extract</td><td> 10%</td><td></td><td></td><td></td><td></td><td></td>

<td>baking soda</td><td></td><td> 20%</td><td></td><td></td><td></td><td></td>

<td>Sodium Fluoride</td><td></td><td></td><td></td><td> 0,243%</td><td></td><td></td>

<td>Nystatin</td><td></td><td></td><td></td><td></td><td> 0,03%</td><td></td>

² Indopol H-40, MW = 750, tradename BP Amoco Chemicals (Chicago, IL).

PL 204 658 B1

Examples 13 - 19

<td rowspan="2">Ingredient</td><td colspan="7">Example</td>

<td> 13</td><td> 14</td><td> 15</td><td> 16</td><td> 17</td><td> 18</td><td> 19</td>

<td>Polybutene³</td><td> 90%</td><td> 90%</td><td> 90%</td><td> 99,76%</td><td> 99,76%</td><td> 99,76%</td><td> 99,066%</td>

<td>Carvacrol</td><td> 10%</td><td></td><td></td><td></td><td></td><td></td><td></td>

<td>Grapevine seed extract</td><td></td><td> 10%</td><td></td><td></td><td></td><td></td><td></td>

<td>Opatint D &amp; C Red 27</td><td></td><td></td><td></td><td> 0,24%</td><td></td><td></td><td></td>

<td>Red 7</td><td></td><td></td><td></td><td></td><td> 0,24%</td><td></td><td></td>

<td>Red 30</td><td></td><td></td><td></td><td></td><td></td><td> 0,24%</td><td></td>

<td>Grapefruit seed extract</td><td></td><td></td><td> 10%</td><td></td><td></td><td></td><td></td>

<td>Calcium peroxide</td><td></td><td></td><td></td><td></td><td></td><td></td><td> 0,934%</td>

Indopol H-100, MW = 940, tradename BP Amoco Chemicals (Chicago, IL).

Examples 20 - 25

<td rowspan="2">Ingredient</td><td colspan="6">Example</td>

<td> 20</td><td> 21</td><td> 22</td><td> 23</td><td> 24</td><td> 25</td>

<td>Polybutene⁴</td><td> 90%</td><td> 99%</td><td> 99,47%</td><td> 97,95%</td><td> 99,24%</td><td> 92,5%</td>

<td>Xylitol</td><td> 10%</td><td></td><td></td><td></td><td></td><td></td>

<td>Chlororexidine</td><td></td><td> 1%</td><td></td><td></td><td></td><td></td>

<td>Stannous fluoride</td><td></td><td></td><td> 0,53%</td><td></td><td></td><td></td>

<td>Tetrasodium pyrophosphate</td><td></td><td></td><td></td><td> 2,05%</td><td></td><td></td>

<td>Eugenol</td><td></td><td></td><td></td><td></td><td></td><td> 7,5%</td>

<td>Monofluorophosphate</td><td></td><td></td><td></td><td></td><td> 0,76%</td><td></td>

⁴ Indopol H-1900, MW = 2270, tradename BP Amoco Chemicals (Chicago, IL).

Examples 26 - 33

<td rowspan="2">Ingredient</td><td colspan="8">Example</td>

<td> 26</td><td> 27</td><td> 28</td><td> 29</td><td> 30</td><td> 31</td><td> 32</td><td> 33</td>

<td>Polybutene⁵</td><td> 81%</td><td> 81%</td><td> 81%</td><td> 80%</td><td> 56%</td><td> 80%</td><td> 81%</td><td> 100%</td>

<td>Sodium percarbonate</td><td> 19%</td><td></td><td></td><td> 19%</td><td> 19%</td><td></td><td></td><td></td>

<td>Urea peroxide</td><td></td><td> 19%</td><td></td><td></td><td></td><td></td><td></td><td></td>

<td>Calcium peroxide</td><td></td><td></td><td> 19%</td><td></td><td></td><td></td><td></td><td></td>

<td>Silica</td><td></td><td></td><td></td><td> 1%</td><td></td><td></td><td></td><td></td>

<td>Petrolatum</td><td></td><td></td><td></td><td></td><td> 25%</td><td></td><td></td><td></td>

<td>Benzocaine</td><td></td><td></td><td></td><td></td><td></td><td> 20%</td><td></td><td></td>

<td>Complex (polyvinylpyrrolidone) -peroxide</td><td></td><td></td><td></td><td></td><td></td><td></td><td> 19%</td><td></td>

Indopol H-300, MW = 1330, tradename BP Amoco Chemicals (Chicago, IL).

PL 204 658 B1

Examples 34-37

<td rowspan="2">Ingredient</td><td colspan="4">Examples</td>

<td> 34</td><td> 35</td><td> 36</td><td> 37</td>

<td>Polybutene⁶</td><td> 63,76%</td><td> 54,5%</td><td> 60,5%</td><td> 61,5%</td>

<td>Petrolatum</td><td> 10,00%</td><td> 12,5%</td><td> 12,5%</td><td> 12.5%</td>

<td>Silica</td><td> 1,00%</td><td> 1,0%</td><td> 1,0%</td><td> 1,0%</td>

<td>Glass-H</td><td> 25,00%</td><td> 25,0%</td><td> 25,0%</td><td> 25,0%</td>

<td>Peppermint oil</td><td></td><td> 6,0%</td><td></td><td></td>

<td>Aspartame</td><td></td><td> 1,0%</td><td> 1,0%</td><td></td>

<td>Opatint 27</td><td> 0,24%</td><td></td><td></td><td></td>

Indopol H-300, MW = 1330, tradename BP Amoco Chemicals (Chicago, IL).

The composition of the second layer is applied to the strip of material. The second layer may form a coating that is a uniform, continuous layer on the strip. Alternatively, the second layer can be a laminate or discrete layers of components, an amorphous mixture of components, dots, or a different arrangement of different components, or a combination of these structures.

One embodiment of the invention has been described above. Also contemplated is the possibility of using the strip of material as an applicator for applying the second layer composition to the teeth and then removing the strip material. The material of the second layer is sufficiently stable to provide a sustained release of the cosmetic and therapeutic actives in the oral cavity without leaving a strip in the oral cavity. According to the invention, it is also possible to have a water-permeable pouch-like structure in the shape of a strip or a slice that contains and releases cosmetic and therapeutic active substances in the oral cavity over time, which can be held in place by the second layer composition in the system of the invention.