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    • 专利摘要:
    zinc amino acid / trimethylglycine halide The invention provides a skin care personal care composition comprising a skin care or hair care composition comprising a zinc halide x and a cosmetically acceptable base, wherein x is a amino acid or trimethylglycine. Methods for producing and using the compositions are also provided. Zinc halide x can be used to provide zinc salts to block perspiration and provide antibacterial effects.
    公开号:BR112015014501B1
    申请号:R112015014501-9
    申请日:2012-12-19
    公开日:2019-04-02
    发明作者:Long Pan；Jairajh Mattai；Shamim Ansari；Jianhong Qiu；James G. Masters；Ying Yang
    申请人:Colgate-Palmolive Company；
    IPC主号:
    专利说明:

    COMPOSITION OF PERSONAL CARE FOR APPLICATION ON SKIN OR HAIR AND USE OF A ZINC HALOGENIDE COMPLEX BACKGROUND OF THE INVENTION [001] Antiperspirants based on aluminum or aluminum / zirconium salts are known. These materials work as antiperspirants by clogging the pores thus blocking the release of sweat. Antiperspirant compositions containing aluminum or aluminum zirconium salts tend to exhibit polymerization of these salts over time, forming species with molecular weights ranging from about 500 to about 500,000 g / mol. In general, smaller molecular weight species have a greater antiperspirant effect than higher molecular weight species. Without being limited by theory, it is believed that smaller molecules more quickly and more effectively occlude pore sweat, thereby producing the desired antiperspirant effect. Maintaining a relatively low molecular weight and avoiding excessive polymerization increases the antiperspirant effect and, in addition, reduces the amount of antiperspirant salt that is needed to control sweating.
    [002] Deodorants control odor by eliminating odor causing bacteria. Conventional antiperspirant salts tend to be acidic in aqueous solution, a property that makes them effective bactericides, thus providing a deodorant benefit.
    [003] There is a need for additional active antiperspirant agents that provide molecular weight complexes of a size capable of plugging pores to block sweat and provide efficacy to
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    2/22 deodorant / antibacterial.
    BRIEF SUMMARY OF THE INVENTION [004] The invention provides a personal care composition, for example, an antiperspirant or deodorant composition, which provides the skin with a zinc halide X, that is, a complex of zinc ion, residue X, and ion halide, such as zinc lysine chloride (ZnLys2CÍ2 or ZnLisina3CÍ2), for example, from a cosmetically acceptable base. X refers to the amino acid or trimethylglycine. Trimethylglycine as used throughout refers to N, N, N-trimethylglycine.
    [005] The complex solubilizes the zinc salt to allow its application to the skin or hair from a personal care composition.
    [006] In one embodiment, the personal care composition is an antiperspirant or deodorant in which zinc salts can be applied to the pores to block the pores to reduce perspiration.
    [007] As the zinc halide X provides antibacterial properties, the invention also encompasses other personal care compositions for application to the skin, for example, soaps or body washes, comprising a zinc halide X and / or the precursors of the same.
    [008] The invention further provides sweat reduction methods that comprise applying the composition to the skin, and methods for killing bacteria comprising contacting the bacteria with the composition.
    [009] Other areas of applicability of the present invention will become evident from the description
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    Detailed 3/22 provided hereafter. It should be understood that the detailed description and specific examples, while indicating the preferred embodiment of the invention, are intended for purposes of illustration only and are not intended to limit the scope of the invention.
    DETAILED DESCRIPTION OF THE INVENTION [010] The following description of the preferred embodiments is merely exemplary in nature and is in no way intended to limit the invention, its application or uses.
    [011] In one embodiment, the invention provides a composition comprising zinc halide X and / or zinc halide precursor materials which form a zinc halide X in situ (e.g., zinc ion source, plus a hydro -halide X, or zinc halide plus X, or a source of zinc ion plus halogen acid plus X). The source of zinc ion to produce zinc halide X is a material that can release Zn 2+ in aqueous solution in the presence of an X, for example, zinc oxide, tetrabasic zinc chloride, zinc chloride, zinc carbonate , zinc citrate, zinc nitrate, or zinc phosphate.
    [012] The invention therefore provides, in a first embodiment, a personal care composition for application to the skin or hair, which comprises a zinc halide X in a cosmetically acceptable base (Composition 1), for example,
    1.1. Any of the foregoing compositions, in which the zinc halide X is formed from precursors, in which the precursors are a source of zinc ion, an X source, and a halide source, in which the halide source
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    4/22 can be part of the zinc ion source, the X source, or a halogen acid.
    1.2. The above composition, wherein the source of zinc ion is at least one of zinc oxide, zinc chloride, tetrabasic zinc chloride, zinc carbonate, zinc nitrate, zinc citrate, and zinc phosphate.
    1.3. Compositions 1.1 or 1.2, where source X is at least one of a basic amino acid, lysine, arginine, and glycine.
    1.4. Any of the above compositions, wherein the zinc halide X is made by combining zinc oxide with an amino acid hydrohalide.
    1.5. Any of the above compositions, in which the zinc halide X is made by combining TBZC with an amino acid hydrohalide, an amino acid, or trimethylglycine, optionally zinc halide X is made by combining TBZC with lysine, hydrochloride lysine, or trimethylglycine.
    1.6. Any of the foregoing compositions, where the zinc halide X has the formula ZnXaHaA, where Zn is the divalent zinc ion, X is the amino acid or trimethylglycine residue, and Hal is a halide ion.
    1.7. Any of the above compositions, wherein a total amount of zinc present in the composition is 0.05 to 10% by weight.
    1.8. Any of the above compositions, where the amino acid is lysine.
    1.9. Any of the foregoing compositions, wherein the zinc halide X is present in an amount of 0.05 to 40% by weight of the composition, optionally at least
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    5/22
    0.1 at least 0.2, at minus 0.3, at least 0.4, fur minus 0.5, at least minus 1, at least 2, at least 3 , or at least 4 up to 40% by weight gives composition, or, optionally 0 , 1 to 30% , up to 20%, up to 10%, up to 5%, up until 4%, up to 3%, up to 2%, or even 1% by weight gives composition.1.10. Any of the compositions previous, in what
    a molar ratio of zinc to X is 2: 1 to 1: 4, optionally 1: 1 to 1: 4, 1: 2 to 1: 4, 1: 3 to 1: 4, 2: 1 to 1: 3 , 2: 1 to 1: 2, 2: 1 to 1: 1, or 1: 3.
    1.11. Any of the above compositions, wherein the halide is selected from the group consisting of chloride, bromide, and iodide, preferably chloride.
    1.12. Any of the above compositions, wherein the zinc amino acid halide is zinc lysine chloride.
    1.13. Any of the above compositions in an anhydrous vehicle.
    1.14. Any of the foregoing compositions comprising a zinc amino acid halide formed from zinc oxide and an amino acid hydrohalide.
    1.15. Any of the foregoing compositions, wherein the zinc amino acid halide is zinc lysine chloride (ZnLisin2C12 or ZnLisin3C12).
    1.16. Any of the above compositions in a cosmetically acceptable base suitable for application to the skin, for example, a cosmetically acceptable base comprising one or more of the water-soluble alcohols (such as, C2-8 alcohols including ethanol); glycols (including propylene glycol, dipropylene glycol, tripropylene glycol and
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    6/22 mixtures thereof); glycerides (including mono-, di- and triglycerides); long to medium organic acids, alcohols and esters; surfactants (including emulsifying and dispersing agents); additional amino acids;
    structuring agents (including thickening agents and gelling agents, for example, emollient polymers, silicates and dioxide;
    Perfumes; and dyes (including dyes and pigments).
    1.17. The above composition, in which the cosmetically acceptable base is substantially anhydrous, for example, comprises less than 5% water.
    1.18. Any of the above compositions, where the composition is an antiperspirant and / or deodorant, for example, an antiperspirant stick, an aerosol antiperspirant spray, or a liquid roll on antiperspirant.
    1.19. Any of the above compositions 1-17, wherein the composition is a body wash, a shower gel, a bar of soap, a shampoo or hair conditioner.
    [013] The invention further provides methods of reducing perspiration which comprises applying an effective antiperspirant amount of any of Composition 1, et seq. on the skin, methods of reducing body odor comprising the application of an effective amount of deodorant from any of Composition 1, et seq. for the skin, and methods of killing bacteria comprising contacting the bacteria with an antibacterially effective amount of a composition of zinc halide X, for example, any of Composition 1, et seq.
    [014] The invention further provides a method of making a
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    7/22 composition comprising a zinc halide X, for example, any of Composition 1, et seq. in a cosmetically acceptable vehicle.
    [015] The invention further provides (i) the use of a zinc halide X to kill bacteria, reduce perspiration, and / or reduce body odor; (ii) the use of a zinc X halide in the manufacture of a composition to kill bacteria, reduce sweating, and / or zinc X for use in eliminating bacteria, reducing sweating, and / or reducing body odor.
    [016] Without claiming to be limited by theory, it is believed that the formation of zinc halide X proceeds through the formation of zinc halide, then the coordination of the X residues around a central zinc. Use the reaction of zinc oxide with lysine hydrochloride in water, as an example, ZnO reacts with lysine.HC1
    through gives dissociation hydrochloride to will allow reaction: ZnO + HC1 7 ZnCl 2 + 7 H 2 0. One mole of ZnCÍ2 will to react with 3 mo1e s in lysine for to form a solution limpid in complex in Zn- chloride -lysine (ZnLisina2CÍ2
    described in or ZnLisina3CÍ2), it is believed that the structure
    Formula 1, where R represents the side chain X.
    O
    °] ; ..... ° i
    N ......- Zn —- N ..... h
    V N
    O
    R
    2+
    R
    Cl 2
    Formula I [017] In this configuration, Zn is located in an octahedral center coordinated with two oxygen atoms and
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    8/22 two nitrogen atoms in the equatorial plane from two lysine carboxylic acids and the amine groups, respectively. Zinc is also coordinated with the third lysine through its nitrogen and carboxylic oxygen, at the apical position of the metal geometry. This appears to be the dominant complex. Other zinc and lysine complexes are possible, for example, if there is insufficient halide, for example, ZnOLys2, which has a pyramid geometry, with the equatorial plane being the same as the compound above (Zn is linked to two oxygen atoms and two nitrogen atoms from different lysines), where the upper part of the pyramid is occupied by an atom of 0. More complex structures involving several zinc ions are also possible, based on the TBZC structure. The zinc may also have the zinc structure present in zinc stearate.
    [018] The interaction of zinc and X converts insoluble ZnO or TBZC to a highly soluble complex at about neutral pH. In the sweat duct, which contains charged molecules, such as proteins and fatty acids, the complex will flocculate, forming a precipitate that blocks the sweat ducts. As the complex is disrupted in these conditions, releasing free zinc ion, the zinc ion can hydrolyze to form amorphous zinc hydroxide precipitate, further blocking the ducts and, in addition, the zinc ion can kill bacteria axillary, thus reducing underarm odor. An advantage over conventional aluminum / zirconium or aluminum antiperspirant salts is that the complex is close to neutral pH, whereas antiperspirant salts
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    Conventional 9/22 are acidic, which can cause skin irritation.
    [019] It should be understood that other Xs can be used in place of lysine in the previous scheme. It will also be understood that, although zinc, X and halide may be essentially in the form of precursor materials or in the form of a complex, there may be some degree of equilibrium, so that the material ratio is actually in complex compared to the precursor-shaped relationship may vary depending on the precise formulation conditions, concentration of materials, pH, presence or absence of water, presence or absence of other charged molecules, and so on.
    [020] The zinc halide precursors X, for example, lysine hydrochloride and ZnO in the previous example, can be incorporated in a suitable base, for example, an anhydrous or aerosol stick. After sweating, the soluble zinc halide X complex is formed, which can reduce sweat and odor, as described above. Alternatively, the soluble complex can be incorporated into a product with an aqueous base, such as a roll-on or spray to reduce sweat and odor.
    [021] As used herein, the term antiperspirant can refer to any material that can form a plug in one of the pores to reduce perspiration, or antiperspirant refers to materials classified as antiperspirants by the Food and Drug Administration under 21 CFR part 350. Antiperspirants can also be deodorants, particularly in the case of the present invention, as zinc halide X has properties
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    10/22 antibacterial and can reduce odor-causing bacteria on the skin.
    [022] The combination of zinc, ο X, and the halide forms a cationic complex halide salt. Zinc halide X is a water-soluble complex formed from the acid addition salt of zinc halide (eg, zinc chloride) and an X, or from the acid addition salt of an X halide (eg example, lysine hydrochloride) and source of zinc ion, for example, zinc oxide or TBZC, and / or from the combination of all three of a halogen acid, an X, and a source of zinc ion.
    [023] The zinc ion source for the combination with an amino acid hydrohalide or an X plus halogen acid can be any source that efficiently supplies Zn 2 + ions, for example, zinc oxide, zinc chloride, tetrabasic zinc chloride, zinc carbonate, zinc nitrate, zinc citrate, and zinc phosphate. Zinc oxide is a white powder, insoluble in water. Tetrabasic zinc chloride (TBZC) or zinc chloride hydroxide monohydrate is a zinc hydroxy compound with the formula Zns (OH) 8CI2 Ή2Ο, also referred to as basic zinc chloride, zinc hydroxychloride, or zinc oxychloride. It is a colorless crystalline solid insoluble in water. Both of these materials are found to be soluble
    in water in presence of a X and provide a source of ions of zinc, while restricting available anions, as a A lot of anions that can interfere with the formation complex.[024] A source of amino acid can to be any
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    11/22 amino acid. Examples of amino acids include, but are not limited to, common natural amino acids, for example: lysine, arginine, histidine, glycine, serine, threonine, asparagine, glutamine, cysteine, selenocysteine, proline, alanine, valine, isoleucine, leucine, methionine, phenylalanine, tyrosine, tryptophan, aspartic acid, and glutamic acid.
    [025] In some embodiments, the amino acid is a basic amino acid. By basic amino acid means the naturally occurring basic amino acids, such as arginine, lysine, and histidine, as well as any basic amino acid having a carboxyl group and an amino group in the molecule, which is soluble in water and provides an aqueous solution with a pH of about 7 or higher. Consequently, basic amino acids include, but are not limited to, arginine, lysine, citrulline, ornithine, creatine, histidine, diaminobutanoic acid, diaminoproprionic acid, salts thereof or combinations thereof. In certain embodiments, the amino acid is lysine. In other embodiments, the amino acid is arginine. Neutral amino acids, such as glycine, and even acidic amino acids, such as aspartic acid, however, are also capable of forming salts with strong acids, such as halogen acids. In some embodiments, the amino acid is a neutral or acidic amino acid, for example, glycine.
    [026] The halide source may be part of the zinc source, such as zinc chloride or tetrabasic zinc chloride. The halide source may be part of the amino acid, such as an amino acid hydrohalide. In addition, the halide source may be an acid of
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    12/22 halogen. The halide can be chlorine, bromine, or iodine, more typically, chlorine. The acid addition salt of an amino acid and a halogen acid (e.g., HCl, HBr, or HI) is sometimes referred to herein as an amino acid hydrohalide. Thus, an example of an amino acid hydrohalide is lysine hydrochloride.
    [027] In certain embodiments, the amount of zinc halide X in the composition is 0.05 to 40% by weight of the composition. In certain embodiments, precursors, for example, zinc oxide and amino acid hydrohalide, are present in amounts such that, when combined
    in the halide in zinc X, the halide of zinc X would be present in an amount from 0.05 to 10% by weight gives composition. In any one of these modalities, The
    amount of the zinc halide X can be varied for the desired purpose, such as an antibacterial agent or an antiperspirant. In other embodiments, the amount of zinc halide X is at least 0.1, at least 0.2, at least 0.3, at least 0.4, at least 0.5, at least 1, at least 2, at least 3, or at least 4 to 10% by weight of the composition. In other embodiments, the amount of zinc halide X is less than 9, less than 8, less than 7, less than 6, less than 5, less than 4, less than 3, less than 2, less than 1, less than 0.5 to 0.05% by weight of the composition. In other embodiments, the amounts are 0.05 to 5%, 0.05 to 4%, 0.05 to 3%, 0.05 to 2%, 0.1 to 5%, 0.1 to 4%, 0.1 to 3%, 0.1 to 2%, 0.5 to 5%, 0.5 to 4%, 0.5 to 3%, or 0.5 to 2% by weight of the composition.
    [028] When zinc halide X is formed from
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    13/22 of precursor materials, preferably used as necessary for desired, although desirable, in balancing the pH against to provide zinc to provide buffer X. Halide de is limited, halide little encourages For example, lysine of molar ratios of will include about molar equivalents [029] In some zinc in the composition is In other embodiments, at least 0.1, at 0.4, at least 0.5, the materials in molar ratios produce the halide an excess of a certain material formulations, for other antibacterial components preferably, not in a modality for zinc precursors, are of approximately zinc X or another example, for the formulation, additional, or however, the amount as restricting the level of interaction between zinc and ο X. the production of chloride or ZnLisin3C2), the molar precursor materials of Zn 2 +: 3 molars of Cl ~.
    total composition. zinc is at least by weight of the (ZnLisina2CÍ2 elements in the equivalent of Lys: 2 equivalent modalities, the amount
    0.05 to 10% by weight of the total amount less
    0.2 at least
    0.3, or at least 1 to 10% composition. In other embodiments, the total amount of zinc in the composition is less than 5, less than 4, less than 3, less than 2, or less than 1 to 0.05% by weight of the composition.
    [030] In certain embodiments, a molar ratio of zinc to X is at least 2: 1. In other embodiments, the molar ratio is at least 1: 1, at least 1: 2, at least 1: 3, at least 1: 4, 2: 1 to 1: 4, 1: 1 to 1: 4, 1 : 2 to 1: 4, 1: 3 to 1: 4, 2: 1 to 1: 3, 2: 1 to 1: 2, 2: 1 to 1: 1, or 1: 3. Above 1: 4, it is expected that the zinc will be fully dissolved.
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    14/22 [031] In certain embodiments, the composition is anhydrous. Per anhydrous, there is less than 5% by weight of water, optionally less than
    4, less than
    3, less than 2, less than 1, less than 0.5, less than 0.1 to 0% by weight of water.
    [032]
    In certain embodiments, zinc halide may have a conductivity greater than 8000, optionally greater than
    9000, greater than 10,000, or greater than
    12,000 pS / cm, preferably when the pH is at least [033] The composition can be any type of composition.
    In certain embodiments, the composition is any composition in which it is desired to include an antibacterial agent for application to the skin. Examples of such compositions include, but are not limited to, personal care compositions, antiperspirants, deodorants, body washes, shower gels, bar soaps, shampoo, hair conditioners, cosmetics.
    [034] The vehicle represents all other materials in a different composition than zinc halide X. The amount of vehicle is then the amount to reach 100%, adding to the weight of zinc halide X.
    [035] For antiperspirant / deodorant compositions, the vehicle can be any vehicle that is used for deodorants / antiperspirants. The vehicle can be in the form of a stick, a gel, a roll-on, or an aerosol. For stick formulations, the vehicle may include oils and / or silicones and gelling agents. An example of a formulation can be found in US2011 / 0076309A1,
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    15/22 incorporated herein by reference.
    [036] Optional ingredients that can be included in an antiperspirant and / or deodorant formulation of the compositions of the present invention include solvents; water-soluble alcohols, such as C2-8 alcohols including ethanol; glycols including propylene glycol, dipropylene glycol, tripropylene glycol and mixtures thereof;
    including mono-, di- and triglycerides; long to medium organic glyceride acids, alcohols and esters;
    surfactants including emulsifying agents and dispersing agents;
    amino acids including glycine;
    structuring agents including thickeners and gelling agents, for example, polymers, silicates and silicon dioxide; emollients; Perfumes; and dyes including dyes and pigments.
    antiperspirant and / or zinc halide deodorant X may be included,
    If desired, an addition to, for example, an odor reducing agent, such as a sulfur precipitating agent, for example, copper gluconate, zinc gluconate, zinc citrate, etc.
    [037] Antiperspirant compositions can be formulated in antiperspirant and / or topical deodorant formulations suitable for application to the skin, illustratively, a stick, a gel, a cream, a roll-on, a soft solid, a powder, a liquid , an emulsion, a suspension, a dispersion or a spray. The composition can comprise a single phase or it can be a multiphase system, for example, a system comprising a polar phase and an oil phase, optionally in the form of a stable emulsion. The composition can be liquid, semi-solid or solid. The antiperspirant and / or deodorant formulation
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    16/22 can be supplied in any suitable container, such as an aerosol can, tube or container with a porous lid, roll-on container, bottle, container with an open end, etc.
    [038] The compositions can be used in a method to reduce perspiration by applying the composition to the skin. In certain embodiments, the application is for the armpit. In addition, the compositions can be used to kill bacteria by contact of the bacteria with the composition. For example, in one embodiment, the combination of an amino acid or amino acid hydrohalide with zinc oxide increases the availability of zinc ions, which can kill bacteria and then reduce sweat.
    [039] Thus, the invention provides (i) a method for controlling sweating which comprises applying to the skin an effective antiperspirant amount of a formulation of any embodiment incorporated or specifically described herein, for example, any of Compositions 1 et seq .; and (ii) a method for controlling odor from perspiration comprises applying an effective amount of deodorant to the skin of a formulation of any embodiment incorporated or specifically described herein, for example, any of Compositions 1 et seq.
    [040] Unless otherwise stated, all percentages of composition components provided in this specification are by weight, based on a total composition or 100% formulation weight.
    [041] Unless otherwise specifically identified, the ingredients to be used in the compositions and formulations of the present invention are,
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    17/22 preferably, cosmetically acceptable ingredients. By cosmetically acceptable it means suitable for use in a formulation for topical application on human skin. A cosmetically acceptable excipient, for example, is an excipient that is suitable for external application, in amounts and concentrations contemplated in the formulations of the present invention, and includes, for example, excipients that are Generally Recognized as Safe (GRAS) by the Drug Administration. and United States Food.
    Example 1 - Solubilization of zinc by amino acid [042] Zn concentration of TBZC is compared with ZnO and TBZC with amino acids. The ingredients are dispersed in water, balanced overnight, and the supernatant analyzed for free Zn 2 + by atomic absorption. Table 1 shows the comparison of TBZC-free Zn concentration with ZnO and TBZC mixed with different amino acids.
    Table 1
    Free zn (ppm) TBZC + Arginine (4 + 4%) 1819 TBZC + Lysine-HCl (4 + 4%) 6000 TBZC + Lysine (4 + 4%) 5000 TBZC (4%) 64.8 ZnO (4%) 11 ZnO + Lysine-HCl (4 + 4%) 21700
    [043] Free zinc ion concentration provided by TBZC is slightly higher than with ZnO. This shows that, although both have low solubility, the TBZC solubility is slightly better than ZnO. The concentration of free Zn is increased dramatically when the amino acid is added. For example, solubility increases 28 times when arginine is added and about 100 times when lysine hydrochloride is mixed with TBZC. Lysine hydrochloride also greatly increases the solubility of oxide
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    18/22 zinc.
    Example 2 - Antibacterial effects [044] An inhibition test zone is conducted on several materials: zinc oxide and amino acid hydrohalide alone and a mixture formed, from zinc oxide and amino acid hydrohalide. The method involves creating a thin tissue from a bacterial culture freshly prepared on TSA (trypticase soy agar) plates. Sterile filter paper discs, which are seeded with 20 μΐ of test sample (supernatant or mixture). Sample coated filter paper discs are air dried and applied to the bacterial layer on TSA plates. The plates are incubated for 20 hours at 37 ° C. The results are shown below in Table 2.
    Table 2
    Materi al Sample Inhibition Zone(mm)Wet sample Inhibition Zone(mm)Dry sample s.aureus S.epiderm ç.xerosis s.aureus S.epiderm ç.xerosis ZnO a4% Supernatural 0 0 0 0 0 0 Mixture 7 12 0 7 10 0 23.2% Lysine-HC1 Such as 0 0 0 0 0 0 ZnO a4% +LysineHC1 a23.2% Supernatural 12 23 18 13 22 17 Mixture 14 25 19 14 24 18
    [045] As can be seen from the table, when zinc amino acid halide is formed, the compositions increase antibacterial activity compared to zinc oxide alone or amino acid hydrohalide alone.
    [046] Similar antibacterial efficacy is seen when tetrabasic zinc chloride is used in place of
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    19/22 zinc oxide, such as the source of zinc ions. The results are shown in Table 3 below.
    Table 3
    SampleInhibition Zone (mm) S. aureus Ç.very minute 4% Arginine0 0 4% Lysine0 0 Lysine HC1 a4%0 0 4% TBZC Supernatant 6 7 Mixture 6 7 4% TBZC +4% Arginine Supernatant 8 12 Mixture 7.5 16 4% TBZC +4% Lysine Supernatant 7 21 Mixture 9 16 4% TBZC +Lysine HC1 a4% Supernatant 9 20 Mixture 7 17
    [047] As can be seen from the table, when the zinc amino acid halide is formed, the compositions increase in antibacterial activity compared to tetrabasic zinc chloride alone or amino acid alone.
    Example 3: Sweat reduction mechanisms [048] A zinc lysine hydrochloride (ZLC) is prepared by mixing ZnO + 2 (Lysine.HC1) in the presence of water to obtain [Zn (Lysine) 2CI] +01 “.2H2O.
    [049] Hydrolysis reaction: A 185 mg / ml ZLC solution is prepared and diluted several times and aged in an oven at 37 ° C for 5 hours for turbidity studies. A white precipitate forms as the solution is diluted. The turbidity of the solutions is measured using a nephelometer, the results being presented in nephelometric turbidity units (NTU). Table 4 shows a comparison of pH and turbidity before and after aging, which shows an increase in dilution and aging turbidity.
    Table 4
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    20/22
    185 mg / ml 92.5 mg / ml 46.25 mg / ml 23.125 mg / ml 11.56 mg / ml 5.78 mg / ml initial pH 6, 8 7 7.4 7.7 7.8 8 Initial turbidity (NTU) 4.7 2.8 1.5 0.7 14.8 40.1 pH afteraging 6.8 7 7.4 7.7 7.8 8 Turbidity after aging (NTU) 4.1 2, 6 2.8 247.4 > 1000 > 1000
    [050] The precipitates formed in the diluted solutions 8x, 16x and 32x are collected by centrifugation and identified as crystalline ZnO by PXRD. From the supernatant, a single crystal is cultured and demonstrated by X-ray diffraction to be Lysine Monohydrochloride Dihydrate (lysine.HC1.2H2O). These data indicate that the ZLC complex dissociates by dilution, with the consequent precipitation of zinc oxide.
    [051] The mechanism of the ZLC hydrolysis reaction can be expressed as [Zn (Lysine) 2CI] + C1 “. 2H 2 O + H 2 O -> ZnO + Lysine. HC1.2H 2 O [052] In an underarm product, a mixture of ZnO + lysine HC1, in the presence of sweat, will form ZLC, which will enter the sweat duct and form a ZnO layer.
    [053] Flocculation: Another mechanism by which the ZLC blocks the release of sweat involves the flocculation of ZLC in the presence of protein. Bovine Serum Albumin (BSA) is used as the protein in this study. The control solution (DI water) and three aqueous solutions of 1% BSA with different pH are prepared as set out in Table 5:
    Table 5
    Sample 1 Sample 2 Sample 3 H 2 O 15 ml 15 ml 15 ml BSA 0 g 155.1 mg 155.2 mg % BSA w / w 0% 1% 1% pH 6, 4 7.2 adjusted for
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    21/22
    5.1 Turbidity (NTU) 0.35 3.6 10, 6 Note Transparent Transparent Transparent
    [054] ZLC powder is added to the above samples to study the interaction between ZLC and BSA and to determine whether ZLC has astringent properties, that is, whether it can form a precipitate and thus behave as an antiperspirant. The turbidity and pH of the solutions are measured 5 hours after the mixtures are placed in a 37 ° C oven, and the results are shown in the Table
    6.
    Table 6
    Sample 1 Sample 2 Sample 3 ZLC added 151.1 mg 151.1 mg 150.9 mg ZLC concentration insolution about 0.98% w / w or 15 mg / ml about 0.96% w / w or 15 mg / ml about 0.96% w / w or 15 mg / ml Note Transparent solution becomes slightly cloudy A white precipitate formed in batch, solution becomes slightly cloudy A white precipitate formed in batch, solution becomes slightly cloudy pH 8 8.2 8 Turbidity (NTU) 357 > 1000 > 1000
    [055] Thus, in the sweat duct (pH = 5-7), ZLC will hydrolyze to insoluble ZnO to physically block the sweat ducts. In addition, ZLC also has the ability to flocculate proteins, such as BSA, in sweat, thereby increasing the formation of plugs in sweat ducts.
    [056] As used throughout, the ranges are used as an abbreviation to describe each and every value is within the range. Any value within the range can be selected as the end of the range. In addition, all references cited herein are hereby incorporated by
    Petition 870180131133, of 9/17/2018, p. 31/39
    22/22 reference in its entirety. In the event of a conflict in a definition in the present invention and that a reference is cited, the present invention controls.
    [057] Unless otherwise stated, all percentages and quantities expressed here and elsewhere in the specification should be understood to refer to percentages by weight. The quantities supplied are based on the active weight of the material.
    Petition 870180131133, of 9/17/2018, p. 32/39
    权利要求:
    Claims (15)
    [1]
    1. Personal care composition for application to skin or hair, characterized by the fact that it comprises a zinc halide complex X and a cosmetically acceptable base, where X is lysine, in which the zinc halide complex X has the formula ZnX2Hal2 or ZnX3Hal2, where Zn is a divalent zinc ion and Hal is a halide ion, and where zinc halide X is present in an amount of 0.05 to 40% by weight of the composition.
    [2]
    2. Personal care composition according to claim 1, characterized by the fact that the zinc halide complex X is formed from precursors, where the precursors are a source of zinc ion, a source X, and a halide source, wherein the halide source may be part of the zinc ion source, the X source, or a halogen acid.
    [3]
    3. Personal care composition according to claim 1 or 2, characterized by the fact that the source of zinc ion comprises one of zinc oxide, zinc chloride, tetrabasic zinc chloride, zinc carbonate, zinc nitrate , zinc citrate, and zinc phosphate.
    [4]
    Personal care composition according to any one of claims 1 to 3, characterized by the fact that the zinc halide complex X is made by combining zinc oxide with an amino acid hydrohalide.
    [5]
    Personal care composition according to any one of claims 1 to 4, characterized by the
    Petition 870180131133, of 9/17/2018, p. 33/39
    2/3 the fact that the zinc halide X complex is made by combining TBZC with lysine or lysine hydrochloride.
    [6]
    Personal care composition according to any one of claims 1 to 5, characterized in that the total amount of zinc present in the composition is 0.05 to 10% by weight.
    [7]
    Personal care composition according to any one of claims 1 to 6, characterized in that the zinc halide complex X is present in an amount of 0.1 to 40% by weight of the composition.
    [8]
    Personal care composition according to any one of claims 1 to 7, characterized by the fact that a molar ratio of zinc to X in the zinc halide complex X is 2: 1 to 1: 4.
    [9]
    9. Personal care composition according to any one of claims 1 to 8, characterized by the fact that the halide is chloride.
    [10]
    Personal care composition according to any one of claims 1 to 9, characterized in that the zinc halide complex X is zinc lysine chloride.
    [11]
    11. Personal care composition according to any one of claims 1 to 10, characterized by the fact that the zinc halide complex X is ZnLisina2C12 or ZnLisina3C12.
    [12]
    12. Personal care composition according to any one of claims 1 to 11, characterized in that the cosmetically acceptable base comprises an ingredient selected from soluble alcohols.
    Petition 870180131133, of 9/17/2018, p. 34/39
    3/3 water; glycols; glycerides; long to medium organic acids, alcohols and esters; surfactants; additional amino acids; structuring; emollients; Perfumes; and dyes.
    [13]
    13. Personal care composition according to any one of claims 1 to 12, characterized in that the composition is an antiperspirant or a deodorant.
    [14]
    14. Personal care composition according to any one of claims 1 to 13, characterized in that the composition is a body wash, a shower gel, a bar of soap, a shampoo, or a hair conditioner.
    [15]
    15. Use of a zinc halide complex X characterized by the fact that it is in the preparation of a personal care composition to kill bacteria, reduce sweating or reduce body odor, where X is lysine, and in which zinc halide X has the formula ZnX2Hal2 or ZnXaHaA, where Zn is a divalent zinc ion and Hal is a halide ion, in which the zinc halide complex X is provided in a personal care composition, and in which the halide complex zinc X is present in an amount of 0.05 to 40% by weight of the composition.
    类似技术:
    公开号 | 公开日 | 专利标题
    BR112015014501B1|2019-04-02|Personal care composition for skin or hair application and use of a zinc halide complex X
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    同族专利:
    公开号 | 公开日
    MX368741B|2019-10-14|
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    CN104853721A|2015-08-19|
    US20150328117A1|2015-11-19|
    RU2621130C2|2017-05-31|
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    BR112015014501A2|2017-07-11|
    AR095456A1|2015-10-21|
    WO2014098813A1|2014-06-26|
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    法律状态:
    2017-12-12| B07D| Technical examination (opinion) related to article 229 of industrial property law|Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
    2018-01-16| B07B| Technical examination (opinion): publication cancelled|
    2018-06-19| B07A| Technical examination (opinion): publication of technical examination (opinion)|
    2019-01-29| B09A| Decision: intention to grant|
    2019-01-29| B15K| Others concerning applications: alteration of classification|Free format text: AS CLASSIFICACOES ANTERIORES ERAM: A61K 8/27 , A61K 8/44 , A61Q 15/00 , A61P 31/04 Ipc: A61K 8/27 (2006.01), A61K 8/44 (2006.01), A61Q 15/ |
    2019-04-02| B16A| Patent or certificate of addition of invention granted|Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/12/2012, OBSERVADAS AS CONDICOES LEGAIS. (CO) 20 (VINTE) ANOS CONTADOS A PARTIR DE 19/12/2012, OBSERVADAS AS CONDICOES LEGAIS |
    优先权:
    申请号 | 申请日 | 专利标题
    PCT/US2012/070489|WO2014098813A1|2012-12-19|2012-12-19|Zinc amino acid/trimethylglycine halide|
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