JP2006290894A - リポソーム及びリポソーム製剤 - Google Patents
リポソーム及びリポソーム製剤 Download PDFInfo
- Publication number
- JP2006290894A JP2006290894A JP2006131001A JP2006131001A JP2006290894A JP 2006290894 A JP2006290894 A JP 2006290894A JP 2006131001 A JP2006131001 A JP 2006131001A JP 2006131001 A JP2006131001 A JP 2006131001A JP 2006290894 A JP2006290894 A JP 2006290894A
- Authority
- JP
- Japan
- Prior art keywords
- acid
- group
- liposome
- fatty acid
- general formula
- 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.)
- Granted
Links
- 239000002502 liposome Substances 0.000 title claims abstract description 94
- 238000002360 preparation method Methods 0.000 title claims description 36
- -1 20C fatty acid Chemical class 0.000 claims abstract description 106
- 150000001875 compounds Chemical class 0.000 claims abstract description 57
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 52
- 229930195729 fatty acid Natural products 0.000 claims abstract description 52
- 239000000194 fatty acid Substances 0.000 claims abstract description 52
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 28
- 125000002252 acyl group Chemical group 0.000 claims abstract description 20
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims abstract description 15
- 125000001424 substituent group Chemical group 0.000 claims abstract description 14
- 125000000524 functional group Chemical group 0.000 claims abstract description 13
- 125000001165 hydrophobic group Chemical group 0.000 claims abstract description 13
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims abstract description 5
- 150000004665 fatty acids Chemical class 0.000 claims description 29
- 150000003839 salts Chemical class 0.000 claims description 28
- 125000004432 carbon atom Chemical group C* 0.000 claims description 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 17
- 235000012000 cholesterol Nutrition 0.000 claims description 14
- 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 12
- 229910019142 PO4 Inorganic materials 0.000 claims description 11
- 229920006395 saturated elastomer Polymers 0.000 claims description 11
- 239000013543 active substance Substances 0.000 claims description 9
- 125000000217 alkyl group Chemical group 0.000 claims description 9
- 125000004122 cyclic group Chemical group 0.000 claims description 9
- 239000010452 phosphate Substances 0.000 claims description 9
- 125000000542 sulfonic acid group Chemical group 0.000 claims description 9
- 230000015572 biosynthetic process Effects 0.000 claims description 8
- 150000001841 cholesterols Chemical class 0.000 claims description 8
- 150000004671 saturated fatty acids Chemical class 0.000 claims description 8
- 235000021122 unsaturated fatty acids Nutrition 0.000 claims description 8
- 150000004670 unsaturated fatty acids Chemical class 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 239000002736 nonionic surfactant Substances 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 5
- 239000001257 hydrogen Substances 0.000 claims description 5
- 150000005215 alkyl ethers Chemical class 0.000 claims description 4
- 239000003945 anionic surfactant Substances 0.000 claims description 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 4
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 125000000539 amino acid group Chemical group 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000012528 membrane Substances 0.000 abstract description 2
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 2
- 210000002472 endoplasmic reticulum Anatomy 0.000 abstract 1
- 239000000758 substrate Substances 0.000 abstract 1
- 239000002253 acid Substances 0.000 description 56
- 229920003171 Poly (ethylene oxide) Polymers 0.000 description 40
- 239000000203 mixture Substances 0.000 description 26
- 238000004519 manufacturing process Methods 0.000 description 24
- 150000003855 acyl compounds Chemical class 0.000 description 21
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 20
- 239000000284 extract Substances 0.000 description 20
- 229940024606 amino acid Drugs 0.000 description 16
- 235000001014 amino acid Nutrition 0.000 description 16
- 238000000034 method Methods 0.000 description 15
- 150000001413 amino acids Chemical class 0.000 description 13
- 239000003921 oil Substances 0.000 description 13
- 235000019198 oils Nutrition 0.000 description 13
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 12
- 125000003277 amino group Chemical group 0.000 description 12
- 239000003795 chemical substances by application Substances 0.000 description 12
- 229920001296 polysiloxane Polymers 0.000 description 12
- 239000000843 powder Substances 0.000 description 12
- 235000000346 sugar Nutrition 0.000 description 12
- 239000010445 mica Substances 0.000 description 11
- 229910052618 mica group Inorganic materials 0.000 description 11
- 239000002202 Polyethylene glycol Substances 0.000 description 10
- 239000004744 fabric Substances 0.000 description 10
- 235000021317 phosphate Nutrition 0.000 description 10
- 229920001223 polyethylene glycol Polymers 0.000 description 10
- 125000003396 thiol group Chemical group [H]S* 0.000 description 10
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 9
- RTAQQCXQSZGOHL-UHFFFAOYSA-N Titanium Chemical compound [Ti] RTAQQCXQSZGOHL-UHFFFAOYSA-N 0.000 description 9
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 9
- 239000000126 substance Substances 0.000 description 9
- 239000010936 titanium Substances 0.000 description 9
- 229910052719 titanium Inorganic materials 0.000 description 9
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 8
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 8
- 239000004166 Lanolin Substances 0.000 description 8
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 8
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 8
- 235000019388 lanolin Nutrition 0.000 description 8
- 229940039717 lanolin Drugs 0.000 description 8
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 8
- 239000000049 pigment Substances 0.000 description 8
- 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 8
- 238000003756 stirring Methods 0.000 description 8
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 7
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 7
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 7
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 7
- 238000009472 formulation Methods 0.000 description 7
- 239000000600 sorbitol Substances 0.000 description 7
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 6
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 6
- 230000002378 acidificating effect Effects 0.000 description 6
- 239000002585 base Substances 0.000 description 6
- 150000002148 esters Chemical class 0.000 description 6
- 230000003287 optical effect Effects 0.000 description 6
- UQDJGEHQDNVPGU-UHFFFAOYSA-N serine phosphoethanolamine Chemical compound [NH3+]CCOP([O-])(=O)OCC([NH3+])C([O-])=O UQDJGEHQDNVPGU-UHFFFAOYSA-N 0.000 description 6
- 229920001214 Polysorbate 60 Polymers 0.000 description 5
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 5
- 150000001412 amines Chemical class 0.000 description 5
- 229940107161 cholesterol Drugs 0.000 description 5
- 239000003240 coconut oil Substances 0.000 description 5
- 235000019864 coconut oil Nutrition 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 5
- 229910052751 metal Inorganic materials 0.000 description 5
- 239000002184 metal Substances 0.000 description 5
- 239000002904 solvent Substances 0.000 description 5
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 5
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 4
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical class CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 4
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 4
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 4
- QFOHBWFCKVYLES-UHFFFAOYSA-N Butylparaben Chemical compound CCCCOC(=O)C1=CC=C(O)C=C1 QFOHBWFCKVYLES-UHFFFAOYSA-N 0.000 description 4
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
- 239000005639 Lauric acid Substances 0.000 description 4
- 239000004472 Lysine Substances 0.000 description 4
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 4
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 4
- 235000019482 Palm oil Nutrition 0.000 description 4
- 229920002472 Starch Polymers 0.000 description 4
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 4
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 4
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 4
- TZCXTZWJZNENPQ-UHFFFAOYSA-L barium sulfate Chemical compound [Ba+2].[O-]S([O-])(=O)=O TZCXTZWJZNENPQ-UHFFFAOYSA-L 0.000 description 4
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 description 4
- 239000004359 castor oil Substances 0.000 description 4
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- 229920002678 cellulose Polymers 0.000 description 4
- 239000001913 cellulose Substances 0.000 description 4
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- 238000006243 chemical reaction Methods 0.000 description 4
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- 239000000975 dye Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 4
- 229960002989 glutamic acid Drugs 0.000 description 4
- 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 description 4
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- 239000004615 ingredient Substances 0.000 description 4
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 4
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- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical compound OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 description 3
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- 244000027321 Lychnis chalcedonica Species 0.000 description 3
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- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
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- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical group OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 3
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- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 3
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- 229910052749 magnesium Inorganic materials 0.000 description 3
- 239000011777 magnesium Substances 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 3
- 150000002739 metals Chemical class 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 230000003020 moisturizing effect Effects 0.000 description 3
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 3
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Landscapes
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Abstract
【解決手段】 (A)疎水基と親水基とを分子内に2個以上ずつ有する多鎖多親水基型化合物の1種以上と、(B)水とを含有するリポソーム。多鎖多親水基型化合物としてはm個の官能基を有する炭化水素鎖にn(m≧n)個の下記一般式(2)で表される置換基が結合している化合物であり、nは2〜20の整数を示す。
(式中、Zは炭化水素鎖の有する官能基に由来する結合部であり、R1COは炭素原子数2〜20の脂肪酸から誘導されるアシル基を示し、R2は水素、ヒドロキシル基などを示し、Yはカルボキシル基、スルホン酸基、硫酸エステル基などを示す。j、kは0,1,2のいずれかであり、かつ同時に0ではない。)
【選択図】なし
Description
2.前記多鎖多親水基型化合物は、前記疎水基の少なくとも1種がアシル基であり、前記親水基がカルボキシル基、スルホン酸基、硫酸エステル基、リン酸エステル基またはそれらの塩から選ばれる1種以上であるアニオン性界面活性剤であることを特徴とする上記1.に記載のリポソーム。
3.前記多鎖多親水基型化合物の少なくとも1種が、分子内にさらにアミノ酸残基を有することを特徴とする上記1.または2.に記載のリポソーム。
4.前記多鎖多親水基型化合物の少なくとも1種が、下記一般式(1)に示す化合物であることを特徴とする上記1.〜3.のいずれかに記載のリポソーム。
6.前記多鎖多親水基型化合物の含有量が、0.001質量%以上50質量%以下であることを特徴とする上記1.〜5.のいずれかに記載のリポソーム。
7.(C)非イオン性界面活性剤を含有し、(C)/(A)が質量比で0.1〜50であることを特徴とする上記1.〜6.のいずれかに記載のリポソーム。
8.(D)リポソーム形成助剤を含有し、(D)/(A)が質量比で0.01〜10であることを特徴とする上記1.〜7.のいずれかに記載のリポソーム。
9.前記(D)リポソーム形成助剤が、コレステロール類、該コレステロール類の脂肪酸エステル、該コレステロール類のアルキルエーテル、脂肪酸からなる群から選ばれる1種以上であることを特徴とする上記8.に記載のリポソーム。
10.上記1.〜9.のいずれかに記載のリポソームに、(E)生理活性物質を配合したことを特徴とするリポソーム製剤。
11.上記1.〜9.のいずれかに記載のリポソーム又は上記10.に記載のリポソーム製剤を含有することを特徴とする外用剤。
(アシル化合物の製造例1)
(アシル化合物の製造例3)
[実施例1〜9、比較例1〜9]
○:調製直後にマルテーゼクロスが全体的に確認できた。
△:調製直後にマルテーゼクロスが部分的に確認できた。
×:調製直後にマルテーゼクロスが全く確認できなかった。
評価基準は以下の通りである。
○:1ヶ月後にマルテーゼクロスが全体的に確認できた。
×:1ヶ月後にマルテーゼクロスが全く確認できなかった。
成分名 質量%
製造例1のアシル化合物 0.8
コレステロール 0.4 (理研ビタミン社製、商品名:理研コレステロール)
セラミド2 0.1 (クローダジャパン社製)
クエン酸 0.1
安息香酸ナトリウム 0.1
エタノール 5.0
グリセリン 5.0
アロエエキス 1.0 (一丸ファルコス社製、商品名:アロエエキスベラ)
カミツレエキス 1.0 (一丸ファルコス社製、商品名:カミツレリキッド)
精製水 合計で100とする量
[実施例11]
成分名 質量%
製造例2のアシル化合物 1.0
ジプロピレングリコール 4.0
PEG400 5.0
エデト酸2Na 0.1
ステアリルアルコール 0.5
硬化パーム油 3.0(日清オイリオ社製、商品名:ノムコートPHS)
スクワラン 35.0(日光ケミカルス社製、商品名:NIKKOLスクワラン)
ラウリン酸 0.3
ステアリン酸 0.3
ソルビタンセスキ
オレイン酸エステル 1.5
POE(20)オレイル
アルコールエーテル 2.5
カルボマー水溶液(1%) 15.0(日光ケミカルズ社製、商品名:カーボポール934)
水酸化ナトリウム 0.1
ブチルパラベン 0.3
精製水 合計で100とする量
[実施例12]
成分名 質量%
ベヘニルアルコール 2.0(コグニスジャパン社製、商品名:ラネッテ22)
ステアリルアルコール 4.0
ステアリン酸 2.0
水添ラノリン 4.0(日本精化社製、商品名:ハードラノリン)
スクワラン 9.0(日光ケミカルス社製、商品名:NIKKOLスクワラン)
オクチルドデカノール 10.0
ビタミンE 0.1
製造例3のアシル化合物 1.2
ポリクオタニウム−51 0.2(日本油脂社製、商品名:Lipidure-PMB)
1,3ブチレングリコール 6.0
PEG1500 4.0
ビタミンC 2.0
POE(25)セチル
アルコールエーテル 3.0
モノステアリン酸グリセリン 2.0
ブチルパラベン 0.2
精製水 合計で100とする量
[実施例13]
成分名 質量%
実施例1のアシル化物 2.0
セチルアルコール 3.0
ステアリルアルコール 5.0
ベヘニルアルコール 5.0(コグニスジャパン社製、商品名:ラネッテ22)
ソルビタンモノステアレート 8.0
POE(20)ソルビタン
モノステアレート 25.0
イソステアリン酸コレステリル 6.0
ビタミンE 0.1
ビタミンA油 0.2
ビタミンD油 0.1
グリセリン 8.0
メチルパラベン 0.1
塩化ナトリウム 0.02
フィトステロール 0.1(エーザイ社製、商品名:β−シトステロール)
グリチルレチン酸 0.4
精製水 合計で100とする量
Claims (11)
- (A)疎水基と親水基とを分子内に2個以上ずつ有する多鎖多親水基型化合物の1種以上と、(B)水とを含有することを特徴とするリポソーム。
- 前記多鎖多親水基型化合物は、前記疎水基の少なくとも1種がアシル基であり、前記親水基がカルボキシル基、スルホン酸基、硫酸エステル基、リン酸エステル基またはそれらの塩から選ばれる1種以上であるアニオン性界面活性剤であることを特徴とする請求項1に記載のリポソーム。
- 前記多鎖多親水基型化合物の少なくとも1種が、分子内にさらにアミノ酸残基を有することを特徴とする請求項1または2に記載のリポソーム。
- 前記多鎖多親水基型化合物の少なくとも1種が、下記一般式(1)に示す化合物であることを特徴とする請求項1〜3のいずれかに記載のリポソーム。
- 前記Xの炭素数が、1〜40であることを特徴とする請求項4に記載のリポソーム。
- 前記多鎖多親水基型化合物の含有量が、0.001質量%以上50質量%以下であることを特徴とする請求項1〜5のいずれかに記載のリポソーム。
- (C)非イオン性界面活性剤を含有し、(C)/(A)が質量比で0.1〜50であることを特徴とする請求項1〜6のいずれかに記載のリポソーム。
- (D)リポソーム形成助剤を含有し、(D)/(A)が質量比で0.01〜10であることを特徴とする請求項1〜7のいずれかに記載のリポソーム。
- 前記(D)リポソーム形成助剤が、コレステロール類、該コレステロール類の脂肪酸エステル、該コレステロール類のアルキルエーテル、脂肪酸からなる群から選ばれる1種以上であることを特徴とする請求項8に記載のリポソーム。
- 請求項1〜9のいずれかに記載のリポソームに、(E)生理活性物質を配合したことを特徴とするリポソーム製剤。
- 請求項1〜9のいずれかに記載のリポソーム又は請求項10に記載のリポソーム製剤を含有することを特徴とする外用剤。
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