JP5271454B2 - アルコール性障害緩和剤 - Google Patents
アルコール性障害緩和剤 Download PDFInfo
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- JP5271454B2 JP5271454B2 JP2012531956A JP2012531956A JP5271454B2 JP 5271454 B2 JP5271454 B2 JP 5271454B2 JP 2012531956 A JP2012531956 A JP 2012531956A JP 2012531956 A JP2012531956 A JP 2012531956A JP 5271454 B2 JP5271454 B2 JP 5271454B2
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- krill oil
- ethanol
- alcohol
- alcoholic
- blood
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
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- A61K35/612—Crustaceans, e.g. crabs, lobsters, shrimps, krill or crayfish; Barnacles
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation
- A23L2/52—Adding ingredients
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- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
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- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/115—Fatty acids or derivatives thereof; Fats or oils
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
- A61K31/202—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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Description
(1)オキアミ油を有効成分として含有するアルコール性障害緩和剤。
(2)アルコール性障害の緩和が、血中エタノール濃度の上昇の抑制、酒酔い状態の症状の軽減、酒酔い状態の症状の回復促進、肝障害の抑制、脱水症状の抑制、又は血糖値上昇の抑制のいずれかである、(1)に記載のアルコール性障害緩和剤。
(3)アルコール性障害の緩和がオキアミ油によるアルコール吸収抑制及び/又はアルコール代謝促進に基づくものである、(1)又は(2)に記載のアルコール性障害緩和剤。
(4)オキアミ油が、リン脂質を25重量%以上で含有することを特徴とする(1)ないし(3)いずれかに記載のアルコール性障害緩和剤。
(5)オキアミ油の全脂肪酸の5重量%以上がω3高度不飽和脂肪酸である(1)ないし(4)いずれかに記載のアルコール性障害緩和剤。
(6)オキアミ油の全脂肪酸の2重量%以上がエイコサペンタエン酸である(1)ないし(5)いずれかに記載のアルコール性障害緩和剤。
(7)オキアミ油の全脂肪酸の1重量%以上がドコサヘキサエン酸である(1)ないし(6)いずれかに記載のアルコール性障害緩和剤。
(8)オキアミ油の1日あたりの摂取量が1〜20000mgである(1)ないし(7)いずれかに記載のアルコール性障害緩和剤。
(9)(1)ないし(8)いずれかに記載のアルコール性障害緩和剤を摂取させるための飲食品。
(10)オキアミ油を1回あたり、1〜20000mg摂取させるための(9)に記載の飲食品。
(11)オキアミ油を含有するアルコール代謝促進剤。
(12)オキアミ油がオキアミ由来の原料から有機溶媒によって抽出される、(11)に記載のアルコール代謝促進剤。
(13)オキアミ油がオキアミ由来の原料からエタノールによって抽出される、(11)又は(12)に記載のアルコール代謝促進剤。
(14)オキアミ油がリン脂質を25重量%以上で含有する、(11)〜(13)のいずれかに記載のアルコール代謝促進剤。
(15)オキアミ油において、ω3高度不飽和脂肪酸が全脂肪酸の5重量%以上を占める、(11)〜(14)のいずれかに記載のアルコール代謝促進剤。
(16)オキアミ油がアスタキサンチンを100ppm以上で含有する、(11)〜(15)のいずれかに記載のアルコール代謝促進剤。
オキアミ油を含有するアルコール代謝促進剤を投与することを含む、アルコール代謝の促進法。
オキアミ油を含有するアルコール代謝促進剤を投与することを含む、アルコール性肝障害、脱水症状に伴う組織障害、又は血糖値の上昇に起因する疾患を予防又は改善する方法。
0点: 体姿勢、運動性、正向反射が正常である;
1点: 四肢のバランスは取れないが歩行は可能であり、正向反射は正常である(ほろ酔い状態);
2点: 四肢のバランスが取れず歩行が困難であるが、正向反射は正常である(酩酊、傾眠状態);
3点: 四肢のバランスが取れず歩行が困難であり、正向反射も消失している(泥酔、昏睡状態)。
機器:6890NネットワークGCシステム(アジレント・テクノロジー社);
カラム:DB−WAX(カラム長30m、内径250μm、肉厚0.27μm、型番:122−7032、J&W Scientific社);
カラム温度:180から30℃/分の速度で230℃に昇温後、230℃で15分維持;
注入口温度:250℃;
検出器温度:250℃;
検出器:FID;
キャリアーガス:ヘリウム。
オキアミ油は、例えば、WO2010/03749A1やWO2010/03750A1に記載のいずれの方法によっても製造することができる。製造の具体例を以下に示す。
(1)被験物質の調製
経口投与するオキアミ油は、以下のように調製し、使用するまで褐色のガラス瓶中で保存した。対照群は、同量のオリーブ油のみを投与した。
オキアミ油200mg投与用:乳棒及び乳鉢を用いてオキアミ油をオリーブ油に懸濁し、懸濁液3mL中にオキアミ油が200mg含まれるように調製した。
オキアミ油1,000mg投与用:乳棒及び乳鉢を用いてオキアミ油をオリーブ油に懸濁し、懸濁液3mL中にオキアミ油が1,000mg含まれるように調製した。
エタノール(純度99.5%、和光純薬工業株式会社)と注射用水(株式会社大塚製薬工場)を60.3:39.7の割合で混合することによって調製し、褐色のガラス瓶中で使用するまで室温保存した。
図1に示すスケジュールに従って、被験物質及び60%(v/v)エタノール溶液をラットに投与した。特に言及がない限り、ラットは以下に示す条件で飼育した:
温度: 20〜26℃;
相対湿度: 40〜70%;
換気回数: 10〜20回/時間;
照明時間: 12時間(7:00〜19:00);
飼料: 魚粉抜き粉末飼料(FR−1、株式会社フナバシファーム)の自由摂取;
飲料水: 上水道水を給水瓶から自由摂取。
60%(v/v)エタノール溶液の投与前、投与後1、2、及び24時間において採取した血液にヘパリンを添加し、血中エタノールの濃度を測定し、投与群ごとの平均値を算出した(図2)。
エタノールの投与前、投与後1、2、4、及び24時間におけるラットの一般状態を観察した(図3)。60%(v/v)エタノール溶液を投与しなかった無処理群(A1)を除く全ての投与群(A2〜A4)において、エタノール投与1時間後からほろ酔い状態、酩酊、傾眠状態及び泥酔、昏睡状態が観察され、エタノール投与による酒酔いの状態が観察された。その中でオキアミ油1,000mg/kg投与群(A4)においては、オリーブ油投与群と比較して酒酔いの状態が有意に抑制され、その効果は60%(v/v)エタノール溶液の投与後24時間においてより顕著になった。
60%(v/v)エタノール溶液の投与前、投与後4時間、及び24時間において採取した血液にEDTA−2Kを添加し、HCTの測定に用いた(図4)。
60%(v/v)エタノール溶液の投与前、及び投与後24時間において採取した血液にヘパリンを添加し、1700×g、4℃で15分間遠心分離することによって血漿を得た。この血漿をAST活性の測定に用いた(図5)。
60%(v/v)エタノール溶液の投与前、及び投与後24時間において採取した血液にヘパリンを添加し、1700×g、4℃で15分間遠心分離することによって血漿を得た。この血漿をALT活性の測定に用いた(図6)。
60%(v/v)エタノール溶液の投与前、及び投与後24時間において採取した血液にヘパリンを添加し、1700×g、4℃で15分間遠心分離することによって血漿を得た。この血漿を用いてグルコース濃度の測定を行った(図7)。
オキアミ油のヒトにおけるアルコール摂取への影響をアルコール摂取後の呼気中のエタノール濃度及び呼気中のアセトアルデヒド濃度を測定することにより検討した。
実施例1で調製したオキアミ油又は精製オリーブ油を1粒あたり250mg含有するゼラチンのソフトカプセルを調製した。両ソフトカプセルは着色したものを用い、外観から中身の区別が出来ないようにした。
40歳以上の健康な男性5名。
オリーブ油を対照とした二重盲検クロスオーバー試験を実施した。ウォッシュアウト期間は2週間とした。
エタノールは被験者(5名)から採取した全ての呼気において検出された。呼気中のエタノール濃度の経時変化を図8に示した。図中のエタノール濃度は、被験者(5名)から採取した呼気中のエタノール濃度の平均値を示す。アルコール摂取開始後30分の呼気においてエタノール濃度が最も高くなったが、オキアミ油を摂取した場合とオリーブ油を摂取した場合のエタノール濃度の相違に有意差は認められなかった。しかし、アルコール摂取開始後60分の呼気において、オキアミ油を摂取した場合にはオリーブ油を摂取した場合に比べて有意(P=0.04、Wilcoxon signed rank test)にエタノール濃度が減少していることが示された。
差を確認しやすい指標として呼気中のアセトアルデヒドを選択し、実施例3で呼気中にアセトアルデヒドを検出した被験者において、大豆レシチン、精製魚油による効果と比較した。
他の油として市販の精製魚油(総脂肪酸中、EPA 28重量%、DHA 12重量%)及び大豆レシチン(リン脂質60重量%)を使用した。実施例3と同様に精製魚油又は大豆レシチンを250mg含有するソフトカプセルを調製した。
実施例3で呼気中にアセトアルデヒドが検出された50歳の健康な男性(体重65kg)。
実施例3と同様の方法で精製魚油、及び大豆レシチンのソフトカプセルを被験者に摂取させ、被験者から呼気を採取し、アセトアルデヒド濃度の測定に供した。
呼気中のアセトアルデヒド濃度の経時変化を図9の結果と合わせて、図10に示した。オキアミ油を摂取した場合、オリーブ油、精製魚油、及び大豆レシチンを摂取した場合に比べて、呼気中のアセトアルデヒド濃度が著しく低いことが示された。
Claims (8)
- オキアミ油を有効成分として含有するアルコール性障害緩和剤。
- アルコール性障害の緩和が、血中エタノール濃度の上昇の抑制、酒酔い状態の症状の軽減、酒酔い状態の症状の回復促進、肝障害の抑制、脱水症状の抑制、又は血糖値上昇の抑制のいずれかである、請求項1に記載のアルコール性障害緩和剤。
- アルコール性障害の緩和がオキアミ油によるアルコール吸収抑制及び/又はアルコール代謝促進に基づくものである、請求項1又は2に記載のアルコール性障害緩和剤。
- オキアミ油が、リン脂質を25重量%以上で含有することを特徴とする請求項1ないし3いずれか1項に記載のアルコール性障害緩和剤。
- オキアミ油の全脂肪酸の5重量%以上がω3高度不飽和脂肪酸である請求項1ないし4いずれか1項に記載のアルコール性障害緩和剤。
- オキアミ油の全脂肪酸の2重量%以上がエイコサペンタエン酸である請求項1ないし5いずれか1項に記載のアルコール性障害緩和剤。
- オキアミ油の全脂肪酸の1重量%以上がドコサヘキサエン酸である請求項1ないし6いずれか1項に記載のアルコール性障害緩和剤。
- オキアミ油の1日あたりの摂取量が1〜20000mgである請求項1ないし7いずれか1項に記載のアルコール性障害緩和剤。
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EP2570126B1 (en) * | 2011-09-16 | 2014-03-26 | Darius Rassoulian | Use of melatonin for treating acute alcohol intoxication |
WO2015027463A1 (en) * | 2013-08-30 | 2015-03-05 | Nippon Suisan Kaisha, Ltd. | Agents for preventing or treating alcoholic fatty liver |
JP6203577B2 (ja) * | 2013-09-03 | 2017-09-27 | 雪印メグミルク株式会社 | アルコール生成物代謝促進剤 |
JP2017006011A (ja) * | 2015-06-17 | 2017-01-12 | 京華堂實業股▲ふん▼有限公司 | 酒酔い時間短縮効能を有する酒類飲料組成物 |
CN106361739A (zh) * | 2016-08-29 | 2017-02-01 | 大连槿藏商贸有限公司 | 共轭亚油酸或其衍生物在制备乙醛脱氢酶促进剂方面的应用 |
MX2019009337A (es) * | 2017-02-07 | 2019-09-19 | Fresenius Kabi Deutschland Gmbh | Eficacia a largo plazo de tratamiento de enfermedad hepatica con epa y dha. |
CN111920052A (zh) * | 2019-05-13 | 2020-11-13 | 安琪酵母股份有限公司 | 具有解酒护肝功能的组合物及其制备方法和应用 |
CN112535716B (zh) * | 2019-09-20 | 2022-04-15 | 江阴持一堂医药科技有限公司 | 一种用于治疗酒精性肝损伤的颗粒剂及其制备方法和应用 |
KR20230106065A (ko) * | 2022-01-05 | 2023-07-12 | 주식회사 제핏 | 숙취해소 및 간 기능 개선용 조성물 |
CN117814318A (zh) * | 2024-01-18 | 2024-04-05 | 逢时(青岛)海洋科技有限公司 | 一种护肝复方组合物、制备方法及其应用 |
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CN103096904A (zh) | 2013-05-08 |
US9061035B2 (en) | 2015-06-23 |
US20130156861A1 (en) | 2013-06-20 |
JPWO2012029898A1 (ja) | 2013-10-31 |
WO2012029898A1 (ja) | 2012-03-08 |
US8691297B2 (en) | 2014-04-08 |
US20140120172A1 (en) | 2014-05-01 |
CN103096904B (zh) | 2016-03-09 |
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