CN1099610A - 用于吸烟者的制剂 - Google Patents
用于吸烟者的制剂 Download PDFInfo
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- CN1099610A CN1099610A CN94104147A CN94104147A CN1099610A CN 1099610 A CN1099610 A CN 1099610A CN 94104147 A CN94104147 A CN 94104147A CN 94104147 A CN94104147 A CN 94104147A CN 1099610 A CN1099610 A CN 1099610A
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/08—Anti-ageing preparations
-
- A—HUMAN NECESSITIES
- 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
- 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
- A23L33/12—Fatty acids or derivatives thereof
-
- 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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A—HUMAN NECESSITIES
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- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
- A23V2200/318—Foods, ingredients or supplements having a functional effect on health having an effect on skin health and hair or coat
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S424/00—Drug, bio-affecting and body treating compositions
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Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nutrition Science (AREA)
- Food Science & Technology (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Mycology (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Emergency Medicine (AREA)
- Polymers & Plastics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- Grain Derivatives (AREA)
- General Preparation And Processing Of Foods (AREA)
- Jellies, Jams, And Syrups (AREA)
Abstract
制备一种用于减轻吸烟致病作用的制剂,其中使
用了选自GLA、DGLA和AA中的一种或多种n—
6EFAs和选自SA、20∶4n—3、EPA、DPA和DHA
中的一种或多种n—3EFAs,优选各种脂肪酸的日剂
量在1mg到100g/天的范围内。在其它目的中该
制剂还可以用于治疗或预防吸烟者的皮肤老化。
Description
在众多不同的健康问题中,特别是肺癌,慢性肺病如支气管炎,以及冠状和外周动脉疾病中,吸烟被确认是一个主要因素。然而,虽然开展了大量的研究工作,却仍不能完全阐明吸烟诱发损害的机制。而且,在吸烟与疾病之间却出现重要的异常现象。例如,尽管日本所吸的香烟与其它地方所吸的一样,并且在日本人和其它地方的人中由吸烟会引起相似的生理上和生化方面的变化,但在日本比在其它国家中吸烟似乎只有很小的危害。对此,还不能很好地解释。
作为有关外周血管疾病调查部分,120名年龄在40和70岁的健康个体和120名患有外周血管疾病的病人完成有关本人吸烟习惯的详细问卷。从而对每人吸烟期的香烟消耗量作出一个估计,以踝/臂压力指数(ABPI)作为一个测量指标的外周血管疾病的严重程度是与吸烟量有关的。在仰卧状态的健康个体中,踝部和臂部血压相同,其踝部压力/臂部压力的指数为1.0。随着动脉病(该疾病对腿动脉的影响必乎总是多于对臂动脉的影响)严重程度的增加,踝部压力变得低于臂部压力。因此,ABPI是腿部动脉阻塞严重程度的一个测量指标。
我们已发现吸烟期所吸的香烟量与ABPI成反比。吸烟量越大,股动脉(腿主动脉)阻塞越严重。这种对应关系非常显著(P<0.001)。这一观察结果证实了早期有关吸烟和动脉疾病的研究。
研究是从全部个体抽取血样。从血浆中提取出脂质并用薄层层析分离成磷脂,胆甾醇酯和甘油三酯组分。然后将每个组分甲基化,并用定量气相色谱测定形成的脂肪酸甲基酯组合物。测定必需脂肪酸,按照Spearman等级(rank)对比法它们的浓度与吸烟期限相关。表1中总结出了这种关系的显著性和指向特性。
在吸烟习惯(所吸香烟总量的烟期估计)与血浆脂质组分中某些必需脂肪酸的含量水平之间进行对比。用Spearman等级对比法,各值都是统计学上显著相关的。所有对应关系都呈反比,吸烟量越大,脂肪酸含量越低(ns=不显著)。
表1
亚油酸 -甘油三酯 P<0.05
-胆甾醇酯 P<0.05
-磷脂 ns
花生四烯酸 -甘油三酯 P<0.05
-胆甾醇酯 P<0.05
-磷脂 ns
二十碳五烯酸 -甘油三酯 P<0.05
-胆甾醇酯 P<0.05
-磷脂 P<0.1
二十二碳六烯酸 -甘油三酯 P<0.05
-胆甾醇酯 P<0.001
-磷脂 P<0.001
可以看出,吸烟与降低总组分中的亚油酸含量有关。吸烟引起亚油酸含量降低以前已有许多文献记载。但,吸烟也能使花生四烯酸(AA),二十碳五烯酸(EPA),二十二五烯酸(DPAn-3)和二十二碳六烯酸(DHA)的浓度降低,却是一个新发现。
我们相信,这四种长链高级不饱和脂肪酸的缺乏在吸烟的副作用中具有重要作用。这些酸一定在体内具有重要功能,它们是每个细胞膜的重要成分,许多第二信使系统调节剂,其它第二信使如前列腺素和白三烯的来源。特别有趣的是这样一个事实;这四种酸在大多数国家的食物中存在量仅为中等,而在日本的食物中含量较高。在多油的鱼类中发现了大量的AA,EPA,n-3DPA和DHA,而与其它国家相比,多油的鱼类是日本食物更重要的一部分。这样一个吸烟又食用传统的日本食物的日本人就不会遭到其它国家人相同的吸烟生化后果。经表2所示的反应程序在体内形成长链必需脂肪酸。
表2
n-6 n-3
18:2δ-9,12 18:3δ-9,12,15
(亚油酸) (α-亚麻酸)
↓
δ-6-去饱和酶
↓
18:3δ-6,9,12 18:4δ-6,9,12,15
(γ-亚麻酸) (stearidonic acid)
↓
伸长
↓
20:3δ-8,11,14 20:4δ-8,11,14,17
(二高-γ-亚麻酸)
↓
δ-5去饱和酶
↓
20:4δ-5,8,11,14 20:5δ-5,8,11,14,17
(花生四烯酸) (二十碳五烯酸)
↓
伸长
↓
20:4δ-7,10,13,16 22:5δ-7,10,13,16,19
(肾上腺酸)
↓
δ-4去饱和酶
↓
22:5δ-4,7,10,13,16 22:6δ-4,7,10,13,16,19
(二十二碳六烯酸)
按照系统命名法把这些天然为顺式构型的酸相应地命名为十八烷酸,二十烷酸或二十二烷酸的衍生物,例如,δ-9,13-十八碳二烯酸或δ-4,7,10,13,16,19-二十二碳六烯酸。但数值表示如相应为18:2n-6或22:6n-3是更方便的。大写字母如用于表示20:5n-3酸(二十碳五烯酸)的EPA或用于表示22:6n-3酸(二十二碳六烯酸)的DHA也可以使用,但当相同链长和不饱和度的n-3和n-6系列中或多或少常用的俗名已列出。尽管用于表示18:4n-3酸的Stearidonic acid这一名称已开始使用,并且二十碳五烯酸和二十二碳六烯酸这些名称也一样在使用,但n-3系列中仅18:3n-3有常用的俗名α-亚麻酸。
主要食物的必需脂肪酸是亚油酸(LA)和α-亚麻酸(ALA),它们经一系列的降低饱和度和伸长反应转化为较高级的酸。然而,这些反应中的第一步非常慢且限定速率,通过改变LA和ALA的摄入量来改变长链酸的含量一般是不可能的。但是用就n-6E-FAs而言给予GLA,DGLA或AA,就n-3EFAs而言给予Stearidonic acid(SA),20:4n-3酸,EPA,DPA,或DHA的方法绕过开始限速的步骤来使吸烟者体内的这四种特定长链酸的含量降低却是可能的。在吸烟者中通过提供如实施例中说明的一种或多种特定n-6和n-3EFAs组的成员之一来校正EFA含量的缺少是可能的。那些EFAs对吸烟者的益处可以书写在提供EFAs包装的标签上或相关文献上。
这种必需的长链脂肪酸(其含量由吸烟降低)在皮肤中是很重要的。经血流或局部使用可向皮肤补充这些脂肪酸。吸烟最重要的作用之一是加速皮肤老化。就此而言,吸烟者体内20和22碳EFAs的含量降低很可能特别重要。
因此本发明提供了选自GLA,DGLA和AA中一种或多种n-6EFAs和/选自SA,20:4n-3,EPA,DPA或DHA的一种或多种n-3EFAs用于制备减轻吸烟致病作用的制剂,优选每种脂肪酸的日剂量在1mg到100g/天范围内。
本发明也提供了选自GLA,DGLA和AA中的一种或多种n-6EFAs和/或选自SA,20:4n-3,EPA,DPA或DHA中的一种或多种n-3EFAs用于制备治疗和预防吸烟者皮肤老化的制剂,优选每种脂肪酸日剂量在1mg到100g/天范围内。
本发明还提供了一种减轻吸烟致病作用的方法,其中包括对吸烟者使用选自GLA,DGLA和AA中的一种或多种n-6EFAs和/或选自SA,20:4n-3EPA,DPA或DHA中的一种或多种n-3EFAs,优选每种脂肪酸的日剂量在1mg到100g/天范围内。
这种EFAs可任意与已知对吸烟者有益的其它营养成分,如维生素C,维生素E,β-胡萝卜素,B族维生素,钙和硒合用。
可制成药用或营养补品制剂而使吸烟者每天获得每种脂肪酸1mg到100g,优选10mg到10g,特别优选50mg到4g,理想的是100mg到2g。另一方面可制成含脂肪酸总量为0.001到50wt%的局部用制剂或食品供吸烟者使用。这种脂肪酸可以是任何合适的形式,包括游离酸,任何合适的盐,单、双或三甘油酯,包含胆甾醇酯,酰胺或磷脂在内的任何合适的酯。
下列常用的合适制剂本身或其减轻吸烟致病作用的用途来说明本发明。
实施例
1.供吸烟者使用的含有100mgGLA,100mgAA,100mgEPA和100mgDHA的软胶囊或硬胶囊,或锭剂或片剂或其它药用或营养剂型。
2.用阿拉伯胶,明胶,淀粉或其它合适材料制成的供吸烟者使用的颗粒或粉末,其中按重量计每克中含50mgDGLA,50mgAA,50mgSA和50mgDHA。
3.供吸烟者用作色拉油或渗入到任何合适食物中去的油剂,其中含有按重计10%的GLA,5%的AA,5%的EPA,5%的DHA。
4.供吸烟者用作食物的餐后甜食、泡沫、膏状物、奶油冻或其它液体或半液体制剂,其中含有按重量计2%的GLA、2%的AA,2%的DGLA、2%SA、2%的EPA和2%的DHA。
5.供吸烟者局部使用的膏剂、霜剂、洗液、洗头膏、膏药、枝条剂、阴道药栓、塞药或任何其它剂型,其中活性成分是一种含有重百分比为5%DGLA、2%AA、3%EPA和3%DHA的油状物。
6-10供吸烟者使用的如1-5的制剂,其中的活性成分是选自GLA、DGLA和AA中的一种或多种n-6EFAs,和选自SA,20:4n-3、DPA、EPA或DHA中的一种或多种n-3EFAs。
11-15供吸烟者使用的如1-5的制剂,其中的活性成分是n-6系列中的GLA或DGLA和n-3系列中的EPA或DHA或它们两者。
16-30,如1-5的供吸烟者使用的制剂或食物,其中除了E-FAs外,还渗有其它必需营养物,包括维生素和矿物质,特别是维生素C(按每天20到2000mg的量),B族维生素,维生素E(按每天10到2000国际单位的量),β-胡萝卜素和生物可利用的锌和硒。
31-60,如1-30的制剂,其中含有n-6或n-3的EFAs,但二者不共存。
Claims (10)
1、选自GLA,DGLA和AA中的一种或多种n-6EFAs和或选自SA,20∶4n-3,EPA,DPA或DHA中的一种或多种n-3E-FAs用于制备一种减轻吸烟致病作用的制剂。
2、如权利要求1的用途,其中的制剂既含n-6EFAs又含n-3EFAs。
3、如权利要求1或2的用途,其中的制剂尤其适用于治疗或预防皮肤过早老化。
4、如权利要求1,2或3的用途,其中的制剂是一种油状、粉末、餐后甜食、泡沫、颗粒、薄片、奶油冻或任何其它合适形式的营养补品,并且其中脂肪酸的含量(按总重量计)为0.001到50%的浓度。
5、如权利要求1,2或3的用途,其中的制剂是膏剂、霜剂、洗液、油剂、枝条剂、膏药或其它任何适当形式的皮肤吸收局部制剂,其中脂肪酸的含量(按总重量计)为0.001到50%的浓度。
6、一种减轻吸烟致病作用的方法,其中包括给吸烟者使用选自GLA、DGLA和AA中的一种或多种n-6EFAs和/或选自SA、20:4n-3EPA、DPA和DHA中的一种或多种n-3EFs的制剂,使每种脂肪酸的日剂量在1mg到100g范围内。
7、一种治疗或预防吸烟者皮肤过早老化的方法,其中包括对吸烟者使用选自GLA,DGLA和AA中的一种或多种n-6EFAs和/或选自SA,20:4n-3,EPA、DPA和DHA中的一种或多种n-3EFAs的制剂,使每种脂肪酸的日剂量在1mg到100g范围内。
8、一种如权利要求6或7的方法,其中的制剂含有n-6酸和n-3酸。
9、一种如权利要求6,7或8的方法,其中制剂是以油状、粉末、餐后甜食、泡沫、颗粒、薄片、奶油冻或其它任何合适形式的营养补品,并且其中的脂肪酸含量(按总重量计)为0.001到50%的浓度。
10、一种如权利要求6、7或8的方法,其中制剂是膏剂、霜剂、洗液、油剂、枝条剂、膏药或其它任何适宜形式的皮肤吸收局部制剂,并且其中的脂肪酸含量(按总重量计)为0.001到50%的浓度。
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GB939305737A GB9305737D0 (en) | 1993-03-19 | 1993-03-19 | Formulation for use in smokers |
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Family Cites Families (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1446431A (en) * | 1972-04-20 | 1976-08-18 | Williams J | Nutritional supplement |
FR2197605A1 (en) * | 1972-09-06 | 1974-03-29 | Williams John | Foodstuff or skin nutrient to combat cholesterolaemia - contains arachidonic acid or gamma linolenic acid or esters and salts thereof |
FR2557452B1 (fr) * | 1983-12-28 | 1986-08-14 | Roussel Uclaf | Nouvelles compositions pour les soins de la peau renfermant de l'huile d'onagre et des traits tissulaires de rate |
FR2597337B2 (fr) * | 1984-10-19 | 1992-07-03 | Courtin Olivier | Cosmetique pour retarder le vieillissement de la peau et procede d'application. |
JPS62138411A (ja) * | 1985-12-12 | 1987-06-22 | Kanebo Ltd | 皮膚老化防止用化粧料 |
FR2609630B1 (fr) * | 1987-01-19 | 1991-01-04 | Rochas Parfums | Nouvelles compositions cosmetiques ou dermatologiques renfermant un extrait des fruits de silybum marianum riche en silymarine associe a des acides gras essentiels |
JPS63277604A (ja) * | 1987-05-11 | 1988-11-15 | Showa Denko Kk | α−リノレン酸含有化粧料 |
GB8806737D0 (en) * | 1988-03-22 | 1988-04-20 | Efamol Holdings | Therapeutic composition & method |
JPH0253706A (ja) * | 1988-08-18 | 1990-02-22 | Kurooda Japan Kk | 化粧料組成物 |
GB8906369D0 (en) * | 1989-03-20 | 1989-05-04 | Tisdale Michael J | Eicosapentaenoic acid |
GB8916734D0 (en) * | 1989-07-21 | 1989-09-06 | Efamol Holdings | Pharmaceutical and dietary uses of fatty acids |
GB8920228D0 (en) * | 1989-09-07 | 1989-10-18 | Efamol Holdings | Fatty acid therapy |
DE59107305D1 (de) * | 1990-05-22 | 1996-03-07 | Harold Bumann | Verfahren zur herstellung eines fruchtsaft-getränkes |
DK0457950T3 (da) * | 1990-05-23 | 1994-03-07 | Nestle Sa | Anvendelse af stearidonsyre til behandling af inflammatorisk betingede sygdomme |
DE4133694C2 (de) * | 1991-10-11 | 1993-10-07 | Fresenius Ag | Verwendung einer Emulsion mit mehrfach ungesättigten Fettsären zur i.v.-Verabreichung zur Behandlung von Hauterkrankungen |
GB9217781D0 (en) * | 1992-08-21 | 1992-10-07 | Efamol Holdings | Fatty acid treatment |
-
1994
- 1994-03-14 CA CA002119000A patent/CA2119000A1/en not_active Abandoned
- 1994-03-15 EP EP94301853A patent/EP0615753A1/en not_active Withdrawn
- 1994-03-16 AU AU57849/94A patent/AU677275B2/en not_active Ceased
- 1994-03-18 US US08/214,553 patent/US5562913A/en not_active Expired - Fee Related
- 1994-03-18 CN CN94104147A patent/CN1099610A/zh active Pending
- 1994-03-18 JP JP6048396A patent/JPH0716076A/ja active Pending
- 1994-03-18 KR KR1019940005425A patent/KR940021057A/ko not_active Application Discontinuation
- 1994-03-18 NO NO940994A patent/NO940994L/no unknown
- 1994-03-18 NZ NZ260133A patent/NZ260133A/en unknown
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1091363C (zh) * | 1997-12-23 | 2002-09-25 | 利尔生公司 | 脂肪掺合物 |
CN109152759A (zh) * | 2016-06-01 | 2019-01-04 | 雀巢产品技术援助有限公司 | 用于预防变应性疾病的组合物 |
Also Published As
Publication number | Publication date |
---|---|
US5562913A (en) | 1996-10-08 |
KR940021057A (ko) | 1994-10-17 |
CA2119000A1 (en) | 1994-09-20 |
NO940994D0 (no) | 1994-03-18 |
NZ260133A (en) | 1997-06-24 |
AU677275B2 (en) | 1997-04-17 |
AU5784994A (en) | 1994-09-22 |
EP0615753A1 (en) | 1994-09-21 |
JPH0716076A (ja) | 1995-01-20 |
NO940994L (no) | 1994-09-20 |
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