MXPA98001116A - Compositions containing hydroxyacy or retinoi - Google Patents
Compositions containing hydroxyacy or retinoiInfo
- Publication number
- MXPA98001116A MXPA98001116A MXPA/A/1998/001116A MX9801116A MXPA98001116A MX PA98001116 A MXPA98001116 A MX PA98001116A MX 9801116 A MX9801116 A MX 9801116A MX PA98001116 A MXPA98001116 A MX PA98001116A
- Authority
- MX
- Mexico
- Prior art keywords
- composition
- acid
- irritation
- tri
- cum
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 108
- 239000000284 extract Substances 0.000 claims abstract description 43
- 241001180933 Trichodesma <angiosperm> Species 0.000 claims abstract description 38
- 150000001261 hydroxy acids Chemical class 0.000 claims abstract description 21
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 claims description 33
- 208000003251 Pruritus Diseases 0.000 claims description 26
- AEMRFAOFKBGASW-UHFFFAOYSA-N glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 26
- 239000004615 ingredient Substances 0.000 claims description 25
- 229960003471 retinol Drugs 0.000 claims description 17
- 235000020944 retinol Nutrition 0.000 claims description 17
- 239000011607 retinol Substances 0.000 claims description 17
- 239000002537 cosmetic Substances 0.000 claims description 15
- 230000000699 topical Effects 0.000 claims description 9
- 150000004492 retinoid derivatives Chemical class 0.000 claims description 6
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 5
- 235000014655 lactic acid Nutrition 0.000 claims description 5
- 239000004310 lactic acid Substances 0.000 claims description 5
- SHGAZHPCJJPHSC-NWVFGJFESA-N Tretinoin Chemical compound OC(=O)/C=C(\C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-NWVFGJFESA-N 0.000 claims description 4
- 229960001727 Tretinoin Drugs 0.000 claims description 4
- 229930002330 retinoic acid Natural products 0.000 claims description 4
- WWDMJSSVVPXVSV-YCNIQYBTSA-N Retinyl ester Chemical compound CC1CCCC(C)(C)C1\C=C\C(\C)=C\C=C\C(\C)=C\C(O)=O WWDMJSSVVPXVSV-YCNIQYBTSA-N 0.000 claims description 3
- 229930002945 all-trans-retinaldehyde Natural products 0.000 claims description 2
- 235000020945 retinal Nutrition 0.000 claims description 2
- 239000011604 retinal Substances 0.000 claims description 2
- 230000002207 retinal Effects 0.000 claims description 2
- NCYCYZXNIZJOKI-OVSJKPMPSA-N retinal group Chemical group C\C(=C/C=O)\C=C\C=C(\C=C\C1=C(CCCC1(C)C)C)/C NCYCYZXNIZJOKI-OVSJKPMPSA-N 0.000 claims description 2
- 125000002523 retinol group Chemical group 0.000 claims 1
- 239000002085 irritant Substances 0.000 abstract description 8
- 239000003795 chemical substances by application Substances 0.000 abstract description 6
- 210000003491 Skin Anatomy 0.000 description 30
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 19
- 206010015150 Erythema Diseases 0.000 description 15
- 231100000321 erythema Toxicity 0.000 description 15
- 239000000463 material Substances 0.000 description 14
- 229940098330 GAMMA LINOLEIC ACID Drugs 0.000 description 13
- VZCCETWTMQHEPK-QNEBEIHSSA-N γ-Linolenic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/CCCCC(O)=O VZCCETWTMQHEPK-QNEBEIHSSA-N 0.000 description 13
- 241001072256 Boraginaceae Species 0.000 description 11
- 235000007689 Borago officinalis Nutrition 0.000 description 11
- 238000011156 evaluation Methods 0.000 description 10
- 206010040880 Skin irritation Diseases 0.000 description 9
- 239000002253 acid Substances 0.000 description 9
- 235000021324 borage oil Nutrition 0.000 description 8
- 231100000475 skin irritation Toxicity 0.000 description 8
- 230000036556 skin irritation Effects 0.000 description 8
- -1 GLA Chemical class 0.000 description 7
- QIQXTHQIDYTFRH-UHFFFAOYSA-N Stearic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 7
- 239000004480 active ingredient Substances 0.000 description 7
- 239000007764 o/w emulsion Substances 0.000 description 7
- 239000000126 substance Substances 0.000 description 7
- 241000196324 Embryophyta Species 0.000 description 6
- LXCFILQKKLGQFO-UHFFFAOYSA-N Methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 6
- JIWBIWFOSCKQMA-LTKCOYKYSA-N Stearidonic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/CCCCC(O)=O JIWBIWFOSCKQMA-LTKCOYKYSA-N 0.000 description 6
- 239000000839 emulsion Substances 0.000 description 6
- 229920001296 polysiloxane Polymers 0.000 description 6
- 238000010998 test method Methods 0.000 description 6
- 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 6
- CXQXSVUQTKDNFP-UHFFFAOYSA-N Simethicone Chemical compound C[Si](C)(C)O[Si](C)(C)O[Si](C)(C)C CXQXSVUQTKDNFP-UHFFFAOYSA-N 0.000 description 5
- 239000010474 borage seed oil Substances 0.000 description 5
- 150000001875 compounds Chemical class 0.000 description 5
- 201000004624 dermatitis Diseases 0.000 description 5
- 150000002148 esters Chemical group 0.000 description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 5
- 230000004054 inflammatory process Effects 0.000 description 5
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 5
- QGNJRVVDBSJHIZ-QHLGVNSISA-N retinyl acetate Chemical compound CC(=O)OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C QGNJRVVDBSJHIZ-QHLGVNSISA-N 0.000 description 5
- 239000002562 thickening agent Substances 0.000 description 5
- 235000015112 vegetable and seed oil Nutrition 0.000 description 5
- 239000003981 vehicle Substances 0.000 description 5
- HVYWMOMLDIMFJA-DPAQBDIFSA-N (3β)-Cholest-5-en-3-ol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 4
- BXWNKGSJHAJOGX-UHFFFAOYSA-N Cetyl alcohol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 4
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 description 4
- 206010061218 Inflammation Diseases 0.000 description 4
- DXGLGDHPHMLXJC-UHFFFAOYSA-N Oxybenzone Chemical compound OC1=CC(OC)=CC=C1C(=O)C1=CC=CC=C1 DXGLGDHPHMLXJC-UHFFFAOYSA-N 0.000 description 4
- 235000001466 Ribes nigrum Nutrition 0.000 description 4
- 241001312569 Ribes nigrum Species 0.000 description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N Salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 4
- 244000269722 Thea sinensis Species 0.000 description 4
- 229960000541 cetyl alcohol Drugs 0.000 description 4
- 239000006071 cream Substances 0.000 description 4
- 229940008099 dimethicone Drugs 0.000 description 4
- 239000004205 dimethyl polysiloxane Substances 0.000 description 4
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 4
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 description 4
- ZGTMUACCHSMWAC-UHFFFAOYSA-L disodium;2-[2-[carboxylatomethyl(carboxymethyl)amino]ethyl-(carboxymethyl)amino]acetate Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 4
- 235000009569 green tea Nutrition 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 239000003921 oil Substances 0.000 description 4
- 150000008442 polyphenolic compounds Chemical class 0.000 description 4
- 235000013824 polyphenols Nutrition 0.000 description 4
- VBICKXHEKHSIBG-UHFFFAOYSA-N rac-1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 4
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 4
- 210000003467 Cheek Anatomy 0.000 description 3
- 208000005679 Eczema Diseases 0.000 description 3
- YBGZDTIWKVFICR-JLHYYAGUSA-N Octyl methoxycinnamate Chemical compound CCCCC(CC)COC(=O)\C=C\C1=CC=C(OC)C=C1 YBGZDTIWKVFICR-JLHYYAGUSA-N 0.000 description 3
- 239000004264 Petrolatum Substances 0.000 description 3
- 229940066842 Petrolatum Drugs 0.000 description 3
- 241000208829 Sambucus Species 0.000 description 3
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Tris Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 3
- 150000001280 alpha hydroxy acids Chemical class 0.000 description 3
- 230000003110 anti-inflammatory Effects 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 239000004927 clay Substances 0.000 description 3
- 229910052570 clay Inorganic materials 0.000 description 3
- 229940086555 cyclomethicone Drugs 0.000 description 3
- 231100001003 eczema Toxicity 0.000 description 3
- 239000003974 emollient agent Substances 0.000 description 3
- 235000008995 european elder Nutrition 0.000 description 3
- 235000011187 glycerol Nutrition 0.000 description 3
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 3
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 3
- 229960002216 methylparaben Drugs 0.000 description 3
- 229960001679 octinoxate Drugs 0.000 description 3
- 235000019198 oils Nutrition 0.000 description 3
- 235000019271 petrolatum Nutrition 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 201000004681 psoriasis Diseases 0.000 description 3
- 229960000342 retinol acetate Drugs 0.000 description 3
- 235000019173 retinyl acetate Nutrition 0.000 description 3
- 239000011770 retinyl acetate Substances 0.000 description 3
- 125000000946 retinyl group Chemical group [H]C([*])([H])/C([H])=C(C([H])([H])[H])/C([H])=C([H])/C([H])=C(C([H])([H])[H])/C([H])=C([H])/C1=C(C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])C1(C([H])([H])[H])C([H])([H])[H] 0.000 description 3
- 230000000475 sunscreen Effects 0.000 description 3
- 239000000516 sunscreening agent Substances 0.000 description 3
- 150000004670 unsaturated fatty acids Chemical class 0.000 description 3
- 235000021122 unsaturated fatty acids Nutrition 0.000 description 3
- 238000005406 washing Methods 0.000 description 3
- XEYBRNLFEZDVAW-ARSRFYASSA-N (5Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-5-oxocyclopentyl]hept-5-enoic acid Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1C\C=C/CCCC(O)=O XEYBRNLFEZDVAW-ARSRFYASSA-N 0.000 description 2
- FPIPGXGPPPQFEQ-HWCYFHEPSA-N 13-cis-retinol Chemical compound OC/C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-HWCYFHEPSA-N 0.000 description 2
- CWSZBVAUYPTXTG-UHFFFAOYSA-N 5-[6-[[3,4-dihydroxy-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxymethyl]-3,4-dihydroxy-5-[4-hydroxy-3-(2-hydroxyethoxy)-6-(hydroxymethyl)-5-methoxyoxan-2-yl]oxyoxan-2-yl]oxy-6-(hydroxymethyl)-2-methyloxane-3,4-diol Chemical compound O1C(CO)C(OC)C(O)C(O)C1OCC1C(OC2C(C(O)C(OC)C(CO)O2)OCCO)C(O)C(O)C(OC2C(OC(C)C(O)C2O)CO)O1 CWSZBVAUYPTXTG-UHFFFAOYSA-N 0.000 description 2
- 206010000496 Acne Diseases 0.000 description 2
- PZZYQPZGQPZBDN-UHFFFAOYSA-N Aluminium silicate Chemical compound O=[Al]O[Si](=O)O[Al]=O PZZYQPZGQPZBDN-UHFFFAOYSA-N 0.000 description 2
- 240000004355 Borago officinalis Species 0.000 description 2
- 229940107161 Cholesterol Drugs 0.000 description 2
- 206010012438 Dermatitis atopic Diseases 0.000 description 2
- RFVNOJDQRGSOEL-UHFFFAOYSA-N Glycol stearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 2
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 2
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 2
- XUGNVMKQXJXZCD-UHFFFAOYSA-N Isopropyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(C)C XUGNVMKQXJXZCD-UHFFFAOYSA-N 0.000 description 2
- 210000002510 Keratinocytes Anatomy 0.000 description 2
- VODZWWMEJITOND-OWWNRXNESA-N N-Stearoylsphingosine Chemical compound CCCCCCCCCCCCCCCCCC(=O)NC(CO)C(O)\C=C\CCCCCCCCCCCCC VODZWWMEJITOND-OWWNRXNESA-N 0.000 description 2
- 229940100460 PEG-100 Stearate Drugs 0.000 description 2
- 229920002701 Polyoxyl 40 Stearate Polymers 0.000 description 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N Propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
- 208000006641 Skin Disease Diseases 0.000 description 2
- 229940010747 Sodium Hyaluronate Drugs 0.000 description 2
- 229920002385 Sodium hyaluronate Polymers 0.000 description 2
- 229950011392 Sorbitan stearate Drugs 0.000 description 2
- YYGNTYWPHWGJRM-RUSDCZJESA-N Squalene Natural products C(=C\CC/C(=C\CC/C=C(\CC/C=C(\CC/C=C(\C)/C)/C)/C)/C)(\CC/C=C(\C)/C)/C YYGNTYWPHWGJRM-RUSDCZJESA-N 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N Stearyl alcohol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- HVUMOYIDDBPOLL-IIZJTUPISA-N [2-[(2R,3S,4R)-3,4-dihydroxyoxolan-2-yl]-2-hydroxyethyl] octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)[C@H]1OC[C@@H](O)[C@@H]1O HVUMOYIDDBPOLL-IIZJTUPISA-N 0.000 description 2
- 230000002378 acidificating Effects 0.000 description 2
- WMGSQTMJHBYJMQ-UHFFFAOYSA-N aluminum;magnesium;silicate Chemical class [Mg+2].[Al+3].[O-][Si]([O-])([O-])[O-] WMGSQTMJHBYJMQ-UHFFFAOYSA-N 0.000 description 2
- VHUUQVKOLVNVRT-UHFFFAOYSA-N ammonium hydroxide Chemical compound [NH4+].[OH-] VHUUQVKOLVNVRT-UHFFFAOYSA-N 0.000 description 2
- 239000000908 ammonium hydroxide Substances 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 235000010323 ascorbic acid Nutrition 0.000 description 2
- 229960005070 ascorbic acid Drugs 0.000 description 2
- 239000011668 ascorbic acid Substances 0.000 description 2
- 201000008937 atopic dermatitis Diseases 0.000 description 2
- PUPZLCDOIYMWBV-UHFFFAOYSA-N butylene glycol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- 239000004202 carbamide Substances 0.000 description 2
- 235000012000 cholesterol Nutrition 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 229960002986 dinoprostone Drugs 0.000 description 2
- KCXVZYZYPLLWCC-UHFFFAOYSA-N edta Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 229940075529 glyceryl stearate Drugs 0.000 description 2
- 235000019447 hydroxyethyl cellulose Nutrition 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
- 238000000338 in vitro Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 230000003522 irritant Effects 0.000 description 2
- 231100000021 irritant Toxicity 0.000 description 2
- 229940075495 isopropyl palmitate Drugs 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- 239000006210 lotion Substances 0.000 description 2
- 229960001173 oxybenzone Drugs 0.000 description 2
- 230000035515 penetration Effects 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 2
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 2
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 2
- 229960003415 propylparaben Drugs 0.000 description 2
- 229960004889 salicylic acid Drugs 0.000 description 2
- 230000035807 sensation Effects 0.000 description 2
- CRPCXAMJWCDHFM-DFWYDOINSA-M sodium;(2S)-5-oxopyrrolidine-2-carboxylate Chemical compound [Na+].[O-]C(=O)[C@@H]1CCC(=O)N1 CRPCXAMJWCDHFM-DFWYDOINSA-M 0.000 description 2
- MAKUBRYLFHZREJ-JWBQXVCJSA-M sodium;(2S,3S,4R,5R,6R)-3-[(2S,3R,5S,6R)-3-acetamido-5-hydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5,6-trihydroxyoxane-2-carboxylate Chemical compound [Na+].CC(=O)N[C@@H]1C[C@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](C([O-])=O)O[C@@H](O)[C@H](O)[C@H]1O MAKUBRYLFHZREJ-JWBQXVCJSA-M 0.000 description 2
- 239000008117 stearic acid Substances 0.000 description 2
- 230000002522 swelling Effects 0.000 description 2
- 239000004408 titanium dioxide Substances 0.000 description 2
- 239000011732 tocopherol Substances 0.000 description 2
- 229930003799 tocopherols Natural products 0.000 description 2
- VYGQUTWHTHXGQB-FFHKNEKCSA-N trans-Retinyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C VYGQUTWHTHXGQB-FFHKNEKCSA-N 0.000 description 2
- 150000003626 triacylglycerols Chemical class 0.000 description 2
- 239000000230 xanthan gum Substances 0.000 description 2
- 229920001285 xanthan gum Polymers 0.000 description 2
- 235000010493 xanthan gum Nutrition 0.000 description 2
- 229940082509 xanthan gum Drugs 0.000 description 2
- ILLYYNHLCANIBL-YCNIQYBTSA-N (2E,4E,6E,8E)-3,7-dimethyl-9-(2,6,6-trimethylcyclohex-2-en-1-yl)nona-2,4,6,8-tetraenoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1C(C)=CCCC1(C)C ILLYYNHLCANIBL-YCNIQYBTSA-N 0.000 description 1
- LGEZTMRIZWCDLW-UHFFFAOYSA-N 14-methylpentadecyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCCCCCCCCCCCCC(C)C LGEZTMRIZWCDLW-UHFFFAOYSA-N 0.000 description 1
- JSOVGYMVTPPEND-UHFFFAOYSA-N 16-methylheptadecyl 2,2-dimethylpropanoate Chemical compound CC(C)CCCCCCCCCCCCCCCOC(=O)C(C)(C)C JSOVGYMVTPPEND-UHFFFAOYSA-N 0.000 description 1
- DUFKCOQISQKSAV-UHFFFAOYSA-N 2-(2-hydroxypropoxy)propan-1-ol Chemical compound CC(O)COC(C)CO DUFKCOQISQKSAV-UHFFFAOYSA-N 0.000 description 1
- GHPVDCPCKSNJDR-UHFFFAOYSA-N 2-hydroxydecanoic acid Chemical compound CCCCCCCCC(O)C(O)=O GHPVDCPCKSNJDR-UHFFFAOYSA-N 0.000 description 1
- YDZIJQXINJLRLL-UHFFFAOYSA-N 2-hydroxylauric acid Chemical compound CCCCCCCCCCC(O)C(O)=O YDZIJQXINJLRLL-UHFFFAOYSA-N 0.000 description 1
- JKRDADVRIYVCCY-UHFFFAOYSA-N 2-hydroxyoctanoic acid Chemical compound CCCCCCC(O)C(O)=O JKRDADVRIYVCCY-UHFFFAOYSA-N 0.000 description 1
- ICIDSZQHPUZUHC-UHFFFAOYSA-N 2-octadecoxyethanol Chemical compound CCCCCCCCCCCCCCCCCCOCCO ICIDSZQHPUZUHC-UHFFFAOYSA-N 0.000 description 1
- RMTFNDVZYPHUEF-XZBKPIIZSA-N 3-O-methyl-D-glucose Chemical compound O=C[C@H](O)[C@@H](OC)[C@H](O)[C@H](O)CO RMTFNDVZYPHUEF-XZBKPIIZSA-N 0.000 description 1
- ALYNCZNDIQEVRV-UHFFFAOYSA-N 4-Aminobenzoic acid Chemical class NC1=CC=C(C(O)=O)C=C1 ALYNCZNDIQEVRV-UHFFFAOYSA-N 0.000 description 1
- KGIJOOYOSFUGPC-MSFIICATSA-N 5-HETE Chemical compound CCCCCC=CCC=CCC=C\C=C\[C@@H](O)CCCC(O)=O KGIJOOYOSFUGPC-MSFIICATSA-N 0.000 description 1
- KGIJOOYOSFUGPC-CABOLEKPSA-N 5-HETE Natural products CCCCC\C=C/C\C=C/C\C=C/C=C/[C@H](O)CCCC(O)=O KGIJOOYOSFUGPC-CABOLEKPSA-N 0.000 description 1
- 229940061720 Alpha Hydroxy Acids Drugs 0.000 description 1
- 239000005995 Aluminium silicate Substances 0.000 description 1
- 102000001381 Arachidonate 5-Lipoxygenase Human genes 0.000 description 1
- 108010093579 Arachidonate 5-Lipoxygenase Proteins 0.000 description 1
- 206010003246 Arthritis Diseases 0.000 description 1
- 208000006673 Asthma Diseases 0.000 description 1
- 229940095259 Butylated Hydroxytoluene Drugs 0.000 description 1
- 239000004322 Butylated hydroxytoluene Substances 0.000 description 1
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N Carbonic acid Chemical class OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 description 1
- 229940113118 Carrageenan Drugs 0.000 description 1
- 240000001644 Cola acuminata Species 0.000 description 1
- 235000010205 Cola acuminata Nutrition 0.000 description 1
- 235000015438 Cola nitida Nutrition 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- 241000195493 Cryptophyta Species 0.000 description 1
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Abstract
The present invention relates to compositions containing hydroxy acids and / or retinoids and which also contain seed extract of Trichodesma lanicum as an anti-irritant / anti-itch agent.
Description
COMPOSITIONS CONTAINING HYDROXYACY OR RETINOIPES
CAMPQ OF THE INVENTION
The present invention relates to the use of Tri chode sma l an i cum seed extract in a composition and method for reducing or eliminating skin irritation or itching induced by hydroxy acids or retinoids.
BACKGROUND OF THE INVENTION
It has been proven that hydroxy acids and retinoids provide cosmetic benefits, such as improvement in the appearance of photodamaged or naturally aged skin, skin brightening, treatment of age spots, etc. Unfortunately, its use at high concentrations can occasionally be associated with skin irritation, for example, a reddish skin and itching sensation after application. The irritation can be reduced by reducing the amount of an active ingredient in the composition or by reducing the penetration of the active ingredient through the skin. A serious disadvantage of both aspects is that the effectiveness is damaged. The irritation related to HA can be reduced by increasing the pH of the composition, but this method produces a reduced efficiency due to a reduced penetration of HA through the skin. It is desirable to reduce or eliminate the potential irritation of the HAs and / or retinoids, as long as they maintain their efficacy. The patent application. ^ European 0631722
(Johnson &Johnson) describes the use of glycolic acid to reduce skin irritation through retinol. The United States Patent
,252,604 (Nagy et al.) Teaches the use of tocopherols for irritation induced by retinoic acid. U.S. Patent 5,516,793 (Duffy) describes the use of ascorbic acid to reduce irritation caused by various topical ingredients, including HAs and retinoids. U.S. Patent 5,476,661
(Pillai et al.) Describe cosmetic compositions containing 25-hydroxylic acid and a lipid ingredient. Numerous optional ingredients are listed, among which may be mentioned HAs and / or retinoids and unsaturated fatty acids, such as gamma-linoleic acid (GLA). Pillai et al. They do not direct the problem to skin irritations, they do not teach the use of any agent to reduce skin irritation and they do not teach the use of Tri Chode sma l ani cum seed extract. European Patent Application 0416855 (Efamol) describes the treatment of damaged skin due to radiotherapies with gamma-1-inoléic acid (GLA) and also teaches a variety of suitable plant sources of GLA, including the Borraja species. The PCT application. WO 90/07331 (Went) teaches the treatment of inflammation caused by arthritis or headache by topical application of GAL; Borage seed is known to be an adequate source. European Patent Application 0173478 (Efamol) describes the treatment of inflammatory disorders in the skin with compositions containing GAL and glucocorticoids; Borage species such as Borago officinalis is mentioned as a rich source in GLA. French Patent 2,704,390 (Boiron) describes an oral supplement containing borage seed oil to provide anti-aging benefits to the skin. French Patent 2,604,624 (Parfums Rochas) discloses skin care compositions containing polyunsaturated carboxylic acids such as GLA, the borage is said to be rich in GLA. British Patent 2,271,928 (Laing) describes the use of plant extracts from the borage family to alleviate skin disorders and irritations. U.S. Patent 5,445,822 (Braceo) discloses cosmetic compositions containing a mixture of triglycerides of polyunsaturated acids, wherein the fatty acids include ear acidic acid. Borage oil is listed as a suitable oil. The role played by lipids (triglycerides) in anti-inflammatory processes is described. Tollesson et al., "Transepidermal Water Loss and Water Content in the Stratum Corneum in Infantile Sebhorroeic Dermatitis", Derm Venereol Act (Sweden), Feb. 1993, 73 (1), p. 18-20, describe the use of topically applied borage oil for the treatment of seborrheic dermatitis. Bahmer et al., "Treatment of
Atopic Dermatitis with Borage Seed Oil (Glandol) - A
Time Series Analytic Study ", Kinderarztl Prax
(Germany), Oct. 1992, 60 (7), p. 199-202 describes the use of borage oil for the treatment of atopic dermatitis.
U.S. Patent 5,690,947 (Habif et al.) Discloses the use of borage seed oil to alleviate irritation caused by hydroxyl or retinoid acids. United States Patent 5,158,975
(Guichardant et al.) Describes the use of tearidonic acid to inhibit leucot rénos. The composition can be used topically to treat inflammations in the skin, for example acne eczema or psoriasis. Coupland et al describe in the documents presented at IFSCC on October 22-25, 1996 (Sydney) that the acid is known to be tearidonic possesses anti-inflammatory properties and that Crosses sential SA 6 (Tri chode sma l ani cum ) is a powerful moderator of UV-induced inflammation. However, there are numerous compounds that are capable of reducing UV-induced irritation, but not irritation induced by hydroxy acids or retinoids (see Example 4). Tri chodesma l ani cum is a plant different from borage seed oil, although both belong to the Boragenous family of plants and Tri codesma l ani cum is known under a similar name in English "wild borage". The Latin names for the two plants differ: Tri codesma l ani cum for wild borage and Borago officinalis for borage. Although the technique teaches the use of borage seed oil, as a source of GAL, Trichodesma lanicum or wild borage seed extract is not mentioned. Actually, the Trichodesma lanicum seed contains perhaps 5 times less of the amount of GLA than the borage seed. In the constitution of the. unsaturated fatty acid from the seed of Trichodesma lanicum and borage seed is very different:
The technique discussed above does not teach any composition containing seed extract of Trichodesma lanicum in combination with HAs and / or retinoids. The technique does not seem to teach the use of Trichodesma lanicum seed extract or any of its unsaturated fatty acids as constituents to reduce the irritation or itching associated with the use of HAs and / or retinoids.
BRIEF DESCRIPTION OF THE INVENTION
The present invention includes, in part, a composition containing a beneficial cosmetic ingredient selected from the group consisting of hydroxy acids ("HAs") and certain retinoids, and which additionally contains seed extract of Tri chodesma l ani cum. The invention also includes a cosmetic method for reducing or eliminating irritation or itching induced by the topical application of a composition containing HAs or retinoids, the method comprising topically applying Tri chodesma l an i cum seed extract in an effective amount to reduce or eliminate the irritation induced by the composition. According to the method of the invention, the seed extract of Tri chodesma l ani cum may be co-present with HAs and / or retinoids in the same composition, or the seed extract Tri chodesma l an i cum may be applied to from a separate composition.
In accordance with the present invention, by virtue of the topical application of the Tri chode sma l ani cu seed extract, the irritation or itching induced by the topical application of HAs and / or retinoids is reduced or eliminated. It has been found as part of the present invention that all anti-irritants, even those with GLA or stearidonic acid, improve the irritation induced by HA / retinoid. In addition, a compound that alleviates UV-induced erythema does not necessarily control the irritation induced by hydroxy acids or retinoids.
DETAILED DESCRIPTION OF THE INVENTION
The seed extract of Trichodesma lanicum is an essential ingredient of the compositions of the invention. The seed extract of Tri chode sma l ani cum is obtained from the seeds of the plant of
Tri chodesma l an i cum, also known as Borraja
Wild, which is a plant, native to tropical Asia and Australia. The seed extract of Tri chodesma l an i cum is used in accordance with the present invention to reduce or eliminate skin irritation induced by hydroxy acids and / or retinoids. The amount of seed extract from
Tri-burn in the compositions of the invention generally ranges from 0.05% to 10% by weight of the composition, preferably from 0.1% to 5%, most preferably from 0.5% to 2%. Hydroxy acids improve proliferation and increase ceramide biosynthesis in keratinocytes, increase epidermal thickness, and increase the peeling of normal skin resulting in smoother, more youthful looking skin. The hydroxy acid may be selected from α-hydroxy acids, β-hydroxy acids, (eg, salicylic acid), other hydroxycarboxylic acids (eg, dihydroxy carboxylic acid, hydroxy-dicarboxylic acid, hydroxy tricarboxylic acid) and mixtures thereof or combination of its stereoisomers (DL, D or L). Preferably, the hydroxy acid is selected from a-hydroxy acids having the general structure (1):
OH
MCHCOOH (1)
where M is hydrogen or a straight or branched hydrocarbon chain, saturated or unsaturated, containing from 1 to 27 carbon atoms. Even more preferably, the hydroxy acid is selected from lactic acid, 2-hydroxyoctanoic acid, hydroxylauric acid, glycolic acid and mixtures thereof. When stereoisomers exist, the most preferred is L-isomer. It should be understood that depending on the pH of the composition, the hydroxy acid may be present as a salt, for example as an ammonium or potassium or sodium salt. Although the compositions of the invention may have any pH in the general scale of 2.5 to 10, the compositions of the invention are particularly useful when they are at an acidic pH (especially if they contain a hydroxy acid), more preferably at a pH of 3-4. , because such compositions are particularly irritating. Retinoids improve keratinocyte proliferation in vitro, increase epidermal thickness and increase collagen synthesis through dermal fibroblasts. This results in protection from sun damage and wrinkled skin softness. The term "retinoids" as used herein, includes retinoic acid, retinol, retinal and retinyl esters of C2-C5, since these are the most irritant. Included in the term "retinoic acid" are 13-cis-retinoic acid and all trans-retinoic acids. The term "retinol" includes the following isomers of retinol: complete rans-re-inol, 13-cis-retinol, 11-cis-re t inol, 9-c is-re t inol, 3,4-didehydro-re t inol. The preferred isomers are full-length t -rans-re, 13-cis-ret inol, 3,4-didehydro-ret inol, 9-ci-s-re t inol. More preferred is complete trans-ret, due to its wide commercial availability. The retinyl ester is an ester of retinol. The term "retinol" has been identified above. Suitable retinyl esters for use in the present invention are C2-C5 retinol esters, preferably C2 and C3 esters, and more preferably C2 ester, since it is the most commercially available. The retinyl esters included in the invention are also known as retinyl acetate, retinyl propionate, retinyl butyrate and retinyl pentanolate. A particular advantage of the compositions of the invention is that higher amounts of hydroxy acids or retinoids can be used, without causing skin irritation. Preferably, the amount of the hydroxy acid component present in the composition according to the invention is from * 0.01 to 20%, more preferably from 0.1 to 12% and more preferably from 4 to 12% by weight of the composition. A retinoid may be present in the compositions of the invention in an amount of 33 to 330, 000 IU per gram of the composition, preferably from 330 to 16,500 IU, and most preferably from 1,650 to 6,600 IU. Again, a higher amount of a retinoid may be employed in the compositions of the invention, without causing skin damage, due to the co-presence of the Tri chodesma l ani cum seed extract. The most preferred compositions of the invention containing the anti-inflammatory agent of T i chorasema seed extract include retinol and / or retinyl acetate and / or glycolic acid and / or lactic acid, since these ingredients are has been found to cause irritation although they are particularly effective in providing cosmetic benefits. The skin treatment composition of the invention also includes a cosmetically acceptable vehicle or carrier, which is inert, usually an ingredient present in the highest amounts, and functioning to supply active or operating ingredients. Vehicles other than water may include liquid or solid emollients, solvents, humectants, thickeners and powders. An especially preferred non-aqueous vehicle is a poly idimet ilsiloxane and / or a poly idimet i 1 pheny1-siloxane. The silicones of this invention can be those with viscosities ranging from about 10 to 10,000,000 centistokes at 25 ° C. Especially desirable are low and high viscosity silicone blends. These silicones are available from the General Electric Company under the trade names of Vicasil, SE and SF and the Dow Corning Company under the Series 200 and 550. Amounts of silicone can be used in the compositions of this invention ranging from 5 to 95%, preferably from 25 to 90% by weight of the composition. The amount of vehicle can vary from about 2 to about 99% by weight, preferably from about 50 to about 99%, more preferably from about 80 to 99% by weight of the total composition. According to the present invention, the vehicle is preferably at least 60% by weight of water, by weight of the vehicle. The compositions of the invention are preferably water-oil emulsions, in order to improve the supply of hydroxy acids in the dermis (See Sah A., "An in-vitro study of the effect of formulation variables and product structure on the delivery of alpha-hydroxy acid (Lactic acid) to skin ", MS Thesis, Department of Pharmaceutical Sciences of the College of Pharmacy, University of Cincinnati, OH, July 1996). Improved delivery is often accompanied by increased irritation / itching, making the use of Tri chomsma l ani cum seed extract in such emulsions particularly critical. In the preferred water-in-water water emulsions according to the present invention, the water comprises at least 50% by weight of the emulsion of the invention, more preferably from 50 to 70% by weight, by weight of the composition. ion.
Beneficial Materials Lar a Skin Optional and
Auxiliary Cosmetics
Various types of active ingredients may be present in the cosmetic compositions of the present invention. Active ingredients are defined as skin beneficial agents other than emollients and other than ingredients that merely improve the physical characteristics of the composition. Although this category is not limited, general examples include anti-wrinkle compounds and sunscreens and sunscreens. Agents for the sun include those materials commonly used to block ultra violet light. Illustrative compounds are titanium dioxide, PABA derivatives, cinnamate and salicylate. For example, octyl methoxycinnamate and 2-hydroxy-4-methoxybenzophenone (also known as oxybenzone) can be used. Octyl methoxycinnamate and 2-hydroxy-4-methoxybenzophenone are commercially available under the tradenames of Parsol MCX and Benzophenone-3, respectively. The exact amount of sunscreen used in the emulsions can vary depending on the degree of protection desired from the sun's UV radiation. Another category of functional ingredients within the cosmetic compositions of the present invention are thickeners. A thickener will usually be present in amounts of 0.1 to 20% by weight, preferably from about 0.5% to 10% by weight of the composition. Illustrative thickeners are entangled polyacrylate materials available under the trade name Carbopol from B.F. Goodrich Company. Gums can be used, such as xanthan gum, carrageenan, gelatin, carayá, pectin and locust bean gum. Under certain circumstances the function of the thickener can be achieved through a material that also serves as a silicone or emollient. For example, silicone gums in an excess of 10 centistokes and esters such as glycerol stearate have a double functionality.
The powders can be incorporated into the cosmetic composition of the invention. These powders include clay, talc, Fullers earth, kaolin, starch, smectite clays, chemically modified magnesium aluminum silicate, organically modified montmorillonite clay, hydrous aluminum silicate, fumed silica, aluminum starch octenyl succinate , and mixtures of the same. They can also be incorporated into cosmetic compositions. other minor auxiliary components. These ingredients may include coloring agents, opacifiers and perfumes. The amounts of these other component materials may vary from 0.001% to 20% by weight of the composition.
Use of Composition
The composition according to the invention is primarily intended to be a product for topical application to the skin of the human being, especially as an agent for conditions and to soften the skin, and to avoid or reduce the appearance of wrinkled or aged skin.
During use, a small amount of the composition, for example from 1 to 100 ml, is applied to the exposed areas of the skin, from a suitable container or applicator and, if necessary, then extended over and / or or rubbed on the skin using your hand or fingers or a suitable device. According to the method of the present invention, skin irritation induced by the active ingredient is reduced or eliminated through the topical application of T i chode sma l ani cum seed extract. The seed extract of Tri chodesma l ani cum may be co-present with the active ingredient, or may be applied to the skin separately from the active ingredient.
Form and Product Packaging
The topical skin treatment composition of the present invention can be formulated as a lotion, a fluid cream, a cream or a gel. The composition can be packed in a suitable container to adapt its viscosity and its intended use by the consumer. For example, a lotion or fluid cream can be packaged in a bottle or ball applicator, or a capsule or an aerosol device driven by a propellant, or a container equipped with a pump suitable for finger operation. When the composition is a cream, it can simply be stored in a non-deformable bottle or compressible container, such as a tube or a jar with a lid. Accordingly, the invention also provides a closed container containing a cosmetically acceptable composition as defined herein. The seed extract of Tri chode sma l ani cum can be packaged separately from the composition containing HAs and / or retinoids. The following specific examples further illustrate the invention, but the invention is not limited thereto. The seed extract Tri chodesma l ani cum (Wild Borage) used in the examples was obtained from Croda Oleochemicals (England) under the trade name of Crossessential SA-6.
EXAMPLE 1 Itching Test Method The object was to compare the level of itching and / or burning produced by a test material against a control after a single application to the cheek / nasolabial fold. Subjects were first classified for their ability to experience an itching / burn sensation in response to 8% glycolic acid compared to the base formula. 20 Subjects with balanced left / right itching responses were used in the study. The subjects were washed the test sites for (cheek / nasolabial fold) for 30 seconds with an Ivory soap and hot water. The test sites were stained by drying and 0.025 ml of the test and control material was applied, simultaneously, by the study staff to the left and right of the cheek / nasolabial folds. The materials were rubbed on the skin for 30 seconds. The products were applied in a random and balanced order across the subject. Subjects rated the degree of itching / burning perceived on each side of the face before washing the test sites, immediately after washing the test sites, and during the attack immediately (time equal to 0) and at 2.5, 5.0 and 7.5 minutes after the study staff applied the test materials. The subjects recorded intensity using the following scale: 0 - none 1 - very light 2 - light 3 - moderate 4 - highly moderate 5 - high 6 - extreme Also, at the end of 7.5 minutes, the subjects recorded that the side of the face experiment more discomfort (itch / burn), and at most (: Scarcely more, Slightly more, Moderately more or Extremely more).
Statistic analysis
The parametric pair t test (two extremes) was performed to compare the degree of itching / burn changes from the baseline (immediately after washing the test sites) at each time point of the evaluation (0, 2.5, 5.0 and 7.5 minutes) between each treatment comprising a comparison test in pairs, the subject acting as a block in these analyzes. [Ref. S ta t i s t i ca l Me thoAa. , Snedecor and Cochran, Iowa State University Press, 7th Edition, 1980, p. 84-86]. These results are shown in Table 1 below. In addition, for each subject, the area under the curve was calculated with respect to the change of the baseline response profile, one for each of the two treatments comprising a comparison test in pairs, using the trapezoidal rule. In order to compare the degree of difference in the whole itch / burn response, the difference in the areas under the curve between the two treatments for each subject was compared using a t test in parametric pairs (double extreme), the subject acting as a block in these analyzes. [Ref. Sta t i s t i ca l Me thods r Snedecor and Cochran, Iowa State University Press, 7th Edition, 1980, p. 84-86] a p-value not greater than 0.1 was considered statistically significant. These results are shown in Table IA below. In addition, the subjects' union response to the two general questions, "Which side of the face has more itching?", Along with "How much more?", Became the individual classification, then it was decoded and classified according to the treatment perceived as the comparatively most itchy. This gives a direct measure of the perceived attribute difference between the treatments, based on the category of 9 points addressed in the scale of ordinal difference shown below:
Ordinal Difference Scale Directed Traíamienío A Treatment B More Itching / Burn Point No More Itching / Burn Than the Trace B difference than the Extreme End Treatment I -4 -2 or +? +2 +3 +4
(0) == No Difference (+/- 1) = Scarcely More (+ / - 2) = Slightly More (+/- 3) = Moderately More (+/- 4) = Extremely More
For each pairwise comparison, these directed differences were compared using the Wilcoxon nonparametric rank-assigned test Pratt-Lehmann version, with the subject acting as a block. [Ref. Nonpara e t r ics: Statiscal Methods Based on Ranks, by Erich L. Lehmann, Holden-Day, 1975, pp. 130]. These results are shown in Table 1 below. An emulsion base was prepared having the following formula.
Additional ingredients in the Examples below were added instead of water. Compositions 1-4 containing the ingredients indicated in Table 1 were tested using the itch test method. The results that were obtained are summarized in Tables 1 and ÍA. The higher the average intensity and the area under the curve, the more severe the sensory irritation (itch / burn).
TABLE 1 - Itch Test Results
* Significantly less itching / burn than composition # 2 (p < 0.05) b Significantly less itching / burn than composition # 2 (p < 0.10)
a Significantly less itching / burn than composition # 2 (p < 0.05) It can be seen from the results in Tables 1 and 1A that the addition of Tri chodesma l ani cum seed extract significantly reduced itching compared to the composition containing 8% glycolic acid, but none of the seed extract of Tri chodesma l ani cum.
EXAMPLE 2 Subjects were tested according to the irritation test method described below.
üáfcQ CLCL-d-B-JPc..u eb
Four Exposure Patch Test: The object is to compare the level of irritation produced by various test materials after repeated patch applications. The test materials were kept in contact with the skin under occlusive conditions. The external upper arm of the panelist was designated as the application area. A bandage-type bandage (Scanpor7 tape) was used to hold the patches (25 mm Hill Top7 Chamber equipped with a 18 mm diameter disc of Webril7 pad) in place. Both upper arms of the panelist were used. The patches were applied in a balanced random order. The patches were applied at 9:00 am on Monday morning and were removed at 9:00 am on Tuesday morning (24-hour exposure). A new patch group was applied at 3:00 in the afternoon on Tuesday and was removed at 9:00 in the morning on Wednesday (18 hours exposure). A third group of patches was applied at 3:00 in the afternoon on Wednesday and was removed at 9:00 in the morning on Thursday (18-hour exposure). A final group of patches was applied at 3:00 in the afternoon on Thursday and was removed at 9:00 in the morning on Friday (18-hour exposure). Each time the patches were removed, the sites were washed with hot water and dried. The test sites were then marked with a surgical marker pen for the skin to ensure the location for classification and for subsequent applications of the patch. The test sites were evaluated at 3:00 in the afternoon of Tuesday, Wednesday, Thursday and Friday of the study, before replacing the patches. Irritation on the skin such as a moderate reddish appearance, dryness and / or welts of the test site, was expected. Swelling may be present at the test sites. If any test has moderate reddish skin or any swelling in the evaluation, that particular site should not be re-patched. The test sites on each arm were visually assessed by two examiners trained under consistent light. The test sites were evaluated in order of severity. The evaluation of the examiner responds to a first period of evaluation that continues evaluating the sites every day through the study.
To evaluate the reactions, the site with the most severe response was given the lowest mark. The siege with the second most severe response was given the second lowest mark, etc. There was no forced evaluation. If two or more sites had no response or had the same response (no difference between the sites), an average of the evaluations was assigned. If a site was discontinued, due to the degree of irritation, the site retained the evaluation it received at the time of removing the two information.
Análisjs s a ístico
The results of the evaluation of the treatments with patches were statistically compared with two nonparametric statistical methods. Test materials containing anti- irritants were compared to the corresponding control containing only hydroxy acid and / or retinoid, using the Friedman Evaluation sum. The treatments were compared with Formula 2 (control) at each evaluation point using Friefman's analysis with the panelist acting as a block (ie, each panelist was tested with each trial treatment). The p value of < 0.1 was considered statistically significant. The compositions containing the ingredients as indicated in Tables 2, 2A and 2B were tested using the Irritation Test Method. 20 subjects were tested for each test in Table 2 and for the test in Table 2A and 17 subjects were tested to stop the test in Table 2B. The results that were obtained are summarized in Tables 2 and 2A. The higher the Sum of Assessments, the less severe the irritation.
Table 2 Irritation Test Results COMPOSITION INGREDIENTS SUM OF% GL? % SA ** CLASSIFICATIONS (OIA 4) Base Formula 68. 5 * Control: Formula of 46. 5 Base + 8% Glycolic Acid and 0.075% Retinol Composition # 5 + 3% 58.0 0.51 0.06-0.12 of Cassis Seed Oil Composition # 5 * 1% 44.5 of Sambucus
* Significantly less irritating than composition # 5.
* SA = stearidonic acid
Table 2A Proof of Proof of Irrigation
COMPOSITION INGREDIENTS SUM OF SUM OF EVALUATIONS EVALUATIONS% SA (DAY 3) (DAY 4) Base Formula 861 84 'Base Formula + 8% 60 62 Glycolic 8 Composition # 2 + 1% 801 77 0.065 of Trichodesma lanicum
* Significantly less irritating than composition # 2.
Table 2B Irritation Test Results
COMPOSITION INGREDIENTS Sum of Evaluations (Day 4)% SA
Base Formula + 8% 27 glycolic + 0.064%
Base formula + 8% of 24 0.065 glycolic: + 0. 076% of retinol SUM + 1% EVALUATIONS Tri chodesma lanicum It can be seen from the results in Table 2 that after four exposures, 8% glycolic acid with 0.075% retinol (# 5) was significantly more irritating than the base formula # 1. 1% Sambucus (# 7) or 3% cassis seed oil (# 6) did not significantly reduce irritation. Sambucus and cassis seed oil are known anti-irritants. Cassis seed oil also contains 17% GLA and 2-4% stearidonic acid. However, no agent was effective in reducing the irritation induced by alpha hydroxy acid / retinoic acid. In contrast, as demonstrated by the results in Table 2A, the Tri chodesma l ani cum seed extract (composition # 8) significantly reduced the irritation induced with composition # 2 (containing 8% glycolic acid), although the The composition contained the same or even less amount of stearidonic acid than the composition with cassis seed oil. As demonstrated by the results in Table 2B, the addition of the Tri chode sma l ani cum extract to the formula allowed an addition of -20% more retinol, without any increase in irritation.
U.S. Patent No. 5,158,975, (Guichardant et al.) Teaches that the anti-inflammatory effect of stearidonic acid is through the inhibition of 5-lipoxygenase and the prevention of the formation of 5-HETE and LTB4, which play a predominant part in several inflammatory processes of the allergenic type (ie asthma) of the cutaneous type (ie psoriasis and eczema) or rheumatic type. Since the irritation induced by HA or retinol is not related to these skin disorders or inflammations (acne, eczema, psoriasis), it is surprising that the Tri chodesma l an i cum seed extract reduces the irritation induced by HA or retinol In addition, the effect of Tri chodasma l an i cum seed extract can not be attributed to stearidonic acid or GLA, since compounds containing higher amounts of GLA and the same or even higher amounts of SA were not effective.yea
COMPARATIVE EXAMPLE 3
Compositions 1, 5 and 11-14 were tested containing ingredients as indicated in Table 3, using the irritation test method described in Example 2. 17 subjects were tested. The results that were obtained are summarized in Table 3. The higher the sum of evaluations, the lower the irritation.
TABLE 3 Irritation Test Results
a Statistically less irritating than composition # 5. * An anti-irritant from Centerchem (containing water, butylene glycol, kola beam extract, guarana extract and mate extract).
** An anti-irritant of Penederm, Inc. (CFTA name PPG-12 / SMDI). It can be seen from the results of Table 3 that none of the known anti-irritants tested (none containing GLA or SA) were able to significantly reduce the irritation induced by composition # 5 (containing 8% glycolic acid and 0.075% ret inol).
COMPARATIVE EXAMPLE 4 UV Induced Erythema Method
The purpose was to determine if the pre-treatment of the skin before irritation with UV light could reduce the level of erythema produced.
Twenty-two subjects, aged 18 s and older, were used in this study, with Skin Types of
Fitzpatrick I, II or III. They determined the MEDs (minimum erythemal dose) (UVA and UVB scale, 290-400 nm) for each subject before the test using a sun simulator. The test compositions were applied to 4.0 cm2 (2.0 cm x 2.0 cm) test sites at a dose of 2 mg / cm2 on the lower back using a positive displacement pipette. The test compositions were rubbed on the test sites using the tips of the fingers with gloves. After 15 minutes, the test sites were irradiated with an individual light exposure of 1.5 MED UVA / UVB using a solar simulator. The erythema was evaluated visually 24 hours after the irradiation, through a trained clinical assessor using a scale of 0-4 (0 = no erythema, 0.5 = barely noticeable erythema, faint or diffuse, 1 = slight erythema but having a response uniform within the area of irradiation, 2 = definitive erythema 3 = moderate erythema and 4 = severe erythema). The evaluation test assigned by Wilcoxon without parameters, Pratt-Lehman version, was used to compare the differences in the erythema between the test compositions and the base compositions, with a subject acting as a block. The test compositions containing ingredients as indicated in Table 4 were tested using this method. The results that were obtained are summarized in Table 4.
Base Formula A (composition 17):
INGREDIENT% P / P
2% interlaced polymer solution of acrylates / C10-30 alkyl acrylate 18.00 dimet icone / sil ivone oils 6.45 glycerin 5.00
PPG-15 stearyl ester 3.00 isocetyl stearate 2.75 squalene 2.35 methyl glucose distearate / is glyceryl ield 2.15 butylene glycol 1.65 diisopropyl dimer dilinoleate 1.30 pollen extract / soybean and olive oils and non-saponifiable wheat germ 1.25 estearet-21 1.2 mixture of amino acid 1.1 polymethyl methacrylate 1.00 glycerides of C8 ~ i8 1.00
Sodium PCA 1.00 hydrolized glycosamine glycans / sodium hyaluronate 0.50 algae extract solution 0.50 PEG-8 acid ester 0- ^ 2-20 0.80 triethanolamine 99% 0.80 1% solution of sodium hyaluronate 0.75 polyacrylamide / Isoparaffin of Ci 3 _ 14 / laure t - 7 0.50 arachidyl bejenate 0.50 Disodium EDTA 0.10 estearet - 2 0.30
DL-panthenol 0.25 methylparaben 0.20 behenyl alcohol 80 0.20 butter 0.20 ether perfluoropol imet il isopropyl 1 ico 0.20 propylparaben 0.10 diazodinil urea 0.10 ceramide 6 0.02 water q.s. for 100
Table 4 Results of ÜV-Induced Erythema Test INSERT PAGE 28 The compositions containing the ingredients as set forth in Tables 4A and 4B were tested using the irritation test method described in Example 2, in two separate experiments. . 22 subjects were tested for the experiment in Table 4A and 19 subjects for the experiment in Table 4B. The results that were obtained are summarized in Tables 4A and 4B.
Table 4A Results Irritation Test
* Significantly less irritating than composition # 2.
Table 4B Irritation Test Results
# OF COMPOSITION INGREDIENTS SUM OF EVALUATIONS (DAY 4) Base Formula * 8% of 72 .5 Glycolic 18 Composition # 2 + S% of 77. 5 α-Icopherol 19 Composition # 2 + 5% of 56. 5 a-tocopherol + 5% 1.2% green tea polyphenols As shown in Table 4, when green tea a-tocopherol and polyphenol were added to Base Formula A (composition 17) a significant reduction in the UV-induced erythema. However, the results in Tables 4A and 4B show that a-tocopherol and green tea polyphenols were not effective in reducing HA-induced irritation. In the CRODA product of the literature "Moderation of ultraviolet inducet inflammation in skin by (n-3) and (n-6) lipids-" Coupland et al. The use of Tri chod sma l ani cum extract (Trichodesma; Crossential SA6) as a released PGE2 inhibitor that is induced by UVB light is reported, however, it is not obvious that the materials that exhibit PGE2 production induced by UV and subsequent irritation, may be effective in reducing irritation induced by HA or retinoid, since several materials that exhibit UV-induced erythema (such as α-tocopherol and green tea polyphenols) are not effective in reducing HA-induced erythema.
EXAMPLE 5 An oil-in-water emulsion within the scope of the invention is as follows:
Chemical Name% P Propi glycol 1 glycerin 1 hydroxyethylcellulose 0.5 magnesium silicate io - aluminum 0.5 imidazolidinylurea 0.5
Tetrasodium EDTA 0.05 petrolatum 2 isopropyl palmitate 5 dimethicone 0.5 cholesterol 0.5 cetyl alcohol 0.5 isostearic acid 3 retinyl palmitate 0.1 peg-40 stearate 1 peg-100 stearate 1 sorbitan stearate 1 Tri chodesma seed extract l an i cum 0.5 glycolic acid 7 ammonium hydroxide for a ph 4.0 water DI cs for 100%
EXAMPLE 6 Another oil-in-water emulsion within the scope of the invention is as follows:
Chemical Name% p Propylene glycol 1 hydroxyethylcellulose 0.5 magnesium aluminum silicate 0.5 imidazolidinylurea. 0.2 petrolatum 2 isopropyl palmitate 5 dimethicone 0.5 cholesterol 0.5 stearic acid 3 isostearic acid 1.5 glycerol stearate 1.5 peg-40 stearate 1 peg-100 stearate 1 sorbitan stearate 1 cetyl alcohol 0.5 Tri chodesma seed extract l ani cum 2 glycolic acid 10 ammonium hydroxide for a ph 3.8 water DI cs for 100%
JEMPLO 7 A dispersion of water in oil within the scope of the invention is as follows:
Chemical Name% P
Isostearyl Neopentanoate 20 caprylic / capric glycerides peg-8 6 cetyl octanoate 17 polyol Ilearyl dioleate - 6 15 cyclomethicone 20 glyceryl isostearate 0.5 isostearic acid 0.5 ceramide III 0.1 ppg- 5 -cetet -20 3 acid 1 - lac potassium icoate 6 hydroxycapric acid 1 ico 0.1 water DI 1.3 Tri chodama seed extract l an i cum 0.5 EXAMPLE 8 The following oil-in-water emulsion was prepared within the scope of the invention:
Chemical Name% p gl icerine 1 Tetrasodium EDTA 0.1 Cetyl alcohol 1 stearyl alcohol 1 mineral oil 5 dimethicone 1 cyclomethicone 0.5 dimetolol 0.2 polyquaternium-37 2 steareth-21 1 est earet - 2 0.5 salicylic acid 2 Tri chodesma l ani seed extract cum or .5 triethanolamine at a pH of 3.0 water DI cs for 100%
EXAMPLE 9 The following oil-in-water emulsion was prepared within the scope of the invention:
Chemical Name% p xanthan gum 0.2
Disodium EDTA 0.1 Sodium PCA 0.5 diazodinil urea 0.3 titanium dioxide 1 stearic acid 3 cyclomethicone 0.3 cetyl alcohol 0.5 glyceryl stearate. 0.5 stearate of peg-100 1 est eare t - 2 1 leci ina 0.5 tocopherol 0.2 methoxycinnamate octyl 6 extract of Tri chodesma seed l ani cum 0.5 glycolic acid 3 malic acid 2 lactic acid 2 green tea extract 1 triethanolamine for a pH 3.8 water DI cs for 100% EXAMPLE 10 The following oil-in-water emulsion was prepared within the scope of the invention:
Chemical Name% p trans-re t inoic acid 0.05 light mineral oil 10 is tearoxi trimethyl if tin and stearyl alcohol 5 dimethicone 2 stearyl stearate-10 quaternium-15 3 glycol copolymer peg-22 dodecyl 1 seed extract from Tri chode sma l an i cum 1 sorbitol 0.5 methylparaben 0.2
Disodium EDTA 0.1-hydroxytoluene butylated 0.1 water DI cs for 100
EXAMPLE 11 The following oil-in-water emulsion was prepared within the scope of the invention:
Chemical Name% p squalane 20 macadamia oil 5 pentaerythritol tetraoctanoate 15 petrolatum 5 glyceryl stearate '3 tocopherol acetate 0.5 butylated hydroxytoluene 0.05 methylparaben 0.15 propylparaben 0.15 retinol. 0.1 seed extract, from Tri chodesma l an i cum 0.25 sodium citrate 1 ascorbic acid 1 butylene glycol 2 glycerol 2 benthic clay 0.2 disodium EDTA 0.05 water DI cs for 100%
EXAMPLE 12 The following oil-in-water emulsion was prepared within the scope of the invention:
Claims (7)
1. A composition comprising: (i) a cosmetic benefit ingredient selected from the group consisting of a hydroxy acid, retinol, retinoic acid, retinal, C2-C5 retinyl ester, and mixtures thereof; (ii) Trichodesma lanicum seed extract; and (iii) a cosmetically acceptable vehicle.
2. The composition of claim 1 wherein the cosmetic benefit ingredient is a hydroxy acid, which is present in an amount of 0.01 to 20% by weight of the composition.
3. The composition of claim 2, wherein the amount of the hydroxy acid is from 0.1 to 12% by weight of the composition. *
4. The composition of claim 1, wherein the cosmetic benefit ingredient is a retinol or a retinyl ester, which is present in an amount of 33 to 330,000 IU per gram of the composition.
5. The composition of claim 1, wherein the cosmetic benefit ingredient is selected from the group consisting of retinol, glycolic acid, lactic acid and mixtures thereof.
6. The composition according to any one of claims 1-5, wherein the Tri chodasma l an i cum seed extract is present in an amount of 0.05% to 10% by weight of the composition.
7. A cosmetic method for reducing itching or irritation induced by topical application of a composition containing a hydroxy acid or a retinoid, the method comprises topically applying Tri chozema l ani cum seed extract in an effective amount to reduce irritation induced by composition.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US038008 | 1988-04-05 |
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MXPA98001116A true MXPA98001116A (en) | 1999-06-01 |
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