JP2016505579A - クルクミン可溶化物 - Google Patents
クルクミン可溶化物 Download PDFInfo
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- JP2016505579A JP2016505579A JP2015548242A JP2015548242A JP2016505579A JP 2016505579 A JP2016505579 A JP 2016505579A JP 2015548242 A JP2015548242 A JP 2015548242A JP 2015548242 A JP2015548242 A JP 2015548242A JP 2016505579 A JP2016505579 A JP 2016505579A
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- VFLDPWHFBUODDF-FCXRPNKRSA-N curcumin Chemical compound C1=C(O)C(OC)=CC(\C=C\C(=O)CC(=O)\C=C\C=2C=C(OC)C(O)=CC=2)=C1 VFLDPWHFBUODDF-FCXRPNKRSA-N 0.000 title claims abstract description 148
- 235000012754 curcumin Nutrition 0.000 title claims abstract description 74
- 239000004148 curcumin Substances 0.000 title claims abstract description 74
- 229940109262 curcumin Drugs 0.000 title claims abstract description 73
- VFLDPWHFBUODDF-UHFFFAOYSA-N diferuloylmethane Natural products C1=C(O)C(OC)=CC(C=CC(=O)CC(=O)C=CC=2C=C(OC)C(O)=CC=2)=C1 VFLDPWHFBUODDF-UHFFFAOYSA-N 0.000 title claims abstract description 73
- 239000000203 mixture Substances 0.000 claims abstract description 17
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims abstract description 14
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims abstract description 14
- 229920000053 polysorbate 80 Polymers 0.000 claims abstract description 14
- 229940068968 polysorbate 80 Drugs 0.000 claims abstract description 14
- 229920001213 Polysorbate 20 Polymers 0.000 claims abstract description 11
- 239000000693 micelle Substances 0.000 claims abstract description 11
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims abstract description 11
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims abstract description 11
- 229940068977 polysorbate 20 Drugs 0.000 claims abstract description 10
- 239000003995 emulsifying agent Substances 0.000 claims abstract description 3
- 239000006166 lysate Substances 0.000 claims description 28
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 20
- 239000002775 capsule Substances 0.000 claims description 13
- 238000010790 dilution Methods 0.000 claims description 11
- 239000012895 dilution Substances 0.000 claims description 11
- 238000005259 measurement Methods 0.000 claims description 10
- 229930153442 Curcuminoid Natural products 0.000 claims description 8
- 239000012530 fluid Substances 0.000 claims description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
- 239000007903 gelatin capsule Substances 0.000 claims description 6
- 108010010803 Gelatin Proteins 0.000 claims description 5
- 235000013361 beverage Nutrition 0.000 claims description 5
- 239000008273 gelatin Substances 0.000 claims description 5
- 229920000159 gelatin Polymers 0.000 claims description 5
- 235000019322 gelatine Nutrition 0.000 claims description 5
- 235000011852 gelatine desserts Nutrition 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 4
- 235000013305 food Nutrition 0.000 claims description 3
- 235000011187 glycerol Nutrition 0.000 claims description 3
- 239000002537 cosmetic Substances 0.000 claims description 2
- 239000000843 powder Substances 0.000 description 17
- 238000009472 formulation Methods 0.000 description 14
- 239000000047 product Substances 0.000 description 7
- 239000007788 liquid Substances 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 239000008601 oleoresin Substances 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
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- 238000003756 stirring Methods 0.000 description 3
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- 208000005623 Carcinogenesis Diseases 0.000 description 2
- 235000014375 Curcuma Nutrition 0.000 description 2
- 244000163122 Curcuma domestica Species 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 230000002378 acidificating effect Effects 0.000 description 2
- 230000036952 cancer formation Effects 0.000 description 2
- 231100000504 carcinogenesis Toxicity 0.000 description 2
- 239000007795 chemical reaction product Substances 0.000 description 2
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- 238000010438 heat treatment Methods 0.000 description 2
- 230000004766 neurogenesis Effects 0.000 description 2
- 238000005191 phase separation Methods 0.000 description 2
- 150000003904 phospholipids Chemical class 0.000 description 2
- 238000001556 precipitation Methods 0.000 description 2
- 230000007928 solubilization Effects 0.000 description 2
- 238000005063 solubilization Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- 244000215068 Acacia senegal Species 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 240000002791 Brassica napus Species 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 229920004482 WACKER® Polymers 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 238000000149 argon plasma sintering Methods 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000009172 bursting Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 239000013065 commercial product Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 235000020241 curcumin extract Nutrition 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 239000000576 food coloring agent Substances 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 230000011164 ossification Effects 0.000 description 1
- 239000001814 pectin Substances 0.000 description 1
- 235000010987 pectin Nutrition 0.000 description 1
- 229920001277 pectin Polymers 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 230000004962 physiological condition Effects 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 229930182490 saponin Natural products 0.000 description 1
- 150000007949 saponins Chemical class 0.000 description 1
- 235000017709 saponins Nutrition 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 230000002226 simultaneous effect Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 235000013599 spices Nutrition 0.000 description 1
- 235000000891 standard diet Nutrition 0.000 description 1
- 239000008513 turmeric extract Substances 0.000 description 1
- 229940052016 turmeric extract Drugs 0.000 description 1
- 235000020240 turmeric extract Nutrition 0.000 description 1
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23D—EDIBLE OILS OR FATS, e.g. MARGARINES, SHORTENINGS, COOKING OILS
- A23D7/00—Edible oil or fat compositions containing an aqueous phase, e.g. margarines
- A23D7/005—Edible oil or fat compositions containing an aqueous phase, e.g. margarines characterised by ingredients other than fatty acid triglycerides
- A23D7/0053—Compositions other than spreads
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- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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Abstract
Description
930gのポリソルベート80及び70gの95%クルクミン粉末のみを可溶化物の作製に使用する。70g中に95%のクルクミン、すなわち66.5gのクルクミンが含有される。
894gのポリソルベート20及び106gの95%クルクミン粉末のみを可溶化物の作製に使用する。106g中に95%のクルクミン、すなわち100.7gのクルクミンが含有される。
天然形態、粉末、95%クルクミン(BCM 95)のクルクミン抽出物。12gの粉末を1リットルの水に導入した。
粉末の17.5%クルクミン微粉化物(micronisate)(Raps)。65.1gの粉末を1リットルの水に導入した。
粉末の13%クルクミン配合物(Wacker Chemie)。87.7gの粉末を1リットルの水に導入した。
実施例1に従う本発明によるクルクミン可溶化物。200gの液体可溶化物を1リットルの水に導入した。
Claims (12)
- 10重量%以下、好ましくは7.5重量%、特に好ましくは6重量%以下の量のクルクミンと、
HLB値が13〜18の範囲の少なくとも1つの乳化剤、特にポリソルベート80若しくはポリソルベート20、又はポリソルベート20とポリソルベート80との混合物と、
から構成される可溶化物であって、クルクミンを充填したミセルの平均直径が5nm〜40nm、好ましくは6nm〜20nm、特に好ましくは7nm〜10nmである、可溶化物。 - 前記ミセルの直径分布の幅がおよそ4nm〜およそ30nmの範囲であることを特徴とする、請求項1に記載の可溶化物。
- 請求項1又は2に記載の可溶化物の形態での500mgのクルクミンの経口投与の1時間後に測定されるヒト血漿中の総クルクミノイド濃度が、血漿1mL当たりおよそ500ngのクルクミノイド±血漿1mL当たり100ngのクルクミノイドであることを特徴とする、請求項1又は2に記載の可溶化物。
- 総クルクミン血漿濃度−時間曲線下面積(総クルクミン血漿濃度−時間曲線下面積AUC)として24時間にわたって測定されるヒト血漿中の総クルクミノイド濃度が、およそ9500nmol h/L〜およそ10000nmol h/Lの範囲であることを特徴とする、請求項1〜3のいずれか一項に記載の可溶化物。
- 1000倍という水中での可溶化物の希釈率でISO 7027標準の要件に準じた赤外光による散乱光測定によって決定される前記可溶化物の濁度が30FNU未満、好ましくは20FNU未満、特に好ましくは0.5FNU〜2FNUの範囲であることを特徴とする、請求項1〜4のいずれか一項に記載の可溶化物。
- 1000倍という水中での可溶化物の希釈率でISO 7027標準の要件に準じた赤外光による散乱光測定によって決定される21℃及びpH7で24時間の貯蔵後の前記可溶化物の濁度が30FNU未満、好ましくは20FNU未満、特に好ましくは0.5FNU〜2FNUの範囲であることを特徴とする、請求項1〜5のいずれか一項に記載の可溶化物。
- 1000倍という水中での可溶化物の希釈率でISO 7027標準の要件に準じた赤外光による散乱光測定によって決定される37℃及びpH1.1で1時間の貯蔵後の前記可溶化物の濁度が30FNU未満、好ましくは20FNU未満、特に好ましくは0.5FNU〜2FNUの範囲であることを特徴とする、請求項1〜5のいずれか一項に記載の可溶化物。
- 最大5重量%の水を含有することを特徴とする、請求項1〜7のいずれか一項に記載の可溶化物。
- 12重量%〜20重量%のグリセリンを含有することを特徴とする、請求項1〜8のいずれか一項に記載の可溶化物。
- 請求項1〜9のいずれか一項に記載の可溶化物を充填したカプセルであって、ソフトゼラチンカプセル若しくはハードゼラチンカプセル、又はソフトゼラチンフリーカプセル若しくはハードゼラチンフリーカプセルとして形成されることを特徴とする、カプセル。
- 請求項1〜10のいずれか一項に記載の可溶化物を含有する流体であって、食品、飲料、化粧品及び医薬品を含む群から選択されることを特徴とする、流体。
- 前記可溶化物の水性希釈物を含むことを特徴とする、請求項11に記載の流体。
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DE202012012130.8U DE202012012130U1 (de) | 2012-12-19 | 2012-12-19 | Curcuminsolubilisat |
PCT/EP2013/001427 WO2014094921A1 (de) | 2012-12-19 | 2013-05-15 | Curcuminsolubilisat |
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JP2020529974A (ja) * | 2017-07-11 | 2020-10-15 | アクアノヴァ アクチエンゲゼルシャフト | クルクミンと、任意選択で少なくとも1つの他の活性物質とを有する可溶化物 |
JP2021524488A (ja) * | 2018-07-11 | 2021-09-13 | アクアノヴァ アクチエンゲゼルシャフト | クルクミンと、更なる活性剤としての少なくともカンナビノイドthcとを含む可溶化物 |
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RU2615815C2 (ru) | 2017-04-11 |
US20220202713A1 (en) | 2022-06-30 |
CY1118432T1 (el) | 2017-06-28 |
WO2014094921A1 (de) | 2014-06-26 |
SI2934185T1 (sl) | 2017-02-28 |
CN104902765A (zh) | 2015-09-09 |
EP2934185A1 (de) | 2015-10-28 |
UA113573C2 (xx) | 2017-02-10 |
RU2015129577A (ru) | 2017-01-24 |
CN109330980B (zh) | 2021-12-21 |
HK1211801A1 (en) | 2016-06-03 |
US20150342881A1 (en) | 2015-12-03 |
JP6324989B2 (ja) | 2018-05-16 |
PT2934185T (pt) | 2017-01-18 |
US11311483B2 (en) | 2022-04-26 |
KR20180007005A (ko) | 2018-01-19 |
MY175753A (en) | 2020-07-08 |
PL2934185T3 (pl) | 2017-07-31 |
KR101983332B1 (ko) | 2019-09-03 |
CN109330980A (zh) | 2019-02-15 |
ES2609504T3 (es) | 2017-04-20 |
KR20150095698A (ko) | 2015-08-21 |
US20160128939A9 (en) | 2016-05-12 |
DK2934185T3 (en) | 2017-01-23 |
EP2934185B1 (de) | 2016-10-12 |
BR112015014654A2 (pt) | 2017-07-11 |
DE202012012130U1 (de) | 2014-03-21 |
RS55490B1 (sr) | 2017-04-28 |
BR112015014654B1 (pt) | 2020-08-18 |
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