Compositions comprising zinc and an antimicrobial agent

Abstract

A composition is disclosed comprising: (i) 0.1 to 10 wt% of bipolar antimicrobial particles, the precursor of which is an asymmetric 1:1 or 2:1:1 type clay particle comprising alternating tetrahedral and octahedral sheets terminating with tetrahedral sheets at one external surface plane and terminating with octahedral sheets at another external surface plane, having an antimicrobial agent attached to a coordinating cation on one of the external surface planes, wherein the antimicrobial agent is a quaternary ammonium compound; and (ii) 0.001 to 10 wt% of a zinc compound, wherein the particles have a median diameter (D50) of 0.1 to 10 μm.

Description

Technical Field

[0001] The present invention relates to antimicrobial home care and personal care compositions, wherein the antimicrobial efficacy may be manifested, for example, as inhibition of bacterial growth, malodor control or even prolonged or longer lasting hygiene benefits. The composition may be embodied in a variety of forms, such as toothpaste, or even hard surface cleaning compositions. Background Art

[0002] There are many kinds of microorganisms in our environment. They can be bacteria, viruses or even protozoa. While some microorganisms are useful to humans, some are symbiotic, and a wide variety of microorganisms are undesirable, they inhabit many living and inanimate surfaces of concern to humans.

[0003] Typically, these undesirable microorganisms multiply rapidly, and their biological activity can manifest itself, for example, as malodors on certain animate surfaces and even on inanimate surfaces. For example, when human skin is involved, such as in the armpits, on the feet, and on the scalp and hair, malodor control assumes importance. Malodor control is also important in the case of washed textiles and hard surfaces such as toilet bowls and tableware.

[0004] A wide variety of home care and personal care compositions are used for an equally wide variety of applications, including for preventing, stopping or controlling microbial activity, so that certain undesirable effects can in turn be prevented, stopped or controlled.

[0005] Certain bacteria are known to cause bad odors, such as body odor, underarm odor, and oral odor.

[0006] Generally speaking, malodor is caused by the activity of bacteria that produce certain malodorous compounds, which are called volatile sulfur compounds, such as hydrogen sulfide, methyl mercaptan, dimethyl sulfide, 3-mercapto-2-methyl-butan-1-ol and 3-mercapto-3-methylhexan-1-ol, ammonia and amines, such as trimethylamine, putrescine (1,4-diaminobutane), indole, skatole (3-methylindole), pyrazine; aldehydes, such as acrolein and butyraldehyde, alcohols, such as oct-1-en-3-ol, ketones, such as oct-1-en-3-one. On the other hand, common malodorous compounds in sweat include volatile fatty acids (VFA) and electrolytes, such as isovaleric acid, 3-methyl-2-hexenoic acid and 4-methyloctanoic acid.

[0007] Oral malodor is also known as bad breath or halitosis. It is a common non-therapeutic condition that can be alleviated by the use of toothpaste or other cosmetic oral care compositions. In extreme cases, bad breath can become a therapeutic condition requiring the use of prescription oral care products.

[0008] It is generally believed that the cause of this disease is due to anaerobic bacteria in the oral cavity, especially gram-negative anaerobes. These bacteria generate volatile sulfur compounds (VSCs) known to cause oral or breath malodor. It is also recognized in the art that oral malodor comes not only from the back of the tongue, but also from the periodontal pocket. In addition, people with gingivitis or periodontal disease may increase oral malodor due to disintegrated epithelial cells. If there is inflammation, epithelial cells are renewed faster. Therefore, a large amount of these dead epithelial cells remain in the oral cavity and degrade into malodorous compounds. The functions of dentifrice, mouthwash and similar products include neutralizing and / or removing unpleasant odors in the oral cavity, and making the user confident of fresh breath.

[0009] Dentifrice compositions such as toothpaste are a type of personal care composition that generally quickly neutralizes and drives off odor-causing compounds, and also masks any residue of odorous compounds for a short period of time thereafter. Any enhancement in the efficacy of such dentifrice compositions is highly desirable.

[0010] The addition of substances with antibacterial / antimicrobial properties to toothpastes and mouthwashes and their effect are well known. However, the effect of the active substances is only short-lived, since the concentration of the substances in question drops rapidly after oral hygiene and microbial development and bacterial growth immediately start again. In this context, it has been found that commercial oral care products show a limited long-term effect in the oral cavity, e.g. most of the active ingredients are removed from the oral cavity after cleaning the teeth by rinsing with water or, for example, by drinking or by eating food. Thus, for example, oral malodor cannot be prevented over a long period of time.

[0011] US2009010857 A (Unilever) discloses a toothpaste comprising calcium carbonate as an abrasive, water and a zinc salt, substantially all of which is in the form of water-soluble zinc citrate.

[0012] WO17167535 A1 (Unilever) discloses a toothpaste composition having a zinc salt for providing antimicrobial benefit, and having a calcium-based abrasive, montmorillonite clay and a buffering agent.

[0013] WO9939685 A1 (Unilever) discloses an oral care composition provided in the form of a transparent gel, the oral care composition comprising abrasive silica, thickening silica, a liquid vehicle containing a polyol humectant, and a low level of sodium bicarbonate. Despite the presence of bicarbonate, the product is a transparent gel or white paste, provides a teeth whitening effect and a reduction in oral malodor, and neutralizes the acid formed in the oral cavity by microbial decomposition of sugars. The composition can be colored, and different compositions with different colors, such as blue or white compositions, can be dispensed from a single compartment or multi-compartment container.

[0014] WO2003 / 002056 (Church And Dwight Co Inc.) discloses an oral composition having an antibacterial effective amount of cetylpyridinium chloride and guar hydroxypropyltrimonium chloride combined with a compound that undesirably binds to cetylpyridinium chloride, thereby enabling cetylpyridinium chloride to effectively bind to tooth surfaces and perform antibacterial functions.

[0015] US2012 / 0177712A1 (Unilever) discloses a bipolar clay-based antimicrobial particle. The precursor of this particle is an asymmetric 1:1 or 2:1:1 type clay particle comprising alternating tetrahedral and octahedral sheets terminating with tetrahedral sheets at one external surface plane and terminating with octahedral sheets at another external surface plane, with an antimicrobial group attached to a coordinating cation on one of the external surface planes, the antimicrobial group being selected from a group comprising a carbonyl group having a carbonyl group greater than or equal to C 20 A quaternary ammonium material having a single alkyl or alkenyl long chain with an average chain length of, or a quaternary ammonium material.

[0016] WO14102032 A1 (Unilever) discloses an oral care composition having bipolar antimicrobial particles as above, and wherein the antibacterial agent is a quaternary ammonium material. The composition controls bacterial regrowth and provides immediate control of bacterial counts. The composition contains chalk or any calcium-based abrasive. Summary of the invention

[0017] Applicants have now surprisingly determined that the aforementioned bipolar antimicrobial particles interact synergistically with zinc compounds, such as zinc sulfate, to provide a variety of antimicrobial benefits, particularly controlling or reducing malodor, especially oral malodor.

[0018] Thus, this synergistic interaction can be provided to consumers in the form of a variety of home care and personal care compositions.

[0019] According to a first aspect, a composition is disclosed, comprising:

[0020] (i) 0.1 to 10 wt. % of a bipolar antimicrobial particle whose precursor is an asymmetric 1:1 or 2:1:1 type clay particle comprising alternating tetrahedral and octahedral sheets terminating with tetrahedral sheets at one exterior surface plane and terminating with octahedral sheets at the other exterior surface plane, having an antimicrobial agent attached to a coordinating cation on one of the exterior surface planes, wherein the antimicrobial agent is a quaternary ammonium compound; and

[0021] (ii) 0.001 to 10 wt% of a zinc compound, wherein the median diameter (D50) of the particles is 0.1 to 10 μm.

[0022] Preferably, the composition is a home care composition. Alternatively, it is a personal care composition.

[0023] According to a second aspect, there is disclosed the non-therapeutic use of the composition of the first aspect in the form of an oral care composition for improving oral hygiene.

[0024] According to a third aspect, there is disclosed a non-therapeutic method of improving oral hygiene, the method comprising the step of applying in the oral cavity the composition of the first aspect in the form of an oral care composition.

[0025] According to another aspect, there is disclosed a packaged oral care product comprising the composition of the first aspect in the form of an oral care composition in a package, preferably with a set of instructions for using the composition. DETAILED DESCRIPTION OF THE INVENTION

[0027] By reading the following specific detailed description and the appended claims, these and other aspects, features and advantages will become clear to those of ordinary skill in the art. For the avoidance of doubt, any feature of one aspect of the present invention may be used for any other aspect of the present invention. The word "comprising" is intended to mean "including", but not necessarily "consisting of" or "consisting of". In other words, the steps or options listed do not need to be exhaustive. It should be noted that the examples given in the following description are intended to illustrate the present invention and are not intended to limit the present invention to those embodiments themselves. Similarly, unless otherwise indicated, all percentages are weight / weight percentages. Except in the operating and comparative examples or where otherwise clearly indicated, all numbers indicating the amount of material or reaction conditions, the physical properties of the material and / or the use in this specification and claims should be understood to be modified by the word "about". Numerical ranges expressed in the form of "x to y" should be understood to include x and y. When multiple preferred ranges are described in the form of "x to y" for a particular feature, it should be understood that all ranges combining different endpoints are also contemplated.

[0028] "Home care compositions" are compositions used for the treatment, cleaning, care or conditioning of the home or any of its contents. The foregoing includes, but is not limited to, compositions, products, or combinations thereof, and preparations of all of the foregoing products, that are directed to or have use or application in the treatment, cleaning, washing, care or conditioning of the home and home contents such as clothing, fabrics and / or cloth fiber surfaces, furniture and atmosphere.

[0029] "Personal care composition" is a composition used for the treatment, cleaning, care or conditioning of an individual. The foregoing includes, but is not limited to, chemicals, compositions, products, or combinations thereof, and preparations of all the foregoing, that are involved in or have uses or applications in the treatment, cleaning, washing or conditioning of a person, including, in particular, the skin, hair and oral cavity.

[0030] Unless otherwise indicated, all referring terms / expressions "weight %" or "% by weight" shall mean weight percent of the composition.

[0031] "Oral care composition" refers to a composition whose intended use may include oral care, oral hygiene, or oral appearance, or whose intended method of use may include administration to the oral cavity. In some embodiments, the oral care composition is not intended to be swallowed, but is retained in the oral cavity for a time sufficient to affect the intended utility. The oral care compositions disclosed herein can be used in non-human mammals, such as companion animals (e.g., dogs and cats), as well as humans. In some embodiments, the oral care compositions disclosed herein are for human use.

[0032] Abnormal breath is the technical term for bad breath or malodor. This is common and may affect the quality of life. Sometimes people with bad breath may still not notice it. Oral malodor is caused by the microbial action that leads to the production of volatile sulfur compounds ("VSC"), i.e., hydrogen sulfide, methyl mercaptan, and dimethyl sulfide. Therefore, treatments that can be cosmetic (non-therapeutic) or even therapeutic usually involve the reduction of microorganisms in the oral cavity, or the neutralization of VSC compounds, or by masking the malodor. A variety of oral care compositions that can be obtained in various forms can be used for this purpose. The two most common forms or products are toothpaste and mouthwash. Such compositions usually contain one or more active ingredients, which account for, for example, 0.05% by weight to up to 10% by weight of the composition. However, some actives may not reach the target site, partly because they are not combined with the desired surface.

[0033] In some cases, one or more actives can be easily washed away and therefore do not remain in the oral cavity for a long time.Therefore, there is a need for oral care compositions that enable the counteracting of malodor or the reduction of malodor over an extended period of time.

[0034] Oral malodor can be evaluated or measured by a variety of techniques. These include subjective assessment by human judgement (sensory evaluation), industrial sulfide monitoring instruments that analyze exhaled air or microbial samples taken from the mouth, and gas chromatography of exhaled air or bacterial samples taken from the mouth. Another approach is to identify bacteria that produce hydrogen sulfide (H2S) in the tongue biofilm microbial community and study the relationship between the bacterial community and H2S levels in the oral air. Oral malodor can be evaluated by gas chromatography, Breathtron, and sensory scoring. Another approach is to use a portable sulfide monitor

[0035] We used a soft tissue model to determine the efficacy of oral care compositions according to the present invention.

[0036] The procedure is as follows:

[0037] The soft tissue model is an in vitro model for measuring volatile sulfur compounds generated by salivary bacteria. The method involves collecting morning saliva from volunteers with good general and oral health. Saliva is collected, oral epithelial cells are separated, sterilized and layered on an agarose surface in a 12-well plate. The mixed salivary bacteria are then added to the plate. Next, an oral care composition is treated, in this case a toothpaste sample. Cysteine-HCl is added after treatment as a precursor for volatile sulfur compounds. Lead acetate test paper is placed on the plate to serve as an indicator of the volatile sulfur compounds generated. The dark coloration of the lead acetate test paper is recorded in the form of L*a*b* values ​​using a reflectometer, and the difference [ΔE] between the initial and final L*a*b* values ​​is used as a quantitative measure of the volatile sulfur compounds so formed. A lower ΔE indicates a more effective composition.

[0038]

[0039] Preferably, the mean measurements of three replicates are compared and the data are statistically analyzed using Tukey-Kramer analysis.

[0040] Formulation scientists have many options to choose from, as the variety of active ingredients ranges from flavorings to plant-based actives and to chemicals such as zinc compounds. For more persistent activity, a common approach is to increase the dosage of the ingredient in question. However, this can lead to secondary issues such as instability, or may even affect some other desired properties of the composition. For example, an excess of ingredients may make the formulation unpalatable or too astringent. Since the composition of the present invention may be a personal care composition, and in particular an oral care composition, a good mouthfeel may be preferred by consumers.

[0041] A variety of zinc compounds are used, for example, in oral care compositions. The most common are zinc sulfate and zinc citrate. The applicant has disclosed oral care compositions comprising the aforementioned bipolar antimicrobial particles. The aforementioned materials each provide one or more of the aforementioned technical effects. However, we have now surprisingly observed that, when used in combination, these two materials counteract or reduce malodor.

[0042] It is known that a group of technical features is considered to be a combined effect of features if the functional interaction between the features achieves a combined technical effect that is different from, for example, greater than the sum of the technical effects of the individual features. In other words, the interaction of the individual features produces a synergistic effect. This is different from a simple collection of features or characteristics.

[0043] It is believed that the bipolar antimicrobial particles and the zinc compound interact synergistically to provide a combined effect that is not simply additive.

[0044] Thus, according to a first aspect, there is disclosed a composition comprising:

[0045] (i) 0.1 to 10 wt. % of a bipolar antimicrobial particle whose precursor is an asymmetric 1:1 or 2:1:1 type clay particle comprising alternating tetrahedral and octahedral sheets terminating with tetrahedral sheets at one exterior surface plane and terminating with octahedral sheets at the other exterior surface plane, having an antimicrobial agent attached to a coordinating cation on one of the exterior surface planes, wherein the antimicrobial agent is a quaternary ammonium compound; and

[0046] (ii) 0.001 to 10 wt% of a zinc compound, wherein the median diameter (D50) of the particles is 0.1 to 10 μm.

[0047] Preferably, the composition is a home care composition. More preferably, the home care composition is a laundry detergent, a fabric conditioner, a floor cleaning composition, a toilet cleaning composition, a dishwashing composition or a surface disinfecting composition.

[0048] Alternatively, the composition is a personal care composition. Preferably, such a personal care composition is a leave-on toner, a cream, an antiperspirant, a deodorant, a lipstick, a foundation, a mascara, a sunless tanning agent, a sunscreen, a serum, a shampoo, a hair conditioner, a hair serum, a hair spray, an oral care composition, a hand wash, a shower gel, a shower gel or a soap.

[0049] It is preferred that in the antimicrobial particle the antimicrobial agent is attached to coordinating cations on the outer surfaces of the octahedral surface planes.

[0050] As the particles have an increased size, the available surface area is believed to be lower. Therefore, as the preferred particles have a significantly lower size, it is believed that a larger area is available for the antimicrobial agent to form an adduct therewith. Without being further bound by theory, it is believed that this allows for a more efficient use of the antimicrobial agent, thereby providing the opportunity to significantly reduce the dosage of the antimicrobial agent. While conventional antimicrobials require an optimized dosage of 0.2 to 0.5 wt%, the antimicrobial agent delivered in the form of the disclosed bipolar antimicrobial particles has been found to be highly effective even at a (practical) dosage of 0.001%.

[0051] While not wishing to be further bound by theory, it is believed that the preferred particles are suitably sized to fit within the interstitial spaces on the tooth surface, which is believed to be responsible for the prolonged efficacy. It is further believed that the smaller size of the particles greatly reduces any adverse interactions between the anionic surfactant and the antibacterial agent, which is believed to be responsible for a longer lasting antibacterial benefit even when the particles contain, for example, cetylpyridinium chloride, a quaternary ammonium compound.

[0052] Lower size particles also provide an effective mechanism for increasing antimicrobial loading, if so desired.

[0053] Particle size distribution (D50) is also called the median diameter or median of the particle size distribution, which is the particle size value at 50% in the cumulative distribution. It is an important parameter for characterizing particle size. For example, if D50 = 5.8 μm, 50% of the particles in the sample are larger than 5.8 μm, and 50% of the particles are smaller than 5.8 μm. D50 is often used to indicate the size of a group of particles. D50 is the size in microns, which divides the distribution into half above this diameter and half below this diameter.

[0054] The precursor of the antimicrobial particles having bipolar topospecific characteristics is preferably an asymmetric 1:1 or 2:1:1 type clay particle having alternating tetrahedral and octahedral sheets terminating with tetrahedral and octahedral sheets at the outer surface plane. 1:1 clay particles are particularly preferred as precursors. Preferred 1:1 clays include kaolinite and serpentine subclass minerals. Species included in the kaolinite subclass include, but are not limited to, kaolinite, dickite, halloysite and nacrite. Species within the serpentine subclass include, but are not limited to, chrysolite, lizardite and magnesia chlorite. Preferred 2:1:1 clays include chlorite class minerals. Chlorite contains tetrahedron-octahedron-tetrahedron sheets like 2:1 clays, with particularly weakly bonded brucite-like layers between the tetrahedral sheets. The tetrahedral sheets preferably contain coordinated tetrahedral cations of silicon. The tetrahedral sheets may also include coordinated tetrahedral cations that are not isomorphously substituted for silicon. Isomorphously substituted coordinating tetrahedral cations include, but are not limited to, cations of aluminum, iron, or boron.

[0055] The octahedral sheet preferably has a coordinated octahedral cation of aluminum. The octahedral sheet may also contain a coordinated octahedral cation that is not isomorphously substituted with aluminum. The coordinated octahedral cation of isomorphously substituted includes a cation of magnesium or iron. It is preferred that the antimicrobial agent is connected to the coordinated cation on the outside of one of the outer surface planes. Therefore, the antimicrobial agent is connected to the coordinated cation on the outside of the tetrahedral sheet. Alternatively, the antimicrobial molecule is connected to the coordinated cation on the outside of the octahedral sheet. The coordinated cation on the outside of each of the tetrahedral and octahedral surface sheets is connected to the antimicrobial molecule, provided that the antimicrobial molecule connected to the coordinated cation on the outside of the tetrahedral surface sheet is not the same as the molecule connected to the coordinated cation on the outside of the octahedral surface sheet. The antimicrobial agent is preferably connected to the coordinated cation on the outer surface of the octahedral surface plane, rather than preferably connected to the coordinated cation on the inside of the non-external tetrahedron or octahedral plane or surface sheet.

[0056] In the above mentioned antimicrobial particles, the clay:antimicrobial agent ratio is 1:0.001 to 1:1, more preferably 1:0.001 to 1:0.1. It is preferred that in the antimicrobial particles, the antimicrobial agent is attached to coordinating cations on the outer surface of the octahedral surface planes.

[0057] Further preferably, the antibacterial agent is contained in an amount of 0.05 to 20 parts by weight, more preferably 0.1 to 10 parts by weight per 100 parts of the bipolar antimicrobial particles. The median diameter (D50) of the particles is preferably 0.1 to 10 μm, more preferably 0.4 to 1 μm and most preferably 0.5 to 0.8 μm.

[0058] It is further preferred that the quaternary ammonium material is at least one of cetylpyridinium chloride (CPC), cetyltrimethylammonium chloride (CTAC), cetyltrimethylammonium bromide (CTAB), benzalkonium chloride (BKC), benzethonium chloride, cetrimonium bromide, quaternary ammonium salt, tetrabutylammonium bromide, undecylenamide propyl trimethylammonium methylsulfate, methylbenzethonium chloride, cetylethyldimethylammonium bromide, cetrimonium toluenesulfonate, coconut trimethylammonium chloride, dodecylbenzyltrimethylammonium chloride, dodecylisoquinoline bromide, dodecylpyridinium chloride, dequalinium chloride or domiphene. More preferably, the quaternary ammonium material is selected from cetylpyridinium chloride (CPC), cetyltrimethylammonium chloride (CTAC), cetyltrimethylammonium bromide (CTAB), benzalkonium chloride (BKC), benzethonium chloride, cetrimonium bromide or quaternary ammonium salt.

[0059] A particularly preferred antimicrobial agent is cetylpyridinium chloride. Without being bound by theory, it is believed that the antimicrobial activity of cetylpyridinium chloride is related to the cationic charge of its amine group. Thus, cetylpyridinium chloride is attracted to and binds to negatively charged protein moieties on the cell membrane or cell wall of microorganisms and to the tooth surface, which is also generally negatively charged. The resulting attachment to the microorganism disrupts the cell wall structure, leading to leakage of intracellular fluid and ultimately killing the associated microorganism. However, cetylpyridinium chloride is often ineffective in many systems because it tends to complex with components that carry a negative charge. When combined with clay in this manner, cetylpyridinium chloride is not available for effective contact with the tooth surface and microorganisms, rendering the active agent ineffective for its intended purpose.

[0060] For this reason, cetylpyridinium chloride is not completely effective in typical oral care products used to treat and / or prevent gingivitis, dental plaque, periodontal disease and / or breath malodor. For example, toothpaste compositions typically include anionic surfactants and artificial sweeteners. These components of toothpaste compositions will often bind to cetylpyridinium chloride, rendering it ineffective or substantially less effective as an antibacterial agent. Other components such as abrasives that are typically present in toothpaste compositions will also bind to cetylpyridinium chloride. Therefore, the use of cetylpyridinium chloride in toothpaste compositions is problematic. Even in commercial mouthwash products containing cetylpyridinium chloride, the availability of cetylpyridinium chloride on the tooth surface is very low, so its antibacterial effect is limited.

[0061] Further details of the particles can be found in WO 2011 / 036031 A1 (Unilever).

[0062] Zinc compounds

[0063] It is preferred that the zinc compound has a solubility of 0.001 to 80 g / 100 g water at 20°C.

[0064] It is preferred that the zinc compound is at least one of zinc sulfate, zinc chloride, zinc nitrate, zinc citrate, zinc oxide, zinc lactate, zinc gluconate, zinc glycinate, zinc oleate, zinc hydroxide or zinc peroxide, zinc oxide, zinc lactate, zinc chloride, zinc citrate, zinc acetate, zinc borate, zinc butyrate, zinc carbonate, zinc formate, zinc gluconate, zinc glycerate, zinc glycolate, zinc phosphate, zinc picolinate, zinc propionate, zinc salicylate, zinc silicate, zinc stearate, zinc tartrate, zinc undecylenate, zinc phosphate, zinc ricinoleate or a mixture thereof. Both insoluble and soluble zinc salts may be used alone or in combination, but it is preferred to use soluble zinc salts (zinc salts having a water solubility greater than 0.01 g / 100 g water).

[0065] Preferably, the composition comprises at least one of zinc sulfate, zinc chloride, zinc nitrate, zinc citrate, zinc oxide, zinc lactate, zinc gluconate, zinc glycinate, zinc oleate, zinc hydroxide or zinc peroxide. In some embodiments, a mixture of zinc sulfate and zinc citrate is preferred. In other embodiments, a mixture of zinc oxide and zinc sulfate is preferred.

[0066] It is particularly preferred that the personal care composition is an oral care composition.Preferably the composition is a toothpaste, a tooth powder, a breath freshening spray, a breath freshening strip, a breath freshening film, or a mouthwash.

[0067] More preferably, the composition is a toothpaste. Alternatively, and more preferably, the composition is a mouthwash.

[0068] One of the functions of mouthwashes and similar products is to remove unpleasant oral odor and reassure the user that their breath is not unpleasant. However, there remains a need for further reduction of oral odor, especially by commercially available mouthwashes with mild formulations. Mild formulations contain low levels of alcohol / no alcohol, and contain no or low levels of anionic surfactants. The term "mouthwash" generally refers to a liquid formulation used to rinse the oral surfaces and provide the user with a clean and fresh feeling in the mouth. Mouthwash is an oral care composition that is not intended to be swallowed for the purpose of systemic administration of a therapeutic agent, but is applied to the oral cavity, used to treat the oral cavity, and then expectorated.

[0069] Other ingredients

[0070] When the composition of the present invention is an oral care composition, it preferably comprises one or more of the ingredients discussed below. The exact ingredients and dosages (weight %) may depend on the nature and type of the oral care composition. For example, while toothpaste always contains an abrasive, a mouthwash does not require any abrasive.

[0071] When the composition is a toothpaste it preferably comprises from 20 to 60% by weight of one or more humectants.

[0072] For a soft and supple mouthfeel, a humectant is generally included in toothpaste. Humectants also reduce the tendency of toothpaste to lose moisture. Preferably, the humectant is at least one of glycerol, sorbitol, maltitol and xylitol. Sorbitol can be obtained as a 70% aqueous solution. Preferably, the composition contains glycerol and sorbitol for a lubricated mouthfeel, but their cumulative levels do not exceed the disclosed upper limit. Lower humectant content provides an effective way to reduce product cost.

[0073] When the composition of the present invention is a toothpaste, it preferably comprises an abrasive. The primary function of a cleaning agent or abrasive is to provide the cleaning and decontamination required for a toothpaste formulation. Typically, cleaning is directly related to the abrasiveness of the silica to the dentin and is measured by the RDA. In other words, the higher the RDA, the higher the abrasiveness. While this is generally true, some of our cleanings can provide high cleaning efficiency at reduced abrasive levels when compared to competing cleanings.

[0074] In one aspect, the abrasive is silica. Such toothpastes are typically transparent or translucent gels. The term gel indicates the physical appearance of the composition. Gel compositions are transparent to light, i.e., they allow visible light to pass through. Transparent gel toothpastes are popular with consumers. When the oral care composition of the present invention is a toothpaste in gel form, it is preferred that the composition does not contain more than 5 wt%, preferably more than 2 wt%, and more preferably more than 1 wt% of a calcium-based abrasive. Calcium-based abrasives may affect the transparent nature of the composition.

[0075] On the other hand, there are some other types of dentifrice compositions which are not gels but are not transparent. This is because such compositions usually contain opaque ingredients such as chalk or other calcium-based abrasives.

[0076] Preferably, the composition comprises 5 to 20 wt% silica. Further preferably, the composition of silica consists of medium abrasive and high abrasive silica, wherein the medium abrasive silica is in the majority. Their relative proportions may vary. Preferably, the abrasive silica is a low refractive index silica, with an apparent refractive index in the range of 1.41 to 1.47, preferably 1.435 to 1.4451, preferably with a weight average particle size of 5 to 15 μm and a BET (nitrogen) surface area of ​​10 to 100 m 2 / g, and the oil absorption is about 70 to 150cm 3 / 100g. Examples of suitable low refractive index abrasive silicas with an RI between 1.435 and 1.445 are Tixosil 63 and 73 available from Rhone Poulenc; Sident 10 available from Degussa; Zeodent 113 available from Zeofinn; Sorbosil AC 77 available from Ineos with an RI of approximately 1.440. Other examples include and A series of abrasive silica.

[0077] Further preferably, the oral care composition comprises 2 to 15 wt % thickening silica. The main function of thickening silica is to build viscosity without increasing the level of abrasion (RDA) in the overall formulation. Moreover, they can be used as structuring agents in formulations using alternative abrasives other than silica. The grades of our thickening silica can be classified according to their physical characteristics. These physical characteristics have an impact on the rheology of the formulation. For example, and perhaps more relevantly, the higher the oil absorption of the thickener, the higher the viscosity imparted to the formulation. In addition to having a significant impact on the viscosity of the toothpaste system, thickening silica also plays a role in the mouthfeel of the paste. If the content of detergent in the system is low, the formulator may wish to use a less effective thickener to achieve a total solids level consistent with the desired mouthfeel. Typically, the paste formulation should include a total silica concentration of at least 15% up to 30%. The division of this percentage between thickener and detergent depends on the choice of silica, the desired cleaning level, etc.

[0078] This is particularly true when the composition includes silica as an abrasive. A wide variety of thickening silicas are commercially available to choose from. When present, preferred thickening silicas include T series (from Degussa) or CAB-O- series (obtained from Cabot Corporation), silica gel, such as or series (obtained from WR Grace & Co), or precipitated silica, such as 265 (available from JM Huber Corporation). Useful silica thickeners also include 165. 163 and / or 167 and 153, 177 and / or 265 silica (all available from JM Huber Corporation). Other preferred thickening silicas include -P (obtained from Madhu Silica), 22S and 200 (purchased from Evonik Industries), and Thickening silica (available from WR Grace & Company), and 43 and 331 (available from Rhodia), synthetic finely divided fumed silica, such as those sold under the trademark 244, 266 and Those sold by D-200.

[0079] Alternatively, the oral care composition of the present invention comprises a calcium-based abrasive. A particularly preferred abrasive is finely ground natural chalk (FGNC). It is obtained from limestone or marble. FGNC can also be chemically or physically modified by thermal treatment during or after grinding by coating. Typical coating materials include magnesium stearate and magnesium oleate. The morphology of FGNC can also be changed during the grinding process by using different grinding techniques such as ball milling, air classification grinding or spiral jet grinding. FGNC can be used as the only calcium-containing abrasive. However, FGNC can also be used together with other calcium-containing abrasives to balance abrasion.

[0080] Other preferred calcium-based abrasives include dicalcium phosphate (DCP), calcium pyrophosphate and precipitated calcium carbonate (PCC). When a combination of calcium-based abrasives is used, it is preferred that FGNC is 35 to 100%, more preferably 75 to 100% and especially 95 to 100% of the total abrasive. In this case, the remainder is most preferably PCC.

[0081] Other abrasives may also be used, depending on the desired degree of wear and the composition of the paste. These include synthetic abrasive polishing agents such as amorphous precipitated silica and silica gel. Other abrasives include magnesium carbonate, sodium metaphosphate, potassium metaphosphate, zirconium silicate, potassium metaphosphate, magnesium orthophosphate, tricalcium phosphate, magnesium orthophosphate, trimagnesium phosphate, aluminum silicate, zirconium silicate and perlite.

[0082] Accordingly, the mouthwash composition preferably comprises an aqueous continuous phase. The amount of water is typically in the range of 70 to 99 wt%. The mouthwash composition preferably comprises other ingredients that enhance performance and / or consumer acceptability, such as humectants and surfactants. The amount of humectant is typically in the range of 4 to 20 wt%, more preferably 7 to 15 wt%, based on the total weight of the mouthwash. Preferred humectants present at the above levels include polyols, particularly preferred is sorbitol.

[0083] Surfactants

[0084] Oral care compositions, especially toothpastes, typically contain surfactants, which are also commonly referred to as foaming agents. Suitable surfactants are those that are reasonably stable over a wide pH range and provide foam. It is preferred that the composition comprises an anionic surfactant.

[0085] Anionic surfactants useful herein include water-soluble alkyl sulfates having 8 to 20 carbon atoms in the alkyl group (e.g., sodium alkyl sulfate), and water-soluble salts of sulfonated monoglycerides of fatty acids having 8 to 20 carbon atoms. Sodium lauryl sulfate and sodium coconut monoglyceride sulfonate are examples of this type of anionic surfactant.

[0086] Preferably, the oral care composition comprises from 0.25 to 12 wt %, more preferably from 0.5 to 8 wt %, and most preferably from 1 to about 6 wt % of anionic surfactant.

[0087] Some anionic surfactants, particularly sodium lauryl sulfate, have an antimicrobial effect of their own. Such an action provides a degree of immediate antimicrobial effect. However, this effect is usually very short-lived. Other surfactants may also be included, such as nonionic, amphoteric or zwitterionic surfactants.

[0088] Nonionic surfactants can be broadly defined as compounds produced by the condensation of alkylene oxide groups (hydrophilic in nature) with an organic hydrophobic compound which may be aliphatic or alkyl aromatic in nature.

[0089] Examples of suitable nonionic surfactants include poloxamers (available under the trade name Sold), polyoxyethylene, polyoxyethylene sorbitan esters (trade name sell), 40 Hydrogenated castor oil, fatty alcohol ethoxylates, polyethylene oxide condensates of alkylphenols, products derived from the condensation reaction of ethylene oxide with the reaction product of propylene oxide and ethylenediamine, ethylene oxide condensates of aliphatic alcohols, long chain tertiary amine oxides, long chain tertiary phosphine oxides, long chain dialkyl sulfoxides, and mixtures of these materials.

[0090] Further preferably, the oral care composition of the present invention comprises a thickening system comprising thickening silica and at least one of carboxymethyl cellulose, xanthan gum or guar gum. Other binders and thickeners such as sodium carboxymethyl cellulose, xanthan gum, gum arabic, and synthetic polymers such as polyacrylates and carboxyvinyl polymers such as It is preferred that the dentifrice composition of the present invention comprises a thickening system comprising thickening silica and at least one of carboxymethylcellulose, xanthan gum or guar gum.

[0091] Preferred oral care compositions comprise a binder which imparts good structure to the paste. Cellulosic binders are particularly preferred. Preferred cellulosic binders include cellulose ethers, including hydroxyethyl cellulose (HEC), hydroxypropyl cellulose (HPC), ethyl hydroxyethyl cellulose (EHEC), carboxymethyl cellulose (CMC), carboxymethyl hydroxyethyl cellulose (CMHEC), hydroxypropyl hydroxyethyl cellulose (HPHEC), methyl cellulose (MC), methyl hydroxypropyl cellulose (MHPC), methyl hydroxyethyl cellulose (MHEC), carboxymethyl methyl cellulose (CMMC), hydrophobically modified carboxymethyl cellulose (HMCMC), hydrophobically modified hydroxyethyl cellulose (HMHEC), hydrophobically modified hydroxypropyl cellulose (HMHPC), hydrophobically modified ethyl hydroxyethyl cellulose (HMEHEC), hydrophobically modified carboxymethyl hydroxyethyl cellulose (HMCMHEC), hydrophobically modified hydroxypropyl hydroxyethyl cellulose (HMHPHEC), hydrophobically modified methyl cellulose (HMMC), hydrophobically modified methyl hydroxypropyl cellulose (HMMHPC), hydrophobically modified methyl hydroxyethyl cellulose (HMMHEC), and hydrophobically modified carboxymethyl methyl cellulose (HMCMMC).

[0092] Other cellulosic binders include cationic hydroxyethyl cellulose (cationic HEC), cationic hydrophobically modified hydroxyethyl cellulose (cationic HMHEC), and microcrystalline cellulose.

[0093] A highly preferred binder is sodium carboxymethylcellulose (SCMC). Particularly preferred sodium carboxymethylcelluloses include those having a degree of substitution of from 0.6 to 0.99, preferably from 0.7 to 0.95.

[0094] Preferred toothpaste compositions may also include one or more other thickening agents, such as carboxyvinyl polymers, including A series of carbomers commercially available from BF Goodrich include 934, 940, 941 and 956.

[0095] Other preferred grades include Acrylate / Acrylic C 10-30 Alkyl ester crosslinked polymers, which can twenty one, TR-1 and TR-2 is commercially available from Noveon Corporation.Preferred compositions may include from 0.05 to 10 wt %, more preferably from 0.1 to 5 wt %, even more preferably from 0.25 to about 4 wt % of other thickeners.

[0096] The oral care compositions of the present invention may contain optional other ingredients, such as a cosmetically acceptable carrier, such as starch or sucrose.

[0097] Preferred compositions may have an alkali metal silicate. The alkali metal is sodium or potassium, preferably sodium. Sodium silicate is usually available as a 10 to 40% aqueous solution, most commonly a 30% solution. Sodium silicate may be available as a neutral sodium silicate or an alkaline sodium silicate. Preferred toothpastes have a neutral sodium silicate. Sodium silicate is available in different Na2O:SiO2 ratios.

[0098] Sodium silicate having a Na2O:SiO2 ratio in the range of 3.0 to 3.8 is preferred, with a more highly preferred range of 3.25 to 3.5. Preferred toothpastes include 0.1 to 5% by weight of silicate (on a dry weight basis). Thus, a 30% sodium silicate solution is added to the composition in an amount of 0.3 to 16% by weight.

[0099] Flavoring agents such as peppermint and spearmint oils, as well as preservatives, colorants, pH adjusters, sweeteners, and the like may also be included. Suitable flavoring components include wintergreen oil, peppermint oil, spearmint oil, clove bud oil, menthol, anethole, methyl salicylate, eucalyptol, cinnamon, 1-menthyl acetate, sage, eugenol, parsley oil, oxanone, α-ionone, marjoram, lemon, orange, allyl guaiacol, cinnamon, vanillin, ethyl vanillin, jasminaldehyde, 4-cis-heptenal, diacetyl, methyl-p-tert-butylphenyl acetate, and mixtures thereof. Cooling agents may also be part of the flavoring system. Preferred cooling agents are p-menthane carboxyamide agents, such as N-ethyl-p-menthane-3-carboxamide (commercially known as "WS- ”) and mixtures thereof. Flavoring agents are generally present in an amount of 0.001 to 5% by weight.

[0100] Anti-caries agents may also be included, such as sodium fluoride and stannous fluoride, amine fluoride, monosodium fluorophosphate, casein, plaque buffers such as urea, pyruvate, arginine, small peptides, calcium lactate, calcium glycerophosphate, strontium polyacrylate. A preferred anti-caries agent is sodium monofluorophosphate. Other optional ingredients include vitamins such as vitamin C and plant extracts.

[0101] Desensitizing agents such as potassium bicarbonate, potassium oxalate, potassium nitrate, and strontium salts may also be included.

[0102] Buffers and salts may also be included to buffer the pH and ionic strength of the composition.Liposomes and other capsules may also be used to improve the delivery or stability of active ingredients.

[0103] Additionally, the oral care composition may contain anticalculus agents such as alkaline earth metal pyrophosphates, hypophosphite-containing polymers, organic phosphonates, phospho-citrate salts, and the like.

[0104] Other optional ingredients that may be included are, for example, bleaching agents such as peroxy compounds, for example potassium peroxydiphosphate, effervescent systems such as sodium bicarbonate / citric acid systems, and color change systems.

[0105] The compositions of the present invention may also contain colored particles suspended therein, such as colored silica agglomerates or other colored particles, to give the dentifrice a "muddy" appearance. The oral care composition may also contain stripes of colored paste to provide a visually clear gel-type dentifrice with colored stripes or a separate colored phase.

[0106] Toothpastes with calcium-containing abrasives, especially chalk, are susceptible to bacterial growth. Certain preservatives, such as methyl, ethyl, butyl, propyl and isopropyl p-hydroxybenzoates, are particularly useful in combating bacterial growth. A mixture of methyl, ethyl, butyl and propyl p-hydroxybenzoates is particularly preferred.

[0107] The activity of the mixture can be enhanced by the addition of phenoxyethanol. Formaldehyde and dimethylhydantoin are other preferred preservatives. Typically 0.005 to 0.8% by weight of preservative is included.

[0108] The oral care composition of the present invention is prepared by conventional methods for preparing oral care compositions. Such methods include mixing the ingredients under moderate shear and atmospheric pressure.

[0109] Typically, the compositions are packaged.

[0110] In toothpaste or gel form, the composition may be packaged in conventional plastic laminates, metal tubes or single compartment dispensers. It may be applied directly to the tooth surface to sensitive areas by any physical means such as a toothbrush, fingertips or through an applicator.

[0111] The composition is effective even when used in an individual's daily oral hygiene routine. For example, the composition can be brushed onto the teeth. The composition can, for example, be in contact with the teeth for a period of 1 second to 20 hours. More preferably 1 second to 10 hours, still more preferably 10 seconds to 1 hour and most preferably 30 seconds to 5 minutes. The composition can be used daily, for example, once, twice or three times a day by an individual. When the oral care composition is a two-phase composition, the two phases of the composition are mixed during application. The mixed phase is usually left on the teeth for 3 minutes to 10 hours, more preferably 3 minutes to 8 hours. Application can be performed one to five times per month.

[0112] In some embodiments, the method includes the step of rinsing the oral cavity with a composition as described herein. In some embodiments, 5 ml or more of the composition is rinsed. In some embodiments, 10 ml or more is used. In some embodiments, 10-50 ml is used. In some embodiments, 15-25 ml or more is used. In some embodiments, 15 ml or more is used. In some embodiments, the individual rinses the mouth with the composition multiple times a day. In some embodiments, the individual rinses the mouth with the composition over multiple days. In some embodiments, the individual rinses the mouth with the composition up to 6 times every 4 to 6 hours per day.

[0113] According to a second aspect, there is disclosed the non-therapeutic use of the composition of the first aspect in the form of an oral care composition for treating halitosis.

[0114] Preferably, the oral hygiene is improved at least by reducing oral malodour in the user. Preferably, oral malodour is caused by the activity of salivary bacteria which generate volatile sulphur-containing compounds at least on the soft tissues in the oral cavity. Further preferably, the malodour is reduced due to a reduction in the volatile sulphur-containing compounds. In one aspect, the use is for non-therapeutic purposes. Alternatively, the use is for therapeutic purposes.

[0115] Therapeutic treatment can be summarized as measures involving the maintenance (prevention) or restoration (therapy) of health. "Therapy" involves restoring the body to its normal healthy state from a pathological state as well as preventing pathological states. Treatment in the therapeutic sense is defined as any treatment designed to cure, alleviate, remove or lessen the symptoms of any disorder or malfunction of the human or animal body, or to prevent or reduce the likelihood of contracting any condition or malfunction.

[0116] According to a third aspect, there is disclosed a non-therapeutic method of treating bad breath, the method comprising the step of applying in the oral cavity the composition of the first aspect in the form of an oral care composition.

[0117] According to another aspect, a composition for use as a medicament for treating abnormal breath or halitosis is disclosed, the composition comprising:

[0118] (i) 0.1 to 10 wt. % of a bipolar antimicrobial particle whose precursor is an asymmetric 1:1 or 2:1:1 type clay particle comprising alternating tetrahedral and octahedral sheets terminating with tetrahedral sheets at one exterior surface plane and terminating with octahedral sheets at the other exterior surface plane, having an antimicrobial agent attached to a coordinating cation on one of the exterior surface planes, wherein the antimicrobial agent is a quaternary ammonium compound; and

[0119] (ii) 0.001 to 10 wt% of a zinc compound, wherein the median diameter (D50) of the particles is 0.1 to 10 μm.

[0120] Preferably, the use of the above composition reduces at least one volatile sulfur-containing compound present in the oral cavity by at least 30%. Further preferably, the reduction is 30% to 90%. The volatile sulfur-containing compound is preferably at least one of hydrogen sulfide, methyl mercaptan, or dimethyl sulfide.

[0121] According to another aspect, a packaged oral care product is disclosed, comprising the oral care composition of the first aspect in a package, preferably with a set of instructions for using the composition.

[0122] The invention will now be further described with reference to the following non-limiting examples. DETAILED DESCRIPTION

[0123] Example

[0124] Example-1: Oral Care Compositions—Formulation and Testing

[0125] A series of toothpastes were prepared. Details are included in Table 1. Compositions 1, 2 and 3 are outside the scope of the present invention, PL indicates a placebo formulation. Compositions Example 1 and Example 2 are within the scope of the present invention.

[0126] All formulations of Table 1, including placebo, were subjected to malodor evaluation using the soft tissue model described above. The observations are also summarized in the table, including statistical significance according to Anova and Tukey tests.

[0127] Table 1

[0128]

[0129] Note*: This particle has 2.7% cetylpyridinium chloride on kaolin. Therefore, the composition of the particle is 2.7% by weight cetylpyridinium chloride and 97.3% by weight kaolin. For example, in Example 2, the effective amount of quaternary ammonium compound in the toothpaste formulation is 0.027% by weight. The D50 of the particle is 0.5 μm.

[0130] For statistical significance, since the experiments were paired, compositions not associated with the same letter are significantly different.

[0131] Because ΔE represents malodor reduction, it is inversely proportional to the efficacy of the composition. In other words, a composition with a lower ΔE is more effective than a composition with a higher ΔE.

[0132] Therefore, the data in Table 1 clearly indicate that Example 1 and Example 2 produce statistically significant improvements in oral hygiene compared to placebo. The data in Table 1 also clearly show that Example 1 and Example 2 produce significant improvements in oral hygiene compared to Compositions 1, 2 and 3 of Comparative Compositions outside the scope of the present invention. Oral hygiene improves the reduction of oral malodor in the user. According to the procedure, malodor is caused by the activity of salivary bacteria, which produce volatile sulfur-containing compounds at least on the soft tissue (tongue) in the oral cavity. It is clearly clear that the use of the composition according to the present invention reduces oral malodor by reducing volatile sulfur-containing compounds.

[0133] The exemplary embodiments clearly demonstrate that the bipolar antimicrobial particles interact synergistically with the zinc compound (zinc sulfate in the embodiments) to provide a variety of antimicrobial benefits, especially controlling or reducing malodor, especially oral malodor. Thus, this synergistic interaction can be utilized and provided to consumers in a variety of home care and personal care compositions.

Claims

1. A composition comprising: i) 0.1 to 10 wt. % of a bipolar antimicrobial particle whose precursor is an asymmetric 1:1 or 2:1:1 type clay particle comprising alternating tetrahedral and octahedral sheets terminating with tetrahedral sheets at one exterior surface plane and terminating with octahedral sheets at the other exterior surface plane, an antimicrobial agent attached to a coordinating cation on one of the exterior surface planes, wherein the antimicrobial agent is cetylpyridinium chloride; and ii) 0.001 to 10% by weight of a zinc compound, wherein the median diameter D50 of the bipolar antimicrobial particles is 0.1 to 10 μm; The zinc compound is zinc sulfate, zinc chloride, zinc nitrate, zinc citrate, zinc oxide, zinc lactate, zinc gluconate, zinc glycinate, zinc oleate, zinc hydroxide or zinc peroxide.

2. The composition according to claim 1, wherein the composition is a home care composition.

3. The composition of claim 2, wherein the home care composition is a laundry detergent, a fabric conditioner, a floor cleaning composition, a toilet cleaning composition, a dishwashing composition or a surface disinfecting composition.

4. The composition of claim 1, wherein the composition is a personal care composition.

5. The composition of claim 4, wherein the personal care composition is a leave-on toner, a cream, an antiperspirant, a deodorant, a lipstick, a foundation, a mascara, a sunless tanning agent, a sunscreen, a serum, a shampoo, a hair conditioner, a hair spray, an oral care composition, a hand wash, a body wash, a shower gel, or a soap.

6. The composition of claim 4, wherein the personal care composition is a hair serum.

7. The composition according to any one of claims 1 to 6, wherein the zinc compound has a solubility of 0.001 to 80 g / 100 g water at 20°C.

8. The composition of any one of claims 4 or 5, wherein the personal care composition is an oral care composition.

9. Non-therapeutic use of a composition according to any one of claims 1 to 8 for treating halitosis.

10. A non-therapeutic method for treating bad breath, comprising the step of applying the composition according to any one of claims 1 to 8 in the oral cavity.

11. A composition for use as a medicine for treating abnormal breath or halitosis, comprising: i) 0.1 to 10 wt. % of a bipolar antimicrobial particle whose precursor is an asymmetric 1:1 or 2:1:1 type clay particle comprising alternating tetrahedral and octahedral sheets terminating with tetrahedral sheets at one exterior surface plane and terminating with octahedral sheets at the other exterior surface plane, an antimicrobial agent attached to a coordinating cation on one of the exterior surface planes, wherein the antimicrobial agent is cetylpyridinium chloride; and ii) 0.001 to 10% by weight of a zinc compound, wherein the median diameter D50 of the bipolar antimicrobial particles is 0.1 to 10 μm; The zinc compound is zinc sulfate, zinc chloride, zinc nitrate, zinc citrate, zinc oxide, zinc lactate, zinc gluconate, zinc glycinate, zinc oleate, zinc hydroxide or zinc peroxide.

Images