JP2020055879A - フラボノイド組成物及び使用方法 - Google Patents
フラボノイド組成物及び使用方法 Download PDFInfo
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Abstract
Description
本出願は、その開示内容の全体が参照により本明細書に組み込まれている、2015年9月23日に出願された米国仮特許出願第62/222,667号に対する優先権を主張するものである。
いくつかの実施形態において、活性成分及び活性成分の混合物は、例えば、保管及び後の投与のために調製された薬学的に許容される担体を含む治療用組成物において使用されうる。また、いくつかの実施形態は、薬学的に許容される担体又は希釈剤と合わせた上述の活性成分の使用を含む。治療用途に許容される担体又は希釈剤は薬学の技術分野で周知であり、例えば、全体が参照により本明細書に組み込まれている、Remington's Pharmaceutical Sciences、18th Ed.、Mack Publishing Co.、Easton、Pa.(1990)に記載されている。保存料、安定剤、染料、及び更には香味剤が、治療用組成物中に供給されてよい。例えば、安息香酸ナトリウム、アスコルビン酸、及びp-ヒドロキシ安息香酸のエステルが、保存料として添加されうる。加えて、抗酸化剤及び懸濁化剤が使用されてもよい。
第5,688,529号(経口懸濁液)、同第5,445,829号(持続放出製剤)、同第5,653,987号(液体製剤)、同第5,641,515号(制御放出製剤)、及び同第5,601,845号(スフェロイド製剤)を参照されたい。治療用組成物は、それ自体が公知である様式において、例えば、従来の混合、溶解、顆粒化、ドラジェ作製、浮遊、乳化、カプセル化、封入、又は凍結乾燥プロセスによって製造することができる。
いくつかの実施形態は、本開示の組成物を作製及び投与するための方法も包含する。かかる本開示の方法は、とりわけ、本開示の化合物を生体組織と接触させるために当業者が適切とみなした場合は(a)カプセル、錠剤、顆粒、スプレー、シロップ、又はそのような他の形態での投与を含む、経口経路による投与、(b)局所投与、(c)直腸投与、又は(d)経膣投与、及び(e)制御放出製剤、デポー製剤による投与を含む。そのような投与形態の更なる例として、また投与形態の更なる開示として、本明細書には、眼内経路、鼻腔内経路、及び耳介内経路による投与形態を含む、本開示の組成物の様々な投与方法が開示される。
本明細書に記載の組成物は、ケルセチンの生体利用能、吸収、分布、代謝、及び/又は排泄を向上させるために使用することができる。本明細書に記載の組成物は、血圧及びLDLコレステロールの低減のため、又は運動能力の向上のために使用されてもよい。したがって、いくつかの実施形態において、本明細書に記載の組成物は、高い血圧又は高いLDLコレステロールを有するヒトに投与される。いくつかの実施形態において、本明細書に記載の組成物は、運動能力を向上させるためにヒトに投与される。
フラボノイド咀嚼錠製剤
以下の実施例は、フラボノイドを含み、且つ咀嚼錠として製剤化された組成物の例示的な実施形態を示す。
フラボノイド錠剤製剤
以下の実施例は、フラボノイドを含み、且つ錠剤として製剤化された組成物の例示的な実施形態を示す。
フラボノイドに富んだサプリメントの摂取がヒトメタボローム及び尿中フェノール類濃度に及ぼす影響
以下の実施例は、体重過多又は肥満の対象におけるフラボノイドに富んだ組成物の摂取の効果を示す。
Claims (25)
- 咀嚼錠であって、
約7.9%〜約16%(w/w)の量で存在するケルセチン、
ビルベリー抽出物、
緑茶葉抽出物、
ビタミンC、
カフェイン、及び
オメガ3脂肪酸
を含む、咀嚼錠。 - ビタミンCが、アスコルビン酸として存在する、請求項1に記載の咀嚼錠。
- ビタミンCが、約100mgの量で存在する、請求項1に記載の咀嚼錠。
- 前記ビルベリー果実抽出物が、約25%の全アントシアニンを含む、請求項1に記載の咀嚼錠。
- 前記オメガ3脂肪酸が、N3多価不飽和脂肪酸(N3-PUFA)を含む、請求項1に記載の咀嚼錠。
- 前記N3-PUFAが、約60mgの量で存在する、請求項5に記載の咀嚼錠。
- 前記N3-PUFAが、ドコサヘキサエン酸及びエイコサペンタエン酸を含む、請求項5に記載の咀嚼錠。
- 糖、天然及び人工の香味料、セルロースガム、スクラロース、竹全植物抽出物、グアーガム、キサンタンガム、クエン酸、リンゴ酸及びL-酒石酸のうちの1つ又は複数をさらに含む、請求項1に記載の咀嚼錠。
- 前記咀嚼錠が、1日2回の2つの錠剤の用量での対象への投与のために製剤化される、請求項1に記載の咀嚼錠。
- 前記咀嚼錠が、食事中における対象への投与のために製剤化される、請求項1に記載の咀嚼錠。
- フラボノイドの生体利用能を増加させるための経口摂取可能な医薬であって、前記医薬が、
約7.9%〜約16%(w/w)の量で存在するフラボノイド、
抗酸化剤、
アントシアニジン、
刺激薬、
脂質、
アスコルビン酸、
オメガ3脂肪酸、及び
パルミチン酸アスコルビル
を含み、
前記経口摂取可能な医薬が、カプセル、咀嚼錠又はグミとして製剤化され、
前記フラボノイドの生体利用能が増加する、医薬。 - 前記フラボノイドが、約10〜500mgの範囲の量で存在する、請求項11に記載の経口摂取可能な医薬。
- 前記フラボノイドが、約100mgの量で存在する、請求項12に記載の経口摂取可能な医薬。
- 前記フラボノイドが、約52mgの量で存在する、請求項12に記載の経口摂取可能な医薬。
- フラボノイドが約10〜500mgの量で存在し、前記抗酸化剤が約10〜500mgの量で存在し、前記アントシアニジンが約10〜500mgの量で存在し、前記刺激薬が約10〜500mgの量で存在し、前記脂質が約10〜500mgの量で存在し、アスコルビン酸が約10〜500mgの量で存在し、前記オメガ3脂肪酸が約10〜500mgの量で存在し、前記パルミチン酸アスコルビルが約10〜500mgの量で存在する、請求項11に記載の経口摂取可能な医薬。
- 前記フラボノイドが約52mgの量で存在し、前記抗酸化剤が約90mgの量で存在し、前記アントシアニジンが約225mgの量で存在し、前記刺激薬が約52mgの量で存在し、前記脂質が約100mgの量で存在し、アスコルビン酸が約50mgの量で存在し、前記オメガ3脂肪酸が約100mgの量で存在し、パルミチン酸アスコルビルが約60mgの量で存在する、請求項11に記載の経口摂取可能な医薬。
- 前記経口摂取可能な医薬が、毎日2回から4回の対象への投与のために製剤化される、請求項11に記載の経口摂取可能な医薬。
- 前記経口摂取可能な医薬が、単回用量における2単位の投与のために製剤化される、請求項11に記載の経口摂取可能な医薬。
- 前記経口摂取可能な医薬が、水性炭水化物源と組み合わせた投与のために製剤化される、請求項11に記載の経口摂取可能な医薬。
- 前記経口摂取可能な医薬が、約3〜約4のpHで製剤化される、請求項11に記載の経口摂取可能な医薬。
- 電荷遮蔽化合物、可溶化化合物、還元化合物、安定化化合物、潤滑化化合物、腸溶コーティング及び透過性向上化合物からなる群から選択される生体利用能向上剤をさらに含む、請求項11に記載の経口摂取可能な医薬。
- 前記フラボノイドが、ケルセチン若しくはその誘導体、ケンフェロール、ミリセチン、イソラムネチン、ルテオリン、アピゲニン、ヘスペレチン、ナリンゲニン、エリオジクチオール、カテキン、エピガロカテキン、テアフラビン、シアニジン、デルフィニジン、マルビジン、ペラルゴニジン、ペオニジン、ペツニジン、ダイゼイン、ゲニステイン又はグリシテインである、請求項11に記載の経口摂取可能な医薬。
- 野生のビルベリー果実抽出物、緑茶葉抽出物、ケルセチンアグリコン及びオメガ3脂肪酸を含む組成物。
- 前記野生のビルベリー果実抽出物が約156mgの量で存在し、前記緑茶葉抽出物が約180mgの量で存在し、前記ケルセチンアグリコンが約100mgの量で存在し、前記オメガ3脂肪酸が約200mgの量で存在する、請求項23に記載の組成物。
- 約100mgの量で存在するビタミンC及び約100mgの量で存在するカフェインをさらに含む、請求項23に記載の組成物。
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