EP1406583A2 - Körperpflegemittel enthaltend folsäure - Google Patents
Körperpflegemittel enthaltend folsäureInfo
- Publication number
- EP1406583A2 EP1406583A2 EP02746199A EP02746199A EP1406583A2 EP 1406583 A2 EP1406583 A2 EP 1406583A2 EP 02746199 A EP02746199 A EP 02746199A EP 02746199 A EP02746199 A EP 02746199A EP 1406583 A2 EP1406583 A2 EP 1406583A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- oil
- folic acid
- water emulsion
- phase
- water
- 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.)
- Withdrawn
Links
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 title claims abstract description 190
- 235000019152 folic acid Nutrition 0.000 title claims abstract description 116
- 239000011724 folic acid Substances 0.000 title claims abstract description 104
- OVBPIULPVIDEAO-UHFFFAOYSA-N N-Pteroyl-L-glutaminsaeure Natural products C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-UHFFFAOYSA-N 0.000 title claims abstract description 85
- 229960000304 folic acid Drugs 0.000 title claims abstract description 85
- 239000007764 o/w emulsion Substances 0.000 claims abstract description 45
- 230000001329 hyperkeratotic effect Effects 0.000 claims abstract description 12
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 47
- 239000003921 oil Substances 0.000 claims description 31
- 239000000416 hydrocolloid Substances 0.000 claims description 29
- 239000003995 emulsifying agent Substances 0.000 claims description 28
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 27
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 claims description 26
- 239000000203 mixture Substances 0.000 claims description 24
- 229940088594 vitamin Drugs 0.000 claims description 20
- 229930003231 vitamin Natural products 0.000 claims description 20
- 235000013343 vitamin Nutrition 0.000 claims description 20
- 239000011782 vitamin Substances 0.000 claims description 20
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 19
- 238000000034 method Methods 0.000 claims description 17
- 229920002125 Sokalan® Polymers 0.000 claims description 16
- -1 fatty acid ester Chemical class 0.000 claims description 16
- 229940109239 creatinine Drugs 0.000 claims description 13
- 230000000694 effects Effects 0.000 claims description 12
- 150000002191 fatty alcohols Chemical class 0.000 claims description 12
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 11
- 239000000654 additive Substances 0.000 claims description 10
- 238000003756 stirring Methods 0.000 claims description 10
- 229920001285 xanthan gum Polymers 0.000 claims description 10
- 229960001631 carbomer Drugs 0.000 claims description 9
- 238000010438 heat treatment Methods 0.000 claims description 9
- 238000009281 ultraviolet germicidal irradiation Methods 0.000 claims description 9
- 235000019156 vitamin B Nutrition 0.000 claims description 9
- 239000011720 vitamin B Substances 0.000 claims description 9
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 8
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 8
- 230000000996 additive effect Effects 0.000 claims description 8
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 8
- 239000000194 fatty acid Substances 0.000 claims description 8
- 229930195729 fatty acid Natural products 0.000 claims description 8
- 230000008569 process Effects 0.000 claims description 8
- 238000011282 treatment Methods 0.000 claims description 8
- 239000002253 acid Substances 0.000 claims description 7
- 229920002678 cellulose Chemical class 0.000 claims description 7
- 239000001913 cellulose Chemical class 0.000 claims description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 6
- 150000003722 vitamin derivatives Chemical class 0.000 claims description 6
- 108010076525 DNA Repair Enzymes Proteins 0.000 claims description 5
- 102000011724 DNA Repair Enzymes Human genes 0.000 claims description 5
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims description 5
- 235000001014 amino acid Nutrition 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims description 5
- 235000018417 cysteine Nutrition 0.000 claims description 5
- 239000002480 mineral oil Substances 0.000 claims description 5
- 230000000699 topical effect Effects 0.000 claims description 5
- GJCOSYZMQJWQCA-UHFFFAOYSA-N 9H-xanthene Chemical class C1=CC=C2CC3=CC=CC=C3OC2=C1 GJCOSYZMQJWQCA-UHFFFAOYSA-N 0.000 claims description 4
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims description 4
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims description 4
- 150000001413 amino acids Chemical class 0.000 claims description 4
- 150000001720 carbohydrates Chemical class 0.000 claims description 4
- 229930195712 glutamate Natural products 0.000 claims description 4
- 229930182817 methionine Natural products 0.000 claims description 4
- 235000010446 mineral oil Nutrition 0.000 claims description 4
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims description 3
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims description 3
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 3
- 239000006185 dispersion Substances 0.000 claims description 3
- 229920000570 polyether Polymers 0.000 claims description 3
- 229920001296 polysiloxane Polymers 0.000 claims description 3
- 239000004721 Polyphenylene oxide Substances 0.000 claims description 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims description 2
- 239000010696 ester oil Substances 0.000 claims description 2
- 229920002545 silicone oil Polymers 0.000 claims description 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims description 2
- 239000007788 liquid Substances 0.000 abstract description 39
- 239000011159 matrix material Substances 0.000 abstract description 6
- 230000001684 chronic effect Effects 0.000 abstract 1
- 239000000839 emulsion Substances 0.000 description 67
- 239000012071 phase Substances 0.000 description 63
- 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 48
- 239000000047 product Substances 0.000 description 40
- 210000003491 skin Anatomy 0.000 description 33
- 235000019198 oils Nutrition 0.000 description 22
- 229940014144 folate Drugs 0.000 description 19
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 18
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 description 13
- 150000001875 compounds Chemical class 0.000 description 12
- 150000002224 folic acids Chemical class 0.000 description 12
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 11
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 9
- 244000027321 Lychnis chalcedonica Species 0.000 description 9
- 230000015572 biosynthetic process Effects 0.000 description 8
- 239000011726 vitamin B6 Substances 0.000 description 8
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 description 7
- 230000008901 benefit Effects 0.000 description 7
- 238000010348 incorporation Methods 0.000 description 7
- 238000002156 mixing Methods 0.000 description 7
- 239000000126 substance Substances 0.000 description 7
- 235000019158 vitamin B6 Nutrition 0.000 description 7
- GHOKWGTUZJEAQD-UHFFFAOYSA-N Chick antidermatitis factor Natural products OCC(C)(C)C(O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-UHFFFAOYSA-N 0.000 description 6
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 6
- 239000008346 aqueous phase Substances 0.000 description 6
- 239000004202 carbamide Substances 0.000 description 6
- 125000004432 carbon atom Chemical group C* 0.000 description 6
- 239000002537 cosmetic Substances 0.000 description 6
- CVSVTCORWBXHQV-UHFFFAOYSA-N creatine Chemical compound NC(=[NH2+])N(C)CC([O-])=O CVSVTCORWBXHQV-UHFFFAOYSA-N 0.000 description 6
- 238000004090 dissolution Methods 0.000 description 6
- 150000002148 esters Chemical class 0.000 description 6
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 6
- 229940011671 vitamin b6 Drugs 0.000 description 6
- 235000010493 xanthan gum Nutrition 0.000 description 6
- 239000000230 xanthan gum Substances 0.000 description 6
- 229940082509 xanthan gum Drugs 0.000 description 6
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 5
- UDMBCSSLTHHNCD-KQYNXXCUSA-N adenosine 5'-monophosphate Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@H]1O UDMBCSSLTHHNCD-KQYNXXCUSA-N 0.000 description 5
- 235000010980 cellulose Nutrition 0.000 description 5
- 235000005911 diet Nutrition 0.000 description 5
- 239000000284 extract Substances 0.000 description 5
- 235000013305 food Nutrition 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 238000004519 manufacturing process Methods 0.000 description 5
- 230000004060 metabolic process Effects 0.000 description 5
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 description 5
- 235000021468 vitamin B8 Nutrition 0.000 description 5
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 description 4
- QFOHBWFCKVYLES-UHFFFAOYSA-N Butylparaben Chemical compound CCCCOC(=O)C1=CC=C(O)C=C1 QFOHBWFCKVYLES-UHFFFAOYSA-N 0.000 description 4
- 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 4
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 4
- 229930003571 Vitamin B5 Natural products 0.000 description 4
- 238000004220 aggregation Methods 0.000 description 4
- 230000009286 beneficial effect Effects 0.000 description 4
- FAPWYRCQGJNNSJ-UBKPKTQASA-L calcium D-pantothenic acid Chemical compound [Ca+2].OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O.OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O FAPWYRCQGJNNSJ-UBKPKTQASA-L 0.000 description 4
- 229960002079 calcium pantothenate Drugs 0.000 description 4
- 150000004665 fatty acids Chemical class 0.000 description 4
- 229930182478 glucoside Natural products 0.000 description 4
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 4
- 229960003512 nicotinic acid Drugs 0.000 description 4
- WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 description 4
- 229960005323 phenoxyethanol Drugs 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 238000012545 processing Methods 0.000 description 4
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 4
- 235000009492 vitamin B5 Nutrition 0.000 description 4
- 239000011675 vitamin B5 Substances 0.000 description 4
- 235000004866 D-panthenol Nutrition 0.000 description 3
- 239000011703 D-panthenol Substances 0.000 description 3
- 230000005778 DNA damage Effects 0.000 description 3
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- 108090000790 Enzymes Proteins 0.000 description 3
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- FDJOLVPMNUYSCM-WZHZPDAFSA-L cobalt(3+);[(2r,3s,4r,5s)-5-(5,6-dimethylbenzimidazol-1-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl] [(2r)-1-[3-[(1r,2r,3r,4z,7s,9z,12s,13s,14z,17s,18s,19r)-2,13,18-tris(2-amino-2-oxoethyl)-7,12,17-tris(3-amino-3-oxopropyl)-3,5,8,8,13,15,18,19-octamethyl-2 Chemical compound [Co+3].N#[C-].N([C@@H]([C@]1(C)[N-]\C([C@H]([C@@]1(CC(N)=O)C)CCC(N)=O)=C(\C)/C1=N/C([C@H]([C@@]1(CC(N)=O)C)CCC(N)=O)=C\C1=N\C([C@H](C1(C)C)CCC(N)=O)=C/1C)[C@@H]2CC(N)=O)=C\1[C@]2(C)CCC(=O)NC[C@@H](C)OP([O-])(=O)O[C@H]1[C@@H](O)[C@@H](N2C3=CC(C)=C(C)C=C3N=C2)O[C@@H]1CO FDJOLVPMNUYSCM-WZHZPDAFSA-L 0.000 description 3
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- ZQCIPRGNRQXXSK-UHFFFAOYSA-N 1-octadecoxypropan-2-ol Chemical compound CCCCCCCCCCCCCCCCCCOCC(C)O ZQCIPRGNRQXXSK-UHFFFAOYSA-N 0.000 description 2
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- 235000021122 unsaturated fatty acids Nutrition 0.000 description 1
- 229940035893 uracil Drugs 0.000 description 1
- 239000010913 used oil Substances 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 238000011179 visual inspection Methods 0.000 description 1
- 208000002670 vitamin B12 deficiency Diseases 0.000 description 1
- 235000011912 vitamin B7 Nutrition 0.000 description 1
- 239000011735 vitamin B7 Substances 0.000 description 1
- 208000030401 vitamin deficiency disease Diseases 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/0295—Liquid crystals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/06—Emulsions
- A61K8/062—Oil-in-water emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
-
- 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
- A61Q19/004—Aftersun preparations
Definitions
- the invention concerns an oil-in water emulsion, said oil-in-water emulsion for cosmetical use, a process to prepare said emulsion, a premix for said oil-in-water emulsion and a two chamber dispenser.
- the US Food and Nutrition Board has suggested to increase the recommended folate intake for adults to 400 micrograms per day from the previous 200 microgram per day.
- the reason for the widespread occurrence of folate deficiency is the absence in humans of enzymes to synthesize folate from the basic building blocks so that there is a total dependence upon dietary intake.
- fruit and vegetables contain relatively high
- topically applied folate or folic acid reports describing the effects of topically applied folate or folic acid. It is even unknown if topically applied folates or folic acid can penetrate the skin to add to the subcutaneous folate levels.
- Folate or its synthetic precursor folic acid are also known as vitamin B9 and these compounds thus belong to the group of B-vitamins. Folate (i.e. vitamin B9) plays an important role in the one- carbon mechanism required for DNA and RNA synthesis
- vitamin B12 cyanobalamin
- vitamin B6 pyridoxine
- vitamin B12 plays a crucial role and like folate, vitamin B 12 deficiencies have also been linked with inadequate DNA metabolism and increased chromosome damages (J Sci Food Agric 80: 795-824 (2000)).
- Vitamin B6 is involved as a cofactor in the enzymatic transformation of homocysteine
- vitamin B3 (niacin)
- B-vitamins such as vitamin B5 (panthothenic acid) and vitamin B8 (biotin or
- vitamin H have no known direct effects on the metabolism of DNA, but exhibit several beneficial topical effects if incorporated in personal care products.
- proven benefits of vitamin B5 include skin moisturisation and anti-
- Vitamin B8 is associated with the process of cell development and lipid metabolism. In personal care
- topically applied vitamins are capable of normalizing the microbiological flora of the skin, for example in relation to the
- At least one of the immiscible liquids is present in a
- amphiphilic products are usually referred to as "emulsifiers”.
- Multi-phase systems are usually stabilised by self-aggregation of the amphiphilic products.
- This self-aggregation is characterised by a structured agglomeration of the amphiphilic products to such an extent that hydrophilic-hydrophobic repulsion is
- Emulsifiers an Alternative to Traditional Emulsifiers based on Stability of Multi-Phase
- micelles Such micelles are frequently encountered in wash-active products such as shampoos, detergents, etc. and are not relevant within the scope of the present invention.
- Such plate-like structures are characterised by a double layer of head-tail/ tail-head oriented amphiphilic molecules that physically separate the dispersed droplets and thus stabilise the emulsion.
- liquid crystalline double layer formed is possible using advanced methods but is usually done by visually estimating the concentration of the Maltese crosses or oily streaks
- consistency enhancers such as fatty acids or hydroxy fatty acids
- the liquid crystalline double layer is blanketed with a suitable rheological additive usually a hydrocolloid.
- a suitable rheological additive usually a hydrocolloid.
- the interaction by and between the liquid crystalline double layer and the hydrocolloid is based on Vanderwaals interactions.
- Suitable hydrocolloids are polysaccharides such as tree and
- shrub exudates like gum arabic, fermentation products such as xanthan gum, seed extracts such as guar gum, seaweed extracts such as alginates, plant derived materials such as pectins, starches, cellulose or cellulose derivatives such as hydroxy ethyl cellulose.
- synthetic rheological additives such acrylic homo- and copolymers, and
- modified clays such as smectites, hectorites, bentonites, hydrated silica and fumed silica
- Personal care products and especially skin care products are usually based upon very
- Water (O/W) emulsions are typically prepared by dissolving the hydrocolloid as well as
- the other water soluble components for example water-soluble vitamins belonging to the group of B-vitamins, in the water phase.
- the suitable emulsifiers are dissolved in the water phase.
- oil phase and then the oil phase is added to the water phase (usually at elevated
- a suitable homogeniser such as a rotor-stator mixer at high velocity.
- folic acid cannot be incorporated in a stable and bio-available form. In later life the epidermal skin can reveal several types of imperfections such as general
- blemishes can include small spots with a
- erythrosis as well as epidermal lesions known as maculae, naevi, ulcers, scales and local hyperkeratosis. Blemishes may also occur on the scalp. However, blemishes occur, or
- B-vitamins are useful to treat tactility or visibility of superficial skin blemishes or to treat tactility or visibility of
- the invention provides therefore an oil-in-water emulsion of the type stated in the preamble comprising substantially dissolved folic acid and a hydrocolloid, with the proviso that this oil-in-water emulsion does not contain L-arginin or derivatives thereof.
- the folic acid is preferably present in an amount of 0.01 - 0.5 wt%, preferably in an
- hydrocolloid is preferably selected of the
- the hydrocolloid is present in an amount of of 0.01 - 2 wt%, more preferably in an amount of 0.1 - 0.5 wt%.
- the oil-in-water emulsion comprises as further additive one or more amino acids, preferably selected from the group consisting of glutamate, methionine, cysteine
- the oil-in-water emulsion is especially suitable for cosmetical use, more especially for topical use, preferably for one or more of the following treatments:
- the present invention provides furthermore a process to prepare an oil-in-water
- emulsion according to the invention by a. preparing an oil phase by heating cosmetically acceptable oil or a mixture of
- cosmetically acceptable oils at least one cosmetically acceptable emulsifier and at least one cosmetically acceptable polar wax to a temperature of about 50 - 90 °C, preferably
- hydrocolloid in water and heating this dispersion to about 50 - 90 °C, preferably
- preparing an aqueous folic acid phase by dissolving folic acid either in water adjusted at a pH of 0.5 - 3 or in water with creatinine in an amount of at least 3 times the amount of folic acid and
- step c preferably the amount of creatinine applied is at least 1 gr per 0.5 g of
- folic acid in 10 gr of water and the amount of ureum applied is at least 5 gr per 0,5 gr of folic acid in 10 gr of water.
- Acidification occurs preferably by using an acid selected from the group consisting of citric acid, acetic acid, phosphoric acid or hydrochloric acid.
- the oil phase is prepared comprising oil selected from the group consisting of
- an ester oil a mineral oil, a natural triglyceride, a silicone oil, or a mixture thereof. More
- oil phase is prepared comprising an emulsifier selected from the group
- oil phase consisting of an alkoxylated fatty alcohol, a silicone polyether, a fatty acid ester of a polyglycerin or a carbohydrate, or a mixture thereof.
- oil phase is prepared comprising as polar wax a fatty alcohol.
- aqueous hydrocolloid phase is prepared from a hydrocolloid selected
- the invention also provides a premix for the oil-in water emulsion according to the invention consisting substantially of a solution of folic acid at a pH of about 0.5 - 3 or
- the invention provides a two-chamber dispenser with in one chamber an oil-in- water emulsion according to the present invention and in the second chamber one or
- Personal care products are products that are applied to skin, hair, nails and mucous
- Emulsions are defined as systems of at least two mutually immiscible liquids whereby at least one of these liquids is present in a finely divided state in at least one of
- Oil-in-Water (O/W) emulsions are considered in which the water phase is the continuous phase and the oil phase the dispersed phase.
- oils are suitable for the incorporation into O/W emulsions intended for personal
- Examples are mono- or diesters of linear or branched mono- or
- acids as for example methyl laureate, oleate and erucate as well as isopropyl palmitate, myristate, stearate and isopropyloleate also form suitable oils.
- suitable mono esters are for example n-butylstearate, n-hexyllaureate, n-decyloleate, isooctylstearate,
- Di-n-butyl adipate, di-(2-hehexyldecyl)-succinate, ethyleneglycoldioleate, propylene glycol-di-(2-ethylhexanoate and butane diol-di-isostearate can also be used as well as mineral oils, sillicon oils and naturally occurring oils such as olive, sunflower,
- structures include ethoxylated/propoxylated fatty alcohols, ethers of fatty alcohols and
- copolymers of ethylene oxide, propylene oxide, tetrahydrofuran, and combinations thereof are also included.
- electrically charged emulsifiers form a liquid crystalline bilayer such as lecithins and kephalins (1,2-diacyl glycerophosphates, as a condensate with serine,
- inositol, choline or monoethanolamine or other phospholipids or sphingolipids or
- glycolipids are glycolipids.
- these foreign chemical compounds should preferably be dissolved in the liquid crystalline double layer. For example, it has been shown that
- corticosteroids can be dissolved in a double layer formed by lecithin.
- hydrophilic substances with a conflicting dielectricum may molecularly dissolve in particular double layers while substances with a non-conflicting dielectricum may not.
- hydrophilic substances with a conflicting dielectricum may molecularly dissolve in particular double layers while substances with a non-conflicting dielectricum may not.
- dissolved in the liquid crystalline double layer comprise alkyl glucosides such lauryl,
- polyglyceryl esters and ethers of common fatty acids and fatty alcohols Preferred
- emulsifiers enabling the formation of emulsions containing dissolved folic acid are fatty acid esters of polyglycerin or carbohydrates, ethoxylated fatty alcohols and silicone polyethers. Most preferred emulsifyers enabling the formation of emulsions containing
- the folic acid added can be substantially dissolved in the liquid crystalline layers of the emulsion.
- substantially dissolved meaning that less than 10 %, preferably less than 1 % of folic acid added is visible as crystallites in the final emulsion as judged by optical microscopy (magnification 200-400 x) in combination with polarized light.
- a liquid phase is prepared in which the folic acid is properly dissolved.
- folic acid is unsoluble in water but can be dissolved to some extent in boiling water or under alkaline or acidic conditions.
- an aqueous phase can be prepared under mildly acidic conditions and
- processing temperatures between 50 to 90 degrees C, preferably 60 to 80 degrees C that allows the incorporation of relatively high amounts of folic acid in a substantially dissolved form into O/W emulsions. More surprisingly we have found that the
- incorporation of either urea or creatinine into the aqueous phase allows the dissolution of high amounts of folic acid under near neutral pH conditions enabling the preparation of O/W emulsions containing substantially dissolved folic acid. For example dissolving
- O/W emulsions according to the invention may incorporate folic acid in quantities that range from 0.1 microgram g emulsion to 5
- liquid crystalline double layers holding the folic acid and formed by the selected emulsifiers are reinforced by a suitable
- hydrocolloid or a mixture of suitable hydrocolloids.
- suitable hydrocolloids include
- polysaccharides such as tree and shrub exudates (karaya gum, tragacanth gum, gum arabic, gum ghatti, etc), fermentation products such as xanthan gum, seed extracts such as guar gum (and derivatives), locust bean gum, quince seed gum, psyllium seed gum,
- seaweed extracts such as alginates (and esters thereof) and
- carrageenan (various forms), agar-agar, pectins, starches, cellulose derivatives such as
- methylcellulose hydroxyethylcellulose, hydroxypropyl methylcellulose.
- synthetic hydrocolloids such acrylic homo- and copolymers, and modified clays such as smectites, hectorites, bentonites, hydrated silica and fumed silica are useful. Preferred
- carbomers are carbomers, alkyl modified carbomers, xanthan gum, locust bean gum,
- hydroxyethylcellulose hydroxypropylcellulose and hydroxypropyl methylcellulose.
- concentration of thesehydrocolloids may vary depending on the nature of the
- hydrocolloid chosen but typically ranges from 0.01-2.00 %.
- an oil phase such as mineral oil, isopropyl stearate, isopropyl palmitate, caprylic/capric triglyceride, cyclopentasiloxane( 1-40%), a selected emulsifier
- cetearyl glucoside/cetearyl alcohol 0.5-15%, preferably 2.5%) and folic acid
- compositions are added to stabilise the emulsion or to improve the performance of the final personal care product, for example consistency enhancers such as fatty alcohols or hydroxy fatty alcohols of 12 to 22,
- a suitable hydrocolloid such as xanthan gum (0.05-
- smoothing of the skin such as mineral hydrocarbons, fatty acid esters, polydimethylsiloxanes, vegetable oils, ethoxylated or propoxylated fatty alcohols, benzoic acid esters etc (0.1-20 %), humectants such as alcohols and/or polyols such as
- glycols glycerol, sorbitol, methylglucose, polyglycerol or polysaccharides and
- ethoxylates/ propoxylates thereof 0.05-20%), cosmetically acceptable preservatives such as parabene cocktails supported by co-preservatives (0.1-1.0 %) and cosmetic actives such as vitamins, UV filters such as octylmethoxycinnamates or titanium
- DNA repair enzymes such as photolyases or bacteriophage T4 endonuclease V (Jean Krutmann, Skin Pharmacol Appl Skin Physiol
- the emulsion can be made in a temperature range of 30-90 °C, preferably 55-80 °C, in a pH range of 4.0-9.0,
- the emulsion obtained will contain large numbers of liquid crystalline
- samples of the emulsions have been applied daily and for extended periods of time on the skin of a
- verruceous tissue was also found to decline as the result of the regular exposure to the folic acid containing emulsion according to the invention.
- synergistically working vitamins are the water-soluble vitamins of the B-group which include vitamin
- B12 cyanobalamin
- vitamin B6 pyridoxol
- vitamin B3 niacin
- vitamin B5 panthothenic acid or its precursor panthenol
- vitamin B8 biotin
- vitamins B3, B6 and B 12 are vitamins B3, B6 and B 12. Suitable concentrations of these vitamins in the end
- vitamins into the liquid crystalline double layer i.e. these vitamins can be added to the
- methionine, cysteine and serine can be added for improved performance of the final product.
- Arlatone, Arlamol and Estol are registered trademarks of Uniqema; Glucam is a registered trademark of Union Carbide c/o Amerchol; Phenonip & Nipaguard are registered trademarks of NIP A Laboratories; Rhodicare is a registered trademark of Rhodia; Myritol and Lanette are registered trademarks of Cognis; Dow Corning is a registered trademark of Dow Chemical. Folic acid was obtained from E.Merck, Darmstadt, Germany.
- phase A ARLATONE 2121 is mixed with water and heated to 85-90°C. A gel will be formed. The gel is cooled to 60°C. Propylene glycol and Glucam E20 are added and mixed until homogeneous. Phenonip and Nipaguard DCB are added.
- Rhodicare D is dispersed in water and heated to 60°C while stirring gently.
- Phase B then added to phase A and stirred until homogeneous. The temperature is maintained at 60°C.
- Phase C is prepared by heating the folic acid plus the 10% citric acid to 80 degrees and then adding the demineralised water at a temperature of 60°C while mixing gently. Phase C is then added to phase ⁇ A+B ⁇ while stirring gently. The gel is monitored by microscope (100-400times magnification) for the absence of crystallites of folic acid.
- Phase D is prepared by heating and mixing to 60°C. Phase D is then added to phase ⁇ A+B+C ⁇ without mixing. The mixture is homogenized during 20 seconds and the emulsion is subsequently stirred until ambient temperature has been reached.
- the emulsion obtained After cooling down the emulsion obtained has a viscosity of 12.500 cPs Brookfield viscosity (S5; 20 rpm; 20°C) and a pH of 6,15.
- the emulsion is evaluated microscopically for the absence of crystallites and the presence of "Maltese crosses". If crystallites are present, step 4 of the procedure has not been performed up to the requirements and it is recommended to increase the temperature of phase C and phase ⁇ A+B ⁇ just before mixing to 80 degrees C.
- the solution of 10% citric acid can be replaced by dilute phosphoric or hydrochloric acid to obtain a clear phase C at a pH of 0.5 to 1.0. If no or little Maltese crosses can be observed, the liquid crystalline phase has not been formed.
- TNCI Caprylic/Capric Triglyceride ARLAMOL® E 4.00 %
- Phase-F PRICERINE 9099 5.00 %
- Brij, Arlamol, Pricerine and Estol are registered trademarks of Uniqema; Glucam is a registered trademark of Union Carbide c/o Amerchol ; Phenonip & Nipaguard are registered trademarks of NIPA Laboratories; Carbopol is a registered trademark of BF Goodrich; Myritol and Lanette are registered trademarks of Cognis; Dow Coming is a registered trademark of Dow Chemical. Folic acid was obtained from E.Merck, Darmstadt, Germany.
- PROCEDURE
- phase A BRIJ 721 is mixed with water and heated to 75-80°C. A low viscous semi-transparent solution will be formed. The solution is cooled to 60°C. Propylene glycol and Glucam E20 are added and mixed until homogeneous. Phenonip and Nipaguard DCB are added.
- Rhodicare D is dispersed in water, and subsequently Carbopol
- ETD2020 and Carbopol 2050 are dispersed. The dispersion is heated to 60°C while stirring gently. 2 Phase B is added to phase A and stirred until homogeneous. The temperature is maintained at 60°C.
- Phase C is prepared by heating the folic acid plus the 10% citric acid to 80 degrees and then adding the demineralised water at a temperature of 60°C while mixing gently. Phase C is added to phase ⁇ A+B ⁇ while stirring gently. The mixture is homogenized during 20 seconds and the emulsion is subsequently stirred for 5 minutes, and phase D is added. The temperature of the emulsion is maintained at 60°C while stirring during 30 minutes.
- phase E The sodium hydroxide solution (phase E) is added to neutralize the acrylic resins present.
- phase F is added while stirring gently.
- the emulsion is cooled to ambient temperature while mixing gently.
- PRODUCT EVALUATION The emulsion obtained has a viscosity of 10.300 cPs Brookfield viscosity (S5; 20 rpm; 20°C) and a pH of 5,80.
- the emulsion is evaluated microscopically for the absence of crystallites and the occurrence of Maltese crosses. If crystallites are present, step 4 of the procedure has not been performed up to the requirements and it is recommended to increase the temperature of phase C and phase ⁇ A+B ⁇ just before mixing to 80 degrees C.
- the solution of 10% citric acid can be replaced by dilute phosphoric or hydrochloric acid to obtain a clear phase C at a pH of 0.5 to 1.0. If no or few Maltese crosses are observed, the liquid crystalline phase has not been formed.
- EXAMPLE 3 The following formula illustrates the composition and production of a cosmetic formulation in which folic acid has been dissolved in an aqueous phase using creatinine
- ABIL ® , TEGINACID ® , TEGO ® ' TEGIN ® and COSMOCAIR ® are registered trademarks of Goldschmidt AG, Essen, Germany.
- PROCEDURE 1. Phase A and Phase B are heated to 70 °C and combined without stirring.
- the stability of the emulsion can be improved by increasing the concentration of either the polar wax or the hydrocolloid or both.
- the tactility as well as colour of the spots was found to be reduced and much more in line with the touch and complexion of the surrounding, normal skin.
- the epidermis of the skin exhibited a softer touch and featured a visibly less scaly character.
- provitamin B5 in the aqueous phase A male person of 48 years old with a hyperkeratotic area on one of his hands resulting from the handling of benzedine powder for a limited period of time some 30 years ago, was asked to use an emulsion according to the formula as provided in Example 2.
- Example 1 A male person of 52 years old with a small verrucous outgrowth on his face was asked to use an emulsion according to the formula provided in Example 1.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Dispersion Chemistry (AREA)
- Crystallography & Structural Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Cosmetics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02746199A EP1406583A2 (de) | 2001-07-10 | 2002-07-09 | Körperpflegemittel enthaltend folsäure |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01202646A EP1275369A1 (de) | 2001-07-10 | 2001-07-10 | Folsäure enthaltende Körperpflegemittel |
| EP01202646 | 2001-07-10 | ||
| EP02746199A EP1406583A2 (de) | 2001-07-10 | 2002-07-09 | Körperpflegemittel enthaltend folsäure |
| PCT/NL2002/000449 WO2003005974A2 (en) | 2001-07-10 | 2002-07-09 | Folic acid containing personal care product |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EP1406583A2 true EP1406583A2 (de) | 2004-04-14 |
Family
ID=8180625
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP01202646A Withdrawn EP1275369A1 (de) | 2001-07-10 | 2001-07-10 | Folsäure enthaltende Körperpflegemittel |
| EP02746199A Withdrawn EP1406583A2 (de) | 2001-07-10 | 2002-07-09 | Körperpflegemittel enthaltend folsäure |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP01202646A Withdrawn EP1275369A1 (de) | 2001-07-10 | 2001-07-10 | Folsäure enthaltende Körperpflegemittel |
Country Status (6)
| Country | Link |
|---|---|
| EP (2) | EP1275369A1 (de) |
| JP (1) | JP2004536837A (de) |
| CN (1) | CN1525848A (de) |
| AU (1) | AU2002315952A1 (de) |
| BR (1) | BR0210890A (de) |
| WO (1) | WO2003005974A2 (de) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102006032413A1 (de) * | 2006-07-13 | 2008-01-17 | Beiersdorf Ag | Kosmetische oder dermatologische Zubereitungen mit einem Gehalt an Folsäure und einem oder mehreren Polyolen |
| CN101862274B (zh) * | 2010-05-28 | 2012-06-06 | 骆琦 | 一种含有叶酸的护肤品组合物及其制备方法 |
| CN101862275B (zh) * | 2010-05-28 | 2011-09-28 | 骆琦 | 一种含有叶酸的清洁护肤品组合物及其制备方法 |
| EP3775116A4 (de) * | 2018-04-05 | 2022-03-23 | Bausch Health Ireland Limited | Systeme zur abgabe einer polymeremulsion |
| CN112336644A (zh) * | 2019-08-07 | 2021-02-09 | 北京大学 | 叶酸-金属离子组合物及其制备方法和在防晒中的用途 |
| CN115414274B (zh) * | 2022-09-29 | 2024-09-10 | 宁波博雅格致健康科技有限公司 | 叶酸银离子材料在制备头皮护理组合物中的应用、头皮护理组合物和制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR6224M (de) * | 1966-08-23 | 1968-08-05 | ||
| JPS59173124A (ja) * | 1983-03-19 | 1984-10-01 | Shiseido Co Ltd | 乳化組成物 |
| JPH0748991B2 (ja) * | 1984-08-29 | 1995-05-31 | 日本油脂株式会社 | 経管栄養組成物 |
| LU87145A1 (fr) * | 1988-02-26 | 1989-09-20 | Oreal | Methode pour ameliorer l'aspect esthetique de la peau a l'aide de melanges polyvitaminiques |
| DE4341001A1 (de) * | 1993-12-02 | 1995-06-08 | Beiersdorf Ag | Topische Zubereitungen mit einem Gehalt an L-Arginin |
| DE4405545A1 (de) * | 1994-02-22 | 1995-08-31 | Dietl Hans | Fettlösliche Vitamine enthaltende Zubereitung zur oralen Applikation |
| EP0704199B1 (de) * | 1994-04-20 | 2003-03-19 | Mitsubishi Pharma Corporation | Transfusionsbehälter,transfusionspräparat sowie umfassendes,vitamine enthaltendes,kaloriereiches präparat |
| DE10036797A1 (de) * | 2000-07-28 | 2002-02-07 | Beiersdorf Ag | Verwendung von Kombinationen mit einem Gehalt an Carnitinen |
| DE10062401A1 (de) * | 2000-12-14 | 2002-06-20 | Beiersdorf Ag | Verwendung von Folsäure und/oder deren Derivaten zur Herstellung kosmetischer oder dermatologischer Zubereitungen zur Prophylaxe von Schäden an der hauteigenen DNA und/oder zur Reparatur bereits eingetretener Schäden an der hauteigenen DNA |
-
2001
- 2001-07-10 EP EP01202646A patent/EP1275369A1/de not_active Withdrawn
-
2002
- 2002-07-09 JP JP2003511782A patent/JP2004536837A/ja active Pending
- 2002-07-09 AU AU2002315952A patent/AU2002315952A1/en not_active Abandoned
- 2002-07-09 WO PCT/NL2002/000449 patent/WO2003005974A2/en not_active Ceased
- 2002-07-09 BR BR0210890-9A patent/BR0210890A/pt not_active Application Discontinuation
- 2002-07-09 CN CNA028139135A patent/CN1525848A/zh active Pending
- 2002-07-09 EP EP02746199A patent/EP1406583A2/de not_active Withdrawn
Non-Patent Citations (1)
| Title |
|---|
| See references of WO03005974A3 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1275369A1 (de) | 2003-01-15 |
| WO2003005974A2 (en) | 2003-01-23 |
| AU2002315952A1 (en) | 2003-01-29 |
| JP2004536837A (ja) | 2004-12-09 |
| CN1525848A (zh) | 2004-09-01 |
| WO2003005974A3 (en) | 2003-09-04 |
| BR0210890A (pt) | 2004-06-22 |
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