CN107233303A - A kind of aminolevulinic acid cold cream and its preparation method and application - Google Patents
A kind of aminolevulinic acid cold cream and its preparation method and application Download PDFInfo
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- CN107233303A CN107233303A CN201710666915.XA CN201710666915A CN107233303A CN 107233303 A CN107233303 A CN 107233303A CN 201710666915 A CN201710666915 A CN 201710666915A CN 107233303 A CN107233303 A CN 107233303A
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- Prior art keywords
- aminolevulinic acid
- cold cream
- acid cold
- emulsion
- skin
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- ZGXJTSGNIOSYLO-UHFFFAOYSA-N 88755TAZ87 Chemical compound NCC(=O)CCC(O)=O ZGXJTSGNIOSYLO-UHFFFAOYSA-N 0.000 title claims abstract description 95
- 239000008294 cold cream Substances 0.000 title claims abstract description 86
- 229960002749 aminolevulinic acid Drugs 0.000 title claims abstract description 71
- 238000002360 preparation method Methods 0.000 title claims abstract description 17
- 239000000839 emulsion Substances 0.000 claims abstract description 25
- 239000003814 drug Substances 0.000 claims abstract description 19
- 239000000203 mixture Substances 0.000 claims abstract description 15
- 238000011282 treatment Methods 0.000 claims abstract description 15
- 239000002537 cosmetic Substances 0.000 claims abstract description 11
- 239000004094 surface-active agent Substances 0.000 claims abstract description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 9
- 239000000463 material Substances 0.000 claims abstract description 5
- QUCHWTCTBHQQDU-UHFFFAOYSA-N 2-amino-4-oxopentanoic acid Chemical class CC(=O)CC([NH3+])C([O-])=O QUCHWTCTBHQQDU-UHFFFAOYSA-N 0.000 claims abstract 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 26
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 25
- 239000003921 oil Substances 0.000 claims description 21
- 239000012071 phase Substances 0.000 claims description 21
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 18
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 14
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 13
- 229920000053 polysorbate 80 Polymers 0.000 claims description 13
- 239000003995 emulsifying agent Substances 0.000 claims description 12
- 235000011187 glycerol Nutrition 0.000 claims description 12
- 239000004166 Lanolin Substances 0.000 claims description 11
- 235000013871 bee wax Nutrition 0.000 claims description 11
- 239000012166 beeswax Substances 0.000 claims description 11
- 235000019388 lanolin Nutrition 0.000 claims description 11
- 229940039717 lanolin Drugs 0.000 claims description 11
- 239000002994 raw material Substances 0.000 claims description 11
- 238000002156 mixing Methods 0.000 claims description 9
- 239000008363 phosphate buffer Substances 0.000 claims description 9
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 claims description 8
- 239000008346 aqueous phase Substances 0.000 claims description 8
- 230000008569 process Effects 0.000 claims description 8
- 229940083466 soybean lecithin Drugs 0.000 claims description 8
- 238000009413 insulation Methods 0.000 claims description 6
- 239000002253 acid Substances 0.000 claims description 5
- 235000019198 oils Nutrition 0.000 claims description 5
- 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 claims description 4
- IXXIIAPIURLROR-UHFFFAOYSA-N 2-aminopentanoic acid;hydrochloride Chemical compound Cl.CCCC(N)C(O)=O IXXIIAPIURLROR-UHFFFAOYSA-N 0.000 claims description 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical class NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 4
- 239000000787 lecithin Substances 0.000 claims description 4
- 235000010445 lecithin Nutrition 0.000 claims description 4
- 229940067606 lecithin Drugs 0.000 claims description 4
- XWNWBYZHOAIHTK-UHFFFAOYSA-N 5-amino-4-oxopentanoic acid;phosphoric acid Chemical compound OP(O)(O)=O.NCC(=O)CCC(O)=O XWNWBYZHOAIHTK-UHFFFAOYSA-N 0.000 claims description 3
- 206010059313 Anogenital warts Diseases 0.000 claims description 3
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 3
- 238000003756 stirring Methods 0.000 claims description 3
- 240000000203 Salix gracilistyla Species 0.000 claims description 2
- 238000001816 cooling Methods 0.000 claims description 2
- 206010024217 lentigo Diseases 0.000 claims description 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- SECOZAIJMYAARA-UHFFFAOYSA-N C(CCCC)(=O)O.NC(=O)N Chemical compound C(CCCC)(=O)O.NC(=O)N SECOZAIJMYAARA-UHFFFAOYSA-N 0.000 claims 1
- 206010020649 Hyperkeratosis Diseases 0.000 claims 1
- 208000001126 Keratosis Diseases 0.000 claims 1
- 244000046052 Phaseolus vulgaris Species 0.000 claims 1
- 235000010627 Phaseolus vulgaris Nutrition 0.000 claims 1
- 150000004702 methyl esters Chemical class 0.000 claims 1
- 230000035699 permeability Effects 0.000 abstract description 11
- 239000000126 substance Substances 0.000 abstract description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 16
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 14
- 230000000694 effects Effects 0.000 description 14
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 9
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 8
- 238000002428 photodynamic therapy Methods 0.000 description 8
- 229960004889 salicylic acid Drugs 0.000 description 8
- 229910000403 monosodium phosphate Inorganic materials 0.000 description 7
- 235000019799 monosodium phosphate Nutrition 0.000 description 7
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 7
- 230000001225 therapeutic effect Effects 0.000 description 7
- 239000003795 chemical substances by application Substances 0.000 description 6
- 229910000397 disodium phosphate Inorganic materials 0.000 description 6
- 235000019800 disodium phosphate Nutrition 0.000 description 6
- 239000001488 sodium phosphate Substances 0.000 description 6
- 210000001519 tissue Anatomy 0.000 description 6
- 206010015150 Erythema Diseases 0.000 description 5
- 206010028980 Neoplasm Diseases 0.000 description 5
- 206010000496 acne Diseases 0.000 description 5
- 231100000321 erythema Toxicity 0.000 description 5
- 239000008055 phosphate buffer solution Substances 0.000 description 5
- 230000005808 skin problem Effects 0.000 description 5
- 230000002087 whitening effect Effects 0.000 description 5
- 201000010099 disease Diseases 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 230000003020 moisturizing effect Effects 0.000 description 4
- 230000037311 normal skin Effects 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 4
- 206010067484 Adverse reaction Diseases 0.000 description 3
- 230000006838 adverse reaction Effects 0.000 description 3
- 230000006378 damage Effects 0.000 description 3
- 238000011084 recovery Methods 0.000 description 3
- 230000001235 sensitizing effect Effects 0.000 description 3
- ZLHFONARZHCSET-UHFFFAOYSA-N 5-aminolevulinic acid hydrochloride Chemical compound Cl.NCC(=O)CCC(O)=O ZLHFONARZHCSET-UHFFFAOYSA-N 0.000 description 2
- 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 description 2
- 208000003351 Melanosis Diseases 0.000 description 2
- 230000032683 aging Effects 0.000 description 2
- 230000003796 beauty Effects 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 230000033228 biological regulation Effects 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 239000006071 cream Substances 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 description 2
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 229940005605 valeric acid Drugs 0.000 description 2
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- 206010004146 Basal cell carcinoma Diseases 0.000 description 1
- 208000013165 Bowen disease Diseases 0.000 description 1
- 208000019337 Bowen disease of the skin Diseases 0.000 description 1
- YDNKGFDKKRUKPY-JHOUSYSJSA-N C16 ceramide Natural products CCCCCCCCCCCCCCCC(=O)N[C@@H](CO)[C@H](O)C=CCCCCCCCCCCCCC YDNKGFDKKRUKPY-JHOUSYSJSA-N 0.000 description 1
- 206010008570 Chloasma Diseases 0.000 description 1
- 208000034657 Convalescence Diseases 0.000 description 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- CRJGESKKUOMBCT-VQTJNVASSA-N N-acetylsphinganine Chemical compound CCCCCCCCCCCCCCC[C@@H](O)[C@H](CO)NC(C)=O CRJGESKKUOMBCT-VQTJNVASSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 description 1
- 208000012641 Pigmentation disease Diseases 0.000 description 1
- 241000219000 Populus Species 0.000 description 1
- 229920000297 Rayon Polymers 0.000 description 1
- 206010040954 Skin wrinkling Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 206010043189 Telangiectasia Diseases 0.000 description 1
- 208000009621 actinic keratosis Diseases 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000000337 buffer salt Substances 0.000 description 1
- 208000035269 cancer or benign tumor Diseases 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 229940106189 ceramide Drugs 0.000 description 1
- ZVEQCJWYRWKARO-UHFFFAOYSA-N ceramide Natural products CCCCCCCCCCCCCCC(O)C(=O)NC(CO)C(O)C=CCCC=C(C)CCCCCCCCC ZVEQCJWYRWKARO-UHFFFAOYSA-N 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- SEGLCEQVOFDUPX-UHFFFAOYSA-N di-(2-ethylhexyl)phosphoric acid Chemical compound CCCCC(CC)COP(O)(=O)OCC(CC)CCCC SEGLCEQVOFDUPX-UHFFFAOYSA-N 0.000 description 1
- QDOXWKRWXJOMAK-UHFFFAOYSA-N dichromium trioxide Chemical compound O=[Cr]O[Cr]=O QDOXWKRWXJOMAK-UHFFFAOYSA-N 0.000 description 1
- 238000009513 drug distribution Methods 0.000 description 1
- 239000008344 egg yolk phospholipid Substances 0.000 description 1
- 239000003974 emollient agent Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 230000008020 evaporation Effects 0.000 description 1
- 239000004519 grease Substances 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
- 239000008309 hydrophilic cream Substances 0.000 description 1
- 206010020718 hyperplasia Diseases 0.000 description 1
- 238000005286 illumination Methods 0.000 description 1
- 238000002649 immunization Methods 0.000 description 1
- 230000003053 immunization Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000007154 intracellular accumulation Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 210000003470 mitochondria Anatomy 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- VVGIYYKRAMHVLU-UHFFFAOYSA-N newbouldiamide Natural products CCCCCCCCCCCCCCCCCCCC(O)C(O)C(O)C(CO)NC(=O)CCCCCCCCCCCCCCCCC VVGIYYKRAMHVLU-UHFFFAOYSA-N 0.000 description 1
- 150000007523 nucleic acids Chemical class 0.000 description 1
- 102000039446 nucleic acids Human genes 0.000 description 1
- 108020004707 nucleic acids Proteins 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 230000003287 optical effect Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 231100000760 phototoxic Toxicity 0.000 description 1
- 230000019612 pigmentation Effects 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 239000002964 rayon Substances 0.000 description 1
- 239000003507 refrigerant Substances 0.000 description 1
- 230000008439 repair process Effects 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 239000002884 skin cream Substances 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 235000013599 spices Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 208000009056 telangiectasis Diseases 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 230000037303 wrinkles Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K41/00—Medicinal preparations obtained by treating materials with wave energy or particle radiation ; Therapies using these preparations
- A61K41/0057—Photodynamic therapy with a photosensitizer, i.e. agent able to produce reactive oxygen species upon exposure to light or radiation, e.g. UV or visible light; photocleavage of nucleic acids with an agent
- A61K41/0061—5-aminolevulinic acid-based PDT: 5-ALA-PDT involving porphyrins or precursors of protoporphyrins generated in vivo from 5-ALA
-
- 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
-
- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/06—Emulsions
- A61K8/064—Water-in-oil emulsions, e.g. Water-in-silicone emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
- 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
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
- A61K2800/81—Preparation or application process involves irradiation
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Dermatology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Birds (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Dispersion Chemistry (AREA)
- Biochemistry (AREA)
- Cosmetics (AREA)
Abstract
The invention discloses a kind of aminolevulinic acid cold cream, it includes acceptable auxiliary material in aminolevulinic acid derivative, emulsion and other pharmacies or cosmetics；Wherein, the emulsion includes at least one aqueous components, at least one alcohol and at least one surfactant.Present invention also offers the preparation method of above-mentioned aminolevulinic acid cold cream and its application in medicine and cosmetics.The aminolevulinic acid cold cream of the present invention; in dept. of dermatology field; main function is the local treatment to skin, protects damaged part not contacted with the external world, it is possible to increase drugloading rate and bioavilability; it is easy to use; skin sense is comfortable, and composition is uniform, and chemical property is stable; ALA permeability can be improved, and then strengthens the permeability of skin and tissue；Technically it is easier to promote.
Description
Technical field
The present invention relates to a kind of aminolevulinic acid cold cream and its preparation method and application, belong to technical field of pharmaceuticals.
Background technology
5-ALA (ALA) is a kind of photosensitive drug, and treatment can be played with reference to the illumination of appropriate energy and wavelength
Effect, ALA photodynamic therapies have been widely used in dermatological field at present, and its technical merit is also constantly being opened up.
The treatment basis of photodynamic therapy (Photodynamic therapy, PDT) is：Body is first given to tumor tissues
The sensitising agent of selective intake effect, then with specific wavelength laser irradiation tumor tissues, the photochemistry for inducing sensitising agent is anti-
Activity very strong singlet oxygen should be generated, and then occurs oxidation reaction with large biological molecule, CDCC is produced swollen to kill
Oncocyte and show therapeutic action.Compared with the tumour traditional remedies such as operation, radiotherapy, chemotherapy and immunization therapy, photodynamics is controlled
It is that can carry out selective destruction to cancerous tissue to treat biggest advantage, and side effect is smaller.
5-ALA (5-aminolevulinic acid, ALA) is as second generation Porphyrin-Based Sensitizer, gradually
As clinical the most frequently used sensitising agent.ALA is a kind of endogenic optical dynamic therapy medicine, is animal ferroheme and plant leaf green
The precursor substance of plain biosynthesis, itself and unglazed toxic action.Under normal circumstances, the content that body passes through intracellular ferroheme
Negative feedback inhibition ALA synzyme, controls ALA growing amount, so being accumulated in vivo without excessive ALA.But a large amount of exogenous ALA
Into after in vivo, it can be absorbed by tumour cell and the vigorous cell selective of other hyperplasia, the tool for making intracellular accumulation excessive
There is strong photosensitive material protoporphysin Ⅸ (Pp Ⅸ), Pp Ⅸ can chemically react under the irradiation of certain wavelength, produce a large amount of
Active oxygen (ROS) and free radical, cause the damage of cell membrane, mitochondria and nucleic acid, make meronecrosis or apoptosis, are controlled so as to reach
Treat the effect of disease.ALA is small-molecule substance, can local application, without special after no obvious adverse reaction, and topical application ALA
Different lucifuge, because protoporphysin Ⅸ has been degraded or has been quenched after red light irradiation.Because ALA-PDT has, adverse reaction is small, curative effect
Definite the advantages of, the treatment of tumour, precancerous lesion and some Non-cancerous disease of skin is widely used to, its therapeutic domain is
Expand to that the skins such as basal-cell carcinoma, squamous cell carcinoma, bowen's disease, solar keratosis, condyloma acuminatum are benign and neoplasm
Property disease.Meanwhile, ALA-PDT also has more application in terms of beauty, the tender skin of light, cosmetics.Multinomial research has shown that PDT is treated
Method can repair the damaged skin of light aging, wherein, the photodynamic therapy effect with reference to ALA is more notable, can effectively improve skin
The skin problems such as skin relaxation, wrinkle, pigmentation, chloasma, pachylosis, telangiectasis.
However, ALA photodynamic therapies also have certain limitation.Because ALA is polar compound, percutaneous permeability compared with
It is low, it is difficult to reach the damaged part of skin histology.Current China is generally adopted by higher concentration 20% on clinical treatment
ALA solution, needs the aminolevulinic acid normal saline solution of Fresh when using, dropped in rayon balls and then be covered in
Need the region for the treatment of.This method is inconvenient for use, and drug distribution is uneven, and bioavilability is low.Also, due to drug concentration
Too high, the patient more than half can produce phototoxic side effect.In order to improve ALA clinical effectiveness, it would be highly desirable to the problem of solving
Raising ALA permeability is how, the permeability of its consumption, enhancing skin and tissue is reduced.
Cold cream, also referred to as face cream or face cream, are a kind of oil-in-water creams, are applied on skin and have moisture separation
Out, moisture evaporation takes away the heat of skin, skin is had refrigerant sensation, so referred to as cold cream.In cold cream oil phase into
Divide content higher, it is in solid that not only can effectively pin under moisture of skin, and cold cream normal temperature, be also beneficial to improve amino ketones
The storage stability of valeric acid.
The content of the invention
In view of the defect that above-mentioned prior art is present, can the purpose of the present invention is to propose to a kind of aminolevulinic acid cold cream
Drugloading rate and bioavilability are improved, convenient use improves ALA permeability, and then strengthen the permeability of skin and tissue.
The purpose of the present invention is achieved by the following technical programs：
A kind of aminolevulinic acid cold cream, it includes aminolevulinic acid derivative, emulsion and other pharmacies or cosmetics
In acceptable auxiliary material；
Counted using the gross weight of emulsion as 100%, the content of the aqueous components is 50%-98%, the content of the alcohol
For 1%-10%, the content of the surfactant is 0.1%-5%.
In above-mentioned aminolevulinic acid cold cream, pharmacy or the acceptable auxiliary material of cosmetic field include but is not limited to list firmly
Glycerol, preservative, albolene, white oil, beeswax, lanolin, glycerine, water, salicylic acid etc..
In above-mentioned aminolevulinic acid cold cream, emulsion include at least one aqueous components and carrier (at least one alcohol, extremely
A kind of few surfactant), wherein aqueous components are mainly to form buffer salt system.
In above-mentioned aminolevulinic acid cold cream, it is preferred that the aminolevulinic acid cold cream includes the following raw material component：
In above-mentioned aminolevulinic acid cold cream, it is preferred that the aminolevulinic acid derivative includes MAL
One or more of combinations in hydrochloride, aminolevulinic acid phosphate and aminovaleric acid hydrochloride.
In above-mentioned aminolevulinic acid cold cream, it is preferred that the aminolevulinic acid cold cream includes the following raw material component：
In above-mentioned aminolevulinic acid cold cream, it is preferred that the monostearate that the emulsifying agent includes 270-330 parts by weight is sweet
The Tween 80 of grease and 15-20 parts by weight.
In above-mentioned aminolevulinic acid cold cream, it is preferred that the aminolevulinic acid cold cream includes the following raw material component：
In above-mentioned aminolevulinic acid cold cream, it is preferred that the emulsifying agent includes the glycerin monostearate of 319 parts by weight
With the Tween 80 of 19 parts by weight.
In above-mentioned aminolevulinic acid cold cream, it is preferred that the alcohol includes isopropanol.
In above-mentioned aminolevulinic acid cold cream, it is preferred that the aqueous components include phosphate buffer.
In above-mentioned aminolevulinic acid cold cream, surfactant is used for film forming, can select phosphatide or ceramide；It is preferred that
, the surfactant includes lecithin.
In above-mentioned aminolevulinic acid cold cream, lecithin is preferably soybean lecithin or egg lecithin；It is preferred that, it is described
Surfactant is soybean lecithin.
The aminolevulinic acid cold cream of the present invention is a kind of reagent of water in oil form, and this composition causes the stability of medicine
It is improved.Isopropanol rather than ethanol are selected, is due to that isopropanol may be such that the yardstick of particulate in uniform emulsion is smaller, particle
Reduce the stability for being conducive to improving reagent.
In above-mentioned aminolevulinic acid cold cream, it is preferred that in the emulsion described in per unit, include 2g soybean lecithin
The phosphate buffer of fat, 6g isopropanol and 90mL.
In above-mentioned aminolevulinic acid cold cream, phosphate buffer is common agents, can be made by conventional method, side
Method is as follows：Sodium dihydrogen phosphate 3g is taken, is dissolved in 100ml water, obtains sodium dihydrogen phosphate；Disodium hydrogen phosphate 1g is taken, 20ml is dissolved in
In water, disodium phosphate soln is obtained；Take sodium dihydrogen phosphate 85ml and disodium phosphate soln 15ml respectively again, mixing is mixed
It is even, adjust pH value to 6, produce phosphate buffer solution.
The present invention also provides the preparation method of above-mentioned aminolevulinic acid cold cream, comprises the following steps：
Obtain carrying medicine phases after aminolevulinic acid derivative is mixed with emulsion；
Albolene, white oil, lanolin, beeswax are mixed with emulsifying agent, heat is standby to 70 DEG C of -80 DEG C of insulations altogether, during which
It is stirred continuously, obtains oil phase；
Water and glycerine are mixed, addition bigcatkin willow acid for adjusting pH value is about 6, and heat is standby to 70 DEG C of -80 DEG C of insulations altogether, obtains water
Phase；
Under 70 DEG C of -80 DEG C of water bath conditions, aqueous phase is slowly added into oil phase, adition process and is stirred continuously；(preferably 5min
The mixture stirred is removed into water bath afterwards), natural cooling, when mixture temperature is down to 50 DEG C, adds and carries medicine phases,
Room temperature is cooled to after stirring, aminolevulinic acid cold cream is obtained.
In above-mentioned preparation method, it is preferred that the emulsion is by being fallen after soybean lecithin is mixed with isopropanol
Enter in phosphate buffer, be mixed to get.
In above-mentioned preparation method, it is preferred that the emulsifying agent is by the way that glycerin monostearate and Tween 80 are mixed
Prepare.
The present invention also provides a kind of composition, and it includes above-mentioned aminolevulinic acid cold cream.
In combinations of the above thing, in cosmetic field, for the different purposes of final products, the examination of non-therapeutic can be added
Agent, such as：Emollient, colouring agent, spices etc., for the purpose of local beauty, it should be noted that avoid hindering the transparency of product.
The present invention also provides above-mentioned aminolevulinic acid cold cream is including condyloma acuminatum, solar lentigines angling as preparation treatment
Application in the dermopathic medicine of disease and squamous cell carcinoma.
The present invention also provides application of the above-mentioned aminolevulinic acid cold cream in as cosmetics and skincare product or cosmetics.It can use
In the tender skin of light, whitening, improve freckle, microgroove, the light aging problem such as pachylosis, it is good and cold cream is in faintly acid using comfort,
The acid-base value of suitable skin.
The present invention protrusion effect be：
The aminolevulinic acid cold cream of the present invention, in dept. of dermatology field, main function is the local treatment to skin, protection by
Damage position not contact with the external world, it is possible to increase drugloading rate and bioavilability, easy to use, skin sense is comfortable, and composition is uniform, chemistry
Property is stable, it is possible to increase ALA permeability, and then strengthens the permeability of skin and tissue；Technically it is easier to promote.
Embodiment
The technical scheme in the present invention is clearly and completely described below in conjunction with specific embodiment, it is clear that retouched
The embodiment stated is only a part of embodiment of the invention, rather than whole embodiments.Based on the embodiment in the present invention, sheet
The every other embodiment that field those of ordinary skill is obtained under the premise of creative work is not made, belongs to the present invention
The scope of protection.
Embodiment 1
The present embodiment provides a kind of aminolevulinic acid cold cream (10wt% aminolevulinic acid contents cold cream), and it includes following original
Expect component：
MAL hydrochloride 0.5g, glycerin monostearate 0.33g, Tween 80 0.019g, albolene
0.39g, white oil 1.36g, lanolin 0.16g, beeswax 0.23g, salicylic acid 0.01g (are used to adjust pH), glycerine 0.2g, water
1.2g, uniform emulsion 0.62g.
The preparation method of the MAL hydrochloride cold cream of the present embodiment is as follows：
Step 1：Prepare emulsion：Soybean lecithin 2g is taken in centrifuge tube, 6g isopropanols are added；Vibration is well mixed；
Mixture is slowly added into 90ml phosphate buffers, is well mixed, produces；
Above-mentioned phosphate buffer solution is to be prepared via a method which：Sodium dihydrogen phosphate 3g is taken, is dissolved in 100ml water,
Obtain sodium dihydrogen phosphate；Disodium hydrogen phosphate 1g is taken, is dissolved in 20ml water, obtains disodium phosphate soln；Take di(2-ethylhexyl)phosphate respectively again
Hydrogen sodium solution 85ml and disodium phosphate soln 15ml, mixing is mixed, and regulation pH value produces phosphate buffer solution to 6；
Step 2：Prepare and carry medicine phases：MAL hydrochloride is weighed, emulsion is added, vibration is well mixed, i.e.,
；
Step 3：Prepare oil phase：Albolene, white oil, lanolin, beeswax are weighed, emulsifying agent (glycerol monostearate is added
Ester and Tween 80, which are mixed with, to be obtained), mixing is hot standby to 75 DEG C of insulations altogether by oil phase and emulsifying agent, is during which stirred continuously；
Step 4：Prepare aqueous phase：By water and glycerine by mixing, a certain amount of salicylic acid is added, is about 6 for adjusting pH, altogether
Heat is incubated standby to 70-80 DEG C；
Step 5：Under 70-80 DEG C of water bath condition, aqueous phase is slowly added into oil phase, adition process using dropper and uses magnetic
Power agitator is stirred continuously, and speed is about 1300r/min, obtains mixture；
Step 6：When the temperature of mixture in step 5 is cooled down into 50 DEG C, load medicine phases are slowly added into using dropper, are stirred
Room temperature is cooled to after uniform, that is, obtains aminolevulinic acid cold cream.
Embodiment 2
The present embodiment provides a kind of MAL hydrochloride cold cream (16% aminolevulinic acid content cold cream), and it is wrapped
Include the following raw material component：
MAL hydrochloride 0.8g, glycerin monostearate 0.27g, Tween 80 0.016g, albolene
0.32g, white oil 1.12g, lanolin 0.13g, beeswax 0.19g, salicylic acid 0.01g (are used to adjust pH), glycerine 0.16g, water
1.0g, uniform emulsion 1.0g.
The preparation method of the MAL hydrochloride cold cream of the present embodiment is as follows：
Step 1：Prepare emulsion：Soybean lecithin 2g is taken in centrifuge tube, 6g isopropanols are added；Vibration is well mixed；
Mixture is slowly added into 90ml phosphate buffers, is well mixed, produces；
Above-mentioned phosphate buffer solution is to be prepared via a method which：Sodium dihydrogen phosphate 3g is taken, is dissolved in 100ml water, obtains
Sodium dihydrogen phosphate；Disodium hydrogen phosphate 1g is taken, is dissolved in 20ml water, obtains disodium phosphate soln；Take biphosphate respectively again
Sodium solution 85ml and disodium phosphate soln 15ml, mixing is mixed, and regulation pH value produces phosphate buffer solution to 6；
Step 2：Prepare and carry medicine phases：Weigh MAL hydrochloride appropriate, add appropriate uniform emulsion, vibration
It is well mixed；
Step 3：Prepare oil phase：Albolene, white oil, lanolin, beeswax are weighed, emulsifying agent (glycerol monostearate is added
Ester and Tween 80, which are mixed with, to be obtained), mixing is hot standby to 75 DEG C of insulations altogether by oil phase and emulsifying agent, is during which stirred continuously；
Step 4：Prepare aqueous phase：By water and glycerine by mixing, a certain amount of salicylic acid is added, is about 6 for adjusting pH, will
Heat, to 70-80 DEG C, is incubated standby aqueous phase altogether；
Step 5：Under 70-80 DEG C of water bath condition, aqueous phase is slowly added into oil phase, adition process using dropper and uses magnetic
Power agitator is stirred continuously, and speed is about 1300r/min, obtains mixture；
Step 6：When the temperature of mixture in step 5 is cooled down into 50 DEG C, load medicine phases are slowly added into using dropper, are stirred
Room temperature is cooled to after uniform, that is, obtains aminolevulinic acid cold cream.
Embodiment 3
The present embodiment provides a kind of aminolevulinic acid cold cream (20% aminolevulinic acid content cold cream), and it includes the following raw material
Component：
MAL hydrochloride 1g, glycerin monostearate 0.032g, Tween 80 0.019g, albolene
0.37g, white oil 1.13g, lanolin 0.15g, beeswax 0.23g, salicylic acid 0.01g (it is about 6 to be used to adjust pH value), glycerine
0.19g, water 1.12g, uniform emulsion 1.25g.
The preparation method process be the same as Example 1,2 of the MAL hydrochloride cold cream of the present embodiment.
Embodiment 4
The present embodiment provides a kind of aminolevulinic acid cold cream, and it includes the following raw material component：
Aminolevulinic acid phosphate 1g, glycerin monostearate 0.032g, Tween 80 0.019g, albolene 0.37g,
White oil 1.13g, lanolin 0.15g, beeswax 0.23g, salicylic acid 0.01g (it is about 6 to be used to adjust pH value), glycerine 0.19g, water
1.12g, uniform emulsion 1.25g.
The preparation method process be the same as Example 1,2 of the MAL hydrochloride cold cream of the present embodiment.
Embodiment 5
The present embodiment provides a kind of aminolevulinic acid cold cream, and it includes the following raw material component：
Aminovaleric acid hydrochloride 1g, glycerin monostearate 0.032g, Tween 80 0.019g, albolene 0.37g,
White oil 1.13g, lanolin 0.15g, beeswax 0.23g, salicylic acid 0.01g (it is about 6 to be used to adjust pH value), glycerine 0.19g, water
1.12g, uniform emulsion 1.25g.
The preparation method process be the same as Example 1,2 of the MAL hydrochloride cold cream of the present embodiment.
Embodiment 6
The present embodiment provides a kind of aminolevulinic acid cold cream, and it includes the following raw material component：
MAL hydrochloride and aminovaleric acid hydrochloride are (according to 2:1 weight is than mixing) 1g, it is single stearic
Acid glyceride 0.032g, Tween 80 0.019g, albolene 0.37g, white oil 1.13g, lanolin 0.15g, beeswax 0.23g, water
Poplar acid 0.01g (it is about 6 to be used to adjust pH value), glycerine 0.19g, water 1.12g, uniform emulsion 1.25g.
The preparation method process be the same as Example 1,2 of the MAL hydrochloride cold cream of the present embodiment.
Embodiment 7
The present embodiment provides a kind of clinical practice of aminolevulinic acid cold cream, the amino ketones penta for verifying embodiment 1-3
The action effect of sour cold cream：
Randomly select 20 suffer from skin problem patients, be randomly divided into 3 groups, respectively using 10%, 16%, 20% this three
The aminolevulinic acid cold cream of various concentrations is planted, coordinates photodynamic therapy, external curing skin problem carries out comparative study, observation
The curative effect of various concentrations and its adverse reaction.Treatment method is：Medication once, after coating 2h, is cleaned, then shone with feux rouges weekly
Penetrate, irradiation time, irradiation gross energy about 100J/cm are adjusted according to irradiated area2, medicine is shared three times, after each course for the treatment of terminates
Follow-up is carried out, therapeutic effect is tracked in time.
1st, skin whitening, moisturizing effect expedition
The moisturizing effect of cold cream made from embodiment 1-3 is evaluated using the cutaneous sensibility of human body.Subject is every
After secondary use, used cold cream is given a mark.The total score of every using effect is 5 points, 5 points to be very satisfied, 4 points be compared with
Satisfied, 3 points are to receive, and 2 points are bad, and 1 point is very poor.It is below every average, is shown in Table 1.
The skin whitening, moisturizing effect expedition of the aminolevulinic acid cold cream of table 1 embodiment 1-3, tri- kinds of different contents
| Whitening | Moistness | |
| 10% aminolevulinic acid cold cream | 4.2 | 4.6 |
| 16% aminolevulinic acid cold cream | 4.6 | 4.8 |
| 20% aminolevulinic acid cold cream | 4.7 | 4.6 |
As a result show, whitening and moisturizing effect of the subject to the aminolevulinic acid cold cream of the present invention are had higher rating.
2nd, clinical therapeutic efficacy
Criterion of therapeutical effect：Recovery from illness：Erythema comedo disappears, and recovers normal skin tone.It is evident in efficacy：Erythema comedo disappear it is most of or
It has been reduced that, the damaged skin for crossing semi-area recovers normal skin tone.Effectively：Erythema comedo has taken a turn for the better, and recovers normal skin
Area is more than 10.It is invalid：Erythema comedo is unchanged, recovers normal skin area and is less than 10.Recovery from illness, curative effect
Significantly, effective three combine and calculate as effective percentage.Therapeutic effect is shown：Most patients after the treatment of three courses for the treatment of,
Skin of face problem has taken a turn for the better, and has indivedual skin problems more serious patient after second is treated, the increase of erythema area,
Acne increase, continues medication, has alleviated after being treated at three times, by bimestrial convalescence after treatment, the big portion of skin problem
Divide and recover normal.Specific curative effect see the table below：
The clinical effectiveness of the aminolevulinic acid cold cream of table 2 embodiment 1-3, tri- kinds of different contents
| Number of cases | Recovery from illness | It is evident in efficacy | Effectively | It is invalid | It is efficient | |
| 10% aminolevulinic acid cold cream | 7 | 1 | 2 | 2 | 2 | 71.43% |
| 16% aminolevulinic acid cold cream | 6 | 1 | 3 | 1 | 1 | 83.33% |
| 20% aminolevulinic acid cold cream | 7 | 2 | 3 | 1 | 1 | 85.71% |
It can be seen that, the raising of drugloading rate can improve the clinical effectiveness of aminolevulinic acid cold cream, meanwhile, the amino ketones of high concentration
Valeric acid cold cream, which also has, preferably moistens degree, and skin experience sense is preferable.
That is, above-described embodiment is visible, aminolevulinic acid cold cream of the invention, in dept. of dermatology field, main function
For the local treatment to skin, damaged part is protected not contacted with the external world, it is possible to increase drugloading rate and bioavilability, user
Just, comfortably, composition is uniform for skin sense, and chemical property is stable, it is possible to increase ALA permeability, and then strengthens skin and oozing for organizing
Permeability；Technically it is easier to promote.
The foregoing description of the disclosed embodiments, enables professional and technical personnel in the field to realize or using the present invention.
A variety of modifications to these embodiments will be apparent for those skilled in the art, as defined herein
General Principle can be realized in other embodiments without departing from the spirit or scope of the present invention.Therefore, it is of the invention
The embodiments shown herein is not intended to be limited to, and is to fit to and principles disclosed herein and features of novelty phase one
The most wide scope caused.
Claims (13)
1. a kind of aminolevulinic acid cold cream, it is included in aminolevulinic acid derivative, emulsion and other pharmacies or cosmetics
Acceptable auxiliary material；
Wherein, the emulsion includes at least one aqueous components, at least one alcohol and at least one surfactant；
Counted using the gross weight of emulsion as 100%, the content of the aqueous components is 50%-98%, and the content of the alcohol is
1%-10%, the content of the surfactant is 0.1%-5%.
2. aminolevulinic acid cold cream according to claim 1, wherein, the aminolevulinic acid cold cream includes the following raw material group
Point：
3. aminolevulinic acid cold cream according to claim 2, wherein, the aminolevulinic acid derivative includes amino ketones penta
One or more of combinations in acid methyl ester hydrochloride salt, aminolevulinic acid phosphate and aminovaleric acid hydrochloride.
4. aminolevulinic acid cold cream according to claim 3, wherein, the aminolevulinic acid cold cream includes the following raw material group
Point：
5. the aminolevulinic acid cold cream according to claim any one of 2-4, wherein, the emulsifying agent includes 270-330 weights
Measure the glycerin monostearate of part and the Tween 80 of 15-20 parts by weight.
6. aminolevulinic acid cold cream according to claim 4, wherein, the aminolevulinic acid cold cream includes the following raw material group
Point：
It is preferred that, the emulsifying agent includes the glycerin monostearate of 319 parts by weight and the Tween 80 of 19 parts by weight.
7. the aminolevulinic acid cold cream according to claim any one of 1-6, wherein, the alcohol includes isopropanol；It is preferred that,
The aqueous components include phosphate buffer；It is preferred that, the surfactant includes lecithin；It is further preferred that institute
Surfactant is stated for soybean lecithin.
8. aminolevulinic acid cold cream according to claim 7, wherein, in the emulsion described in per unit, including 2g's is big
The phosphate buffer of beans lecithin, 6g isopropanol and 90mL.
9. the preparation method of the aminolevulinic acid cold cream described in claim any one of 1-8, comprises the following steps：
Obtain carrying medicine phases after aminolevulinic acid derivative is mixed with emulsion；
Albolene, white oil, lanolin, beeswax are mixed with emulsifying agent, heat is standby to 70 DEG C of -80 DEG C of insulations altogether, obtains oil phase；
Water and glycerine are mixed, addition bigcatkin willow acid for adjusting pH value is 6, and heat is standby to 70 DEG C of -80 DEG C of insulations altogether, obtains aqueous phase；
Under 70 DEG C of -80 DEG C of water bath conditions, aqueous phase is added and is stirred continuously in oil phase, adition process；By the mixture after stirring
Water bath is removed, cooling, when mixture temperature is down to 50 DEG C, adds and carries medicine phases, be cooled to room temperature after stirring, obtain amino
Ketone valeric acid cold cream.
10. preparation method according to claim 9, wherein, the emulsion is by by soybean lecithin and isopropanol
Pour into phosphate buffer, be mixed to get after mixing.
11. preparation method according to claim 9, wherein, the emulsifying agent is by by glycerin monostearate and telling
Temperature 80 is mixed with what is obtained.
12. aminolevulinic acid cold cream described in claim any one of 1-8 as prepare treatment include condyloma acuminatum, it is solar lentigines
Application in the dermopathic medicine of keratosis and squamous cell carcinoma.
13. application of the aminolevulinic acid cold cream described in claim any one of 1-8 in as cosmetics and skincare product or cosmetics.
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