DE102005029388B4 - Active ingredient combinations of glycopyrronium bromide and one or more partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid - Google Patents
Active ingredient combinations of glycopyrronium bromide and one or more partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid Download PDFInfo
- Publication number
- DE102005029388B4 DE102005029388B4 DE102005029388.3A DE102005029388A DE102005029388B4 DE 102005029388 B4 DE102005029388 B4 DE 102005029388B4 DE 102005029388 A DE102005029388 A DE 102005029388A DE 102005029388 B4 DE102005029388 B4 DE 102005029388B4
- Authority
- DE
- Germany
- Prior art keywords
- monoglycerides
- diglycerides
- fatty acids
- citric acid
- saturated fatty
- 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.)
- Expired - Fee Related
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- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 title claims abstract description 36
- 150000002148 esters Chemical class 0.000 title claims abstract description 20
- 229960002462 glycopyrronium bromide Drugs 0.000 title claims abstract description 17
- OGBUMNBNEWYMNJ-UHFFFAOYSA-N batilol Chemical class CCCCCCCCCCCCCCCCCCOCC(O)CO OGBUMNBNEWYMNJ-UHFFFAOYSA-N 0.000 title claims abstract description 11
- 150000004671 saturated fatty acids Chemical class 0.000 title claims abstract description 11
- 235000003441 saturated fatty acids Nutrition 0.000 title claims abstract description 11
- VPNYRYCIDCJBOM-UHFFFAOYSA-M Glycopyrronium bromide Chemical compound [Br-].C1[N+](C)(C)CCC1OC(=O)C(O)(C=1C=CC=CC=1)C1CCCC1 VPNYRYCIDCJBOM-UHFFFAOYSA-M 0.000 title claims abstract description 8
- 239000004480 active ingredient Substances 0.000 title claims description 9
- 239000000890 drug combination Substances 0.000 claims abstract description 10
- 239000002537 cosmetic Substances 0.000 claims description 30
- 238000002360 preparation method Methods 0.000 claims description 30
- 239000000203 mixture Substances 0.000 claims description 19
- 239000002781 deodorant agent Substances 0.000 claims description 18
- 230000001166 anti-perspirative effect Effects 0.000 claims description 7
- 239000003213 antiperspirant Substances 0.000 claims description 7
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 5
- 229940075529 glyceryl stearate Drugs 0.000 claims description 5
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 claims description 4
- NKEQOUMMGPBKMM-UHFFFAOYSA-N 2-hydroxy-2-[2-(2-hydroxy-3-octadecanoyloxypropoxy)-2-oxoethyl]butanedioic acid Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)COC(=O)CC(O)(C(O)=O)CC(O)=O NKEQOUMMGPBKMM-UHFFFAOYSA-N 0.000 claims description 2
- 229960000541 cetyl alcohol Drugs 0.000 claims description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims 2
- ILCOCZBHMDEIAI-UHFFFAOYSA-N 2-(2-octadecoxyethoxy)ethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCOCCO ILCOCZBHMDEIAI-UHFFFAOYSA-N 0.000 claims 1
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims 1
- 239000007957 coemulsifier Substances 0.000 claims 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 claims 1
- 229950011392 sorbitan stearate Drugs 0.000 claims 1
- 229940098760 steareth-2 Drugs 0.000 claims 1
- 229940012831 stearyl alcohol Drugs 0.000 claims 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 18
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 13
- -1 citric acid ester Chemical class 0.000 description 12
- 239000003921 oil Substances 0.000 description 12
- 235000019198 oils Nutrition 0.000 description 12
- 239000003963 antioxidant agent Substances 0.000 description 10
- 235000006708 antioxidants Nutrition 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- ANGKOCUUWGHLCE-UHFFFAOYSA-N 2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester Chemical compound C1[N+](C)(C)CCC1OC(=O)C(O)(C=1C=CC=CC=1)C1CCCC1 ANGKOCUUWGHLCE-UHFFFAOYSA-N 0.000 description 8
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 8
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 8
- 235000011187 glycerol Nutrition 0.000 description 8
- 239000000839 emulsion Substances 0.000 description 7
- 239000003755 preservative agent Substances 0.000 description 7
- 235000002639 sodium chloride Nutrition 0.000 description 7
- 239000000126 substance Substances 0.000 description 7
- 229920002125 Sokalan® Polymers 0.000 description 6
- 150000001298 alcohols Chemical class 0.000 description 6
- 235000014113 dietary fatty acids Nutrition 0.000 description 6
- 239000004205 dimethyl polysiloxane Substances 0.000 description 6
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 6
- 239000000194 fatty acid Substances 0.000 description 6
- 229930195729 fatty acid Natural products 0.000 description 6
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 description 6
- 239000002304 perfume Substances 0.000 description 6
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 6
- 150000003839 salts Chemical class 0.000 description 6
- 229920002545 silicone oil Polymers 0.000 description 6
- OSCJHTSDLYVCQC-UHFFFAOYSA-N 2-ethylhexyl 4-[[4-[4-(tert-butylcarbamoyl)anilino]-6-[4-(2-ethylhexoxycarbonyl)anilino]-1,3,5-triazin-2-yl]amino]benzoate Chemical compound C1=CC(C(=O)OCC(CC)CCCC)=CC=C1NC1=NC(NC=2C=CC(=CC=2)C(=O)NC(C)(C)C)=NC(NC=2C=CC(=CC=2)C(=O)OCC(CC)CCCC)=N1 OSCJHTSDLYVCQC-UHFFFAOYSA-N 0.000 description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 5
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 5
- DLAHAXOYRFRPFQ-UHFFFAOYSA-N dodecyl benzoate Chemical compound CCCCCCCCCCCCOC(=O)C1=CC=CC=C1 DLAHAXOYRFRPFQ-UHFFFAOYSA-N 0.000 description 5
- 229920006395 saturated elastomer Polymers 0.000 description 5
- 239000002562 thickening agent Substances 0.000 description 5
- WAYINTBTZWQNSN-UHFFFAOYSA-N 11-methyldodecyl 3,5,5-trimethylhexanoate Chemical compound CC(C)CCCCCCCCCCOC(=O)CC(C)CC(C)(C)C WAYINTBTZWQNSN-UHFFFAOYSA-N 0.000 description 4
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 4
- LEACJMVNYZDSKR-UHFFFAOYSA-N 2-octyldodecan-1-ol Chemical compound CCCCCCCCCCC(CO)CCCCCCCC LEACJMVNYZDSKR-UHFFFAOYSA-N 0.000 description 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
- ANGKOCUUWGHLCE-HKUYNNGSSA-N [(3s)-1,1-dimethylpyrrolidin-1-ium-3-yl] (2r)-2-cyclopentyl-2-hydroxy-2-phenylacetate Chemical compound C1[N+](C)(C)CC[C@@H]1OC(=O)[C@](O)(C=1C=CC=CC=1)C1CCCC1 ANGKOCUUWGHLCE-HKUYNNGSSA-N 0.000 description 4
- 239000000443 aerosol Substances 0.000 description 4
- BTFJIXJJCSYFAL-UHFFFAOYSA-N arachidyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCO BTFJIXJJCSYFAL-UHFFFAOYSA-N 0.000 description 4
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 4
- 229940008099 dimethicone Drugs 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 239000000499 gel Substances 0.000 description 4
- QAOJADINKLMTRR-UHFFFAOYSA-N octan-3-yl 16-methylheptadecanoate Chemical compound CCCCCC(CC)OC(=O)CCCCCCCCCCCCCCC(C)C QAOJADINKLMTRR-UHFFFAOYSA-N 0.000 description 4
- 235000019645 odor Nutrition 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 239000002994 raw material Substances 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- 239000001993 wax Substances 0.000 description 4
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 3
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 3
- 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 3
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 3
- 208000008454 Hyperhidrosis Diseases 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 150000007513 acids Chemical class 0.000 description 3
- 230000000845 anti-microbial effect Effects 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 229920001577 copolymer Polymers 0.000 description 3
- 229940086555 cyclomethicone Drugs 0.000 description 3
- 230000001877 deodorizing effect Effects 0.000 description 3
- 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 3
- PKPOVTYZGGYDIJ-UHFFFAOYSA-N dioctyl carbonate Chemical compound CCCCCCCCOC(=O)OCCCCCCCC PKPOVTYZGGYDIJ-UHFFFAOYSA-N 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000003792 electrolyte Substances 0.000 description 3
- 150000004665 fatty acids Chemical class 0.000 description 3
- 239000000945 filler Substances 0.000 description 3
- 229940015042 glycopyrrolate Drugs 0.000 description 3
- 229930195733 hydrocarbon Natural products 0.000 description 3
- 150000002430 hydrocarbons Chemical class 0.000 description 3
- 229940119170 jojoba wax Drugs 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000003380 propellant Substances 0.000 description 3
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 3
- 210000004243 sweat Anatomy 0.000 description 3
- 210000000106 sweat gland Anatomy 0.000 description 3
- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 description 3
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 3
- DURPTKYDGMDSBL-UHFFFAOYSA-N 1-butoxybutane Chemical compound CCCCOCCCC DURPTKYDGMDSBL-UHFFFAOYSA-N 0.000 description 2
- LEEDMQGKBNGPDN-UHFFFAOYSA-N 2-methylnonadecane Chemical compound CCCCCCCCCCCCCCCCCC(C)C LEEDMQGKBNGPDN-UHFFFAOYSA-N 0.000 description 2
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 description 2
- 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
- 241000894006 Bacteria Species 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
- GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Natural products CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 2
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 235000019486 Sunflower oil Nutrition 0.000 description 2
- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- 150000001450 anions Chemical class 0.000 description 2
- 239000003212 astringent agent 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
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000000812 cholinergic antagonist Substances 0.000 description 2
- 229920006037 cross link polymer Polymers 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- SOROIESOUPGGFO-UHFFFAOYSA-N diazolidinylurea Chemical compound OCNC(=O)N(CO)C1N(CO)C(=O)N(CO)C1=O SOROIESOUPGGFO-UHFFFAOYSA-N 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- 239000001245 distarch phosphate Substances 0.000 description 2
- 235000013804 distarch phosphate Nutrition 0.000 description 2
- WSDISUOETYTPRL-UHFFFAOYSA-N dmdm hydantoin Chemical compound CC1(C)N(CO)C(=O)N(CO)C1=O WSDISUOETYTPRL-UHFFFAOYSA-N 0.000 description 2
- 239000000975 dye Substances 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 239000003349 gelling agent Substances 0.000 description 2
- 230000037315 hyperhidrosis Effects 0.000 description 2
- ZCTXEAQXZGPWFG-UHFFFAOYSA-N imidurea Chemical compound O=C1NC(=O)N(CO)C1NC(=O)NCNC(=O)NC1C(=O)NC(=O)N1CO ZCTXEAQXZGPWFG-UHFFFAOYSA-N 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- NNPPMTNAJDCUHE-UHFFFAOYSA-N isobutane Chemical compound CC(C)C NNPPMTNAJDCUHE-UHFFFAOYSA-N 0.000 description 2
- 230000003020 moisturizing effect Effects 0.000 description 2
- 239000007764 o/w emulsion Substances 0.000 description 2
- 229960005323 phenoxyethanol Drugs 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- 229920005862 polyol Polymers 0.000 description 2
- 150000003077 polyols Chemical class 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- 235000012239 silicon dioxide Nutrition 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 239000002600 sunflower oil Substances 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- 235000012222 talc Nutrition 0.000 description 2
- REZOIPSCCRVWNN-UHFFFAOYSA-N tetratriacontan-17-ol Chemical compound CCCCCCCCCCCCCCCCCC(O)CCCCCCCCCCCCCCCC REZOIPSCCRVWNN-UHFFFAOYSA-N 0.000 description 2
- 229960003500 triclosan Drugs 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- 229930003231 vitamin Natural products 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- 239000000230 xanthan gum Substances 0.000 description 2
- 235000010493 xanthan gum Nutrition 0.000 description 2
- 229920001285 xanthan gum Polymers 0.000 description 2
- 229940082509 xanthan gum Drugs 0.000 description 2
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 1
- CRDAMVZIKSXKFV-FBXUGWQNSA-N (2-cis,6-cis)-farnesol Chemical compound CC(C)=CCC\C(C)=C/CC\C(C)=C/CO CRDAMVZIKSXKFV-FBXUGWQNSA-N 0.000 description 1
- 239000000260 (2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ol Substances 0.000 description 1
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 description 1
- YHHHHJCAVQSFMJ-FNORWQNLSA-N (3e)-deca-1,3-diene Chemical compound CCCCCC\C=C\C=C YHHHHJCAVQSFMJ-FNORWQNLSA-N 0.000 description 1
- YYGNTYWPHWGJRM-UHFFFAOYSA-N (6E,10E,14E,18E)-2,6,10,15,19,23-hexamethyltetracosa-2,6,10,14,18,22-hexaene Chemical compound CC(C)=CCCC(C)=CCCC(C)=CCCC=C(C)CCC=C(C)CCC=C(C)C YYGNTYWPHWGJRM-UHFFFAOYSA-N 0.000 description 1
- NKJOXAZJBOMXID-UHFFFAOYSA-N 1,1'-Oxybisoctane Chemical compound CCCCCCCCOCCCCCCCC NKJOXAZJBOMXID-UHFFFAOYSA-N 0.000 description 1
- SBASXUCJHJRPEV-UHFFFAOYSA-N 2-(2-methoxyethoxy)ethanol Chemical group COCCOCCO SBASXUCJHJRPEV-UHFFFAOYSA-N 0.000 description 1
- FLPJVCMIKUWSDR-UHFFFAOYSA-N 2-(4-formylphenoxy)acetamide Chemical compound NC(=O)COC1=CC=C(C=O)C=C1 FLPJVCMIKUWSDR-UHFFFAOYSA-N 0.000 description 1
- LWLRMRFJCCMNML-UHFFFAOYSA-N 2-ethylhexyl dodecanoate Chemical compound CCCCCCCCCCCC(=O)OCC(CC)CCCC LWLRMRFJCCMNML-UHFFFAOYSA-N 0.000 description 1
- SFAAOBGYWOUHLU-UHFFFAOYSA-N 2-ethylhexyl hexadecanoate Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(CC)CCCC SFAAOBGYWOUHLU-UHFFFAOYSA-N 0.000 description 1
- MWKPHOIHTLQZIY-UHFFFAOYSA-N 2-hexyldecyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(CCCCCC)CCCCCCCC MWKPHOIHTLQZIY-UHFFFAOYSA-N 0.000 description 1
- 229940100555 2-methyl-4-isothiazolin-3-one Drugs 0.000 description 1
- QWGRWMMWNDWRQN-UHFFFAOYSA-N 2-methylpropane-1,3-diol Chemical compound OCC(C)CO QWGRWMMWNDWRQN-UHFFFAOYSA-N 0.000 description 1
- RUDXBXPTJPNTSO-UHFFFAOYSA-N 2-octyldodecyl hexadecanoate Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(CCCCCCCC)CCCCCCCCCC RUDXBXPTJPNTSO-UHFFFAOYSA-N 0.000 description 1
- UIVPNOBLHXUKDX-UHFFFAOYSA-N 3,5,5-trimethylhexyl 3,5,5-trimethylhexanoate Chemical compound CC(C)(C)CC(C)CCOC(=O)CC(C)CC(C)(C)C UIVPNOBLHXUKDX-UHFFFAOYSA-N 0.000 description 1
- AGNTUZCMJBTHOG-UHFFFAOYSA-N 3-[3-(2,3-dihydroxypropoxy)-2-hydroxypropoxy]propane-1,2-diol Chemical class OCC(O)COCC(O)COCC(O)CO AGNTUZCMJBTHOG-UHFFFAOYSA-N 0.000 description 1
- NJLKZOZYTRRDBO-UHFFFAOYSA-N 3-iodopropyl n-butylcarbamate Chemical compound CCCCNC(=O)OCCCI NJLKZOZYTRRDBO-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- 229940090248 4-hydroxybenzoic acid Drugs 0.000 description 1
- QYYMDNHUJFIDDQ-UHFFFAOYSA-N 5-chloro-2-methyl-1,2-thiazol-3-one;2-methyl-1,2-thiazol-3-one Chemical compound CN1SC=CC1=O.CN1SC(Cl)=CC1=O QYYMDNHUJFIDDQ-UHFFFAOYSA-N 0.000 description 1
- SJIDAAGFCNIAJP-UHFFFAOYSA-N 6-methylheptyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCCCCC(C)C SJIDAAGFCNIAJP-UHFFFAOYSA-N 0.000 description 1
- XUVVLJKRLAXOKZ-UHFFFAOYSA-N 7-methyloctyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCCCCCC(C)C XUVVLJKRLAXOKZ-UHFFFAOYSA-N 0.000 description 1
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 1
- 235000019489 Almond oil Nutrition 0.000 description 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 1
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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
- A61K8/37—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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4913—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Cosmetics (AREA)
Abstract
Wirkstoffkombinationen aus
(i) Glycopyrroniumbromid und
(ii) einem oder mehreren partiell neutralisierten Ester von Monoglyceriden und/oder Diglyceriden gesättigter Fettsäuren mit Zitronensäure.Drug combinations from
(i) glycopyrronium bromide and
(ii) one or more partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid.
Description
Die vorliegende Erfindung betrifft Wirkstoffkombinationen aus Glycopyrroniumbromid und einem oder mehreren partiell neutralisierten Ester von Monoglyceriden und/oder Diglyceriden gesättigter Fettsäuren mit Zitronensäure, kosmetische Zubereitungen, solche Wirkstoffkombinationen enthaltend sowie die Verwendung solcher Wirkstoffkombinationen als wirksames Prinzip kosmetischer Desodorantien und Antitranspirantien.The present invention relates to active ingredient combinations of glycopyrronium bromide and one or more partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid, cosmetic preparations containing such drug combinations and the use of such drug combinations as an effective principle of cosmetic deodorants and antiperspirants.
Der Mensch besitzt zwei unterschiedliche Formen von Schweißdrüsen. Die ekkrinen Schweißdrüsen sondern hauptsächlich Salz und Wasser ab und tragen üblicherweise nicht zur Geruchsbildung bei. Für den Geruch sind die apokrinen Schweißdrüsen verantwortlich, die Fettsäuren, Cholesterine und andere Verbindungen ausscheiden. Diese Substanzen werden von Bakterien auf der Haut zersetzt, wobei die Abbauprodukte den für Schweiß typischen Geruch erzeugen.Humans have two different forms of sweat glands. The eccrine sweat glands secrete mainly salt and water and usually do not contribute to the formation of odors. The smell is caused by the apocrine sweat glands, which excrete fatty acids, cholesterols and other compounds. These substances are decomposed by bacteria on the skin, whereby the degradation products produce the typical smell of sweat.
Um den Schweißgeruch über einen längeren Zeitraum zu unterdrücken, ist der Einsatz kosmetischer Zubereitungen unerlässlich. Den üblichen kosmetischen Desodorantien liegen unterschiedliche Wirkprinzipien zugrunde, die auch kombiniert werden können: Zum einen werden Deowirkstoffe eingesetzt, die das Wachstum der den Schweißgeruch verursachenden Bakterien unterdrücken. Zu diesen keimhemmenden (bakteriostatischen) Mitteln zählen beispielsweise Triclosan, Chlorhexidin oder die natürlich vorkommenden Verbindungen wie Farnesol und Phenoxyethanol.In order to suppress the smell of sweat over a longer period of time, the use of cosmetic preparations is essential. The usual cosmetic deodorants are based on different principles of action, which can also be combined: On the one hand Deodorant agents are used, which suppress the growth of the odor causing bacteria. These antimicrobial (bacteriostatic) agents include, for example, triclosan, chlorhexidine or the naturally occurring compounds such as farnesol and phenoxyethanol.
Zum anderen werden Antitranspirantien eingesetzt, welche die Schweißabsonderung durch Blockierung der Schweißdrüsenausgänge behindern. In den weitaus meisten Antitranspirantien kann durch Adstringentien - vorwiegend Aluminiumsalze wie Aluminiumhydroxychlorid (Aluchlorhydrat) oder Aluminium/Zirkoniumsalze - die Bildung des Schweißes reduziert werden.On the other hand, antiperspirants are used, which hinder the sweating by blocking the sweat gland exits. In the vast majority of antiperspirants, the formation of perspiration can be reduced by astringents, predominantly aluminum salts such as aluminum hydroxychloride (aluminum chlorohydrate) or aluminum / zirconium salts.
Auch die Kombination von Adstringentien mit antimikrobiell wirksamen Stoffen in ein und derselben Zusammensetzung ist gebräuchlich. Ferner werden Parfümstoffe zur Überdeckung des Schweißgeruches eingesetzt.The combination of astringents with antimicrobial substances in the same composition is also common. Furthermore, perfumes are used to cover the sweat odor.
Nachteilig bei der Verwendung von Aluchlorhydrat ist beispielsweise, dass Rückstände die Kleidung in unschöner Weise verfärben können und der niedrige pH-Wert (sauer) der kosmetischen Zubereitung das biologische Gleichgewicht der Haut unvorteilhaft beeinflusst.A disadvantage of the use of Aluchlorhydrat is, for example, that residues can discolor the clothes in unsightly manner and the low pH (acidic) of the cosmetic preparation affects the biological balance of the skin unfavorably.
Bekannt und gebräuchlich sind neben den flüssigen Desodorantien wie Zerstäuber und Rollon auch feste Zubereitungen, beispielsweise Deo-Stifte („Sticks“), Puder, Pudersprays, Intimreinigungsmittel usw.Besides the liquid deodorants such as atomizers and rollons, solid preparations are also known and customary, for example deodorant sticks ("sticks"), powders, powder sprays, intimate cleaning agents, etc.
An ein zufriedenstellendes Deo-Mittel werden folgende Voraussetzungen geknüpft: 1) Schonung der natürlichen Biologie der Haut 2) Duftneutralität 3) Wirksamkeit nur in Bezug auf Desodorierung, d.h. nur Vermeidung und/oder Beseitigung von Körpergeruch 4) Vermeidung der Bildung von resistenten Bakterienstämmen 5) Vermeidung der Akkumulation der Wirkstoffe auf der Haut 6) Unschädlichkeit bei Überdosierung oder sonstiger nicht bestimmungsgemäßer Anwendung 7) Gute kosmetische Anwendung 8) Leichte Handhabung (z.B. als Flüssigkeit) und universelle Verwendbarkeit in verschiedensten kosmetischen und externen Zubereitungen. 9) Ausgezeichnete Haut- und Schleimhautverträglichkeit 10) Einsatz umweltfreundlicher StoffeThe following conditions are attached to a satisfactory deodorant: 1) protection of the natural biology of the skin 2) odor neutrality 3) effectiveness only with respect to deodorization, i. only avoidance and / or elimination of body odor 4) prevention of the formation of resistant bacterial strains 5) avoidance of accumulation of the active ingredients on the skin 6) harmlessness in case of overdose or other improper use 7) good cosmetic application 8) easy handling (eg as liquid) and universal usability in a wide variety of cosmetic and external preparations. 9) Excellent skin and mucous membrane compatibility 10) Use of environmentally friendly substances
Eine Aufgabe der vorliegenden Erfindung war es also, Zubereitungen zu entwickeln, welche als Grundlage für kosmetische Desodorantien bzw. Antitranspirantien geeignet sind, und die Nachteile des Standes der Technik nicht aufweisen.An object of the present invention was thus to develop formulations which are suitable as a basis for cosmetic deodorants or antiperspirants, and do not have the disadvantages of the prior art.
Weiterhin war es also eine Aufgabe der Erfindung, kosmetische Grundlagen für kosmetische Desodorantien zu entwickeln, die sich durch gute Hautverträglichkeit auszeichnen.Furthermore, it was therefore an object of the invention to develop cosmetic bases for cosmetic deodorants, which are characterized by good skin compatibility.
Die
In der
Die
Glycopyrroniumbromid (Internationaler Freiname für (±)-(R*)-3-[(S*)-(Cyclopentylhydroxyphenylacetoxy]-1,1-dimethylpyrrolidiniumbromid) ist ein seit 1960 bekanntes Anticholinergikum und Spasmolytikum. Es wird, vor allem im englischen Sprachgebrauch als „Glycopyrrolat“ bezeichnet und zeichnet sich durch folgende chemische Struktur aus:
Es war nach all diesem überraschend und nicht vorhersehbar, dass Wirkstoffkombinationen aus
- (i) Glycopyrroniumbromid und
- (ii) und einem oder mehreren partiell neutralisierten Ester von Monoglyceriden und/oder Diglyceriden gesättigter Fettsäuren mit Zitronensäure,
bzw. kosmetische Zubereitungen, solche Wirkstoffkombinationen enthaltend, sowie die Verwendung solcher Wirkstoffkombinationen als wirksames Prinzip kosmetischer Desodorantien und Antitranspirantien, die Nachteile des Standes der Technik beseitigen.It was surprising and unpredictable after all this drug combinations
- (i) glycopyrronium bromide and
- (ii) and one or more partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid,
or cosmetic preparations containing such drug combinations, as well as the use of such drug combinations as an effective principle of cosmetic deodorants and antiperspirants that eliminate the disadvantages of the prior art.
Der Zusatz von oberflächenaktiven Glucosederivaten steigert die antitranspirierende Wirkung von Glycopyrroniumbromid in überraschender und nicht vorhersehbarer Weise. Weiterhin war es für den Fachmann nicht vorauszusehen gewesen, dass die erfindungsgemäßen Wirkstoffkombinationen bzw. kosmetische oder dermatologische Zubereitungen, diese enthaltend
- - sich durch bessere Pflegewirkung auszeichnen,
- - durch Hautneutralität das biologische Gleichgewicht der Haut weniger belasten,
- - besser als Vehikel für kosmetische und medizinische-dermatologische Wirkstoffe dienen,
- - sich durch bessere Bioverträglichkeit auszeichnen,
- - durch eine bessere physikochemische Stabilität der Rezeptur auszeichnet
- - bessere sensorische Eigenschaften, wie beispielsweise die Verteilbarkeit oder das Einzugsvermögen in die Haut, besitzen,
- - are characterized by a better care effect,
- - reduce the biological balance of the skin through skin neutrality,
- - better serve as a vehicle for cosmetic and medical dermatological agents,
- - are characterized by better biocompatibility,
- - characterized by a better physicochemical stability of the formulation
- - have better sensory properties, such as dispersibility or ability to penetrate the skin,
Ein besonders vorteilhafter Citronensäureester ist das Glycerylstearatcitrat. Solche Citronensäureester sind beispielsweise erhältlich unter der Produktbezeichnung „IMWITOR® 370“ der Firma SASOL.A particularly advantageous citric acid ester is glyceryl stearate citrate. Such citric acid esters are obtainable, for example, under the product name "IMWITOR® 370" from SASOL.
Es ist erfindungsgemäß vorteilhaft, das molare Verhältnis von Glycopyrroniumbromid zu einem oder mehreren partiell neutralisierten Ester von Monoglyceriden und/oder Diglyceriden gesättigter Fettsäuren mit Zitronensäure aus dem Bereich von 100 : 1 bis 1 : 100 , bevorzugt 50 : 1 bis 1 : 50, insbesondere bevorzugt 20 : 1 bis 1 : 20 zu wählen. It is advantageous according to the invention, the molar ratio of glycopyrronium bromide to one or more partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid in the range of 100: 1 to 1: 100, preferably 50: 1 to 1: 50, particularly preferred 20: 1 to 1:20 to choose.
Entsprechend der erfindungsgemäßen Verwendung sind die Desodorantien besonders vorteilhaft dadurch gekennzeichnet, dass das Glycopyrroniumbromid in Konzentrationen von 0,01 - 10,00 Gew.-%, bevorzugt 0,05 - 5,00 Gew.-%, besonders bevorzugt 0,1 - 3,00 Gew.-%, jeweils bezogen auf das Gesamtgewicht der Zusammensetzung, vorliegt oder vorliegen.According to the use according to the invention, the deodorants are particularly advantageously characterized in that the glycopyrronium bromide is present in concentrations of 0.01-10.00% by weight, preferably 0.05-5.00% by weight, more preferably 0.1-3 , 00 wt .-%, each based on the total weight of the composition, is present or present.
Entsprechend der erfindungsgemäßen Verwendung sind die Desodorantien besonders vorteilhaft dadurch gekennzeichnet, dass die partiell neutralisierten Ester von Monoglyceriden und/oder Diglyceriden gesättigter Fettsäuren mit Zitronensäure, in Konzentrationen von 0,01 - 10,00 Gew.-%, bevorzugt 0,05 - 5,00 Gew.-%, besonders bevorzugt 0,1 - 3,00 Gew.-%, jeweils bezogen auf das Gesamtgewicht der Zusammensetzung, vorliegen.According to the use according to the invention, the deodorants are particularly advantageously characterized in that the partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid, in concentrations of 0.01-10.00% by weight, preferably 0.05-5, 00 wt .-%, particularly preferably 0.1 to 3.00 wt .-%, each based on the total weight of the composition.
Entsprechend der erfindungsgemäßen Verwendung können die kosmetischen Desodorantien in Form von Aerosolen, also aus Aerosolbehältern, Quetschflaschen oder durch eine Pumpvorrichtung versprühbaren Präparaten vorliegen oder in Form von mittels Roll-on-Vorrichtungen auftragbaren flüssigen Zusammensetzungen, als Deo-Stifte (Deo-Sticks) und in Form von aus normalen Flaschen und Behältern auftragbaren W/O- oder O/W-Emulsionen, z.B. Cremes oder Lotionen. Weiterhin können die kosmetischen Desodorantien vorteilhaft in Form von desodorierenden Tinkturen, desodorierenden Intimreinigungsmitteln, desodorierenden Shampoos, desodorierenden Dusch- oder Badezubereitungen, desodorierenden Pudern oder desodorierenden Pudersprays vorliegen.According to the use according to the invention, the cosmetic deodorants may be present in the form of aerosols, ie aerosol containers, squeeze bottles or preparations which can be sprayed by a pump device or in the form of liquid compositions which can be applied by means of roll-on devices, as deodorant sticks (deodorant sticks) and in Form of W / O or O / W emulsions which can be applied from normal bottles and containers, eg Creams or lotions. Furthermore, the cosmetic deodorants may advantageously be present in the form of deodorant tinctures, deodorizing intimate cleansing agents, deodorizing shampoos, deodorizing shower or bath preparations, deodorising powders or deodorising powder sprays.
Es ist dem Fachmann natürlich bekannt, dass kosmetische Zubereitungen zumeist nicht ohne die üblichen Hilfs- und Zusatzstoffe denkbar sind. Die erfindungsgemäßen kosmetischen und dermatologischen Zubereitungen können dementsprechend ferner kosmetische Hilfsstoffe enthalten, wie sie üblicherweise in solchen Zubereitungen verwendet werden; beispielsweise Konsistenzgeber, Konservierungsmittel, Stabilisatoren, Füllstoffe, Parfüme, Pigmente, die färbende Wirkung haben, Verdickungsmittel, oberflächenaktive Substanzen, Emulgatoren, weichmachende, anfeuchtende und/oder feuchthaltende Substanzen, entzündungshemmende Substanzen, zusätzliche Wirkstoffe wie Vitamine oder Proteine, Lichtschutzmittel, Insektenrepellentien, Bakterizide, Viruszide, Wasser, Salze, antimikrobiell, proteolytische oder keratolytisch wirksame Substanzen, Medikamente oder andere übliche Bestandteile einer kosmetischen oder dermatologischen Formulierung wie Alkohole, Polyole, Polymere, Schaumstabilisatoren, organische Lösungsmittel oder auch Elektrolyte.It is of course known to the person skilled in the art that cosmetic preparations are usually not conceivable without the customary auxiliaries and additives. Accordingly, the cosmetic and dermatological preparations according to the invention may further comprise cosmetic adjuvants such as are conventionally used in such preparations; for example, bodying agents, preservatives, stabilizers, fillers, perfumes, pigments which have coloring properties, thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, antiinflammatory substances, additional active ingredients such as vitamins or proteins, light stabilizers, insect repellents, bactericides, Viruszide, water, salts, antimicrobial, proteolytic or keratolytic active substances, medicaments or other conventional ingredients of a cosmetic or dermatological formulation such as alcohols, polyols, polymers, foam stabilizers, organic solvents or electrolytes.
Elektrolyte können beispielsweise gewählt werden aus der Gruppe der Salze mit folgenden Anionen: Chloride, ferner organische Oxo-Element-Anionen, von diesen insbesondere Sulfate, Carbonate, Phosphate, Borate und Aluminate. Auch auf organischen Anionen basierende Elektrolyte sind vorteilhaft, z.B. Lactate, Acetate, Benzoate, Propionate, Tartrate, Citrate, Aminosäuren, Ethylendiamintetraessigsäure und deren Salzen und andere mehr. Als Kationen der Salze werden bevorzugt Ammonium-, Alkylammonium-, Alkalimetall-, Erdalkalimetall-, Magnesium-, Eisen- bzw. Zinkionen verwendet. Es bedarf an sich keiner Erwähnung, dass in Kosmetika nur physiologisch unbedenkliche Elektrolyte verwendet werden sollten. Besonders bevorzugt sind Kaliumchlorid, Natriumchlorid, Magnesiumsulfat, Zinksulfat und Mischungen daraus.Electrolytes can be selected, for example, from the group of salts with the following anions: chlorides, and also organic oxo element anions, of these in particular sulfates, carbonates, phosphates, borates and aluminates. Also, organic anion-based electrolytes are advantageous, e.g. Lactates, acetates, benzoates, propionates, tartrates, citrates, amino acids, ethylenediaminetetraacetic acid and its salts and others. As cations of the salts it is preferred to use ammonium, alkylammonium, alkali metal, alkaline earth metal, magnesium, iron or zinc ions. There is no need to mention that only cosmetically acceptable electrolytes should be used in cosmetics. Particularly preferred are potassium chloride, sodium chloride, magnesium sulfate, zinc sulfate and mixtures thereof.
Vorteilhafte Konservierungsmittel im Sinne der vorliegenden Erfindung sind beispielsweise Benzylalkohol, Sorbinsäure und dessen Salze, Formaldehydabspalter (wie z. B. Diazolidinylharnstoff (Handelsbezeichnung Germall II von ISP), Imidazolidinylharnstoff (Handelsbezeichnung Germall 115) oder DMDM Hydantoin, welches beispielsweise unter der Handelsbezeichnung Glydant™ von der Fa. Lonza erhältlich ist), Methylisothiazolinon und entsprechende Derivate (Handelsname Kathon CG), lodopropylbutylcarbamate (z. B. die unter den Handelsbezeichnungen Glycacil-L, Glycacil-S von der Fa. Lonza erhältlichen und/oder Dekaben LMB von Jan Dekker), Parabene (d. h. p-Hydroxybenzoesäurealkylester, wie Methyl-, Ethyl-, Propyl- und/oder Butylparaben), Phenoxyethanol, Ethanol, Triclosan, Benzoesäure und dergleichen mehr. Üblicherweise umfaßt das Konservierungssystem erfindungsgemäß ferner vorteilhaft auch Substanzen, die die Wirksamkeit von klassischen Konservierungsmitteln verbessern, wie beispielsweise Hexandiol, Pentandiol, Butylenglycol und Methylpropandiol.Advantageous preservatives for the purposes of the present invention are, for example, benzyl alcohol, sorbic acid and its salts, formaldehyde releasers (such as diazolidinyl urea (trade name Germall II from ISP), imidazolidinyl urea (trade name Germall 115) or DMDM hydantoin, which is available, for example, under the trade name Glydant ™ from available from Lonza), methylisothiazolinone and corresponding derivatives (trade name Kathon CG), iodopropylbutylcarbamate (eg those available under the trade names Glycacil-L, Glycacil-S from Lonza and / or Dekaben LMB from Jan Dekker) , Parabens (ie, p-hydroxybenzoic acid alkyl esters such as methyl, ethyl, propyl and / or butylparaben), phenoxyethanol, ethanol, triclosan, benzoic acid, and the like. The preservation system according to the invention furthermore advantageously also comprises substances which improve the effectiveness of classical preservatives, for example hexanediol, pentanediol, butylene glycol and methylpropanediol.
Es ist ebenfalls vorteilhaft, den Zubereitungen im Sinne der vorliegenden Erfindung übliche Antioxidantien zuzufügen. Erfindungsgemäß können als günstige Antioxidantien alle für kosmetische und/oder dermatologische Anwendungen geeigneten oder gebräuchlichen Antioxidantien verwendet werden.It is likewise advantageous to add conventional antioxidants to the preparations for the purposes of the present invention. According to the invention, all antioxidants which are suitable or customary for cosmetic and / or dermatological applications can be used as favorable antioxidants.
Die Menge der Antioxidantien (eine oder mehrere Verbindungen) in den Zubereitungen beträgt vorzugsweise 0,001 bis 30 Gew.-%, besonders bevorzugt 0,05 - 20 Gew.-%, insbesondere 1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung. The amount of antioxidants (one or more compounds) in the preparations is preferably from 0.001 to 30% by weight, particularly preferably from 0.05 to 20% by weight, in particular from 1 to 10% by weight, based on the total weight of the preparation ,
Besonders vorteilhaft im Sinne der vorliegenden Erfindung können Öl-lösliche Antioxidantien eingesetzt werden.Particularly advantageous for the purposes of the present invention, oil-soluble antioxidants can be used.
Besonders vorteilhaft im Sinne der vorliegenden Erfindung können wasserlösliche Antioxidantien eingesetzt werden, wie beispielsweise Vitamine, z. B. Ascorbinsäure und deren Derivate.Particularly advantageous for the purposes of the present invention, water-soluble antioxidants can be used, such as vitamins, eg. As ascorbic acid and its derivatives.
Bevorzugte Antioxidantien sind ferner Vitamin E (α-Tocopherol) und dessen Derivate.Preferred antioxidants are also vitamin E (α-tocopherol) and its derivatives.
Sofern die kosmetische oder dermatologische Zubereitung im Sinne der vorliegenden Erfindung eine Lösung oder Emulsion oder Dispersion darstellt, können als Lösungsmittel verwendet werden:
- - Wasser oder wäßrige Lösungen
- - Öle, wie Triglyceride der Caprin- oder der Caprylsäure, Fettsäureether wie Dicaprylether, Kohlensäureester wie Dicaprylylcarbonat, ferner natürlich Öle wie z.B. Rizinusöl oder Sonnenblumenöl;
- - Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugsweise Ester von Fettsäuren mit Alkoholen niedriger C-Zahl, z.B. mit Isopropanol, Propylenglykol oder Glycerin, oder Ester von Fettalkoholen mit Alkansäuren niedriger C-Zahl oder mit Fettsäuren;
- - Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugsweise Ethanol, Isopropanol, Propylenglykol, Glycerin, Ethylenglykol, Ethylenglykolmonoethyl- oder -monobutylether, Propylenglykolmonomethyl, -monoethyl- oder - monobutylether, Diethylenglykolmonomethyl- oder -monoethylether und analoge Produkte.
- - water or aqueous solutions
- Oils, such as triglycerides of capric or caprylic acid, fatty acid ethers, such as dicapryl ether, carbonic acid esters, such as dicaprylyl carbonate, and, of course, oils such as castor oil or sunflower oil;
- Fats, waxes and other natural and synthetic fatty substances, preferably esters of fatty acids with lower C-number alcohols, for example with isopropanol, propylene glycol or glycerol, or esters of fatty alcohols with lower C-number alkanoic acids or with fatty acids;
- Alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products.
Die Ölphase der Emulsionen, Oleogele bzw. Hydrodispersionen oder Lipodispersionen im Sinne der vorliegenden Erfindung wird vorteilhaft gewählt aus der Gruppe der Ester aus gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkancarbonsäuren einer Kettenlänge von 3 bis 30 C-Atomen und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen, aus der Gruppe der Ester aus aromatischen Carbonsäuren und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen. Solche Esteröle können dann vorteilhaft gewählt werden aus der Gruppe Isopropylmyristat, Isopropylpalmitat, Isopropylstearat, Isopropyloleat, n-Butylstearat, n-Hexyllaurat, n-Decyloleat, Isooctylstearat, Isononylstearat, Isononylisononanoat, 2-Ethylhexylpalmitat, 2-Ethylhexyllaurat, 2-Hexyldecylstearat, 2-Octyldodecylpalmitat, Oleyloleat, Oleylerucat, Erucyloleat, Erucylerucat sowie synthetische, halbsynthetische und natürliche Gemische solcher Ester, z.B. Jojobaöl.The oil phase of the emulsions, oleogels or hydrodispersions or lipodispersions in the context of the present invention is advantageously selected from the group of esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 3 to 30 carbon atoms and saturated and / or or unsaturated, branched and / or unbranched alcohols having a chain length of 3 to 30 carbon atoms, from the group of esters of aromatic carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of 3 to 30 carbon atoms. Such ester oils can then be advantageously selected from the group isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononyl isononanoate, 2-ethylhexyl palmitate, 2-ethylhexyl laurate, 2-hexyldecyl stearate, 2 Octyldodecyl palmitate, oleyl oleate, oleyl erucate, erucyl oleate, erucyl erucate and synthetic, semi-synthetic and natural mixtures of such esters, eg Jojoba oil.
Ferner kann die Ölphase vorteilhaft gewählt werden aus der Gruppe der verzweigten und unverzweigten Kohlenwasserstoffe und -wachse, der Silkonöle, der Dialkylether, der Gruppe der gesättigten oder ungesättigten, verzweigten oder unverzweigten Alkohole, sowie der Fettsäuretriglyceride, namentlich der Triglycerinester gesättigter und/oder ungesättigter, verzweigter und/oder unverzweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen. Die Fettsäuretriglyceride können beispielsweise vorteilhaft gewählt werden aus der Gruppe der synthetischen, halbsynthetischen und natürlichen Öle, z.B. Olivenöl, Sonnenblumenöl, Sojaöl, Erdnußöl, Rapsöl, Mandelöl, Palmöl, Kokosöl, Palmkernöl und dergleichen mehr.Furthermore, the oil phase can be advantageously selected from the group of branched and unbranched hydrocarbons and waxes, the silicone oils, the dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and the fatty acid triglycerides, in particular the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids of a chain length of 8 to 24, in particular 12 to 18 carbon atoms. For example, the fatty acid triglycerides can be advantageously selected from the group of synthetic, semi-synthetic and natural oils, e.g. Olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil, and the like.
Auch beliebige Abmischungen solcher Öl- und Wachskomponenten sind vorteilhaft im Sinne der vorliegenden Erfindung einzusetzen. Es kann auch gegebenenfalls vorteilhaft sein, Wachse, beispielsweise Cetylpalmitat, als alleinige Lipidkomponente der Ölphase einzusetzen.Any mixtures of such oil and wax components are also advantageous to use in the context of the present invention. It may also be advantageous, if appropriate, to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
Vorteilhaft wird die Ölphase gewählt aus der Gruppe 2-Ethylhexylisostearat, Octyldodecanol, Isotridecylisononanoat, Isoeicosan, 2-Ethylhexylcocoat, C12-15-Alkylbenzoat, Capryl-Caprinsäure-triglycerid, Dicaprylylether.The oil phase is advantageously selected from the group 2-ethylhexyl isostearate, octyldodecanol, isotridecyl isononanoate, isoeicosane, 2-ethylhexyl cocoate, C 12-15 -alkyl benzoate, caprylic-capric triglyceride, dicaprylyl ether.
Besonders vorteilhaft sind Mischungen aus C12-15-Alkylbenzoat und 2-Ethylhexylisostearat, Mischungen aus C12-15-Alkylbenzoat und Isotridecylisononanoat sowie Mischungen aus C12-15-Alkylbenzoat, 2-Ethylhexylisostearat und Isotridecylisononanoat. Particularly advantageous are mixtures of C 12-15 -alkyl benzoate and 2-ethylhexyl isostearate, mixtures of C 12-15 -alkyl benzoate and isotridecyl isononanoate and mixtures of C 12-15 -alkyl benzoate, 2-ethylhexyl isostearate and isotridecyl isononanoate.
Von den Kohlenwasserstoffen sind Paraffinöl, Squalan und Squalen vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden.Of the hydrocarbons, paraffin oil, squalane and squalene are to be used advantageously in the context of the present invention.
Vorteilhaft kann die Ölphase ferner einen Gehalt an cyclischen oder linearen Silikonölen aufweisen oder vollständig aus solchen Ölen bestehen, wobei allerdings bevorzugt wird, außer dem Silikonöl oder den Silikonölen einen zusätzlichen Gehalt an anderen Ölphasenkomponenten zu verwenden.Advantageously, the oil phase may further comprise a content of cyclic or linear silicone oils or consist entirely of such oils, although it is preferred to use an additional content of other oil phase components in addition to the silicone oil or silicone oils.
Vorteilhaft wird Cyclomethicon (Octamethylcyclotetrasiloxan) als erfindungsgemäß zu verwendendes Silikonöl eingesetzt. Aber auch andere Silikonöle sind vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden, beispielsweise Hexamethylcyclotrisiloxan, Polydimethylsiloxan, Poly(methylphenylsiloxan).Advantageously, cyclomethicone (octamethylcyclotetrasiloxane) is used as the silicone oil to be used according to the invention. However, other silicone oils are also advantageous for the purposes of the present invention, for example hexamethylcyclotrisiloxane, polydimethylsiloxane, poly (methylphenylsiloxane).
Besonders vorteilhaft sind ferner Mischungen aus Cyclomethicon und Isotridecylisononanoat, aus Cyclomethicon und 2-Ethylhexylisostearat.Also particularly advantageous are mixtures of cyclomethicone and isotridecyl isononanoate, cyclomethicone and 2-ethylhexyl isostearate.
Ganz besonders bevorzugte Ölkomponenten sind Octyldodecanol, Capryli/Capric-Triglycerid, Cyclometicone, Dimeticone, C12-15 Alkylbenzoat und Dicaprylylcarbonat.Very particularly preferred oil components are octyldodecanol, caprylic / capric triglyceride, cyclomethtrone, dimethicone, C12-15 alkyl benzoate and dicaprylyl carbonate.
Kosmetische Zubereitungen im Sinne der vorliegenden Erfindung können auch als Gele vorliegen, die neben einem wirksamen Gehalt am erfindungsgemäßen Wirkstoff und dafür üblicherweise verwendeten Lösungsmitteln, bevorzugt Wasser, noch organische und / oder anorganische Verdickungsmittel enthalten. Weiterhin sind diese Verdickungsmittel Bestandteil kosmetischer Emulsionen.Cosmetic preparations in the sense of the present invention can also be present as gels which, in addition to an effective content of the active ingredient according to the invention and solvents used for this purpose, preferably water, also contain organic and / or inorganic thickeners. Furthermore, these thickeners are part of cosmetic emulsions.
Vorteilhafte Verdickungsmittel für derartige Zubereitungen sind beispielsweise Copolymere aus C10-30-Alkylacrylaten und einem oder mehreren Monomeren der Acrylsäure, der Methacrylsäure oder deren Ester. Die INCI-Bezeichnung für solche Verbindungen ist „Acrylates/C 10-30 Alkyl Acrylate Crosspolymer“. Insbesondere vorteilhaft sind die Pemulen® Typen TR 1, TR 2 und TRZ von der Fa. Goodrich (Noveon).Advantageous thickeners for such preparations are, for example, copolymers of C 10-30 -alkyl acrylates and one or more monomers of acrylic acid, methacrylic acid or their esters. The INCI name for such compounds is "Acrylates / C 10-30 Alkyl Acrylate Crosspolymer". The Pemulen® types TR 1, TR 2 and TRZ from Goodrich (Noveon) are particularly advantageous.
Auch Carbopole sind vorteilhafte Gelbildner für derartige Zubereitungen. Carbopole sind Polymere der Acrylsäure, insbesondere auch Acrylat-Alkylacrylat-Copolymere. Vorteilhafte Carbopole sind beispielsweise die Typen 980, 981, 984 1342, 1382, 2984 und 5984. ebenso die ETD-Typen 2001, 2020, 2050 und Carbopol Ultrez 10, PVM/MA Decadien Crosspolymer (Handelsname Stabileze 06), Polyglycerylmethacrylat sowie Polyacrylamid. Weitere vorteilhafte Gelbildner für derartige Zubereitungen sind Xanthan Gummi, Polyvinylpyrrolidon, Cellulose Derivate, insbesondere Celluloseether wie zum Beispiel Hydroxypropylmethylcellulose, Stärke und Stärkederivate, Hyaluronsäure Johannisbrotkernmehl, Siliciumdioxid und Aluminiumsilikate.Carbopols are also advantageous gelling agents for such preparations. Carbopols are polymers of acrylic acid, especially acrylate-alkyl acrylate copolymers. Examples of advantageous carbopols are types 980, 981, 984 1342, 1382, 2984 and 5984. Likewise ETD types 2001, 2020, 2050 and Carbopol Ultrez 10, PVM / MA Decadiene Crosspolymer (trade name Stabileze 06), polyglyceryl methacrylate and polyacrylamide. Further advantageous gelling agents for such preparations are xanthan gum, polyvinylpyrrolidone, cellulose derivatives, in particular cellulose ethers such as, for example, hydroxypropylmethylcellulose, starch and starch derivatives, hyaluronic acid locust bean gum, silicon dioxide and aluminum silicates.
Das Verdickungsmittel ist in dem Gel, der Dispersion bzw. der Emulsion z.B. in einer Menge zwischen 0,01 und 5 Gew.-%, bevorzugt zwischen 0,1 und 2 Gew.-%, enthalten.The thickening agent is present in the gel, dispersion or emulsion e.g. in an amount of between 0.01 and 5% by weight, preferably between 0.1 and 2% by weight.
Als Treibmittel für aus Aerosolbehältern versprühbare kosmetische und/oder dermatologische Zubereitungen im Sinne der vorliegenden Erfindung sind die üblichen bekannten leichtflüchtigen, verflüssigten Treibmittel, beispielsweise Kohlenwasserstoffe (Propan, Butan, Isobutan) geeignet, die allein oder in Mischung miteinander eingesetzt werden können. Auch Druckluft ist vorteilhaft zu verwenden.Suitable propellants for sprayable from aerosol containers cosmetic and / or dermatological preparations in the context of the present invention, the usual known volatile, liquefied propellants, such as hydrocarbons (propane, butane, isobutane) are suitable, which can be used alone or in mixture with each other. Also, compressed air is advantageous to use.
Natürlich weiß der Fachmann, dass es an sich nichttoxische Treibgase gibt, die grundsätzlich für die Verwirklichung der vorliegenden Erfindung in Form von Aerosolpräparaten geeignet wären, auf die aber dennoch wegen bedenklicher Wirkung auf die Umwelt oder sonstiger Begleitumstände verzichtet werden sollte, insbesondere Fluorkohlenwasserstoffe und Fluorchlorkohlenwasserstoffe (FCKW).Of course, the person skilled in the art knows that there are per se nontoxic propellants which would in principle be suitable for the realization of the present invention in the form of aerosol preparations, but which should nevertheless be dispensed with because of a harmful effect on the environment or other concomitant circumstances, in particular fluorohydrocarbons and chlorofluorocarbons (US Pat. CFC).
Vorteilhaft ist es, den pH-Wert erfindungsgemäßer Zubereitungen im Bereich von 4,5 bis 7,5 zu puffern.It is advantageous to buffer the pH of preparations according to the invention in the range from 4.5 to 7.5.
Es folgen vorteilhafte Ausführungsbeispiele der vorliegenden Erfindung.Following are advantageous embodiments of the present invention.
Rezepturbeispiel: O/W Emulsion Formulation example: O / W emulsion
Rezepturbeispiel: (O/W-Emulsion)Recipe example: (O / W emulsion)
Rezepturbeispiel: (O/W-Emulsion)Recipe example: (O / W emulsion)
Rezepturbeispiel: (O/W-Emulsion)Recipe example: (O / W emulsion)
Claims (8)
Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102005029388.3A DE102005029388B4 (en) | 2005-06-23 | 2005-06-23 | Active ingredient combinations of glycopyrronium bromide and one or more partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid |
| BRPI0519481-4A BRPI0519481A2 (en) | 2004-12-27 | 2005-12-27 | glycopyrrolate in cosmetic preparations |
| EP05850500A EP1835812B1 (en) | 2004-12-27 | 2005-12-27 | Glycopyrrolate in cosmetic preparations |
| PCT/EP2005/057186 WO2006069998A2 (en) | 2004-12-27 | 2005-12-27 | Glycopyrrolate in cosmetic preparations |
| AT05850500T ATE520390T1 (en) | 2004-12-27 | 2005-12-27 | GLYCOPYRROLATE IN COSMETIC PREPARATIONS |
| US11/722,992 US8343467B2 (en) | 2004-12-27 | 2005-12-27 | Glycopyrrolate in cosmetic preparations |
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| DE102005029388.3A DE102005029388B4 (en) | 2005-06-23 | 2005-06-23 | Active ingredient combinations of glycopyrronium bromide and one or more partially neutralized esters of monoglycerides and / or diglycerides of saturated fatty acids with citric acid |
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| DE102005029388A1 DE102005029388A1 (en) | 2007-01-04 |
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| EP2191868A1 (en) * | 2008-11-28 | 2010-06-02 | Cognis IP Management GmbH | Ethylene oxide-free antiperspirant/deodorant preparations |
| DE102010022064A1 (en) * | 2010-05-31 | 2011-12-01 | Beiersdorf Ag | Deodorant or antiperspirant preparation with polyol partial ester |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19802205A1 (en) | 1998-01-22 | 1999-07-29 | Beiersdorf Ag | Cosmetic or dermatological composition with electrolyte-containing aqueous phase, stable against phase separation, e.g. sunscreens |
| US5962505A (en) | 1998-08-31 | 1999-10-05 | Bobrove; Arthur M. | Method for treating hot flashes in humans |
| DE10136404A1 (en) | 2001-07-26 | 2003-02-20 | Johannes Wohlrab | Topical medicament for treating or preventing hyperhidrosis, e.g. hyperhidrosis axillaris, comprises glycopyrrolate compound in gel and/or colloid-containing vehicle system |
| WO2003026585A2 (en) | 2001-09-26 | 2003-04-03 | Lukacsko Alison B | Compositions and methods for inhibiting eccrine perspiration in humans |
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| DE4343264A1 (en) * | 1993-12-17 | 1995-06-22 | Henkel Kgaa | Deodorising preparations |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19802205A1 (en) | 1998-01-22 | 1999-07-29 | Beiersdorf Ag | Cosmetic or dermatological composition with electrolyte-containing aqueous phase, stable against phase separation, e.g. sunscreens |
| US5962505A (en) | 1998-08-31 | 1999-10-05 | Bobrove; Arthur M. | Method for treating hot flashes in humans |
| DE10136404A1 (en) | 2001-07-26 | 2003-02-20 | Johannes Wohlrab | Topical medicament for treating or preventing hyperhidrosis, e.g. hyperhidrosis axillaris, comprises glycopyrrolate compound in gel and/or colloid-containing vehicle system |
| WO2003026585A2 (en) | 2001-09-26 | 2003-04-03 | Lukacsko Alison B | Compositions and methods for inhibiting eccrine perspiration in humans |
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