CN116585207A - Transparent uniform salicylic acid preparation and preparation method and application thereof - Google Patents
Transparent uniform salicylic acid preparation and preparation method and application thereof Download PDFInfo
- Publication number
- CN116585207A CN116585207A CN202310451415.XA CN202310451415A CN116585207A CN 116585207 A CN116585207 A CN 116585207A CN 202310451415 A CN202310451415 A CN 202310451415A CN 116585207 A CN116585207 A CN 116585207A
- Authority
- CN
- China
- Prior art keywords
- sodium
- amphoacetate
- amphoteric surfactant
- salicylic acid
- betaine
- 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
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- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 title claims abstract description 310
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 title claims abstract description 154
- 229960004889 salicylic acid Drugs 0.000 title claims abstract description 154
- 238000002360 preparation method Methods 0.000 title claims abstract description 31
- 239000002280 amphoteric surfactant Substances 0.000 claims abstract description 120
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 18
- 239000004094 surface-active agent Substances 0.000 claims abstract description 14
- 239000000654 additive Substances 0.000 claims abstract description 7
- 239000011734 sodium Substances 0.000 claims description 122
- 229910052708 sodium Inorganic materials 0.000 claims description 122
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 81
- 239000000203 mixture Substances 0.000 claims description 43
- MRUAUOIMASANKQ-UHFFFAOYSA-N cocamidopropyl betaine Chemical compound CCCCCCCCCCCC(=O)NCCC[N+](C)(C)CC([O-])=O MRUAUOIMASANKQ-UHFFFAOYSA-N 0.000 claims description 41
- 229940073507 cocamidopropyl betaine Drugs 0.000 claims description 40
- 238000009472 formulation Methods 0.000 claims description 39
- 125000002252 acyl group Chemical group 0.000 claims description 32
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 claims description 31
- KWIUHFFTVRNATP-UHFFFAOYSA-N Betaine Natural products C[N+](C)(C)CC([O-])=O KWIUHFFTVRNATP-UHFFFAOYSA-N 0.000 claims description 22
- -1 alkyl betaine Chemical compound 0.000 claims description 20
- 229960003237 betaine Drugs 0.000 claims description 17
- 206010000496 acne Diseases 0.000 claims description 16
- ZKWJQNCOTNUNMF-QXMHVHEDSA-N 2-[dimethyl-[3-[[(z)-octadec-9-enoyl]amino]propyl]azaniumyl]acetate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)NCCC[N+](C)(C)CC([O-])=O ZKWJQNCOTNUNMF-QXMHVHEDSA-N 0.000 claims description 15
- 239000010480 babassu oil Substances 0.000 claims description 15
- MRUAUOIMASANKQ-UHFFFAOYSA-O carboxymethyl-[3-(dodecanoylamino)propyl]-dimethylazanium Chemical compound CCCCCCCCCCCC(=O)NCCC[N+](C)(C)CC(O)=O MRUAUOIMASANKQ-UHFFFAOYSA-O 0.000 claims description 14
- 229940110456 cocoa butter Drugs 0.000 claims description 14
- 235000019868 cocoa butter Nutrition 0.000 claims description 14
- 229940075468 lauramidopropyl betaine Drugs 0.000 claims description 14
- 239000003921 oil Substances 0.000 claims description 12
- 235000019198 oils Nutrition 0.000 claims description 12
- 239000000243 solution Substances 0.000 claims description 11
- 235000019486 Sunflower oil Nutrition 0.000 claims description 10
- 239000002600 sunflower oil Substances 0.000 claims description 10
- 235000020238 sunflower seed Nutrition 0.000 claims description 10
- 238000011282 treatment Methods 0.000 claims description 9
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 7
- 208000008742 seborrheic dermatitis Diseases 0.000 claims description 7
- 206010020649 Hyperkeratosis Diseases 0.000 claims description 6
- 206010039793 Seborrhoeic dermatitis Diseases 0.000 claims description 6
- 239000011148 porous material Substances 0.000 claims description 6
- PSBDWGZCVUAZQS-UHFFFAOYSA-N (dimethylsulfonio)acetate Chemical compound C[S+](C)CC([O-])=O PSBDWGZCVUAZQS-UHFFFAOYSA-N 0.000 claims description 5
- 229910019142 PO4 Inorganic materials 0.000 claims description 5
- 230000000996 additive effect Effects 0.000 claims description 5
- 239000008346 aqueous phase Substances 0.000 claims description 5
- 125000002091 cationic group Chemical group 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- MTNDZQHUAFNZQY-UHFFFAOYSA-N imidazoline Chemical compound C1CN=CN1 MTNDZQHUAFNZQY-UHFFFAOYSA-N 0.000 claims description 5
- 239000010452 phosphate Substances 0.000 claims description 5
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 5
- 229940117986 sulfobetaine Drugs 0.000 claims description 5
- 230000003110 anti-inflammatory effect Effects 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- GOJYXPWOUJYXJC-UHFFFAOYSA-M sodium;2-[1-(2-hydroxyethyl)-2-undecyl-4,5-dihydroimidazol-1-ium-1-yl]acetate;hydroxide Chemical compound [OH-].[Na+].CCCCCCCCCCCC1=NCC[N+]1(CCO)CC([O-])=O GOJYXPWOUJYXJC-UHFFFAOYSA-M 0.000 claims description 4
- 208000003643 Callosities Diseases 0.000 claims description 3
- 201000004624 Dermatitis Diseases 0.000 claims description 3
- 102000011782 Keratins Human genes 0.000 claims description 3
- 108010076876 Keratins Proteins 0.000 claims description 3
- 201000004681 Psoriasis Diseases 0.000 claims description 3
- 240000008042 Zea mays Species 0.000 claims description 3
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 claims description 3
- 235000002017 Zea mays subsp mays Nutrition 0.000 claims description 3
- 239000007864 aqueous solution Substances 0.000 claims description 3
- 208000010668 atopic eczema Diseases 0.000 claims description 3
- 230000003385 bacteriostatic effect Effects 0.000 claims description 3
- 229940096362 cocoamphoacetate Drugs 0.000 claims description 3
- 235000005822 corn Nutrition 0.000 claims description 3
- 229940047642 disodium cocoamphodiacetate Drugs 0.000 claims description 3
- GLSRFBDXBWZNLH-UHFFFAOYSA-L disodium;2-chloroacetate;2-(4,5-dihydroimidazol-1-yl)ethanol;hydroxide Chemical compound [OH-].[Na+].[Na+].[O-]C(=O)CCl.OCCN1CCN=C1 GLSRFBDXBWZNLH-UHFFFAOYSA-L 0.000 claims description 3
- 210000004907 gland Anatomy 0.000 claims description 3
- 239000012071 phase Substances 0.000 claims description 3
- 230000009467 reduction Effects 0.000 claims description 3
- 231100000241 scar Toxicity 0.000 claims description 3
- 230000028327 secretion Effects 0.000 claims description 3
- 201000010153 skin papilloma Diseases 0.000 claims description 3
- 229940096501 sodium cocoamphoacetate Drugs 0.000 claims description 3
- 238000003756 stirring Methods 0.000 claims description 3
- 208000032544 Cicatrix Diseases 0.000 claims description 2
- 230000006872 improvement Effects 0.000 claims description 2
- 238000011321 prophylaxis Methods 0.000 claims description 2
- 230000037387 scars Effects 0.000 claims description 2
- KWIUHFFTVRNATP-UHFFFAOYSA-O N,N,N-trimethylglycinium Chemical compound C[N+](C)(C)CC(O)=O KWIUHFFTVRNATP-UHFFFAOYSA-O 0.000 claims 3
- 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 125000002801 octanoyl group Chemical group C(CCCCCCC)(=O)* 0.000 claims 2
- 238000004140 cleaning Methods 0.000 claims 1
- 229940047648 cocoamphodiacetate Drugs 0.000 claims 1
- YASOXPMFSCKYDU-UHFFFAOYSA-M sodium;2-[2-hydroxyethyl-[2-(octanoylamino)ethyl]amino]acetate Chemical compound [Na+].CCCCCCCC(=O)NCCN(CCO)CC([O-])=O YASOXPMFSCKYDU-UHFFFAOYSA-M 0.000 claims 1
- 238000000034 method Methods 0.000 abstract description 9
- 239000002563 ionic surfactant Substances 0.000 abstract description 4
- 230000000052 comparative effect Effects 0.000 description 12
- 230000000694 effects Effects 0.000 description 11
- 210000003491 skin Anatomy 0.000 description 9
- 229910052739 hydrogen Inorganic materials 0.000 description 8
- 239000001257 hydrogen Substances 0.000 description 8
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 230000005496 eutectics Effects 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 4
- 238000006386 neutralization reaction Methods 0.000 description 4
- 208000001840 Dandruff Diseases 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 238000001816 cooling Methods 0.000 description 3
- 239000002537 cosmetic Substances 0.000 description 3
- 239000013078 crystal Substances 0.000 description 3
- 238000010494 dissociation reaction Methods 0.000 description 3
- 230000005593 dissociations Effects 0.000 description 3
- 238000004090 dissolution Methods 0.000 description 3
- 239000000499 gel Substances 0.000 description 3
- 238000010438 heat treatment Methods 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 239000000178 monomer Substances 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 150000003839 salts Chemical class 0.000 description 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000003750 conditioning effect Effects 0.000 description 2
- 238000005538 encapsulation Methods 0.000 description 2
- 230000007794 irritation Effects 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 239000003002 pH adjusting agent Substances 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 230000000717 retained effect Effects 0.000 description 2
- 229960001860 salicylate Drugs 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 2
- 239000001509 sodium citrate Substances 0.000 description 2
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical group O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- CFXSFDXXYYHZFU-UHFFFAOYSA-N 2-hydroxybenzoic acid;2-(trimethylazaniumyl)acetate Chemical compound C[N+](C)(C)CC(O)=O.OC(=O)C1=CC=CC=C1[O-] CFXSFDXXYYHZFU-UHFFFAOYSA-N 0.000 description 1
- JVKVEOKPRHZKNW-UHFFFAOYSA-N 2-hydroxybenzoic acid;hydrate Chemical compound O.OC(=O)C1=CC=CC=C1O JVKVEOKPRHZKNW-UHFFFAOYSA-N 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 244000021150 Orbignya martiana Species 0.000 description 1
- 235000014643 Orbignya martiana Nutrition 0.000 description 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- 241001303601 Rosacea Species 0.000 description 1
- 206010039792 Seborrhoea Diseases 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 125000005233 alkylalcohol group Chemical group 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 239000003945 anionic surfactant Substances 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 229940041488 betaine salicylate Drugs 0.000 description 1
- 230000002457 bidirectional effect Effects 0.000 description 1
- CDQSJQSWAWPGKG-UHFFFAOYSA-N butane-1,1-diol Chemical compound CCCC(O)O CDQSJQSWAWPGKG-UHFFFAOYSA-N 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- OPGYRRGJRBEUFK-UHFFFAOYSA-L disodium;diacetate Chemical compound [Na+].[Na+].CC([O-])=O.CC([O-])=O OPGYRRGJRBEUFK-UHFFFAOYSA-L 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 238000005265 energy consumption Methods 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 239000000017 hydrogel Substances 0.000 description 1
- 150000001261 hydroxy acids Chemical class 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- PYIDGJJWBIBVIA-UYTYNIKBSA-N lauryl glucoside Chemical compound CCCCCCCCCCCCO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O PYIDGJJWBIBVIA-UYTYNIKBSA-N 0.000 description 1
- 229940048848 lauryl glucoside Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- 229960000502 poloxamer Drugs 0.000 description 1
- 229920001983 poloxamer Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- CMDGQTVYVAKDNA-UHFFFAOYSA-N propane-1,2,3-triol;hydrate Chemical compound O.OCC(O)CO CMDGQTVYVAKDNA-UHFFFAOYSA-N 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 201000004700 rosacea Diseases 0.000 description 1
- 108700004121 sarkosyl Proteins 0.000 description 1
- 210000004761 scalp Anatomy 0.000 description 1
- 230000005808 skin problem Effects 0.000 description 1
- 229940045885 sodium lauroyl sarcosinate Drugs 0.000 description 1
- KSAVQLQVUXSOCR-UHFFFAOYSA-M sodium lauroyl sarcosinate Chemical compound [Na+].CCCCCCCCCCCC(=O)N(C)CC([O-])=O KSAVQLQVUXSOCR-UHFFFAOYSA-M 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/368—Carboxylic acids; Salts or anhydrides thereof with carboxyl groups directly bound to carbon atoms of aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/60—Salicylic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
-
- 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
- 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
- A61K8/442—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof substituted by amido group(s)
-
- 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
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/12—Keratolytics, e.g. wart or anti-corn preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/26—Optical properties
- A61K2800/262—Transparent; Translucent
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Abstract
The invention provides a salicylic acid preparation, which contains salicylic acid, a surfactant, water and optional additives, wherein the surfactant is an ampholytic surfactant; the content of the salicylic acid is 2% -8% and the content of the amphoteric surfactant is 9% -30% based on the total mass of the salicylic acid preparation. The invention also provides a method for preparing the salicylic acid preparation and application thereof.
Description
Technical Field
The invention relates to the field of skin care cosmetics, in particular to a transparent uniform salicylic acid preparation and a preparation method and application thereof.
Background
Salicylic acid has been studied by researchers in various fields for over a hundred years, and in the cosmetic field, salicylic acid has been used for treating rosacea, anti-inflammatory, broad-spectrum antibacterial, bidirectional conditioning of the stratum corneum, etc. The clinical curative effect research of salicylic acid anti-dandruff hair care dew for treating seborrheic dermatitis shows that the anti-dandruff hair care dew containing salicylic acid can effectively improve scalp itch, dandruff and seborrhea of seborrheic dermatitis without obvious irritation reaction.
From the above, it is inferred that if salicylic acid is applied to a transparent uniform salicylic acid formulation, various skin problems will be effectively alleviated. However, the traditional salicylic acid is limited by physical and chemical characteristics, the solubility of the salicylic acid in an aqueous product is low, the solubility in water is about 0.22g/100g at the temperature of between room temperature and 20 ℃, and when the salicylic acid preparation with high concentration is prepared conventionally, a large amount of auxiliary solvents such as ethanol, propylene glycol, butanediol and the like are required to be added for auxiliary dissolution, and the property of the product is unstable due to the material property of the auxiliary solvents, and crystallization is easy to form, so that the efficacy of the product is reduced; or in the process of dilution by water, salicylic acid crystals are precipitated due to the reduced dissolution assisting capability. To be able to dissolve more salicylic acid, more people have used a method of neutralisation to form salts, but this results in a reduced content of monomeric salicylic acid and hence reduced efficacy.
At present, most of the research on salicylic acid utilizes modes of neutralization, encapsulation, high-energy hydrogen bond eutectic salt formation and the like, and the salicylic acid is applied to an aqueous system. For example, CN110840834B discloses a preparation process of 30% concentration liquid slow release salicylic acid, which comprises the following steps: adding salicylic acid into glycerol water solution under the condition of a first set temperature, uniformly mixing, cooling to a second set temperature, homogenizing to be transparent, heating to a third set temperature, sequentially adding poloxamer and polyethylene glycol, uniformly mixing, cooling to a fourth set temperature, adding skin feel regulator, and uniformly mixing. CN106511259B discloses a reversible temperature-sensitive hydrogel composition applicable to various pharmaceutical and cosmetic products, which improves the gel rate in the desired physiologically suitable use temperature range under relatively low polymer concentration conditions, and which remains clear and transparent before and after triggering environmental changes. CN113018205a discloses a low-irritation salicylic acid gel for external use, which comprises salicylic acid as a main active ingredient, and water, a cosolvent, a coating agent, an emulsifier and a gel forming agent as other auxiliary ingredients. CN113620827a provides a betaine salicylic acid eutectic, a preparation method and application thereof, and the betaine salicylic acid eutectic is used for improving the problem of irritation of betaine salicylate.
In the above patents, the effect of the neutralized salicylate, which is a hydroxy acid, will be lost, whether or not the salicylic acid character is still retained or how much is still retained, and further investigation is needed; the generation of the eutectic can be realized under high energy and high pressure, and the requirements on equipment and energy consumption are large; most of the products prepared from the encapsulated salicylic acid have sticky attributes or are slowly released. If a water aqua product containing salicylic acid with quick release and obvious effect needs to be prepared, the salicylic acid effect is difficult to achieve in a short time due to the short contact time with skin and slow release of the product.
Disclosure of Invention
The salicylic acid is directly added into the salicylic acid water-based product without using modes such as neutralization, wrapping or high-energy hydrogen bond eutectic salt formation, and the transparent uniform and stable state can be maintained under a lower pH value, such as the pH value of 2.0-5.0 or 3.0-5.0.
The first aspect of the present invention provides a salicylic acid preparation comprising salicylic acid, a surfactant, water and optionally an additive, wherein the surfactant is an ampholytic surfactant; the content of the salicylic acid is 2% -8% and the content of the amphoteric surfactant is 9% -30% based on the total mass of the salicylic acid preparation.
In one or more embodiments, the amphoteric surfactant is selected from one or more of alkyl betaine type amphoteric surfactant, alkyl propyl betaine type amphoteric surfactant, sulfobetaine type amphoteric surfactant, hydroxysulfobetaine type amphoteric surfactant, phosphate betaine type amphoteric surfactant, imidazoline type amphoteric surfactant, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter acyl amphoacetate, sodium babassu oil acyl amphoacetate, sodium sunflower seed oil acyl amphoacetate, and sodium octanoyl amphoacetate.
In one or more embodiments, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, coco dimethyl betaine, coco amidopropyl hydroxysulfobetaine, lauramidopropyl hydroxysulfobetaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoyl amphoacetate, sodium babassu oil amphoacetate, sodium sunflower seed oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate, and disodium lauroyl amphodiacetate.
In one or more embodiments, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter amphoacetate, sodium babassu oil acyl amphoacetate, sodium sunflower oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate, and disodium lauroyl amphodiacetate.
In one or more embodiments, the amphoteric surfactant is cocamidopropyl betaine and optionally one or more selected from the group consisting of lauramidopropyl betaine, oleamidopropyl betaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter amphoacetate, sodium babassaioyl amphoacetate, sodium sunflower seed oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate, and disodium lauroyl amphodiacetate.
In one or more embodiments, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, sodium lauroyl amphoacetate, disodium cocoyl amphodiacetate, preferably, the amphoteric surfactant is cocamidopropyl betaine and disodium cocoyl amphodiacetate.
In one or more embodiments, the salicylic acid is present in an amount of 3.5% to 4.5% and the amphoteric surfactant is cocamidopropyl betaine, the amphoteric surfactant being present in an amount of 17.5% to 22.5% based on the total mass of the salicylic acid formulation.
In one or more embodiments, the salicylic acid is present in an amount of 3.5% to 4.5% and the amphoteric surfactant is sodium lauroyl amphoacetate and the amphoteric surfactant is present in an amount of 17.5% to 22.5% based on the total mass of the salicylic acid formulation.
In one or more embodiments, the salicylic acid is present in an amount of 4.5% to 5.5% and the amphoteric surfactant is disodium cocoyl amphodiacetate and the amphoteric surfactant is present in an amount of 17.5% to 22.5% based on the total mass of the salicylic acid formulation.
In one or more embodiments, the salicylic acid is present in an amount of 7.0% to 8.0% and the amphoteric surfactant is cocamidopropyl betaine, the amphoteric surfactant being present in an amount of 25.0% to 30.0% based on the total mass of the salicylic acid formulation.
In one or more embodiments, the salicylic acid is present in an amount of 2.0% to 3.0% and the amphoteric surfactant is cocamidopropyl betaine, the amphoteric surfactant being present in an amount of 9.0% to 12.0% based on the total mass of the salicylic acid formulation.
In one or more embodiments, the salicylic acid is present in an amount of 7.0% to 8.0% based on the total mass of the salicylic acid formulation, the amphoteric surfactant is cocamidopropyl betaine and disodium cocoyl amphodiacetate, and the amphoteric surfactant is present in an amount of 25.0% to 30.0%.
In one or more embodiments, the amphoteric surfactant is cationic in nature in the salicylic acid formulation.
In a second aspect the invention provides a process for the preparation of a salicylic acid formulation according to any one of the embodiments herein characterised in that the process comprises adjusting the pH of the ampholytic surfactant solution to 3-5 or 2-5 and then adding salicylic acid.
In one or more embodiments, the amphoteric surfactant solution is an aqueous solution of an amphoteric surfactant.
In one or more embodiments, the solution is heated to 75-85 ℃ after the salicylic acid is added.
In one or more embodiments, the salicylic acid is added with stirring.
In a third aspect the invention provides the use of a salicylic acid formulation according to any one of the embodiments herein in the pharmaceutical industry for the manufacture of a medicament for the treatment and/or prophylaxis of seborrheic dermatitis, acne, comedones, eczema, psoriasis, corns, calluses, viral warts and/or for the manufacture of a medicament for deep cleansing, for the treatment of clogged or enlarged pores, for shrinking pores, for controlling the secretion of fatty glands, for softening keratin, for anti-inflammatory, bacteriostatic, for the treatment of blackheads or comedones, for improving skin darkness, for reducing skin blemishes, for removing acne marks, for lightening scars.
In a fourth aspect, the invention provides the use of an amphoteric surfactant in increasing salicylic acid solubility in an aqueous phase, characterised in that the aqueous phase comprises salicylic acid, a surfactant, water and optionally an additive, wherein the surfactant is an amphoteric surfactant; the content of salicylic acid is 2% -8% and the content of the amphoteric surfactant is 9% -30% based on the total mass of the water phase.
In one or more embodiments, the amphoteric surfactant is selected from one or more of alkyl betaine type amphoteric surfactant, alkyl propyl betaine type amphoteric surfactant, sulfobetaine type amphoteric surfactant, hydroxysulfobetaine type amphoteric surfactant, phosphate betaine type amphoteric surfactant, imidazoline type amphoteric surfactant, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter acyl amphoacetate, sodium babassu oil acyl amphoacetate, sodium sunflower seed oil acyl amphoacetate, and sodium octanoyl amphoacetate.
In one or more embodiments, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, coco dimethyl betaine, coco amidopropyl hydroxysulfobetaine, lauramidopropyl hydroxysulfobetaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoyl amphoacetate, sodium babassu oil amphoacetate, sodium sunflower seed oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate, and disodium lauroyl amphodiacetate.
In one or more embodiments, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter amphoacetate, sodium babassu oil acyl amphoacetate, sodium sunflower oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate, and disodium lauroyl amphodiacetate.
In one or more embodiments, the amphoteric surfactant is cocamidopropyl betaine and optionally one or more selected from the group consisting of lauramidopropyl betaine, oleamidopropyl betaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter amphoacetate, sodium babassaioyl amphoacetate, sodium sunflower seed oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate, and disodium lauroyl amphodiacetate.
In one or more embodiments, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, sodium lauroyl amphoacetate, disodium cocoyl amphodiacetate, preferably, the amphoteric surfactant is cocamidopropyl betaine and disodium cocoyl amphodiacetate.
Drawings
Fig. 1 is a dissociation equation of salicylic acid.
FIG. 2 shows the stability results of example 1 when left for one month at 5 ℃, 25 ℃ and 45 ℃.
FIG. 3 shows the stability results of example 2 when left for one month at 5 ℃, 25 ℃ and 45 ℃.
FIG. 4 shows the stability results of example 3 when left for one month at 5 ℃, 25 ℃ and 45 ℃.
FIG. 5 shows the stability results after completion of the formulation of examples 4-6. From left to right, examples 4, 5 and 6 are respectively.
FIG. 6 shows the stability results after formulation of comparative examples 1-4. From left to right, comparative example 1, comparative example 2, comparative example 3 and comparative example 4, respectively.
FIG. 7 shows the stability results of example 1 when left for one month at 5 ℃.
FIG. 8 shows the stability results after formulation of comparative examples 5-8. Comparative example 5, comparative example 6, comparative example 7, comparative example 8, respectively, from left to right.
Detailed Description
So that those skilled in the art can appreciate the features and effects of the present invention, a general description and definition of the terms and expressions set forth in the specification and claims follows. Unless otherwise defined, 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, and in the event of a conflict, the present specification shall control.
The theory or mechanism described and disclosed herein, whether right or wrong, is not meant to limit the scope of the invention in any way, i.e., the present disclosure may be practiced without limitation to any particular theory or mechanism.
Herein, "comprising," "including," "containing," and similar terms are intended to cover the meaning of "consisting essentially of … …" and "consisting of … …," e.g., "a consisting essentially of B and C" and "a consisting of B and C" should be considered to have been disclosed herein when "a comprises B and C" is disclosed herein.
In this document, all features such as values, amounts, and concentrations that are defined as ranges of values or percentages are for brevity and convenience only. Accordingly, the description of a numerical range or percentage range should be considered to cover and specifically disclose all possible sub-ranges and individual values (including integers and fractions) within the range.
Herein, unless otherwise specified, percentages refer to mass percentages, proportions refer to mass ratios, and parts refer to parts by mass.
Herein, when embodiments or examples are described, it should be understood that they are not intended to limit the invention to these embodiments or examples. On the contrary, all alternatives, modifications, and equivalents of the methods and materials described herein are intended to be included within the scope of the invention as defined by the appended claims.
The sum of the percentages of the components of the composition is 100% herein.
Herein, salicylic acid refers to salicylic acid monomer molecules.
In this context, not all possible combinations of the individual technical features in the individual embodiments or examples are described in order to simplify the description. Accordingly, as long as there is no contradiction between the combinations of these technical features, any combination of the technical features in the respective embodiments or examples is possible, and all possible combinations should be considered as being within the scope of the present specification.
The inventor finds that salicylic acid and the amphoteric surfactant are compounded, so that the salicylic acid aqueous product is a uniform transparent system with good stability and good use feeling on the premise of ensuring the salicylic acid activity effect.
Salicylic acid is also called o-hydroxybenzoic acid, has effects of improving seborrheic dermatitis and treating acne, if salicylic acid is directly added into water formulation, H is dissociated when salicylic acid is dissociated + After that, hydrogen on phenolic hydroxyl forms an intramolecular hydrogen bond with carboxyl anions, and the phenolic hydroxyl does not formThe salicylic acid is favorable for forming hydrogen bonds with water, so that the solubility of the salicylic acid is greatly reduced, crystals are easy to separate out, and a dissociation equation is shown in figure 1. In the prior art, salicylic acid is added into an aqueous preparation system in a mode of neutralization, encapsulation or high-energy hydrogen bond eutectic crystal and the like, but the salicylic acid product treated by the method cannot effectively exert the effect of the salicylic acid product in a short-time contact skin product, so that the salicylic acid is necessary to be directly applied to the aqueous preparation.
Amphoteric surfactants contain both inseparable positive and negative charge centers in the molecule, and this structure determines that they can release a proton and absorb a proton in solution, and change with pH. Thus, amphoteric surfactants have unique isoelectric point properties in solution, which exhibit cationic character when the pH is below the isoelectric point. The inventor inhibits salicylic acid dissociation through the positive characteristic of the amphoteric surfactant at low pH, so that the intramolecular hydrogen bond of salicylic acid is reduced, and the salicylic acid exists in a monomer form, thereby increasing the possibility of forming hydrogen bond between the salicylic acid and water and increasing the dissolving capacity of the salicylic acid. Further, since the amphoteric surfactant itself has the characteristics of a surfactant, the solubility of salicylic acid in water can be increased. It is well known to those skilled in the art that at lower pH values (e.g., pH values of 2-5 or 3-5), the amphoteric surfactant is cationic in character, and that salicylic acid exists as a monomer, and at pH values greater than 5, salicylic acid exists as a salicylate in an aqueous system, although its solubility increases, but not as salicylic acid.
Accordingly, the present invention provides a salicylic acid formulation comprising salicylic acid, a surfactant, water and optionally an additive, wherein the surfactant is an ampholytic surfactant; the content of salicylic acid is 2% -8% and the content of the amphoteric surfactant is 9% -30% based on the total mass of the salicylic acid preparation.
In the salicylic acid preparation of the invention, the amphoteric surfactant has cationic property. Amphoteric surfactants suitable for use in the present invention include, but are not limited to, one or more of alkyl betaine type amphoteric surfactants, alkyl propyl betaine type amphoteric surfactants, sulfobetaine type amphoteric surfactants, hydroxysulfobetaine type amphoteric surfactants, phosphate betaine type amphoteric surfactants, imidazoline type amphoteric surfactants, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter amphoacetate, sodium babassu oil acyl amphoacetate, sodium sunflower oil acyl amphoacetate and sodium capryloyl amphoacetate, such as one or more of cocamidopropylbetaine, lauramidopropyl betaine, oleamidopropylbetaine, coco dimethyl betaine, cocoamidopropyl hydroxysulfobetaine, lauramidopropyl hydroxysulfobetaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter amphoacetate, sodium babassu oil acyl amphoacetate, sodium sunflower oil acyl amphoacetate, sodium capryloyl amphoacetate and sodium di-or di-sodium capryloyl amphoacetate. More preferably, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, cocoamidopropyl betaine, sodium lauroamphoacetate, sodium cocoa butter amphoacetate, sodium babassu oil amphoacetate, sodium sunflower oil amphoacetate, sodium octanoyl amphoacetate, disodium cocoamphodiacetate and disodium lauroamphoacetate, or the amphoteric surfactant may be cocamidopropyl betaine and optionally one or more selected from lauroamphoacetate, oleamidopropyl betaine, sodium cocoamphoacetate, sodium lauroamphoacetate, sodium cocoa butter amphoacetate, sodium babassu amphoacetate, sodium sunflower oil amphoacetate, sodium octanoyl amphoacetate, disodium cocoamphoacetate and disodium lauroamphoacetate. More preferably, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, sodium lauroyl amphoacetate, disodium cocooyl amphodiacetate. In some embodiments, the amphoteric surfactant is cocamidopropyl betaine and disodium cocoyl amphodiacetate.
In the salicylic acid preparation, the content of the amphoteric surfactant is 9-30%. The content of the amphoteric surfactant may be adjusted according to the content of salicylic acid, for example, the content of salicylic acid is 2% based on the total mass of the salicylic acid preparation, and when the amphoteric surfactant is cocamidopropyl betaine, the content is at least 9%; salicylic acid is present in an amount of 8% and, when the amphoteric surfactant is cocamidopropyl betaine, it is present in an amount of up to 30%.
In some embodiments, the salicylic acid formulations described herein have a pH of 2 to 5, such as 3 to 5.
In some embodiments, the salicylic acid formulation has a pH of 3 to 5, a salicylic acid content of 3.5% to 4.5%, and a cocamidopropyl betaine content of 17.5% to 22.5% based on the total mass of the salicylic acid formulation.
In some embodiments, the salicylic acid formulation has a pH of 3 to 5, a salicylic acid content of 3.5% to 4.5%, and a sodium lauroyl amphoacetate content of 17.5% to 22.5% based on the total mass of the salicylic acid formulation.
In some embodiments, the salicylic acid formulation has a pH of 3 to 5, a salicylic acid content of 4.5% to 5.5%, and a cocoyl disodium diacetate content of 18.0% to 22.0% based on the total mass of the salicylic acid formulation.
In some embodiments, the salicylic acid formulation has a pH of 3 to 5, a salicylic acid content of 7.0% to 8.0%, and a cocamidopropyl betaine content of 25.0% to 30.0% based on the total mass of the salicylic acid formulation.
In some embodiments, the salicylic acid formulation has a pH of 3 to 5, the salicylic acid content is 7.0% to 8.0% based on the total mass of the salicylic acid formulation, and the sum of the cocamidopropyl betaine and disodium cocoyl amphodiacetate content is 25.0% to 30.0%.
In some embodiments, the salicylic acid formulation has a pH of 3 to 5, a salicylic acid content of 2.0% to 3.0%, and a cocamidopropyl betaine content of 9.0% to 12.0% based on the total mass of the salicylic acid formulation.
Additives may be conventional in the art, such as pH adjusters, preservatives, skin conditioning agents, thickeners, and the like. In some embodiments, the pH adjuster is sodium citrate or citric acid.
The present invention also provides a method of preparing a salicylic acid formulation according to any one of the embodiments herein comprising adjusting the pH of the amphoteric surfactant solution to 3-5 or 2-5 and then adding salicylic acid. In some embodiments, salicylic acid is added followed by heating to 75-85 ℃ to accelerate dissolution. And can be stirred to dissolve uniformly. Preferably, the amphoteric surfactant solution refers to an aqueous solution of an amphoteric surfactant.
The present invention also provides the use of a salicylic acid formulation according to any one of the embodiments herein in the pharmaceutical industry, including but not limited to the use in the manufacture of a medicament for the treatment and/or prevention of seborrheic dermatitis, acne, comedones, eczema, psoriasis, corns, calluses, viral warts and/or for deep cleansing, treatment of clogged or enlarged pores, shrinking pores, controlling oil and fat gland secretion, softening keratin, anti-inflammatory, bacteriostatic, treatment of blackheads or comedones, improvement of skin darkness, reduction of skin blemishes, removal of acne marks, and scar lightening.
The invention also provides application of the amphoteric surfactant in improving salicylic acid solubility in an aqueous phase. The amphoteric surfactant is as described in any of the embodiments herein.
The invention has the following beneficial effects:
according to the invention, salicylic acid and the amphoteric surfactant are compounded, so that the salicylic acid aqueous agent product is a uniform transparent system under the premise of ensuring the salicylic acid activity effect, and the salicylic acid aqueous agent product has good stability and good use feel.
The invention will be further illustrated by means of specific examples. It should be understood that these examples are illustrative only and are not intended to limit the scope of the invention. The method and reagents used in the examples, the pH adjuster is sodium citrate or citric acid, unless otherwise indicated, are conventional in the art.
The raw material compositions, states and stability results of examples 1 to 3 and comparative examples 1 to 4 are shown in Table 1 below. Adding water and amphoteric surfactant into beaker, adjusting pH of the system to about 5.0 with pH regulator, adding salicylic acid into the system, heating to 80deg.C, stirring to dissolve uniformly, cooling, and testing. Wherein, stability test conditions are: the sample is placed for one month at 5 ℃, 25 ℃ and 45 ℃, the sample is not layered, and the properties are not obviously changed compared with those before the test. The transparency criterion is: placing paper with characters or lines behind a transparent cylindrical glass container filled with a sample, wherein the characters or lines are clearly visible and transparent; the characters or lines are blurred, and the characters or lines are turbid.
Table 1: raw material composition, state and stability of examples and comparative examples
The results are shown in FIGS. 2-8. Wherein, the amphoteric surfactant represented by cocamidopropyl betaine, sodium lauroyl amphoacetate and disodium cocoyl amphoacetate can be compounded with salicylic acid under low pH condition to form a uniform and transparent water phase system with good stability and good use feeling (figures 2-5). And the anionic surfactants such as alkyl alcohol ether sulfate, the nonionic surfactants such as lauryl glucoside and the amino acid surfactants such as sodium lauroyl sarcosinate are compounded with salicylic acid under the low pH condition, so that the conditions such as precipitation, system viscosity and the like can occur (figures 6-8), and a system which is uniform, transparent, good in stability and good in use feel is difficult to obtain.
Claims (10)
1. A salicylic acid formulation comprising salicylic acid, a surfactant, water, and optionally an additive, wherein the surfactant is an amphoteric surfactant; the content of the salicylic acid is 2% -8% and the content of the amphoteric surfactant is 9% -30% based on the total mass of the salicylic acid preparation.
2. The salicylic acid formulation of claim 1, wherein the amphoteric surfactant is selected from one or more of alkyl betaine type amphoteric surfactant, alkyl propyl betaine type amphoteric surfactant, sulfobetaine type amphoteric surfactant, hydroxysulfobetaine type amphoteric surfactant, phosphate betaine type amphoteric surfactant, imidazoline type amphoteric surfactant, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter acyl amphoacetate, sodium babassu oil acyl amphoacetate, sodium sunflower seed oil acyl amphoacetate, and sodium octanoyl amphoacetate.
3. The salicylic acid formulation of claim 2, wherein the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, coco dimethyl betaine, coco amidopropyl hydroxysulfobetaine, lauramidopropyl hydroxysulfobetaine, coco amphoacetate sodium, lauroyl amphoacetate sodium, coco amphoacetate sodium, babassu oil acyl amphoacetate sodium, sunflower seed oil acyl amphoacetate sodium, capryloyl amphoacetate sodium, coco amphodiacetate disodium, and lauroyl amphodiacetate disodium,
preferably, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter amphoacetate, sodium babassu oil amphoacetate, sodium sunflower oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate and disodium lauroyl amphodiacetate.
4. A salicylic acid formulation according to claim 2 or 3, wherein the amphoteric surfactant is cocamidopropyl betaine and optionally one or more selected from lauramidopropyl betaine, oleamidopropyl betaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoa butter amphoacetate, sodium babassaioyl amphoacetate, sodium sunflower oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate and disodium lauroyl amphodiacetate.
5. The salicylic acid formulation according to claim 4, wherein the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, sodium lauroamphoacetate, disodium cocoamphodiacetate,
preferably, the amphoteric surfactant is cocamidopropyl betaine and disodium cocoyl amphodiacetate.
6. The salicylic acid preparation according to claim 1, wherein the salicylic acid is contained in an amount of 3.5-4.5% by weight of the total mass of the salicylic acid preparation, the amphoteric surfactant is cocamidopropyl betaine, and the amphoteric surfactant is contained in an amount of 17.5-22.5%; and/or
The content of the salicylic acid is 3.5-4.5% based on the total mass of the salicylic acid preparation, the amphoteric surfactant is sodium lauroyl amphoacetate, and the content of the amphoteric surfactant is 17.5-22.5%; and/or
The content of the salicylic acid is 4.5-5.5% based on the total mass of the salicylic acid preparation, the amphoteric surfactant is disodium cocoyl amphodiacetate, and the content of the amphoteric surfactant is 17.5-22.5%; and/or
The content of the salicylic acid is 7.0-8.0% based on the total mass of the salicylic acid preparation, the amphoteric surfactant is cocamidopropyl betaine, and the content of the amphoteric surfactant is 25.0-30.0%; and/or
The content of the salicylic acid is 2.0-3.0% based on the total mass of the salicylic acid preparation, the amphoteric surfactant is cocamidopropyl betaine, and the content of the amphoteric surfactant is 9.0-12.0%; and/or
The content of the salicylic acid is 7.0% -8.0% based on the total mass of the salicylic acid preparation, the amphoteric surfactant is cocamidopropyl betaine and disodium cocoyl amphodiacetate, and the content of the amphoteric surfactant is 25.0% -30.0%.
7. The salicylic acid formulation of claim 1, wherein the amphoteric surfactant is cationic in character in the salicylic acid formulation.
8. A process for preparing a salicylic acid formulation according to any one of claims 1-7 comprising adjusting the pH of the amphoteric surfactant solution to 3-5 or 2-5 and then adding salicylic acid,
preferably, the amphoteric surfactant solution is an aqueous solution of an amphoteric surfactant,
preferably, the solution is heated to 75-85 c after the salicylic acid is added,
preferably, the salicylic acid is added with stirring.
9. Use of a salicylic acid formulation according to any one of claims 1-7 in the pharmaceutical industry for the preparation of a medicament for the treatment and/or prophylaxis of seborrheic dermatitis, acne, comedones, eczema, psoriasis, corns, calluses, viral warts and/or for the preparation of a medicament for deep cleaning, for the treatment of clogged or enlarged pores, for the shrinkage of pores, for the control of oil gland secretion, for the softening of keratin, for anti-inflammatory, bacteriostatic, for the treatment of blackheads or comedones, for the improvement of skin darkness, for the reduction of skin blemishes, for the removal of acne marks, for the reduction of scars.
10. Use of an amphoteric surfactant to increase salicylic acid solubility in an aqueous phase, wherein the aqueous phase comprises salicylic acid, a surfactant, water, and optionally an additive, wherein the surfactant is an amphoteric surfactant; the content of salicylic acid is 2-8% based on the total mass of the water phase, the content of the amphoteric surfactant is 9-30%,
preferably, the amphoteric surfactant is selected from one or more of alkyl betaine type amphoteric surfactant, alkyl propyl betaine type amphoteric surfactant, sulfobetaine type amphoteric surfactant, hydroxysulfobetaine type amphoteric surfactant, phosphate betaine type amphoteric surfactant, imidazoline type amphoteric surfactant, cocoyl amphoacetate sodium, lauroyl amphoacetate sodium, cocoa butter acyl amphoacetate sodium, babassu oil acyl amphoacetate sodium, sunflower seed oil acyl amphoacetate sodium and octanoyl amphoacetate sodium,
preferably, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, cocodimethyl betaine, cocoamidopropyl hydroxysulfobetaine, lauramidopropyl hydroxysulfobetaine, sodium cocoamphoacetate, sodium lauroamphoacetate, sodium cocoamphoacetate, sodium babassaioyl amphoacetate, sodium sunflower seed oil acyl amphoacetate, sodium capryloamphoacetate, disodium cocoamphodiacetate and disodium lauroamphoacetate,
preferably, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoyl amphoacetate, sodium babassu oil acyl amphoacetate, sodium sunflower oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate and disodium lauroyl amphodiacetate,
preferably, the amphoteric surfactant is cocamidopropyl betaine and optionally one or more selected from lauramidopropyl betaine, oleamidopropyl betaine, sodium cocoyl amphoacetate, sodium lauroyl amphoacetate, sodium cocoyl amphoacetate, sodium babassu oil amphoacetate, sodium sunflower oil acyl amphoacetate, sodium octanoyl amphoacetate, disodium cocoyl amphodiacetate and disodium lauroyl amphodiacetate,
preferably, the amphoteric surfactant is selected from one or more of cocamidopropyl betaine, sodium lauroyl amphoacetate, disodium cocooyl amphodiacetate,
preferably, the amphoteric surfactant is cocamidopropyl betaine and disodium cocoyl amphodiacetate.
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