JP5717317B2 - 化合物の医薬品的使用 - Google Patents
化合物の医薬品的使用 Download PDFInfo
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- JP5717317B2 JP5717317B2 JP2008539185A JP2008539185A JP5717317B2 JP 5717317 B2 JP5717317 B2 JP 5717317B2 JP 2008539185 A JP2008539185 A JP 2008539185A JP 2008539185 A JP2008539185 A JP 2008539185A JP 5717317 B2 JP5717317 B2 JP 5717317B2
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- psidium guajava
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/61—Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/105—Plant extracts, their artificial duplicates or their derivatives
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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Description
Psidium guajavaの葉から抽出物を調製する製造プロセスは以下の工程により記述される:
−Psidium guajavaの葉を細かい粉末に粉砕する
−エタノールで抽出する
−抽出液を減圧し、エタノールが蒸発するまで濃縮する
−遠心により不溶性の不純物を除去し、浄化された液体を得る
−浄化された液体をマクロ多孔性樹脂を充填したクロマトグラフィーのカラムにロードし、水によりさらに不純物を取り除き、その後エタノールにより脱着してエタノール性溶出液を集める
−抽出液を乾燥させ、Psidium guajava抽出物を得る。
細かく砕いた原料(生のPsidium guajavaの果実)500gが計量され、80%エタノール2000mL中に移される(三口丸底フラスコ)。混合物は60℃にて2時間穏やかに混合される。溶液をろ過する。ろ液を集め、同様の条件下、80%エタノール2000mLを用いて抽出を繰り返す。溶液は再びろ過され、両方のろ液を合わせる。
粉砕されたPsidium guajavaの葉の粉末20kgが計量されて250Lのボイラーに入れられ、その後80%エタノール160Lが添加され、混合物は60℃にて2時間混合される。溶液がろ過され、再び80%エタノール160Lが残渣に注がれる。混合物はさらに60℃にて2時間抽出、ろ過され、その後二つの抽出工程のろ液は一緒に混合される。60℃減圧下でエタノールがほとんどなくなるまで、得られた混合物は濃縮される。真空度は−0.09MPaである。得られた混合物は遠心される。遠心後、水40Lを使用して残渣を洗浄し、ろ液は一緒に混合される。合わせられたろ液は、マクロクロスリンクしたマクロ多孔性樹脂(Type Amberlite XAD4)を通して分離される。まず、水160Lを用いて吸着後の樹脂が洗浄され、それにより不純物の一部を取り除くことができる。次に80%エタノール350Lが脱着工程のために使用される。黄褐色の脱着された液体が集められる。脱着された液体は、60℃減圧下で濃縮される。その後、真空乾燥機中で5時間乾燥される。
方法:
DP−IVの活性は、比色分析によって測定された。
実施例3に従って得られたPsidium guajava抽出物は、攪拌条件下、45℃で24時間、蒸留水に抽出された。その後、抽出物は、遠心(15000rpm、15分)、ろ過(シリンジフィルター、0.45μM)により浄化され、適切に希釈されて試験アッセイにかけられた。
結果は、阻害剤を加えていない試料において得られた試験結果を、阻害剤またはPsidium guajava抽出物(どちらも濃度をふって)を加えた試料において得られた試験結果と比較して得られた%阻害として表される。
アッセイはよく知られた通常の手順を用いて、較正された。
以下において別段の指示がない限り、使用した原料および方法は、実施例4の原料および方法と同じであった。
グアヤベリンはHEPESバッファーに溶解され(20分。超音波処理に続いて室温にて2時間振とう)、適切に希釈されて試験アッセイにかけられた。希釈液はHEPESバッファーの添加により調製された。試験された濃度は、70から280μg/mL試験アッセイの間であった。
結果は、陽性対照試料(阻害剤なし)において得られた試験結果を、グアヤベリンを異なる濃度で加えた試料において得られた試験結果と比較して得られた%活性として表される。
図3および4に示されるように、グアヤベリンは、DP−IVの明確な用量依存性阻害をもたらす。選択された試験アッセイシステムにおいて、140から210μg/mL試験アッセイ(100から150μg/アッセイ体積)間の濃度が、約50%のDP−IV阻害をもたらした。
Claims (3)
- グアヤベリンまたはそれらの薬学的に許容される塩またはエステルを含む、ジペプチジルペプチダーゼIV阻害剤。
- グアヤベリンを0.5重量%またはそれ以上含むことを特徴とする、請求項1に記載の阻害剤。
- グアヤベリンを10から50重量%まで含むことを特徴とする、請求項1または2に記載の阻害剤。
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AT0183305A AT502717A1 (de) | 2005-11-09 | 2005-11-09 | Pharmazeutische verwendung einer verbindung |
ATA1833/2005 | 2005-11-09 | ||
PCT/AT2006/000454 WO2007053865A1 (en) | 2005-11-09 | 2006-11-08 | Pharmaceutical use of a compound |
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JP2009514901A JP2009514901A (ja) | 2009-04-09 |
JP2009514901A5 JP2009514901A5 (ja) | 2012-12-27 |
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US (1) | US20090186110A1 (ja) |
JP (1) | JP5717317B2 (ja) |
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US20080293644A1 (en) * | 2007-04-27 | 2008-11-27 | Thomas Eidenberger | Guava extract |
JP2010105922A (ja) * | 2008-10-28 | 2010-05-13 | Uha Mikakuto Co Ltd | Lox−1アンタゴニスト作用剤 |
KR101816958B1 (ko) | 2010-12-28 | 2018-01-09 | 마리 케이 인코포레이티드 | 피지 조절 및 항여드름 조성물 |
US8877259B2 (en) | 2012-02-09 | 2014-11-04 | Mary Kay Inc. | Cosmetic formulation |
CN103565928A (zh) * | 2013-11-01 | 2014-02-12 | 华南农业大学 | 一种番石榴降糖活性组分、制备方法及用途 |
CN104173975A (zh) * | 2014-08-25 | 2014-12-03 | 河南科技大学第一附属医院 | 一种用于治疗糖尿病的中药组合物 |
MX2017011586A (es) | 2015-03-09 | 2017-10-26 | Intekrin Therapeutics Inc | Metodos para el tratamiento de enfermedad de higado graso no alcoholico y/o lipodistrofia. |
DE102016102271A1 (de) | 2016-02-10 | 2017-08-10 | Pm-International Ag | Zusammensetzung zur Reduzierung und/oder Hemmung einer intestinalen Glucose-Resorption, Nahrungsergänzungsmittel, Verwendung der Zusammensetzung und Verfahren zur Herstellung des Nahrungsergänzungsmittels |
DE102016102265A1 (de) | 2016-02-10 | 2017-08-10 | Pm-International Ag | Zusammensetzung zur Reduzierung und/oder Hemmung einer intestinalen Glucose-Resorption, Nahrungsergänzungsmittel, Verwendung der Zusammensetzung und Verfahren zur Herstellung des Nahrungsergänzungsmittels |
WO2017137405A1 (de) | 2016-02-10 | 2017-08-17 | Pm-International Ag | Zusammensetzung enthaltend guaijaverin zur reduzierung und/oder hemmung einer intestinalen glucose-resorption, nahrungsergänzungsmittel, verwendung der zusammensetzung und verfahren zur herstellung des nahrungsergänzungsmittels |
MX2019011867A (es) | 2017-04-03 | 2020-01-09 | Coherus Biosciences Inc | Agonista de ppary para el tratamiento de la paralisis supranuclear progresiva. |
WO2020025137A1 (de) * | 2018-08-02 | 2020-02-06 | Pm-International Ag | Gänseblümchenextrakt |
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US4921475A (en) * | 1983-08-18 | 1990-05-01 | Drug Delivery Systems Inc. | Transdermal drug patch with microtubes |
JPS6056923A (ja) * | 1983-09-06 | 1985-04-02 | Bizen Kasei Kk | グアバ葉エキスの抽出方法 |
JPS6137731A (ja) * | 1984-07-31 | 1986-02-22 | Bizen Kasei Kk | グアバ葉エキスを有効成分とする経口糖尿病薬 |
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JPS63283563A (ja) * | 1987-05-18 | 1988-11-21 | Morishige Okinaga | グァバ茶の製造方法 |
US5312325A (en) * | 1987-05-28 | 1994-05-17 | Drug Delivery Systems Inc | Pulsating transdermal drug delivery system |
GB8804164D0 (en) * | 1988-02-23 | 1988-03-23 | Tucker J M | Bandage for administering physiologically active compound |
US5008110A (en) * | 1988-11-10 | 1991-04-16 | The Procter & Gamble Company | Storage-stable transdermal patch |
US5088977A (en) * | 1988-12-21 | 1992-02-18 | Drug Delivery Systems Inc. | Electrical transdermal drug applicator with counteractor and method of drug delivery |
PT96059B (pt) * | 1989-12-04 | 1998-07-31 | Searle & Co | Sistema de camada unica para a administracao de um medicamento por via transdermica |
US5352456A (en) * | 1991-10-10 | 1994-10-04 | Cygnus Therapeutic Systems | Device for administering drug transdermally which provides an initial pulse of drug |
ATE132381T1 (de) * | 1992-01-29 | 1996-01-15 | Voelkl Franz Ski | Ballspielschläger, insbesondere tennisschläger |
JP3193441B2 (ja) * | 1992-03-09 | 2001-07-30 | 御木本製薬株式会社 | 美白化粧料 |
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US20060188590A1 (en) * | 2005-01-05 | 2006-08-24 | Mitsunori Ono | Compositions for treating diabetes or obesity |
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JP2009514901A (ja) | 2009-04-09 |
AT502717A1 (de) | 2007-05-15 |
WO2007053865A1 (en) | 2007-05-18 |
US20090186110A1 (en) | 2009-07-23 |
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