EP4291151A1 - Antiperspirant composition - Google Patents
Antiperspirant compositionInfo
- Publication number
- EP4291151A1 EP4291151A1 EP22704914.5A EP22704914A EP4291151A1 EP 4291151 A1 EP4291151 A1 EP 4291151A1 EP 22704914 A EP22704914 A EP 22704914A EP 4291151 A1 EP4291151 A1 EP 4291151A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- weight
- water
- oil emulsion
- emulsion composition
- active ingredients
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 278
- 239000003213 antiperspirant Substances 0.000 title claims abstract description 109
- 230000001166 anti-perspirative effect Effects 0.000 title claims abstract description 106
- 239000007762 w/o emulsion Substances 0.000 claims abstract description 129
- 239000004480 active ingredient Substances 0.000 claims abstract description 78
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 62
- 239000003974 emollient agent Substances 0.000 claims abstract description 42
- 239000002781 deodorant agent Substances 0.000 claims abstract description 29
- 239000002537 cosmetic Substances 0.000 claims abstract description 19
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 16
- 239000000969 carrier Substances 0.000 claims abstract description 15
- 238000002560 therapeutic procedure Methods 0.000 claims abstract description 6
- 239000007921 spray Substances 0.000 claims description 58
- 150000003839 salts Chemical class 0.000 claims description 34
- 229920001577 copolymer Polymers 0.000 claims description 32
- 239000004411 aluminium Substances 0.000 claims description 29
- 229910052782 aluminium Inorganic materials 0.000 claims description 29
- NKJOXAZJBOMXID-UHFFFAOYSA-N 1,1'-Oxybisoctane Chemical compound CCCCCCCCOCCCCCCCC NKJOXAZJBOMXID-UHFFFAOYSA-N 0.000 claims description 28
- 239000003380 propellant Substances 0.000 claims description 26
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims description 25
- 239000004094 surface-active agent Substances 0.000 claims description 24
- DURPTKYDGMDSBL-UHFFFAOYSA-N 1-butoxybutane Chemical compound CCCCOCCCC DURPTKYDGMDSBL-UHFFFAOYSA-N 0.000 claims description 22
- CXMXRPHRNRROMY-UHFFFAOYSA-N n-Decanedioic acid Natural products OC(=O)CCCCCCCCC(O)=O CXMXRPHRNRROMY-UHFFFAOYSA-N 0.000 claims description 21
- 239000003755 preservative agent Substances 0.000 claims description 20
- ZLCMTFCQJBGXGR-UHFFFAOYSA-N 1,2,3-trihydroxyundecan-4-one Chemical compound CCCCCCCC(=O)C(O)C(O)CO ZLCMTFCQJBGXGR-UHFFFAOYSA-N 0.000 claims description 19
- 230000003750 conditioning effect Effects 0.000 claims description 19
- 239000003381 stabilizer Substances 0.000 claims description 18
- 150000001335 aliphatic alkanes Chemical class 0.000 claims description 16
- IIYFAKIEWZDVMP-UHFFFAOYSA-N tridecane Chemical compound CCCCCCCCCCCCC IIYFAKIEWZDVMP-UHFFFAOYSA-N 0.000 claims description 14
- PJHKBYALYHRYSK-UHFFFAOYSA-N triheptanoin Chemical compound CCCCCCC(=O)OCC(OC(=O)CCCCCC)COC(=O)CCCCCC PJHKBYALYHRYSK-UHFFFAOYSA-N 0.000 claims description 14
- 229940078561 triheptanoin Drugs 0.000 claims description 14
- RSJKGSCJYJTIGS-UHFFFAOYSA-N undecane Chemical compound CCCCCCCCCCC RSJKGSCJYJTIGS-UHFFFAOYSA-N 0.000 claims description 14
- NRTKYSGFUISGRQ-UHFFFAOYSA-N (3-heptanoyloxy-2,2-dimethylpropyl) heptanoate Chemical compound CCCCCCC(=O)OCC(C)(C)COC(=O)CCCCCC NRTKYSGFUISGRQ-UHFFFAOYSA-N 0.000 claims description 13
- 230000000699 topical effect Effects 0.000 claims description 10
- WHBKVWBGTBULQY-UHFFFAOYSA-N 2-propylheptyl octanoate Chemical compound CCCCCCCC(=O)OCC(CCC)CCCCC WHBKVWBGTBULQY-UHFFFAOYSA-N 0.000 claims description 8
- QCWXUUIWCKQGHC-UHFFFAOYSA-N Zirconium Chemical compound [Zr] QCWXUUIWCKQGHC-UHFFFAOYSA-N 0.000 claims description 8
- 229940043375 1,5-pentanediol Drugs 0.000 claims description 7
- ZQCIPRGNRQXXSK-UHFFFAOYSA-N 1-octadecoxypropan-2-ol Chemical compound CCCCCCCCCCCCCCCCCCOCC(C)O ZQCIPRGNRQXXSK-UHFFFAOYSA-N 0.000 claims description 7
- GTJOHISYCKPIMT-UHFFFAOYSA-N 2-methylundecane Chemical compound CCCCCCCCCC(C)C GTJOHISYCKPIMT-UHFFFAOYSA-N 0.000 claims description 7
- YUDHLDPCTPRMRB-UHFFFAOYSA-N 4-propyldecan-4-yl hydrogen carbonate Chemical compound CCCCCCC(CCC)(CCC)OC(=O)O YUDHLDPCTPRMRB-UHFFFAOYSA-N 0.000 claims description 7
- XTJFFFGAUHQWII-UHFFFAOYSA-N Dibutyl adipate Chemical compound CCCCOC(=O)CCCCC(=O)OCCCC XTJFFFGAUHQWII-UHFFFAOYSA-N 0.000 claims description 7
- SGVYKUFIHHTIFL-UHFFFAOYSA-N Isobutylhexyl Natural products CCCCCCCC(C)C SGVYKUFIHHTIFL-UHFFFAOYSA-N 0.000 claims description 7
- DJNTZVRUYMHBTD-UHFFFAOYSA-N Octyl octanoate Chemical compound CCCCCCCCOC(=O)CCCCCCC DJNTZVRUYMHBTD-UHFFFAOYSA-N 0.000 claims description 7
- 239000003963 antioxidant agent Substances 0.000 claims description 7
- MQKXWEJVDDRQKK-UHFFFAOYSA-N bis(6-methylheptyl) butanedioate Chemical compound CC(C)CCCCCOC(=O)CCC(=O)OCCCCCC(C)C MQKXWEJVDDRQKK-UHFFFAOYSA-N 0.000 claims description 7
- 229940048300 coco-caprylate Drugs 0.000 claims description 7
- GHVNFZFCNZKVNT-UHFFFAOYSA-M decanoate Chemical compound CCCCCCCCCC([O-])=O GHVNFZFCNZKVNT-UHFFFAOYSA-M 0.000 claims description 7
- 229940100539 dibutyl adipate Drugs 0.000 claims description 7
- PBZAGXRVDLNBCJ-UHFFFAOYSA-N diheptyl butanedioate Chemical compound CCCCCCCOC(=O)CCC(=O)OCCCCCCC PBZAGXRVDLNBCJ-UHFFFAOYSA-N 0.000 claims description 7
- 229940024497 diheptyl succinate Drugs 0.000 claims description 7
- PKPOVTYZGGYDIJ-UHFFFAOYSA-N dioctyl carbonate Chemical compound CCCCCCCCOC(=O)OCCCCCCCC PKPOVTYZGGYDIJ-UHFFFAOYSA-N 0.000 claims description 7
- DLAHAXOYRFRPFQ-UHFFFAOYSA-N dodecyl benzoate Chemical compound CCCCCCCCCCCCOC(=O)C1=CC=CC=C1 DLAHAXOYRFRPFQ-UHFFFAOYSA-N 0.000 claims description 7
- XJFGDLJQUJQUEI-UHFFFAOYSA-N dodecyl decanoate dodecyl octanoate Chemical compound CCCCCCCCCCCCOC(=O)CCCCCCC.CCCCCCCCCCCCOC(=O)CCCCCCCCC XJFGDLJQUJQUEI-UHFFFAOYSA-N 0.000 claims description 7
- NLMOQNHZOQGLSZ-UHFFFAOYSA-N heptyl undec-10-enoate Chemical compound CCCCCCCOC(=O)CCCCCCCCC=C NLMOQNHZOQGLSZ-UHFFFAOYSA-N 0.000 claims description 7
- 229940086561 heptyl undecylenate Drugs 0.000 claims description 7
- PMMXXYHTOMKOAZ-UHFFFAOYSA-N hexadecyl 7-methyloctanoate Chemical compound CCCCCCCCCCCCCCCCOC(=O)CCCCCC(C)C PMMXXYHTOMKOAZ-UHFFFAOYSA-N 0.000 claims description 7
- VKPSKYDESGTTFR-UHFFFAOYSA-N isododecane Natural products CC(C)(C)CC(C)CC(C)(C)C VKPSKYDESGTTFR-UHFFFAOYSA-N 0.000 claims description 7
- XUGNVMKQXJXZCD-UHFFFAOYSA-N isopropyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(C)C XUGNVMKQXJXZCD-UHFFFAOYSA-N 0.000 claims description 7
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims description 7
- WCVRQHFDJLLWFE-UHFFFAOYSA-N pentane-1,2-diol Chemical compound CCCC(O)CO WCVRQHFDJLLWFE-UHFFFAOYSA-N 0.000 claims description 7
- 229940078491 ppg-15 stearyl ether Drugs 0.000 claims description 7
- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 claims description 7
- 229910052726 zirconium Inorganic materials 0.000 claims description 7
- HBTAOSGHCXUEKI-UHFFFAOYSA-N 4-chloro-n,n-dimethyl-3-nitrobenzenesulfonamide Chemical compound CN(C)S(=O)(=O)C1=CC=C(Cl)C([N+]([O-])=O)=C1 HBTAOSGHCXUEKI-UHFFFAOYSA-N 0.000 claims description 6
- 239000001856 Ethyl cellulose Substances 0.000 claims description 6
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 6
- 229920001800 Shellac Polymers 0.000 claims description 6
- 229940031578 diisopropyl adipate Drugs 0.000 claims description 6
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 6
- 229920001249 ethyl cellulose Polymers 0.000 claims description 6
- VAMFXQBUQXONLZ-UHFFFAOYSA-N n-alpha-eicosene Natural products CCCCCCCCCCCCCCCCCCC=C VAMFXQBUQXONLZ-UHFFFAOYSA-N 0.000 claims description 6
- 239000004208 shellac Substances 0.000 claims description 6
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 claims description 6
- 229940113147 shellac Drugs 0.000 claims description 6
- 235000013874 shellac Nutrition 0.000 claims description 6
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims description 5
- 239000003981 vehicle Substances 0.000 claims description 5
- 229910052725 zinc Inorganic materials 0.000 claims description 5
- 239000011701 zinc Substances 0.000 claims description 5
- POAOYUHQDCAZBD-UHFFFAOYSA-N 2-butoxyethanol Chemical compound CCCCOCCO POAOYUHQDCAZBD-UHFFFAOYSA-N 0.000 claims description 4
- 230000003078 antioxidant effect Effects 0.000 claims description 4
- 229920001451 polypropylene glycol Polymers 0.000 claims description 4
- 230000002335 preservative effect Effects 0.000 claims description 4
- LEACJMVNYZDSKR-UHFFFAOYSA-N 2-octyldodecan-1-ol Chemical compound CCCCCCCCCCC(CO)CCCCCCCC LEACJMVNYZDSKR-UHFFFAOYSA-N 0.000 claims description 2
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 claims description 2
- 150000001252 acrylic acid derivatives Chemical class 0.000 claims description 2
- BTFJIXJJCSYFAL-UHFFFAOYSA-N arachidyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCO BTFJIXJJCSYFAL-UHFFFAOYSA-N 0.000 claims description 2
- 238000000034 method Methods 0.000 abstract description 43
- 230000008569 process Effects 0.000 abstract description 22
- 238000002360 preparation method Methods 0.000 abstract description 17
- 239000000839 emulsion Substances 0.000 description 51
- 210000004243 sweat Anatomy 0.000 description 37
- 239000012071 phase Substances 0.000 description 32
- 235000002639 sodium chloride Nutrition 0.000 description 32
- 239000003921 oil Substances 0.000 description 27
- 238000012360 testing method Methods 0.000 description 27
- 230000000052 comparative effect Effects 0.000 description 25
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 24
- 230000000694 effects Effects 0.000 description 23
- 238000011156 evaluation Methods 0.000 description 19
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 17
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 17
- -1 /7-propanol Chemical compound 0.000 description 16
- 229920001296 polysiloxane Polymers 0.000 description 15
- NNPPMTNAJDCUHE-UHFFFAOYSA-N isobutane Chemical compound CC(C)C NNPPMTNAJDCUHE-UHFFFAOYSA-N 0.000 description 14
- 238000006243 chemical reaction Methods 0.000 description 12
- 238000002474 experimental method Methods 0.000 description 12
- BARWIPMJPCRCTP-CLFAGFIQSA-N oleyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCCOC(=O)CCCCCCC\C=C/CCCCCCCC BARWIPMJPCRCTP-CLFAGFIQSA-N 0.000 description 11
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 10
- 239000004615 ingredient Substances 0.000 description 10
- 238000005259 measurement Methods 0.000 description 10
- 239000002245 particle Substances 0.000 description 10
- 239000000047 product Substances 0.000 description 10
- 230000002159 abnormal effect Effects 0.000 description 9
- 208000008454 Hyperhidrosis Diseases 0.000 description 8
- VSCWAEJMTAWNJL-UHFFFAOYSA-K aluminium trichloride Chemical compound Cl[Al](Cl)Cl VSCWAEJMTAWNJL-UHFFFAOYSA-K 0.000 description 8
- 239000000463 material Substances 0.000 description 8
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 8
- 239000011148 porous material Substances 0.000 description 8
- 239000001294 propane Substances 0.000 description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 7
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 7
- 229910021502 aluminium hydroxide Inorganic materials 0.000 description 7
- 238000009472 formulation Methods 0.000 description 7
- 239000003205 fragrance Substances 0.000 description 7
- 239000001282 iso-butane Substances 0.000 description 7
- 239000007788 liquid Substances 0.000 description 7
- 238000011282 treatment Methods 0.000 description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- 206010040914 Skin reaction Diseases 0.000 description 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
- 239000002253 acid Substances 0.000 description 6
- 150000007513 acids Chemical class 0.000 description 6
- 235000006708 antioxidants Nutrition 0.000 description 6
- 239000004205 dimethyl polysiloxane Substances 0.000 description 6
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 6
- 201000010099 disease Diseases 0.000 description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 230000007717 exclusion Effects 0.000 description 6
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 description 6
- 230000005923 long-lasting effect Effects 0.000 description 6
- 238000002156 mixing Methods 0.000 description 6
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 6
- 229940116351 sebacate Drugs 0.000 description 6
- CXMXRPHRNRROMY-UHFFFAOYSA-L sebacate(2-) Chemical compound [O-]C(=O)CCCCCCCCC([O-])=O CXMXRPHRNRROMY-UHFFFAOYSA-L 0.000 description 6
- 230000035483 skin reaction Effects 0.000 description 6
- 231100000430 skin reaction Toxicity 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
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- 229940008099 dimethicone Drugs 0.000 description 5
- 230000037315 hyperhidrosis Effects 0.000 description 5
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- 229960004063 propylene glycol Drugs 0.000 description 5
- 230000001105 regulatory effect Effects 0.000 description 5
- 239000002562 thickening agent Substances 0.000 description 5
- NPNPZTNLOVBDOC-UHFFFAOYSA-N 1,1-difluoroethane Chemical compound CC(F)F NPNPZTNLOVBDOC-UHFFFAOYSA-N 0.000 description 4
- VQTUBCCKSQIDNK-UHFFFAOYSA-N Isobutene Chemical compound CC(C)=C VQTUBCCKSQIDNK-UHFFFAOYSA-N 0.000 description 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 4
- 239000002202 Polyethylene glycol Substances 0.000 description 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 4
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- 230000003592 biomimetic effect Effects 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 230000000875 corresponding effect Effects 0.000 description 4
- LVYZJEPLMYTTGH-UHFFFAOYSA-H dialuminum chloride pentahydroxide dihydrate Chemical compound [Cl-].[Al+3].[OH-].[OH-].[Al+3].[OH-].[OH-].[OH-].O.O LVYZJEPLMYTTGH-UHFFFAOYSA-H 0.000 description 4
- 230000014509 gene expression Effects 0.000 description 4
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical class CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 4
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- 235000019645 odor Nutrition 0.000 description 4
- 229920003229 poly(methyl methacrylate) Polymers 0.000 description 4
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- 239000004926 polymethyl methacrylate Substances 0.000 description 4
- 230000002035 prolonged effect Effects 0.000 description 4
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- 229940051271 1,1-difluoroethane Drugs 0.000 description 3
- 208000035985 Body Odor Diseases 0.000 description 3
- 101100310593 Candida albicans (strain SC5314 / ATCC MYA-2876) SOD4 gene Proteins 0.000 description 3
- 206010013786 Dry skin Diseases 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 101100096123 Zantedeschia aethiopica SODCP gene Proteins 0.000 description 3
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
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- 125000004432 carbon atom Chemical group C* 0.000 description 3
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- 150000002430 hydrocarbons Chemical group 0.000 description 3
- OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 description 3
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- DUNKXUFBGCUVQW-UHFFFAOYSA-J zirconium tetrachloride Chemical compound Cl[Zr](Cl)(Cl)Cl DUNKXUFBGCUVQW-UHFFFAOYSA-J 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
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- HBXWUCXDUUJDRB-UHFFFAOYSA-N 1-octadecoxyoctadecane Chemical compound CCCCCCCCCCCCCCCCCCOCCCCCCCCCCCCCCCCCC HBXWUCXDUUJDRB-UHFFFAOYSA-N 0.000 description 2
- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 description 2
- SVTBMSDMJJWYQN-UHFFFAOYSA-N 2-methylpentane-2,4-diol Chemical compound CC(O)CC(C)(C)O SVTBMSDMJJWYQN-UHFFFAOYSA-N 0.000 description 2
- ANZUDYZHSVGBRF-UHFFFAOYSA-N 3-ethylnonane-1,2,3-triol Chemical compound CCCCCCC(O)(CC)C(O)CO ANZUDYZHSVGBRF-UHFFFAOYSA-N 0.000 description 2
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- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
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- 239000004322 Butylated hydroxytoluene Substances 0.000 description 2
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 2
- QFOHBWFCKVYLES-UHFFFAOYSA-N Butylparaben Chemical compound CCCCOC(=O)C1=CC=C(O)C=C1 QFOHBWFCKVYLES-UHFFFAOYSA-N 0.000 description 2
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- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- XMSXQFUHVRWGNA-UHFFFAOYSA-N Decamethylcyclopentasiloxane Chemical compound C[Si]1(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O1 XMSXQFUHVRWGNA-UHFFFAOYSA-N 0.000 description 2
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
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- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 229910052746 lanthanum Inorganic materials 0.000 description 1
- FZLIPJUXYLNCLC-UHFFFAOYSA-N lanthanum atom Chemical compound [La] FZLIPJUXYLNCLC-UHFFFAOYSA-N 0.000 description 1
- JXNPEDYJTDQORS-UHFFFAOYSA-N linoleyl alcohol Natural products CCCCCC=CCC=CCCCCCCCCO JXNPEDYJTDQORS-UHFFFAOYSA-N 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 239000007791 liquid phase Substances 0.000 description 1
- 239000000711 locust bean gum Substances 0.000 description 1
- 235000010420 locust bean gum Nutrition 0.000 description 1
- 235000011147 magnesium chloride Nutrition 0.000 description 1
- 229910052943 magnesium sulfate Inorganic materials 0.000 description 1
- 235000019341 magnesium sulphate Nutrition 0.000 description 1
- 238000004949 mass spectrometry Methods 0.000 description 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 229960002216 methylparaben Drugs 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 230000003020 moisturizing effect Effects 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 235000011929 mousse Nutrition 0.000 description 1
- 229940043348 myristyl alcohol Drugs 0.000 description 1
- 235000005152 nicotinamide Nutrition 0.000 description 1
- 229960003966 nicotinamide Drugs 0.000 description 1
- 239000011570 nicotinamide Substances 0.000 description 1
- 229960002715 nicotine Drugs 0.000 description 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical class CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Chemical class CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 229940055577 oleyl alcohol Drugs 0.000 description 1
- XMLQWXUVTXCDDL-UHFFFAOYSA-N oleyl alcohol Natural products CCCCCCC=CCCCCCCCCCCO XMLQWXUVTXCDDL-UHFFFAOYSA-N 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- GTLACDSXYULKMZ-UHFFFAOYSA-N pentafluoroethane Chemical compound FC(F)C(F)(F)F GTLACDSXYULKMZ-UHFFFAOYSA-N 0.000 description 1
- 239000002304 perfume Substances 0.000 description 1
- 238000011458 pharmacological treatment Methods 0.000 description 1
- 229960005323 phenoxyethanol Drugs 0.000 description 1
- CTYRPMDGLDAWRQ-UHFFFAOYSA-N phenyl hydrogen sulfate Chemical compound OS(=O)(=O)OC1=CC=CC=C1 CTYRPMDGLDAWRQ-UHFFFAOYSA-N 0.000 description 1
- 229940057874 phenyl trimethicone Drugs 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- GRLPQNLYRHEGIJ-UHFFFAOYSA-J potassium aluminium sulfate Chemical compound [Al+3].[K+].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GRLPQNLYRHEGIJ-UHFFFAOYSA-J 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- ULWHHBHJGPPBCO-UHFFFAOYSA-N propane-1,1-diol Chemical compound CCC(O)O ULWHHBHJGPPBCO-UHFFFAOYSA-N 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- FGVVTMRZYROCTH-UHFFFAOYSA-N pyridine-2-thiol N-oxide Chemical class [O-][N+]1=CC=CC=C1S FGVVTMRZYROCTH-UHFFFAOYSA-N 0.000 description 1
- 229960002026 pyrithione Drugs 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical class OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 229940043230 sarcosine Drugs 0.000 description 1
- 108700004121 sarkosyl Proteins 0.000 description 1
- 231100000241 scar Toxicity 0.000 description 1
- 230000037387 scars Effects 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 230000003248 secreting effect Effects 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 230000001953 sensory effect Effects 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 230000036556 skin irritation Effects 0.000 description 1
- 231100000475 skin irritation Toxicity 0.000 description 1
- 239000000344 soap Substances 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 229960003885 sodium benzoate Drugs 0.000 description 1
- ADWNFGORSPBALY-UHFFFAOYSA-M sodium;2-[dodecyl(methyl)amino]acetate Chemical compound [Na+].CCCCCCCCCCCCN(C)CC([O-])=O ADWNFGORSPBALY-UHFFFAOYSA-M 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000012798 spherical particle Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 230000007480 spreading Effects 0.000 description 1
- 238000003892 spreading Methods 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 239000008117 stearic acid Chemical class 0.000 description 1
- 229940012831 stearyl alcohol Drugs 0.000 description 1
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- CRDAMVZIKSXKFV-UHFFFAOYSA-N trans-Farnesol Natural products CC(C)=CCCC(C)=CCCC(C)=CCO CRDAMVZIKSXKFV-UHFFFAOYSA-N 0.000 description 1
- ZDHXKXAHOVTTAH-UHFFFAOYSA-N trichlorosilane Chemical compound Cl[SiH](Cl)Cl ZDHXKXAHOVTTAH-UHFFFAOYSA-N 0.000 description 1
- 239000005052 trichlorosilane Substances 0.000 description 1
- ICUTUKXCWQYESQ-UHFFFAOYSA-N triclocarban Chemical compound C1=CC(Cl)=CC=C1NC(=O)NC1=CC=C(Cl)C(Cl)=C1 ICUTUKXCWQYESQ-UHFFFAOYSA-N 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- 239000001069 triethyl citrate Substances 0.000 description 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
- 235000013769 triethyl citrate Nutrition 0.000 description 1
- FAGMGMRSURYROS-UHFFFAOYSA-M trihexadecyl(methyl)azanium;chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+](C)(CCCCCCCCCCCCCCCC)CCCCCCCCCCCCCCCC FAGMGMRSURYROS-UHFFFAOYSA-M 0.000 description 1
- UUJLHYCIMQOUKC-UHFFFAOYSA-N trimethyl-[oxo(trimethylsilylperoxy)silyl]peroxysilane Chemical compound C[Si](C)(C)OO[Si](=O)OO[Si](C)(C)C UUJLHYCIMQOUKC-UHFFFAOYSA-N 0.000 description 1
- LINXHFKHZLOLEI-UHFFFAOYSA-N trimethyl-[phenyl-bis(trimethylsilyloxy)silyl]oxysilane Chemical compound C[Si](C)(C)O[Si](O[Si](C)(C)C)(O[Si](C)(C)C)C1=CC=CC=C1 LINXHFKHZLOLEI-UHFFFAOYSA-N 0.000 description 1
- VXYADVIJALMOEQ-UHFFFAOYSA-K tris(lactato)aluminium Chemical compound CC(O)C(=O)O[Al](OC(=O)C(C)O)OC(=O)C(C)O VXYADVIJALMOEQ-UHFFFAOYSA-K 0.000 description 1
- 238000002255 vaccination Methods 0.000 description 1
- 229960005486 vaccine Drugs 0.000 description 1
- 230000000007 visual effect Effects 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 238000004018 waxing Methods 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
- 229940043810 zinc pyrithione Drugs 0.000 description 1
- PICXIOQBANWBIZ-UHFFFAOYSA-N zinc;1-oxidopyridine-2-thione Chemical compound [Zn+2].[O-]N1C=CC=CC1=S.[O-]N1C=CC=CC1=S PICXIOQBANWBIZ-UHFFFAOYSA-N 0.000 description 1
- 150000003754 zirconium Chemical class 0.000 description 1
- 239000002888 zwitterionic surfactant Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/06—Emulsions
- A61K8/064—Water-in-oil emulsions, e.g. Water-in-silicone emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/26—Aluminium; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/37—Esters of carboxylic acids
- A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
- A61K8/85—Polyesters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/927—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of insects, e.g. shellac
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q15/00—Anti-perspirants or body deodorants
Abstract
The present invention relates to a pharmaceutical or cosmetic water-in-oil emulsion composition comprising: (a) a therapeutically or cosmetically effective amount of one or more antiperspirant active ingredients; (b) one or more film-forming agents; and (c) one or more emollients; (d) together with one or more pharmaceutically or cosmetically acceptable excipients or carriers. It also refers to a process for its preparation and its use in therapy and in cosmetic; particularly as a antiperspirant/deodorant agent.
Description
Antiperspirant composition
This application claims the benefit of European Patent Application EP21382105.1 filed on February 11th,
2022
The present invention relates to the antiperspirant and deodorant field. In particular to an effective long lasting invisible water-in-oil emulsion antiperspirant. It also relates to processes for their preparation and their uses in therapy and in cosmetic; such as an antiperspirant and a deodorant agent. Background Art
Antiperspirant and deodorant compositions are popular personal care products used to prevent or eliminate perspiration and body odor caused by perspiration. Most of antiperspirant compositions commonly used include at least one antiperspirant active ingredient that minimize or prevent the secretion of perspiration by blocking or plugging ducts of sweat-secreting glands. Further, most of the deodorant compositions include at least one deodorant active agent that minimize, prevent and/or eliminate malodor associated with perspiration.
The most common antiperspirant active ingredients typically used in these compositions are salts of strong inorganic acids, such as aluminium-containing and/or zirconium-containing salts. These salts upon contact with perspiration enter the sweat duct via diffusion or convection and react with the basic components of perspiration blocking it. Further, these antiperspirants and some other components of the composition often leaves a chalky film on the skin. When the composition dries on the skin or on clothing (which has come into contact with the skin after application of the antiperspirant), the antiperspirant salt often remains visible as a white residue. These white marks attack cellulosic fabrics due to liberation of strong acids from the salts, discolouring and ruining them over time, leaving the clothes with hard-to-remove stains. Besides, most of the antiperspirant compositions contain a high amount of oil components which increase the drying time upon contact with skin, providing an uncomfortable greasy and sticky feeling on application; and also leading to fabric staining.
Due to this fact, the antiperspirant industry has migrated away from the use of these antiperspirant active ingredients in order to develop less or non-irritating antiperspirant active ingredients and more aesthetically pleasing feeling. Unfortunately, most of these compositions that have been developed used to reduce skin irritation but also reduces significantly the antiperspirant efficacy and/or the long-lasting antiperspirant effect. Particularly, the use of aluminium-containing salts of weaker acids as non-irritating antiperspirant active ingredients has been disclosed. However, these compounds have proved much less effective in inhibiting perspiration and they also do not prevent odors as well as the salts of strong acids traditionally used.
Thus, from what is known in the art it is derived that there is still the need of developing an efficient and non irritant antiperspirant composition having a long-lasting antiperspirant protection and also an appropriate cosmetic acceptability.
Summary of Invention
Inventors have found that a water-in-oil emulsion composition comprising an effective amount of antiperspirant active ingredients, in combination with at least one of the film-forming agents and at least one of the emollients disclosed in the present application allows having a stable and effective long lasting antiperspiration effect for about 48 hours after its application without causing irritation on skin (of. antiperspirant activity test of the experimental section).
Particularly, the composition of the present invention contains natural and gentle components being non irritant to the skin, having at the same time a pleasant long lasting mild fragrance without the need of using silicones. In fact, as it is demonstrated in the use test of the experimental section, the composition of the present invention not only cares the skin but also strength and moisturize the skin.
Furthermore, inventors have also demonstrated that the composition of the invention had a good cosmeticity, having a very satisfactory acceptability for the users. In fact, after its application, the composition is uniformly distributed and quickly absorbed/dried without providing any oily or sticky feeling, leaving a dry skin with a comfortable feeling and clean appearance.
Finally, the composition of the invention, after its application, does not leave any white marks on the skin and clothes; as well as any stain in textile. In fact, as it is shown in the use test, all users stated that the composition of the invention prevent the appearance of stains on clothing.
To sum up, the water-in-oil emulsion composition of the invention reduces the extent of excessive/abnormal/normal perspiration for a long period of time, as well as avoid the occurrence of unsightly sweat marks on clothing and at the same time minimizing the body odour. Besides, the water-in-oil emulsion composition also allows having a good cosmeticity taking care of the skin without providing an oily or sticky feeling, leaving a dry skin with a comfortable feeling and clean appearance.
Thus, the first aspect of the invention refers to a pharmaceutical or cosmetic water-in-oil emulsion composition comprising: (a) a therapeutically or cosmetically effective amount of one or more antiperspirant active ingredients; (b) one or more film-forming agents selected from the group consisting of capryloyl glycerine/sebacic acid copolymer; polyester-7 (and) neopentyl glycol diheptanoate; ethylcellulose (and) diisopropyl adipate; VP/acrylates/lauryl methacrylate copolymer; VP/eicosene copolymer; triacontanyl PVP; and pentylene glycol (and) shellac; and (c) one or more emollients selected from the group consisting of
dicaprylyl ether; PPG-14 butyl ether; triheptanoin (and) (C13-C16) isoparaffin; heptyl undecylenate (and) (C13- C15) alkane; triheptanoin (and) (C13-C15) alkane; diisooctyl succinate; neopentyl glycol diheptanoate; diheptyl succinate; isododecane; dipropylheptyl carbonate; caprylyl caprylate/caprate; propylheptyl caprylate; cetearyl isononanoate; undecane (and) tridecane; (Ci2-Cis)alkyl benzoate, dibutyl adipate; coco-caprylate; dicaprylyl carbonate; PPG-15 stearyl ether; coco-caprylate/caprate; caprylic/capric triglyceride; cocoglycerides; octyldodecanol, isopropyl myristate, and isopropyl palmitate; (d) together with one or more pharmaceutically or cosmetically acceptable excipients or carriers.
The second aspect of the invention refers to the composition of the first aspect of the invention for use in therapy, particularly for the prophylaxis or treatment of a disease or condition that involves an excessive or abnormal transpiration.
The third aspect of the invention refers to the use of the composition of the first aspect of the invention as antiperspirant and deodorant agent.
Detailed description of the invention
All terms as used herein in this application, unless otherwise stated, shall be understood in their ordinary meaning as known in the art. Other more specific definitions for certain terms as used in the present application are as set forth below and are intended to apply uniformly throughout the specification and claims unless an otherwise expressly set out definition provides a broader definition.
For the purposes of the present invention, any ranges given include both the lower and the upper end-points of the range. Ranges given, such as weight, temperatures, times, weights, and the like, should be considered approximate, unless specifically stated.
The terms "percentage (%) by weight”, "weight/weight %" and “w/w%" have the same meaning and are used interchangeable. They refer to the percentage of each ingredient of the composition in relation to the total weight of the composition.
For the purpose of the invention, the term "alkyl” refers to a saturated straight, or branched hydrocarbon chain which contains the number of carbon atoms specified in the description or claims. Examples include, among others, the group methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, and tert-butyl. And, the term "alcohol” refers to an "alkane” wherein at least one hydrogen atom is substituted by a hydroxyl group and which contains the number of carbon atoms specified in the description or claims. The term "alkane" refers to a saturated, branched or linear hydrocarbon which contains the number of carbon atoms specified in the description or claims. Examples include methanol, ethanol, /7-propanol, iso-propanol, butanol, iso-butanol, and sec-butanol.
As it is mentioned above, the composition of the first aspect of the invention is a "water-in-oil” emulsion. The terms "water-in oil”, "water-in-oil” and "W/O” emulsion have the same meaning and are used interchangeably. They refer to an emulsion that includes a discontinuous phase, that is "water" phase (W) or predominantly aqueous phase, and a continuous phase, that is an "oil" phase, or predominantly organic liquid phase. The oil phase is at least partially immiscible with the water phase. This "water-in-oil emulsion" (W/O) is forming "particles” in a discontinuous water phase. The terms "particles” or "drops” have the same meaning and are used interchangeably. The term "particle size" refers to the particle diameter of the inner water drops (W) discontinuous phase based on an approximate spherical shape of the particle based on a volumetric measurement of the particle. In addition to spherical particles, the oil-in-water emulsions of the present invention can also comprise without limitation ellipsoidal and/or cylindrical particles. The method for determining the particle size of the compositions of the present invention can be any method known in the state of the art, for the purpose of the invention the particle size is measured by dynamic light scattering (DLS) technique.
In an embodiment, the water-in-oil emulsion composition of the present invention comprises
(a) a therapeutically or cosmetically effective amount of one or more antiperspirant active ingredients;
(b) one or more film-forming agents selected from the group consisting of capryloyl glycerine/sebacic acid copolymer; polyester-7 (and) neopentyl glycol diheptanoate; ethylcellulose (and) diisopropyl adipate; VP/acry I ates/l au ry I methacrylate copolymer; VP/eicosene copolymer; triacontanyl PVP; and pentylene glycol
(and) shellac; and
(c) one or more emollients selected from the group consisting of dicaprylyl ether; PPG-14 butyl ether; triheptanoin (and) (C13-C16) isoparaffin; heptyl undecylenate (and) (C13-C15) alkane; triheptanoin (and) (C13- C15) alkane; diisooctyl succinate; neopentyl glycol diheptanoate; diheptyl succinate; isododecane; dipropylheptyl carbonate; caprylyl caprylate/caprate; propylheptyl caprylate; cetearyl isononanoate; undecane (and) tridecane; (Ci2-Ci5)alkyl benzoate, dibutyl adipate; coco-caprylate; dicaprylyl carbonate; PPG-15 stearyl ether; coco-caprylate/caprate; caprylic/capric triglyceride; cocoglycerides; and isopropyl palmitate;
(d) together with one or more pharmaceutically or cosmetically acceptable excipients or carriers. In an embodiment, the water-in-oil emulsion composition of the present invention has a viscosity from 0 to 800 ops. In an embodiment, the water-in-oil emulsion composition of the present invention has a viscosity from 100 to 400 ops (1 centipoise (ops) corresponds to ImPa'S). The method for determining the viscosity can be any method known in the state of the art. For the purpose of the invention, the viscosity of the water-in-oil emulsion composition is measured by a Brookfield Dv-e Ametek LVDVE115 Digital Low Range Viscometer (splindle: 3 and speed:30 rpm) following the method disclosed in the European Pharmacopoeia 7.0 - 2.2.10. viscosity - rotating viscometer method.
Furthermore, the water-in-oil emulsion composition of the present invention comprises (a) a therapeutically or
cosmetically effective amount of one or more antiperspirant active ingredients. The term an "effective amount of the antiperspirant active ingredient" refers to the amount of the antiperspirant active ingredients that provides the therapeutic and/or cosmetic effect after its application on the skin (that is an antiperspirant and/or deodorant effect).
The term "antiperspirant" active ingredient refers to any compound having antiperspirant activity. Appropriate antiperspirant active ingredients for the present invention may include astringent metallic salts, especially inorganic and organic salts of aluminium, zirconium and zinc, and mixture thereof. Even more specifically, the antiperspirant active ingredients may include aluminium-containing and/or zirconium-containing salts or materials, such as, for example, aluminium halides, aluminium chlorohydrate, aluminium hydroxy halides, zirconyl oxyhalides, zirconyl hydroxy halides, and mixtures thereof.
In an embodiment, the antiperspirant active ingredient is at least an aluminium-containing salt of formula:
AI2(0H)aClb.xH20 wherein: a is comprised from 2 to 5; the sum of a and b is 6; x is comprised from 1 to 6; and a, b, and x is selected from the group consisting of an integer or a non-integer value.
In an embodiment, the antiperspirant active ingredient is a zirconium salt of formula:
Zr0(0H)2-aCia.xH20, wherein: a is comprised from 1.5 to 1.87; x is comprised from 1 to 7; and a and x is selected from the group consisting of an integer or a non-integer value.
Examples of aluminium-containing salts appropriate for the present invention include, but are not limited to, hydrated aluminium chloride ([AI2(OH) 5CI] nH20), hydrated sesquihydrate chloride alumina ([AI2(OH) 4.5CI1 5] nH20), dihydrochloride hydrated alumina ([AI2(OH) 4CI2] nH20), hydrogen chloride hydrated alumina (aluminium-containing salt chlorohydrex) propylene glycol (PG) or polyethylene glycol (PEG) ([AI2(OH) 5CI] nH20 + CH3CHOHCH2OH or H (OCH)2(CH2)2OH), hydrated aluminium sesqui hydrogen chloride PG or PEG, aluminium PG or hydrated dihydrochloride PEG, hydrated aluminium hydroxide (AI(OH) 3nH20), aluminium hydroxide, aluminium chloride, aluminium potassium, chlorine hydrate aluminium glycine and calcium
chloride; zirconium chloride hydrated salt, such as hydrated aluminium zirconium trichlorosilane ([A eZr (OH) 12.4013] nH20), hydrated aluminium hydroxide, zirconium tetrachloride ([AI3 6Zr (OH) H.6CI32] nH20), pentachlorophenol hydrated zirconium hydroxide ([AlsZr (OH) 23Cls] nH20), eight chlorine hydrate zirconium hydroxide ([AlsZr (OH) 2(C¾] hH2q), hydrated trichlorosilane aluminium zirconium glycine ([AI3.8Zr (OH) 12.4013] nH20 + H2NCH2COOH), hydrated zirconium tetrachloride glycine aluminium hydroxide, hydrated zirconium glycine pentachlorophenol aluminium hydroxide, aluminium hydroxide, chlorine hydrate eight zirconium glycine, aluminium sulfate potassium salt (KAI (SO4) 21 2H2O), aluminium undecylenoyl collagen amino acids, aluminium lactate + aluminium sulfate (Ah(S04)3 + Na2HAI (OOCCHOHCH3)2- (OH) 6), glycolic acid chloride sodium aluminium bromide, aluminium sesquichlorohydrate, aluminium hydroxide, hydrated (AhBr (OH) 5nH20), hydrated aluminium (AICI36H2O) chloride, complex compound of zinc and sodium, lanthanum and cerium complexes and fatty acids aluminium-containing salt.
In an embodiment, the antiperspirant active ingredient is selected from the group consisting of aluminium halo hydrate, aluminium-zirconium halo hydrate, aluminium nitro hydrate compounds and mixture thereof. In an embodiment, the antiperspirant active ingredient is hydrated aluminium chloride ([Ah(OH) 5CI] nH20), optionally with glycine and calcium chloride.
In an embodiment, the water-in-oil emulsion comprises from 20 to 60% by weight of one or more antitranspirant active ingredients; particularly an aluminium-containing salt. In an embodiment, the water-in-oil emulsion comprises from 40 to 55% by weight of one or more antitranspirant active ingredients; particularly an aluminium-containing salt. In an embodiment, the water-in-oil emulsion comprises from 20 to 60% by weight of hydrated aluminium chloride; particularly from 40 to 55% by weight.
Furthermore, the water-in-oil emulsion composition of the first aspect of the invention comprises (b) one or more film-forming agents disclosed herein. For the purpose of the present invention, the term "film-forming agent" refers to a compound capable of building a thin layer covering the area of application, for example within the armpit skin area. The water-in-oil emulsion composition of the first aspect of the invention comprises: (b) one or more film-forming agents selected from the group consisting of capryloyl glycerine/sebacic acid copolymer; polyester-7 (and) neopentyl glycol diheptanoate; ethylcellulose (and) diisopropyl adipate; VP/acry I ates/l au ry I methacrylate copolymer; VP/eicosene copolymer; triacontanyl PVP; and pentylene glycol (and) shellac. In an embodiment, the water-in-oil emulsion composition of the invention comprises (b) at least capryloyl glycerine/sebacic acid copolymer as the film-forming agents. For the purpose of the present invention the term "capryloyl glycerine/sebacic acid copolymer” is the I NCI name of a copolymer of capryloyl glycerine and sebacic acid monomers, which has the CAS number 1190099-88-7.
In an embodiment, the water-in-oil emulsion comprises from 0.1 to 10% by weight of one or more film-forming agents as disclosed in the present application; particularly capryloyl glycerine/sebacic acid copolymer. In an embodiment, the water-in-oil emulsion comprises from 1 to 5% by weight of one or more film-forming agents
as disclosed in the present application; particularly capryloyl glycerine/sebacic acid copolymer.
All the film-forming agents disclosed herein are commercially available. The name of the commercial product is herein disclosed: capryloyl glycerine/sebacic acid copolymer (LEXFILM SUN NATURAL); polyester-7 (and) neopentyl glycol diheptanoate (LEXFILM SUN); ethylcellulose (and) diisopropyl adipate (ANTARON™ ECO GEL); VP/acry I ates/l au ry I methacrylate copolymer (ANTARON™ SENSORY POLYMER); VP/eicosene copolymer (ANTARON™ V-220 POLYMER); triacontanyl PVP (ANTARON™ WP-660 POLYMER); and pentylene glycol (and) shellac (ACTISHELL WR).
Furthermore, the water-in-oil emulsion composition of the first aspect of the invention comprises (c) one or more emollients disclosed herein. The term "emollient” refers to a substance that makes something soft, and for the purpose of the invention, is capable of soften skin. The water-in-oil emulsion composition of the first aspect of the invention comprises (c) one or more emollient selected from the group consisting of dicaprylyl ether; PPG-14 butyl ether; triheptanoin (and) (C13-C16) isoparaffin; heptyl undecylenate (and) (C13-C15) alkane; triheptanoin (and) (C13-C15) alkane; diisooctyl succinate; neopentyl glycol diheptanoate; diheptyl succinate; isododecane; dipropylheptyl carbonate; caprylyl caprylate/caprate; propylheptyl caprylate; cetearyl isononanoate; undecane (and) tridecane; (Ci2-Cis)alkyl benzoate, dibutyl adipate; coco-caprylate; dicaprylyl carbonate; PPG-15 stearyl ether; coco-caprylate/caprate; caprylic/capric triglyceride; cocoglycerides; and isopropyl palmitate. In an embodiment, the water-in-oil emulsion composition of the invention comprises (c) at least one of the emollients selected from the group consisting of dicaprylyl ether and PPG-14 butyl ether. In an embodiment, the water-in-oil emulsion composition of the invention comprises (c) a mixture of dicaprylyl ether and PPG-14 butyl ether as emollients. For the purpose of the invention, the term "dicaprylyl ether” is the I NCI name of dioctyl ether, 1-octoxyoctane which has the CAS number 629-82-3. And, the term "PPG-14 butyl ether” is the I NCI name of polypropylene glycol monobutyl ether being 14 the number of units of propylene glycol having the CAS number 9003-13-8.
In an embodiment, the water-in-oil emulsion comprises from 12 to 40% by weight of at least one of the emollients disclosed in the present application; particularly at least one selected from dicaprylyl ether, PPG-14 butyl ether and a mixture thereof. In an embodiment, the water-in-oil emulsion composition of the invention comprises (c) a mixture of dicaprylyl ether and PPG-14 butyl ether; particularly from 10 to 30% by weight of dicaprylyl ether and from 2 to 10% by weight of PPG-14 butyl ether. In an embodiment, the water-in-oil emulsion comprises from 20 to 30% by weight of at least one of the emollients disclosed in the present application; particularly at least one selected from dicaprylyl ether, PPG-14 butyl ether and a mixture thereof.
In an embodiment, the water-in-oil emulsion composition of the invention comprises (c) a mixture of dicaprylyl ether and PPG-14 butyl ether as emollients; particularly from 18 to 26% by weight of dicaprylyl ether and from 3 to 7% by weight of PPG-14 butyl ether
All the emollients disclosed herein are commercially available. The name of the commercial product are herein disclosed: dicaprylyl ether (CETIOL OE); PPG-14 butyl ether (TEGOSOFT PBE); triheptanoin (and) (C13-C16) isoparaffin (LEXFEEL WOW); heptyl undecylenate (and) (C13-C15) alkane (LEXFEEL WOW-A DT); triheptanoin (and) (C13-C15) alkane (LEXFEEL WOW A); diisooctyl succinate (SUSTOLEO DCS); neopentyl glycol diheptanoate (LEXFEEL 7); diheptyl succinate (LEXFEEL N50 MB); isododecane (CREASIL® ID JSQI); dipropylheptyl carbonate (CETIOL 4 ALL); caprylyl caprylate/caprate (CETIOL RLF); propylheptyl caprylate (CETIOL SENSOFT); cetearyl isononanoate (CETIOL SN); undecane (and) tridecane (CETIOL ULTIMATE); (Ci2-Ci5)alkyl benzoate (CETIOL AB), dibutyl adipate (CETIOL B); coco-caprylate (CETIOL C5); dicaprylyl carbonate (CETIOL CC); PPG-15 stearyl ether (CETIOL E); coco-caprylate/caprate (CETIOL LC); caprylic/capric triglyceride (MYRITOL 318); cocoglycerides (MYRITOL 331); and isopropyl palmitate (WAGLINOL 6016).
In an embodiment, the water-in-oil emulsion composition of the invention comprises:
(a) at least one of the antiperspirant active ingredients is an aluminium containing salts; (b) at least one of the film-forming agents is capryloyl glycerine/sebacic acid copolymer; and
(c) at least one of the emollients is selected from the group consisting of dicaprylyl ether and polypropylene glycol butyl ether
In an embodiment, the water-in-oil emulsion composition of the invention comprises: (a) from 20 to 60 % by weight of one or more antiperspirant active ingredients;
(b) from 0.1 to 10 % by weight of one or more film-forming agents; and
(c) from 12 to 40 % by weight of one or more emollient; being the sum of the components up to 100% by weight. In an embodiment, the water-in-oil emulsion composition of the invention comprises:
(a) from 40 to 55 % by weight of one or more antiperspirant active ingredients;
(b) from 1 to 5 % by weight of one or more film-forming agents; and
(c) from 20 to 30 % by weight of one or more emollient; being the sum of the components up to 100% by weight.
As it is mentioned above, the water-in-oil emulsion composition of the invention comprises one or more (d) pharmaceutically or cosmetically acceptable excipients or carriers. The term "pharmaceutically acceptable” refers to that excipients or carriers suitable for use in the pharmaceutical technology for preparing compositions with medical use. And the terms "cosmetically acceptable” or "dermatological acceptable” have the same meaning and which are herein used interchangeably. They refer to that excipients or carriers suitable for use in contact with human skin without undue toxicity, incompatibility, instability, allergic response, among others. The excipients or carriers used have affinity for the skin, are well tolerated, stable, and are used in an amount adequate to provide the desired consistency, and ease application. The appropriate
excipients and/or carriers, and their amounts, can readily be determined by those skilled in the art according to the type of formulation being prepared to provide the desired consistency and ease application
Examples of appropriate excipients or carriers can include, but not limited to, surfactant, vehicle, preservative, propellant, pH-regulating agent, stabilizing agents, viscosity agent, skin conditioning agent, antioxidant and mixture thereof.
The term "surfactant” refers to a material which lowers the surface tension of a liquid and the interfacial tension between two liquids, allowing their easier spreading. Surfactants have a hydrophilic head that is attracted to water molecules and a hydrophobic tail that repels water and simultaneously attaches itself to oil and grease in dirt. These opposing forces loosen the dirt and suspend it in the water, having the ability to remove it from surfaces such as the human skin, textiles, and other solids, when surfactants are dissolved in water. Examples of appropriate surfactant agents include, but are not limited to, non-ionic surfactants, cationic surfactants, amphoteric surfactants, zwitterionic surfactants, and mixtures thereof. Examples of specific surfactants appropriate for the present invention include, but are not limited to, polyglyceryl-4 diisostearate/ polyhydroxystearate/sebacate, hydrogenated castor oil, polyoxyethylene 2 stearyl ether, polyoxyethylene 20 stearyl ether, and mixture thereof; particularly polyglyceryl-4 diisostearate/ polyhydroxystearate/sebacate (I SOLAN GPS). If present, the amount of surfactant in the compositions of the present invention is from 1% to 8% by weight; particularly from 2 to 5% by weight.
In an embodiment, the water-in-oil emulsion composition of the invention comprises an emulsifying system having a hydrophile lipophile balance (HLB) from 1 to 9. For the purpose of the invention the term "emulsifying system” encompasses either one or more surfactants having each of them a HLB from 1 to 9; or a mixture of surfactants having the mixture a HLB from 1 to 9. In an embodiment, the water-in-oil emulsion composition of the invention comprises from 2 to 5% by weight of an emulsifying system having a hydrophile lipophile balance (HLB) from 1 to 9; particularly selected from those mentioned above.
The term "vehicle” refers to a substance that facilitates the use of the active ingredients mixed with it. Examples of vehicles include, but are not limited to, water, glycols such as propylene glycol and butylene glycol; alcohols such as ethanol and isopropanol; particularly water.
The term "preservative" refers to a material that prevents or reduces or slows down microbial growth, providing that the stability of the emulsion is not affected. Examples of appropriate preservative agents include, but are not limited to, benzoic acid, butylparaben, ethylparaben, propylparaben, methylparaben, sorbic acid, potassium sorbate, sodium benzoate, potassium sorbate, phenoxyethanol, triclosan, or their mixtures. If present, the amount of the preservatives in the compositions of the present invention is from 0.2 to 3% by weight.
The composition of the present invention can be in form of spray optionally comprising one or more propellants. The term "propellant" refers to one or more gases that are used to pressurize the composition to facilitate the pulverization of the composition from the container. Some propellants may be a mixture of gases (e.g., A-46 which is a mixture of isobutane, butane and propane). A propellant may be in the form of a liquid (i.e., a liquefied gas) when under pressure within the reservoir of a spray device. In addition, a propellant may be in its gaseous state within the head space of the reservoir. A propellant may be present in both a liquefied form and its gaseous state within the reservoir. Unless specified otherwise (e.g., liquid propellant or gaseous propellant), the term propellant is intended to encompass the liquefied form and the gaseous state individually and collectively. Example of appropriate propellant include, but are not limited to, compressed air, nitrogen, inert gases, carbon dioxide, and mixtures thereof. Propellants may also include gaseous hydrocarbons like propane, n-butane, isobutane, isobutene, cyclopropane, and mixtures thereof. Halogenated hydrocarbons like 1 , 1 -difluoroethane may also be used as propellants. Some non-limiting examples of propellants include 1,1,1 ,2,2-pentafluoroethane, 1,1, 1 ,2-tetrafluoroethane, 1,1, 1 ,2,3,3,3-heptafluoropropane, trans-1 ,3,3,3- tetrafluoroprop-1-ene, dimethyl ether, dichlorodifluoromethane (propellant 12), 1 , 1-dichloro-1 , 1,2,2- tetrafluoroethane (propellant 114), 1 -chloro-1 , 1 -difluoro-2,2-trifluoroethane (propellant 115), 1-chloro-1,1- difluoroethylene (propellant 142B), 1,1 -difluoroethane (propellant 152A), monochlorodifluoromethane, and mixtures thereof. Some other propellants suitable for use include, but are not limited to, A-46 (a mixture of isobutane, butane and propane), A-31 (isobutane), A-17 (n-butane), A-108 (propane), AP70 (a mixture of propane, isobutane and n-butane), AP40 (a mixture of propane, isobutene and n-butane), AP30 (a mixture of propane, isobutane and n-butane), 152A (1,1 difluoroethane), and PROPEL-45 (a mixture of isobutane, propane and butane). If present, the amount of the propellant is from 70 to 90% by weight. In an embodiment, the water-in-oil emulsion composition of the invention is in form of spray, and optionally further comprises one or more propellants.
The term "thickening agent” or "thickener” or "viscosity agent” which is herein used interchangeably refers to a material that increases its viscosity without substantially modifying its other properties. Appropriate thickener includes, but are not limited to, natural and synthetic or semi-synthetic thickeners which derive from various sources and consist of very different molecular structures including polysaccharides, proteins and alcohols. Examples of appropriate thickener include cetyl alcohol, stearyl alcohol, stearic acid, and cellulose derivatives such as hydroxyethylcellulose, guar gum, locust bean gum, xanthan gum, and gelatine. If present, the amount of the viscosity agent is from 0.1 to 10% by weight.
The term "stabilizing agent" refers to a substance that improves stability of the liquid formulation. Examples of appropriate preservative agents include, but are not limited to, sodium chloride, magnesium dichloride, magnesium sulfate or mixtures thereof. If present, the amount of stabilizing agent is from 0.1 to 5% by weight.
The term "skin conditioning agent” refers to a substance that increase the water content of the top layers of the skin and/or give the skin a soft and smooth appearance. Examples of appropriate skin conditioning agent
agents can include, but are not limited to, esters of glycerine and C15-C25 fatty acid such as glyceryl oleate; C15-C25 fatty alcohol such as lauryl alcohol, myristyl alcohol, palmityl alcohol, stearyl alcohol, linoleyl alcohol, and oleyl alcohol; diols such as propyleneglycol, propanediol, 1,2-hexanediol, ethylhexylglycerine, glycerol, propylene glycol, butylene glycol, pentylene glycol, hexylene glycol, and dipropylene glycol or diethylene glyco. If present, the amount of skin conditioning agent is from 0.1 to 10% by weight.
The terms "pH regulating agent” and "buffer” and "buffering agent” have the same meaning and are used interchangeable. They refer to a substance that active adjust and regulates the pH value of a solution to which they have been added. Examples of pH regulating agents can include, but are not limited to, strong acids (i.e., acids that are completely dissociated in aqueous solution) and strong bases (i.e., bases that are completely dissociated in aqueous solution), acidic buffering agents and alkaline buffering agents, and nicotine. If present, the amount of pH regulating agent is from 0.1 to 1% by weight.
The term "antioxidant” refers to any substance that delays or prevents the oxidation of any oxidizable component of the emulsion, such as for example fatty or oil components. Examples of antioxidants can include, but are not limited to, vitamin C, vitamin E such as tocopheryl acetate, vitamin A, niacinamide, butylated hydroxy-toluene (BHT), butylated hydroxyanisol (BHA) and mixture thereof. If present, the amount of antioxidants is from 0.05 to 1% by weight.
As it is mentioned above, the water-in-oil emulsion composition of the present invention can further comprise (e) one or more additional pharmaceutically or cosmetically active ingredients. The presence of additional active ingredients and their amounts, can readily be determined by those skilled in the art according to the type of formulation being prepared to provide the appropriate pharmaceutically or cosmetically effect. Examples of appropriate additional active ingredients can include, but are not limited to, deodorant agents. If present, the amount of additional pharmaceutically or cosmetically active ingredients is from 0.1 to 5%.
The term "deodorant" active ingredient refers to any topical material that is known or otherwise effective in preventing or eliminating malodor associated with perspiration. Suitable deodorant active agents may be selected from the group consisting of antimicrobial agents (e.g., bacteriocides, fungicides), malodor-absorbing material, and mixture thereof. Examples of appropriate deodorants can include, but are not limited to, cetyl- trimethylammonium bromide, cetyl pyridinium chloride, benzethonium chloride, diisobutyl phenoxy ethoxy ethyl dimethyl benzyl ammonium chloride, 2-methyl 5-cyclohexyl pentanol, sodium N-lauryl sarcosine, sodium N-palmethyl sarcosine, lauroyl sarcosine, N-myristoyl glycine, potassium N-lauryl sarcosine, trimethyl ammonium chloride, sodium aluminium chlorohydroxy lactate, triethyl citrate, tricetylmethyl ammonium chloride, 2,4,4'-trichloro-2'-hydroxy diphenyl ether, 3,4,4'-trichlorocarbanilide, diaminoalkyl amides such as L- lysine hexadecyl amide, heavy metal salts of citrate, salicylate, and piroctose, especially zinc salts, and acids thereof, heavy metal salts of pyrithione, especially zinc pyrithione, zinc phenolsulfate, farnesol,
ethylhexylglycerine and mixture thereof. If present, the amount of deodorant active ingredients is from 0.1% to 1% by weight.
In an embodiment, the water-in-oil emulsion composition of the invention comprises: (a) from 20 to 60 % by weight of one or more antiperspirant active ingredients, particularly aluminium containing salts;
(b) from 0.1 to 10 % by weight of one or more film-forming agents, particularly capryloyl glycerine/sebacic acid copolymer;
(c) from 12 to 40 % by weight of one or more emollient, particularly dicaprylyl ether, PPG-14 butyl ether and a mixture thereof;
(d) from 0 to 8% by weight of surfactants, particularly polyglyceryl-4 diisostearate/ polyhydroxystearate/Sebacate; from 0 to 3% by weight of preservatives; from 0 to 5% of stabilizing agent; from 0 to 10% of skin conditioning; and
(e) from 0 to 5% by weight of additional active ingredients; being the sum of the components up to 100% by weight.
In an embodiment, the water-in-oil emulsion composition of the invention comprises: (a) from 20 to 60 % by weight of one or more antiperspirant active ingredients, particularly aluminium containing salts;
(b) from 0.1 to 10 % by weight of one or more film-forming agents, particularly capryloyl glycerine/sebacic acid copolymer;
(c) from 12 to 40 % by weight of one or more emollient, particularly dicaprylyl ether, PPG-14 butyl ether and a mixture thereof;
(d) from 1 to 8% by weight of surfactants, particularly polyglyceryl-4 diisostearate/ polyhydroxystearate/Sebacate; from 0.1 to 3% by weight of preservatives; from 0.1 to 3% of stabilizing agent; from 0.1 to 10% of skin conditioning; and
(e) from 0.1 to 1% by weight of deodorant active ingredients; being the sum of the components up to 100% by weight.
In an embodiment, the water-in-oil emulsion composition of the invention comprises: (a) from 40 to 55 % by weight of one or more antiperspirant active ingredients, particularly aluminium containing salts;
(b) from 1 to 5 % by weight of one or more film-forming agents, particularly capryloyl glycerine/sebacic acid copolymer;
(c) from 20 to 30 % by weight of one or more emollient, particularly dicaprylyl ether, PPG-14 butyl ether and a mixture thereof;
(d) from 0 to 5% by weight of surfactants, particularly polyglyceryl-4 diisostearate/ polyhydroxystearate/Sebacate; from 0 to 3% by weight of preservatives; from 0 to 3% of stabilizing agent; from 0 to 6% of skin conditioning; and
(e) from 0 to 5% by weight of additional active ingredients; being the sum of the components up to 100% by weight.
In an embodiment, the water-in-oil emulsion composition of the invention comprises:
(a) from 40 to 55 % by weight of one or more antiperspirant active ingredients, particularly aluminium containing salts;
(b) from 1 to 5 % by weight of one or more film-forming agents, particularly capryloyl glycerine/sebacic acid copolymer;
(c) from 20 to 30 % by weight of one or more emollient, particularly dicaprylyl ether, PPG-14 butyl ether and a mixture thereof;
(d) from 2 to 5% by weight of surfactants, particularly polyglyceryl-4 diisostearate/ polyhydroxystearate/Sebacate; from 0.1 to 3% by weight of preservatives; from 0.1 to 3% of stabilizing agent; from 0.1 to 6% of skin conditioning; and
(e) from 0.3 to 1% by weight of deodorant active ingredients; being the sum of the components up to 100% by weight.
In an embodiment, the water-in-oil emulsion composition of the present invention is a topical pharmaceutical or cosmetic composition comprising one or more appropriate topical pharmaceutically or cosmetically acceptable excipients or carriers. The topical water-in-oil emulsion compositions of the invention can be formulated in several forms that include, but are not limited to, creams, stick, roll-on, spray, soft solids, gels, mousses, ointments and pastes. In an embodiment, the topical water-in-oil emulsion composition of the present invention is in form of a spray, optionally the composition further comprises one or more propellants as defined above. In an embodiment, the topical water-in-oil emulsion composition of the present invention is in form of a spray, and the composition further comprises one or more propellants as defined above. Additionally, the composition of the present invention may contain other ingredients, such as fragrances, colorants, and other components known in the state of the art for use in topical formulations.
In an embodiment, the composition of the present invention is "substantially free” of silicones. For the purpose of the invention, the terms "silicone”, "polymerized siloxanes” and "polysiloxanes” have the same meaning and are used interchangeable. They refer to an inorganic silicon-oxygen backbone chain (-Si-0— Si-O— Si-O— ) with two organic groups attached to each silicon atom. Commonly, the organic groups are alkyl moieties, particularly methyl. The silicones can be cyclic or lineal; and straight, or branched (such as cage-like). By varying the -Si-O- chain lengths, side groups, and crosslinking, silicones can have a wide variety of consistency (from liquid to gel to rubber to hard plastic), properties and compositions. For the purpose of the invention, the term "silicone” encompasses dimethicone, dimethicone copolyol, stearyl dimethicone, dimethiconol, amodimethicon, cyclomethicone, cetyl dimethicone, behenoxy dimethicone, stearoxy dimethicone, trimethylsilylamodimethicone, lauryl methicone copolyol, hydroxypropyl polysiloxane, phenyl trimethicone, cetearyl methicone, trimethylsiloxysilicate, polydimethylsiloxane, cyclopentasiloxane and cyclosiloxane. For the purpose of the invention, the term "substantially free” refers to a composition comprises less than 1 % by weigth of silicones. In an embodiment, the composition of the invention is "free” of silicones. The term "free of” refers to a composition whose content of silicones. is not detectable by any of the commonly used techniques defined in the state of the art. For the purpose of the invention, the method for determining the content of ion silicones can be gas chromatography coupled to mass spectrometry. In an embodiment, the composition of the invention is "substantially free” or "free” of silicones.
It is also a part of the invention a process for the preparation of the water-in-oil emulsion composition of the present invention. The appropriate process can readily be determined by those skilled in the art from those disclosed in the state of the art according to the type of formulation being prepared. Typically, the process for the preparation of emulsions comprises: (i) firstly, preparing the aqueous phase(s) and the oil phase separately; and (ii) secondly, mixing both phases until obtaining the water-in-oil-emulsion as it is shown in the experimental section.
By way of illustration, the water-in-oil emulsion composition can be prepared following the general process as defined herein below:
(i) Preparing Phase A by mixing the emollients, the film-forming agents and optionally the surfactants, additional active ingredients (such as deodorant active ingredients) and fragrances.
(ii) Preparing Phase B by mixing the antiperspirant active ingredients, and optionally the stabilizing agents, with water.
(iii) Optionally, preparing Phase C by mixing the preservatives, skin conditioning agents, antioxidants and additional active ingredients.
(iv) mixing Phase A and Phase B; and
(v) optionally mixing the resulting mixture of step (iv) with Phase C.
The water-in-oil emulsion of the present invention can be defined by its preparation process. Thus, a water-in- oil emulsion composition of the first aspect of the invention obtainable by the process as defined above is also
part of the invention. For the purposes of the invention the expressions "obtainable", "obtained" and equivalent expressions are used interchangeably, and in any case, the expression "obtainable" encompasses the expression "obtained". All the embodiments disclosed above for the process of the invention applies also for water-in-oil emulsion composition obtainable by this process.
It is also part of the invention a water-in-oil emulsion composition for use in therapy, with the proviso that the composition comprises: a therapeutically effective amount of one or more antiperspirants, and pharmaceutically acceptable excipients or carriers. In an embodiment, the water-in-oil emulsion composition of the invention is useful for the prophylaxis and/or treatment of a disease or condition which involves an excessive or abnormal perspiration. Disease or conditions which involve an excessive or abnormal perspiration include hyperhidrosis, chromhidrosis and bromhidrosis. This aspect could be also formulated as the use of water-in-oil emulsion composition as defined above for the preparation of a medicament for the prophylaxis and/or treatment of a disease or condition which involves an excessive or abnormal perspiration.
It also relates to a method for the prophylaxis and/or treatment of a mammal suffering or is susceptible to suffer from a disease or condition which involves an excessive or abnormal perspiration, the method comprises administering to said mammal an effective amount of a water-in-oil emulsion composition of the present invention.
The water-in-oil emulsion composition of the invention can be used for reducing the normal perspiration of the skin. Thus, another aspect of the present invention is a water-in-oil emulsion composition of the invention as defined above in cosmetic; particularly as an antiperspirant agent and a deodorant agent. Then, the composition comprises: a cosmetically effective amount of antiperspirant active ingredients, and cosmetically acceptable excipients or carriers. The topical cosmetic water-in-oil emulsion composition of the invention reduces the extent of sweating, the occurrence of unsightly sweat marks on clothing as well as minimizing body odour. Besides, the water-in-oil emulsion composition also allows strengthen and moisturizing the skin. The topical cosmetic composition of the present invention is designed to apply to the body to improve its appearance or to beautify, preserve, cleanse and protect the skin. Therefore, the above cosmetic compositions are adjectivally used for a non-medical application. Throughout the description and claims the word "comprise" and variations of the word, are not intended to exclude other technical features, additives, components, or steps. Furthermore, the word "comprise” encompasses the case of "consisting of. Additional objects, advantages and features of the invention will become apparent to those skilled in the art upon examination of the description or may be learned by practice of the invention. The following examples are provided by way of illustration, and they are not intended to be limiting of the present invention. Furthermore, the present invention covers all possible combinations of particular and preferred embodiments described herein.
Examples
1. Water-in-oil emulsion compositions
1.1. Water-in-oil emulsion composition in form of spray of the present invention (Example 1)
1.1.1. Composition
This example illustrates a water-in-oil-emulsion composition in form of spray (Spray 1) in accordance with the present invention. Table 1 shows the qualitive and quantitative composition of the water-in-oil emulsion (Emulsion 1) forming part of the spray of the present invention.
Table 1
(a) It corresponds to 15% by weight of the aluminium chlorohydrate antiperspirant active ingredient
And, Table 2 shows the qualitive and quantitative composition of the water-in-oil spray composition (Spray 1) of the present invention containing the water-in-oil emulsion composition (emulsion 1) disclosed in Table 1.
Table 2
1.1.2. Preparation process Water-in-oil emulsion 1 (emulsion 1)
The water-in-oil emulsion 1 was prepared at room temperature following the process disclosed herein below:
1. Preparation of Phase A. Phase A ingredients were mixed one by one under stirring in a first reactor.
2. Preparation of Phase B. In a separate second reactor, all ingredients of Phase B were mixed one by one under stirring.
3. Preparation of emulsion. Phase B was added to Phase A with high-shear mixer and the resulting mixture was stirred for 25 minutes. Then, all Phase C ingredients one by one were added to the resulting mixture (i.e., phase A+B) under stirring.
Water-in-oil emulsion spray composition 1 (Spray 1)
The water-in-oil emulsion spray composition 1 of the present invention disclosed in Table 2 was prepared following the process disclosed herein below.
The water-in-oil emulsion 1 was loaded into a container and charged with 85% by weight of the propellant mixture.
1.2. Comparative water-in-oil emulsion spray composition falling outside the scope of the present invention (Comparative Example 1)
1.2.1. Composition
This example illustrates a comparative water-in-oil emulsion composition in form of spray (Comparative Spray 1) falling outside the scope of the present invention because the water-in-oil emulsion does not contain any film-forming agent. Table 3 shows the qualitive and quantitative composition of the comparative water-in-oil emulsion (Comparative Emulsion 1) forming part of the comparative spray 1 falling outside of the present invention.
(a) It corresponds to 15% by weight of the aluminium chlorohydrate antiperspirant active ingredient
And, Table 4 shows the qualitive and quantitative composition of the comparative water-in-oil spray composition (comparative Spray 1) falling outside the scope of the present invention containing the comparative water-in-oil emulsion composition (comparative emulsion 1) disclosed in Table 3.
Table 4
Preparation process
Comparative Water-in-oil emulsion 1 (comparative emulsion 1)
The comparative water-in-oil emulsion 1 was prepared following the same process as defined above for the water-in-oil emulsion 1 using the ingredients and amounts disclosed in Table 3, which implies that the film forming agent is not incorporated to the emulsion.
Comparative Water-in-oil emulsion spray composition 1 (comparative Spray 1)
The comparative water-in-oil emulsion spray composition 1 was prepared following the same process as defined above for the water-in-oil emulsion spray composition 1 using the ingredients and amounts disclosed in Table 4.
2. Antiperspirant Activity
2.1. In-vivo antiperspirant effect evaluation
The aim of this study was the evaluation of the antiperspirant efficacy of the composition of the present invention (Emulsion 1) by the olfactory evaluation of the corporal odor by trained examinators. 20 volunteers were recruited and the olfactory evaluation was performed at Oh, 24h and 48h after a unique application of two spray doses in the armpit at a distance of 10-15cm. The study has been carried out under medical responsibility, in accordance with the relevant experimental protocol and following the standards of Good Clinical Practice in its corresponding sections.
Volunteers selection
Study participants were selected according to the following inclusion and exclusion criteria:
Inclusion criteria
The most important inclusion criteria, defined in the protocol, were as follow:
- Age: 18-65 years old
- Sex: both
- regular users of spray deodorants
- Adequate cultural level and understanding of the clinical study on the part of the participants.
- Agreement to voluntary participation and written informed consent.
Non-inclusion criteria The specific non-inclusion criteria, defined in the protocol, were as follow:
- acute or chronic pathologies at the moment of starting the study or within 3 weeks before the study.
- Pathologies in the experimental area within 3 weeks before the study.
- Treatment with any medicine.
- pregnant or breastfeeding women - Allergies to the components of the composition of the invention
- no users of spray deodorants
- Adequate cultural level and understanding of the clinical study on the part of the participants.
- Agreement to voluntary participation and written informed consent. The volunteers should follow these recommendations:
- do not apply any cosmetic product in the experimental area.
- do not vaccine during the study
- do not shave or waxing the armpits within 72 hours before the study
- do not expose to intense sun radiation within 1 week before the study and during the study.
Experimental procedure
Method of use:
1. Shake the spray before use
2. applying the composition of the invention (Spray 1) in the right armpit; and applying the common use invisible spray of the state of the art falling outside the scope of the invention as comparative test in the left armpit.
3. Spraying twice on each armpit, keeping the spray at 10-15 cm.
The olfactory evaluation took place for 45 hours. Selection phase
Before including the participants in the study, the participants were given the Participant Information Sheet and once they had understood everything about the study, they gave their written informed consent for their participation.
The principal investigator examined and interviewed each of the participants prior to the start of the experimental phase to collect information regarding their personal and demographic data and to complete their medical history, with special emphasis on aspects related to axillary health. The researcher also verified that the participants met all the inclusion criteria and none of the exclusion criteria.
The study involves the following visits:
- Day 0 (Baseline) (DO/TO)
After verifying that the informed consent form had been signed, the researcher confirmed that the participants met all the inclusion criteria and none of the exclusion criteria and gave them the product containers, explained the mode of use and the recommendations to be followed during the study. The volunteer washed its armpits with sponges impregnated of neutral soap without parfum. The research made the olfactory evaluation in both armpits and the composition of the invention at the right armpit was applied. The volunteers were asked to return to the consultation after 24h.
- Day 1 (at 24h after application) (D1/T24)
The research made the olfactory evaluation in both armpits and a side effects register, if any.
- Day 2 (at 48h after application) (D2/T48) The research made the olfactory evaluation in both armpits and a side effects register, if any.
Results
Body odor was assessed using an ordinal scale from 0 to 10:
0= very pleasant smell 5= neutral smell and
10= very unpleasant smell.
The corporal smell at day 0 should be about neutral smell.
Absolute values The average results of the smell punctuation are shown in Table below, as well as the number and percentage of "reactive” volunteers:
Statistical values The statistical analysis (test t of Student for paired series) of the results shows a great significant difference between the statistical control area and the treated area at any experimental time after the application of the composition of the present invention.
The results obtained after the statistical treatment using a parametric test, t-student test (p <0.05, 95% Cl) allows concluding that that there were significant differences between the control area and the treated area with the composition of the present invention in all experimental times (that is T24H and T48H).
Average percentage of antiperspirant efficacy
The average results are shown in table below:
Conclusion
The analysis of individual results expressed in percentage of antiperspirant efficacy at each experimental time shows a VERY GOOD antiperspirant effect at 24hours after application of the composition of the present invention, with a 65% of average efficacy. Further, a GOOD antiperspirant effect at 48hours after application of the composition of the present invention was observed with a 53% of average antiperspirant effect.
2.2. In-vitro comparative antiperspirant effect evaluation (Burst pressure Test)
The aim of this test is to determine the ultimate pressure resistance. In particular, the measurement of the ultimate pressure resistance for breaking the clot (film) obtained after the application of the composition of the present invention on the armpit skin allows deducing the efficiency of the antiperspirant composition. The test was performed with the composition of the present invention (Emulsion 1) and the comparative emulsion 2 (without a film-forming agent) falling outside of the scope of the present invention using the SOD4 instrument.
Materials and Methods
The SOD4 machine is designed to test the efficiency of antiperspirant formulations. The machine is a fully automated biomimetic system that imitates the sweating process. It allows recreating the contact between the sweat and the antiperspirant, to observe the reaction inside the transparent mimetic pores. When it creates a clot, it is possible to characterize the resistance of the clot and deduce the efficiency of the antiperspirant.
To perform that experiment the machine includes:
- Smart-Pore™, a silicone microfluidic chip containing microchannels mimicking skin pores.
- An integrated pressure system controlling the flow of sweat in the pores down to nanolitre precision.
- A climatic chamber regulated in humidity/temperature, reproducing actual perspiration conditions.
- An optical system to monitor and record the evolution of the interaction between the antiperspirant and the
sweat
Artificial sweat used in the present test is as follows:
Sodium Chloride 0.5% Lactic Acid 0.1%
Urea 0.1%
Bovine Serum Albumin 0.1%
Millipore Water Up to 100%
Fluorescein 0.1% Ammonium Hydroxide for having a pH = 6.5
All the ingredients are mixed during the preparation of a sweat batch. After the adjustment of the pH, the solution is filtered and divided in 10ml aliquot that are frozen until use. One aliquot is defrosted each day for the measurements. Although fluorescein is not a component of the human sweat, it is a great help for the visualization of the clogging process. Control experiments showed previously that the fluorescein does not impact the clogging process. This sweat model is known in the state of the art and it is the most simple and non-specific one used in the cosmetic field. It is possible to replace this sweat by a natural one or another formulation of artificial one. Component Quantity
Microfluidics chip: SMART-PORE™
The channel network is composed of 4 independent channels. The wider parts are the inlet channels and measure roughly 500 pm x 60 pm x 10 mm. Each fluidic line finishes with a thin microfluidic channel: the biopore. They are biomimetic channels representing the sweat duct of a human body. They are 60 pm wide, 60 pm high and 2 mm long. These biopores end on a flat surface representing the skin.
Experimental protocol
It is disclosed herein below a summary describing the method used for the tested compositions with an application directly on the surface of the Smart-pore™. The liquid was removed from the recipient and then the propellant present on the spray was also removed. A stencil that had a thickness of 100 pm was used, in order to assured that the quantity of composition is sufficient to react with the sweat and respect the rules imposed by the FDA (2mg /cm2).
Each experiment was performed on a 4-channel Smart-poretm, providing 4 results in parallel. The experiments were performed in a controlled environment where the relative humidity was kept at 80% and 30°C.
The protocol was as follows: Firstly, a new Smart-Pore™ with the artificial sweat was filled. Once the channels were full, the stabilization process of the flow was launched. Then, the hanging drop of sweat was removed to
create "armpit-on-a-chip” conditions and the composition to be tested was applied. The contact between the sweat and the product lasted 1 hour, during which the image of each clot while it was growing was recorded.
During these experiments, the following parameters were measured:
• Coverage Rate (%): at least 20 independent measurements were made. A various number of clot formation was observed. The coverage rate was the ratio between the total clot that has been formed and the total number of sweat channels. This is an indicator of the composition capability to do an homogenous layer.
• The Burst pressure (mbars) that is the average of the maximal pressure applied to push out the clot inside the channel.
• The clot length (pm) that was observed corresponding of the penetration of the composition into the pores.
• The claim estimation (24h/48h/72h/96h): indications about the possible claim associated to each tested composition.
Results
The values of the burst pressure, the coverage rate and the clot length, as well as the antiperspirant claim estimation are summarised herein below:
As it is shown in the results above, the composition of the present invention allows obtaining a bigger clot with a high coverage rate than the comparative composition. Furthermore, the composition of the present invention also has an increase of about 50% in the burst pressure value in comparison with the comparative composition without the film-forming agent. It means that the composition of the present invention is more effective in terms of antiperspirant effect for a prolonged period of time (48h).
Therefore, it is concluded that only the water-in-oil emulsion compositions of the present invention with the specific combination of antiperspirants, film-forming agents and emollients disclosed in the present application allows having an effective and prolonged antiperspirant effect.
3. Use Test
The aim of the use test is the assessment of skin acceptability and safety of the composition of the present invention. The study has been carried out under medical responsibility, in accordance with the relevant
experimental protocol and following the standards of Good Clinical Practice in its corresponding sections.
This study was performed under dermatological control on healthy adult female volunteers. 20 women volunteers were recruited. The study was conducted to verify the absence of discomfort and cumulative irritation reactions (functional and physical signs) associated with the application of the composition of the present invention (Spray 1) under study for 2 weeks, under normal conditions of use. At the end of the study, the assessment made by the participants was collected on the basis of a specific, targeted and adapted questionnaire, making it possible to assess the tolerance of the composition of the present invention under investigation and its acceptability.
Volunteers selection
Study participants were selected according to the following inclusion and exclusion criteria:
Inclusion criteria
- Healthy women. - Aged between 25 and 55 years.
- Volunteers with skin phototypes I to IV.
- Regular users of deodorant spray.
- Adequate cultural level and understanding of the clinical study on the part of the participants.
- Agreement to voluntary participation and written informed consent. Non-inclusion criteria
- Present chronic or acute illness at the time of starting the study or during the 3 weeks prior to the study.
- Present skin pathologies during the 3 weeks prior to the start of the study.
- To be under pharmacological treatment.
- Women with skin marks in the experimental area that could interfere with the evaluation of skin reactions (pigmentation disorders, scars, ephelides and nevi in quantity, sunburn, etc.).
- Women with allergy to any of the components of the composition of the invention under study.
- Having had any vaccination within the 3 weeks prior to the study.
- Pregnant or lactating women.
- Women who are not users of deodorant sprays.
The volunteers should follow these recommendations:
- Do not apply cosmetic products (other than the one tested) on the experimental area.
- Do not expose to extensive solar radiation for 1 week before the test. Experimental procedure
Method of use:
Shake the spray of the invention (Aerosl 1) before use. Spray two seconds on the right armpit, keeping the spray at 10-15 cm.
Selection phase
Before including the participants in the study, the participants were given the Participant Information Sheet and once they had understood everything about the study, they gave their written informed consent for their participation. The principal investigator examined and interviewed each of the participants prior to the start of the experimental phase to collect information regarding their personal and demographic data and to complete their medical history, with special emphasis on aspects related to axillary health. The researcher also verified that the participants met all the inclusion criteria and none of the exclusion criteria. The study involved the following visits:
- Day 0 (Baseline) (DO/TO)
After verifying that the informed consent form had been signed, the researcher confirmed that the participants met all the inclusion criteria and none of the exclusion criteria and gave them the composition of the invention containers, explained the mode of use and the recommendations to be followed during the study. The first application was performed in consultation to confirm the correct use of the composition of the invention, under dermatological control. During the study, the volunteers applied the composition of the present invention under study in the right armpit and their usual deodorant in the left armpit, which will be their own control. They will apply at least one application per day; if they apply more, this will be reflected in the table describing the participating sample in this report.
- Day 7
On day 7 of the study, they visited the clinic for dermatological evaluation. No incidences were observed in the area of application of the composition of the invention duct under study or in the control area. - Day 14
On the final visit of the study, each participant underwent a dermatological clinical examination and adverse events, if any, were recorded. In addition, participants were asked to complete the subjective evaluation questionnaire of the composition of the invention. Results
Assessment of reactions observed by the participants.
The satisfaction questionnaire completed by the participants was evaluated using 4-point scales:
0= I do not like it at all (Completely disagree)
1= I do not like it (disagree) 2= I like it (agree)
3= I like it very much (Strongly agree)
The results were expressed in % of volunteers satisfied with the composition of the invention (score 2 and 3).
Volunteers were considered satisfied for an item if they answered 2 or 3 and not satisfied if they answered 0 or 1. The ranges for the calculation of the overall satisfaction obtained taking into account all the items of the questionnaire follow the following scheme:
Equal to or higher than 75% of the points for the entire test (Very satisfied)
Equal to 50% and less than 75% of the points for the entire test (Satisfied)
Equal to 25% and less than 50% of the points for the entire test (Poorly satisfied)
Less than 25% of the points for the entire test (Not at all satisfied)
A descriptive analysis of the frequency of reactions considered as undesirable effects related to the composition of the present invention under study observed by the dermatologist and another of the frequency of reactions observed by the participants were carried out.
Results of evaluation of undesirable skin reactions
For the evaluation of undesirable skin reactions, an analysis of the frequency of appearance of these reactions observed by the dermatologist in the participants, after 14 days of use of the composition of the invention under study, was carried out. In addition, the reactions reported by the participants themselves were evaluated.
- Skin reactions observed by the dermatologist: none of the participants included in the study presented undesirable skin reactions after use of the composition of the invention for 14 days.
- Reactions reported by the volunteers:
The researcher consulted the participants about any undesirable reactions observed by them during the study, related or not to the use of the composition of the invention under study. In all cases the answers given by the participants were negative.
Results of product satisfaction survey
During the final visit, and after 14 days of the use of the composition of the invention, the participants were asked to complete a questionnaire on their satisfaction with the composition of the invention and with the subjective efficacy observed after use.
A summary of the evaluation of the composition of the invention is included herein below:
A. General Opinion
- 65% of the participants confirmed that they liked the composition of the invention VERY MUCH and the other 35% LIKED the composition of the invention.
- 60% of the participants confirmed that they liked the composition of the invention spray VERY MUCH and the other 40% LIKED the composition of the invention.
B. Anti perspi rant and deodorant effect
- 80% of the participants FULLY AGREED that the composition of the invention protects 24 hours or until the next application and the remaining 24% AGREED with this statement.
- 90% of the participants FULLY AGREED that the composition of the invention protects against odor, and the remaining 10% AGREED with this statement.
- 65% of the participants FULLY AGREED that the composition of the invention reduces the appearance of sweat and the remaining 65% AGREED with this statement.
B. Cosmeticity - 75% of the participants FULLY AGREED that the composition of the invention dries the armpit skin quickly and the remaining 25% AGREED with this statement.
-85% of the participants COMPLETELY AGREED that the composition of the invention is not sticky and the remaining 15% AGREED with this statement. C. White marks and stain appearance
-100% of the participants FULLY AGREED that the composition of the invention prevents the appearance of stains on clothing.
D. Organoleptic Opinion -10% of the participants completely agreed that the composition of the invention has a pleasant fragrance,
80% agreed and the remaining 10% disagreed with this statement.
-75% of the participants fully agreed that the fragrance lasts all day and the remaining 25% agreed with this statement. E. Skin care
-75% of the participants FULLY AGREED that the composition of the invention CARES for armpit skin and the remaining 25% AGREED with this statement.
- 50% of the participants FULLY AGREED that the composition of the invention strengthens the skin of the armpit and the remaining 50% AGREED with this statement. - 65% of the participants FULLY AGREED that the product keeps the underarm skin moisturized and the remaining 35% AGREED with this statement.
Conclusion
After carrying out the present use test, the following conclusions were obtained: 1. The composition of the present invention did not produce any undesirable skin reaction after 14 days of use, according to the evaluation of the researchers.
2. During the 14 days of the study, no undesirable perceptive reactions were reported by any of the participants.
3. Regarding the subjective assessment of the composition of the present invention, the questionnaire revealed that the overall opinion of the composition of the present invention was positive for 100% of the surveys. Particularly: a. 100% of the participants showed that they were very satisfied or satisfied with the composition of the present invention in general, the spray and the packaging. b. 90% of the participants were satisfied or very satisfied with the overall organoleptic properties, such as for example smell, pleasant fragrance, and with the statement that it is the best they have ever tried. c. 100% of the participants were very satisfied or satisfied with the statement that it protects 24 hours, prevents the appearance of spots, long-lasting fragrance and strengthens the skin. d. 100% of the participants showed to be very satisfied or satisfied with the statement that it protects against odor, reduces the appearance of sweat, dries quickly and is not sticky. e. 100% of the participants stated that it meets their expectations. f. Between 95%-90% of the participants stated that they like it better than their usual product and it is the best they have tried.
4. Further Examples of Water-in-oil emulsion compositions of the present invention
4.1. Water-in-oil emulsion composition in form of spray of the present invention (Examples 2-5)
4.1.1. Compositions comprising aluminium salts as antiperspirant agents These examples further illustrate water-in-oil-emulsion compositions in form of spray (Sprays 2-5) in accordance with the present invention. Table 5 shows the qualitive and quantitative composition of the water- in-oil emulsions (Emulsions 2-5) forming part of the sprays of the present invention.
Table 4
(a) It corresponds to 15% by weight of the aluminium chlorohydrate antiperspirant active ingredient q.s. refers to the sufficient amount of distilled water for achieving 100% by weight of the composition
And, Table 5 shows the qualitive and quantitative composition of the water-in-oil spray compositions (Sprays 2-5) of the present invention containing the water-in-oil emulsion composition (emulsions 2-5) disclosed in
Table 4.
Table 5
The water-in-oil emulsions of Ex. 3-5 were prepared following the preparation process as disclosed in section 1.1.2. using the components disclosed in Table 4. The water-in-oil emulsions of Ex. 2 was prepared following the preparation process as disclosed in section 1.1.2, but heating the resulting mixture of ingredients of phase A at about 65°C before its subsequent mixture with phase B.
Besides, the water-in-oil emulsion spray compositions Ex. 2-5 were also prepared by the process as defined in section 1.1.2 using the water-in-oil emulsions of Ex 2-5.
4.1.2. Compositions comprising Zirconium salts as antiperspirant agents
These examples further illustrate water-in-oil-emulsion compositions in form of spray (Sprays 6-7) in accordance with the present invention. Table 6 shows the qualitive and quantitative composition of the water- in-oil emulsions (Emulsions 6-7) forming part of the sprays of the present invention.
(a) It corresponds to 15% by weight of the aluminium zirconium chloride hydroxide antiperspirant active ingredient q.s. refers to the sufficient amount of distilled water for achieving 100% by weight of the composition
And Table 7 shows the qualitive and quantitative composition of the water-in-oil spray compositions (Sprays 6-7) of the present invention containing the water-in-oil emulsion composition (emulsions 6-7) disclosed in Table 6.
Table 7
The water-in-oil emulsions of Ex. 6-7 were prepared following the preparation process as disclosed in section
1.1.2. using the components disclosed in Table 6. Besides, the water-in-oil emulsion spray compositions Ex. 6-7 were also prepared by the process as defined in section 1.1.2 using the water-in-oil emulsions of Ex 6-7.
4.2. Appearance
4.2.1. Naked eye assessment
The observation of the emulsions of Ex. 2-7 (just after their preparation) was performed at naked eye.
Results: it was confirmed that all the emulsions Ex.1-7 of the present invention were stables water-in-oil emulsions.
4.2.2. Microscopic appearance
The microscopic appearance of the water-in-oil emulsions of Examples 1-7 was determined:
1. With a clean and dry slip, a drop of the emulsion of the invention (Ex. 1 -7) was placed in the center of the slide;
2. Taking care of not to dirty or fill the slip, a coverslip was placed at an angle of about 45° in which one end touches the slip and the sample remains below.
3. Gradually lower the coverslip, avoiding the generation of air bubbles.
4. The resuting slip was placed on the stage of a LEICA DM1000LED microcope;
5. The observation of the sample through it was performed.
The observation was perfomed starting with the objectives of lower magnification, to have a general view and following with increasing in magnification to be able to visualize in detail. All samples were viewed at 40x magnification.
Result: in all the emulsions of the present invention (Ex. 1-7) a stable emulsion formed by an oil continuous phase and a water dispersed phase with a small particle (about 0.2 to 100 pm) size were observed. Therefore, it was concluded that the emulsions of Examples 1-7 were stable water-in-oil emulsions.
4.3. Film-forming properties 4.3.1. Film-forming Test
The aim of the film-forming test was the evaluation of the filmogenous properties of the water-in-oil emulsions of Examples 1-7 of the present invention by the spreader box technique.
Therefore, a film of 30mm and 100mm of thickness were prepared following the method disclosed herein below:
1. selecting the 30 microns gap or 100 microns gap respectively of a quadruplex applicator
2. Placing the applicator on the plane smooth surface (such as a glass plate)
3. applying the emulsion of the invention in the centre of the Quadruplex applicator near the correct opening.
4. Drawed down the applicator over the surface.
5. leaving the film thus obtained to dry for 1 hour at 20°C and 40% relative humidity;
6. Once dried, the visual appearance of the film created was observed.
Results: in all the emulsions of the present invention, the films of 30mm and 100mm thus obtained were considered appropriate because the film was continuous and uniform; and no furrows without product were appreciated. In the particular case of the lOOmicrons film forming test, the results thus obtained assures that the rules imposed by the food and Drug Administartion (FDA) were ensured (that is 2mg/cm2)
4.4. Wettability properties and antiperspirant actvity 4.4.1. Measurement of the contact angle
The aim of this measurement of the contact angle is the evaluation of the wettability properties of the film created after the deposition of the emulions of the water-in-oil emulsion of the present invention (Ex.1-7) on the PMMA support.
Particularly, the wettability properties of the film is directly correlated with the reaction of the film made by the emulsion of the invention with sweat, and therefore, directly correlated with the antiperspirant activity of the emulsions of the invention.
In fact, a contact angle in a range from 0 to 30 assures the appropriate hydrophilic properties of the emulsion of the present invention for achieving the appropriate antiperspirant effect in a short period of time after its application.
Material:
A polymethylmethacrylate (PMMA) plate that simulates the roughness of human skin (ISO plates (Ra=2 and 5 pm) supplied by Schoneberg GmbH & Co.) was used as a support for the creation of the film and to simulate the behavior of the film created by the emulsions of the invention on top of the skin.
Method:
1. The PMMA plate was tared on the scale in order to control the weight of the emu
2. The emuslion was applied in the center of the plate (0.17g of emulsion/plate)
3. then, the emulsion was spreaded in a circular sense with two fingers (wearing gloves), gradually expanding the spread area until it reached the edges.
4. To secure the extension, an oval-shaped extension was made from left to right of the plate and from top to bottom.
5. Finally, in order to ensure a good reading, a straight extension is made from top to bottom, as close together as possible so that the line was straight.
6. Once the emulsion was well spread, the plates were left to dry for an hour and a half at 20°C and 40% relative humidity; 7. Subsequently, the contact angle measurement was performed.
The measurement of the contact angle was made with the DSA25E instrument of the KrCiss brand, through the "sessile drop" method and the measurement was taken 15 seconds after the drop of water has fallen on the support with the film formed by the emuslion of the invention.
Results:
The values of the contact angles and its standard deviation are summarized hereinbelow:
(1) standard deviation
As it is shown in Table above, the values of contact angle of all the water-in-oil emulsions of the present invention are similar, being all of them between the suitable range mentioned above (0-30). It means that all the water-in-oil emulsions of the invention have the appropriate wettability (hydrophilic character), and therefore, useful as anti perspi rants for a long period of time, avoiding the occurrence of unsightly sweat marks on clothing; minimizing the body odour; and having a good cosmeticity taking care of the skin without providing an oily or sticky feeling, leaving a dry skin with a comfortable feeling and clean appearance; as it is demonstrated for the emulsion of example 1 (see section 3).
5. Medical use 5.1. In-vitro therapeutic effect evaluation of an abnormal transpiration (Hyperhidrosis)
Materials and Methods
The SOD4 machine is designed to test the efficiency of antiperspirant formulations. The machine is a fully automated biomimetic system that imitates the sweating process. It allows recreating the contact between the sweat and the antiperspirant, to observe the reaction inside the transparent mimetic pores. When it creates a clot, it is possible to characterize the resistance of the clot and deduce the efficiency of the antiperspirant.
To perform that experiment the machine includes:
- Smart-Pore™, a silicone microfluidic chip containing microchannels mimicking skin pores. - An integrated pressure system controlling the flow of sweat in the pores down to nanolitre precision.
- A climatic chamber regulated in humidity/temperature, reproducing actual perspiration conditions.
- An optical system to monitor and record the evolution of the interaction between the antiperspirant and the sweat
Artificial sweat used in the present test is as follows:
Sodium Chloride 0.5%
Lactic Acid 0.1%
Urea 0.1%
Bovine Serum Albumin 0.1%
Millipore Water Up to 100%
Fluorescein 0.1%
Ammonium Hydroxide for having a pH = 6.5
All the ingredients are mixed during the preparation of a sweat batch. After the adjustment of the pH, the solution is filtered and divided in 10ml aliquot that are frozen until use. One aliquot is defrosted each day for the measurements. Although fluorescein is not a component of the human sweat, it is a great help for the visualization of the clogging process. Control experiments showed previously that the fluorescein does not impact the clogging process. This sweat model is known in the state of the art and it is the most simple and non-specific one used in the cosmetic field. It is possible to replace this sweat by a natural one or another formulation of artificial one.
Component Quantity Microfluidics chip: SMART-PORE™
The channel network is composed of 4 independent channels. The wider parts are the inlet channels and measure roughly 500 pm x 60 pm x 10 mm. Each fluidic line finishes with a thin microfluidic channel: the biopore. They are biomimetic channels representing the sweat duct of a human body. They are 60 pm wide, 60 pm high and 2 mm long. These biopores end on a flat surface representing the skin.
Experimental protocol
It is disclosed herein below a summary describing the method used for the tested compositions with an application directly on the surface of the Smart-pore™.
The liquid was removed from the recipient and then the propellant present on the spray was also removed. A stencil that had a thickness of 100 pm was used, in order to assured that the quantity of composition is sufficient to react with the sweat and respect the rules imposed by the FDA (2mg /cm2).
Each experiment was performed on a 4-channel Smart-poretm, providing 4 results in parallel. The experiments were performed in a controlled environment where the relative humidity was kept at 80% and 30°C.
Contrary to the in-vitro test performed in section 2.2. for a normal perspiration conditions implying a sweat Flow Rate of 0,02 mI/min; the hyperhidrosis conditions of the current in-vitro test implies a sweat flow Rate of 0,06 pl/min. The protocol was as follows: Firstly, a new Smart-Pore™ with the artificial sweat was filled. Once the channels were full, the stabilization process of the flow was launched. Then, the hanging drop of sweat was removed to create "armpit-on-a-chip” conditions and the composition to be tested was applied. The contact between the sweat and the product lasted 1 hour, during which the image of each clot while it was growing was recorded. During these experiments, the following parameters were measured:
• The Burst pressure (mbars) that is the average of the maximal pressure applied to push out the clot inside the channel.
• The clot length (pm) that was observed corresponding of the penetration of the composition into the pores.
Tested Samples:
- Water-in-oil emulsion composition in form of spray of the present invention (Example 1)
- Comparative water-in-oil emulsion composition in form of spray falling outside the scope of the present invention (Comparative Example 1)
Results
The comparative sample DID NOT form clot. Meanwhile, the values of the burst pressure, the coverage rate and the clot length of the clot formed by the tested composition of the present invention are summarised herein below:
As it is shown in the results above, the composition of the present invention allows obtaining a clot under abnormal perspiration conditions (i.e. hyperhidrosis conditions) with an appropriate burst pressure and length for having an antiperspirant effect for a prolonged period of time under hyperhidrosis conditions.
Therefore, it is concluded that only the water-in-oil emulsion compositions of the present invention with the specific combination of antiperspirants, film-forming agents and emollients disclosed in the present application allows having an effective and prolonged therapeutical antiperspirant effect; and being useful for the treatment or prevention of a disease or condition which involve an excessive or abnormal perspiration such as hhyperhidrosis,
For reasons of completeness, various aspects of the invention are set out in the following numbered clauses:
Clause 1. A pharmaceutical or cosmetic water-in-oil emulsion composition comprising:
(a) a therapeutically or cosmetically effective amount of one or more antiperspirant active ingredients;
(b) one or more film-forming agents selected from the group consisting of capryloyl glycerine/sebacic acid copolymer; polyester-7 (and) neopentyl glycol diheptanoate; ethylcellulose (and) diisopropyl adipate; VP/acry I ates/l au ry I methacrylate copolymer; VP/eicosene copolymer; triacontanyl PVP; and pentylene glycol (and) shellac; and
(c) one or more emollients selected from the group consisting of dicaprylyl ether; PPG-14 butyl ether; triheptanoin (and) (C13-C16) isoparaffin; heptyl undecylenate (and) (C13-C15) alkane; triheptanoin (and) (C13- C15) alkane; diisooctyl succinate; neopentyl glycol diheptanoate; diheptyl succinate; isododecane; dipropylheptyl carbonate; caprylyl caprylate/caprate; propylheptyl caprylate; cetearyl isononanoate; undecane (and) tridecane; (Ci2-Cis)alkyl benzoate, dibutyl adipate; coco-caprylate; dicaprylyl carbonate; PPG-15 stearyl ether; coco-caprylate/caprate; caprylic/capric triglyceride; cocoglycerides; and isopropyl palmitate;
(d) together with one or more pharmaceutically or cosmetically acceptable excipients or carriers.
Clause 2. The water-in-oil emulsion composition according to clause 1, wherein:
(a) the one or more antiperspirant active ingredients are selected from the group consisting of aluminium containing salts, zirconium containing salts and zinc containing salts.
Clause 3. The water-in-oil emulsion composition according to any of the clauses 1 or 2, wherein: (a) at least one of the antiperspirant active ingredients is an aluminium containing salts.
Clause 4. The water-in-oil emulsion composition according to any of the clauses 1-3, wherein: (b) at least one of the film-forming agents is capryloyl glycerine/sebacic acid copolymer.
Clause 5. The water-in-oil emulsion composition according to any of the clauses 1-4, wherein: (c) at least one of the emollients is selected from the group consisting of dicaprylyl ether and PPG-14 butyl ether.
Clause 6. The water-in-oil emulsion composition according to any of the clauses 1-5, comprising:
(a) at least one of the antiperspirant active ingredients is an aluminium containing salts;
(b) at least one of the film-forming agents is capryloyl glycerine/sebacic acid copolymer; and
(c) at least one of the emollients is selected from the group consisting of dicaprylyl ether and polypropylene glycol butyl ether.
Clause 7. The water-in-oil emulsion composition according to any of the clauses 1-6, comprising:
(a) from 20 to 60 % by weight of one or more antiperspirant active ingredients;
(b) from 0.1 to 10 % by weight of one or more film-forming agents; and
(c) from 12 to 40 % by weight of one or more emollient; being the sum of the components up to 100% by weight.
Clause 8. The water-in-oil emulsion composition according to any of the clauses 1-7, comprising: (a) from 40 to 55 % by weight of one or more antiperspirant active ingredients;
(b) from 1 to 5 % by weight of one or more film-forming agents; and
(c) from 20 to 30 % by weight of one or more emollient; being the sum of the components up to 100% by weight. Clause 9. The water-in-oil emulsion composition according to any of the clauses 1-7, wherein:
(d) the pharmaceutically or cosmetically acceptable excipients or carriers are selected from the group consisting of surfactant, vehicle, preservative, propellant, pH-regulating agent, stabilizing agents, viscosity agent, skin conditioning agent, antioxidant and mixture thereof; and optionally, the water-in-oil emulsion composition further comprises: (e) one or more additional pharmaceutically or cosmetically active ingredients.
Clause 10. The water-in-oil emulsion composition according to any of the clauses 1-7 or 9 comprising:
(a) from 20 to 60 % by weight of one or more antiperspirant active ingredients;
(b) from 0.1 to 10 % by weight of one or more film-forming agents; (c) from 12 to 40 % by weight of one or more emollient;
(d) from 0 to 8% by weight of surfactants; from 0 to 3% by weight of preservatives; from 0 to 5% of stabilizing agent; from 0 to 10% of skin conditioning; and (e) from 0 to 5% by weight of additional active ingredients; being the sum of the components up to 100% by weight.
Clause 11. The water-in-oil emulsion composition according to any of the clauses 1-7, 9 or 10 comprising: (a) from 20 to 60 % by weight of one or more antiperspirant active ingredients; (b) from 0.1 to 10 % by weight of one or more film-forming agents;
(c) from 12 to 40 % by weight of one or more emollient;
(d) from 1 to 8% by weight of surfactants; from 0.1 to 3% by weight of preservatives; from 0.1 to 3% of stabilizing agent; from 0.1 to 10% of skin conditioning; and
(e) from 0.1 to 1% by weight of deodorant active ingredients; being the sum of the components up to 100% by weight.
Clause 12. The water-in-oil emulsion composition according to any of the clauses 1-11 comprising:
(a) from 40 to 55 % by weight of one or more antiperspirant active ingredients;
(b) from 1 to 5 % by weight of one or more film-forming agents;
(c) from 20 to 30 % by weight of one or more emollient;
(d) from 0 to 5% by weight of surfactants; from 0 to 3% by weight of preservatives; from 0 to 3% of stabilizing agent; from 0 to 6% of skin conditioning; and
(e) from 0 to 5% by weight of additional active ingredients; being the sum of the components up to 100% by weight.
Clause 13. The water-in-oil emulsion composition according to any of the clauses 1-12 comprising:
(a) from 40 to 55 % by weight of one or more antiperspirant active ingredients;
(b) from 1 to 5 % by weight of one or more film-forming agents;
(c) from 20 to 30 % by weight of one or more emollient;
(d) from 2 to 5% by weight of surfactants; from 0.1 to 3% by weight of preservatives; from 0.1 to 3% of stabilizing agent; from 0.1 to 6% of skin conditioning; and
(e) from 0.3 to 1% by weight of deodorant active ingredients; being the sum of the components up to 100% by weight.
Clause 14. The water-in-oil emulsion composition according to any of the clauses 1-13, which is a topical water-in-oil emulsion spray composition, optionally comprising one or more propellants.
Clause 15. The water-in-oil emulsion composition as defined in any of the clauses 1-14 for use in therapy; or alternatively the use of water-in-oil emulsion composition in cosmetic; particularly as antiperspirant and deodorant agent.
Claims
1. A pharmaceutical or cosmetic water-in-oil emulsion composition comprising:
(a) a therapeutically or cosmetically effective amount of one or more antiperspirant active ingredients; (b) one or more film-forming agents selected from the group consisting of capryloyl glycerine/sebacic acid copolymer; polyester-7 (and) neopentyl glycol diheptanoate; ethylcellulose (and) diisopropyl adipate; VP/acrylates/lauryl methacrylate copolymer; VP/eicosene copolymer; triacontanyl PVP; and pentylene glycol (and) shellac; and
(c) one or more emollients selected from the group consisting of dicaprylyl ether; PPG-14 butyl ether; triheptanoin (and) (C13-C16) isoparaffin; heptyl undecylenate (and) (C13-C15) alkane; triheptanoin (and) (C13- C15) alkane; diisooctyl succinate; neopentyl glycol diheptanoate; diheptyl succinate; isododecane; dipropylheptyl carbonate; caprylyl caprylate/caprate; propylheptyl caprylate; cetearyl isononanoate; undecane (and) tridecane; (Ci2-Ci5)alkyl benzoate, dibutyl adipate; coco-caprylate; dicaprylyl carbonate; PPG-15 stearyl ether; coco-caprylate/caprate; caprylic/capric triglyceride; cocoglycerides; octyldodecanol, isopropyl myristate and isopropyl palmitate;
(d) together with one or more pharmaceutically or cosmetically acceptable excipients or carriers.
2. The water-in-oil emulsion composition according to claim 1, wherein: (c) the one or more emollients are selected from the group consisting of dicaprylyl ether; PPG-14 butyl ether; triheptanoin (and) (C13-C16) isoparaffin; heptyl undecylenate (and) (C13-C15) alkane; triheptanoin (and) (C13-C15) alkane; diisooctyl succinate; neopentyl glycol diheptanoate; diheptyl succinate; isododecane; dipropylheptyl carbonate; caprylyl caprylate/caprate; propylheptyl caprylate; cetearyl isononanoate; undecane (and) tridecane; (Ci2-Cis)alkyl benzoate, dibutyl adipate; coco-caprylate; dicaprylyl carbonate; PPG-15 stearyl ether; coco-caprylate/caprate; caprylic/capric triglyceride; cocoglycerides; and isopropyl palmitate.
3. The water-in-oil emulsion composition according to any of the claims 1 or 2, wherein:
(a) the one or more antiperspirant active ingredients are selected from the group consisting of aluminium containing salts, zirconium containing salts and zinc containing salts.
4. The water-in-oil emulsion composition according to any of the claims 1-3, wherein: (a) at least one of the antiperspirant active ingredients is an aluminium containing salts.
5. The water-in-oil emulsion composition according to any of the claims 1-4, wherein: (b) at least one of the film-forming agents is capryloyl glycerine/sebacic acid copolymer.
6. The water-in-oil emulsion composition according to any of the claims 1-5, wherein: (c) at least one of the emollients is selected from the group consisting of dicaprylyl ether and PPG-14 butyl ether.
7. The water-in-oil emulsion composition according to any of the claims 1-6, comprising:
(a) at least one of the antiperspirant active ingredients is an aluminium containing salts;
(b) at least one of the film-forming agents is capryloyl glycerine/sebacic acid copolymer; and
(c) at least one of the emollients is selected from the group consisting of dicaprylyl ether and polypropylene glycol butyl ether.
8. The water-in-oil emulsion composition according to any of the claims 1-7, comprising:
(a) from 20 to 60 % by weight of one or more antiperspirant active ingredients;
(b) from 0.1 to 10 % by weight of one or more film-forming agents; and
(c) from 12 to 40 % by weight of one or more emollient; being the sum of the components up to 100% by weight.
9. The water-in-oil emulsion composition according to any of the claims 1-8, comprising:
(a) from 40 to 55 % by weight of one or more antiperspirant active ingredients;
(b) from 1 to 5 % by weight of one or more film-forming agents; and
(c) from 20 to 30 % by weight of one or more emollient; being the sum of the components up to 100% by weight.
10. The water-in-oil emulsion composition according to any of the claims 1-9, wherein:
(d) the pharmaceutically or cosmetically acceptable excipients or carriers are selected from the group consisting of surfactant, vehicle, preservative, propellant, pH-regulating agent, stabilizing agents, viscosity agent, skin conditioning agent, antioxidant and mixture thereof; and optionally, the water-in-oil emulsion composition further comprises: (e) one or more additional pharmaceutically or cosmetically active ingredients.
11. The water-in-oil emulsion composition according to any of the claims 1-8 or 10 comprising:
(a) from 20 to 60 % by weight of one or more antiperspirant active ingredients;
(b) from 0.1 to 10 % by weight of one or more film-forming agents;
(c) from 12 to 40 % by weight of one or more emollient;
(d) from 0 to 8% by weight of surfactants; from 0 to 3% by weight of preservatives; from 0 to 5% of stabilizing agent; from 0 to 10% of skin conditioning; and
(e) from 0 to 5% by weight of additional active ingredients; being the sum of the components up to 100% by weight.
12. The water-in-oil emulsion composition according to any of the claims 1-8, 10 or 11 comprising:
(a) from 20 to 60 % by weight of one or more antiperspirant active ingredients;
(b) from 0.1 to 10 % by weight of one or more film-forming agents;
(c) from 12 to 40 % by weight of one or more emollient;
(d) from 1 to 8% by weight of surfactants; from 0.1 to 3% by weight of preservatives; from 0.1 to 3% of stabilizing agent; from 0.1 to 10% of skin conditioning; and
(e) from 0.1 to 1% by weight of deodorant active ingredients; being the sum of the components up to 100% by weight.
13. The water-in-oil emulsion composition according to any of the claims 1-12 comprising:
(a) from 40 to 55 % by weight of one or more antiperspirant active ingredients;
(b) from 1 to 5 % by weight of one or more film-forming agents;
(c) from 20 to 30 % by weight of one or more emollient;
(d) from 0 to 5% by weight of surfactants; from 0 to 3% by weight of preservatives; from 0 to 3% of stabilizing agent; from 0 to 6% of skin conditioning; and
(e) from 0 to 5% by weight of additional active ingredients; being the sum of the components up to 100% by weight.
14. The water-in-oil emulsion composition according to any of the claims 1-13 comprising:
(a) from 40 to 55 % by weight of one or more antiperspirant active ingredients;
(b) from 1 to 5 % by weight of one or more film-forming agents;
(c) from 20 to 30 % by weight of one or more emollient; (d) from 2 to 5% by weight of surfactants; from 0.1 to 3% by weight of preservatives; from 0.1 to 3% of stabilizing agent; from 0.1 to 6% of skin conditioning; and (e) from 0.3 to 1% by weight of deodorant active ingredients; being the sum of the components up to 100% by weight.
15. The water-in-oil emulsion composition according to any of the claims 1-14, which is a topical water-in-oil emulsion spray composition, optionally comprising one or more propellants.
16. The water-in-oil emulsion composition as defined in any of the claims 1-15 for use in therapy; or alternatively the use of water-in-oil emulsion composition in cosmetic; particularly as antiperspirant and deodorant agent.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP21382105 | 2021-02-11 | ||
PCT/EP2022/053190 WO2022171712A1 (en) | 2021-02-11 | 2022-02-10 | Antiperspirant composition |
Publications (1)
Publication Number | Publication Date |
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EP4291151A1 true EP4291151A1 (en) | 2023-12-20 |
Family
ID=74732836
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP22704914.5A Pending EP4291151A1 (en) | 2021-02-11 | 2022-02-10 | Antiperspirant composition |
Country Status (3)
Country | Link |
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EP (1) | EP4291151A1 (en) |
CO (1) | CO2023011644A2 (en) |
WO (1) | WO2022171712A1 (en) |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
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FR3046056B1 (en) * | 2015-12-28 | 2019-12-27 | L'oreal | ANTI-BREATHING ANHYDROUS COMPOSITION IN AEROSOL FORM COMPRISING AN ANTI-BREATHING ACTIVE INGREDIENT AND A VINYLPYRROLIDONE-DERIVED POLYMER |
BR112019011682A2 (en) * | 2016-12-14 | 2019-10-15 | Colgate Palmolive Co | aluminum free antiperspirant / deodorant compositions |
-
2022
- 2022-02-10 EP EP22704914.5A patent/EP4291151A1/en active Pending
- 2022-02-10 WO PCT/EP2022/053190 patent/WO2022171712A1/en active Application Filing
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2023
- 2023-09-01 CO CONC2023/0011644A patent/CO2023011644A2/en unknown
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CO2023011644A2 (en) | 2023-11-20 |
WO2022171712A1 (en) | 2022-08-18 |
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