Antiperspirant composition
By using phytochemicals such as phenylacrylic acid and natural extract cinnamon extract as antiperspirants, the health risks and environmental concerns of aluminum salts are addressed, achieving an effective effect of reducing or preventing sweating.
Patent Information
- Application Number
- CN202480009715.5
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2023-08-08
- Filing Date
- 2024-05-29
- Publication Date
- 2025-10-10
AI Technical Summary
Existing antiperspirants primarily rely on aluminum or aluminum zirconium salts, which pose health risks and environmental concerns, and there is a need to find alternative compounds to match or improve sweat reduction performance.
Antiperspirants use phytochemicals such as phenylacrylic acid and natural extracts such as cinnamon extract or amla extract to reduce or prevent sweating by blocking the pores of sweat glands.
Provides antiperspirant effectiveness comparable to aluminum or aluminum zirconium salts while avoiding health risks, imparting a pleasant odor, and demonstrating at least a 20% reduction in sweat in 50% of test subjects.
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Abstract
Description
Technical Field
[0001] The present invention relates to an antiperspirant composition. The present invention also relates to a method of reducing or preventing perspiration and the use of certain naturally available ingredients, particularly phytochemicals, as antiperspirants. Background Art
[0002] Antiperspirant compositions are a well-known class of products in the personal care field used to eliminate or reduce body odor, which is important for daily hygiene. These compositions can be applied in a variety of forms, such as solid sticks, roll-ons, wipes, aerosol sprays, and pump sprays.
[0003] The composition typically contains an active ingredient, often called an antiperspirant, which narrows or blocks the sweat gland ducts to reduce or prevent sweating. If the antiperspirant can mask odors or has antimicrobial activity, it can also provide a deodorizing effect.
[0004] Commonly used antiperspirants are usually aluminum or aluminum zirconium salts, such as aluminum chlorohydrate or aluminum zirconium tetrachloroglycinate (AZG). These salts dissolve in the skin and clog the pores, reducing or preventing sweating.
[0005] People have been searching for alternative compounds with similar functions to match or improve the sweat-reducing properties of aluminum or aluminum zirconium salts. Summary of the Invention
[0006] In a first aspect, the present invention provides an antiperspirant composition. The antiperspirant composition comprises an antiperspirant, wherein the antiperspirant comprises an optionally substituted benzenepropenoic acid. The optionally substituted benzenepropenoic acid may be a phytochemical.
[0007] The first aspect of the present invention also provides an antiperspirant composition comprising an antiperspirant, wherein the antiperspirant comprises a phytochemical which is an optionally substituted phenylacrylic acid.
[0008] In a second aspect, the present invention further provides an antiperspirant composition comprising: (a) a natural extract or (b) an antiperspirant obtained or obtainable from a natural extract.
[0009] The natural extract of the second aspect is cinnamon extract, or cinnamon extract and Emblica officinalis extract. Preferably, the natural extract is cinnamon extract.
[0010] The antiperspirant in (b) may be present in the antiperspirant composition in the form of a natural extract in (a).
[0011] Surprisingly, it has been discovered that certain classes of phytochemicals or plant extracts possess antiperspirant properties. These naturally derived materials can be used as antiperspirants, particularly in personal care products. They can provide an antiperspirant effect comparable to the aluminum or aluminum zirconium salts typically included in most commercially available antiperspirant products. Therefore, phytochemicals or plant extracts can replace aluminum or aluminum zirconium salts as antiperspirants. These substances, particularly natural extracts, can also impart a pleasant scent to antiperspirant compositions. There are also no health risks associated with these ingredients.
[0012] The third aspect of the present invention relates to a method for reducing or preventing perspiration, said method comprising applying to the skin an antiperspirant composition according to the first or second aspect of the present invention.
[0013] The third aspect of the present invention also includes the use of the antiperspirant composition for reducing or preventing perspiration.
[0014] A fourth aspect of the present invention relates to the use of optionally substituted phenylacrylic acid for reducing or preventing sweating.
[0015] The fourth aspect also includes the use of a phytochemical as an antiperspirant for reducing or preventing sweating, wherein the phytochemical is an optionally substituted phenylacrylic acid.
[0016] A fifth aspect of the present invention relates to the use of a natural extract as an antiperspirant for reducing or preventing sweating. The natural extract of the fifth aspect is cinnamon extract, or cinnamon extract and emblica extract. Preferably, the natural extract is cinnamon extract. DETAILED DESCRIPTION
[0017] The following definitions apply to the disclosure herein, including all aspects of the invention and embodiments thereof.
[0018] As used herein, the term "personal care," whether used alone or in combination with other terms, refers to non-therapeutic uses, such as non-therapeutic cosmetic uses. The term generally refers to uses for personal hygiene.
[0019] The compounds and intermediates described herein may be named according to the IUPAC (International Union of Pure and Applied Chemistry) or CAS (Chemical Abstracts Service) nomenclature system or by their commercial trade names. It should also be understood that any reference to a compound described herein, such as a polyurea, primary monoamine, diamine, or triamine, encompasses all stereoisomers (e.g., cis and trans isomers) and / or optical isomers (e.g., R and S enantiomers) of these compounds, in substantially pure form and / or in any proportion of mixtures thereof.
[0020] As used herein, the term “phytochemical” refers to a compound produced by a plant (e.g., through primary or secondary metabolism). In other words, a phytochemical is a naturally occurring biologically active compound found in a plant. Phytochemicals often have a biological activity that protects the plant from environmental, disease, or predator attack.
[0021] As used herein, the term “flavonoid” refers to a compound having a 15-carbon core structure (e.g., backbone) consisting of two phenyl rings (referred to as “A” and “B” rings) and a heterocyclic ring containing oxygen atoms (referred to as “C” ring). The term “flavonoid” is used in the conventional, limiting sense to refer only to compounds having a C6-C3-C6 carbon framework (e.g., core structure or backbone) having a chromatan or 1-benzopyran (chromene) structure, wherein the fused phenyl ring is designated as ring A, the 3,4-dihydro-2H-pyran or pyran is designated as ring C, and the phenyl group on ring C (ring B) (see, e.g., A. P. Rauter et al., “Nomenclature of flavonoids” - Reference 1). The general structure of a flavonoid with ring labels is shown below.
[0022]
[0023] Depending on the position of attachment of ring B to the chromatan / 1-benzopyran (chromene) moiety, the term “flavonoid” includes or consists of the subgroups of compounds referred to as 2-flavonoids, 3-flavonoids (e.g., also referred to as iso-flavonoids), and 4-flavonoids (e.g., also referred to as neo-flavonoids).
[0024] As used herein, the term “2-flavonoid” refers to a compound having a core structure or backbone represented by formula (A-1).
[0025]
[0026] In formula (A-1), the atoms of the core structure are numbered according to the IUPAC numbering scheme for this subgroup of compounds.
[0027] For the avoidance of doubt, formula (A-1) represents the core structure or backbone of a 2-flavonoid. Rings A to C of the core structure can comprise substituents. Ring C can comprise a carbon-carbon double bond (in addition to the unsaturated bond resulting from the fused phenyl group (ring A)) and / or a carbonyl group.
[0028] In general, the term “2-flavonoid” includes a flavan, flavone, or flavanol.
[0029] When ring C in formula (A-1) does not comprise a carbon-carbon double bond or a carbonyl group, then formula (A-1) represents a flavan. The term “flavan” refers to a compound having a 2-phenyl-3,4-dihydro-2H-1-benzopyran backbone.
[0030] When the ring C in formula (A-1) is substituted by a hydroxyl group, for example, substituted by a hydroxyl group at the 3-position and / or the 4-position of the ring C, the 2-flavonoid is a flavanol.
[0031] The core structure or skeleton of the flavanol can be flavan-3-ol (as shown in formula (A-2)), flavan-4-ol (as shown in formula (A-3)), or flavan-3,4-diol (as shown in formula (A-4)).
[0032]
[0033]
[0034] When Ring C in Formula (A-1) contains a carbonyl group, such that the compound is derived from a 2-phenyl-2,3-dihydro-4H-1-chromen-4-one skeleton, then the 2-flavonoid is a flavanone, specifically a flavan-4-one (e.g., as shown in Formula (A-5)).
[0035]
[0036] Preferably, the core structure or backbone of the 2-flavonoid is not anthocyanidin (also known as anthocyanin). Anthocyanidin is a molecule derived from the flavylium ion (2-phenyl-1λ 4 -chromen-1-ylium ion or 2-phenylchromenylium ion).
[0037] As used herein, the term "glucogallin" refers to the following compound.
[0038]
[0039] Glucogallanin is usually present in natural extracts of Phyllanthus emblica. Therefore, Glucogallanin may be obtained or obtainable from the extract of Phyllanthus emblica.
[0040] As used herein, the terms "saberry" or "saberry extract" are synonymous with emblica or emblica extract, respectively, and refer to the fruit or fruit extract of emblica (synonymous with phyllanthus emblica), which is commonly known as amla berry or Indian gooseberry.
[0041] As used herein, "substituted" alone or in combination with one or more other terms means that a hydrogen atom on a molecule has been replaced by a different atom or group of atoms. The atom or group of atoms that replaces the hydrogen atom is a "substituent." It should be understood that the terms "substituent," "moiety," or "group" refer to a substituent.
[0042] The various hydrocarbon-containing moieties provided herein may be described using a prefix that designates the minimum and maximum number of carbon atoms in the moiety, i.e., "C a -C b For example, C a -C b Alkyl refers to an alkyl moiety having an integer "a" to an integer "b" number of carbon atoms, inclusive.
[0043] As used herein, the term "alkyl," whether used alone or in combination with another term, refers to a branched or unbranched saturated hydrocarbon chain, unless otherwise indicated. An alkyl group is typically unsubstituted, unless otherwise indicated. An alkyl group can have from 1 to 6 carbon atoms, such as from 1 to 4 carbon atoms. Representative examples include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, and n-hexyl.
[0044] As used herein, the term "alkoxy" refers to an alkyloxy group in which alkyl is as defined above. Alkoxy groups are typically unsubstituted unless otherwise indicated. Representative examples include -OMe, -OEt, -O n Pr, -O i Pr.
[0045] As used herein, the term "deodorant" refers to an agent, material or composition that masks or inhibits the development of unpleasant body odor.
[0046] The amount of a material such as a compound, composition or ingredient is often defined in terms of wt % of the composition.
[0047] The term "about," when used herein in connection with a measurable value, encompasses reasonable variation from that value, eg, allowing for experimental error in the measurement of the value.
[0048] As used in this disclosure, the term "comprising" has an open meaning that allows for the presence of other unspecified features. This term includes, but is not limited to, the semi-closed term "consisting essentially of" and the closed term "consisting of." Unless the context indicates otherwise, the term "comprising" can be replaced with "consisting essentially of" or "consisting of." The term "consisting essentially of" can also be replaced with "consisting of.
[0049] For the avoidance of doubt, the expression "consisting essentially of" as used herein limits the scope of a feature to include the specified materials and any other materials or steps that do not materially affect the basic and novel properties of the feature, such as, for example, trace impurities. The expression "consisting essentially of" encompasses the expression "consisting of."
[0050] antiperspirant
[0051] The present invention relates to the use of naturally derived or obtainable products as antiperspirants.
[0052] Antiperspirants are used to reduce or prevent sweating. Thus, antiperspirants are the active ingredients in the antiperspirant compositions of the present invention that reduce or prevent sweating.
[0053] Sweating is a physiological bodily function that helps control and maintain body temperature at approximately 37°C. Sweat is produced by sweat glands, which are skin appendages composed of an outer layer of myoepithelial contractile cells and an inner layer of secretory cells. When body temperature rises, sweat glands are activated by signals from the brain to produce sweat. In addition to maintaining a stable body temperature, sweat moisturizes the skin and releases toxins. Excessive perspiration can cause discomfort, such as underarm odor and lesions.
[0054] Antiperspirants work by creating a buffer that limits the amount of sweat released by the skin through the sweat gland ducts.
[0055] The antiperspirants of the present invention are for external use (eg, on the human body).
[0056] The antiperspirant composition or antiperspirant is intended for application to body surfaces, particularly the skin.
[0057] The antiperspirant comprises optionally substituted phenylacrylic acid.The antiperspirant may consist essentially of optionally substituted phenylacrylic acid.
[0058] For all aspects of the present invention, the antiperspirant will now be further described by the following numbered paragraphs:
[0059] 1. The antiperspirant comprises or consists essentially of optionally substituted phenylacrylic acid.
[0060] 2. The antiperspirant according to paragraph 1, wherein the optionally substituted phenylacrylic acid is trans-phenylacrylic acid.
[0061] 3. The antiperspirant according to paragraph 2, wherein the optionally substituted phenylacrylic acid is represented by formula (I):
[0062]
[0063] where R 1 to R 5 Each is independently selected from H, hydroxyl and C1-C6 alkoxy.
[0064] Hydroxyl (—OH) and C 1 -C 6 alkoxy are optional substituents mentioned in paragraphs 1 and 2.
[0065] Phenylic acid can exhibit excellent antiperspirant activity, as demonstrated by the results with trans-cinnamic acid.
[0066] 4. The antiperspirant according to paragraph 3, wherein the C1-C6 alkoxy group is an ethoxy group or a methoxy group.
[0067] 5. The antiperspirant according to paragraph 4, wherein the C1-C6 alkoxy group is a methoxy group.
[0068] 6. An antiperspirant according to any one of paragraphs 3 to 5, wherein R 1 to R 5 At least three of them are hydrogen.
[0069] 7. An antiperspirant according to any one of paragraphs 3 to 6, wherein R 1 to R 5 The two adjacent groups in are each independently selected from hydroxyl and C1-C6 alkoxy (or C1-C6 alkoxy as defined in paragraph 4 or 5).
[0070] For example, (i) R 1 and R 2 or (ii) R 2 and R 3 Each is independently selected from hydroxy and C1-C6 alkoxy (or C1-C6 alkoxy as defined in paragraph 4 or 5).
[0071] 8. An antiperspirant according to any one of paragraphs 3 to 7, wherein R 1 、R 4 and R 5 is hydrogen, and R 2 and R 3 Each is independently selected from hydroxy and C1-C6 alkoxy (or C1-C6 alkoxy as defined in paragraph 4 or 5).
[0072] 9. An antiperspirant according to any one of paragraphs 1 to 3, wherein the optionally substituted phenylacrylic acid is selected from cinnamic acid, o-coumaric acid, m-coumaric acid, p-coumaric acid, caffeic acid, ferulic acid, 5-hydroxyferulic acid and sinapic acid.
[0073] 10. The antiperspirant of paragraph 9, wherein the optionally substituted phenylacrylic acid is caffeic acid.
[0074] 11. The antiperspirant of paragraph 9, wherein the optionally substituted phenylacrylic acid is trans-cinnamic acid.
[0075] Trans-cinnamic acid can be found in some cinnamon extracts.
[0076] 12. An antiperspirant according to paragraph 1 consisting essentially of an optionally substituted phenylacrylic acid as defined in any one of paragraphs 2 to 11.
[0077] 13. An antiperspirant according to any of paragraphs 1 to 11 further comprising an ester of gallic acid.
[0078] 14. The antiperspirant according to paragraph 13, wherein the ester of gallic acid is selected from flavonoid esters of gallic acid and sugar esters of gallic acid.
[0079] 15. The antiperspirant according to paragraph 14, wherein the ester of gallic acid is a sugar ester of gallic acid.
[0080] 16. The antiperspirant according to paragraph 14 or paragraph 15, wherein the sugar ester of gallic acid is glucogalloside (eg, β-glucogalloside).
[0081] 17. The antiperspirant according to paragraph 14, wherein the ester of gallic acid is a flavonoid ester of gallic acid.
[0082] 18. The antiperspirant according to paragraph 14 or paragraph 17, wherein the flavonoid ester of gallic acid is a flavan-3-ol ester of gallic acid.
[0083] Flavan-3-ol esters of gallic acid generally contain the following structural moieties:
[0084]
[0085] The term "part" is used because the above structures may contain one or more substituents on the 2-flavonoid backbone or core structure.
[0086] 19. The antiperspirant of paragraph 18, wherein the flavan-3-ol ester of gallic acid is selected from the group consisting of catechin gallate, epicatechin gallate, epigallocatechin gallate, and mixtures of two or more thereof.
[0087] 20. The antiperspirant of paragraph 18, wherein the flavan-3-ol ester of gallic acid is epigallocatechin gallate.
[0088] 21. The antiperspirant of paragraph 18, wherein the flavan-3-ol ester of gallic acid is selected from the group consisting of catechin gallate, epicatechin gallate, and mixtures thereof.
[0089] The cinnamon extract used in the examples contained a mixture of catechin gallate and epicatechin gallate.
[0090] 22. The antiperspirant of paragraph 1 comprising an optionally substituted phenylacrylic acid as defined in any of paragraphs 2 to 11, such as trans-cinnamic acid, and an ester of gallic acid as defined in any of paragraphs 13 to 21. The antiperspirant may be a combination or mixture of the optionally substituted phenylacrylic acid and the ester of gallic acid.
[0091] 23. The antiperspirant of any one of paragraphs 1 to 22 obtained or obtainable from a natural extract.
[0092] 24. An antiperspirant according to paragraph 23, wherein the natural extract is a cinnamon extract, or a cinnamon extract and a phyllanthus extract, such as a mixture of a cinnamon extract and a phyllanthus extract. Preferably the natural extract is a cinnamon extract.
[0093] 25. An antiperspirant according to any one of paragraphs 1 to 24, which does not include aluminium chlorohydrate or aluminium zirconium tetra-chlorohydrex gly.
[0094] 26. An antiperspirant according to any one of paragraphs 1 to 24, which does not include an aluminium-containing antiperspirant, preferably which does not include aluminium.
[0095] 27. An antiperspirant according to paragraph 26, which does not include zirconium.
[0096] 28. An antiperspirant according to any one of paragraphs 1 to 27, wherein the antiperspirant is an antioxidant.
[0097] 29. An antiperspirant according to any one of paragraphs 1 to 28, wherein the antiperspirant is a protein coagulant.
[0098] 30. An antiperspirant according to any one of paragraphs 1 to 29, wherein the antiperspirant is an antiseptic.
[0099] 31. An antiperspirant according to any one of paragraphs 1 to 30, wherein the antiperspirant is an antibacterial agent.
[0100] The antiperspirant of any one of paragraphs 1 to 31 above can be present in the antiperspirant composition in the form of a natural extract, such as in the second aspect of the application.
[0101] For all aspects of the application, the natural extract will now be further described by the following numbered paragraphs:
[0102] 32. The natural extract is a cinnamon extract and optionally a phyllanthus extract, such as a mixture of a cinnamon extract and a phyllanthus extract. Preferably the natural extract is a cinnamon extract (e.g. a cinnamon extract only).
[0103] 33. The natural extract according to paragraph 32, wherein the cinnamon extract comprises one or more 2- flavonoids.
[0104] 34. The natural extract according to paragraph 33, wherein at least one of the one or more 2- flavonoids is a flavanol, preferably a flavan-3-ol.
[0105] 35. The natural extract of paragraph 34, wherein the flavanol or flavan-3-ol is afzelechin, epiafzelechin, catechin, epicatechin, gallocatechin, epigallocatechin, or a combination of two or more thereof.
[0106] 36. The natural extract according to any of paragraphs 33 to 35, wherein at least one of the one or more 2-flavonoids is a flavanone, preferably a flavan-4-one.
[0107] 37. The natural extract according to paragraph 36, wherein the flavanone or flavan-4-one is rutin.
[0108] 38. The natural extract according to any of paragraphs 32 to 37, wherein the cinnamon extract comprises cinnamic acid, preferably trans-cinnamic acid.
[0109] 39. The natural extract of paragraph 32, comprising an extract of Emblica officinalis.
[0110] 40. The natural extract according to paragraph 32 or paragraph 39, wherein the Emblica officinalis extract comprises glucogallocatechin (eg, β-glucogallocatechin).
[0111] 41. The natural extract of any of paragraphs 32 to 40, wherein the natural extract is an antioxidant.
[0112] 42. The natural extract antiperspirant of any of paragraphs 32 to 41, wherein the natural extract is a protein coagulant.
[0113] 43. The natural extract of any of paragraphs 32 to 42, wherein the natural extract is a preservative.
[0114] 44. The natural extract of any of paragraphs 32 to 43, wherein the natural extract is an antimicrobial agent.
[0115] Without wishing to be bound by theory, the antiperspirants of the present invention, whether as individual compounds or in the form of natural extracts, may block the pores of the sweat glands by causing protein aggregation and / or by binding to specific receptors in the walls of the sweat ducts.
[0116] Surprisingly, cinnamic acid has been found to have an antiperspirant effect. This compound is believed to cause proteins to coagulate or aggregate.
[0117] Typically, antiperspirants and / or natural extracts have at least a 20% reduction in sweat in at least 50% of the subjects tested, as measured according to US FDA guidelines (Ref. 3). The term "tested subjects" is synonymous with the "target population" referred to in the US FDA guidelines.
[0118] Often, antiperspirants and / or natural extracts may also be deodorants (eg, deodorants).
[0119] Additionally or alternatively, the antiperspirant and / or the natural extract may have an astringent effect, a toning effect and / or an anti-aging effect on the skin, preferably an astringent effect.
[0120] Antiperspirant composition
[0121] The antiperspirant compositions of the present invention comprise an antiperspirant as defined above in the title section, including as defined in any of paragraphs 1 to 31. The antiperspirant may be present as a natural extract as defined above, including as defined in any of paragraphs 32 to 44. The antiperspirant may be obtained or obtainable from a natural extract.
[0122] Typically, the antiperspirant as defined above is the only antiperspirant in the antiperspirant composition.
[0123] When the antiperspirant composition comprises a natural extract as defined above, preferably said natural extract is the only antiperspirant.
[0124] Typically, the antiperspirant composition does not contain aluminum chlorohydrate or aluminum zirconium tetrachloroglycinate. Preferably, the antiperspirant composition does not contain an aluminum-containing antiperspirant, and more preferably, the antiperspirant composition does not contain aluminum and optionally zirconium.
[0125] Additionally or alternatively, the antiperspirant composition does not comprise 4-hydroxybenzaldehyde. Preferably, the antiperspirant composition does not comprise (i) benzaldehyde or a benzaldehyde-derived compound of formula I:
[0126]
[0127] where R 1 is a residue selected from the group consisting of H, CH2, CH3, OH and OCH3,
[0128] where R 2 is a residue selected from the group consisting of H, OH, OCH3 and OCH2O, and wherein if R 2 is OCH2O, then R 1 is CH2 and / or with R 2forming a bond; and / or (ii) benzaldehyde, 4-methylbenzaldehyde, heliotrope, vanillin, 4-hydroxybenzaldehyde, 3-hydroxybenzaldehyde, 4-methoxybenzaldehyde, 3-methoxybenzaldehyde or 3-hydroxy-4-methoxybenzaldehyde (isovanillin).
[0129] The antiperspirant composition comprises an effective amount of an antiperspirant or natural extract. An effective amount is an amount that reduces or prevents sweating.
[0130] Antiperspirant compositions typically comprise a total amount of about 0.1 to about 25.0 wt % antiperspirant, preferably about 0.5 to about 15.0 wt %, more preferably about 1.0 to about 10.0 wt %, such as about 1.0 to about 5.0 wt % antiperspirant.
[0131] The antiperspirant composition preferably comprises a total amount of from about 0.1 to about 4.0 wt % antiperspirant, such as from about 0.5 to about 4.0 wt %, more preferably from about 1.0 to 4.0 wt %, such as from about 1.0 to about 3.5 wt % antiperspirant.
[0132] When the antiperspirant comprises or consists essentially of an optionally substituted phenylacrylic acid, such as trans-cinnamic acid, the antiperspirant composition comprises a total amount of from about 0.5 to about 25.0 wt % (e.g., from 1.5 to about 25.0 wt %), preferably from about 1.0 to about 20.0 wt % (e.g., from about 3.0 to about 20.0 wt %), more preferably from about 1.5 to about 15.0 wt % (e.g., from about 5.0 to 15.0 wt %), such as from about 2.0 to about 10.0 wt % of the optionally substituted phenylacrylic acid (e.g., trans-cinnamic acid).
[0133] The antiperspirant compositions typically comprise a total amount of from about 5.0 to about 40.0 wt. % of natural extracts, preferably from about 10.0 to about 30.0 wt. %, more preferably from about 15.0 to about 25.0 wt. % of natural extracts.
[0134] The amount of natural extract included in the antiperspirant composition depends on the composition of the extract, particularly the type and amount of ingredients present in the natural extract.
[0135] Typically, the antiperspirant composition is a cosmetic antiperspirant composition, particularly a cosmetic antiperspirant composition for personal care.
[0136] Antiperspirant compositions are typically intended for topical use. Thus, the antiperspirant composition may be a topical antiperspirant composition.
[0137] Antiperspirant compositions are intended for topical application to the skin, preferably to the surface of the skin.Antiperspirant compositions can be formulated for a specific mode of topical application.
[0138] Typically, antiperspirant compositions comprise a topically acceptable carrier. The topically acceptable carrier will depend on the type of formulation and its mode of topical application.
[0139] Topically acceptable carriers may be water, alcohols, ethers, oils or waxes.
[0140] For example, when the antiperspirant composition is in the form of a gel, paste, liquid, lotion, or foam, the topically acceptable carrier can be water or a combination of water and oil.
[0141] The topically acceptable carrier can be an alcohol. The alcohol can be a monohydric alcohol or a polyhydric alcohol (eg, an alcohol compound having two or more hydroxyl groups).
[0142] When the alcohol is a monohydric alcohol, the monohydric alcohol may be ethanol or a fatty alcohol. The fatty alcohol may have a linear chain length of 6 to 18 carbon atoms. Preferably, the fatty alcohol is stearyl alcohol.
[0143] When the alcohol is a polyol, the polyol can be a polymeric alcohol or a monomeric alcohol. The polymeric alcohol can be a polyalkylene glycol, such as PEG or PPG. The monomeric alcohol can be ethylene glycol, propylene glycol, glycerol, or a sugar, such as glucose, sorbitol, or xylitol.
[0144] The topically acceptable carrier may be an ether. The ether may be PPG-14 butyl ether.
[0145] The topically acceptable carrier may be an oil. The oil may be hydrogenated castor oil.
[0146] The antiperspirant composition may be provided as a deodorant or included in a deodorant, such as a body deodorant for personal hygiene purposes.
[0147] Antiperspirant compositions may be in the form of a cream, gel, paste, liquid, lotion, foam, scrub or powder.
[0148] Typically, antiperspirant compositions are leave-on compositions that are applied to the skin or skin surface and left on for a period of time (e.g., 1 minute to 24 hours) before being wiped off or rinsed off with water, typically during normal washing.
[0149] When the antiperspirant composition is in liquid form, the liquid may be a water-in-oil emulsion or an oil-in-water emulsion.
[0150] Typically, when the antiperspirant composition is in liquid form, the liquid can be a sprayable liquid.
[0151] The antiperspirant composition can be delivered as an aerosol.The topically acceptable carrier can comprise a propellant.
[0152] The antiperspirant composition may contain a lubricant. The lubricant may be, for example, cyclomethicone, dimethicone, phenyl trimethicone or ethyl methicone. Preferably, the lubricant is cyclomethicone and / or phenyl trimethicone.
[0153] The antiperspirant compositions of the present invention may also contain natural oils.Natural oils may be included for skin care benefits.
[0154] Typically, natural oils contain unsaturated fats, such as polyunsaturated fats (eg, triglycerides derived from linoleic acid) and / or monounsaturated fats (eg, triglycerides derived from oleic acid).
[0155] The antiperspirant composition may also contain an antioxidant component.Antioxidant components may be included to chemically stabilize the antiperspirant or any other natural ingredients that may be present, such as natural oils, particularly natural oils containing polyunsaturated fats and / or monounsaturated fats.
[0156] The antioxidant component may be selected from ascorbic acid, butylhydroxytoluene, pentaerythritol tetrakis(di-tert-butylhydroxyhydrocinnamate) and tris(tetramethylhydroxypiperidinol) citrate.
[0157] Antiperspirant compositions may contain a fragrance.
[0158] The antiperspirant composition may include a thickener. The thickener may be fumed silica or a cellulose ether, such as hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, carboxymethyl cellulose, cetyl hydroxyethyl cellulose, hydroxybutyl methylcellulose, methyl hydroxyethyl cellulose, or xanthan gum. Preferably, the thickener is fumed silica.
[0159] The antiperspirant composition may comprise a surfactant. The surfactant may be an anionic surfactant, a cationic surfactant, a nonionic surfactant or an amphoteric surfactant.
[0160] The antiperspirant composition may comprise a personal care ingredient. The personal care ingredient may be a skin care agent, such as an emollient, a humectant, a skin barrier enhancer, or a skin appearance modifier.
[0161] The antiperspirant composition may contain a variety of other optional components, such as adhesives, biological additives, buffering agents, colorants, fragrances, conditioning agents, exfoliants, pH adjusting agents, preservatives, skin soothing agents, or skin healing agents.
[0162] Preferably, the antiperspirant composition comprises a preservative and optionally one or more components selected from the group consisting of adhesives, biological additives, buffers, colorants, fragrances, conditioners, exfoliants, pH adjusters, skin soothing agents, and skin healing agents.
[0163] Typically, an antiperspirant composition provides at least a 20% reduction in sweat in at least 50% of the subjects tested, as measured according to US FDA guidelines (Ref. 3).
[0164] Typically, the antiperspirant composition is also a deodorant composition.
[0165] The antiperspirant composition can be prepared by conventional methods known in the art.
[0166] Methods and uses
[0167] The methods or uses of the present invention are non-therapeutic.
[0168] The antiperspirant compositions of the present invention are useful as cosmetics, particularly for personal care.
[0169] The antiperspirant composition or antiperspirant is applied to the skin, preferably topically.
[0170] The antiperspirant composition or antiperspirant is applied to the skin surface.
[0171] Typically, the skin is mammalian, preferably human skin.
[0172] Typically, antiperspirant compositions or antiperspirants are applied to areas of the skin that sweat, preferably areas of the skin that have sweat glands (such as apocrine sweat glands or eccrine sweat glands, preferably apocrine sweat glands).
[0173] The skin area can be on the thigh (e.g., inner thigh), groin, back, upper lip, armpit, forehead, knee (e.g., behind the knee), neck (e.g., back of the neck), buttocks, chest, scalp, or hand. Preferably, the skin area is the armpit.
[0174] Antiperspirant compositions or antiperspirants can be applied by means of an applicator that contacts the body directly, such as a roll-on lotion or a solid stick product.
[0175] Alternatively, the antiperspirant composition or antiperspirant can be applied by a non-contact applicator, such as by spraying onto the skin. The non-contact applicator can be an aerosol sprayer, a pump sprayer, or a squeeze sprayer.
[0176] The antiperspirant, natural extract and / or antiperspirant composition may be used as a deodorant.
[0177] Example
[0178] The invention will now be illustrated by the following non-limiting examples.
[0179] Examples 1 to 3
[0180] Formulation Examples 1 to 3 shown in Table 1 were prepared by conventional methods.
[0181] Table 1
[0182]
[0183] In Table 1 above, E1 is cinnamon extract; E2 is emblica officinalis extract; and E3 is trans-cinnamic acid. The extracts were obtained from Sabinsa. Each natural extract was included in each formulation in an amount to provide the same amount of antiperspirant in the formulation.
[0184] Comparative Example
[0185] The formulations shown in Table 2 were prepared to provide a comparison with the formulations in Table 1. These formulations did not contain natural extracts.
[0186] Table 2
[0187]
[0188] In Table 2 above, AP1 is aluminum chlorohydrate and AP2 is aluminum zirconium tetrachloroglycinate (AZG).
[0189] Roll-on antiperspirants
[0190] The method of manufacturing the roll-on product is as follows.
[0191] 1. Combine cyclomethicone, phenyl trimethicone, stearyl alcohol, PPG-14 butyl ether, and hydrogenated castor oil.
[0192] 2. Heat to 82°C to melt the solid.
[0193] 3. Maintaining the temperature at 82°C, slowly add the silica using a high-speed disc dispenser.
[0194] 4. After all the silica has been added, increase the mixing speed to a line speed of almost 4000 ft / min or higher to achieve satisfactory dispersion.
[0195] 5. Add starch, then add natural AP powder.
[0196] 6. It is important to disperse each component evenly before adding the next component.
[0197] 7. After all components have been added, cool the mixture to 55°C.
[0198] In vivo testing procedures
[0199] Study Design
[0200] The formulation examples were tested in a standard hot room evaluation clinical study. Study subjects were subjected to heat stress after application of the antiperspirant composition. Sweat reduction was determined by gravimetric collection of sweat.
[0201] Subjects: 40 female subjects.
[0202] Conditions: A 17-day washout period during which the test members did not use any antiperspirants.
[0203] Test design: Subjects underwent a 5-day administration period, in which each person was given 400 mg + 50 mg of one of the formulation examples. After the 5th day, sweat collection was performed after the test members entered a hot room (100°F ± 2°F and 35% ± 5% relative humidity) for 80 minutes to induce sweating.
[0204] Data Analysis: Data were transformed to their natural logarithm and analyzed as means according to the method described by Murphy and Levine (Ref. 2). The covariance analysis model included the factors sequence, subject in sequence, test article, axilla, and baseline as a covariate.
[0205] For each formulation, the percent change in sweat reduction was determined. Clinical study data showed that all formulations were effective in reducing sweat, with formulations F1 to F3 demonstrating greater than 30% sweat reduction compared to baseline. A sweat reduction of at least 20% is considered suitable for commercial use as an antiperspirant.
[0206] Formulation F3 showed comparable sweat efficacy results when compared to comparative products containing aluminum or aluminum zirconium.
[0207] Examples 4 and 5
[0208] Further experiments were conducted using Formulation No. 3 (see Table 1 above), except that the amount of trans-cinnamic acid was varied. Formulation No. 4 contained 3 wt% trans-cinnamic acid. Formulation No. 5 contained 10 wt% trans-cinnamic acid. These formulations were prepared using the same method as described above for the roll-on antiperspirant product.
[0209] In vivo testing
[0210] In vivo testing was performed using each formulation.
[0211] To be included in the study, participants were required to show a sweat volume of 150 mg per armpit during the initial assessment. The same methods described above were used to conduct these tests, with the following details.
[0212] Formulation 4: 30 test members participated in the study, and each test member was given 400 mg of the formulation during a 5-day administration period.
[0213] Formulation 5: 33 subjects participated in the study with an 18-day washout period. Each subject was given 400 mg of the formulation.
[0214] When pre-treatment records were available in the study (baseline), the rate of axillary sweating after the last application of the study product was adjusted for the ratio of the right to left axillary sweat rate for each individual, defined as follows:
[0215] Z=(PC×T) / (PT×C)
[0216] wherein Z is the adjusted left-to-right ratio; PC is the amount of sweat obtained in the control axilla before treatment; PT is the amount of sweat obtained in the axilla to be treated before treatment; T is the amount of sweat obtained in the axilla using the formulation of the present invention; and C is the amount of sweat obtained in the control axilla.
[0217] The results are shown in Tables 3 and 4 below.
[0218] Table 3: Formulation 4
[0219]
[0220] Table 4: Formulation 5
[0221]
[0222] In both studies, no statistically significant differences were found in median sweat values between the products and the control. Based on the method used to evaluate antiperspirant efficacy, Formulations 4 and 5 demonstrated a reduction in sweat eight hours after the last application. Both tests showed that at least 50% of the study participants experienced a reduction in sweat of at least 20%.
[0223] Example 6
[0224] A study was conducted to evaluate the deodorizing effect using Formulation 5. The deodorizing study was designed as a single-center, single-blind, randomized trial to determine the deodorizing effect of trans-cinnamic acid.
[0225] In this study, 12 subjects were pretreated by using only soap and no deodorant, antiperspirant, fragrance, or medicated products for at least 48 hours, as described in the above studies.
[0226] On the test day, the odor of the test members was evaluated by 3 judges. The odor score was measured from 0 (no odor) to 4 (severe). In order to participate in the study, the test members needed to have an odor score of at least 3 points.
[0227] After the test members were evaluated and identified, Formulation 5 was immediately applied to one armpit. All test members were randomly administered. The test members' odor was then evaluated at 8 hours, 24 hours, and 48 hours.
[0228] Notably, the results showed statistically significant decreases in odor scores at the 8-hour, 24-hour, and 48-hour time points.
[0229] References
[0230] The following documents are cited in the description.
[0231] 1.APRauter et al.; "Nomenclature of flavonoids (IUPACRecommendations2017)"; Pure Appl.Chem., 90(9), (2018), 1429-1486.
[0232] 2. TDMurphy&M.J.Levine; "Analysis of Antiperspirant Efficacy TestResults"; Journal of the Society of Cosmetic Chemists, 42, (1991), 167-197.
[0233] 3. "Guidelines for Effectiveness Testing of OTC Antiperspirant DrugProducts", published by the US FDA, when read in conjunction with §350.60 (21CFR350.60) of the final monograph (final rule) for OTC antiperspirant drug products, published in the US FEDERAL REGISTER on June 9, 2003 (68FR 34273).
[0234] The entire disclosure of each document cited herein is hereby incorporated by reference.All references cited in this disclosure are incorporated by reference as if each reference were individually incorporated by reference in its entirety.
[0235] The citation and incorporation of patent documents herein is for convenience only and does not reflect any view of the validity, patentability, and / or enforceability of these patent documents.
[0236] A number of embodiments of the present disclosure have been described. However, it will be appreciated that various modifications can be made without departing from the spirit and scope of the present disclosure. Accordingly, other embodiments are within the scope of the following claims.
[0237] All headings and sub-headings are used herein for convenience only and should not be construed as limiting the invention in any way.
[0238] The use of any and all examples or exemplary language (e.g., "such as") provided herein is intended solely to better illustrate the invention and does not limit the scope of the invention unless otherwise specified. No language in the specification should be construed as indicating any unspecified element is essential to the practice of the invention.
Claims
1. An antiperspirant composition comprising an antiperspirant, wherein the antiperspirant comprises an optionally substituted phenylacrylic acid.
2. An antiperspirant composition according to claim 1, wherein the optionally substituted phenylacrylic acid is a phytochemical.
3. The antiperspirant composition according to claim 1 or claim 2, wherein the optionally substituted phenylacrylic acid is trans-phenylacrylic acid.
4. The antiperspirant composition according to any one of claims 1 to 3, wherein the optionally substituted phenylacrylic acid is represented by formula (I): where R 1 to R 5 Each is independently selected from H, hydroxyl and C1-C6 alkoxy.
5. The antiperspirant composition according to claim 4, wherein R 1 to R 5 At least three of them are hydrogen.
6. The antiperspirant composition according to claim 4 or claim 5, wherein R 1 to R 5 The two adjacent groups are each independently selected from hydroxyl and C1-C6 alkoxy.
7. The antiperspirant composition according to any one of claims 4 to 6, wherein R 1 、R 4 and R 5 is hydrogen, and R 2 and R 3 Each is independently selected from hydroxyl and C1-C6 alkoxy.
8. The antiperspirant composition according to any one of claims 1 to 4, wherein the optionally substituted phenylacrylic acid is selected from cinnamic acid, o-coumaric acid, m-coumaric acid, p-coumaric acid, caffeic acid, ferulic acid, 5-hydroxyferulic acid and sinapinic acid.
9. The antiperspirant composition of claim 8, wherein the optionally substituted phenylacrylic acid is trans-cinnamic acid.
10. The antiperspirant composition of any one of claims 1 to 10, wherein the antiperspirant further comprises an ester of gallic acid.
11. The antiperspirant composition according to claim 10, wherein the ester of gallic acid is selected from flavonoid esters of gallic acid and sugar esters of gallic acid.
12. The antiperspirant composition according to claim 11, wherein the ester of gallic acid is a sugar ester of gallic acid, preferably the sugar ester of gallic acid is glucogalloside (eg β-glucogalloside).
13. An antiperspirant composition according to any one of claims 1 to 12, wherein the antiperspirant is obtained or obtainable from a natural extract, preferably the natural extract is cinnamon extract and optionally emblica extract, such as a mixture of cinnamon extract and emblica extract.
14. The antiperspirant composition of any preceding claim comprising a total amount of about 0.1 to about 25.0 wt% of the antiperspirant.
15. The antiperspirant composition according to any of the preceding claims, comprising a total amount of from about 0.5 to about 25.0 wt%, preferably from 1.5 to about 25.0 wt%, more preferably from about 3.0 to about 20.0 wt% of the optionally substituted phenylacrylic acid.
16. The antiperspirant composition according to any one of the preceding claims, which does not comprise 4-hydroxybenzaldehyde.
17. An antiperspirant composition comprising a natural extract which is a cinnamon extract and an emblica extract, such as a mixture of a cinnamon extract and an emblica extract.
18. The antiperspirant composition of claim 17, wherein the cinnamon extract comprises one or more 2-flavonoids.
19. The antiperspirant composition of claim 18, wherein at least one of the one or more 2-flavonoids is a flavanol, preferably a flavan-3-ol.
20. The antiperspirant composition of claim 19, wherein the flavanol or flavan-3-ol is affecatechin, epicatechin, catechin, epicatechin, gallocatechin, epigallocatechin, or a combination of two or more thereof.
21. The antiperspirant composition according to any one of claims 18 to 20, wherein at least one of the one or more 2-flavonoids is a flavanone, preferably a flavan-4-one.
22. The antiperspirant composition according to claim 21, wherein the flavanone or flavan-4-one is rutin.
23. An antiperspirant composition according to any one of claims 17 to 22, wherein the cinnamon extract comprises cinnamic acid, preferably trans-cinnamic acid.
24. The antiperspirant composition of any one of claims 17 to 23, wherein the natural extract comprises an emblica fruit extract, wherein the emblica fruit extract comprises glucogallocatechin (eg, β-glucogallocatechin).
25. The antiperspirant composition of any one of claims 17 to 24, comprising the natural extract in a total amount of about 5.0 to about 40.0 wt%.
26. The antiperspirant composition of any preceding claim further comprising a topically acceptable carrier.
27. An antiperspirant composition according to any preceding claim in the form of a cream, gel, paste, liquid, lotion, foam, scrub or powder.
28. The antiperspirant composition of any preceding claim, further comprising a lubricant.
29. The antiperspirant composition of any preceding claim further comprising a fragrance.
30. The antiperspirant composition of any preceding claim, further comprising a thickener.
31. The antiperspirant composition of any preceding claim, further comprising a preservative.
32. A method of reducing or preventing perspiration comprising the step of applying to the skin an antiperspirant composition according to any one of claims 1 to 31.
33. Use of an antiperspirant composition according to any one of claims 1 to 31 for reducing or preventing perspiration.
34. Use of an optionally substituted phenylacrylic acid, optionally in combination with an ester of gallic acid, as an antiperspirant for reducing or preventing sweating, preferably wherein the optionally substituted phenylacrylic acid is as defined in any one of claims 2 to 9 or 13 and the ester of gallic acid is as defined in any one of claims 11 to 13.
35. Use of a natural extract as an antiperspirant for reducing or preventing sweating, wherein the natural extract is a cinnamon extract and optionally an emblica extract, preferably wherein the natural extract is as defined in any one of claims 17 to 25.