JP2010260856A - Gip上昇抑制剤 - Google Patents
Gip上昇抑制剤 Download PDFInfo
- Publication number
- JP2010260856A JP2010260856A JP2010089206A JP2010089206A JP2010260856A JP 2010260856 A JP2010260856 A JP 2010260856A JP 2010089206 A JP2010089206 A JP 2010089206A JP 2010089206 A JP2010089206 A JP 2010089206A JP 2010260856 A JP2010260856 A JP 2010260856A
- Authority
- JP
- Japan
- Prior art keywords
- gip
- mass
- catechins
- catechin
- gallate
- 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
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- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 description 1
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- 235000010384 tocopherol Nutrition 0.000 description 1
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- 239000011732 tocopherol Substances 0.000 description 1
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- 235000019155 vitamin A Nutrition 0.000 description 1
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- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Images
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Abstract
【解決手段】カテキン類を有効成分とするGIP上昇抑制剤。
【選択図】なし
Description
(1)カテキン類を有効成分とするGIP上昇抑制剤。
(2)カテキン類が、カテキン、カテキンガレート、ガロカテキン、ガロカテキンガレート、エピカテキン、エピガロカテキン、エピカテキンガレート、エピガロカテキンガレートのうち、一種以上の成分を含有するものである、上記(1)記載のGIP上昇抑制剤。
(3)カテキン類が、茶カテキンである、上記(1)記載のGIP上昇抑制剤。
カテキン類におけるガレート体カテキンの含有率は、GIP上昇抑制効果向上のため、カテキン類中10〜100質量%が好ましく、20〜100質量%がより好ましく、25〜100質量%が更に好ましい。
当該製茶された茶葉には、(1)煎茶、番茶、玉露、てん茶、釜煎り茶等の緑茶類、(2)総称して烏龍茶と呼ばれる鉄観音、色種、黄金桂、武夷岩茶等の半発酵茶、(3)紅茶と呼ばれるダージリン、ウバ、キーマン等の発酵茶が含まれる。
抽出助剤としては、アスコルビン酸ナトリウム等の有機酸又はこれら有機酸塩類が挙げられる。
当該茶抽出物の濃縮は、上記抽出物を濃縮することにより行うことができ、当該茶抽出物の精製は、溶剤やカラムを用いて精製することにより行うことができる。茶抽出物の濃縮物や精製物の形態としては、固体、水溶液、スラリー状等種々のものがあげられる。
例えば、当該茶抽出物は、特開昭59−219384号公報、特開平4−20589号公報、特開平5−260907号公報、特開平5−306279号公報等に詳細に例示されている方法で調製することができる。
また、呈味性を改善するため、ガレート体カテキンの含有率は、カテキン類中10〜100質量%が好ましく、より20〜90質量%、更に25〜80質量%が望ましい。なお、カテキン類中のガレート体カテキンの含有比率は、タンナーゼ処理などの方法により調整することができる(特開2007−61083号公報)。
従って、本製剤の使用目的に応じて、カテキン類単体や植物抽出物等にカフェインを添加して、あるいは植物抽出物に脱カフェイン処理を施してカフェインを低減して用いることができる。カフェインは苦味を有するため、特に飲食品においては脱カフェイン処理したカテキン類を使用する場合には、カテキン類に対しカフェインが20質量%以下、好ましくは5質量%以下、さらに好ましくは2質量%以下、特に1質量%以下にすることが望ましい。
カフェイン量を低減した茶カテキン組成物の製法としては、例えば特開2006−8580号公報、特開2006−160656号公報、特開2006−206483号公報、特開2008−79609号公報、特開2008−141987号公報などが挙げられる。
また、当該GIP上昇抑制剤等は、カテキン類を含有し、GIP分泌抑制作用等を有することをコンセプトとし、必要に応じてGIP上昇抑制;GIP上昇により症状の悪化する疾患の発症リスクの低下、予防、改善;胃酸分泌能改善、胃もたれ改善等に用いられるものである旨の表示を付した健康食品、美容食品、病者用食品、特定保健用食品、栄養機能性食品等の機能性食品の有効成分として使用できる。
投与形態としては、経口、経腸、経粘膜、注射等が挙げられる。経口投与のための剤型としては、たとえば、錠剤、被覆錠剤、カプセル剤、顆粒剤、散剤、粉剤、徐放性製剤、糖衣錠、丸剤、際粒剤等の経口用固形製剤;懸濁液、エマルジョン剤、内服液、内服液剤、シロップ剤、エリキシル剤等の経口用液体製剤等が挙げられる。
非経口投与のための剤型としては、静脈内注射剤、筋肉注射剤、吸入剤、輸液、坐剤、吸入剤、経皮吸入剤、点眼剤、点鼻剤等が挙げられる。
医薬品、たとえば錠剤、顆粒剤、カプセル剤などの経口用固形製剤中のカテキン類の含有量は、好ましくは通常0.01〜95質量%、より好ましくは5〜90質量%、さらに好ましくは20〜50質量%であり、内服液剤、シロップ剤などの経口用液体製剤中のカテキン類の含有量は、好ましくは通常0.01〜50質量%、より好ましくは0.1〜10質量%、さらに好ましくは0.1〜5質量%である。
本発明のGIP上昇抑制剤等の投与又は摂取の対象者としては、それを必要としているものであれば特に限定されないが、空腹時血中GIP値が30pg/mL以上、または胃液分泌機能検査において、基礎分泌量が30mL/時間以下のヒトは好ましい。
マウス(C57BL/6J雄、9週令)を、各群の体重の平均値が等しくなるように、対照群、茶カテキンA群の2群に分けた(各群10匹)。茶カテキンAは、緑茶(Camellia sinensis)葉熱水抽出物の乾燥粉末を熱水に溶解した後、等量のクロロホルム、3倍量のエタノールを加えて混合し水相を回収、再乾燥して調製した。絶食16時間後に、対照溶液(20質量%エタノール)を対照群に、または茶カテキンA溶液(濃度1質量%/20質量%エタノール溶液)を茶カテキンA群に、それぞれゾンデにて経口投与(カテキン類総量にして100mg/kg体重)し、連続して各群に卵製レシチン(和光純薬)(0.02g/kg体重)を用いて乳化したデンプン・コーン油混合溶液(各成分2g/kg体重)を投与した。
なお、本試験で用いた茶カテキンAの組成は、全カテキン類中、カテキン3.2%、エピカテキン9.7%、ガロカテキン6.9%、エピガロカテキン51.1%、エピカテキンガレート3.3%、ガロカテキンガレート1.2%、エピガロカテキンガレート24.4%(ガレート体組成 29.0%)だった。
投与前および、投与後経時的に眼底より採血し、血中GIP値をELISA法(Gastric Inhibitory Peptide EIA Kit,Phenix Pharmaceutical Inc.)により測定した。測定結果を図1に示す。
茶カテキンBとして、ポリフェノンHG(三井農林)水溶液を121℃、20分間加熱処理し、重曹でpH6.5に調整した後、凍結乾燥した粉末を、茶カテキンCとしてテアフラン90S(伊藤園)を用いた。
マウス(C57BL/6J雄、9週令)を、各群の体重の平均値が等しくなるように対照群、茶カテキンB群及び茶カテキンC群の3群に分けた(各群10匹)。絶食16時間後に、対照溶液(20質量%エタノール)を対照群に、茶カテキンB溶液(濃度2質量%/20質量%エタノール溶液)を茶カテキンB群に、茶カテキンC溶液(濃度2質量%/20質量%エタノール溶液)を茶カテキンC群に、それぞれゾンデにて経口投与(カテキン類総量にして200mg/kg体重)し、連続して各群に卵製レシチン(和光純薬)(0.02g/kg体重)を用いて乳化したデンプン・コーン油混合溶液(各成分4g/kg体重)を投与した。
なお、本試験で用いた茶カテキンB及びCの組成を表1に示す。
投与前および、投与10分後に眼底より採血し、血中GIP値をELISA法(Gastric Inhibitory Peptide EIA Kit,Phenix Pharmaceutical Inc.)により測定した。投与10分後の変化値(投与10分後の血中GIP値−投与前の血中GIP値)を図2に示す。
茶カテキン(エピガロカテキンガレート98%、テアビゴ(DMS Nutritional Products))45質量%、乳糖20質量%、アスコルビン酸15質量%、結晶セルロース10質量%、クエン酸7質量%、ステアリン酸マグネシウム2質量%、アスパルテーム1質量%からなる処方で、日本薬局方(製剤総則「錠剤」)に準じて錠剤を製造し、茶カテキンを含有するチュアブル錠剤を得た。
カカオ抽出物(カテキン類10%)40質量%、乳糖20質量%、アスコルビン酸15質量%、結晶セルロース10質量%、ココア粉末8質量%、果糖4質量%、ステアリン酸マグネシウム2質量%、アスパルテーム1質量からなる処方で、日本薬局方(製剤総則「錠剤」)に準じて錠剤を製造した。
茶カテキン(カテキン2%、エピカテキン10%、ガロカテキン7%、エピガロカテキン24%、カテキンガレート1%、エピカテキンガレート11%、ガロカテキンガレート4%、エピガロカテキンガレート41%)50質量%、ビタミンC 15質量%、セルロース13質量%、乳糖13質量%、コーンスターチ7質量%、トコフェロール2質量%を混合し、カプセル剤を得た。
サンフェノン(太陽化学株式会社)30質量%、果糖30質量%、ブドウ糖20質量%、脱脂粉乳10質量%、ミネラル類(Na,K,Ca,Mg,P,Cl,Fe等の有機又は無機塩混合物)8質量%、ビタミン類(ビタミンA,D,E,B1,B2,B6、B12,C,ナイアシン、パントテン酸などの混合物)2質量%を混合し、エタノールを適量加えて練和して造粒し、乾燥して顆粒剤とした。
茶カテキン(カテキン6%、エピカテキン7%、ガロカテキン21%、エピガロカテキン16%、カテキンガレート5%、エピカテキンガレート8%、ガロカテキンガレート16%、エピガロカテキンガレート21%)30質量%、リンゴ酸ナトリウム20質量%、パラチノース15質量%、アスコルビン酸15質量%、ビタミンミックス(日本香料薬品社製)5質量%、結晶セルロース5質量%、卵殻カルシウム5質量%、ショ糖エステル4質量%、二酸化ケイ素1質量%を混合し、常法によりカテキン類を含有する錠剤を調製した。
茶カテキン(カテキン3%、エピカテキン10%、ガロカテキン7%、エピガロカテキン51%、エピカテキンガレート3%、ガロカテキンガレート1%、エピガロカテキンガレート25%)25質量%、コーンスターチ 25質量%、セルロース 25質量%、乳糖 15質量%、ビタミンC 10質量%を混合し、常法により錠剤を作製した。
Claims (3)
- カテキン類を有効成分とするGIP上昇抑制剤。
- カテキン類が、カテキン、カテキンガレート、ガロカテキン、ガロカテキンガレート、エピカテキン、エピガロカテキン、エピカテキンガレート、エピガロカテキンガレートのうち、一種以上の成分を含有するものである請求項1記載のGIP上昇抑制剤。
- カテキン類が、茶カテキンである請求項1記載のGIP上昇抑制剤。
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EP (1) | EP2418208A4 (ja) |
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2018124010A1 (ja) | 2016-12-26 | 2018-07-05 | 花王株式会社 | 認知機能改善剤 |
WO2018124009A1 (ja) | 2016-12-26 | 2018-07-05 | 花王株式会社 | 低体温改善剤 |
JP2019043858A (ja) * | 2017-08-30 | 2019-03-22 | 花王株式会社 | Glp−1分泌促進剤 |
Families Citing this family (1)
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KR20190048502A (ko) * | 2017-10-31 | 2019-05-09 | (주)아모레퍼시픽 | 성분 함량이 변화된 차 추출물을 포함하는 순환기 질환 개선용 조성물 |
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- 2010-04-09 EP EP10761463.8A patent/EP2418208A4/en not_active Ceased
- 2010-04-09 CN CN201080016243.4A patent/CN102388031B/zh active Active
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2018124010A1 (ja) | 2016-12-26 | 2018-07-05 | 花王株式会社 | 認知機能改善剤 |
WO2018124009A1 (ja) | 2016-12-26 | 2018-07-05 | 花王株式会社 | 低体温改善剤 |
JP2019043858A (ja) * | 2017-08-30 | 2019-03-22 | 花王株式会社 | Glp−1分泌促進剤 |
JP7025864B2 (ja) | 2017-08-30 | 2022-02-25 | 花王株式会社 | Glp-1分泌促進剤 |
Also Published As
Publication number | Publication date |
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CN102388031B (zh) | 2014-12-17 |
JP5576694B2 (ja) | 2014-08-20 |
EP2418208A4 (en) | 2013-04-17 |
WO2010116760A1 (ja) | 2010-10-14 |
CN102388031A (zh) | 2012-03-21 |
US20120035254A1 (en) | 2012-02-09 |
EP2418208A1 (en) | 2012-02-15 |
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