CN117100644A - Semitransparent to transparent aqueous solution containing sphingosine and non-salt derivatives and preparation method thereof - Google Patents
Semitransparent to transparent aqueous solution containing sphingosine and non-salt derivatives and preparation method thereof Download PDFInfo
- Publication number
- CN117100644A CN117100644A CN202311133372.7A CN202311133372A CN117100644A CN 117100644 A CN117100644 A CN 117100644A CN 202311133372 A CN202311133372 A CN 202311133372A CN 117100644 A CN117100644 A CN 117100644A
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- CN
- China
- Prior art keywords
- peg
- sphingosine
- salt derivatives
- fatty acid
- oil
- 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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- WWUZIQQURGPMPG-KRWOKUGFSA-N sphingosine Chemical compound CCCCCCCCCCCCC\C=C\[C@@H](O)[C@@H](N)CO WWUZIQQURGPMPG-KRWOKUGFSA-N 0.000 title claims abstract description 61
- WWUZIQQURGPMPG-UHFFFAOYSA-N (-)-D-erythro-Sphingosine Natural products CCCCCCCCCCCCCC=CC(O)C(N)CO WWUZIQQURGPMPG-UHFFFAOYSA-N 0.000 title claims abstract description 60
- 150000003839 salts Chemical class 0.000 title claims abstract description 58
- 239000007864 aqueous solution Substances 0.000 title claims abstract description 27
- 238000002360 preparation method Methods 0.000 title claims abstract description 20
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 61
- 239000004359 castor oil Substances 0.000 claims abstract description 34
- 235000019438 castor oil Nutrition 0.000 claims abstract description 34
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims abstract description 34
- 239000011550 stock solution Substances 0.000 claims abstract description 34
- 238000000034 method Methods 0.000 claims abstract description 28
- 239000007788 liquid Substances 0.000 claims abstract description 20
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 16
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 16
- 229930195729 fatty acid Natural products 0.000 claims abstract description 16
- 239000000194 fatty acid Substances 0.000 claims abstract description 16
- -1 glycerol fatty acid ester Chemical class 0.000 claims abstract description 15
- 150000003904 phospholipids Chemical class 0.000 claims abstract description 13
- 230000007935 neutral effect Effects 0.000 claims abstract description 12
- 238000010438 heat treatment Methods 0.000 claims abstract description 11
- 229920000136 polysorbate Polymers 0.000 claims abstract description 10
- 230000008569 process Effects 0.000 claims abstract description 9
- 239000004094 surface-active agent Substances 0.000 claims abstract description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229930182558 Sterol Natural products 0.000 claims abstract description 8
- 150000001413 amino acids Chemical class 0.000 claims abstract description 8
- 150000003432 sterols Chemical class 0.000 claims abstract description 8
- 235000003702 sterols Nutrition 0.000 claims abstract description 8
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 8
- 238000001914 filtration Methods 0.000 claims abstract description 4
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 42
- 239000000243 solution Substances 0.000 claims description 26
- AERBNCYCJBRYDG-UHFFFAOYSA-N D-ribo-phytosphingosine Natural products CCCCCCCCCCCCCCC(O)C(O)C(N)CO AERBNCYCJBRYDG-UHFFFAOYSA-N 0.000 claims description 19
- AERBNCYCJBRYDG-KSZLIROESA-N phytosphingosine Chemical compound CCCCCCCCCCCCCC[C@@H](O)[C@@H](O)[C@@H](N)CO AERBNCYCJBRYDG-KSZLIROESA-N 0.000 claims description 19
- 229940033329 phytosphingosine Drugs 0.000 claims description 19
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 18
- LUZYTSCABOWJAC-HLJNGVMWSA-N 6-hydroxysphing-4E-enine Chemical compound CCCCCCCCCCCCC(O)\C=C\[C@@H](O)[C@@H](N)CO LUZYTSCABOWJAC-HLJNGVMWSA-N 0.000 claims description 14
- 239000003921 oil Substances 0.000 claims description 13
- 235000019198 oils Nutrition 0.000 claims description 13
- 229930182830 galactose Natural products 0.000 claims description 12
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 10
- WQZGKKKJIJFFOK-PHYPRBDBSA-N alpha-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 claims description 10
- 229930091371 Fructose Natural products 0.000 claims description 9
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 9
- 239000005715 Fructose Substances 0.000 claims description 9
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 9
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 9
- 150000004665 fatty acids Chemical group 0.000 claims description 9
- 239000008103 glucose Substances 0.000 claims description 9
- 229950004354 phosphorylcholine Drugs 0.000 claims description 9
- PYJNAPOPMIJKJZ-UHFFFAOYSA-N phosphorylcholine chloride Chemical compound [Cl-].C[N+](C)(C)CCOP(O)(O)=O PYJNAPOPMIJKJZ-UHFFFAOYSA-N 0.000 claims description 9
- 150000004671 saturated fatty acids Chemical class 0.000 claims description 9
- 239000000126 substance Substances 0.000 claims description 9
- 235000021122 unsaturated fatty acids Nutrition 0.000 claims description 9
- 150000004670 unsaturated fatty acids Chemical class 0.000 claims description 9
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 8
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims description 8
- 238000012377 drug delivery Methods 0.000 claims description 8
- 229940015975 1,2-hexanediol Drugs 0.000 claims description 7
- 235000011187 glycerol Nutrition 0.000 claims description 7
- FHKSXSQHXQEMOK-UHFFFAOYSA-N hexane-1,2-diol Chemical compound CCCCC(O)CO FHKSXSQHXQEMOK-UHFFFAOYSA-N 0.000 claims description 7
- 229940068065 phytosterols Drugs 0.000 claims description 7
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 7
- 229920000053 polysorbate 80 Polymers 0.000 claims description 7
- XMVBHZBLHNOQON-UHFFFAOYSA-N 2-butyl-1-octanol Chemical compound CCCCCCC(CO)CCCC XMVBHZBLHNOQON-UHFFFAOYSA-N 0.000 claims description 6
- XULHFMYCBKQGEE-UHFFFAOYSA-N 2-hexyl-1-Decanol Chemical compound CCCCCCCCC(CO)CCCCCC XULHFMYCBKQGEE-UHFFFAOYSA-N 0.000 claims description 6
- DKPFZGUDAPQIHT-UHFFFAOYSA-N Butyl acetate Natural products CCCCOC(C)=O DKPFZGUDAPQIHT-UHFFFAOYSA-N 0.000 claims description 6
- 229920000604 Polyethylene Glycol 200 Polymers 0.000 claims description 6
- 235000018936 Vitellaria paradoxa Nutrition 0.000 claims description 6
- 241001135917 Vitellaria paradoxa Species 0.000 claims description 6
- 150000001414 amino alcohols Chemical class 0.000 claims description 6
- 235000021302 avocado oil Nutrition 0.000 claims description 6
- 239000008163 avocado oil Substances 0.000 claims description 6
- 235000021324 borage oil Nutrition 0.000 claims description 6
- 239000008169 grapeseed oil Substances 0.000 claims description 6
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 claims description 6
- 125000000311 mannosyl group Chemical group C1([C@@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 claims description 6
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 6
- 239000004006 olive oil Substances 0.000 claims description 6
- 235000008390 olive oil Nutrition 0.000 claims description 6
- 239000003813 safflower oil Substances 0.000 claims description 6
- 229940057910 shea butter Drugs 0.000 claims description 6
- 239000010508 watermelon seed oil Substances 0.000 claims description 6
- 239000004480 active ingredient Substances 0.000 claims description 5
- 125000004432 carbon atom Chemical group C* 0.000 claims description 5
- 239000006071 cream Substances 0.000 claims description 5
- 238000010790 dilution Methods 0.000 claims description 5
- 239000012895 dilution Substances 0.000 claims description 5
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 claims description 4
- JZNWSCPGTDBMEW-UHFFFAOYSA-N Glycerophosphorylethanolamin Natural products NCCOP(O)(=O)OCC(O)CO JZNWSCPGTDBMEW-UHFFFAOYSA-N 0.000 claims description 4
- WERYXYBDKMZEQL-UHFFFAOYSA-N butane-1,4-diol Chemical compound OCCCCO WERYXYBDKMZEQL-UHFFFAOYSA-N 0.000 claims description 4
- 235000012000 cholesterol Nutrition 0.000 claims description 4
- 229940107161 cholesterol Drugs 0.000 claims description 4
- DTPCFIHYWYONMD-UHFFFAOYSA-N decaethylene glycol Chemical compound OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO DTPCFIHYWYONMD-UHFFFAOYSA-N 0.000 claims description 4
- GHLKSLMMWAKNBM-UHFFFAOYSA-N dodecane-1,12-diol Chemical compound OCCCCCCCCCCCCO GHLKSLMMWAKNBM-UHFFFAOYSA-N 0.000 claims description 4
- 150000008104 phosphatidylethanolamines Chemical class 0.000 claims description 4
- YPFDHNVEDLHUCE-UHFFFAOYSA-N propane-1,3-diol Chemical compound OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 claims description 4
- HCEPYODGJFPWOI-UHFFFAOYSA-N tridecane-1,13-diol Chemical compound OCCCCCCCCCCCCCO HCEPYODGJFPWOI-UHFFFAOYSA-N 0.000 claims description 4
- XSMIOONHPKRREI-UHFFFAOYSA-N undecane-1,11-diol Chemical compound OCCCCCCCCCCCO XSMIOONHPKRREI-UHFFFAOYSA-N 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 3
- WODOUQLMOIMKAL-FJSYBICCSA-L disodium;(2s)-2-(octadecanoylamino)pentanedioate Chemical compound [Na+].[Na+].CCCCCCCCCCCCCCCCCC(=O)N[C@H](C([O-])=O)CCC([O-])=O WODOUQLMOIMKAL-FJSYBICCSA-L 0.000 claims description 3
- 150000007529 inorganic bases Chemical class 0.000 claims description 3
- 150000007522 mineralic acids Chemical class 0.000 claims description 3
- 150000007524 organic acids Chemical class 0.000 claims description 3
- 150000007530 organic bases Chemical class 0.000 claims description 3
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims description 3
- 150000003905 phosphatidylinositols Chemical class 0.000 claims description 3
- 229940043375 1,5-pentanediol Drugs 0.000 claims description 2
- ALVZNPYWJMLXKV-UHFFFAOYSA-N 1,9-Nonanediol Chemical compound OCCCCCCCCCO ALVZNPYWJMLXKV-UHFFFAOYSA-N 0.000 claims description 2
- OJRJDENLRJHEJO-UHFFFAOYSA-N 2,4-diethylpentane-1,5-diol Chemical compound CCC(CO)CC(CC)CO OJRJDENLRJHEJO-UHFFFAOYSA-N 0.000 claims description 2
- ZJWDJIVISLUQQZ-UHFFFAOYSA-N 2,4-dimethylpentane-1,5-diol Chemical compound OCC(C)CC(C)CO ZJWDJIVISLUQQZ-UHFFFAOYSA-N 0.000 claims description 2
- DSKYSDCYIODJPC-UHFFFAOYSA-N 2-butyl-2-ethylpropane-1,3-diol Chemical compound CCCCC(CC)(CO)CO DSKYSDCYIODJPC-UHFFFAOYSA-N 0.000 claims description 2
- AJKXDPSHWRTFOZ-UHFFFAOYSA-N 2-ethylhexane-1,6-diol Chemical compound CCC(CO)CCCCO AJKXDPSHWRTFOZ-UHFFFAOYSA-N 0.000 claims description 2
- SDQROPCSKIYYAV-UHFFFAOYSA-N 2-methyloctane-1,8-diol Chemical compound OCC(C)CCCCCCO SDQROPCSKIYYAV-UHFFFAOYSA-N 0.000 claims description 2
- QWGRWMMWNDWRQN-UHFFFAOYSA-N 2-methylpropane-1,3-diol Chemical compound OCC(C)CO QWGRWMMWNDWRQN-UHFFFAOYSA-N 0.000 claims description 2
- LEACJMVNYZDSKR-UHFFFAOYSA-N 2-octyldodecan-1-ol Chemical compound CCCCCCCCCCC(CO)CCCCCCCC LEACJMVNYZDSKR-UHFFFAOYSA-N 0.000 claims description 2
- SXFJDZNJHVPHPH-UHFFFAOYSA-N 3-methylpentane-1,5-diol Chemical compound OCCC(C)CCO SXFJDZNJHVPHPH-UHFFFAOYSA-N 0.000 claims description 2
- ALQSHHUCVQOPAS-UHFFFAOYSA-N Pentane-1,5-diol Chemical compound OCCCCCO ALQSHHUCVQOPAS-UHFFFAOYSA-N 0.000 claims description 2
- 229920001213 Polysorbate 20 Polymers 0.000 claims description 2
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 2
- YIMQCDZDWXUDCA-UHFFFAOYSA-N [4-(hydroxymethyl)cyclohexyl]methanol Chemical compound OCC1CCC(CO)CC1 YIMQCDZDWXUDCA-UHFFFAOYSA-N 0.000 claims description 2
- 238000001816 cooling Methods 0.000 claims description 2
- 150000002009 diols Chemical class 0.000 claims description 2
- 229940079784 disodium stearoyl glutamate Drugs 0.000 claims description 2
- BWELVAFPJUDDFX-UHFFFAOYSA-N dodecane-1,10-diol Chemical compound CCC(O)CCCCCCCCCO BWELVAFPJUDDFX-UHFFFAOYSA-N 0.000 claims description 2
- SXCBDZAEHILGLM-UHFFFAOYSA-N heptane-1,7-diol Chemical compound OCCCCCCCO SXCBDZAEHILGLM-UHFFFAOYSA-N 0.000 claims description 2
- XXMIOPMDWAUFGU-UHFFFAOYSA-N hexane-1,6-diol Chemical compound OCCCCCCO XXMIOPMDWAUFGU-UHFFFAOYSA-N 0.000 claims description 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 2
- ASKIVFGGGGIGKH-UHFFFAOYSA-N isostearic acid monoglyceride Natural products CC(C)CCCCCCCCCCCCCCC(=O)OCC(O)CO ASKIVFGGGGIGKH-UHFFFAOYSA-N 0.000 claims description 2
- SLCVBVWXLSEKPL-UHFFFAOYSA-N neopentyl glycol Chemical compound OCC(C)(C)CO SLCVBVWXLSEKPL-UHFFFAOYSA-N 0.000 claims description 2
- OEIJHBUUFURJLI-UHFFFAOYSA-N octane-1,8-diol Chemical compound OCCCCCCCCO OEIJHBUUFURJLI-UHFFFAOYSA-N 0.000 claims description 2
- 229940049964 oleate Drugs 0.000 claims description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims description 2
- ZBPYFGWSQQFVCJ-UHFFFAOYSA-N pentadecane-1,15-diol Chemical compound OCCCCCCCCCCCCCCCO ZBPYFGWSQQFVCJ-UHFFFAOYSA-N 0.000 claims description 2
- 229940075999 phytosterol ester Drugs 0.000 claims description 2
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims description 2
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims description 2
- 229940045898 sodium stearoyl glutamate Drugs 0.000 claims description 2
- KDHFCTLPQJQDQI-BDQAORGHSA-M sodium;(4s)-4-amino-5-octadecanoyloxy-5-oxopentanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC(=O)OC(=O)[C@@H](N)CCC([O-])=O KDHFCTLPQJQDQI-BDQAORGHSA-M 0.000 claims description 2
- NTYZDAJPNNBYED-UHFFFAOYSA-M sodium;2-(2-dodecanoyloxypropanoyloxy)propanoate Chemical compound [Na+].CCCCCCCCCCCC(=O)OC(C)C(=O)OC(C)C([O-])=O NTYZDAJPNNBYED-UHFFFAOYSA-M 0.000 claims description 2
- XLKZJJVNBQCVIX-UHFFFAOYSA-N tetradecane-1,14-diol Chemical compound OCCCCCCCCCCCCCCO XLKZJJVNBQCVIX-UHFFFAOYSA-N 0.000 claims description 2
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- 239000000463 material Substances 0.000 abstract description 34
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- VVGIYYKRAMHVLU-UHFFFAOYSA-N newbouldiamide Natural products CCCCCCCCCCCCCCCCCCCC(O)C(O)C(O)C(CO)NC(=O)CCCCCCCCCCCCCCCCC VVGIYYKRAMHVLU-UHFFFAOYSA-N 0.000 description 14
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- FHQVHHIBKUMWTI-ZCXUNETKSA-N 1-palmitoyl-2-oleoyl phosphatidylethanolamine Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(COP(O)(=O)OCCN)OC(=O)CCCCCCC\C=C/CCCCCCCC FHQVHHIBKUMWTI-ZCXUNETKSA-N 0.000 description 2
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- ATGQXSBKTQANOH-UWVGARPKSA-N N-oleoylphytosphingosine Chemical compound CCCCCCCCCCCCCC[C@@H](O)[C@@H](O)[C@H](CO)NC(=O)CCCCCCC\C=C/CCCCCCCC ATGQXSBKTQANOH-UWVGARPKSA-N 0.000 description 2
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- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
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- 230000009467 reduction Effects 0.000 description 2
- 238000010008 shearing Methods 0.000 description 2
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 description 2
- 238000005728 strengthening Methods 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 230000002087 whitening effect Effects 0.000 description 2
- ALFPYCWNTIZXMT-MHYRICRISA-N (E,2R,3R)-2-aminooctadec-4-ene-1,1,3-triol Chemical compound OC(O)[C@H](N)[C@H](O)\C=C\CCCCCCCCCCCCC ALFPYCWNTIZXMT-MHYRICRISA-N 0.000 description 1
- NRJAVPSFFCBXDT-HUESYALOSA-N 1,2-distearoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCCCC NRJAVPSFFCBXDT-HUESYALOSA-N 0.000 description 1
- HMUNWXXNJPVALC-UHFFFAOYSA-N 1-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)C(CN1CC2=C(CC1)NN=N2)=O HMUNWXXNJPVALC-UHFFFAOYSA-N 0.000 description 1
- WTJKGGKOPKCXLL-VYOBOKEXSA-N 1-hexadecanoyl-2-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/CCCCCCCC WTJKGGKOPKCXLL-VYOBOKEXSA-N 0.000 description 1
- PZNPLUBHRSSFHT-RRHRGVEJSA-N 1-hexadecanoyl-2-octadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[C@@H](COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCCCCCCCCCC PZNPLUBHRSSFHT-RRHRGVEJSA-N 0.000 description 1
- RFVFQQWKPSOBED-PSXMRANNSA-N 1-myristoyl-2-palmitoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)O[C@@H](COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCCCCCCCC RFVFQQWKPSOBED-PSXMRANNSA-N 0.000 description 1
- MZWGYEJOZNRLQE-KXQOOQHDSA-N 1-stearoyl-2-myristoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCC MZWGYEJOZNRLQE-KXQOOQHDSA-N 0.000 description 1
- VZSRBBMJRBPUNF-UHFFFAOYSA-N 2-(2,3-dihydro-1H-inden-2-ylamino)-N-[3-oxo-3-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)propyl]pyrimidine-5-carboxamide Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C(=O)NCCC(N1CC2=C(CC1)NN=N2)=O VZSRBBMJRBPUNF-UHFFFAOYSA-N 0.000 description 1
- KILNVBDSWZSGLL-UHFFFAOYSA-O 2-[2,3-di(hexadecanoyloxy)propoxy-hydroxyphosphoryl]oxyethyl-trimethylazanium Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(COP(O)(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCC KILNVBDSWZSGLL-UHFFFAOYSA-O 0.000 description 1
- SXAMGRAIZSSWIH-UHFFFAOYSA-N 2-[3-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]-1,2,4-oxadiazol-5-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C1=NOC(=N1)CC(=O)N1CC2=C(CC1)NN=N2 SXAMGRAIZSSWIH-UHFFFAOYSA-N 0.000 description 1
- WZFUQSJFWNHZHM-UHFFFAOYSA-N 2-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)CC(=O)N1CC2=C(CC1)NN=N2 WZFUQSJFWNHZHM-UHFFFAOYSA-N 0.000 description 1
- YJLUBHOZZTYQIP-UHFFFAOYSA-N 2-[5-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]-1,3,4-oxadiazol-2-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C1=NN=C(O1)CC(=O)N1CC2=C(CC1)NN=N2 YJLUBHOZZTYQIP-UHFFFAOYSA-N 0.000 description 1
- CONKBQPVFMXDOV-QHCPKHFHSA-N 6-[(5S)-5-[[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]piperazin-1-yl]methyl]-2-oxo-1,3-oxazolidin-3-yl]-3H-1,3-benzoxazol-2-one Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)N1CCN(CC1)C[C@H]1CN(C(O1)=O)C1=CC2=C(NC(O2)=O)C=C1 CONKBQPVFMXDOV-QHCPKHFHSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 1
- GZDFHIJNHHMENY-UHFFFAOYSA-N Dimethyl dicarbonate Chemical compound COC(=O)OC(=O)OC GZDFHIJNHHMENY-UHFFFAOYSA-N 0.000 description 1
- 101001105486 Homo sapiens Proteasome subunit alpha type-7 Proteins 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- BBAFBDLICMHBNU-MFZOPHKMSA-N N-(2-hydroxyoctadecanoyl)-4-hydroxysphinganine Chemical compound CCCCCCCCCCCCCCCCC(O)C(=O)N[C@@H](CO)[C@H](O)[C@H](O)CCCCCCCCCCCCCC BBAFBDLICMHBNU-MFZOPHKMSA-N 0.000 description 1
- 102100021201 Proteasome subunit alpha type-7 Human genes 0.000 description 1
- 206010070834 Sensitisation Diseases 0.000 description 1
- 206010040844 Skin exfoliation Diseases 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 230000001914 calming effect Effects 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 239000008406 cosmetic ingredient Substances 0.000 description 1
- 239000004064 cosurfactant Substances 0.000 description 1
- 230000035618 desquamation Effects 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- CITHEXJVPOWHKC-UHFFFAOYSA-N dimyristoyl phosphatidylcholine Chemical compound CCCCCCCCCCCCCC(=O)OCC(COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCC CITHEXJVPOWHKC-UHFFFAOYSA-N 0.000 description 1
- 229960003724 dimyristoylphosphatidylcholine Drugs 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 231100000321 erythema Toxicity 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 150000002430 hydrocarbons Chemical group 0.000 description 1
- 229940099578 hydrogenated soybean lecithin Drugs 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 description 1
- SZUJJDLBXJCDNT-ZCNNSNEGSA-N n-[(2s,3s,4r)-1,3,4-trihydroxyoctadecan-2-yl]acetamide Chemical compound CCCCCCCCCCCCCC[C@@H](O)[C@@H](O)[C@H](CO)NC(C)=O SZUJJDLBXJCDNT-ZCNNSNEGSA-N 0.000 description 1
- 239000005543 nano-size silicon particle Substances 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 229940101267 panthenol Drugs 0.000 description 1
- 235000020957 pantothenol Nutrition 0.000 description 1
- 239000011619 pantothenol Substances 0.000 description 1
- 229940023462 paste product Drugs 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 125000001095 phosphatidyl group Chemical group 0.000 description 1
- 229920005862 polyol Polymers 0.000 description 1
- 150000003077 polyols Chemical class 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 230000008439 repair process Effects 0.000 description 1
- 230000001932 seasonal effect Effects 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 230000037307 sensitive skin Effects 0.000 description 1
- 230000008313 sensitization Effects 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 230000008591 skin barrier function Effects 0.000 description 1
- 239000002195 soluble material Substances 0.000 description 1
- 229940083466 soybean lecithin Drugs 0.000 description 1
- 150000003408 sphingolipids Chemical class 0.000 description 1
- 229940032094 squalane Drugs 0.000 description 1
- 239000008227 sterile water for injection Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 229910021642 ultra pure water Inorganic materials 0.000 description 1
- 239000012498 ultrapure water Substances 0.000 description 1
- 229930195735 unsaturated hydrocarbon Natural products 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
- A61K8/92—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
- 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
- A61K8/41—Amines
-
- 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
- A61K8/42—Amides
-
- 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
- A61K8/55—Phosphorus compounds
- A61K8/553—Phospholipids, e.g. lecithin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
-
- 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
- A61K8/63—Steroids; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
-
- 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
- A61Q19/005—Preparations for sensitive 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
- A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
- A61K2800/26—Optical properties
- A61K2800/262—Transparent; Translucent
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Chemical & Material Sciences (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Cosmetics (AREA)
Abstract
The application belongs to the technical field of cosmetics, and in particular relates to an aqueous solution containing sphingosine and non-salt derivatives and a preparation method thereof. The stock solution containing sphingosine and its non-salt derivatives comprises: sphingosine and its non-salt derivatives, guerbet alcohol, polyalcohol, glycerol fatty acid ester, neutral phospholipid, sterols, amino acid surfactant, PEG-hydrogenated castor oil or PEG-glycerol fatty acid esters, tween series, and pH regulator; the aqueous solution containing sphingosine and non-salt derivatives comprises stock solution and water. The method comprises the steps of controlling temperature, heating, co-dissolving, filtering to obtain yellowish to yellow transparent liquid, and completing the preparation of the stock solution; taking the stock solution, and diluting with deionized water or oily solvent to obtain semitransparent or transparent liquid. The method solves the application problem of sphingosine and non-salt derivatives thereof in a cosmetic system, and has the advantages of convenient preparation, strong process adaptability, simple equipment requirement, lower material cost and more convenient mass production.
Description
Technical Field
The application relates to the technical field of cosmetics, in particular to semitransparent to transparent aqueous solution containing sphingosine and non-salt derivatives and a preparation method thereof.
Background
Prior art 1: application number CN202310021900.3 discloses a composition with repairing effect, and a preparation method and application thereof. The preparation process comprises the following steps: s1: sequentially adding phytosphingosine, cholesterol, panthenol and carboxymethyl polysaccharide into deionized water, uniformly mixing for 30min, then adding ceramide composition, and uniformly stirring for 20min to obtain a water phase;
s2: uniformly mixing squalane and nano silicon dioxide to obtain an oil phase;
s3: adding the oil phase into the water phase while stirring, controlling the adding time of the oil phase to be 3min, and homogenizing for 1 h. Description of the product obtained: oil-in-water emulsions.
The products obtained by the prior art cannot be used for preparing stable semitransparent to transparent water solution.
In addition, prior art 2: the application number is: 201480076699.8, which discloses information on related patents of ceramide dispersion compositions
The following is a description of the manufacturing method of this embodiment.
< Pre-Dispersion Process >)
In the preparation of the coarse dispersion liquid in the pre-dispersion treatment step, the dispersion treatment is performed in a state where a solution (pre-dispersion treatment solution) containing a specific ceramide and a nonionic surfactant is heated to 100 ℃ or higher, whereby a coarse dispersion liquid in which dispersed particles (dispersed phase) containing a specific ceramide in a molten state by heating are coarsely dispersed in a continuous phase is obtained.
In the pre-dispersion treatment solution, the specific ceramide and nonionic surfactant are simply mixed. The method of mixing the specific ceramide and the nonionic surfactant is not particularly limited, and examples thereof include a method of mixing by stirring.
The pre-dispersion treatment solution may contain other components than the specific ceramide and nonionic surfactant, as required. Examples of the other component include components such as polyol and cholesterol.
In the preparation of the crude dispersion, the pre-dispersion treatment solution is heated to 100 ℃ or higher from the viewpoint of melting the ceramide. The temperature of the pre-dispersion treatment solution reaches more than 100 ℃ when the pre-dispersion treatment solution is subjected to dispersion treatment. The dispersion treatment may be performed in a state where the temperature of the liquid is kept at 100 ℃ or higher by heating the pre-dispersion treatment solution to 100 ℃ or higher, or may be performed while heating the pre-dispersion treatment solution to 100 ℃ or higher.
The method of heating the pre-dispersion treatment solution to 100 ℃ or higher is not particularly limited, and a heating device is usually used. Examples of the heating device include a thermostatic chamber.
The method of dispersing the pre-dispersion treatment solution to obtain a crude dispersion is not particularly limited, and a general stirring device is used. Examples of the stirring device include a magnetic stirrer, a household mixer, a paddle mixer, an impeller mixer, a homomixer, a dispersion mixer, and a super mixer.
The time of the dispersion treatment is not particularly limited, and may be appropriately set according to the type of stirring device, the composition of the pre-dispersion treatment solution, and the like.
< procedure of formal dispersion treatment >)
In the main dispersion treatment step, after mixing the coarse dispersion liquid obtained by the pre-dispersion treatment with water or the like, a dispersion treatment by an ultrasonic dispersion method (hereinafter referred to as ultrasonic dispersion treatment) or a dispersion treatment by a high-pressure emulsification method (hereinafter referred to as high-pressure emulsification treatment) can be performed.
In the main dispersion treatment step, a coarse dispersion liquid containing a molten ceramide and water or the like are mixed and subjected to dispersion treatment, whereby a ceramide dispersion composition containing dispersed particles containing a specific ceramide can be obtained.
From the viewpoint of preventing abrupt boiling, the temperature of the crude dispersion liquid such as mixed water is preferably set to 100 ℃ or less, more preferably set to 90 ℃ to 100 ℃.
The temperature of water and the like is not particularly limited. The temperature of water or the like is preferably set to 50 to 90 ℃.
The crude dispersion and water may be mixed at one time, or may be mixed while adding a small amount of the other. The crude dispersion and water and the like may be simply mixed. As a method of mixing the crude dispersion with water or the like, for example, a method of mixing by stirring is mentioned.
The mixing ratio of the crude dispersion and water or the like is not particularly limited. The ratio (mass basis) of the coarse dispersion liquid to water or the like is preferably 1/20 to 10/1, more preferably 1/10 to 5/1, and even more preferably 1/2 to 2/1, from the viewpoint of the fine particles to be dispersed.
From the viewpoints of the miniaturization of the dispersed particles and the stability with time, the crude dispersion and water are preferably mixed so that the ratio of the dispersed phase to the continuous phase in the ceramide dispersion composition (mass basis) is 1/1000 to 1/5, more preferably 1/100 to 1/10, and still more preferably 1/50 to 1/10.
In view of the fine size of the dispersed particles, the dispersion treatment in the present dispersion step is preferably a high-pressure emulsification treatment.
The high-pressure emulsification treatment is a dispersion treatment in which a shearing force of 50MPa or more is applied to the dispersion. From the viewpoint of the fine particles to be dispersed, the shearing force applied to the object to be dispersed is preferably 100MPa or more, more preferably 180MPa or more. From the viewpoints of temperature rise and pressure resistance, the upper limit of the shear force applied to the dispersion is 300MPa or less in a commercially available apparatus.
The method of the high-pressure emulsification treatment is not particularly limited, and a general high-pressure emulsification apparatus is used. Examples of the high-pressure emulsifying device include ULTIMIZER HJP-25005 (manufactured by SUGINO MACHINE LIMITED), a microfluidizer (manufactured by MICROFLUIDICS INTERNATIONAL CORP.), a nanosize machine (manufactured by yoshida kikai co., ltd.), a Gaulin type homogenizer (manufactured by APV Co.), a Lanier type homogenizer (manufactured by Lanier Co., ltd.), a high-pressure homogenizer (manufactured by Nirosoavi Co., ltd.), a homogenizer (manufactured by SANWA MACHINERY TRADING CO., LTD.), a high-pressure homogenizer (manufactured by IZUMIFOOD MACHINERY CO., LTD.), and an ultra-high-pressure homogenizer (manufactured by IKA-Werke GmbH & Co.KG.).
The temperature during the high-pressure emulsification treatment is preferably set to 20 to 80 ℃, more preferably 40 to 70 ℃.
The number of times of performing the high-pressure emulsification treatment may be 1. In order to improve the uniformity of the entire solution, the high-pressure emulsification treatment is preferably performed 2 times or more, more preferably 2 to 5 times. From the viewpoint of maintaining the particle diameter of the dispersed particles, it is preferable that the emulsified composition, that is, the emulsion, is cooled by an optional cooler within 30 seconds, preferably within 3 seconds, of immediately passing through the chamber.
The dispersion treatment in the present dispersion step may be ultrasonic dispersion treatment. From the viewpoint of improving the dispersion effect, it is preferable to perform ultrasonic dispersion treatment after mixing the crude dispersion with water or the like and before the high-pressure emulsification treatment. A general ultrasonic dispersing device can be used for the dispersion treatment based on the application of ultrasonic waves.
Examples of the ultrasonic dispersing device include ultrasonic homogenizers US-600, US-1200-T, RUS-1200-T, MUS-1200T (manufactured by NISSEI corporation, supra), ultrasonic processors UIP2000, UIP4000, UIP8000, UIP16000 (manufactured by Hielscher Ultrasonics GmbH, supra), and the like. These ultrasonic dispersing devices can use frequencies of 25kHz or less, preferably 15kHz to 20 kHz.
< other procedures >
In addition to the above-described pre-dispersion treatment step and main dispersion treatment step, other steps may be included as necessary. Other steps include a heat sterilization step and the like.
Although the average particle diameter of the dispersed particles can be smaller than 60nm (theoretical value), the technical scheme is long in process flow, equipment required by the process is high-energy-consumption equipment, related equipment such as a high-pressure emulsifying machine and the like, and the ultrahigh energy consumption requirement during operation does not meet the general recognition requirement of energy conservation and emission reduction. Further, according to the present inventors' searches, no technology has been found in the disclosed patent that can prepare sphingosine and its derivatives as stable and translucent to transparent aqueous solutions.
Disclosure of Invention
In order to solve the problems, the application provides semitransparent to transparent aqueous solution containing sphingosine and non-salt derivatives and a preparation method thereof, and the method for solving the application problem of the sphingosine and the non-salt derivatives thereof in a cosmetic system in the aqueous system is obtained, so that the sufficient addition of active substances is ensured, stable and non-layered products are obtained, and the preparation is convenient, the process adaptability is strong, the equipment requirement is simple, the material cost is lower, and the mass production is more convenient.
In order to achieve the above purpose, the present application provides the following technical solutions:
in a first aspect, the present application provides a semitransparent to transparent aqueous solution containing sphingosine and non-salt derivatives, wherein the stock solution containing sphingosine and non-salt derivatives thereof comprises the following components in percentage by mass: 0.1 to 10.0 percent of sphingosine and non-salt derivatives thereof, 0 to 15.0 percent of guerbet alcohol, 10.0 to 90.0 percent of polyalcohol, 0.1 to 15.0 percent of glycerin fatty acid ester, 0 to 15.0 percent of neutral phospholipid, 0 to 15.0 percent of sterols, 0 to 15.0 percent of amino acid surfactant, 0 to 15.0 percent of PEG-hydrogenated castor oil or PEG-glycerin fatty acid ester, 0.1 to 15.0 percent of tween series and 0 to 5 percent of PH regulator; the aqueous solution containing sphingosine and non-salt derivatives comprises a stock solution and water, wherein the stock solution is prepared from the following components: the mass ratio of water is in the range of 1:10-1:200.
Preferably, the sphingosine and its non-salt derivatives are sphingosine, phytosphingosine and 6-hydroxy sphingosine, and the sphingosine, phytosphingosine and 6-hydroxy sphingosine comprise amino alcohol with 18 carbon atoms and non-salt derivatives generated by corresponding base chains, and also comprise the general name of amino alcohols with other than 18 carbon atoms.
Preferably, the phytosphingosine and its non-salt derivatives have a general structural formula
When r1=h, it is phytosphingosine; when R1 provides a corresponding chain for other substances, the sphingosine non-salt derivative is obtained, wherein R1 is a fatty acid structure such as saturated fatty acid and unsaturated fatty acid with a C number of more than 12, galactose sulfate, phosphorylcholine, glucose, fructose, mannose structure, ethyl acetate, butyl acetate, avocado oil, grape seed oil, borage oil, katsumade oil, watermelon seed oil, shea butter, safflower seed oil and olive oil;
the general structural formula of sphingosine and its non-salt derivatives is
When r2=h, it is sphingosine; when R2 provides a corresponding chain for other substances, the sphingosine non-salt derivative is obtained, wherein R2 is a saturated fatty acid with a C number of more than 12, a fatty acid structure such as unsaturated fatty acid, galactose sulfate, phosphorylcholine, glucose, fructose, mannose structure, ethyl acetate, butyl acetate, avocado oil, grape seed oil, borage oil, south American oil vine oil, watermelon seed oil, shea butter, safflower seed oil and olive oil;
the general structural formula of the hydroxysphingosine and the non-salt derivatives thereof is generally
When r3=h, it is 6-hydroxysphingosine; when R3 provides a corresponding chain for other substances, namely the 6-hydroxy sphingosine non-salt derivative, R3 is a saturated fatty acid with the C number more than 12, a fatty acid structure such as unsaturated fatty acid, a galactose sulfate, a phosphorylcholine, a glucose, a fructose and a mannose structure.
Preferably, the guerbet alcohol is one or more of 2-hexyldecanol, 2-octyldodecanol and 2-butyloctanol.
Preferably, the glycerin fatty acid ester is one or more of monoglyceride stearate, monoglyceride oleate, diglyceride stearate and triglyceride stearate.
Preferably, the neutral phospholipid is one or more of phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol and neutral synthetic phospholipid.
Preferably, the sterols are one or more of cholesterol, phytosterols and phytosterol esters.
Preferably, the amino acid surfactant is one or more of sodium lauroyl lactylate, sodium stearoyl glutamate and disodium stearoyl glutamate.
Preferably, the PEG-hydrogenated castor oil or PEG-glycerid fatty acid ester is one or more of PEG-10 hydrogenated castor oil, PEG-100 hydrogenated castor oil, PEG-2 hydrogenated castor oil, PEG-20 hydrogenated castor oil triisostearate, PEG-200 hydrogenated castor oil, PEG-25 hydrogenated castor oil, PEG-30 hydrogenated castor oil, PEG-35 hydrogenated castor oil, PEG-40 hydrogenated castor oil, PEG-45 hydrogenated castor oil, PEG-5 hydrogenated castor oil, PEG-200 hydrogenated castor oil, PEG-60 hydrogenated castor oil, PEG-5 glycerol stearate, PEG-30 glycerol stearate, PEG-40 glycerol stearate, PEG-10 glycerol stearate, PEG-100 glycerol stearate, PEG-120 glycerol stearate, PEG-15 glycerol stearate, PEG-20 glycerol isostearate and PEG-200 glycerol stearate;
the Tween series is one or more of Tween 20, tween 40, tween 60 and Tween 80;
the polyhydric alcohol is glycol without side chains such as ethylene glycol, 1, 3-propylene glycol, 1, 4-butanediol, 1, 5-pentanediol, 1, 2-hexanediol, 1, 6-hexanediol, 1, 7-heptanediol, 1, 8-octanediol, 1, 9-nonanediol, 1, 10-dodecanediol, 1, 11-undecanediol, 1, 12-dodecanediol, 1, 13-tridecanediol, 1, 14-tetradecanediol, 1, 15-pentadecanediol, etc.; diols having a side chain such as 2-methyl-1, 8-octanediol, 2-ethyl-1, 6-hexanediol, 2-methyl-1, 3-propanediol, 3-methyl-1, 5-pentanediol, 2, 4-dimethyl-1, 5-pentanediol, 2, 4-diethyl-1, 5-pentanediol, 2-butyl-2-ethyl-1, 3-propanediol, and 2, 2-dimethyl-1, 3-propanediol; one or more of 1, 4-cyclohexanedimethanol and 2-bis (4-hydroxycyclohexyl) propane cyclic diol;
the pH regulator comprises an organic acid and/or an inorganic acid; or organic bases and/or inorganic bases.
In a second aspect, the present application also provides a method for preparing a translucent to transparent aqueous solution containing sphingosine and a non-salt derivative, comprising the steps of:
step one: heating at 60-80deg.C to co-dissolve sphingosine and its non-salt derivatives, guerbet alcohol, polyalcohol, glycerol fatty acid ester, neutral phospholipid, sterols, amino acid surfactant, PEG-hydrogenated castor oil or PEG-glycerol fatty acid ester and Tween series, filtering to obtain yellowish to yellow transparent liquid, and preparing stock solution from microemulsified drug delivery system;
step two: taking the stock solution, diluting with 10-200 times of water to obtain semitransparent or transparent liquid.
The method for solving the application problem of sphingosine and its non-salt derivatives in cosmetic system in water system can ensure sufficient addition of active substances and stable and non-layering.
The product obtained by the self-microemulsifying drug delivery system disclosed by the application is free from obvious layering, sedimentation or material accumulation after centrifugal treatment under the condition of 3.0krpm and 25 min.
The application adopts the following technical scheme: self-microemulsifying drug delivery system (Self-Microemulsifying Drug Delivery System, SMEDDS for short) is a formulation technique for enhancing solubility, stability and bioavailability of poorly water-soluble materials. It belongs to the broad category of lipid-based drug delivery systems.
SMEDDS is generally composed of three main components: oil phase, surfactant and cosurfactant. Some cosmetic ingredients have low solubility in water, which limits their absorption capacity. By using SMEDDS technology, these ingredients can be converted into self-emulsifying systems, increasing their solubility in water, thus improving their absorption properties.
Advantages of using SMEDDS include: enhanced solubility and dissolution, enhanced bioavailability, skin penetration enhancers, delivery of certain specific ingredients, potential controlled release properties.
The percutaneous action rate of the whole system is improved from the above layers, so that higher efficiency is achieved.
The self-microemulsifying drug delivery system of the application is added with sphingosine and non-salt derivatives thereof, which are as follows: sphingosine, phytosphingosine, 6-hydroxysphingosine. Sphingosine, phytosphingosine and 6-hydroxysphingosine are usually non-salt derivatives of amino alcohols having 18 carbon atoms and their corresponding base chains. However, in the present specification, "phytosphingosine", "sphingosine" and "6-hydroxysphingosine" are defined as a generic term that includes amino alcohols having a carbon number other than 18. These substances are not soluble in water, oil, and form transparent liquids within the range of conventional usage.
More specifically:
phytosphingosine: is a natural inflammation regulator for skin, has the effects of relieving and calming, desensitizing and preventing sensitization, eliminating sensitive phenomena such as skin redness, itching, pimple, desquamation and the like, enhancing skin resistance, relieving discomfort such as dryness, erythema, itching, allergy and the like caused by seasonal change or environmental change stimulation, also can deeply repair and regulate sensitive skin, and enhances the defensive capability of the skin. Can alleviate the irritation of various inflammatory factors to skin, so that the skin is quickly relieved, and the traditional Chinese medicine composition has obvious curative effect on the long-term disturbance of the skin.
The general structural formula of phytosphingosine and its non-salt derivatives is:
when r1=h, it is phytosphingosine;
r1 can also be provided by other substances with corresponding chains, commonly:
fatty acid structures such as saturated fatty acids and unsaturated fatty acids having a C number of 12 or more;
galactose, galactose sulfate, phosphorylcholine, glucose, fructose, mannose and other structures;
other: ethyl acetate, butyl acetate, avocado oil, grape seed oil, borage oil, celastrus orbiculatus oil, watermelon seed oil, shea butter, safflower seed oil, olive oil, etc. provide a chain.
More specifically, non-salt derivatives of phytosphingosine are listed below:
sphingosine: the school name 2-amino-4-octadecene-1, 3-diol is an octadecanol containing an unsaturated hydrocarbon chain. Sphingosine belongs to sphingolipids, and is one of the components of cell membrane composition.
The general structural formula of sphingosine and its non-salt derivatives is:
when r2=h, it is sphingosine;
r2 can also be provided by other materials with corresponding chains, commonly:
fatty acid structures such as saturated fatty acids and unsaturated fatty acids having a C number of 12 or more;
galactose, galactose sulfate, phosphorylcholine, glucose, fructose, mannose and other structures;
other: ethyl acetate, butyl acetate, avocado oil, grape seed oil, borage oil, celastrus orbiculatus oil, watermelon seed oil, shea butter, safflower seed oil, and olive oil.
More specifically, non-salt derivatives of sphingosine are listed below:
the general structural formula of 6-hydroxysphingosine and its non-salt derivatives is:
when r3=h, it is 6-hydroxysphingosine;
r3 can also be provided with a corresponding chain by other substances, commonly:
fatty acid structures such as saturated fatty acids and unsaturated fatty acids having a C number of 12 or more;
galactose, galactose sulfate, phosphorylcholine, glucose, fructose, mannose, and the like.
Neutral phospholipids, the phospholipids of the application are selected from the group consisting of: phosphatidylcholine (lecithin), phosphatidylethanolamine, phosphatidylinositol, neutral synthetic phospholipids, and the like. The specific molecules include: soybean lecithin (SPC), hydrogenated soybean lecithin (HSPC), didecanoyl lecithin (DDPC), dilauroyl Lecithin (DLPC), dimyristoyl lecithin (DMPC), dipalmitoyl lecithin (DPPC), distearoyl lecithin (DSPC), dioleoyl lecithin (DOPC), dityristoyl lecithin (DEPC), 1-myristoyl-2-palmitoyl lecithin (MPPC), 1-myristoyl-2-stearoyl lecithin (MSPC), 1-palmitoyl-2-myristoyl lecithin (PMPC), 1-palmitoyl-2-stearoyl lecithin (PMPC), 1-stearoyl lecithin (PSPC), 1-stearoyl-2-myristoyl lecithin (SMPC), 1-stearoyl-2-palmitoyl lecithin (SPPC), 1-myristoyl-2-oleoyl lecithin (MOPC), 1-palmitoyl-2-oleoyl lecithin (poic), 1-palmitoyl-2-oleoyl phosphatidyl (pe), stearoyl phosphatidyl (pe), distearoyl phosphatidyl-2-stearoyl phosphatidyl (pe (DPPE), distearoyl phosphatidyl pe (pe), and distearoyl phosphatidyl-2-phosphatidyl, one or more of 1-palmitoyl-2-oleoyl phosphatidylethanolamine (DLPE), 1-palmitoyl-2-oleoyl phosphatidylethanolamine (POPE) and the like.
Compared with the prior art, the semitransparent to transparent aqueous solution containing sphingosine and non-salt derivatives and the preparation method thereof have the following beneficial effects: the water solution is added with functional components with moisturizing, whitening, anti-aging and barrier repairing functions, and after the water solution is prepared by the preparation method, the obtained water solution not only can tighten skin, nourish and moisturize and improve the self-oxidation resistance of the skin, but also has the anti-allergy and soothing functions, and can quickly regulate and relieve inflammatory reaction and uncomfortable symptoms of the skin by strengthening the barrier function of the skin, repairing the cutin barrier, repairing the immune barrier and the like, so that the skin can maintain a stable healthy state. The method for solving the application problem of the sphingosine and the non-salt derivatives thereof in the cosmetic system in the water system not only ensures the sufficient addition of the active substances, but also obtains stable and non-layered products, and has the advantages of convenient preparation, strong process adaptability, simple equipment requirement, lower material cost and more convenient mass production.
These and other aspects of the application will be more readily apparent from the following description of the embodiments. It is to be understood that both the foregoing general description and the following detailed description are exemplary and explanatory only and are not restrictive of the application as claimed.
Detailed Description
The present application will be described in further detail with reference to the following examples in order to make the objects, technical solutions and advantages of the present application more apparent. It should be understood that the specific embodiments described herein are for purposes of illustration only and are not intended to limit the scope of the application.
According to the semitransparent to transparent aqueous solution containing the sphingosine and the non-salt derivatives and the preparation method, functional components with moisturizing, whitening, anti-aging and barrier repairing functions are added into the aqueous solution, and after the aqueous solution is prepared by the preparation method, the aqueous solution can tighten skin, nourish and moisturize, improve the self oxidation resistance of the skin, has the anti-allergy and soothing effects, and can quickly regulate and relieve inflammatory reaction and discomfort symptoms of the skin by strengthening the skin barrier function, repairing the cutin barrier, repairing the immune barrier and the like, so that the skin can maintain a stable health state. The method for solving the application problem of the sphingosine and the non-salt derivatives thereof in the cosmetic system in the water system not only ensures the sufficient addition of the active substances, but also obtains stable and non-layered products, and has the advantages of convenient preparation, strong process adaptability, simple equipment requirement, lower material cost and more convenient mass production.
In order to prepare a stock solution containing sphingosine and non-salt derivatives, the following components (see the following table) are required in percentage by mass:
remarks:
the "mass fraction" in the table refers to the statistical amount of the corresponding material used in combination by selecting one or more components in the range to which the material belongs.
The preparation method of the application comprises the following steps:
step one: heating at 60-80deg.C, co-dissolving sphingosine and its non-salt derivatives, guerbet alcohol, polyalcohol, glycerol fatty acid ester, neutral phospholipid, sterols, amino acid surfactant, PEG-hydrogenated castor oil or PEG-glycerol fatty acid esters, tween series, and pH regulator, filtering to obtain yellowish to yellow transparent liquid (transparent liquid when the temperature is enough, and possible to be cream after cooling), and preparing stock solution of self-microemulsifying drug delivery system;
step two: the dilution ratio of the heat stock solution and water is determined by the content of active ingredients, the range of the heat stock solution and the water can be 1:10-1:200, the temperature of the water is 25-95 ℃, and semitransparent or transparent water solution can be obtained.
The operation of the second step does not need to use high-pressure homogenizing, micro-jet and other high-pressure energy-consumption equipment, and the stock solution and the water can be mixed to obtain semitransparent to transparent water solution only by a conventional mixing stirrer and an emulsifying machine, so that the water solution has time stability.
The water used in diluting the stock solution includes, but is not limited to: ion water, pure water, ultrapure water, sterilized water for injection, etc., and transparent water solution which is soluble in the above water-type materials is contained therein.
The pH range from semitransparent to transparent water solution is kept between 5 and 7.
The pH regulator comprises an organic acid and/or an inorganic acid; or organic bases and/or inorganic bases.
In particular, embodiments of the present application are further described.
Examples 1 to 7 below illustrate specific embodiments of transparent stock solutions containing sphingosine and non-salt derivatives thereof:
the materials and mass fractions added in example 1 are as follows:
| selected material | Mass fraction |
| Ceramide NP | 3.0％ |
| Phytosphingosine | 1.0％ |
| 2-hexyldecanol | 3.0％ |
| 1, 2-hexanediol | 62.0％ |
| Glycerol stearate | 2.0％ |
| Hydrogenated lecithin | 10％ |
| Phytosterols | 2.0％ |
| Stearoyl sodium glutamate | 4.0％ |
| PEG-20 Triglycerol isostearate | 5.0％ |
| Tween-80 | 8.0％ |
The materials and mass fractions added in example 2 are as follows:
the materials and mass fractions added in example 3 are as follows:
| selected material | Mass fraction |
| N-acetyl phytosphingosine | 2.5％ |
| 2-hexyldecanol | 3.0％ |
| 1, 2-hexanediol | 67.5％ |
| Glycerol stearate | 2.0％ |
| Hydrogenated lecithin | 5.0％ |
| Phytosterols | 2.0％ |
| Stearoyl sodium glutamate | 4.0％ |
| PEG-20 Triglycerol isostearate | 5.0％ |
| Tween-80 | 9.0％ |
The materials and mass fractions added in example 4 are as follows:
the materials and mass fractions added in example 5 are as follows:
| selected material | Mass fraction |
| Salicylyl phytosphingosine | 5.0％ |
| 2-Butyloctanol | 6.0％ |
| 1, 2-hexanediol | 62.0％ |
| Glycerol stearate | 2.0％ |
| Hydrogenated lecithin | 5.0％ |
| Phytosterols | 2.0％ |
| Stearoyl sodium glutamate | 5.0％ |
| PEG-20 Triglycerol isostearate | 5.0％ |
| Tween-80 | 8.0％ |
The materials and mass fractions added in example 6 are as follows:
| selected material | Mass fraction |
| Ceramide NG/NS | 4.0％ |
| 2-hexyldecanol | 8.0％ |
| 1, 2-hexanediol | 60.0％ |
| Glycerol stearate | 2.0％ |
| Hydrogenated lecithin | 5％ |
| Phytosterols | 2.0％ |
| Stearoyl glutamic acid disodium salt | 5.0％ |
| PEG-20 Triglycerol isostearate | 5.0％ |
| Tween-80 | 9.0％ |
The materials and mass fractions added in example 7 are as follows:
| selected material | Mass fraction |
| Ceramide NP | 4.0％ |
| Ceramide NG/NS | 0.4％ |
| Ceramide AP | 0.2％ |
| Salicylyl phytosphingosine | 0.2％ |
| Phytosphingosine | 0.2％ |
| 2-hexyldecanol | 3.0％ |
| 1, 2-hexanediol | 63.0％ |
| Glycerol stearate | 2.0％ |
| Hydrogenated lecithin | 5.0％ |
| Phytosterols | 2.0％ |
| Stearoyl sodium glutamate | 5.0％ |
| PEG-20 Triglycerol isostearate | 5.0％ |
| Tween-80 | 10.0％ |
In the following examples of the stock solution dilution schemes obtained in examples 8 to 14, the stock solutions and the creams of 1 to 7 in Table 1 should be heated to about 60 ℃ during operation to make the stock solutions and the creams light yellow transparent liquid, deionized water is added according to a certain proportion, and stirring is carried out by stirring paddles and magnetic force, so that the stock solutions and the creams are obtained by stirring:
example 8
| Selected material | Mass fraction |
| The hot stock solution obtained in example 1 | 1％～5％ |
| Deionized water | 95％～99％ |
Example 9
| Selected material | Mass fraction |
| The hot stock solution obtained in example 2 | 1％～5％ |
| Deionized water | 95％～99％ |
Example 10
| Selected material | Mass fraction |
| The hot stock solution obtained in example 3 | 1％～5％ |
| Deionized water | 95％～99％ |
Example 11
| Selected material | Mass fraction |
| The hot stock solution obtained in example 4 | 1％～5％ |
| Deionized water | 95％～99％ |
Example 12
| Selected material | Mass fraction |
| The hot stock solution obtained in example 5 | 1％～5％ |
| Deionized water | 95％～99％ |
Example 13
| Selected material | Mass fraction |
| The hot stock solution obtained in example 6 | 1％～5％ |
| Deionized water | 95％～99％ |
Example 14
| Selected material | Mass fraction |
| The hot stock solution obtained in example 7 | 1％～5％ |
| Deionized water | 95％～99％ |
The following summarizes the tables for stock solution examples 1-7:
the following is a summary table of diluent examples 8-14:
/>
remarks in the above table:
whether the content of the active substances reaches the standard or not means that: on the premise of ensuring the stability of the system, whether the active ingredients can be added in a quality-guaranteeing and quality-guaranteeing manner or not can be ensured;
transmittance refers to: the light transmittance of the product obtained in the embodiment is not less than 80% by using a spectrophotometer, and the stability of the system can be maintained after the product is placed for more than four weeks;
heat resistance means: at 40 ℃ for more than four weeks, the transparent liquid can be obtained after the water is added for dilution, and the content of active ingredients is still stable;
cold resistance means: at the temperature of 18 ℃ below zero, after re-dissolving at room temperature and heating to a transparent liquid, the transparent liquid can be obtained after dilution by adding water, and the content of active ingredients is still stable;
centrifugation parameters: 2krpm,30min;
"v" means: under the corresponding conditions, the material can also keep the stable and transparent state of the final diluted water solution at normal temperature after rewarming;
"X" means: under the corresponding conditions, the materials are unstable.
The conclusions of the implementation of examples 1-7 are summarized as follows: in the material selection range set forth in the application, corresponding materials are added according to the proportion designed by the application, so that a semitransparent to transparent product or a milk or paste product can be prepared finally, and the stability of the product can be effectively maintained.
More examples 8-14 illustrate that the products obtained in the examples 1-7 are heated to be transparent, and then deionized water is added to dilute the products to obtain aqueous solution with light transmittance not less than 80%, so that the subsequent application of the products related to the application is greatly facilitated, and the purposes of simple process, energy conservation, emission reduction, strong applicability and wide application range are achieved.
The above is only a preferred embodiment of the present application, and the preferred embodiments listed in the present application can also be derived from the material ratios, and all the formulation systems derived from the material ranges and the concept of the compatibility system provided in the present patent are included in the application scope of the present patent.
Claims (10)
1. The semitransparent to transparent aqueous solution containing sphingosine and non-salt derivatives is characterized in that the stock solution containing sphingosine and non-salt derivatives thereof comprises the following components in percentage by mass: 0.1 to 10.0 percent of sphingosine and non-salt derivatives thereof, 0 to 15.0 percent of guerbet alcohol, 10.0 to 90.0 percent of polyalcohol, 0.1 to 15.0 percent of glycerin fatty acid ester, 0 to 15.0 percent of neutral phospholipid, 0 to 15.0 percent of sterols, 0 to 15.0 percent of amino acid surfactant, 0 to 15.0 percent of PEG-hydrogenated castor oil or PEG-glycerin fatty acid ester, 0.1 to 15.0 percent of tween series and 0 to 5 percent of PH regulator; the aqueous solution containing sphingosine and non-salt derivatives comprises a stock solution and water, wherein the stock solution is prepared from the following components: the mass ratio of water is in the range of 1:10-1:200.
2. The translucent to transparent aqueous solution containing sphingosine and non-salt derivatives according to claim 1, wherein the sphingosine and the non-salt derivatives thereof are sphingosine, phytosphingosine and 6-hydroxysphingosine, and the sphingosine, phytosphingosine and 6-hydroxysphingosine include amino alcohols having 18 carbon atoms and non-salt derivatives thereof generated from the corresponding base chain, and further include a generic term for amino alcohols having not 18 carbon atoms.
3. The translucent to transparent aqueous solution according to claim 1, wherein said phytosphingosine and its non-salt derivatives have the general structural formula
When r1=h, it is phytosphingosine; when R1 provides a corresponding chain for other substances, the sphingosine non-salt derivative is obtained, wherein R1 is a fatty acid structure such as saturated fatty acid and unsaturated fatty acid with a C number of more than 12, galactose sulfate, phosphorylcholine, glucose, fructose, mannose structure, ethyl acetate, butyl acetate, avocado oil, grape seed oil, borage oil, katsumade oil, watermelon seed oil, shea butter, safflower seed oil and olive oil;
the general structural formula of sphingosine and its non-salt derivatives is
When r2=h, it is sphingosine; when R2 provides a corresponding chain for other substances, the sphingosine non-salt derivative is obtained, wherein R2 is a saturated fatty acid with a C number of more than 12, a fatty acid structure such as unsaturated fatty acid, galactose sulfate, phosphorylcholine, glucose, fructose, mannose structure, ethyl acetate, butyl acetate, avocado oil, grape seed oil, borage oil, south American oil vine oil, watermelon seed oil, shea butter, safflower seed oil and olive oil;
the general structural formula of 6-hydroxy sphingosine and its non-salt derivatives is
When r3=h, it is 6-hydroxysphingosine; when R3 provides a corresponding chain for other substances, namely the 6-hydroxy sphingosine non-salt derivative, R3 is a saturated fatty acid with the C number more than 12, a fatty acid structure such as unsaturated fatty acid, a galactose sulfate, a phosphorylcholine, a glucose, a fructose and a mannose structure.
4. The translucent to transparent aqueous solution containing sphingosine and non-salt derivatives according to claim 1, wherein the guerbet alcohol is one or more of 2-hexyldecanol, 2-octyldodecanol, 2-butyloctanol.
5. The translucent to transparent aqueous solution containing sphingosine and non-salt derivatives according to claim 1, wherein the glycerin fatty acid ester is one or more of monoglyceride stearate, monoglyceride oleate, diglyceride stearate, and triglyceride stearate.
6. The translucent to transparent aqueous solution containing sphingosine and non-salt derivatives according to claim 1, wherein the neutral phospholipids are one or more of phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, neutral synthetic phospholipids.
7. The translucent to transparent aqueous solution containing sphingosine and non-salt derivatives according to claim 1, wherein the sterols are one or more of cholesterol, phytosterols and phytosterol esters.
8. The translucent to transparent aqueous solution containing sphingosine and non-salt derivatives according to claim 1, wherein the amino acid surfactant is one or more of sodium lauroyl lactylate, sodium stearoyl glutamate, disodium stearoyl glutamate.
9. The translucent to transparent aqueous solution containing sphingosine and non-salt derivatives according to claim 1, wherein the PEG-hydrogenated castor oil or PEG-glyceric fatty acid ester is one or more of PEG-10 hydrogenated castor oil, PEG-100 hydrogenated castor oil, PEG-2 hydrogenated castor oil, PEG-20 hydrogenated castor oil triisostearate, PEG-200 hydrogenated castor oil, PEG-25 hydrogenated castor oil, PEG-30 hydrogenated castor oil, PEG-35 hydrogenated castor oil, PEG-40 hydrogenated castor oil, PEG-45 hydrogenated castor oil, PEG-5 hydrogenated castor oil, PEG-200 hydrogenated castor oil, PEG-60 hydrogenated castor oil, PEG-5 glycerol stearate, PEG-30 glycerol stearate, PEG-40 glycerol stearate, PEG-10 glycerol stearate, PEG-100 glycerol stearate, PEG-120 glycerol stearate, PEG-15 glycerol stearate, PEG-20 glycerol isostearate, PEG-200 glycerol stearate;
the Tween series is one or more of Tween 20, tween 40, tween 60 and Tween 80;
the polyhydric alcohol is glycol without side chains such as ethylene glycol, 1, 3-propylene glycol, 1, 4-butanediol, 1, 5-pentanediol, 1, 2-hexanediol, 1, 6-hexanediol, 1, 7-heptanediol, 1, 8-octanediol, 1, 9-nonanediol, 1, 10-dodecanediol, 1, 11-undecanediol, 1, 12-dodecanediol, 1, 13-tridecanediol, 1, 14-tetradecanediol, 1, 15-pentadecanediol, etc.; diols having a side chain such as 2-methyl-1, 8-octanediol, 2-ethyl-1, 6-hexanediol, 2-methyl-1, 3-propanediol, 3-methyl-1, 5-pentanediol, 2, 4-dimethyl-1, 5-pentanediol, 2, 4-diethyl-1, 5-pentanediol, 2-butyl-2-ethyl-1, 3-propanediol, and 2, 2-dimethyl-1, 3-propanediol; one or more of 1, 4-cyclohexanedimethanol and 2-bis (4-hydroxycyclohexyl) propane cyclic diol;
the pH regulator comprises an organic acid and/or an inorganic acid; or organic bases and/or inorganic bases.
10. A process for the preparation of a translucent to transparent aqueous solution containing sphingosine and non-salt derivatives according to claim 1, comprising the steps of:
step one: heating at 60-80deg.C, co-dissolving sphingosine and its non-salt derivatives, guerbet alcohol, polyalcohol, glycerol fatty acid ester, neutral phospholipid, sterols, amino acid surfactant, PEG-hydrogenated castor oil or PEG-glycerol fatty acid esters, tween series, and pH regulator, filtering to obtain yellowish to yellow transparent liquid (transparent liquid when the temperature is enough, and possible to be cream after cooling), and preparing stock solution of self-microemulsifying drug delivery system;
step two: the dilution ratio of the heat stock solution and water is determined by the content of active ingredients, the range of the heat stock solution and the water can be 1:10-1:200, the temperature of the water is 25-95 ℃, and semitransparent or transparent water solution can be obtained.
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