JP2009520020A - 胃炎または胃潰瘍の予防及び治療に有用なラカンカ抽出物及びこれから分離されたモモルディカ・サポニンi - Google Patents
胃炎または胃潰瘍の予防及び治療に有用なラカンカ抽出物及びこれから分離されたモモルディカ・サポニンi Download PDFInfo
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- JP2009520020A JP2009520020A JP2008547108A JP2008547108A JP2009520020A JP 2009520020 A JP2009520020 A JP 2009520020A JP 2008547108 A JP2008547108 A JP 2008547108A JP 2008547108 A JP2008547108 A JP 2008547108A JP 2009520020 A JP2009520020 A JP 2009520020A
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- Prior art keywords
- extract
- gastric
- gastritis
- momordica saponin
- drug
- 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.)
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
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Abstract
Description
薬草市場で購入したラカンカ1kg(乾燥重量)に5Lの50%エタノール水溶液を加え、4時間、80℃の温度を維持しながら抽出した。この過程を2度実施して生薬抽出物を獲得した。抽出液は濾過して、回転蒸発器を用いて60℃で減圧濃縮した後、真空オーブンで溶媒を完全に除去した後、粉末状のエタノール抽出物21gを獲得した。
薬草市場で購入したラカンカ1kg(乾燥重量)を破砕した後、5Lの10%エタノール水溶液を加え、3時間、80℃を維持した水浴で抽出し、この過程を2度実施した。抽出液は濾過して、回転蒸発器を用いて60℃で減圧濃縮した後、真空オーブンで溶媒を完全に除去した後、粉末状のモモルディカ・サポニンI含有抽出物35〜45gを獲得した。
有機溶媒(アセトン)を使用した沈殿法を通して、製造例2で製造された抽出物からモモルディカ・サポニンIを効率的に分離した。製造例2の抽出物10gを100mLの精製水に溶解した後、100mLのアセトンを添加して、50%(v/v)アセトン水溶液を得た。沈殿物を濾過した後、更に400mLのアセトンを濾過液に添加し、80%(v/v)アセトン水溶液を得た。新たに形成した沈殿物を濾紙を利用して分離した後、乾燥させた。
前記製造例2で製造された抽出物または製造例3で製造された分画物に対して、オクタデシルシリル化したシリカ樹脂(YMC*GEL ODS−A 12nm、S−150 m)を用いてカラムクロマトグラフィを実施した。樹脂の量は250g、または抽出物または分画物の重量の25倍であり、10%(v/v)と40%(v/v)メタノール水溶液を各々、樹脂体積の2〜3倍の量を流した後、70%(v/v)のメタノール水溶液を樹脂体積の2〜3倍の量を流し、その結果、溶出分画物を収得し、この分画物を減圧下で濃縮し、真空オーブンで溶媒を完全に除去した。
前記製造例4の70%(v/v)メタノール水溶液分画物からモモルディカ・サポニンIを分離した。アセトニトリルと水の混合溶媒(29:71、0.1%トリフルオロ酢酸)を使用して高速液体クロマトグラフィを実施した。9.5mL/分の速度で溶出させ、約45分でのサポニンピークのみを取った。この分画物を減圧下で濃縮し、真空オーブンで溶媒を完全に除去した。YMC J‘Sphere ODS−H80カラムを使用し、測定波長は210nmであった。
100%エタノールを胃損傷誘発因子として使用したラットモデル実験を行い、ラカンカ抽出物の胃粘膜の保護効能を評価した。製造例1のラカンカ抽出物を0.5%カルボキシメチルセルロース水溶液に10mg/mLの濃度で溶かして試験薬物として使用した。10mg/mLの濃度で0.5%カルボキシメチルセルロース水溶液に溶解されたスティレン(ヨモギ抽出物、東亜製薬(韓))とムコスタ(レバミピド、韓国大塚製薬)を対照薬物として使用した。
100%エタノールを胃損傷誘発因子として使用したラットモデル実験を行い、モモルディカ・サポニンIの胃粘膜の保護効能を評価した。製造例5で分離されたモモルディカ・サポニンIを0.5%カルボキシメチルセルロース水溶液に2mg/mLの濃度で溶かして試験薬物として使用した。10mg/mLの濃度で0.5%カルボキシメチルセルロース水溶液に溶解されたムコスタ(レバミピド、韓国大塚製薬)を対照薬物として使用した。
胃損傷誘発因子として代表的な非ステロイド系抗炎症薬(NSAID)であるジクロフェナクを使用してラットモデル実験を行い、製造例1のラカンカ抽出物の胃炎治療効能を評価した。
実施例3とは異なり、ジクロフェナクと試験薬物を同時に投与し、6時間後に胃粘膜の損傷程度を観察した。この時、ジクロフェナンと試験薬物と直接的な相互作用を防ぐために、試験薬物は腹腔で投与した。前記実施例3と同様に、ジクロフェナクと試験薬物は0.5%カルボキシメチルセルロース水溶液に10mg/mLの濃度で溶解した。
ジクロフェナクと試験薬物を同時に投与し、4時間後に胃粘膜の損傷程度を観察した。ジクロフェナクは0.5%カルボキシメチルセルロース水溶液に40mg/mLの濃度で溶解し、試験薬物は実施例2と同様に準備した。
モモルディカ・サポニンIが胃酸分泌に及ぼす影響を評価するために、Sprague−Dawleyラットにモモルディカ・サポニンを経口投与した後、胃の酸度を測定した。製造例4で分離されたモモルディカ・サポニンIを0.5%カルボキシメチルセルロース水溶液に0.5、1.5及び4.5mg/mLの濃度で溶解した。特定病原体未感染(SPF)の7週齢雄Sprague−Dawleyラットをチャールズ・リバーから購入し、1週間の順応期間を経た後、体重が220〜225gである健康なラットを実験で使用した。各グループ当り2匹ずつとなるように区分した後、水を自由に摂取することができる状態で18時間絶食させ、モモルディカ・サポニンIを5、15及び45mg/kgの容量で投与した。試験薬物を投与してから1時間後に、ラットにエーテルで麻酔をかけた。胃から取り出した胃液0.5mLを蒸留水で10倍に希釈して、5mLの試料を得た。希釈された胃液のpHをpHメーターで測定した。
6週齢の特定病原未感染(SPF)のSprague−Dawleyラットを使用して急性毒性実験を下記のように実施した。
6週齢の特定病原未感染(SPF)のSprague−Dawleyラットを使用して急性毒性実験を下記のように実施した。
本発明のラカンカ抽出物にて湿式顆粒法及び乾式顆粒法を経口投与用錠剤に製造した。
[組成]
ラカンカ抽出物(200mg)、硬質無水ケイ酸(10mg)、ステアリン酸マグネシウム(2mg)、微細結晶セルロース(50mg)、デンプングリコール酸ナトリウム(25mg)、コーンスターチ(113mg)、無水エタノール(適量)。
本発明のモモルディカ・サポニンIにて湿式顆粒法及び乾式顆粒法により経口投与用錠剤を製造した。
[組成]
モモルディカ・サポニンI(20mg)、硬質無水ケイ酸(10mg)、ステアリン酸マグネシウム(2mg)、微細結晶セルロース(50mg)、デンプングリコール酸ナトリウム(25mg)、コーンスターチ(113mg)、無水エタノール(適量)。
本発明のラカンカ抽出物にて軟膏剤を製造した。
[組成]
ラカンカ抽出物(5g)、パルミチン酸セチル(20g)、セタノール(40g)、ステアリル・アルコール(40g)、ミリスチン酸イソプロピル(80g)、モノステアリン酸ソルビタン(20g)、ポリソルベート(60g)、p−ヒドロキシ安息香酸プロピル(1g)、p−ヒドロキシ安息香酸メチル(1g)、リン酸及び精製水(適量)。
本発明のラカンカ抽出物にて注射剤を製造した。
[組成]
ラカンカ抽出物(100mg)、マンニトール(180mg)、二リン酸ナトリウム(25mg)、注射用水(2974mg)。
本発明のラカンカ抽出物にて経皮剤を製造した。
[組成1]
ラカンカ抽出物(0.4g)、ポリアクリル酸ナトリウム(1.3g)、グリセリン(3.6g)、水酸化アルミニウム(0.04g)、メチルパラベン(0.2g)、水(14g)。
[組成2]
ラカンカ抽出物(0.8g)、プロピレングリコール(1.6g)、流動パラフィン(0.8g)、ミリスチン酸イソプロピル(0.4g)、ジェルバー(16.4g)。
本発明のモモルディカ・サポニンIにて経皮剤を製造した。
[組成1]
モモルディカ・サポニンI(20mg)、ポリアクリル酸ナトリウム(1.3g)、グリセリン(3.6g)、水酸化アルミニウム(0.04g)、メチルパラベン(0.2g)、水(14g)。
[組成2]
モモルディカ・サポニンI(40mg)、プロピレングリコール(1.6g)、流動パラフィン(0.8g)、ミリスチン酸イソプロピル(0.4g)、ジェルバー1430(16.4g)。
Claims (5)
- ラカンカ(Momordicae semen)抽出物を有効成分として含有することを特徴とする胃炎または胃潰瘍の予防及び治療用薬剤。
- 前記ラカンカ抽出物は、ラカンカを水またはアルコール水溶液で抽出して得られることを特徴とする、請求項1記載の薬剤。
- 前記アルコールは炭素数1〜6のアルコールであることを特徴とする、請求項2記載の薬剤。
- 前記薬剤は、体重1kg当り0.05〜1mgのモモルディカ・サポニンIを含有することを特徴とする、請求項4記載の薬剤。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
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KR10-2005-0126302 | 2005-12-20 | ||
KR1020050126302A KR20070065652A (ko) | 2005-12-20 | 2005-12-20 | 위염 예방 및 치료에 유용한 목별자 추출물 |
KR10-2006-0128138 | 2006-12-14 | ||
KR1020060128138A KR101132730B1 (ko) | 2006-12-14 | 2006-12-14 | 위염 또는 위궤양 예방 및 치료에 유용한 모모르디카사포닌i |
PCT/KR2006/005603 WO2007073096A1 (en) | 2005-12-20 | 2006-12-20 | Anti-gastritis and anti-ulcer agent containing momordicae semen extract and momordica saponin i isolated from the same |
Publications (3)
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JP2009520020A true JP2009520020A (ja) | 2009-05-21 |
JP2009520020A5 JP2009520020A5 (ja) | 2013-02-28 |
JP5231244B2 JP5231244B2 (ja) | 2013-07-10 |
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US (2) | US20090004309A1 (ja) |
EP (1) | EP1962865A4 (ja) |
JP (1) | JP5231244B2 (ja) |
AU (1) | AU2006328064B2 (ja) |
BR (1) | BRPI0620129A2 (ja) |
RU (1) | RU2429000C2 (ja) |
WO (1) | WO2007073096A1 (ja) |
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US8071844B1 (en) | 2007-09-13 | 2011-12-06 | Nutritional Health Institute Laboratories, Llc | Cultivated momordica species and extract thereof |
KR20090040670A (ko) * | 2007-10-22 | 2009-04-27 | 에스케이케미칼주식회사 | 상처 치료 촉진 효과를 갖는 목별자 추출물 |
US8877259B2 (en) | 2012-02-09 | 2014-11-04 | Mary Kay Inc. | Cosmetic formulation |
Citations (1)
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JPH11302180A (ja) * | 1998-04-16 | 1999-11-02 | Joji Yamahara | 抗潰瘍剤 |
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KR950007046B1 (ko) * | 1992-04-11 | 1995-06-30 | 이형주 | 생약함유 화장수 및 그 제조방법 |
KR960012276B1 (ko) * | 1994-04-21 | 1996-09-18 | 이형주 | 생약함유 미용비누 및 그 제조방법 |
JPH1059858A (ja) | 1996-08-21 | 1998-03-03 | Res Inst For Prod Dev | 抗糖尿病剤 |
CN1100554C (zh) * | 1999-01-19 | 2003-02-05 | 刘明堂 | 一种根治胃下垂的中成药 |
KR20030021714A (ko) * | 2001-09-07 | 2003-03-15 | 에스케이케미칼주식회사 | 독성이 없이 추출된 생약추출물이 복합처방된 생약조성물과 그 제조방법 |
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2006
- 2006-12-20 WO PCT/KR2006/005603 patent/WO2007073096A1/en active Application Filing
- 2006-12-20 AU AU2006328064A patent/AU2006328064B2/en not_active Ceased
- 2006-12-20 BR BRPI0620129-6A patent/BRPI0620129A2/pt not_active IP Right Cessation
- 2006-12-20 EP EP06835307A patent/EP1962865A4/en not_active Withdrawn
- 2006-12-20 RU RU2008129710/15A patent/RU2429000C2/ru not_active IP Right Cessation
- 2006-12-20 JP JP2008547108A patent/JP5231244B2/ja not_active Expired - Fee Related
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Patent Citations (1)
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JPH11302180A (ja) * | 1998-04-16 | 1999-11-02 | Joji Yamahara | 抗潰瘍剤 |
Non-Patent Citations (3)
Title |
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JPN6012040926; IWAMOTO,M. et al: 'Studies on the constituents of Momordica cochinchinensis Spreng. I.' Chem Pharm Bull Vol.33, No.2, 1985, p.464-478 * |
JPN6012040927; 関谷次郎: 'ラカンカ' Foods & Food Ingred J Jpn No.162, 1994, p.24-28 * |
JPN6012040932; WANG,X. et al: 'The antioxidant and antistress activities of the extract of Fructus momordica' Proceedings of the International Symposium on Natural Antioxidants: Molecular Mechanisms and Health , 1996, p.71-81 * |
Also Published As
Publication number | Publication date |
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RU2008129710A (ru) | 2010-01-27 |
WO2007073096A1 (en) | 2007-06-28 |
RU2429000C2 (ru) | 2011-09-20 |
AU2006328064A1 (en) | 2007-06-28 |
EP1962865A4 (en) | 2010-04-28 |
BRPI0620129A2 (pt) | 2011-11-01 |
US20090004309A1 (en) | 2009-01-01 |
JP5231244B2 (ja) | 2013-07-10 |
US20100310687A1 (en) | 2010-12-09 |
EP1962865A1 (en) | 2008-09-03 |
US8158168B2 (en) | 2012-04-17 |
AU2006328064B2 (en) | 2012-11-15 |
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