CN112891242A - Composition for removing freckles, whitening and resisting inflammation and application thereof - Google Patents
Composition for removing freckles, whitening and resisting inflammation and application thereof Download PDFInfo
- Publication number
- CN112891242A CN112891242A CN202110252449.7A CN202110252449A CN112891242A CN 112891242 A CN112891242 A CN 112891242A CN 202110252449 A CN202110252449 A CN 202110252449A CN 112891242 A CN112891242 A CN 112891242A
- Authority
- CN
- China
- Prior art keywords
- composition
- component
- skin
- whitening
- tranexamic acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 55
- 230000002087 whitening effect Effects 0.000 title claims abstract description 30
- 208000003351 Melanosis Diseases 0.000 title claims abstract description 20
- 206010014970 Ephelides Diseases 0.000 title claims abstract description 12
- 206010061218 Inflammation Diseases 0.000 title claims description 10
- 230000004054 inflammatory process Effects 0.000 title claims description 10
- 229960000401 tranexamic acid Drugs 0.000 claims abstract description 35
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 claims abstract description 35
- 229960004352 diosmin Drugs 0.000 claims abstract description 28
- GZSOSUNBTXMUFQ-NJGQXECBSA-N 5,7,3'-Trihydroxy-4'-methoxyflavone 7-O-rutinoside Natural products O(C[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@H](Oc2cc(O)c3C(=O)C=C(c4cc(O)c(OC)cc4)Oc3c2)O1)[C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@H](C)O1 GZSOSUNBTXMUFQ-NJGQXECBSA-N 0.000 claims abstract description 27
- XUMBMVFBXHLACL-UHFFFAOYSA-N Melanin Chemical compound O=C1C(=O)C(C2=CNC3=C(C(C(=O)C4=C32)=O)C)=C2C4=CNC2=C1C XUMBMVFBXHLACL-UHFFFAOYSA-N 0.000 claims abstract description 27
- GZSOSUNBTXMUFQ-YFAPSIMESA-N diosmin Chemical compound C1=C(O)C(OC)=CC=C1C(OC1=C2)=CC(=O)C1=C(O)C=C2O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO[C@H]2[C@@H]([C@H](O)[C@@H](O)[C@H](C)O2)O)O1 GZSOSUNBTXMUFQ-YFAPSIMESA-N 0.000 claims abstract description 27
- IGBKNLGEMMEWKD-UHFFFAOYSA-N diosmin Natural products COc1ccc(cc1)C2=C(O)C(=O)c3c(O)cc(OC4OC(COC5OC(C)C(O)C(O)C5O)C(O)C(O)C4O)cc3O2 IGBKNLGEMMEWKD-UHFFFAOYSA-N 0.000 claims abstract description 27
- VUYDGVRIQRPHFX-UHFFFAOYSA-N hesperidin Natural products COc1cc(ccc1O)C2CC(=O)c3c(O)cc(OC4OC(COC5OC(O)C(O)C(O)C5O)C(O)C(O)C4O)cc3O2 VUYDGVRIQRPHFX-UHFFFAOYSA-N 0.000 claims abstract description 27
- 239000002537 cosmetic Substances 0.000 claims abstract description 21
- 239000003814 drug Substances 0.000 claims abstract description 10
- 150000003839 salts Chemical class 0.000 claims abstract description 8
- 239000000463 material Substances 0.000 claims abstract description 4
- 239000002207 metabolite Substances 0.000 claims abstract description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 34
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 26
- 239000006071 cream Substances 0.000 claims description 20
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 19
- 239000008213 purified water Substances 0.000 claims description 14
- 239000000499 gel Substances 0.000 claims description 13
- 239000006210 lotion Substances 0.000 claims description 13
- -1 astringent Substances 0.000 claims description 10
- 230000002708 enhancing effect Effects 0.000 claims description 9
- 230000002401 inhibitory effect Effects 0.000 claims description 8
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims description 7
- 239000004359 castor oil Substances 0.000 claims description 7
- 235000019438 castor oil Nutrition 0.000 claims description 7
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 7
- 230000037394 skin elasticity Effects 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 239000011505 plaster Substances 0.000 claims description 6
- 239000000843 powder Substances 0.000 claims description 6
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 claims description 4
- 238000009472 formulation Methods 0.000 claims description 4
- 239000008187 granular material Substances 0.000 claims description 4
- 229960003639 laurocapram Drugs 0.000 claims description 4
- 230000003020 moisturizing effect Effects 0.000 claims description 4
- 235000016709 nutrition Nutrition 0.000 claims description 4
- 239000005995 Aluminium silicate Substances 0.000 claims description 3
- 108010010803 Gelatin Proteins 0.000 claims description 3
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 3
- 235000012211 aluminium silicate Nutrition 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000008273 gelatin Substances 0.000 claims description 3
- 229920000159 gelatin Polymers 0.000 claims description 3
- 235000019322 gelatine Nutrition 0.000 claims description 3
- 235000011852 gelatine desserts Nutrition 0.000 claims description 3
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 claims description 3
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 3
- 229910052782 aluminium Inorganic materials 0.000 claims description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims description 2
- 239000004411 aluminium Substances 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- 239000004927 clay Substances 0.000 claims description 2
- 238000010410 dusting Methods 0.000 claims description 2
- 239000006260 foam Substances 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 230000008099 melanin synthesis Effects 0.000 claims description 2
- 229920002401 polyacrylamide Polymers 0.000 claims description 2
- 239000002453 shampoo Substances 0.000 claims description 2
- 239000000344 soap Substances 0.000 claims description 2
- 159000000000 sodium salts Chemical class 0.000 claims description 2
- 239000008406 cosmetic ingredient Substances 0.000 claims 1
- 239000000686 essence Substances 0.000 claims 1
- 239000008269 hand cream Substances 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 abstract description 3
- 208000026935 allergic disease Diseases 0.000 abstract description 3
- 230000007815 allergy Effects 0.000 abstract description 3
- 230000008961 swelling Effects 0.000 abstract description 3
- 230000002195 synergetic effect Effects 0.000 abstract description 3
- 206010067482 No adverse event Diseases 0.000 abstract description 2
- 230000035699 permeability Effects 0.000 abstract description 2
- 230000002829 reductive effect Effects 0.000 abstract description 2
- 201000004624 Dermatitis Diseases 0.000 abstract 1
- 210000004204 blood vessel Anatomy 0.000 abstract 1
- 230000008034 disappearance Effects 0.000 abstract 1
- 210000002780 melanosome Anatomy 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 description 37
- 238000002360 preparation method Methods 0.000 description 29
- 238000012360 testing method Methods 0.000 description 17
- 230000000694 effects Effects 0.000 description 14
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 12
- 239000012071 phase Substances 0.000 description 12
- 238000003756 stirring Methods 0.000 description 12
- 235000011187 glycerol Nutrition 0.000 description 11
- 229960005150 glycerol Drugs 0.000 description 11
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 8
- 241000283973 Oryctolagus cuniculus Species 0.000 description 8
- 229960004063 propylene glycol Drugs 0.000 description 8
- 230000007794 irritation Effects 0.000 description 7
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 6
- 206010040880 Skin irritation Diseases 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 6
- 239000003921 oil Substances 0.000 description 6
- 235000019198 oils Nutrition 0.000 description 6
- 231100000475 skin irritation Toxicity 0.000 description 6
- 230000036556 skin irritation Effects 0.000 description 6
- 235000002639 sodium chloride Nutrition 0.000 description 6
- 230000003110 anti-inflammatory effect Effects 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 description 5
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 description 5
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 description 5
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 description 5
- 238000011156 evaluation Methods 0.000 description 5
- 230000001815 facial effect Effects 0.000 description 5
- 238000002156 mixing Methods 0.000 description 5
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 4
- 206010015150 Erythema Diseases 0.000 description 4
- 229920002125 Sokalan® Polymers 0.000 description 4
- 229960002233 benzalkonium bromide Drugs 0.000 description 4
- KHSLHYAUZSPBIU-UHFFFAOYSA-M benzododecinium bromide Chemical compound [Br-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 KHSLHYAUZSPBIU-UHFFFAOYSA-M 0.000 description 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 4
- 229960001631 carbomer Drugs 0.000 description 4
- 229940075529 glyceryl stearate Drugs 0.000 description 4
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 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
- YPFDHNVEDLHUCE-UHFFFAOYSA-N 1,3-propanediol Substances OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 239000003963 antioxidant agent Substances 0.000 description 3
- 230000003078 antioxidant effect Effects 0.000 description 3
- 235000006708 antioxidants Nutrition 0.000 description 3
- 230000003796 beauty Effects 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 230000036541 health Effects 0.000 description 3
- 239000011159 matrix material Substances 0.000 description 3
- 230000036564 melanin content Effects 0.000 description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 3
- 239000002304 perfume Substances 0.000 description 3
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 3
- 229920000053 polysorbate 80 Polymers 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 239000002562 thickening agent Substances 0.000 description 3
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- 239000005711 Benzoic acid Substances 0.000 description 2
- 229920001661 Chitosan Polymers 0.000 description 2
- 206010008570 Chloasma Diseases 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- XMSXQFUHVRWGNA-UHFFFAOYSA-N Decamethylcyclopentasiloxane Chemical compound C[Si]1(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O1 XMSXQFUHVRWGNA-UHFFFAOYSA-N 0.000 description 2
- 102000009123 Fibrin Human genes 0.000 description 2
- 108010073385 Fibrin Proteins 0.000 description 2
- BWGVNKXGVNDBDI-UHFFFAOYSA-N Fibrin monomer Chemical compound CNC(=O)CNC(=O)CN BWGVNKXGVNDBDI-UHFFFAOYSA-N 0.000 description 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- 229920001214 Polysorbate 60 Polymers 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 229920002385 Sodium hyaluronate Polymers 0.000 description 2
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 2
- 235000021355 Stearic acid Nutrition 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 239000008346 aqueous phase Substances 0.000 description 2
- 235000010233 benzoic acid Nutrition 0.000 description 2
- 229960004365 benzoic acid Drugs 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 238000005282 brightening Methods 0.000 description 2
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 229960000541 cetyl alcohol Drugs 0.000 description 2
- 229940045110 chitosan Drugs 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 239000003086 colorant Substances 0.000 description 2
- 238000001816 cooling Methods 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 229960001760 dimethyl sulfoxide Drugs 0.000 description 2
- 239000003995 emulsifying agent Substances 0.000 description 2
- 230000001804 emulsifying effect Effects 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 239000003623 enhancer Substances 0.000 description 2
- 231100000321 erythema Toxicity 0.000 description 2
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 229950003499 fibrin Drugs 0.000 description 2
- 229940075507 glyceryl monostearate Drugs 0.000 description 2
- 210000004209 hair Anatomy 0.000 description 2
- 238000010438 heat treatment Methods 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 230000000670 limiting effect Effects 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 2
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 2
- 229960002216 methylparaben Drugs 0.000 description 2
- 230000004089 microcirculation Effects 0.000 description 2
- 239000002480 mineral oil Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 2
- KUDPGZONDFORKU-UHFFFAOYSA-N n-chloroaniline Chemical compound ClNC1=CC=CC=C1 KUDPGZONDFORKU-UHFFFAOYSA-N 0.000 description 2
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 2
- 239000002674 ointment Substances 0.000 description 2
- 239000004006 olive oil Substances 0.000 description 2
- 235000008390 olive oil Nutrition 0.000 description 2
- 230000003204 osmotic effect Effects 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 2
- 229940068968 polysorbate 80 Drugs 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 230000002335 preservative effect Effects 0.000 description 2
- BHZOKUMUHVTPBX-UHFFFAOYSA-M sodium acetic acid acetate Chemical compound [Na+].CC(O)=O.CC([O-])=O BHZOKUMUHVTPBX-UHFFFAOYSA-M 0.000 description 2
- 239000001509 sodium citrate Substances 0.000 description 2
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 2
- 229940083575 sodium dodecyl sulfate Drugs 0.000 description 2
- 229940010747 sodium hyaluronate Drugs 0.000 description 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 2
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 2
- 235000010199 sorbic acid Nutrition 0.000 description 2
- 239000004334 sorbic acid Substances 0.000 description 2
- 229940075582 sorbic acid Drugs 0.000 description 2
- 239000000600 sorbitol Substances 0.000 description 2
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 2
- 239000008117 stearic acid Substances 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 235000015112 vegetable and seed oil Nutrition 0.000 description 2
- 239000008158 vegetable oil Substances 0.000 description 2
- 210000003462 vein Anatomy 0.000 description 2
- 239000003871 white petrolatum Substances 0.000 description 2
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 1
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical compound C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 description 1
- DNIAPMSPPWPWGF-VKHMYHEASA-N (+)-propylene glycol Chemical compound C[C@H](O)CO DNIAPMSPPWPWGF-VKHMYHEASA-N 0.000 description 1
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 1
- REPVLJRCJUVQFA-UHFFFAOYSA-N (-)-isopinocampheol Natural products C1C(O)C(C)C2C(C)(C)C1C2 REPVLJRCJUVQFA-UHFFFAOYSA-N 0.000 description 1
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 description 1
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 1
- KIUKXJAPPMFGSW-YXBJCWEESA-N (2s,4s,5r,6s)-6-[(2s,3r,5s,6r)-3-acetamido-2-[(3s,4r,5r,6r)-6-[(3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H](C(O[C@@H]3[C@@H]([C@@H](O)C(O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)C(C(O)=O)O1 KIUKXJAPPMFGSW-YXBJCWEESA-N 0.000 description 1
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- FCGXLCNBWYIEAA-UHFFFAOYSA-N 1,3-benzothiazol-6-ylmethanamine Chemical compound NCC1=CC=C2N=CSC2=C1 FCGXLCNBWYIEAA-UHFFFAOYSA-N 0.000 description 1
- 229940035437 1,3-propanediol Drugs 0.000 description 1
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- SPSPIUSUWPLVKD-UHFFFAOYSA-N 2,3-dibutyl-6-methylphenol Chemical compound CCCCC1=CC=C(C)C(O)=C1CCCC SPSPIUSUWPLVKD-UHFFFAOYSA-N 0.000 description 1
- QAQJMLQRFWZOBN-UHFFFAOYSA-N 2-(3,4-dihydroxy-5-oxo-2,5-dihydrofuran-2-yl)-2-hydroxyethyl hexadecanoate Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(O)C1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-UHFFFAOYSA-N 0.000 description 1
- LCVHZNSIAYNAGX-UHFFFAOYSA-N 2-ethylhexyl 3,5,5-trimethylhexanoate Chemical compound CCCCC(CC)COC(=O)CC(C)CC(C)(C)C LCVHZNSIAYNAGX-UHFFFAOYSA-N 0.000 description 1
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 1
- BGRXBNZMPMGLQI-UHFFFAOYSA-N 2-octyldodecyl tetradecanoate Chemical compound CCCCCCCCCCCCCC(=O)OCC(CCCCCCCC)CCCCCCCCCC BGRXBNZMPMGLQI-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
- GUPXYSSGJWIURR-UHFFFAOYSA-N 3-octoxypropane-1,2-diol Chemical compound CCCCCCCCOCC(O)CO GUPXYSSGJWIURR-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical compound OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- JRLTTZUODKEYDH-UHFFFAOYSA-N 8-methylquinoline Chemical group C1=CN=C2C(C)=CC=CC2=C1 JRLTTZUODKEYDH-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 241000416162 Astragalus gummifer Species 0.000 description 1
- 101800004538 Bradykinin Proteins 0.000 description 1
- 239000004255 Butylated hydroxyanisole Substances 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
- QUVCFQAHXXKABX-UHFFFAOYSA-K C(CO)(=O)[O-].O[Al+]O Chemical compound C(CO)(=O)[O-].O[Al+]O QUVCFQAHXXKABX-UHFFFAOYSA-K 0.000 description 1
- 229920000298 Cellophane Polymers 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
- 208000017701 Endocrine disease Diseases 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 description 1
- 206010018910 Haemolysis Diseases 0.000 description 1
- 206010022998 Irritability Diseases 0.000 description 1
- 102100035792 Kininogen-1 Human genes 0.000 description 1
- 235000000072 L-ascorbyl-6-palmitate Nutrition 0.000 description 1
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 description 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- 235000018330 Macadamia integrifolia Nutrition 0.000 description 1
- 240000000912 Macadamia tetraphylla Species 0.000 description 1
- 235000003800 Macadamia tetraphylla Nutrition 0.000 description 1
- 206010025421 Macule Diseases 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 208000012641 Pigmentation disease Diseases 0.000 description 1
- 206010058679 Skin oedema Diseases 0.000 description 1
- 206010040914 Skin reaction Diseases 0.000 description 1
- NWGKJDSIEKMTRX-AAZCQSIUSA-N Sorbitan monooleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O NWGKJDSIEKMTRX-AAZCQSIUSA-N 0.000 description 1
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- LSNNMFCWUKXFEE-UHFFFAOYSA-N Sulfurous acid Chemical compound OS(O)=O LSNNMFCWUKXFEE-UHFFFAOYSA-N 0.000 description 1
- 206010042674 Swelling Diseases 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- 102000003425 Tyrosinase Human genes 0.000 description 1
- 108060008724 Tyrosinase Proteins 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- 240000008042 Zea mays Species 0.000 description 1
- 235000016383 Zea mays subsp huehuetenangensis Nutrition 0.000 description 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000006838 adverse reaction Effects 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 description 1
- 150000003862 amino acid derivatives Chemical class 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 230000036783 anaphylactic response Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- 230000002421 anti-septic effect Effects 0.000 description 1
- 230000001153 anti-wrinkle effect Effects 0.000 description 1
- 239000003212 astringent agent Substances 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000003157 biological pigment Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 229940116229 borneol Drugs 0.000 description 1
- CKDOCTFBFTVPSN-UHFFFAOYSA-N borneol Natural products C1CC2(C)C(C)CC1C2(C)C CKDOCTFBFTVPSN-UHFFFAOYSA-N 0.000 description 1
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 description 1
- OWBTYPJTUOEWEK-UHFFFAOYSA-N butane-2,3-diol Chemical compound CC(O)C(C)O OWBTYPJTUOEWEK-UHFFFAOYSA-N 0.000 description 1
- 235000019282 butylated hydroxyanisole Nutrition 0.000 description 1
- CZBZUDVBLSSABA-UHFFFAOYSA-N butylated hydroxyanisole Chemical compound COC1=CC=C(O)C(C(C)(C)C)=C1.COC1=CC=C(O)C=C1C(C)(C)C CZBZUDVBLSSABA-UHFFFAOYSA-N 0.000 description 1
- 229940043253 butylated hydroxyanisole Drugs 0.000 description 1
- 229940095259 butylated hydroxytoluene Drugs 0.000 description 1
- 239000010495 camellia oil Substances 0.000 description 1
- 229940049638 carbomer homopolymer type c Drugs 0.000 description 1
- 229940043234 carbomer-940 Drugs 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 229960001777 castor oil Drugs 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000002738 chelating agent Substances 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 229960002152 chlorhexidine acetate Drugs 0.000 description 1
- 229960001231 choline Drugs 0.000 description 1
- OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 description 1
- 230000000295 complement effect Effects 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 229940099112 cornstarch Drugs 0.000 description 1
- 239000000490 cosmetic additive Substances 0.000 description 1
- 238000005336 cracking Methods 0.000 description 1
- 238000004132 cross linking Methods 0.000 description 1
- 229940086555 cyclomethicone Drugs 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
- MSJMDZAOKORVFC-UAIGNFCESA-L disodium maleate Chemical compound [Na+].[Na+].[O-]C(=O)\C=C/C([O-])=O MSJMDZAOKORVFC-UAIGNFCESA-L 0.000 description 1
- DTGKSKDOIYIVQL-UHFFFAOYSA-N dl-isoborneol Natural products C1CC2(C)C(O)CC1C2(C)C DTGKSKDOIYIVQL-UHFFFAOYSA-N 0.000 description 1
- 229940126534 drug product Drugs 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000002124 endocrine Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 210000003743 erythrocyte Anatomy 0.000 description 1
- 229940100549 ethylhexyl isononanoate Drugs 0.000 description 1
- 229940044949 eucalyptus oil Drugs 0.000 description 1
- 239000010642 eucalyptus oil Substances 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 239000003527 fibrinolytic agent Substances 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 235000001727 glucose Nutrition 0.000 description 1
- 229940087068 glyceryl caprylate Drugs 0.000 description 1
- 229940100242 glycol stearate Drugs 0.000 description 1
- 239000008202 granule composition Substances 0.000 description 1
- 239000008169 grapeseed oil Substances 0.000 description 1
- 230000008588 hemolysis Effects 0.000 description 1
- 230000002439 hemostatic effect Effects 0.000 description 1
- ZUVCYFMOHFTGDM-UHFFFAOYSA-N hexadecyl dihydrogen phosphate Chemical compound CCCCCCCCCCCCCCCCOP(O)(O)=O ZUVCYFMOHFTGDM-UHFFFAOYSA-N 0.000 description 1
- 229960001340 histamine Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000003906 humectant Substances 0.000 description 1
- 229920002674 hyaluronan Polymers 0.000 description 1
- 229960003160 hyaluronic acid Drugs 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000002085 irritant Substances 0.000 description 1
- 231100000021 irritant Toxicity 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 210000000265 leukocyte Anatomy 0.000 description 1
- 150000002617 leukotrienes Chemical class 0.000 description 1
- 235000009973 maize Nutrition 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229940057917 medium chain triglycerides Drugs 0.000 description 1
- 210000002752 melanocyte Anatomy 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000013508 migration Methods 0.000 description 1
- 230000005012 migration Effects 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 229940042472 mineral oil Drugs 0.000 description 1
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 1
- 239000004745 nonwoven fabric Substances 0.000 description 1
- 239000010466 nut oil Substances 0.000 description 1
- 235000003715 nutritional status Nutrition 0.000 description 1
- 229940073665 octyldodecyl myristate Drugs 0.000 description 1
- 239000003002 pH adjusting agent Substances 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 230000019612 pigmentation Effects 0.000 description 1
- 229940012957 plasmin Drugs 0.000 description 1
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
- 229940113124 polysorbate 60 Drugs 0.000 description 1
- 229920000166 polytrimethylene carbonate Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 239000000473 propyl gallate Substances 0.000 description 1
- 235000010388 propyl gallate Nutrition 0.000 description 1
- 229940075579 propyl gallate Drugs 0.000 description 1
- MCSINKKTEDDPNK-UHFFFAOYSA-N propyl propionate Chemical compound CCCOC(=O)CC MCSINKKTEDDPNK-UHFFFAOYSA-N 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- GHBFNMLVSPCDGN-UHFFFAOYSA-N rac-1-monooctanoylglycerol Chemical compound CCCCCCCC(=O)OCC(O)CO GHBFNMLVSPCDGN-UHFFFAOYSA-N 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 229920002545 silicone oil Polymers 0.000 description 1
- 230000005808 skin problem Effects 0.000 description 1
- 230000035483 skin reaction Effects 0.000 description 1
- 231100000430 skin reaction Toxicity 0.000 description 1
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 description 1
- 229960005055 sodium ascorbate Drugs 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 229950004959 sorbitan oleate Drugs 0.000 description 1
- 229950011392 sorbitan stearate Drugs 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 229940032094 squalane Drugs 0.000 description 1
- 229960004274 stearic acid Drugs 0.000 description 1
- 230000000475 sunscreen effect Effects 0.000 description 1
- 239000000516 sunscreening agent Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 1
- XPFJYKARVSSRHE-UHFFFAOYSA-K trisodium;2-hydroxypropane-1,2,3-tricarboxylate;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound [Na+].[Na+].[Na+].OC(=O)CC(O)(C(O)=O)CC(O)=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O XPFJYKARVSSRHE-UHFFFAOYSA-K 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- 210000005167 vascular cell Anatomy 0.000 description 1
- 210000003556 vascular endothelial cell Anatomy 0.000 description 1
- 230000002666 vasoprotective effect Effects 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
-
- 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
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
-
- 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
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
-
- 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
- A61Q19/08—Anti-ageing preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/59—Mixtures
- A61K2800/592—Mixtures of compounds complementing their respective functions
- A61K2800/5922—At least two compounds being classified in the same subclass of A61K8/18
Abstract
The invention discloses a composition for removing freckles, whitening and resisting inflammation of skin and application thereof, wherein the composition comprises a component A and a component B, the component A is tranexamic acid or cosmetic and pharmaceutically acceptable salt thereof, and the component B is one or/and a plurality of diosmin and metabolite thereof; the weight ratio of the component A to the component B in the composition is 0.1: 1-20: 1. The composition provided by the invention takes the component A as a main whitening component, so that the generation of melanin is reduced; the matching component B maintains the normal permeability of blood vessels and promotes the transfer and disappearance of melanosomes, the two have the synergistic effect, and have no adverse reactions such as red swelling, allergy and the like, and can be effectively used as materials of functional cosmetics and/or medicaments.
Description
Technical Field
The invention relates to a composition containing tranexamic acid and diosmin as effective components, in particular to a composition for inhibiting melanin generation, enhancing skin elasticity, removing freckles, whitening and resisting inflammation and application thereof.
Background
In recent years, with the development of medical technology, the life of people is prolonged, the quality of life and the demand for health beauty are increased, and further, the interest in skin beauty and health is stronger. Therefore, various functional cosmetics, health products and medicines are developed on the market for preventing, alleviating and improving skin problems, such as skin spot removal, skin whitening and the like.
Melanin is a biological pigment formed by a series of chemical reactions of tyrosine or 3, 4-diphenylalanine. Melanin is actually an amino acid derivative, a protein present in the basal layer of the skin of everyone. The production of melanin is mostly related to endocrine disorders and sunlight irradiation, and the number of melanocytes is mainly determined by heredity, and is also related to endocrine hormones and nutritional status, and diseases caused by melanin are as follows: freckle, chloasma, melanosis, etc. have been the subject of research in the beauty industry.
Tranexamic acid (Tranexamic acid), also known as Tranexamic acid, Tranexamic acid. Tranexamic acid is used as a synthetic amino acid fibrinolytic drug on one hand, can competitively inhibit the combination of the lysine of fibrin and plasmin, thereby inhibiting the cracking of fibrin clot and generating the hemostatic effect. On the other hand, the tranexamic acid has a similar structure with the tyrosine part participating in melanin metabolites and has a carboxyl group, so that the tranexamic acid can competitively inhibit tyrosinase, further reduce the formation of melanin, has the effects of removing black and removing speckles which are about 50 times higher than that of vitamin C and about 10 times higher than that of tartaric acid, and can be used as a cosmetic additive.
Diosmin (Diosmin) is a drug that enhances venous tone and a vasoprotective agent. The functions are mainly embodied in the following three aspects: diosmin has specific affinity to veins, and can enhance the tension of veins without affecting the arterial system; secondly, diosmin can obviously reduce the adhesion, migration and disintegration of leukocytes and vascular endothelial cells to release inflammatory substances, such as histamine, bradykinin, complement, leukotriene, prostaglandin, excessive free radicals and the like, thereby reducing the permeability of capillary vessels and enhancing the tension of the capillary vessels; and the diosmin also has the functions of reducing the viscosity of blood and enhancing the flow rate of red blood cells, thereby reducing the condition of microcirculation stasis.
The research shows that the whitening effect of the tranexamic acid is not obvious enough when the tranexamic acid is used alone, and the tranexamic acid is probably related to that the tranexamic acid can only decompose spots and cannot quickly discharge the spots out of the body. The invention combines tranexamic acid and diosmin, and surprisingly discovers that melanin decomposed by tranexamic acid is quickly discharged due to the action of diosmin on microcirculation, so that the effects of quickly removing freckles and whitening are achieved, and the tranexamic acid and the diosmin have synergistic action.
Disclosure of Invention
In view of the above, the present invention aims to provide a composition having the effects of inhibiting melanin formation, enhancing skin elasticity, removing freckles, whitening skin and resisting inflammation, so as to solve the problems in the prior art.
In order to achieve the purpose, the technical scheme of the invention is as follows:
a composition with effects of inhibiting melanin generation, enhancing skin elasticity, removing macula, whitening skin and resisting inflammation comprises component A and component B, wherein component A is tranexamic acid or its cosmetic, food or pharmaceutically acceptable salt, and component B is one or/and more of diosmin and its metabolite; the composition can be cosmetic or/and pharmaceutical.
In one aspect, the present invention provides a cosmetic composition having melanin production inhibiting, skin elasticity enhancing, spot removing, skin whitening, and anti-inflammatory effects.
In the cosmetic composition, the ratio of the component A to the component B is 0.1: 1-20: 1, preferably 1: 1-10: 1, and more preferably 2: 1-8: 1.
The cosmetic composition of the present invention may include, in addition to the component a and the component B, other additives such as adjuvants, carriers, etc., and may be applied and formulated as required to common ingredients used in general skin cosmetics.
Specifically, the cosmetic composition of the present invention may further include a transdermal enhancer so that the desired ingredients are permeated into the vascular cells of the skin at a high absorption rate. The transdermal enhancers include, but are not limited to, menthol, borneol, eucalyptus oil, laurocapram, dimethyl sulfoxide, propylene glycol, dimethyl isosorbide anhydride, N-alkylbenzisothiazolone.
The cosmetic composition of the present invention may further comprise an oil phase ingredient selected from one or more of, but not limited to, vegetable oils, mineral oils, silicone oils, and synthetic oils. More specifically, mineral oil, cyclomethicone, squalane, octyldodecyl myristate, olive oil, grapeseed oil, macadamia nut oil, glyceryl caprylate, castor oil, ethylhexyl isononanoate, cyclopentasiloxane, and the like can be used.
The cosmetic composition can be added with 0.1-5% of surfactant, higher alcohol and the like to enhance the emulsifying capacity. Wherein the surfactant is selected from one or more of, but not limited to, sorbitan betaquinate, polysorbate 60, glyceryl stearate, lipophilic glyceryl stearate, sorbitan oleate, cetyl phosphate, sorbitan stearate/sucrose ester, glyceryl stearate/polyethylene glycol 100 stearate; the alcohols are selected from one or more of acetyl alcohol, lithol alcohol and octadiol.
The cosmetic composition of the invention can further comprise an aqueous phase component, wherein 0.0001-8% of one or more thickening agents such as xanthan gum, magnesium aluminum silicate, cellulose and the like can be added to adjust the viscosity or hardness of the aqueous phase.
In addition, if necessary, the cosmetic composition of the present invention may further comprise other functional or non-functional ingredients, such as sunscreen cream, vitamins, chelating agent, antioxidant (e.g., dibenzoic acid acetate, butylated hydroxytoluene, etc.), antiseptic (e.g., ethylparaben, methylparaben, benzoic acid and salts thereof, sorbic acid and salts thereof, benzyl alcohol, benzalkonium bromide, chitosan, phenylalamine, chloroaniline), colorant, pH adjuster (e.g., triethanolamine, citric acid, sodium citrate, malic acid, sodium maleate, soft acid, sodium hydroxide, disodium hydrogen phosphate, etc.), humectant (glycerin, sorbitol, propylene glycol, butylene glycol, methyl glucose, etc.), lubricant, perfume (natural perfume, synthetic perfume, etc.), etc., and the selection of the type thereof is not particularly limited, and ingredients well known to those skilled in the art of cosmetics may be used.
The cosmetic compositions of the present invention may be present in forms including, but not limited to, skin lotions, skin softeners, skin toners, astringents, lotions, creams, moisturizing lotions, nutritional lotions, massage creams, nutritional creams, moisturizing creams, hand creams, soaps, shampoos, cleansing foams, cleansing lotions, cleansing creams, body lotions, milky lotions, powders, dusting powders, eye shadows, and the like.
On the other hand, the invention provides a pharmaceutical composition with the functions of inhibiting melanin generation, enhancing skin elasticity, removing freckles, whitening and resisting inflammation.
In the pharmaceutical composition, the ratio of the component A to the component B is 0.1: 1-20: 1, preferably 1: 1-10: 1, and more preferably 2: 1-8: 1.
The pharmaceutical composition of the present invention may be administered orally or topically in the form of a general pharmaceutical preparation.
Solid formulations for oral administration include, but are not limited to, tablets, troches, powders, granules, capsules and the like. Liquid preparations for oral administration include, but are not limited to, suspensions, solvents, emulsions, syrups, and the like. External preparations for skin include, but are not limited to, emulsions, suspensions, lyophilized preparations, ointments, gels or gel plasters, patches or plasters, sprays, and the like. Preferably, the skin preparation is an external preparation.
The pharmaceutical composition of the invention can comprise other pharmaceutically acceptable additives such as auxiliary materials and carriers besides the component A and the component B, for example, a filler, a binder, a disintegrating agent, a lubricant, a coloring agent, an essence and the like can be added into an orally-administered preparation.
The skin external preparation prepared by the medicine composition can also be added with other functional components, such as anti-wrinkle components, whitening components, pore shrinking and the like.
For the skin external preparation prepared from the pharmaceutical composition of the present invention, one or more of an oil phase component, an emulsifier, a water phase component, and a pharmaceutical additive (thickener, osmotic pressure regulator, pH regulator, antioxidant, preservative, etc.) may be added.
More specifically, the oil phase ingredients include, but are not limited to, one or more of vegetable oils (such as soybean oil, tea oil, sesame oil, peanut oil, olive oil, castor oil, and the like), medium chain triglycerides, isopropyl myristate, and the like.
The emulsifier includes, but is not limited to, one or more of tween 80, tween 60, maize 52, glyceryl stearate, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, lecithin, polyethylene glycol stearate, and choline dimyristophosphatidate.
The preservative includes but is not limited to one or more of paraben, ethylparaben, methylparaben, benzoic acid and salts thereof, sorbic acid and salts thereof, benzyl alcohol, benzalkonium bromide, chitosan, phenylalamine, chloroaniline, and chlorhexidine acetate.
The thickening agent includes, but is not limited to, one or more of carbomer, hyaluronic acid, sodium hyaluronate, povidone, tragacanth, cellulosic compounds.
The osmotic pressure regulator includes but is not limited to one or more of glucose, sodium chloride, potassium chloride, mannitol, sucrose, propylene glycol, glycerol, and sorbitol.
The antioxidant includes but is not limited to one or more of butylated hydroxyanisole, dibutyl hydroxytoluene, D-sodium ascorbate, L-ascorbyl palmitate, propyl gallate and sulfite.
The pH regulator includes but is not limited to one or more of hydrochloric acid, sodium hydroxide, potassium hydroxide, tromethamine, acetic acid-sodium acetate, citric acid-sodium citrate and phosphate.
Detailed Description
In the following description, numerous specific details are set forth in order to provide a thorough understanding of the present invention. This invention may, however, be embodied in many different forms and should not be construed as limited to the embodiments set forth herein, but rather should be construed as broadly as the present invention is capable of modification in various respects, all without departing from the spirit and scope of the present invention.
Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. The terminology used in the description of the invention herein is for the purpose of describing particular embodiments only and is not intended to be limiting of the invention.
Example 1 cosmetic preparation
1-1 preparation of face cream
TABLE 1-1 composition Table of cream
| Composition of matter | Parts by weight |
| Tranexamic acid | 1 |
| Diosmin A-D-E | 0.2 |
| Stearic acid | 17 |
| Cetyl alcohol | 1 |
| Potassium hydroxide | 1 |
| Glycerol | 5 |
| EDTA-2Na | 0.02 |
| Propylene glycol | 3 |
| Hydroxyphenyl Ethyl ester | 0.1 |
| Purified water | Is supplemented to 100 |
The preparation method comprises the following steps:
heating propylene glycol, stearic acid and cetyl alcohol to 80-90 ℃, and stirring for dissolving to obtain a mixture A; heating purified water, glycerol and EDTA-2Na to 80-90 ℃, stirring to dissolve, adding the mixture A, and homogenizing for 5 minutes; and cooling to 30-35 ℃, adding ethylparaben, and uniformly stirring to obtain the face cream.
Essence preparation
TABLE 1-2 essence compositions
| Composition of matter | Parts by weight |
| Tranexamic acid | 3 |
| Diosmin A-D-E | 1 |
| EDTA-2Na | 0.02 |
| Hyaluronic acid sodium salt | 1.5 |
| Carbomer | 0.2 |
| Citric acid sodium salt | 0.15 |
| Dimethyl isosorbide anhydride | 1.8 |
| Methyl propylene glycol | 8 |
| 1, 3-propanediol | 15 |
| Purified water | Is supplemented to 100 |
The preparation method comprises the following steps:
adding EDTA-2Na and carbomer into water, stirring, adding sodium hyaluronate, stirring, adding sodium citrate and tranexamic acid, stirring, adding methyl propylene glycol, 1, 3-propylene glycol and isosorbide dimethyl ether, and stirring to obtain the essence.
Example 2 preparation of drug product
2-1 preparation of granules
TABLE 2-1 granule composition
| Composition of matter | Parts by weight |
| Tranexamic acid | 70 |
| Diosmin A-D-E | 10 |
| Corn starch | 10 |
| Lactose | 10 |
The preparation method comprises the following steps:
mixing tranexamic acid, diosmin, corn starch and lactose, , adding appropriate amount of purified water, granulating, drying at 60 deg.C, and grading to obtain granule.
The prepared granular preparation is filled and further tabletted to obtain tablets.
Gel preparation
TABLE 2-2 gel composition
| Composition of matter | Parts by weight |
| Tranexamic acid | 10 |
| Diosmin A-D-E | 2 |
| Carbomer 940 | 10 |
| Tri-ethanol | 4 |
| Glycerol | 40 |
| Hydroxyphenyl Ethyl ester | 0.5 |
| Polysorbate 80 | 2 |
| Potassium hydroxide | 4 |
| Purified water | Is supplemented to 100 |
The preparation method comprises the following steps:
taking carbomer, glycerin, polysorbate 80 and a proper amount of purified water, standing for 4.0-4.5 hours, fully stirring until swelling, adding triethanolamine, stirring uniformly, and adjusting the pH value to 5-6 by using potassium hydroxide to obtain a matrix; mixing tranexamic acid, diosmin, glycerol and ethylparaben uniformly, adding into the matrix while stirring, and adding purified water to make up to a sufficient amount to obtain gel.
Preparation of gel plaster
TABLE 2-3 gel plaster Components
| Composition of matter | Parts by weight |
| Tranexamic acid | 10 |
| Diosmin A-D-E | 2 |
| Polyacrylamide sodium salt | 4.8 |
| Gelatin | 4.8 |
| Kaolin clay | 3.2 |
| Aluminium glycollate | 0.04 |
| Castor oil | 0.08 |
| Glycerol | 44.8 |
| Polyvinyl alcohol | 0.8 |
| EDTA-2Na | 0.12 |
| Laurocapram | 2.4 |
| Propylene glycol | 4 |
| Purified water | Is supplemented to 100 |
The preparation method comprises the following steps:
uniformly mixing sodium polyacrylate, gelatin, dihydroxyaluminum glycolate, kaolin, EDTA-2Na, castor oil and glycerol to obtain a phase A; dissolving polyvinyl alcohol laurocapram, propylene glycol, tranexamic acid and diosmin in purified water to obtain phase B. Pouring the phase B into the phase A quickly, stirring fully and crosslinking to form paste, quickly coating on the non-woven fabric of the backing material, and covering with an anti-sticking film to obtain the gel plaster.
Preparation of gel plaster
Compared with the examples 2-3, the present example only differs from the purified water in weight parts, the present example has 10 weight parts of diosmin, and the purified water is supplemented to 100.
Cream preparation
TABLE 2-5 cream Components
| Composition of matter | Parts by weight |
| Tranexamic acid | 10 |
| Diosmin A-D-E | 2 |
| Glycerol | 3 |
| Sodium dodecyl sulfate | 1 |
| Hydroxyphenyl Ethyl ester | 0.2 |
| Dimethyl sulfoxide | 7 |
| Benzalkonium bromide solution | 3 |
| Glyceryl monostearate | 30 |
| White vaseline | 30 |
| Purified water | Make up the balance |
The preparation method comprises the following steps:
mixing glycerol, sodium dodecyl sulfate, ethylparaben, dimethyl sulfoxide, benzalkonium bromide solution, tranexamic acid, diosmin and purified water at 100 deg.C to obtain water phase; mixing glyceryl monostearate and white vaseline at 95 deg.C for 30 min to obtain oil phase; stirring the water phase and the oil phase in an emulsifying tank under the vacuum degree of 0.05MPa for 30 min, homogenizing at 3000r/min for 30 min, cooling to 50 deg.C, and bottling to obtain ointment.
Example 3 skin irritation test
According to the research technical guide principle of the irritation, the anaphylaxis and the hemolysis of the chemical drugs, the skin irritation investigation of the tranexamic acid-diosmin skin external preparation is carried out by adopting the following method.
The experimental method comprises the following steps: 6 rabbits are selected, male and female are not limited, the weight is 2.5 +/-0.5 kg, and the hairs on two sides of the spine of the back of the rabbit are cut off before the experiment, wherein the range is about 3 cm. Directly coating the skin of the rabbit with hair removed from one side of the skin of the rabbit in the examples 1-1, 1-2, 2-2 and 2-4, covering the skin with two layers of gauze and a layer of cellophane or the like, and fixing the skin with a non-irritant adhesive plaster and a bandage; the other side was coated with a blank formulation as a control. The skin of the rabbit which is unhaired on one side is directly pasted with the skin of the rabbit in the embodiment 2-3; the other side was coated with a blank matrix as a control. The application is carried out for 4 hours. After the application is completed, the test substance is removed and the administration site is cleaned with warm water. The skin irritation test of multiple administration should continuously administer the drug to the same part, each administration time is the same, the application period is 4 days, and irritation phenomenon is observed respectively at 1 day, 2 days, 3 days, 4 days of application and 24 hours, 48 hours, 72 hours after stopping administration.
And (4) observing results: the skin reaction was observed under natural light. Skin erythema and edema were scored according to the scoring criteria given in Table 3-1.
TABLE 3-1 skin irritation response Scoring criteria
TABLE 3-2 evaluation criteria for skin irritation intensity
| Score value | Evaluation of |
| 0-0.49 | Has no irritation |
| 0.5-2.99 | Mild irritation |
| 3.0-5.99 | Moderate irritation |
| 6.0-8.0 | Strong irritation |
Results of rabbit irritability examination: the rabbit skin is coated by the blank preparation and the examples for 1 day, 2 days, 3 days and 4 days, and no erythema or edema appears in 24 hours, 48 hours and 72 hours after the medicine is stopped, the score is 0, and the skin external preparation provided by the invention has no skin irritation and good safety.
Example 4 efficacy testing
The first efficacy test is as follows: melanin content test
Women with pigmentation, black spots and chloasma on the face are selected, 32 people are selected, the age is 20-50 years old, and the women are divided into 4 groups, and each group comprises 8 people. The essence and gel patch of examples 1-2 and 2-3 were used for each of the two groups, the commercially available essence containing only tranexamic acid was used for one group, and the base patch containing no active ingredient was used for the other group. The test subject uses the whitening skin care product once in the morning and at night every day for 28 days, and other whitening skin care products are not applicable in the same test period. After days 0, 14, and 28, the change in facial melanin content (mean) was measured using a memameter MX18 skin pigment analyzer, with smaller values indicating whiter skin. The test results are shown in the following table:
TABLE 4-1 determination of melanin content and rate of change
As can be seen from the above results, the skin melanin values of the subjects were significantly reduced at day 28 in the example group, while the blank group was almost unchanged, indicating that the whitening effect of the complex formulation of the present invention is significant; meanwhile, compared with the commercially available essence under the same test conditions, the whitening effect of the whitening cream is obviously superior to that of the commercially available essence, and the fact that the whitening cream added with diosmin can play a synergistic role together with tranexamic acid is demonstrated, and the whitening effect is enhanced.
And (5) efficacy test II: skin ITA value determination
For the subject in the first efficacy test, the facial skin of the subject was tested by using a VISIA-CR facial imager, and the ITA value of the facial skin was analyzed by using Image-Pro Pus Image analysis software, wherein the higher the ITA value, the brighter and whiter the skin. The results are shown in the following table.
TABLE 4-2 skin ITA value measurement results
As can be seen from the results in the table above, the change rate of the facial skin ITA value of the subject is large at day 28 in the example group, while the blank group is almost unchanged, which indicates that the whitening effect of the composite preparation of the invention is obvious; meanwhile, compared with the commercially available essence under the same test conditions, the whitening effect of the whitening essence is obviously superior to that of the commercially available essence, which shows that the whitening effect of the whitening essence can be further enhanced after the diosmin is added.
And (3) efficacy test: test of freckle-removing and anti-inflammatory soothing effects
For a subject in the first efficacy test, the freckle removing, anti-inflammatory and relieving effects of the subject are automatically evaluated through certain evaluation criteria, wherein the evaluation criteria are as follows:
TABLE 4-3 evaluation criteria for freckle-removing, anti-inflammatory and soothing effects
| Speckle removing effect | Scoring |
| The effect is obvious | 4 |
| Good effect | 3 |
| General effects | 2 |
| Has no obvious effect | 1 |
| Adverse reactions such as erythema and allergy | 0 |
TABLE 4-4 speckle removing and soothing effects test results
The results in the table show that the compound preparation has excellent freckle removing, anti-inflammatory, soothing and repairing effects and has no adverse reactions such as redness and swelling, allergy and the like.
In conclusion, the compound provided by the invention has excellent functions of removing freckles, whitening, brightening, resisting inflammation, relieving and repairing, has no irritation to skin, and can be used in functional cosmetics and/or medicines to play a role in removing freckles, whitening and brightening.
The technical features of the embodiments described above may be arbitrarily combined, and for the sake of brevity, all possible combinations of the technical features in the embodiments described above are not described, but should be considered as being within the scope of the present specification as long as there is no contradiction between the combinations of the technical features.
The above-mentioned embodiments only express several embodiments of the present invention, and the description thereof is more specific and detailed, but not construed as limiting the scope of the invention. It should be noted that, for a person skilled in the art, several variations and modifications can be made without departing from the inventive concept, which falls within the scope of the present invention. Therefore, the protection scope of the present patent shall be subject to the appended claims.
Claims (12)
1. The composition for removing freckles, whitening and resisting inflammation comprises a component A and a component B, and is characterized in that the component A is tranexamic acid or a cosmetic and pharmaceutically acceptable salt thereof, and the component B is diosmin and/or a metabolite thereof or one or more of the cosmetic and pharmaceutically acceptable salts thereof.
2. The composition of claim 1, wherein the weight ratio of component a (calculated as tranexamic acid) to component B is from 0.1:1 to 20: 1.
3. The composition of claim 1, wherein the weight ratio of component a (calculated as tranexamic acid) to component B is from 1:1 to 10: 1.
4. The composition of claim 1, wherein the weight ratio of component a (calculated as tranexamic acid) to component B is from 2:1 to 8: 1.
5. The composition according to claim 1, wherein the component B is one or/and more of diosmin and metabolites thereof.
6. The composition according to claim 1 to 5, wherein the composition is used as a material for cosmetics, pharmaceuticals, and the like.
7. The composition according to claims 1 to 6, wherein the composition is used as a cosmetic ingredient for inhibiting melanin production, enhancing skin elasticity, removing freckles, whitening and resisting inflammation.
8. The composition of claim 7, wherein the composition is present in a form including, but not limited to, skin lotion, skin softener, skin toning agent, astringent, lotion, essence, cream, moisturizing lotion, nutritional lotion, massage cream, nutritional cream, moisturizing cream, hand cream, soap, shampoo, cleansing foam, cleansing lotion, cleansing cream, body lotion, body cleanser, dusting powder, loose powder, eye shadow, and the like.
9. The composition according to claims 1 to 6, wherein the composition is used as a component of a medicine for inhibiting melanin generation, enhancing skin elasticity, removing freckles, whitening and resisting inflammation.
10. The composition of claim 9, wherein the pharmaceutical composition is administered orally or topically via skin, and is in the form of a tablet, granule, powder, capsule, liquid, pill, cream, gel, patch, plaster, gel patch, etc.
11. The composition according to claims 9-10, wherein the composition is administered by a route preferably topical administration to the skin, and the formulation is preferably a gel patch.
12. The composition according to claims 9 to 11, wherein the composition comprises the following components:
。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110252449.7A CN112891242A (en) | 2021-03-09 | 2021-03-09 | Composition for removing freckles, whitening and resisting inflammation and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110252449.7A CN112891242A (en) | 2021-03-09 | 2021-03-09 | Composition for removing freckles, whitening and resisting inflammation and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN112891242A true CN112891242A (en) | 2021-06-04 |
Family
ID=76108628
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202110252449.7A Pending CN112891242A (en) | 2021-03-09 | 2021-03-09 | Composition for removing freckles, whitening and resisting inflammation and application thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN112891242A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115624520A (en) * | 2022-12-21 | 2023-01-20 | 北京中科利华医药研究院有限公司 | Diosmin cream and application thereof |
| CN116531353A (en) * | 2023-07-07 | 2023-08-04 | 晶易医药科技(成都)有限公司 | Tranexamic acid composition, tranexamic acid gel plaster and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20040060157A (en) * | 2002-12-30 | 2004-07-06 | 주식회사 코리아나화장품 | Cosmetic Composition for Skin-Whitening Comprising Tranexamic Acid as Active Ingredient |
| WO2017213346A1 (en) * | 2016-06-09 | 2017-12-14 | 연세대학교 산학협력단 | Composition containing diosmin or salt thereof as active ingredient and having skin moisturizing improvement, skin exfoliation, skin elasticity enhancement, erythema inhibition, skin wrinkle alleviation, or skin photoaging retardation effect |
-
2021
- 2021-03-09 CN CN202110252449.7A patent/CN112891242A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20040060157A (en) * | 2002-12-30 | 2004-07-06 | 주식회사 코리아나화장품 | Cosmetic Composition for Skin-Whitening Comprising Tranexamic Acid as Active Ingredient |
| WO2017213346A1 (en) * | 2016-06-09 | 2017-12-14 | 연세대학교 산학협력단 | Composition containing diosmin or salt thereof as active ingredient and having skin moisturizing improvement, skin exfoliation, skin elasticity enhancement, erythema inhibition, skin wrinkle alleviation, or skin photoaging retardation effect |
Non-Patent Citations (3)
| Title |
|---|
| MOHAMED A. MEDHAT等: "Rare Extraperitoneal Involvement with Fatal Outcome in a Case of Bilateral Luteinized Thecoma of the Ovaries with Sclerosing Peritonitis", CASE REPORTS IN ONCOLOGICAL MEDICINE, 5 June 2014 (2014-06-05), pages 1 - 7 * |
| PUSPALATA BASHYAL 等: "Comparative study on melanin production and collagen expression profile of polyphenols and their glycosides", INDIAN JOURNAL OF BIOCHEMISTRY & BIOPHYSICS, vol. 56, 30 April 2019 (2019-04-30), pages 137 - 143 * |
| 王晓冬等: "地奥司明联合氨甲环酸治疗老年股骨转子间骨折术后隐性失血的疗效分析", 实用临床医药杂志, vol. 17, no. 21, 31 December 2013 (2013-12-31), pages 139 - 142 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115624520A (en) * | 2022-12-21 | 2023-01-20 | 北京中科利华医药研究院有限公司 | Diosmin cream and application thereof |
| CN116531353A (en) * | 2023-07-07 | 2023-08-04 | 晶易医药科技(成都)有限公司 | Tranexamic acid composition, tranexamic acid gel plaster and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US4610978A (en) | Compositions containing 1α-hydroxycholecalciferol for topical treatment of skin disorders and methods employing same | |
| JP6055518B2 (en) | Skin preparation for external use | |
| US6447817B1 (en) | Anti-inflammatory analgesic | |
| WO1999059580A1 (en) | Preventives/remedies for skin diseases | |
| JP2004538308A (en) | Skin treatment using phosphoric acid derivatives of electron transfer agents | |
| KR20110019571A (en) | Composition containing a class of hexamidine and a class of retinoid for improving skin condition | |
| USRE33107E (en) | Compositions containing 1α-hydroxycholecalciferol for topical treatment of skin disorders and methods employing same | |
| JP2000512996A (en) | Preventive and therapeutic measures for skin sensitization and irritation | |
| US7655255B2 (en) | Topical composition for transdermal administration | |
| CN112891242A (en) | Composition for removing freckles, whitening and resisting inflammation and application thereof | |
| JP2011088930A (en) | Carbon dioxide percutaneous and transmucosal absorption composition | |
| US20140302185A1 (en) | Composition for the treatment of skin lesions | |
| JP5643872B2 (en) | Carbon dioxide transdermal / mucosal absorption composition | |
| US9034845B2 (en) | Compositions for treating rosacea | |
| EP1752132A2 (en) | Skin cosmetic compositions | |
| JP5699184B2 (en) | Carbon dioxide transdermal / mucosal absorption composition | |
| JPH0429934A (en) | Externally applicable composition containing extracted essence of ginkgo leaf | |
| JPH08109128A (en) | Preparation for treating allergic dermatopathy for external use | |
| UA122755C2 (en) | Topical skin care compositions | |
| JP2017214343A (en) | Therapeutic agent for acne-vulgaris | |
| KR20070006626A (en) | Topical composition for transdermal administration | |
| JP2013177461A (en) | Composition for percutaneously and transmucosally absorbing carbon dioxide | |
| CN114177219A (en) | Skin medicine composition and preparation method thereof | |
| KR20190132197A (en) | Cosmetic composition for use in the treatment and prevention of acne-prone skin | |
| JPH07223949A (en) | Antiphlogistic analgetic for external use |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| CB02 | Change of applicant information | ||
| CB02 | Change of applicant information |
Address after: Room 801, 8 / F, building A-3, jinruilugu Science Park, 28 Lutian Road, Changsha hi tech Development Zone, Changsha City, Hunan Province, 410000 Applicant after: Changsha Jingyi Pharmaceutical Technology Co.,Ltd. Address before: Room 801, 8 / F, building A-3, jinruilugu Science Park, 28 Lutian Road, Changsha hi tech Development Zone, Changsha City, Hunan Province, 410000 Applicant before: CHANGSHA JINGYI MEDICAL TECHNOLOGY Co.,Ltd. |
|
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination |