EP3709955A1 - Topische zusammensetzungen - Google Patents
Topische zusammensetzungenInfo
- Publication number
- EP3709955A1 EP3709955A1 EP18800091.3A EP18800091A EP3709955A1 EP 3709955 A1 EP3709955 A1 EP 3709955A1 EP 18800091 A EP18800091 A EP 18800091A EP 3709955 A1 EP3709955 A1 EP 3709955A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- range
- phytantriol
- topical composition
- glyceryl caprylate
- skin
- 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 113
- 230000000699 topical effect Effects 0.000 title claims abstract description 39
- CGIHFIDULQUVJG-UHFFFAOYSA-N phytantriol Chemical compound CC(C)CCCC(C)CCCC(C)CCCC(C)(O)C(O)CO CGIHFIDULQUVJG-UHFFFAOYSA-N 0.000 claims abstract description 40
- CGIHFIDULQUVJG-VNTMZGSJSA-N phytantriol Natural products CC(C)CCC[C@H](C)CCC[C@H](C)CCC[C@@](C)(O)[C@H](O)CO CGIHFIDULQUVJG-VNTMZGSJSA-N 0.000 claims abstract description 39
- GHBFNMLVSPCDGN-UHFFFAOYSA-N rac-1-monooctanoylglycerol Chemical compound CCCCCCCC(=O)OCC(O)CO GHBFNMLVSPCDGN-UHFFFAOYSA-N 0.000 claims abstract description 39
- 229940087068 glyceryl caprylate Drugs 0.000 claims abstract description 38
- 241000186427 Cutibacterium acnes Species 0.000 claims abstract description 25
- 238000011282 treatment Methods 0.000 claims abstract description 16
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 229960005323 phenoxyethanol Drugs 0.000 claims abstract description 11
- 229940055019 propionibacterium acne Drugs 0.000 claims abstract description 11
- 230000002265 prevention Effects 0.000 claims abstract description 7
- 239000002537 cosmetic Substances 0.000 claims description 33
- 238000000034 method Methods 0.000 claims description 26
- 238000002360 preparation method Methods 0.000 claims description 26
- ULWHHBHJGPPBCO-UHFFFAOYSA-N propane-1,1-diol Chemical compound CCC(O)O ULWHHBHJGPPBCO-UHFFFAOYSA-N 0.000 claims description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 13
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 12
- 206010000496 acne Diseases 0.000 claims description 12
- 230000000813 microbial effect Effects 0.000 claims description 11
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- 239000003995 emulsifying agent Substances 0.000 claims description 10
- 239000002562 thickening agent Substances 0.000 claims description 9
- 239000000839 emulsion Substances 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 210000004761 scalp Anatomy 0.000 claims description 8
- 244000005714 skin microbiome Species 0.000 claims description 7
- 230000015556 catabolic process Effects 0.000 claims description 6
- 239000003921 oil Substances 0.000 claims description 6
- 239000002453 shampoo Substances 0.000 claims description 6
- 230000036074 healthy skin Effects 0.000 claims description 5
- 230000013632 homeostatic process Effects 0.000 claims description 5
- 239000004599 antimicrobial Substances 0.000 claims description 4
- 239000007764 o/w emulsion Substances 0.000 claims description 4
- 238000011321 prophylaxis Methods 0.000 claims description 4
- 239000004094 surface-active agent Substances 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 230000002147 killing effect Effects 0.000 claims description 3
- 201000010099 disease Diseases 0.000 claims description 2
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 14
- -1 isopropylparabene Chemical compound 0.000 description 14
- 239000000194 fatty acid Substances 0.000 description 12
- 239000000126 substance Substances 0.000 description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 11
- 235000014113 dietary fatty acids Nutrition 0.000 description 11
- 229930195729 fatty acid Natural products 0.000 description 11
- 241000894006 Bacteria Species 0.000 description 10
- 230000000845 anti-microbial effect Effects 0.000 description 10
- 150000004665 fatty acids Chemical class 0.000 description 10
- 230000000694 effects Effects 0.000 description 9
- 239000000499 gel Substances 0.000 description 9
- 239000000047 product Substances 0.000 description 9
- 239000003755 preservative agent Substances 0.000 description 8
- 239000004480 active ingredient Substances 0.000 description 7
- 238000004321 preservation Methods 0.000 description 7
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 229920001577 copolymer Polymers 0.000 description 6
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 6
- 238000009472 formulation Methods 0.000 description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 5
- 206010061218 Inflammation Diseases 0.000 description 5
- 239000000654 additive Substances 0.000 description 5
- 238000011109 contamination Methods 0.000 description 5
- 230000004054 inflammatory process Effects 0.000 description 5
- 239000006210 lotion Substances 0.000 description 5
- 244000005700 microbiome Species 0.000 description 5
- 229920001223 polyethylene glycol Polymers 0.000 description 5
- 150000003839 salts Chemical class 0.000 description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 4
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 4
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 4
- 239000002671 adjuvant Substances 0.000 description 4
- UPOYFZYFGWBUKL-UHFFFAOYSA-N amiphenazole Chemical compound S1C(N)=NC(N)=C1C1=CC=CC=C1 UPOYFZYFGWBUKL-UHFFFAOYSA-N 0.000 description 4
- 229950001798 amiphenazole Drugs 0.000 description 4
- 239000003242 anti bacterial agent Substances 0.000 description 4
- 229940088710 antibiotic agent Drugs 0.000 description 4
- 239000006071 cream Substances 0.000 description 4
- 239000003085 diluting agent Substances 0.000 description 4
- 229940008099 dimethicone Drugs 0.000 description 4
- 239000004205 dimethyl polysiloxane Substances 0.000 description 4
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 4
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 230000003020 moisturizing effect Effects 0.000 description 4
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 206010054107 Nodule Diseases 0.000 description 3
- 229910019142 PO4 Inorganic materials 0.000 description 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 206010037888 Rash pustular Diseases 0.000 description 3
- 229920002125 Sokalan® Polymers 0.000 description 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 238000007792 addition Methods 0.000 description 3
- 230000002411 adverse Effects 0.000 description 3
- AIXMJTYHQHQJLU-UHFFFAOYSA-N chembl210858 Chemical compound O1C(CC(=O)OC)CC(C=2C=CC(O)=CC=2)=N1 AIXMJTYHQHQJLU-UHFFFAOYSA-N 0.000 description 3
- 239000006185 dispersion Substances 0.000 description 3
- 150000002334 glycols Chemical class 0.000 description 3
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 235000021317 phosphate Nutrition 0.000 description 3
- 230000002335 preservative effect Effects 0.000 description 3
- 208000029561 pustule Diseases 0.000 description 3
- 210000002966 serum Anatomy 0.000 description 3
- 229910052708 sodium Inorganic materials 0.000 description 3
- 239000007762 w/o emulsion Substances 0.000 description 3
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 description 2
- MOZDKDIOPSPTBH-UHFFFAOYSA-N Benzyl parahydroxybenzoate Chemical compound C1=CC(O)=CC=C1C(=O)OCC1=CC=CC=C1 MOZDKDIOPSPTBH-UHFFFAOYSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- XPJVKCRENWUEJH-UHFFFAOYSA-N Isobutylparaben Chemical compound CC(C)COC(=O)C1=CC=C(O)C=C1 XPJVKCRENWUEJH-UHFFFAOYSA-N 0.000 description 2
- 239000004166 Lanolin Substances 0.000 description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 2
- 208000012868 Overgrowth Diseases 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 2
- 239000004098 Tetracycline Substances 0.000 description 2
- 150000001252 acrylic acid derivatives Chemical class 0.000 description 2
- 125000002252 acyl group Chemical group 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- 239000002280 amphoteric surfactant Substances 0.000 description 2
- 125000000129 anionic group Chemical group 0.000 description 2
- 230000003712 anti-aging effect Effects 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 239000002585 base Substances 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 229940034794 benzylparaben Drugs 0.000 description 2
- 125000002091 cationic group Chemical group 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 235000015165 citric acid Nutrition 0.000 description 2
- 229960002227 clindamycin Drugs 0.000 description 2
- KDLRVYVGXIQJDK-AWPVFWJPSA-N clindamycin Chemical compound CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@H](C)Cl)[C@@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O1 KDLRVYVGXIQJDK-AWPVFWJPSA-N 0.000 description 2
- 239000003086 colorant Substances 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000008406 cosmetic ingredient Substances 0.000 description 2
- 229920006037 cross link polymer Polymers 0.000 description 2
- 239000007854 depigmenting agent Substances 0.000 description 2
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 239000000975 dye Substances 0.000 description 2
- 229960003276 erythromycin Drugs 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 239000000284 extract Substances 0.000 description 2
- 150000002191 fatty alcohols Chemical class 0.000 description 2
- 229940075529 glyceryl stearate Drugs 0.000 description 2
- 230000036541 health Effects 0.000 description 2
- ZUVCYFMOHFTGDM-UHFFFAOYSA-N hexadecyl dihydrogen phosphate Chemical compound CCCCCCCCCCCCCCCCOP(O)(O)=O ZUVCYFMOHFTGDM-UHFFFAOYSA-N 0.000 description 2
- 239000004310 lactic acid Substances 0.000 description 2
- 235000014655 lactic acid Nutrition 0.000 description 2
- 229940039717 lanolin Drugs 0.000 description 2
- 235000019388 lanolin Nutrition 0.000 description 2
- 239000002932 luster Substances 0.000 description 2
- 239000011777 magnesium Substances 0.000 description 2
- 229910052749 magnesium Inorganic materials 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
- 238000011169 microbiological contamination Methods 0.000 description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
- 239000002674 ointment Substances 0.000 description 2
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 2
- ZNSSPLQZSUWFJT-UHFFFAOYSA-N pentyl 4-hydroxybenzoate Chemical compound CCCCCOC(=O)C1=CC=C(O)C=C1 ZNSSPLQZSUWFJT-UHFFFAOYSA-N 0.000 description 2
- GJLNWLVPAHNBQN-UHFFFAOYSA-N phenyl 4-hydroxybenzoate Chemical compound C1=CC(O)=CC=C1C(=O)OC1=CC=CC=C1 GJLNWLVPAHNBQN-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 2
- 239000010452 phosphate Substances 0.000 description 2
- 229920000151 polyglycol Polymers 0.000 description 2
- 239000010695 polyglycol Substances 0.000 description 2
- 229920001296 polysiloxane Polymers 0.000 description 2
- 229910052700 potassium Inorganic materials 0.000 description 2
- RMGVATURDVPNOZ-UHFFFAOYSA-M potassium;hexadecyl hydrogen phosphate Chemical compound [K+].CCCCCCCCCCCCCCCCOP(O)([O-])=O RMGVATURDVPNOZ-UHFFFAOYSA-M 0.000 description 2
- AOJFQRQNPXYVLM-UHFFFAOYSA-N pyridin-1-ium;chloride Chemical compound [Cl-].C1=CC=[NH+]C=C1 AOJFQRQNPXYVLM-UHFFFAOYSA-N 0.000 description 2
- 229960004889 salicylic acid Drugs 0.000 description 2
- 230000008491 skin homeostasis Effects 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- HEMHJVSKTPXQMS-UHFFFAOYSA-M sodium hydroxide Inorganic materials [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000008117 stearic acid Substances 0.000 description 2
- 150000003871 sulfonates Chemical class 0.000 description 2
- 239000011593 sulfur Substances 0.000 description 2
- 229910052717 sulfur Inorganic materials 0.000 description 2
- 230000002195 synergetic effect Effects 0.000 description 2
- 230000009885 systemic effect Effects 0.000 description 2
- 235000019364 tetracycline Nutrition 0.000 description 2
- 150000003522 tetracyclines Chemical class 0.000 description 2
- 230000001960 triggered effect Effects 0.000 description 2
- 235000013311 vegetables Nutrition 0.000 description 2
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 description 1
- YSRSBDQINUMTIF-SNVBAGLBSA-N (2r)-decane-1,2-diol Chemical compound CCCCCCCC[C@@H](O)CO YSRSBDQINUMTIF-SNVBAGLBSA-N 0.000 description 1
- CUNWUEBNSZSNRX-RKGWDQTMSA-N (2r,3r,4r,5s)-hexane-1,2,3,4,5,6-hexol;(z)-octadec-9-enoic acid Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O.CCCCCCCC\C=C/CCCCCCCC(O)=O CUNWUEBNSZSNRX-RKGWDQTMSA-N 0.000 description 1
- KAKVFSYQVNHFBS-UHFFFAOYSA-N (5-hydroxycyclopenten-1-yl)-phenylmethanone Chemical compound OC1CCC=C1C(=O)C1=CC=CC=C1 KAKVFSYQVNHFBS-UHFFFAOYSA-N 0.000 description 1
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
- WSWCOQWTEOXDQX-MQQKCMAXSA-M (E,E)-sorbate Chemical compound C\C=C\C=C\C([O-])=O WSWCOQWTEOXDQX-MQQKCMAXSA-M 0.000 description 1
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- MTQKMPGBALVEDL-ZPCKWCKBSA-N (z,12r)-12-hydroxy-2-sulfooctadec-9-enoic acid Chemical class CCCCCC[C@@H](O)C\C=C/CCCCCCC(C(O)=O)S(O)(=O)=O MTQKMPGBALVEDL-ZPCKWCKBSA-N 0.000 description 1
- 229940015975 1,2-hexanediol Drugs 0.000 description 1
- 229940043375 1,5-pentanediol Drugs 0.000 description 1
- OWEGWHBOCFMBLP-UHFFFAOYSA-N 1-(4-chlorophenoxy)-1-(1H-imidazol-1-yl)-3,3-dimethylbutan-2-one Chemical compound C1=CN=CN1C(C(=O)C(C)(C)C)OC1=CC=C(Cl)C=C1 OWEGWHBOCFMBLP-UHFFFAOYSA-N 0.000 description 1
- RZRNAYUHWVFMIP-KTKRTIGZSA-N 1-oleoylglycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-KTKRTIGZSA-N 0.000 description 1
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- ILCOCZBHMDEIAI-UHFFFAOYSA-N 2-(2-octadecoxyethoxy)ethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCOCCO ILCOCZBHMDEIAI-UHFFFAOYSA-N 0.000 description 1
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 1
- XHZPRMZZQOIPDS-UHFFFAOYSA-N 2-Methyl-2-[(1-oxo-2-propenyl)amino]-1-propanesulfonic acid Chemical compound OS(=O)(=O)CC(C)(C)NC(=O)C=C XHZPRMZZQOIPDS-UHFFFAOYSA-N 0.000 description 1
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 1
- DZOOROWXIIPFGA-UHFFFAOYSA-N 2-hydroxypropyl heptanoate Chemical compound CCCCCCC(=O)OCC(C)O DZOOROWXIIPFGA-UHFFFAOYSA-N 0.000 description 1
- GHHURQMJLARIDK-UHFFFAOYSA-N 2-hydroxypropyl octanoate Chemical compound CCCCCCCC(=O)OCC(C)O GHHURQMJLARIDK-UHFFFAOYSA-N 0.000 description 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
- TXFPEBPIARQUIG-UHFFFAOYSA-N 4'-hydroxyacetophenone Chemical compound CC(=O)C1=CC=C(O)C=C1 TXFPEBPIARQUIG-UHFFFAOYSA-N 0.000 description 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 1
- VHUUQVKOLVNVRT-UHFFFAOYSA-N Ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 description 1
- 241000086254 Arnica montana Species 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- 235000018185 Betula X alpestris Nutrition 0.000 description 1
- 235000018212 Betula X uliginosa Nutrition 0.000 description 1
- 241000222122 Candida albicans Species 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- 101001042415 Cratylia mollis Mannose/glucose-specific lectin Cramoll Proteins 0.000 description 1
- 244000007835 Cyamopsis tetragonoloba Species 0.000 description 1
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- 229920001059 synthetic polymer Polymers 0.000 description 1
- 238000007910 systemic administration Methods 0.000 description 1
- 238000009121 systemic therapy Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000011269 tar Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229960002180 tetracycline Drugs 0.000 description 1
- 229930101283 tetracycline Natural products 0.000 description 1
- 229940040944 tetracyclines Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 235000015961 tonic Nutrition 0.000 description 1
- 230000001256 tonic effect Effects 0.000 description 1
- 229960000716 tonics Drugs 0.000 description 1
- 239000003860 topical agent Substances 0.000 description 1
- 125000005208 trialkylammonium group Chemical group 0.000 description 1
- GSEJCLTVZPLZKY-UHFFFAOYSA-O triethanolammonium Chemical compound OCC[NH+](CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-O 0.000 description 1
- SJXYCCRUTIHMCE-GOXDOWKOSA-K tripotassium;(z)-12-hydroxyoctadec-9-enoate;propane-1,2,3-triol Chemical compound [K+].[K+].[K+].OCC(O)CO.CCCCCCC(O)C\C=C/CCCCCCCC([O-])=O.CCCCCCC(O)C\C=C/CCCCCCCC([O-])=O.CCCCCCC(O)C\C=C/CCCCCCCC([O-])=O SJXYCCRUTIHMCE-GOXDOWKOSA-K 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
- 235000020234 walnut Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 150000003751 zinc Chemical class 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
- A61K8/18—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
- A61K8/34—Alcohols
- A61K8/345—Alcohols 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
- A61K8/30—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/30—Characterized by the absence of a particular group of ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/52—Stabilizers
- A61K2800/524—Preservatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/59—Mixtures
- A61K2800/592—Mixtures of compounds complementing their respective functions
- A61K2800/5922—At least two compounds being classified in the same subclass of A61K8/18
Definitions
- the present invention relates to topical compositions comprising phytantriol and glyceryl caprylate, characterized in that the composition is free of phenoxyethanol as well as to the use of phytantriol in combination with glyceryl caprylate for the prevention and/or treatment of ailments associated with Propionibacterium acnes and to prevent microbial decay of cosmetic products.
- preservatives To protect cosmetic compositions, household products, plastics, paper and / or paints against mold and bacteria, most products currently on the market contain preservatives. While these preservatives protect against bacteria and fungi, studies have linked daily exposure to many of these substances to an increased risk of skin irritation, cancer and / or endocrine problems. Thus, many manufactures are searching for alternative antimicrobial actives which allow reducing the amount of preservatives and don’t appear to pose any health risks.
- Antimicrobial active compounds furthermore play a key role for many cosmetic applications:
- Acne is taken to mean a skin disorder which is evident in inflamed papules, pustules or nodules, caused by increased talc production and impaired keratinization of the skin.
- the inflammation may be associated with reddening, swelling and pressure pain.
- possible causes of acne formation can be androgens, comedogenic substances (for example in cosmetics), smoking, stress or excessive colonization of the skin by bacteria.
- Acne is in particular triggered by the microorganism Propionibacterium acnes (P. acnes), which is a bacterium which usually colonizes the skin and lives on sebum. Acne may arise, for example, if the number of these bacteria is increased.
- Topical antibiotics which have been utilized to attempt to inhibit the overgrowth of P. acnes are clindamycin, erythromycin, tetracycline, and metronidazole. Each of these topical antibiotics reportedly cause side effects and widespread use also contributes to the risk of bacterial resistance.
- Phenoxyethanol is used as an anti-bacterial in cosmetics but can have significant adverse effects. Thus, there is an ongoing need to replace phenoxyethanol for the treatment of acne with other well accepted cosmetic ingredients.
- the combination of phytantriol and glyceryl caprylate shows a synergistic antimicrobial effect against P. acnes.
- the combination can effectively be used in cosmetic compositions which are free of any phenoxyethanol to control the P. acnes on the skin and / or the scalp and thus overcome the adverse effects resulting from a P. acnes overpopulation on the skin and / or scalp such the treatment of inflammation triggered by P. acnes, red nodules or pustules.
- the present invention relates to topical compositions comprising phytantriol and glyceryl caprylate with the proviso that the composition does not contain any phenoxyethanol.
- the invention relates to a combination of phytantriol and glyceryl caprylate as antimicrobial agent against P. acnes.
- the invention relates to a method for killing and / or inhibiting P. acnes, said method comprising contacting P. acnes with a combination of phytantriol and glyceryl caprylate.
- the combination of phytantriol and glyceryl caprylate is further suitable for the treatment of any adverse skin condition associated with an overpopulation of P. acnes by maintaining a healthy skin homeostasis and / or improving the health of the skin microbiome.
- the invention also relates to a method of treating the skin and / or the scalp, said method comprising the steps of contacting the skin and / or scalp with a topical composition according to the present invention for the treatment, prevention and/or prophylaxis of acne as well as for maintaining a healthy skin homeostasis and / or skin microbiome balance.
- the present invention relates to the use of a topical composition according to the present invention for the treatment, prevention and/or prophylaxis of acne as well as for maintaining skin homeostasis and / or skin microbiome balance.
- Phytantriol [CAS: 74563-64-7] is a colourless to light yellow, viscous liquid with the chemical name 3,7,1 1 ,15-tetramethyl-hexadecane-1 ,2,3-triol. Phytantriol is e.g. commercially available at DSM Nutritional Products Ltd, Kaiseraugst.
- Glyceryl caprylate [26402-26-6] is e.g. commercially available as Dermosoft GMCY at Dr. Straetmann.
- antimicrobial activity means a capability of killing and/or inhibiting the growth of microbial cells such as in particular P. acnes.
- the topical compositions preferably comprise phytantriol in an amount selected in the range of about 0.005 to 5 wt.-%, more preferably in the range of about 0.01 to 3 wt.-% and most preferably in the range of 0.025 to 2 wt.-%, such as in an amount of 0.04 to 1.5 wt.-% and particularly advantageous in an amount of 0.04 to 1 wt.-%, based on the total weight of the composition.
- the topical compositions preferably comprise the glyceryl caprylate in an amount selected in the range of about 0.01 to about 2 wt.-%, preferably in the range of 0.05 to 1.5 wt.-%, most preferably in the range of 0.1 to 1 wt.-%, based on the total weight of the composition.
- the ratio (w/w) of phytantriol to glyceryl caprylate in all embodiments of the present invention is preferably selected in the range of 5: 1 to 1 :5, such as in the range of 2.5:1 to 1 :2.5, such as most preferable in the range of about 1 :1.
- the anti-microbial activity of the combination of phytantriol and glyceryl caprylate can be used in a multiplicity of formulations or applications, such as, for example, topical compositions, medicinal products or household products, also for preservation purposes.
- the invention relates to a method of preventing microbial decay and breakdown of topical compositions according to the present invention, wherein said method comprises adding to the compositions phytantriol in combination with glyceryl caprylate, even more preferably further in combination with propanediol as an antimicrobial agent.
- the method also encompasses the step of appreciating the result.
- the invention also relates to a method of preserving the topical composition according to the present invention against microbiological contamination or growth, wherein said method comprises adding to the compositions, phytantriol in combination with glyceryl caprylate, even more preferably further in combination with propanediol.
- the method also encompasses the step of appreciating the result.
- the compositions next to being isopropylparabene and / or phenoxyethanol free, the compositions also advantageously do not contain isobutylparaben, phenylparaben, benzylparaben and / or pentylparaben. Most preferably in all embodiments of the present invention, the compositions contain no parabenes at all, i.e. no methylparaben, ethylparaben, isopropylparabene, isobutylparaben, phenylparaben, benzylparaben and pentylparaben.
- the present invention relates to method for preserving a topical composition according to the present invention, wherein the formulation is free of isopropylparabene, preferably of any parabenes, said method comprising incorporating into the composition phytantriol and glyceryl caprylate, even more preferably in combination with propanediol.
- the method also encompasses the step of appreciating the result.
- the invention relates to a method of preventing microbial decay and breakdown of topical compositions as outlined herein which compositions furthermore comprise water and at least one further agent selected from the group consisting of surfactants, emulsifiers, thickeners, and oils as such compositions are particular sensitive to microbial growth.
- the compositions do not exhibit a microbial contamination exceeding the initial contamination rate with at least one microorganism in a period of at least 7 days, more preferably of at least 14 days, most preferably of at least 28 days, (assessed according ISO 1 1930). Even more preferably, the number (i.e. Colony Forming Unit, CFU) of at least one bacteria or mold, such as in particular Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and / or Candida albicans is significantly reduced.
- CFU Colony Forming Unit
- Propanediol [CAS: 504-63-2] is e.g. commercially available as ZEMEA from DuPont Tate & Lyle Bio Products Company, LLC.
- the topical compositions preferably comprise the propanediol in an amount selected in the range of about 0.01 to about 10 wt.-%, preferably in the range of 0.5 to 7.5 wt.-%, most preferably in the range of 1 to 5 wt.-%, based on the total weight of the composition.
- the amount of propanediol used in the compositions is higher than the sum of the amounts of phytantriol and glyceryl caprylate, preferably at least two times higher, more preferably at least 3 times higher.
- the use according to the invention of the combination of phytantriol and glyceryl caprylate and optionally propanediol can take place both in the cosmetic sense as well as in the pharmaceutical sense.
- a pharmaceutical application is conceivable, for example, in the case of specific anti-acne compositions.
- the use is however preferably cosmetic (non-therapeutic) such as for maintenance of skin homeostasis and/ or balancing the skin microbiome.
- compositions according to the present invention are preferably cosmetic or pharmaceutical compositions which are topically applied to mammalian keratinous tissue such as in particular to human skin or the human scalp and hair.
- cosmetic composition refers to cosmetic compositions as defined under the heading "Kosmetika” in Rompp Lexikon Chemie, 10th edition 1997, Georg Thieme Verlag Stuttgart, New York as well as to cosmetic compositions as disclosed in A. Domsch, "Cosmetic Compositions", Verlag fOr chemische Industrie (ed. H. Ziolkowsky), 4 th edition, 1992.
- the cosmetic or pharmaceutical compositions according to the present invention preferably further comprise a physiologically acceptable medium, that is to say a medium compatible with keratinous substances, such as the skin, mucosa, and keratinous fibers.
- a physiologically acceptable medium is a cosmetically or pharmaceutically acceptable carrier.
- cosmetically or pharmaceutically acceptable carrier refers to all carriers and/or excipients and/ or diluents conventionally used in cosmetic compositions.
- the topical compositions according to the present invention are generally prepared by admixing phytantriol and glyceryl caprylate in the amounts indicated herein with a suitable carrier.
- carrier e.g., other active ingredients
- the cosmetic or pharmaceutical compositions according to the present invention comprise from about 50% to about 99%, preferably from about 60% to about 98%, more preferably from about 70% to about 98%, such as in particular from about 80% to about 95% of a carrier, based on the total weight of the cosmetic composition.
- the carrier consists furthermore of at least 40 wt.-%, more preferably of at least 50 wt.-%, most preferably of at least 55 wt.-% of water, such as in particular of about 55 to about 90 wt.-% of water.
- compositions of the invention may comprise conventional adjuvants and additives, such as preservatives/antioxidants, fatty substances/oils, organic solvents, silicones, thickeners, softeners, emulsifiers, antifoaming agents, aesthetic components such as fragrances, surfactants, fillers, anionic, cationic, nonionic or amphoteric polymers or mixtures thereof, propellants, acidifying or basifying agents, dyes, colorings/colorants, abrasives, absorbents, chelating agents and / or sequestering agents, essential oils, skin sensates, astringents, pigments or any other ingredients usually formulated into such compositions.
- adjuvants and additives such as preservatives/antioxidants, fatty substances/oils, organic solvents, silicones, thickeners, softeners, emulsifiers, antifoaming agents, aesthetic components such as fragrances, surfactants, fillers, anionic, cationic, nonionic or amphoter
- compositions according to the invention may also comprise further cosmetically active ingredients conventionally used in cosmetic or pharmaceutical compositions.
- active ingredients encompass skin lightening agents; UV-filters, agents for the treatment of hyperpigmentation; agents for the prevention or reduction of inflammation; firming, moisturizing, soothing, and / or energizing agents as well as agents to improve elasticity and skin barrier.
- cosmetic excipients examples include cosmetic excipients, diluents, adjuvants, additives as well as active ingredients commonly used in the skin care industry which are suitable for use in the cosmetic compositions of the present invention are for example described in the International Cosmetic Ingredient Dictionary & Handbook by Personal Care Product Council (http://www.personalcarecouncil.org/), accessible by the online INFO BASE (http://online.personalcarecouncil.org/jsp/Home.jsp), without being limited thereto.
- the necessary amounts of the active ingredients as well as the excipients, diluents, adjuvants, additives etc. can, based on the desired product form and application, easily be determined by the skilled person.
- the additional ingredients can either be added to the oily phase, the aqueous phase or separately as deemed appropriate.
- the cosmetically active ingredients useful herein can in some instances provide more than one benefit or operate via more than one mode of action.
- the cosmetic or pharmaceutical compositions according to the invention are in the form of a suspension or dispersion in solvents or fatty substances, or alternatively in the form of an emulsion or micro emulsion (in particular of 0/W- or W/O-type), PIT-emulsion, nano emulsion, multiple emulsion (e. g. O/W/O- or W/O/W- type), pickering emulsion, hydrogel, lipogel, one- or multiphase solution or vesicular dispersion.
- an emulsion or micro emulsion in particular of 0/W- or W/O-type
- PIT-emulsion nano emulsion
- multiple emulsion e. g. O/W/O- or W/O/W- type
- pickering emulsion hydrogel, lipogel, one- or multiphase solution or vesicular dispersion.
- the cosmetic or pharmaceutical compositions in accordance with the invention can be in the form of a liquid, lotion, a thickened lotion, a gel, a cream, a milk, an ointment or a paste.
- the cosmetic or pharmaceutical compositions according to the invention have a pH in the range of 3-10, preferably in the range of pH of 3-8, most preferred in the range of pH 3-7.5.
- the pH is adjusted by methods known to a person skilled in the art, e.g. by using an acid such as a hydroxy acid including glycolic acid, lactic acid, malic acid, citric acid and tartaric acid or a base such as e.g. sodium or potassium hydroxide or ammonium hydroxide as well as mixtures thereof.
- the acid if present, is used in an amount of at least 0.0001 wt.-%, such as e.g. in an amount of 0.01 -1 wt.-%, in particular in an amount of 0.01 to 0.5 wt.-%.
- the cosmetic compositions according to the present invention advantageously comprise an additional preservative.
- suitable preservatives in all embodiments of the present invention are benzoic acid, sodium benzoate, sorbic acid, potasssium sorbate, dehydroacetic acid, alcohol, alcohol denat.; as well as mixtures thereof.
- the preservative is preferably used in an amount of 0.01 to 2 wt.-%, more preferably in an amount of 0.05 to 1.5 wt.-%, most preferably in an amount of 0.1 to 1.0 wt.-%, based on the total weight of the composition.
- compositions according to the present invention may comprise an additional amount of a preservation booster such as hydroxyacetophenone, caprylyl glycol, pentylene glycol, 1 ,2 hexanediol, decylene glycol, monoglycerides such as glyceryl laurate, propylene glycol caprylate, propylene glycol heptanoate as well as mixtures thereof.
- a preservation booster such as hydroxyacetophenone, caprylyl glycol, pentylene glycol, 1 ,2 hexanediol, decylene glycol, monoglycerides such as glyceryl laurate, propylene glycol caprylate, propylene glycol heptanoate as well as mixtures thereof.
- the preservation booster is preferably used in an amount of 0.01 to 2 wt.-%, more preferably in an amount of 0.05 to 1.5 wt.-%, most preferably in an amount of 0.1 to 1.0 wt.-%, based on the total weight of the composition.
- the cosmetic compositions according to the present invention are in particular skin care preparations, functional preparations and / or hair care preparations such as most in particularly skin or hair care preparations.
- Examples of skin care preparations are, in particular, light protective preparations (sunscreen preparations), anti-ageing preparations, preparations for the treatment of photo-ageing, body oils, body lotions, body gels, treatment creams, skin protection ointments, moisturizing preparations such as moisturizing gels or moisturizing sprays, face and/or body moisturizers, as well as skin lightening preparations.
- light protective preparations unsunscreen preparations
- anti-ageing preparations preparations for the treatment of photo-ageing
- body oils body lotions, body gels, treatment creams, skin protection ointments
- moisturizing preparations such as moisturizing gels or moisturizing sprays
- face and/or body moisturizers as well as skin lightening preparations.
- Examples of functional preparations are cosmetic compositions containing active ingredients such as hormone preparations, vitamin preparations, vegetable extract preparations, anti-ageing preparations, and/or antimicrobial (antibacterial or antifungal) preparations without being limited thereto.
- Examples of hair care preparations which are suitable according to the invention and which may be mentioned are shampoos, hair conditioners (also referred to as hair rinses, hairdressing compositions, hair tonics, hair regenerating compositions, hair lotions, water wave lotions, hair sprays, hair creams, hair gels, hair oils, hair pomades or hair brilliantines. Accordingly, these are always preparations which are applied to the hair and the scalp for a shorter or longer time depending on the actual purpose for which they are used.
- the hair care preparations according to the invention are supplied as shampoos, these can be clear liquids, opaque liquids (with pearly luster effect), in cream form, gel-like or else in powder form or in tablet form, and as aerosols.
- the surfactant raw materials on which these shampoos are based can be anionic, cationic, nonionic and amphoteric in nature and also be present in combinations of these substances.
- anionic surfactants suitable for the incorporation into the shampoo preparations according to the present invention are C 10-20 alkyl- and alkylenecarboxylates, alkyl ether carboxylates, fatty alcohol sulfates, fatty alcohol ether sulfates, alkylolamide sulfates and sulfonates, fatty acid alkylolamide polyglycol ether sulfates, alkanesulfonates and hydroxyalkanesulfonates, olefinsulfonates, acyl esters of isothionates, alpha-sulfo fatty acid esters, alkylbenzenesulfonates, alkylphenol glycol ether sulfonates, sulfosuccinates, sulfosuccinic monoesters and diesters, fatty alcohol ether phosphates, protein-fatty acid condensation products, alkyl monoglyceride sulfates and sulfon
- Suitable cationic surfactants are quaternary ammonium salts such as di(Cio--C 24 alkyl)dimethylammonium chloride or bromide, preferably di (Ci 2 -Ci 8 alkyl)- dimethylammonium chloride or bromide; Cio-C 24 -alkyldimethylethylammonium chloride or bromide; Cio-C 24 -alkyltrimethylammonium chloride or bromide, preferably cetyltrimethylammonium chloride or bromide and C 2 o-C 24 -alkyltrimethylammonium chloride or bromide; C 10 -C 24 4 -alkyldimethylbenzylammonium chloride or bromide, preferably Ci 2 -Ci 8 -alkyldime methylbenzylammoniumchloride; N-(Ci 2 -Cie- alkyl)pyridinium chloride or bromide, preferably N- (C
- Suitable nonionic surfactants which can be used as detergent substances are fatty alcohol ethoxylates (alkylpolyethylene glycols); alkylphenol polyethylene glycols; alkyl mercaptan polyethylene glycols; fattyamine ethoxylates (alkylaminopolyethylene glycols); fatty acid ethoxylates (acylpolyethylene glycols); polypropylene glycol ethoxylates (Pluronic); fatty acid alkylolamides (fatty acid amide polyethylene glycols); sucrose esters; sorbitol esters and polyglycol ether.
- fatty alcohol ethoxylates alkylpolyethylene glycols
- alkylphenol polyethylene glycols alkyl mercaptan polyethylene glycols
- fattyamine ethoxylates alkylaminopolyethylene glycols
- fatty acid ethoxylates acylpolyethylene glycols
- Pluronic fatty
- amphoteric surfactants which can be added to the shampoos are N- (Ci 2 -Ci 8 -alkyl)-.beta.-aminopropionates and N-(Ci 2 -Ci 8 -alkyl)-.beta.- iminodipropionates as alkali metal and mono-, di- and trialkylammonium salts; N- acylamidoalkyl-N,N-dimethylacetobetaine, preferably N-(C8-Ci8-acyl)amidopropyl-N, N-dimethylacetobetaine; Ci 2 -Ci 8 -alkyldimethylsulfopropylbetaine; amphoteric surfactants based on imidazoline (commercial name: Miranol ® , Steinapon ® ), preferably the sodium salt of 1 -(p-carboxymethyloxyethyl)-1-(carboxymethyl)-2- laurylimi
- the hair care preparations according to the invention can additionally contain further additives customary in hair care such as for example perfumes, colorants, also those which simultaneously dye or tint the hair, solvents, opacifying agents and pearly luster agents, for example esters of fatty acids with polyols, magnesium and zinc salts of fatty acids, dispersions based on copolymers, thickening agents such as sodium, potassium and ammonium chloride, sodium sulfate, fatty acid alkylolamides, cellulose derivatives, natural rubbers, also plant extracts, protein derivatives such as gelatin, collagen hydrolysates, polypeptides with a natural or synthetic basis, egg yolk, lecithin, lanolin and lanolin derivatives, fats, oils, fatty alcohols, silicones, deodorizing agents, substances with antimicrobial activity, substances with antiseborrhoeic activity, substances with keratolytic and keratoplastic effect, such as, for example, sulfur, salicylic acid and enzymes as well as further
- the topical cosmetic compositions according to the present invention are advantageously O/W emulsions, W/O emulsions and / or gels such as shower gels.
- topical compositions in the form of O/W emulsions, W/O emulsions and / or gels according to the present invention are skin care preparation intended for the treatment of acne or for maintaining a healthy skin homeostasis and / or for maintaining skin microbiome balance.
- O/W emulsions according to the present invention advantageously comprise (i) phytantriol in an amount selected in the range of about 0.01 to 3 wt.-%, preferably in the range of 0.025 to 2 wt.-%, most preferably in the range of 0.04 to 1.5 wt.-%, based on the total weight of the composition, (ii) glyceryl caprylate in an amount selected in the range of about 0.01 to about 2 wt.-%, preferably in the range of 0.05 to 1 .
- one or more synthetic polymers may be used as an emulsifier such as for example, PVP eicosene copolymer, acrylates/C 10-3o alkyl acrylate crosspolymer, acrylates/steareth-20 methacrylate copolymer, PEG-22/dodecyl glycol copolymer, PEG-45/dodecyl glycol copolymer, and mixtures thereof.
- PVP eicosene copolymer acrylates/C 10-3o alkyl acrylate crosspolymer
- acrylates/steareth-20 methacrylate copolymer acrylates/steareth-20 methacrylate copolymer
- PEG-22/dodecyl glycol copolymer PEG-45/dodecyl glycol copolymer, and mixtures thereof.
- the O/W-emulsifier is selected from the group of cetyl phosphates such as in particular potassium cetyl phosphate (commercially available as Amphisol® K), glyceryl stearate (and) PEG 100 stearate (commercially available as Arlacel® 165) and/ or polyalkylenglycolether such as in particular laureth-35 (lauryl alcohol with 35 EO units; commercially available as Brij® 35).
- the at least one O/W emulsifier is preferably used in an amount of about 0.001 to 10 wt.-%, more preferably in an amount of 0.1 to 7 wt.-% with respect to the total weigh of the composition.
- the cosmetic composition in the form of a O/W emulsion contains advantageously at least one co emulsifier selected from the list of alkyl alcohols such as Cetyl Alcohol (Lorol C16, Lanette 16) Cetearyl Alcohol (Lanette® O), Stearyl Alcohol (Lanette® 18), Behenyl Alcohol (Lanette® 22), Glyceryl Monostearate, Glyceryl Myristate (Estol® 3650), Hydrogenated Coco- Glycerides (Lipocire Na10) without being limited to this and mixtures thereof.
- alkyl alcohols such as Cetyl Alcohol (Lorol C16, Lanette 16) Cetearyl Alcohol (Lanette® O), Stearyl Alcohol (Lanette® 18), Behenyl Alcohol (Lanette® 22), Glyceryl Monostearate, Glyceryl Myristate (Estol® 3650), Hydrogenated Coco- Glycerides (Lipocire Na10) without being limited to this and mixtures thereof.
- the O/W emulsion in addition comprises propanediol selected in an amount of 0.01 to about 10 wt.-%, preferably in the range of 0.5 to 7.5 wt.-%, most preferably in the range of 1 to 5 wt.-%, based on the total weight of the composition.
- W/O emulsions according to the present invention advantageously comprise (i) phytantriol in an amount selected in the range 0.01 to 3 wt.-%, preferably in the range of 0.025 to 2 wt.-%, most preferably in the range of 0.04 to 1.5 wt.-%, based on the total weight of the composition, (ii) glyceryl caprylate in an amount selected in the range of about 0.01 to about 2 wt.-%, preferably in the range of 0.05 to 1 .
- W/Si- emulsifiers are Lauryl Polyglyceryl-3 Polydimethylsiloxyethyl Dimethicone and/or PEG-9 Polydimethylsiloxyethyl Dimethicone and/or Cetyl PEG/PPG-10/1 Dimethicone and/or PEG-12 Dimethicone Crosspolymer and/or PEG/PPG-18/18 Dimethicone.
- the at least one W/O emulsifier is preferably used in an amount of about 0.001 to 10 wt.-%, more preferably in an amount of 0.2 to 7 wt.-% with respect to the total weigh of the composition.
- the W/O emulsion in addition comprises propanediol selected in an amount of 0.01 to about 10 wt.-%, preferably in the range of 0.5 to 7.5 wt.-%, most preferably in the range of 1 to 5 wt- %, based on the total weight of the composition.
- Gel preparations according to the present invention advantageously comprise (i) phytantriol in an amount selected in the range of 0.01 to 3 wt.-%, preferably in the range of 0.025 to 2 wt.-%, most preferably in the range of 0.04 to 1.5 wt.-%, based on the total weight of the composition, (ii) glyceryl caprylate in an amount selected in the range of about 0.01 to about 2 wt.-%, preferably in the range of 0.05 to 1 . 5 wt.-%, most preferably in the range of 0.1 to 1 wt.-%, based on the total weight of the composition, (iii) water and (iv) at least one water soluble thickener.
- Such water- soluble thickeners are well known to a person skilled in the art and are e.g. listed in the "Handbook of Water soluble gums and resins" by Robert L. Davidson (Me Graw Hill Book Company (1980)).
- Particularly suitable water soluble thickeners are selected from the group consisting of polyacrylic acids (e.g. commercially available under the tradename Carbomer or Carbopol ® ), homopolymers of 2-Acrylamido-2- methylpropansulfonic acid (e.g. commercially available as Rheothik ® 1 1-80), acrylate copolymers (e.g.
- the water-soluble thickener is used in an amount of about 0.001 to 10 wt.- %, more preferably in an amount of 0.2 to 7 wt.-%, based on the total weigh of the composition.
- the gel preparation in addition comprises propanediol selected in an amount of 0.01 to about 10 wt.-%, preferably in the range of 0.5 to 7.5 wt.-%, most preferably in the range of 1 to 5 wt.-%, based on the total weight of the composition.
- the topical compositions according to the present invention furthermore comprise glycerin in an amount selected in the range of 0.1 to 15 wt.-%, preferably in the range of 0.5 to 10 wt.-%, most preferably in the range of 1 to 5 wt.-%, based on the total weight of the composition.
- the topical compositions according to the present invention furthermore comprise xanthan gum as thickener in an amount selected in the range of 0.001 to 2 wt.-%, preferably in the range of 0.01 to 1 wt.-%, most preferably in the range of 0.1 to 0.5 wt.-%, based on the total weight of the composition.
- xanthan gum as thickener in an amount selected in the range of 0.001 to 2 wt.-%, preferably in the range of 0.01 to 1 wt.-%, most preferably in the range of 0.1 to 0.5 wt.-%, based on the total weight of the composition.
- solutions of the respective active(s) in ethanol are prepared and further dissolved in physiological serum with 0.85 wt.-% NaCI in the concentrations as outlined in table 1 under sterile conditions.
- Samples containing phytantriol were solubilized in physiological serum supplemented with 10 wt.-% ethanol, samples containing glyceryl caprylate only were solubilized in physiological serum supplemented with 1 wt.-% ethanol.
- the solutions of the active(s) were deposed in 96-deep well plates (1.6 ml/well).
- the wells are contaminated with the Propionibacterium acnes at 2.5*10 5 to 5.6*10 5 cfu/ml to obtain the initial contamination as outlined in table 1. After the contamination, each well was thoroughly mixed to ensure a homogeneous distribution of Propionibacterium acnes. Then each plate was incubated at 22°C for 24h. The counting of the (remaining) population is carried out 24h after contamination.
- the combination of phytantriol and glyceryl caprylate is suitable to suppress microbial growth in a typical cosmetic formulation, which effect is further enhanced by the addition of propanediol.
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Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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EP17202147 | 2017-11-16 | ||
PCT/EP2018/080386 WO2019096635A1 (en) | 2017-11-16 | 2018-11-07 | Topical compositions |
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EP3709955A1 true EP3709955A1 (de) | 2020-09-23 |
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EP18800091.3A Pending EP3709955A1 (de) | 2017-11-16 | 2018-11-07 | Topische zusammensetzungen |
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EP3970803A1 (de) * | 2020-09-22 | 2022-03-23 | Beiersdorf AG | Kosmetische zusammensetzung mit geringer osmolalität |
WO2023242006A1 (en) * | 2022-06-15 | 2023-12-21 | Dsm Ip Assets B.V. | Use of uv filters for the treatment of acne |
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US6284234B1 (en) * | 1998-08-04 | 2001-09-04 | Johnson & Johnson Consumer Companies, Inc. | Topical delivery systems for active agents |
AU4647300A (en) * | 1999-04-19 | 2000-11-02 | Procter & Gamble Company, The | Skin care compositions containing combination of skin care actives |
FR2861989B1 (fr) * | 2003-11-07 | 2005-12-30 | Oreal | Utilisation cosmetique du phytantriol comme agent empechant ou reduisant l'adhesion des microorganismes sur la surface de la peau et/ou des muqueuses |
ATE422350T1 (de) * | 2003-12-12 | 2009-02-15 | Straetmans Chemische Produkte | Anisinsäure und glyceride enthaltende zusammensetzungen |
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