JP2018516871A - ステロール及び可溶化剤を含有するゲルカプセル - Google Patents
ステロール及び可溶化剤を含有するゲルカプセル Download PDFInfo
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- JP2018516871A JP2018516871A JP2017555341A JP2017555341A JP2018516871A JP 2018516871 A JP2018516871 A JP 2018516871A JP 2017555341 A JP2017555341 A JP 2017555341A JP 2017555341 A JP2017555341 A JP 2017555341A JP 2018516871 A JP2018516871 A JP 2018516871A
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- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
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- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
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- 239000003960 organic solvent Substances 0.000 description 1
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- 239000000249 polyoxyethylene sorbitan monopalmitate Substances 0.000 description 1
- 235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
- 239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
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- 230000000087 stabilizing effect Effects 0.000 description 1
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- 125000002328 sterol group Chemical group 0.000 description 1
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- LRBQNJMCXXYXIU-NRMVVENXSA-N tannic acid Chemical compound OC1=C(O)C(O)=CC(C(=O)OC=2C(=C(O)C=C(C=2)C(=O)OC[C@@H]2[C@H]([C@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)O2)OC(=O)C=2C=C(OC(=O)C=3C=C(O)C(O)=C(O)C=3)C(O)=C(O)C=2)O)=C1 LRBQNJMCXXYXIU-NRMVVENXSA-N 0.000 description 1
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
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Abstract
【選択図】なし
Description
ゲルカプセルのためのフィラー材料として働く全配合物に対して、例えば、60、61、62、63、64、66、67、68、69、71、72、73、74、76、77、78、79、81、82、83、84、86、87、89、90重量パーセントなどの、少なくとも60、65重量パーセント又は好ましくは少なくとも70重量パーセント、特に好ましくは少なくとも75重量パーセント、とりわけ好ましくは少なくとも80重量パーセント、例えば、特に好ましくは少なくとも85重量パーセント又はさらに少なくとも88重量パーセント。
レシチン並びにレシチン画分及びリン脂質を含む混合物の場合。それぞれの場合において、ゲルカプセルのためのフィラー材料として働く全配合物に対して、例えば、1.5、1.6、1.7、1.8、1.9、2.0、2.1、2.2、2.3、2.4、2.5、2.6、2.7、2.8、2.9、3.0、3.5、4.0、4.5、5.0重量パーセント及びその間の全ての値などの、下限として、少なくとも1重量パーセント、好ましくは少なくとも1.1重量パーセント、特に好ましくは少なくとも1.2重量パーセント、とりわけ好ましくは、少なくとも1.3重量パーセント及び特に少なくとも1.4重量パーセント、並びに上限として、20重量パーセントまで、好ましくは15まで、特に好ましくは10まで及び特に好ましくは5重量パーセントまで。
水は、0から25重量パーセントの量で存在できる。唯一の可溶化剤としてポリソルベートを使用する場合、使用される水の量は、ゲルカプセルのためのフィラー材料として働く全配合物に対して、0から15重量パーセント、好ましくはゼロから10重量パーセント、並びにまたこれらの端点の間の全ての値である。この文脈においては、「少量」とは、10パーセント以下、好ましくは5パーセント以下の水が配合物中に存在することを意味する。
1種又は複数の油は、全配合物に対して、好ましくは20重量パーセント以下、特に好ましくは15重量パーセント以下、とりわけ好ましくは10重量パーセント以下及び特に好ましくは5重量パーセント以下であるが、0から25重量パーセントの量で存在できる。「少量」とは、10パーセント以下、好ましくは5パーセント以下の油が配合物中に存在することを意味する。
フィトステロールエステル及び乳化剤を合わせ、結晶化を避けるために、及び/又は好ましくは、粘性を低下させるために、60℃まで加熱した。その後、混合を実行した(1分間2000rpmでThinkyミキサーARE-250(Thinky Corporation、USA)、又は約30分間2000rpmでUltra-Turraxチューブドライブ(IKA、Germany)において)。全ての投入材料が液体として存在する場合、Thinkyミキサーを使用したが、その一方で、投入材料の少なくとも1つが、半流動性又は固体物質として存在し、液体フィトステロールエステル相又は約60℃で液化したフィトステロールエステル相に容易に溶解しなかった(例えば、タンパク質、パルミチン酸アスコルビル)場合、Ultra-Turraxミキサーを使用した。製造の間にいずれかの可能な発泡をさせて、一晩で(すなわち、約8から12時間後に)溶解させるために、配合物を室温(約20から25℃)とし、相分離について試験した。相分離が明白でなかった場合、下に記載された適用試験を実行した。
人工胃液
1M塩酸2gを蒸留水900mlに加え、1M塩酸でpHを1.6に調整し、蒸留水を使用して、1リットルとした。
0.42gのNaOHフレーク、3.95gのNaH2PO4 *H2O及び6.19gのNaClを蒸留水900mlに溶解させた。水酸化ナトリウム溶液でpHを6.5に調整し、蒸留水を使用して、溶液を1リットルとした。
均一な液体相を得るために、フィトステロールエステル/乳化剤配合物を約60℃まで加熱した。次に、胃液100ml及び小腸液100mlを37〜38℃までそれぞれ加熱し、配合物1gをそれぞれの場合において加えた。系を、1時間200rpmで撹拌し、次に、目視検査した。
配合物を、いわゆるCaco2モデルにおいて同様に試験した。これは、Caco2細胞中へのコレステロールの取り込みに対する配合物の投与の効果を試験することに関する。これは、配合物中のステロールエステルが、細胞のコレステロールの取り込みを減らすことができるかどうか、及びどのようにうまく減らすことができるかという尺度である。コレステロール取り込みの阻止が高ければ高いほど(すなわち、コレステロール取り込みが低ければ低いほど)、配合物は有効である。
多孔質膜上でのCaco2細胞の培養;栄養分(この場合、コレステロール)を、頂端側で取り込み、基底側で分泌する、細胞の分極構造。コレステロールの輸送が、フィトステロールをさまざまな媒介物と組み合わせて同時補給することによって影響を受ける度合いを試験する。
細胞の培養、いわゆる混合ミセルの生成、細胞毒性の判定及び作用濃度の判定、2通過(passes)における基底区画中のコレステロール濃度の測定(補給の開始後、6及び24時間)、それぞれの場合において3連で測定。
細胞の機能障害なく、全ての試験物質の150μg/mlの濃度を使用することが可能であった。作用濃度50、100、150μg/mlを選択した。
BASF SEからのVegapure 95 Eは、抗酸化剤として、少量のさまざまなトコフェロール及びパルミチン酸アスコルビルを含む。ステロールエステルの割合:少なくとも97%(面積百分率)、遊離ステロールの割合:6%まで(面積百分率)。
- ポリソルベート20:ポリオキシエチレン(20)ソルビタンモノラウレート、E432
- ポリソルベート80:ポリオキシエチレン(20)ソルビタンモノオレエート、E433、「Tween 80」
- Lipoid P 75:ダイズ豆からのレシチン画分及びリン脂質は、約75%のホスファチジルコリン、7%のホスファチジルエタノールアミンを含む。
- Prefera SSL 6000:100から140のエステル化度を有するステアロイル乳酸ナトリウム(sodium stearoyl-2-lactylate)
- Lametop P 65:FDA規格DATEM(DATEM=モノ-及びジグリセリドのジアセチル酒石酸エステル)、E472e
- Phosal 40 IP:約40パーセントのダイズ豆ホスファチジルコリン及びヒマワリ油及びまた混合トコフェロールを含む液体組成物
- MCT:中鎖トリグリセリド、C8からC10の脂肪酸を優勢に含む油
- Lecico SUN FM 580:Lecicoからのヒマワリレシチン、液体、酵素変性ヒマワリレシチン、56% AU
- CholestOff:NatureMade、USAからの市販の比較製品、植物ステロール及びスタノールを含む。
表1(1a及びb):試験した配合物-組成物
図1:(適用された開始濃度の%での)6時間後の基本受容培地のコレステロール含有量
図2:(適用された開始濃度の%での)24時間後の基本受容培地のコレステロール含有量
図3:単独の及び試験される配合物と組み合わせた、コレステロール(「CHOL」)のミセル溶液の赤外線スペクトル
図4:単独の及びさまざまな試験物質(C1からC10)と組み合わせた、コレステロール(「CHOL」)のミセル溶液のPCA分析
図5:表4に関する結果
表2:個別の物質としてのVegapure 95Eと比較した、フィトステロール-媒介物との組合せによるコレステロールの輸送の影響
表3:Caco2モデルからのさらなる結果
表4:胃モデルにおける試験の結果(「ステロールエステル」=BASFからのVegapure 95 E)
コレステロール及びフィトステロールは、水にあまり溶けず、混合ミセル中の脂肪酸及び胆汁酸塩と一緒に体内で輸送される。
結果:Lipoid P75+水を含む配合物は、純粋なコレステロールミセルと最も明確に異なり、Vegapure 95 E、ポリソルベート80、Lametop P65+MCT及びPrefera SSL 6000が続き、これを、ミセルからのコレステロールの置換の尺度として見ることができる。
表4に関する評価:視覚的評価:スケール
1=均質、表面に油がない
2=表面に小から中程度の油滴を有し、ほとんど均質
3=中程度の濁度、表面に目立つ油層
4=わずかに白っぽく濁った外観、表面に厚い油層
5=乳化効果なし、すなわち、事実上、完全な相分離
Claims (15)
- ステロールエステル及び可溶化剤を実質的に含む、ゲルカプセルのための配合物。
- ステロールエステルが、植物由来のステロール(フィトステロール)又はその水素化類似体、スタノールから得られた、請求項1に記載の配合物。
- ステロールエステルが、ステロールから得られた、請求項2に記載の配合物。
- エステル化のための脂肪酸が、天然由来、好ましくは植物又は海洋生物由来である、請求項1から3のいずれか一項に記載の配合物。
- 脂肪酸が、一価不飽和又は多価不飽和脂肪酸、好ましくは多価不飽和脂肪酸である、請求項1から4のいずれか一項に記載の配合物。
- 脂肪酸が、脂肪酸部分に対して少なくとも30重量パーセントの量で、EPA及び/又はDHAなどのオメガ3脂肪酸を含む、請求項5に記載の配合物。
- 可溶化剤として、ポリソルベート、レシチン及びステアロイル乳酸ナトリウムから選択される少なくとも1つの物質が存在する、請求項1から6のいずれか一項に記載の配合物。
- アスコルビン酸の脂肪酸エステル、イソアスコルビン酸の脂肪酸エステル、又は糖エステル中の糖として好ましくはショ糖を有する、脂肪酸の糖エステルから選択される少なくとも1つの物質が存在する、請求項7に記載の配合物。
- 脂肪酸アスコルビルエステル、好ましくはパルミチン酸アスコルビル、並びにまたレシチン及びポリソルベート、好ましくはポリソルベート80が選択される、請求項8に記載の配合物。
- ステロールエステル及び可溶化剤以外に、少量の水及び/又は油を追加的にのみ含む、請求項1から7のいずれか一項に記載の配合物。
- 請求項1から10のいずれか一項に記載の配合物を含む、ゲルカプセル。
- 軟又は硬カプセルの形態の、請求項11に記載のゲルカプセル。
- 栄養補助食品として又は医薬品として使用するための、請求項11又は12に記載のゲルカプセル。
- 請求項1から10のいずれか一項に記載の配合物を製造する方法。
- 請求項11又は12に記載のゲルカプセルを製造する方法。
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