CN113710262B - 黄芩组合物和用于味道调节的方法 - Google Patents
黄芩组合物和用于味道调节的方法 Download PDFInfo
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- CN113710262B CN113710262B CN202080029052.5A CN202080029052A CN113710262B CN 113710262 B CN113710262 B CN 113710262B CN 202080029052 A CN202080029052 A CN 202080029052A CN 113710262 B CN113710262 B CN 113710262B
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- extract
- scutellaria baicalensis
- consumable
- taste
- wogonin
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Abstract
描述了一种黄芩提取物及糖酶处理的黄芩提取物和从黄芩中获得的黄酮,用于在组合物和方法中使用,所述组合物方法用于改善含有具有涩味、苦味或异味的组分的消耗品的味道。
Description
引言
本申请要求于2019年4月15日提交的美国专利申请序列号62/833,839的优先权的权益,将其内容通过援引以其全文并入本文。
背景技术
黄芩(Scutellaria)属含有由多年生的和一年生的草本代表的超过350个种,其中一些由于它们的抗炎性、抗病毒、镇静、抗血栓形成和抗氧化的作用而被广泛用于传统医学(尤其在中国、韩国、和日本)中。这些作用与黄酮类的含量相关联,其中黄芩甙、黄芩素、和汉黄芩苷是主要的化合物。黄芩素和黄芩甙表现出优异的自由基清除能力,并且已被证明可在心肌细胞和神经元细胞中减弱氧化应激。此外,汉黄芩苷具有强大的对抗脂质过氧化的活性和对组胺和IgE生产的抑制作用。在这方面,CN 100423736 C建议在用于治疗流感的组合物中将黄芩甙与盐酸金刚烷胺相结合使用。
KR 101169587 B1建议通过用乳酸细菌发酵提取物从而减少所述提取物的苦味来改善黄芩(Scutellaria baicalensis)提取物的味道。
US 8435586 B2公开了通过向醇中添加2-苯基-色烯-4-酮来加强所述醇的感觉印象的方法。
CN 10480054 A公开了用于治疗苦味的药物,所述药物包括夏枯草(Prunellavulgaris)、金银花、菊花(Dendranthema morifolium)、中国枸杞、地黄(RadixRehmanniae)、麦冬(Radix Ophiopogonis)、龙胆(Radix Gentianae)、栀子(Gardeniajasminoides)、黄芩、和柴胡(Radix Bupleuri)。
发明内容
本发明提供了一种消耗品,所述消耗品包括具有涩味、苦味或异味的组分;和黄芩提取物或其一种或多种黄酮。本发明还提供了一种用于改善消耗品的味道的方法,所述方法通过向具有有涩味、苦味或异味的组分的消耗品以有效减少或抑制所述涩味、苦味或异味的量添加黄芩提取物或其一种或多种黄酮。具有涩味、苦味或异味的组分可以包括蛋白质、碳水化合物甜味剂、人造甜味剂或防腐剂。在一些方面,所述黄芩提取物是糖酶(carbohydrase)处理的黄芩(Scutellaria)提取物或黄芩(Scutellaria baicalensis)提取物。在其他方面,所述一种或多种黄酮包括黄酮苷元(例如,黄芩素、汉黄芩素、千层纸素A或其组合)和/或黄酮糖苷(黄芩甙、汉黄芩苷、千层纸素A葡糖苷酸或其组合)。在某些实施例中,所述黄芩提取物或其一种或多种黄酮以0.01ppm或更大的量存在;以在0.05ppm至500ppm的范围内的量存在;以在0.1ppm至100ppm的范围内的量存在;或以在0.5ppm至50ppm的范围内的量存在。在又一个方面,所述消耗品是食物产品、药物组合物、膳食补充剂、保健营养品、牙齿卫生组合物、桌面甜味剂、饮料、或美容产品。
具体实施方式
现在已经发现,黄芩提取物及其糖酶处理的提取物和从其分离的黄酮有效地遮盖消耗品产品的苦味、涩味和异味。特别地,已经示出,黄芩(S.baicalensis)提取物的黄酮苷元和黄酮糖苷减少或抑制与蛋白质、碳水化合物甜味剂、人造甜味剂、和/或防腐剂(例如苯甲酸或山梨酸)有关的苦味、涩味和异味。因此,本发明提供消耗品和方法,所述消耗品和方法包括黄芩提取物和/或从所述黄芩提取物分离的一种或多种黄酮作为添加剂以通过减少或抑制所述消耗品的涩味、苦味和/或异味改善所述消耗品的味道。
如本文所使用的,黄芩提取物是来自黄芩属植物的根或空气部分的提取物。在一些实施例中,所述黄芩属植物是黄芩、侧花黄芩(S.lateriflora)、吕宋黄芩(S.racemosa)、具单眼黄芩(S.ocellate)、高山黄芩(S.alpine)、盔状黄芩(S.galericulata)、绒毛黄芩(S.tomentosa)、S.wrightii、具须黄芩(S.barbata)、S.litwinowii、滇黄芩(S.amoena)、平卧黄芩(S.prostrata)、S.rivularis、变色黄芩(S.discolor)、多枝黄芩(S.ramosissima)、S.havanensis或仰卧黄芩(S.supina)。在某些实施例中,所述黄芩属植物是黄芩(也称为美黄芩(Skullcap))。在其他实施例中,所述黄芩提取物是来自所述植物的根的提取物。在特别的实施例中,本发明的所述黄芩提取物是黄芩或侧花黄芩的根的提取物。
优选地,所述黄芩提取物富含黄酮,特别是黄酮糖苷例如黄芩甙(5,6-二羟基-7-O-葡糖苷酸黄酮;CAS No.21967-41-9)、汉黄芩苷(汉黄芩素7-O-β-D-葡糖苷酸;CASNo.51059-44-0)、5,7-二羟基-6-甲氧基黄酮-7-O-β-D-葡萄糖醛酸吡喃糖苷(千层纸素A葡糖苷酸);和/或黄酮苷元例如黄芩素(5,6,7-三羟基黃酮或5,6,7-三羟基-2-苯基-色烯-4-酮;CAS No.491-67-8)、汉黄芩素(5,7-二羟基-8-甲氧基黄酮或5,7-二羟基-8-甲氧基-2-苯基-4H-色烯-4-酮;CAS No.632-85-9)和/或5,7-二羟基-6-甲氧基黄酮(千层纸素A)(表1)。
表1
虽然黄芩属植物已经示出包括一种或多种黄芩甙、黄芩素、汉黄芩苷、汉黄芩素(Zhao等人(2016)Sci.Bull.[科学通报](北京)61(18):1391-8;Gao等人(2008)J.Pharm.Pharm.Sci.[药物科学杂志]11(1):77-87;Cole等人(2008)Planta Med.[植物医学].74(4):474-81;Kikuchi等人(1991)Chem.Pharm.Bull.[化学与药学通报]39(1):199-201;Kosakowska等人(2016)HerbaPolonica[波兰古生物学报]62(3):7-19;Islam等人(2010)Metabolomics[代谢组学]7(3):446-53;Tayarani-Najarani等人(2012)Braz.J.Pharmacog.杂志22(2):268-76;Lin&Shieh(1996)Am.J.Chin.Med.[美洲中国医药杂志]24(1):31-6;Marrero,等人(2015)Internatl.J.Pharmaceut.Sci.Rev.Res.[国际药学科学评论与研究杂志]30(2):104-8),这些化合物也已经报道在木蝴蝶(Oroxylumindicum)(印度喇叭花(Indian trumpet flower))(Raghu等人(2013)J.PharmacogPhytochem.[药理学植物化学杂志]2(3):23-27;Majeed等人(2017)J.Liq.Chromatog.Rel.Technol.[液相色谱与相关技术杂志]40(14):732-40),黄芩素已经在麝香草(Thymus vulgaris)中被发现(Fujita等人(2005)Microbiol.Immunol.[微生物免疫学]49(4):391-6),以及汉黄芩苷已经从假马齿苋(Bacopa monnieri)和冬红(Holmskioldia sanguinea)(冬红Chinese hatplant)(Chaudhuri等人(2004)Phytother.Res.[植物疗法研究]18(2):114-7)中分离出。因此,本发明的所述黄酮还可以从一种或多种这些替代的来源中获得。
黄芩提取物可以通过以下方式获得:研磨、碾磨或粉碎干燥的黄芩植物物质(例如,干燥的黄芩根)以获得粉末,以及随后将所述粉末悬浮于50%-75%乙醇(优选地约70%乙醇)中持续足以从所述植物物质中提取所期望的黄酮的时间(例如,30分钟至24小时),以及过滤所述提取物以移除不溶解的植物物质(Yu等人(2013)Oncol.Rep.[肿瘤学报告]30:2411-8;Sun等人(2016)Molecules[分子学]21(8):1067;Khan等人(2017)Sci.Rep.[科学报告]7:43789)。
黄酮糖苷和黄酮苷元可以优选地通过用乙酸锌沉淀从黄芩提取物中分离,其pH已经被用至少约14.7mM氢氧化铵调整(Sun等人(2016)Molecules[分子学]21(8):1067)。可替代地,使用乙酸乙酯、水、1-正-辛基-3-甲基咪唑六氟磷酸盐([C4mim][PF6])(5:5:0.2,v/v)作为两相溶剂系统,黄芩甙和汉黄芩苷可以从黄芩的粗提取物中纯化,获得的纯度分别为99.3%和99.1%,(Wang等人(2013)J.Liquid Chromatography Rel.Technol.[液相色谱与相关技术杂志]37(16):2275-86)。此外,树脂吸附可以用于从黄芩提取物分离和纯化黄芩甙和汉黄芩苷。例如,在用HPD-100树脂进行一轮处理后,黄芩甙和汉黄芩苷获得的回收率分别为85.7%和65.6%(Du等人(2012)J.Chromatogr.BAnalyt.Technol.Biomed.LifeSci.[生物医学和生命科学中的色谱分析技术杂志]908:143-9)。
其他用于分离黄酮的合适方法可以包括基于分子大小、电荷、溶解度和/或极性的色谱分级。根据色谱方法的类型,柱色谱可以用由例如右旋糖酐、琼脂糖、聚丙烯酰胺或二氧化硅组成的基质材料进行,且可以包括以下溶剂:例如二甲亚砜、吡啶、水、二甲基甲酰胺、甲醇、盐水、二氯乙烷、氯仿、丙醇、乙醇、异丁醇、甲酰胺、亚甲基二氯(methylenedichloride)、丁醇、乙腈、异丙醇、四氢呋喃、二氧六环、氯仿/二氯甲烷(dichloromethane)等等。典型地,色谱步骤的产物以多个级分收集,然后使用任何合适的分析技术(例如薄层色谱、质谱分析法)测试所述产物的所期望的化合物的存在。然后可以选择富含所期望的黄酮的级分用于进一步的纯化。在某些实施例中,分离的黄酮的纯度是至少50%、60%、70%、80%、90%、95%、或99%。
可替代地,本发明的所述黄酮可以是化学合成的。例如,黄芩素可以经由蜡菊查耳酮(Helilandin B)(Chen等人(2010)J.Asian Nat.Prod.Res.[亚洲天然产物研究杂志]12(2):124-8)合成,随后进行Koenigs-Knorr糖基化和温和碱性脱保护以生产黄芩甙(Li等人(2015)Tetrahedron Lett.[四面体快报]56(24):3816-9)。同样地,汉黄芩素可以使用2,4-二苄基氧基-6-羟基苯基乙酮和苯甲醛作为起始材料合成(Yuan等人(2016)Chin.J.Organ.Chem.[中国有机化学杂志]36(12):2960),随后进行糖基化以生产汉黄芩苷。
作为另外的替代物,本发明的所述黄酮可以通过重组手段生产。举例来说,黄芩素可以从可用的苯丙氨酸和酪氨酸在重组大肠杆菌细胞中生产(Jianhua等人(2019)Metab.Eng.[代谢工程]52:124-133)。此外,使用稳定表达人CYP1A1酶的全酵母细胞的选择性5,7-二羟黄酮的C6-羟基化已经被用于从白杨素生产黄芩素(Ibidapo等人(2017)J.Agric.Food Chem.[农业与食品化学杂志]65(34):7440-46)。
当黄芩的富含黄酮糖苷的提取物或其分离的黄酮糖苷经受用一种或多种碳水化合物处理,黄酮糖苷被转化成抑制增强的味道调节活性的黄酮苷元。因此,本发明还提供了含有糖酶处理的黄芩提取物、或其一种或多种黄酮苷元的消耗品。在一些实施例中,所述糖酶处理的黄芩(Scutellaria)提取物是糖酶处理的黄芩(S.baicalensis)提取物。在特别的实施例中,所述糖酶处理的黄芩提取物富含一种或多种黄酮苷元,特别是黄酮苷元。
所述糖酶处理的黄芩提取物和/或其的黄酮苷元可以通过用一种或多种糖酶处理黄芩提取物或黄芩植物物质(例如,干燥的根粉末)或黄酮糖苷生产。如本文所使用的,“糖酶”是指任何将碳水化合物水解成单糖的酶。因为在水存在下,糖酶作为催化剂将糖键水解分解为更小的单元(例如葡萄糖或蔗糖),糖酶被认为是水解酶。在一些实施例中,糖酶是一种糖酶或糖酶的组合(即,糖酶的混合物)。所述糖酶或糖酶混合物典型地选自以下的组:糖类酶(saccharidase)、淀粉酶、外切淀粉酶、β-淀粉酶、葡糖淀粉酶、内切淀粉酶、α-淀粉酶、葡聚糖酶、阿拉伯糖酶、半纤维素酶、木聚糖酶、和纤维素酶。在某些实施例中,所述糖酶有水解(1,3)-或1,4-键的内-β-葡聚糖酶活性。在一些实施例中,所述糖酶或糖酶混合物包括至少纤维素酶(例如,从丹麦诺维信公司(Novozyme)获得的XW-G-F纤维素酶),其已经示出从汉黄芩苷和黄芩甙分别产出汉黄芩素和黄芩素(Yu等人(2013)Oncol.Rep.[肿瘤报告]30:2411-8)。来自短乳杆菌(Lactobacillus brevis)的重组的β-葡萄糖醛酸酶也已经示出在3小时内,将黄芩甙和汉黄芩苷分别完全转化成黄芩素和汉黄芩素(Sung等人(2009)J.Microbiol.Biotechnol.[微生物学和生物技术杂志]19(12):1650-5)。还参见KR20100001908 A。在本发明中使用的示例性糖酶在L商标(诺维信,丹麦)下出售。
在水存在下,通过将糖酶添加至黄芩提取物或黄酮糖苷中持续一段时间,并且在足以增加还原糖pH和温度,生产了糖酶处理的黄芩提取物和黄酮苷元。在一些实施例中,在水存在下(例如,5-50份),将黄芩提取物或黄酮糖苷(例如,1份)与糖酶或糖酶混合物(例如0.005至0.1份)组合,并且孵育约30分钟至48小时的时间,更优选地约2小时至约24小时;pH在约3至约6的范围内,或更优选地在约3.3至约5.5的范围内;并且温度在约25℃与55℃之间,或更优选地在约30℃与50℃之间。
本文所描述的黄芩提取物和黄酮通过遮盖消耗品的涩味、苦味和/或异味改善消耗品的味道和/或香味,所述消耗品有赋予涩味、苦味和/或异味的组分。在这方面,消耗品包括任何食物产品、药物组合物、膳食补充剂、保健营养品、牙齿卫生组合物、桌面甜味剂、饮料、或美容产品,这些产品包括涩味、苦味和/或异味的组分。优选地,具有有涩味、苦味或异味的组分的所述消耗品通过添加以下物质改进:(a)黄芩提取物、(b)糖酶处理的黄芩提取物、(c)黄芩提取物、(d)糖酶处理的黄芩提取物、(e)黄芩根提取物、(f)糖酶处理的黄芩根提取物、(g)黄芩根提取物、(h)糖酶处理的黄芩根提取物、(i)从黄芩提取物或其他合适来源获得的一种或多种黄酮、(j)从黄芩根提取物获得的一种或多种黄酮、(k)从黄芩提取物获得的一种或多种黄酮、(l)从黄芩根提取物获得的一种或多种黄酮、(m)从黄芩提取物或其他合适来源获得的一种或多种黄酮苷元、(n)从黄芩根提取物获得的一种或多种黄酮苷元、(o)从黄芩提取物获得的一种或多种黄酮苷元、(p)从黄芩根提取物获得的一种或多种黄酮苷元、(q)从黄芩提取物或其他合适来源获得的一种或多种黄酮糖苷、(r)从黄芩根提取物获得的一种或多种黄酮糖苷、(s)从黄芩提取物获得的一种或多种黄酮糖苷、(t)从黄芩根提取物获得的一种或多种黄酮糖苷、(u)黄芩素、汉黄芩素、千层纸素A、或其组合、(v)黄芩甙、汉黄芩苷、千层纸素A葡糖苷酸、或其组合、(w)黄芩素、汉黄芩素、千层纸素A、黄芩甙、汉黄芩苷、千层纸素A葡糖苷酸、或其组合、或(x)黄芩根提取物或与一种或多种黄芩素、汉黄芩素、千层纸素A、黄芩甙、汉黄芩苷、或千层纸素A葡糖苷酸组合的糖酶处理的黄芩根提取物。
如本文所使用的术语“遮盖”(“mask”或“masking”)被定义为通过添加黄芩提取物和/或黄酮来覆盖、掩盖和/或模糊涩味、苦味和/或异味,其中与涩味、苦味和/或异味有关的所述组分保持不变,但是其令人不愉快的味道不会被消耗所述消耗品人感知到。与不包括本发明的黄芩提取物和/或黄酮作为外源的添加剂的比较消耗品的味道和/或风味特征相比,包括本发明的黄芩提取物和/或黄酮的消耗品的味道和/或风味特征可以改善或增强(例如,1.5-、2.0-、2.5-、5.0-、7.5-或10-倍改善)。理想地,与不包括所述黄芩提取物和/或黄酮的消耗品相比,黄芩提取物和/或黄酮减少异味味道至少约10%、20%、30%、40%、50%、60%、70%、80%、90%、或95%、或从约60%至约99%、或可替代地从约20%至约50%。
在某些实施例中,本发明的黄芩提取物和/或黄酮减少、抑制或遮盖消耗品所述涩味、苦味和/或异味。异味(“off-flavor”或“off-taste”)是指消耗品的苦的、酸的、腥的、泥土味的、涩的、金属的和/或令人不愉快的味道。涩味(“Astringent”或“astringency”)是指在口腔中感觉的皱褶的或口干的感觉。苦味(“Bitter”或“bitterness”)是指主要在舌的背后感知的四种基础味道(通常被描述为刺激性的、辛辣的、或令人不快的)之一。
具有涩味、苦味和/或异味的组分可以是固有地存在于消耗品中的蛋白质、碳水化合物甜味剂、人造甜味剂或防腐剂(例如,含有水果的食物产品)或所述组分被添加至消耗品中。有涩味、苦味和/或异味的蛋白质可以包括消耗品的氨基酸、蛋白质水解物或蛋白质组分,特别是植物蛋白质或食草动物的奶。本发明的甜味剂包括但不限于碳水化合物甜味剂,例如蔗糖、果糖、葡萄糖、高果糖玉米糖浆(含有果糖和葡萄糖)、木糖、阿拉伯糖、鼠李糖,以及糖醇,例如赤藓糖醇、木糖醇、甘露醇、山梨糖醇、或肌醇。人造甜味剂包括但不限于天然甜味#2(WO 2012/129451)、甜菊苷、莱鲍迪甙(rebaudioside)A、莱鲍迪甙B、莱鲍迪甙C、莱鲍迪甙D、莱鲍迪甙E、莱鲍迪甙F、杜克甙(dulcoside)A、杜克甙B、甜菊、α-葡糖基甜菊、果糖基甜菊、半乳糖基甜菊、β-葡糖基甜菊、赛门苷(siamenoside)、罗汉果苷(mogroside)IV、罗汉果苷V、罗汉果(Luo Han Guo)甜味剂、莫那甜(monatin)和其盐类、甘草酸和其盐类(例如,如MAGNASWEET中发现的)、仙茅蛋白(curculin)、奇异果甜蛋白(thaumatin)、应乐果甜蛋白(monellin)、马槟榔甜蛋白(mabinlin)、甜味蛋白(brazzein)、hernandulcin、叶甜素(phyllodulcin)、菝葜苷(glycyphyllin)、根皮苷(phloridzin)、三叶苷(trilobtain)、白元参甙(baiyunoside)、水龙骨甜素(osladin)、polypodoside A、皮提罗苷(pterocaryoside)A、皮提罗苷B、无患子倍半萜甙(mukurozioside)、糙苏甙(phlomisoside)I、巴西甘草甜素(periandrin)I、相思子三萜甙(abrusoside)A、甜茶树苷(cyclocarioside)I、或其组合。具有涩味、苦味和/或异味的防腐剂的实例包括但不限于苯甲酸和山梨酸。
当作为外源的添加剂向消耗品添加时,本发明的黄芩提取物和/或黄酮以有效减少或抑制具有涩味、苦味或异味的消耗品的组分的涩味、苦味或异味的量使用。理想地,包括在消耗品中的黄芩提取物和/或黄酮的量不会给消耗品带来任何异味。优选地,存在于消耗品中的黄芩提取物和/或黄酮的量是低至0.01ppm的量、低至0.05ppm的量、低至1ppm的量、低至5ppm的量、低至7.5ppm的量、或低至10ppm的量。黄芩提取物和/或黄酮可以以高至200ppm的量、高至150ppm的量、高至100ppm的量或高至1000ppm的量包括在消耗品内。黄芩提取物和/或黄酮可以进一步存在于由任何一对上述值限定的任何范围内,例如在0.05ppm与150ppm之间、在0.1ppm与100ppm之间、在0.5ppm与50ppm之间、在0.5ppm与500ppm之间。在特别的实施例中,黄芩提取物和/或黄酮在0.2ppm至2ppm的范围内使用。如本文所使用的术语“ppm”意指按重量计或按体积计每百万之几,例如,每升溶液的组分重量(按毫克),即μg/ml。
本发明的黄芩提取物和黄酮已经和多个可能的治疗益处相关,包括例如治疗炎症、发热、咳嗽、痢疾、和高血压。作为有250mg的份量大小的商业补充剂,黄芩根提取物的推荐使用是1-3份每天1-2次。在临床试验研究中,每日三次剂量(350mg)侧花黄芩的施用与任何负面效应无关(Brock等人(2014)Phytother.Res.[植物疗法研究]28(5):692-8)。相似地,健康受试者口服剂量在100-2800mg范围内的黄芩素已经示出是安全且耐受良好的(Li等人(2014)J.Ethnopharmacol.[民族药理学杂志]156:210-5;Pang等人(2016)Clin.DrugInvest.[临床药物研究杂志]36(9):713-724)。鉴于黄芩提取物和/或黄酮以显著低于为实现治疗益处而建议的量使用,因此本组合物不同于在先前领域中描述的药物制剂、膳食补充剂和保健营养品。如此,本发明的所述组合物可以提供无相关药理学活性的味道调节活性。
如本文所使用的短语“食物产品”包括但不限于水果、蔬菜、果汁、肉产品(例如,火腿、培根和香肠)、蛋产品、水果浓缩物、明胶和明胶样产品(例如,果酱、果冻、蜜饯等)、奶产品(例如,冰淇淋、酸奶油和果子露)、糖衣、包括糖蜜的糖浆、玉米产品、小麦产品、黑麦产品、大豆产品、燕麦产品、大米产品和大麦产品、坚果肉和坚果产品、蛋糕、曲奇饼、糖膏(例如,糖果、胶、果味滴剂和巧克力)、口香糖、薄荷、奶油、冰淇淋、馅饼和面包、和饮料(例如咖啡、茶、碳酸软饮品(例如和/>)、非碳酸软饮品、果汁和其他水果饮品、运动饮品(例如/>)、酒精饮料(例如啤酒、红酒和露酒、和/>))。食物产品还包括调味品,例如草药、香料和调料,和增昧剂,例如谷氨酸一钠。食物产品还包括加工的包装产品,例如膳食甜味剂、液体甜味剂、颗粒状香料混合物,所述产品用水重构后提供非碳酸饮品、速溶布丁混合物、速溶咖啡和茶、咖啡增白剂、麦芽奶混合物、宠物食品、牲畜饲料、烟草、以及用于烘焙应用的材料,例如用于制备面包、饼干、蛋糕、煎饼、甜甜圈等的粉末状烘焙混合物。食物产品还包括低脂或低卡食物和几乎不含蔗糖的饮料。尤其优选的食物产品是碳酸饮料。
消耗品还可以是药物组合物。优选的组合物是含有所述黄芩提取物和/或黄酮和一种或多种药学上可接受的赋形剂的药物组合物。这些药物组合物可以用于配制含有一种或多种活性剂(所述活性剂可以产生除味道调节外的生物效应)的药用的药品。所述药物组合物优选地进一步包括产生生物效应或药理作用的一种或多种活性剂。这样的活性剂包括有除味道调节外的活性的药物和生物制剂。这样的活性剂在本领域中是熟知的。参见,例如The Physician's Desk Reference[医师案头参考]。可以根据本领域已知的步骤制备此类组合物,例如,乳以下文献中描述:Remington's Pharmaceutical Sciences[雷明顿的医药科学],Mack Publishing Co.[马克出版公司],宾夕法尼亚州伊斯顿市。在一个实施例中,这种活性剂包括支气管扩张剂、厌食剂、抗组胺剂、营养补充剂、缓泻剂、镇痛剂、麻醉剂、抗酸剂、H2-受体拮抗剂、抗胆碱能剂、止泻剂、缓和剂、镇咳剂、防恶心剂、抗微生物剂、抗细菌剂、抗真菌剂、抗病毒剂、祛痰剂、抗炎剂、解热剂、及其混合物。在一个实施例中,活性剂是解热剂或镇痛剂,例如布洛芬、对乙酰氨基酚或阿司匹林;缓泻剂,例如酚酞二辛基磺基琥珀酸钠;食欲抑制剂,例如苯丙胺、苯丙醇胺、盐酸苯丙醇胺、或咖啡因;抗酸剂,例如碳酸钙;止喘剂,例如茶碱;抗利尿剂,例如盐酸地芬诺酯;抗肠胃气胀的活性剂,例如西甲硅油(simethecon);偏头痛剂,例如酒石酸麦角胺(ergotaminetartrate);精神病治疗剂,例如氟哌啶醇;解痉剂或镇静剂,例如苯巴比妥;抗多动症剂,例如甲基多巴或哌甲酯;安定剂,例如苯并二氮平、羟丙氨酯(hydroxinmeprobramate)或酚噻嗪;抗组胺剂,例如阿司咪唑、马来酸扑尔敏、马来酸吡拉敏(pyridamine maleate)、琥珀酸多西拉敏(doxlaminesuccinate)、马来酸溴苯那敏、枸椽酸苯托沙敏、盐酸氯环力嗪、马来酸非尼拉敏、或酒石酸苯茚胺;减充血剂,例如盐酸苯丙醇胺、盐酸苯肾上腺素、盐酸伪麻黄碱、硫酸假麻黄碱、苯丙醇胺酒石酸氢盐、麻黄碱;β-受体阻滞剂,例如心得安;用于酒精戒断的剂,例如二硫龙(disulfuram);镇咳剂,例如苯佐卡因、右美沙芬、氢溴酸右美沙芬、那可丁(noscapine)、枸橼酸喷托维林、或盐酸氯苯达诺;氟化钠补充剂,例如氟化钠;局部抗生素,例如四环素或氯洁霉素(cleocine);皮质类固醇补充剂,例如泼尼松或泼尼松龙;抗甲状腺肿形成的剂,例如秋水仙碱或别嘌醇;抗癫痫剂,例如苯妥英钠;抗脱水的剂,例如电解质补充剂;抗菌防腐剂,例如十六烷基氯化吡啶鎓;NSAID,例如对乙酰氨基酚、布洛芬、萘普生、或其盐;胃肠的活性剂,例如洛哌丁胺和法莫替丁;生物碱,例如磷酸可待因、硫酸可待因、或吗啡;用于微量元素的补充剂,例如氯化钠、氯化锌、碳酸钙、氧化镁、或其他的碱金属盐或碱土金属盐;维生素;离子交换树脂,例如消胆胺;胆固醇抑制剂或降脂质物质;抗心律不齐剂,例如N-普鲁卡因酰胺;或祛痰剂,例如愈创甘油醚。
在一些实施例中,消耗品是膳食补充剂或保健营养品。具有不期望的味道的此类组合物的实例包括但不限于肠道营养产品(用于治疗营养不足的、创伤、外科手术、克罗恩病、肾脏疾病、高血压、肥胖症等),以改善运动表现、肌肉增强或一般健康、或例如苯酮尿症的先天性代谢缺陷。特别地,此类组合物可以含有有苦味或金属味或余味的一种或多种氨基酸类化合物。此类氨基酸包括但不限于必需氨基酸,例如亮氨酸、异亮氨酸、组氨酸、赖氨酸、甲硫氨酸、苯丙氨酸、苏氨酸、色氨酸、酪氨酸、和缬氨酸的L异构体。
在另外的实施例中,本发明的消耗品是牙齿卫生组合物,含有本发明的黄芩提取物和/或黄酮。牙齿卫生组合物在本领域是已知的,并且包括但不一定限于牙膏、漱口剂、牙菌斑冲洗液、牙线、牙痛缓解剂(例如ANBESOLTM)等。在一个实施例中,牙齿卫生组合物包括一种甜味剂。在另一个实施例中,牙齿卫生组合物包括多于一种甜味剂。在某些实施例中,牙齿卫生组合物包括蔗糖和玉米糖浆、或蔗糖和阿斯巴甜。
在又一个实施例中,本发明的消耗品是含有本发明的黄芩提取物和/或黄酮的美容产品。例如但不是通过限制,美容产品可以是面霜、口红、唇彩等。本发明的其他合适的组合物包括唇膏,例如在商标或BURT'S />唇膏下出售的那些。
本发明通过下文中的非限制性实例进行了更为详细地描述。
实例1:黄芩提取物
黄芩提取物。通过干燥和碾磨黄芩的根获得美黄芩提取物。向干燥的粉末中添加水和乙醇(30:70)。将所得混合物孵育足以提取物所期望的黄酮的时间,且过滤所述混合物以移除不溶解的植物物质。将过滤的溶液随后在喷雾干燥器中干燥和碾磨。
糖酶处理的黄芩提取物。在5至50份水中重悬浮一份干燥的黄芩提取物。将溶液的pH调节至3-6,以及添加0.005至0.1份在L商标(诺维信,丹麦)下出售的糖酶。在30℃-55℃下孵育所述混合物2-48小时然后随后冷却至室温。然后通过移除水使所述溶液浓缩。在一些情况下,浓缩样品被进一步纯化以通过柱色谱获得所期望的黄酮。
对糖酶处理的和未处理的黄芩提取物进行分析以评估存在于提取物中的黄酮的浓度。本分析的结果在表2中呈现。
表2
NQ,由于低浓度而未量化。
本分析指示出未处理的黄芩提取物有高的黄芩甙和汉黄芩苷含量。用生物-转化,大多数黄芩甙被转化为黄芩素;且汉黄芩苷转化为汉黄芩素。还分析了个别化合物的活性用于味道调节活性。本分析指示出黄芩甙和汉黄芩苷抑制一些活性,但黄芩素和汉黄芩素更加有活性。
实例2:味道调节
在不同申请中使用不同量的所述组合物评价由43%黄芩素和11%汉黄芩素组成的味道调节组合物。本分析的结果在表3中呈现。
表3
*味道调节组合物仅由汉黄芩素组成。
Claims (2)
1.一种改善消耗品的味道的方法,所述方法包括向包含具有异味的组分的消耗品添加有效减少或抑制所述异味的量的黄酮,
其中,所述黄酮选自由如下组成的组:黄芩素、汉黄芩素及它们的混合物,
所述具有异味的组分是蛋白质、碳水化合物甜味剂、人造甜味剂或防腐剂,所述防腐剂是苯甲酸或山梨酸,且
所述黄酮以在0.1ppm至50ppm的范围内的量存在,以及
所述消耗品是食物产品、药物组合物或美容产品。
2.如权利要求1所述的方法,其中所述消耗品是膳食补充剂、保健营养品、牙齿卫生组合物、桌面甜味剂或饮料。
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