CN104812250A - 粉状制剂 - Google Patents
粉状制剂 Download PDFInfo
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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
- A61K31/185—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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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23D—EDIBLE OILS OR FATS, e.g. MARGARINES, SHORTENINGS, COOKING OILS
- A23D7/00—Edible oil or fat compositions containing an aqueous phase, e.g. margarines
- A23D7/005—Edible oil or fat compositions containing an aqueous phase, e.g. margarines characterised by ingredients other than fatty acid triglycerides
- A23D7/0053—Compositions other than spreads
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23D—EDIBLE OILS OR FATS, e.g. MARGARINES, SHORTENINGS, COOKING OILS
- A23D7/00—Edible oil or fat compositions containing an aqueous phase, e.g. margarines
- A23D7/01—Other fatty acid esters, e.g. phosphatides
- A23D7/011—Compositions other than spreads
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23D—EDIBLE OILS OR FATS, e.g. MARGARINES, SHORTENINGS, COOKING OILS
- A23D9/00—Other edible oils or fats, e.g. shortenings, cooking oils
- A23D9/02—Other edible oils or fats, e.g. shortenings, cooking oils characterised by the production or working-up
- A23D9/04—Working-up
- A23D9/05—Forming free-flowing pieces
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
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- Life Sciences & Earth Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
- General Preparation And Processing Of Foods (AREA)
- Edible Oils And Fats (AREA)
- Fats And Perfumes (AREA)
Abstract
本发明涉及包含粉末颗粒的粉状制剂。这些粉末颗粒包含多不饱和油,尤其是多不饱和脂肪酸,且所述粉末同时展示出卓越的感官性状、细粒结构和高油负载。
Description
本文所公开的本发明的实施方式涉及包含粉末颗粒的粉状制剂。这些粉末颗粒包含多不饱和油,尤其是多不饱和脂肪酸。所述粉末同时展示出卓越的感官性状、细粒结构和高油负载。
在最近几年期间,多不饱和油、尤其是多不饱和脂肪酸(PUFA)作为膳食补充剂已吸引了大量关注。现今,存在下述合理证据:增加PUFA的膳食水平对健康具有有益影响并能够通过影响血压、动脉硬化和血栓形成来降低冠心病的死亡率。
由于多不饱和油具有多于一个碳-碳双键这一事实,其易于被氧化。随着双键数目的增加,多不饱和油经受增加的氧化降解和不期望的“异味”(主要是鱼腥气味和味道)发展。当这些油必须被掺入终端市场产品中时,这些不期望的气味和味道可能是挑战。
因此,一直需要提供如何配制多不饱和油的改进方法以使它们稳定(抗氧化),在更长的贮存阶段期间也是如此,且它们不具有任何不期望的“异味”。
出乎意料地,已发现下述乳剂,其包含
(a)至少一种多不饱和油,和
(b)至少一种乳化剂,和
(c)至少一种无乳化性的碳水化合物,和
(d)任选地至少一种助剂,
利用超临界干燥条件干燥所述乳剂,就多不饱和油的稳定性而言,其具有卓越的性能。
因此,本发明的一些实施方式涉及下述粉末颗粒,其包含
(i)乳剂,所述乳剂包含
(a)至少一种多不饱和油,和
(b)至少一种乳化剂,和
(c)至少一种无乳化性的碳水化合物,和
(d)任选地至少一种助剂,和
(ii)气室(gas cell),所述气室包含惰性气体或惰性气体的混合物。这些粉末颗粒(本身和以制剂形式)稳定且不具有不期望的异味。根据本发明的粉末颗粒包含多不饱和油,所述多不饱和油可单独或作为油的混合物被使用。多不饱和油优选地为PUFA。优选的是具有4个碳-碳双键的C18-22PUFA。
根据双键在分子的碳链中的位置,PUFA被分类为n-9、n-6或n-3PUFA。n-6PUFA的实例为亚油酸(C 18∶2)、花生四烯酸(ARA,C20∶4)、γ-亚麻酸(GLA,C 18∶13)和二高-γ-亚麻酸(DGLA,C 20∶3)。n-3PUFA的实例为α-亚麻酸(C 18∶13)、二十碳五烯酸(EPA,C 20∶5)和二十二碳六烯酸(DHA,C 22∶6)。特别地,近年来EPA和DHA已吸引了食品行业的兴趣。这两种脂肪酸的最可用来源是鱼和从其中提取的海产动物油。
在一种实施方式中,至少一种具有4个碳-碳双键的C18-22PUFA选自二十二碳六烯酸(“DHA”)、二十碳五烯酸(“EPA”)、花生四烯酸(“ARA”)、Ω-3二十二碳五烯酸(“DPA n-3”)和Ω-6二十二碳五烯酸(“DPA n-6”)。在一些实施方式中,油包含Ω-3PUFA。在其它实施方式中,Ω-3PUFA选自DHA、EPA、DPA n-3和它们的混合物。
如上所述,油可获自多种来源包括,例如,水产动物,例如,鱼、海产哺乳动物和甲壳纲动物(例如磷虾和其它磷虾目动物);动物来源包括,例如,动物组织包括例如脑、肝脏、眼和动物产品包括,例如,卵和乳;微藻类;植物;和/或种子。在一种实施方式中,油获自鱼、微藻类、植物或种子。
显然,粉末颗粒中使用的油即使用于相同粉末中时,也可来自不同来源。
基于粉末颗粒的总重量,粉末中的油含量为至少5重量-%(wt-%)。优选地,其多于10wt-%。基于粉末颗粒的总重量,优选的范围为5-60wt-%的至少一种多不饱和油。
粉末颗粒还包含至少一种乳化剂。可使用单一的乳化剂以及乳化剂的混合物。乳化剂可以为碳水化合物,单-、二-、寡-、多糖,改性(食物)淀粉。所述乳化剂的实例即Q-naturaleTM(来自National Starch)。基于粉末颗粒的总重量,乳化剂含量为至少2wt-%。基于粉末颗粒的总量,优选的范围为2-45wt-%的至少一种乳化剂。
此外,根据本发明的粉末颗粒还包含至少一种无乳化性的碳水化合物。可使用一种无乳化性的碳水化合物以及无乳化性的碳水化合物的混合物。所述无乳化性的碳水化合物即为麦芽糖糊精和/或海藻糖。基于粉末颗粒的总重量,无乳化性的碳水化合物的含量为至少5wt-%。基于粉末颗粒的总量,优选的范围为5-55wt-%的至少一种无乳化性的碳水化合物。
此外,粉末颗粒可包含一种或多种助剂。所述助剂能够实现宽范围的功能。所述助剂可被用于改善粉末颗粒和/或粉末颗粒的生产和/或粉末掺入其中的制剂和/或所述制剂的生产。所述助剂的实例为抗氧化剂、抗微生物剂、pH-缓冲剂、螯合剂、染料、填充剂等。
基于粉末颗粒的总重量,助剂含量为至多20wt-%。
此外,粉末颗粒包含气室,所述气室包含惰性气体或惰性气体的混合物。这些小室源于超临界干燥工艺,该工艺利用惰性气体进行。优选地,利用CO2。
与一个粉末颗粒的尺寸相比,气室的尺寸(直径,或在非球形小室情况下最长维度)通常很小。粉末颗粒的尺寸在100-600nm范围内。气室尺寸与颗粒尺寸的比率为至少1∶100。
通过超临界干燥来干燥根据本发明的粉末颗粒。通过惯常和普遍已知的程序进行随后被干燥的乳剂的生产。根据本领域已知的方法进行超临界干燥,例如已公开的国际申请WO 02/102947、WO 2011/134627和WO07/024133所证明的那些,每个申请的全部内容通过引用被明确并入本文。
通常,利用CO2(临界点=7.39Mpa下304.25K或1072psi下31.1℃)或氟利昂(临界点≈3.5-4Mpa下300K或500-600psi下25-0℃)进行超临界干燥。
根据本发明的粉末颗粒可被用于使用多不饱和油的任何应用领域中。例如,粉末颗粒可被用于食品、饲料和/或个人护理应用中。粉末颗粒的量涉及具体应用中期望的多不饱和油的量。
因此,本发明的另一实施方式涉及粉末颗粒(如上所限定)在食物、饲料和/或个人护理产品中的用途。
产品可以为任何形式(液体、固体或凝胶状)。优选的是下述产品,其为液体(例如,饮料,尤其是软饮料)。
此外,本文中所公开的某些实施方式涉及包含根据本发明的粉末颗粒(如上所限定)的食物、饲料和/或个人护理产品。
下述实施例阐释了本发明。
实施例中的所有部分和百分比均涉及重量(除非另外指出)且温度以℃给出(除非另外指出)。
实施例
实施例1
在第一步骤中,生产含有如表1中列出的所有成分的乳剂:
表1.
然后,根据WO 07/024133中公开的技术,利用CO2超临界干燥这种乳剂。
颗粒的平均粒度为327nm。颗粒展示出极好的均匀性。
实施例2
在第一步骤中,生产含有如表2中列出的所有成分的乳剂:
表2.
然后,根据WO 07/024133中公开的技术,利用CO2超临界干燥这种乳剂。
颗粒的平均粒度为287nm。颗粒展示出极好的均匀性。
实施例3
将根据上述实施例1和2的两种粉末掺入葡萄汁(DHA含量为32mg/份)中。未检测到鱼腥味。
实施例4
将根据上述实施例1和2的两种粉末掺入可乐饮料(DHA含量为32mg/份)中。未检测到鱼腥味。
Claims (9)
1.粉末颗粒,其包含
(i)乳剂,所述乳剂包含
(a)至少一种多不饱和油,和
(b)至少一种乳化剂,和
(c)至少一种无乳化性的碳水化合物,和
(d)任选地至少一种助剂,和
(ii)气室,所述气室包含惰性气体或惰性气体的混合物。
2.根据权利要求1的粉末颗粒,其中所述多不饱和油选自由EPA、ARA、DHA、DPA和ALA组成的组。
3.根据权利要求1的颗粒,其中所述乳化剂选自由碳水化合物,单-、二-、寡-、多糖,改性(食物)淀粉组成的组。
4.根据权利要求1的颗粒,其中所述助剂选自由抗氧化剂、抗微生物剂、pH-缓冲剂、螯合剂、染料、填充剂组成的组。
5.粉末颗粒,其包含
(i)乳剂,所述乳剂包含
(a)基于所述粉末颗粒的总量,5-60wt-%的至少一种多不饱和油,和
(b)基于所述粉末颗粒的总量,2-45wt-%的至少一种乳化剂,和
(c)基于所述粉末颗粒的总量,5-55wt-%的至少一种无乳化性的碳水化合物,和
(d)基于所述粉末颗粒的总量,至多20wt-%的任选地至少一种助剂。
6.根据权利要求1的粉末颗粒,其中所述气室包含CO2。
7.根据权利要求1的粉末颗粒,其中所述气室与所述颗粒的尺寸的尺寸比率为至少1∶100。
8.根据权利要求1-7中任一项的的粉末颗粒在食物产品、饲料产品和/或个人护理产品的生产中的用途。
9.食物产品、饲料产品和/或个人护理产品,其包含根据在前权利要求中任一项的粉末颗粒。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261730636P | 2012-11-28 | 2012-11-28 | |
US61/730,636 | 2012-11-28 | ||
PCT/EP2013/075007 WO2014083124A1 (en) | 2012-11-28 | 2013-11-28 | Powderous formulation |
Publications (1)
Publication Number | Publication Date |
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CN104812250A true CN104812250A (zh) | 2015-07-29 |
Family
ID=49681028
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CN201380061520.7A Pending CN104812250A (zh) | 2012-11-28 | 2013-11-28 | 粉状制剂 |
Country Status (7)
Country | Link |
---|---|
US (1) | US9918952B2 (zh) |
EP (1) | EP2925153A1 (zh) |
JP (1) | JP2016503303A (zh) |
KR (1) | KR20150089015A (zh) |
CN (1) | CN104812250A (zh) |
BR (1) | BR112015011957A2 (zh) |
WO (1) | WO2014083124A1 (zh) |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA899710A (en) * | 1972-05-09 | H. Bundus Robert | Fat containing injected gas | |
WO2007024133A1 (en) * | 2005-08-23 | 2007-03-01 | Feyecon Development & Implementation B.V. | Process for the preparation of encapsulates through precipitation |
WO2010039036A1 (en) * | 2008-10-01 | 2010-04-08 | Friesland Brands B.V. | Double emulsion and method to produce such |
EP2181604A1 (en) * | 2008-11-04 | 2010-05-05 | Feyecon Development & Implementation B.V. | Dispersion structuring agent |
WO2010149759A1 (en) * | 2009-06-24 | 2010-12-29 | Basf Se | Microparticles comprising a fat soluble fraction comprising dha and their production |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0716598B2 (ja) * | 1987-05-26 | 1995-03-01 | 雪印乳業株式会社 | 油脂類の乳化方法 |
JPH0748992B2 (ja) * | 1990-04-16 | 1995-05-31 | 日本油脂株式会社 | 血栓防止用粉末組成物 |
US6428832B2 (en) * | 1996-03-26 | 2002-08-06 | Dsm N.V. | Late addition of PUFA in infant formula preparation process |
EP1270710A1 (en) | 2001-06-19 | 2003-01-02 | Feyecon Development & Implementation B.V. | A method of processing lipid materials |
JP5767317B2 (ja) | 2010-04-30 | 2015-08-19 | ローダース・クロクラーン・ベスローテンフェンノートシャップ | 食用油組成物 |
-
2013
- 2013-11-28 KR KR1020157013790A patent/KR20150089015A/ko not_active Application Discontinuation
- 2013-11-28 JP JP2015543482A patent/JP2016503303A/ja active Pending
- 2013-11-28 WO PCT/EP2013/075007 patent/WO2014083124A1/en active Application Filing
- 2013-11-28 CN CN201380061520.7A patent/CN104812250A/zh active Pending
- 2013-11-28 US US14/647,633 patent/US9918952B2/en not_active Expired - Fee Related
- 2013-11-28 BR BR112015011957A patent/BR112015011957A2/pt not_active Application Discontinuation
- 2013-11-28 EP EP13798648.5A patent/EP2925153A1/en not_active Withdrawn
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA899710A (en) * | 1972-05-09 | H. Bundus Robert | Fat containing injected gas | |
WO2007024133A1 (en) * | 2005-08-23 | 2007-03-01 | Feyecon Development & Implementation B.V. | Process for the preparation of encapsulates through precipitation |
WO2010039036A1 (en) * | 2008-10-01 | 2010-04-08 | Friesland Brands B.V. | Double emulsion and method to produce such |
EP2181604A1 (en) * | 2008-11-04 | 2010-05-05 | Feyecon Development & Implementation B.V. | Dispersion structuring agent |
WO2010149759A1 (en) * | 2009-06-24 | 2010-12-29 | Basf Se | Microparticles comprising a fat soluble fraction comprising dha and their production |
Also Published As
Publication number | Publication date |
---|---|
BR112015011957A2 (pt) | 2017-07-11 |
EP2925153A1 (en) | 2015-10-07 |
US20150320714A1 (en) | 2015-11-12 |
KR20150089015A (ko) | 2015-08-04 |
WO2014083124A1 (en) | 2014-06-05 |
US9918952B2 (en) | 2018-03-20 |
JP2016503303A (ja) | 2016-02-04 |
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