CN101868231A - Ω-3-脂肪酸的新用途 - Google Patents

Ω-3-脂肪酸的新用途 Download PDF

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CN101868231A
CN101868231A CN200880116755A CN200880116755A CN101868231A CN 101868231 A CN101868231 A CN 101868231A CN 200880116755 A CN200880116755 A CN 200880116755A CN 200880116755 A CN200880116755 A CN 200880116755A CN 101868231 A CN101868231 A CN 101868231A
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fatty acid
omega
purposes
described preparation
analgesia
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R·克伦布赫尔兹
K·克伦布赫尔兹
C·克伦布赫尔兹
N·施拉
P·莱姆布克
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K D Pharma Bexbach GmbH
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/185—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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Abstract

本发明涉及Ω-3-脂肪酸在镇痛制剂中的用途。优选所述制剂包含高度不饱和的Ω-3-脂肪酸，其尤其包括EPA和/或DHA。用于镇痛，优选将Ω-3-脂肪酸以高于2g，特别是高于3至4g的高剂量施用。

Description

Ω-3-脂肪酸的新用途
本发明涉及Ω-3-脂肪酸的新用途。
长久以来，由专业文献中已知，由Ω-3-脂肪酸，特别是高度不饱和的Ω-3-脂肪酸，尤其是EPA和DHA，引发抑制炎症和心血管保护的作用。以介于0.5和1g的剂量每日摄取EPA和DHA，经数周就可以经达到积极效果。在用一克EPA和DHA每天经六个月的治疗后可以确定心肌梗塞风险的显著降低(G Ital Cardiol 1993；23：1053-1061)。用Ω-3-脂肪酸治疗疼痛的炎症和风湿性疾病，在至少一个月后显示积极的效果(Alair A.B.，et.al.Nutrition(2005)；1，2，131-136)。此外，已知Ω-3-脂肪酸用于长期治疗皮炎和牛皮癣(J Am Acad Dematol.(1998)；38，539-547)以及用于治疗各种经期前的症状(Deutsch B.et.al.Nutrition Research  (2000)；5(20)，621-631(11))。
本发明的任务在于，开发Ω-3-脂肪酸的其它应用可能性。
根据本发明将Ω-3-脂肪酸用于镇痛制剂。
发明人认识到，Ω-3-脂肪酸除了已知的上述作用外还适用于直接缓解急性疼痛并且就此而言还发挥短期的数小时内起效的作用。
在镇痛的情况下，特别有效的是高度不饱和的脂肪酸，尤其是EPA(二十碳五烯酸)和DHA(二十二碳六烯酸)。
特别是在高剂量Ω-3-脂肪酸的情形下提供作为镇痛剂的短期起效的作用，例如在剂量高于2g，特别是高于3至4g的情形下。
用于镇痛，优选将总剂量一次性给予。
缓解疼痛的作用机制与阿司匹林-活性物质的作用机制相同。Ω-3-脂肪酸的给予(特别是以高剂量)减少或竞争性阻断由Ω-6-脂肪酸通过COX-酶产生促进炎症、引发疼痛的物质(特别是组织-激素)。
同时通过同一COX-酶由给予的Ω-3-脂肪酸本身形成炎症抑制性物质。
优选，包含Ω-3-脂肪酸的制剂不含其它脂肪酸或在其它脂肪酸方面是贫乏的，特别是Ω-6-脂肪酸。
虽然在镇痛剂中Ω-3-脂肪酸可以与至少一种其它活性物质组合，但是在本发明优选的实施形式中，所述制剂仅包含Ω-3-脂肪酸或/和Ω-3-脂肪酸的化合物作为活性物质。作为添加剂考虑矫味剂。
所述包含Ω-3-脂肪酸的制剂可以例如在炎症和创伤的情形下用于镇痛。
所述制剂尤其可用于对抗头痛、牙痛、关节痛、痛经或/和肌肉疼痛。
有利地是，所述制剂特别是针对肌肉疼痛预防性使用，例如在较长的训练间期后再度接受训练前。所述针对肌肉疼痛的预防性作用还源于在所谓Z-盘中细胞弹性的提高并减少与此相关的撕裂形成。在超出平均水平的强度的肌肉负荷的近前(例如在网球比赛前)摄取Ω-3-脂肪酸显著防止或减缓肌肉疼痛的产生。
以下依据多个实施例描述所述制剂的作用。
1.实施例
针对各种类型的疼痛的效果，尤其是头痛，在多个测试者(Probanten)上试验。在每种情况下一次性施用3g高度不饱和的Ω-3-脂肪酸(K.D.Pharma Bexbach GmbH的产品PUR3：60％EPA+20％DHA+10％其它Ω-3-脂肪酸)在一天内(在头痛的情形下甚至在几小时内)实现显著的疼痛减退。
2.实施例
申请人自身测试Ω-3-脂肪酸的预防肌肉疼痛的作用。在每种情况下摄入3g Ω-3-脂肪酸(K.D.Pharma Bexbach GmbH的产品：70％EPA+12％DHA)在肌肉负荷前一天(耐力性体育锻炼、爬山、园艺劳动)在所有被观察的情况下都完全或部分防止了肌肉疼痛的出现。如果早于所述负荷的三天前摄入，所述效果减弱。
3.实施例
于14.00点开始网球比赛的十个人在上午摄入4g量的Ω-3-脂肪酸(K.D.Pharma产品：39％EPA+43％DHA)。就强度和持续时间而言，该比赛对所有这些人都是或多或少地超出他们习惯程度的体育运动和根据经验将导致肌肉疼痛的肌肉负荷。然而所涉及的人员无一人出现明显程度的肌肉疼痛。

Claims (14)

1.Ω-3-脂肪酸在镇痛制剂中的用途。
2.根据权利要求1的用途，其特征在于，所述Ω-3-脂肪酸包括高度不饱和的Ω-3-脂肪酸。
3.根据权利要求2的用途，其特征在于，所述Ω-3-脂肪酸包括EPA、DHA、DPA、ETA、21:5n3和/或SDA。
4.根据权利要求1至3之一的用途，其特征在于，所述Ω-3-脂肪酸作为游离脂肪酸或以结合的形式，特别是作为酯或盐，使用。
5.根据权利要求1至4之一的用途，其特征在于，所述Ω-3-脂肪酸以高于2g，优选3至4g的剂量施用以用于镇痛。
6.根据权利要求1至5之一的用途，其特征在于，一次性给予特定剂量的所述制剂以用于镇痛。
7.根据权利要求1至6之一的用途，其特征在于，所述制剂不含其它脂肪酸或在其它脂肪酸方面是贫乏的。
8.根据权利要求1至7之一的用途，其特征在于，所述制剂仅包含Ω-3-脂肪酸作为缓解疼痛的活性物质或者包含Ω-3-脂肪酸与其它物质的组合，所述其它物质特别是缓解疼痛的活性物质。
9.根据权利要求8的用途，其特征在于，所述制剂包含矫味剂作为其它物质。
10.根据权利要求1至9之一的用途，其特征在于，所述制剂在炎症或/和创伤的情形下用以镇痛。
11.根据权利要求1至10之一的用途，其特征在于，所述制剂用于对抗头痛、牙痛、关节痛、痛经或/和肌肉疼痛。
12.根据权利要求1至11之一的用途，其特征在于，所述制剂预防性地使用，特别是针对肌肉疼痛预防性地使用。
13.根据权利要求1至12之一的用途，其特征在于，所述Ω-3-脂肪酸静脉内或口服施用。
14.根据权利要求13的用途，其特征在于，所述Ω-3-脂肪酸以胶囊、片剂或/和液体形式施用。
CN200880116755A 2007-11-19 2008-11-18 Ω-3-脂肪酸的新用途 Pending CN101868231A (zh)

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DE102007055344A DE102007055344A1 (de) 2007-11-19 2007-11-19 Neue Verwendung von Omega-3-Fettsäure(n)
DE102007055344.9 2007-11-19
PCT/DE2008/001928 WO2009065395A2 (de) 2007-11-19 2008-11-18 Neue verwendung von omega-3-fettsäure(n)

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ES2492667T3 (es) 2014-09-10
WO2009065395A2 (de) 2009-05-28
RU2501557C2 (ru) 2013-12-20
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