CN101001543B - 硫辛酸浓缩物 - Google Patents
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Abstract
本发明涉及一种无水浓缩物,其由泛醌Q10、中等链的甘油三酯或甘油三酯混合物、α-硫辛酸和/或其衍生物以及一种或多种在食品或药品法律上经批准的HLB-值为9-19的乳化剂组成。
Description
本发明涉及根据DE 10108614A1的α-硫辛酸浓缩物。
自从K.Rett等人(Diabetes und Stoffwechsel,1996,5/3,Suppl.(59-63))的研究以来,已知在超重的患者中,给予α-硫辛酸缓解了其困苦。Min-Seon Kim等人(NATURE MEDCINE Band 10,Nr.7,Juli2004,Seiten 727-734)在小鼠上进行的研究进一步表明,可以把某种抑制食欲的作用归因于α-硫辛酸。因此对于人类来说出现了这样一种可能性,即通过摄入α-硫辛酸而减少的对于食物摄取的需求导致体重减轻。
因此,本发明的目标是提供开始时所述类型的无副作用的组合物,其可以有助于体重减轻或者可以改善之。
德国专利公开文件DE 10108614A1中的实施例d教导了由α-硫辛酸和聚山梨酯组成的水溶性α-硫辛酸-溶解物(Solubilisat)。
对此,本发明提出了一种无水浓缩物,其含有泛醌Q10、中等链的甘油三酯或甘油三酯混合物、α-硫辛酸或其衍生物以及一种或多种在食品或药品法律上经批准的HLB-值为9-19的乳化剂。本发明基于这样的构思,一方面通过提供足够量的Q10来促进脂肪分解,另一方面将脂肪分解局限于在生物体中贮存的脂肪,方法是α-硫辛酸的同时给予通过影响下丘脑而限制了食物摄取。这些所述的本发明浓缩物的成分是在食品法律上经批准的并且无副作用的。当以合适的其成分的重量比率时,在室温下,所述浓缩物是澄清和粘滞的,并且优选地在大约60℃的稍微升高的温度下,其可以毫无困难地加工成胶囊的内含物。每天给予这样的胶囊可以导致生物体的体重减轻。在这期间所进行的科学研究表明,与安慰剂相比,在受试者中给予本发明的浓缩物导致更强的体重损失百分比,即更大的内脏脂肪量损失百分比和更大的腰围差异百分比。
可用于本发明的乳化剂由各国家或国际食品或药品法规决定。在此意义上最优先考虑的增溶剂是到处均被批准的非离子型聚山梨酯,尤其是聚山梨酯20和/或聚山梨酯80。例如在美国和日本还批准了其他乳化剂,其同样也可用于本发明。
除了α-硫辛酸之外,二氢硫辛酸或二氢硫辛酸酰胺也可以成功用于本发明的浓缩物。此外,本发明的优选实施方案在从属权利要求中给出。如果所述浓缩物只含有聚山梨酯80或者任选地含有聚山梨酯80与聚山梨酯20的混合物时,这经证实是合适的。此外,适宜的是使用轻食用油例如蓟子油或者组合物作为中等链的甘油三酯,所述组合物基本上由辛酸和癸酸组成,并且可以以商品名Miglyol 812获得。
聚山梨酯的重量份额对于本发明浓缩物的其余成分的重量份额之和的比例优选为大约4∶1至大约5.5∶1。合适地,Q10与α-硫辛酸的重量比为大约1∶1至大约1∶4,误差不超过20%。
本发明浓缩物的具体的示例性组成在从属权利要求中给出。
本发明的浓缩物适合作为不含酒精的饮料例如水、果汁、蔬菜汁的添加剂,其中浓缩物相对于饮料的浓度为大约1∶0.1至大约1∶5000是适宜的。还可以向奶制品、蜂蜜、植物油中添加该浓缩物,其中浓缩物与最后提到的那些产品的比例合适地为大约1∶0.1至大约1∶100。
为了制备本发明的浓缩物,合适地采取如下步骤:首先获得由Q10、0聚山梨酯80和中等链的甘油三酯组成的溶解物,随后获得由α-硫辛酸和聚山梨酯80或聚山梨酯20组成的溶解物,然后将Q10-溶解物与α-硫辛酸-溶解物混合,并拌和成均匀的、澄清的和在水中可溶的物料(Masse)。适宜的是,合适地在大约60℃的温度下,以大约2∶1,例如1.8∶1的重量比混合Q10-溶解物与α-硫辛酸-溶解物。α-硫辛酸的最佳溶解温度比热敏感的Q10的最佳溶解温度高得多,从而适宜的是在对于它们各自合适的温度下分开地无沉淀地溶解这两种活性物质。
下文中将详细地说明和给出本发明的实施例。
从5%的无水的水溶性Q10-溶解物开始,如在文献WO 03/007907的制备实施例2中所描述的。然后,将790重量份的聚山梨酯80加热至大约85℃。然后加入50重量份的辅酶Q10,并在保持大约85℃的温度的情况下将混合物(840重量份)搅拌一定的时间(大约5分钟)直至其变得均匀和透明。随后,在同样也将蓟子油事先加热至大约85℃之后,向该混合物中加入160重量份的蓟子油,并在保持大约85℃的温度的情况下搅拌一定的时间(大约2分钟)直至总的混合物(1000重量份)同样也变得均匀和透明。在冷却至室温或体温后保持了澄清度和水溶性。1克这样的溶解物含有50mg Q10。
在那篇文献中,提及蓟子油作为一种成分。但是,根据本发明可以用同样量的中等链的甘油三酯混合物来代替蓟子油,所述甘油三酯混合物含有中等链长的饱和植物脂肪酸,基本上由辛酸和癸酸组成,并且例如可以由Sasol GmbH公司以商品名Miglyol 812N提供。
然后,通过首先将900重量份的聚山梨酯20加热至大约60℃来制备10%无水的水溶性α-硫辛酸-溶解物。在该温热的聚山梨酯20中缓慢地淌入100重量份的α-硫辛酸(CAS-Nr.62-46-4;Degussa公司的ALIPURE)。在持续搅拌下,将混合物保温一段时间,直至该混合物在大约100℃下为透明的混合物。冷却至室温后该混合物保持透明,并且在该形式下是完全可溶于水的。1g这样的溶解物含有100mgα-硫辛酸。虽然使用聚山梨酯20使得更容易溶解;但是,在该情况下,出于感觉的原因,相同量的聚山梨酯80是优选的。
为了获得Q10-α-硫辛酸-溶解物,在大约60℃的温度下将大约660重量份的Q10-溶解物与大约370重量份的α-硫辛酸-溶解物搅和成均匀的混合物。该混合物含有33重量份的Q10和37重量份的α-硫辛酸,这两者均包含在颗粒直径为大约10nm的聚山梨酯-胶束中。以470mg的填充重量,用该混合物填充由明胶制成的或无明胶的胶囊。因而,该胶囊的内含物由大约15.02mg的Q10、大约16.68mg的α-硫辛酸、大约48.22mg的甘油三酯和大约389.7mg的聚山梨酯80组成。
在每天摄取例如三颗这样的胶囊的情况下,那么生物体所摄入的为大约
-45.15mg Q10
-50.58mgα-硫辛酸
-144.66mg甘油三酯
-1169.1mg聚山梨酯80。
该数量远远低于在食品法律上对于每种成分官方所批准的最大日剂量。
本发明浓缩物的组成的其他实施例在下表中给出。在这些表中,MCT为上述的Miglyol 812,和将聚山梨酯理解为聚山梨酯80。根据上面对于第一个实施例所给出的说明来制备各个浓缩物实施例。
实施例2
g/kg | 重量% | |
A)Q<sub>10</sub> | 50 | 5 |
B)α-硫辛酸 | 100 | 10 |
C)MCT | 40 | 4 |
D)聚山梨酯 | 810 | 81 |
总计 | 1,000 | 100 |
实施例3
g/kg | 重量% | |
A)Q<sub>10</sub> | 40 | 4 |
B)α-硫辛酸 | 80 | 8 |
C)MCT | 60 | 6 |
D)聚山梨酯 | 820 | 82 |
总计 | 1,000 | 100 |
实施例4
g/kg | 重量% | |
A)Q<sub>10</sub> | 50 | 5 |
B)α-硫辛酸 | 90 | 9 |
C)MCT | 50 | 5 |
g/kg | 重量% | |
D)聚山梨酯 | 810 | 81 |
总计 | 1,000 | 100 |
实施例5
g/kg | 重量% | |
A)Q<sub>10</sub> | 20 | 2 |
B)α-硫辛酸 | 80 | 8 |
C)MCT | 60 | 6 |
D)聚山梨酯 | 840 | 84 |
总计 | 1,000 | 100 |
Claims (18)
1.无水浓缩物,其由泛醌Q10、中等链的甘油三酯、α-硫辛酸和/或二氢硫辛酸或二氢硫辛酸酰胺以及一种或多种在食品或药品法律上经批准的HLB-值为9-19的乳化剂组成,其中所述乳化剂由聚山梨酯组成,其中泛醌Q10与α-硫辛酸的重量比为1∶1至1∶4,并且其中聚山梨酯的重量份额对于其余成分的重量份额之和的比例为4∶1至5.5∶1。
2.无水浓缩物,其由泛醌Q10、中等链的甘油三酯、α-硫辛酸和/或二氢硫辛酸或二氢硫辛酸酰胺以及一种或多种在食品或药品法律上经批准的HLB-值为9-19的乳化剂组成,其中所述乳化剂为非离子型聚山梨酯,其中泛醌Q10与α-硫辛酸的重量比为1∶1至1∶4,并且其中聚山梨酯的重量份额对于其余成分的重量份额之和的比例为4∶1至5.5∶1。
3.根据权利要求2的浓缩物,其中所述乳化剂由聚山梨酯20和/或聚山梨酯80组成。
4.根据前述权利要求中任一项的浓缩物,其中所述中等链的甘油三酯为轻油或者由辛酸和癸酸组成的混合物。
5.根据权利要求4的浓缩物,其中所述轻油为蓟子油。
6.根据权利要求1或2的浓缩物,其由854.4重量份的聚山梨酯、33重量份的Q10、37重量份的α-硫辛酸和105.6重量份的甘油三酯组成。
7.根据权利要求1或2的浓缩物,其由5重量%的Q10、10重量%的α-硫辛酸、4重量%的甘油三酯和81重量%的聚山梨酯80组成。
8.根据权利要求1或2的浓缩物,其由4重量%的Q10、8重量%的α-硫辛酸、6重量%的甘油三酯和82重量%的聚山梨酯80组成。
9.根据权利要求1或2的浓缩物,其由5重量%的Q10、9重量%的α-硫辛酸、5重量%的甘油三酯和81重量%的聚山梨酯80组成。
10.根据权利要求1或2的浓缩物,其由2重量%的Q10、8重量%的α-硫辛酸、6重量%的甘油三酯和84重量%的聚山梨酯80组成。
11.制备根据前述权利要求中任一项的浓缩物的方法,其中首先获得由Q10、聚山梨酯80和甘油三酯组成的溶解物,随后获得由α-硫辛酸和聚山梨酯80或聚山梨酯20组成的溶解物,然后将Q10-溶解物与α-硫辛酸-溶解物在较低温度下混合,并拌和成均匀的物料,其中在比溶解Q10的温度高的温度下获得α-硫辛酸-溶解物。
12.根据权利要求11的方法,其中所述将Q10-溶解物与α-硫辛酸-溶解物混合时所处于的较低温度为60℃。
13.根据权利要求11的方法,其中所述获得α-硫辛酸-溶解物时所处于的温度为100℃。
14.根据权利要求11的方法,其中所述溶解Q10的温度为85℃。
15.根据权利要求11的方法,其中将2份的Q10溶解物与1份的α-硫辛酸-溶解物混合。
16.根据权利要求11的方法,其中将1.8份的Q10溶解物与1份的α-硫辛酸-溶解物混合。
17.根据权利要求1或2的浓缩物,其被以1份的浓缩物对0.1至5000份的饮料这样的比例添加入不含酒精的饮料中。
18.根据权利要求1或2的浓缩物,其被以1份的浓缩物对0.1至500份的食品这样的比例添加入奶制品、蜂蜜或植物油中。
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WO2010008475A2 (en) * | 2008-06-23 | 2010-01-21 | Virun, Inc. | Compositions containing nono-polar compounds |
US10058117B2 (en) * | 2009-11-23 | 2018-08-28 | Randall Scott Hickle | Dietary health food composition, package and method of use |
WO2014132134A1 (en) * | 2013-02-28 | 2014-09-04 | Pronova Biopharma Norge As | A composition comprising a lipid compound, a triglyceride, and a surfactant, and methods of using the same |
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ES2340403T3 (es) | 2010-06-02 |
RU2437584C2 (ru) | 2011-12-27 |
WO2006018301A8 (de) | 2007-03-01 |
WO2006018301A1 (de) | 2006-02-23 |
US20060287384A1 (en) | 2006-12-21 |
EP1781119A1 (de) | 2007-05-09 |
JP2007513994A (ja) | 2007-05-31 |
EP1781119B1 (de) | 2010-01-27 |
ATE456308T1 (de) | 2010-02-15 |
DE502005008953D1 (de) | 2010-03-18 |
CN101001543A (zh) | 2007-07-18 |
RU2007109774A (ru) | 2008-09-27 |
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