CN1252708A - 减轻喉痛的组合物 - Google Patents

减轻喉痛的组合物 Download PDF

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CN1252708A
CN1252708A CN98804263A CN98804263A CN1252708A CN 1252708 A CN1252708 A CN 1252708A CN 98804263 A CN98804263 A CN 98804263A CN 98804263 A CN98804263 A CN 98804263A CN 1252708 A CN1252708 A CN 1252708A
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cephrol
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F·J·D·比林－凯利
B·汉克
P·宁阿贝
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Abstract

本发明涉及润喉糖。该润喉糖含有60－95%可食用的壳和5－40%含水填充物,该填充物含有8－95%水和0.001－10%发泡剂,该发泡剂能把分散在该填充物中的喉痛缓解剂包封在泡内。本发明的润喉糖能使喉或鼻刺激长时间缓解。

Description

减轻喉痛的组合物
                          发明领域
本发明涉及用于减轻喉痛或喉刺激以及缓解鼻通道充血的口服组合物，特别是液体夹心的糖果剂(centre-filled confectionery)组合物。
                          发明背景
早已知道，止咳润喉糖形式的产品是用于释放减轻喉痛或刺激的药剂的载体。这些药剂包括止痛剂、止咳药、祛痰剂、清凉剂(如薄荷醇)和暖和剂(warmingagent)(如乙醇或姜醇)。这些药剂可通过吮吸时释放活性剂的润喉糖(throat dorp)或糖锭给药。特别是在挥发性活性剂的情况下，该产品也可通过清洁鼻通道而缓解感冒症状。
例如，EP-A-431,376描述了用于持续释放治疗喉痛的药物的硬糖果剂。这种糖果剂含有氢化异麦芽酮糖和活性剂，活性剂可以是止咳剂或抗组胺剂，也可以是挥发油(如薄荷醇或桉树油)。该糖果剂一般还含有增香剂，如柠檬、蜂蜜或樱桃，该增香剂也可以是薄荷醇或桉树油。
由这种产品达到长时间释放面临的问题之一是将活性剂保持在喉中足够长的时间。然而，现已发现将活性剂包封在泡中可以明显延长由活性剂提供的喉痛缓解。
卵磷脂是众所周知的食品乳化剂，且也揭示可用作保湿剂。例如，US-A-4,250,196揭示了一种液体夹心的口香糖，其中卵磷脂是夹心填充部分的许多可供选择的保湿剂之一。US-A-4,466,983揭示了一种中央填充基本上非水半液态物质的产品，其中一个实施例将卵磷脂用作乳化剂。如EP-A-140,085所述，卵磷脂也已用于形成释放药物的泡。然而，据认为，以前还未认识到可将包封能减轻喉痛的活性剂的泡用在能在喉或鼻通道中提供长效作用的糖果组合物中。
因此本发明的目的是供能长时间释放减轻喉和鼻症状的药用糖果组合物，特别是润喉糖。
                           发明概述
本发明涉及润喉糖。按润喉糖重量计，该润喉糖含有60-95％(较好75-85％)可食用的壳和5-40％(较好15-25％)含水填充物，该填充物含有8-95％水和0.001-10％发泡剂，该发泡剂把喉痛缓解剂包封在分散在该填充物中的泡内。
如果没有另作说明，所有的量和比率都按重量计。如果没有另作说明，百分数按填充物的重量计。
                        发明的详细描述
本发明提供一种含有包封在泡内的喉痛缓解剂的润喉糖。虽然不想作理论说明，但认为该泡作为生物粘合剂，且能将喉痛缓解剂保持在喉中，提供长效的润喉作用。这些泡悬浮在装在可食用壳内的含水填充物中。润喉糖是指适于在口中吮吸或咀嚼以释放喉痛缓解剂的药用糖果剂。
按填充物的重量计，含水填充物一般含有约8-95％的水，较好含有约8-20％的水，更好含有约10-15％的水。含水量超过约20％不适于制造夹心硬糖。该填充物可以是液体、凝胶或糊状物。
本发明润喉糖的一个必要组分是喉痛缓解剂。本发明中所用的“喉痛缓解剂”是指能缓解人的喉或鼻通道疼痛或刺激的任何有机化合物或这些化合物的混合物。喉痛缓解剂(throat reliefagent)的种类包括，但不限于止痛剂、止咳剂、祛痰剂、生理清凉剂、生理暖和剂(warming agent)以及它们的混合物。喉痛缓解剂较好是选自生理清凉剂、生理暖和剂或它们的混合物。按含水组合物的重量计，喉痛缓解剂的合适用量为约0.001-10％，较好为约0.01-5％，更好为约0.05-3％。
合适的生理清凉剂描述于WO97/06695中，该专利被引证而包括在这里。优选用于本发明中的是选自薄荷醇、薄荷油、N-取代-p-烷-3-羧酰胺、无环叔和仲羧酰胺、3-1-氧基-1，2-丙二醇或它们的混合物。特别优选使用的是薄荷醇和含有薄荷醇的油，如薄荷油。
现已发现最有用的羧酰胺被描述于Watson等的US-A-4,136,163(1979.01.23，)和Rowsell等的US-A-4,230,688(1980.10.28)。US-A-4,136,163中的羧酰胺是N-取代-p-烷-3-羧酰胺。本发明中优选的是购自Wilkinson Sword的WS-3即N-乙基-p-烷-3-羧酰胺。US-A-4,230,688中的羧酰胺是一些无环叔和仲羧酰胺。优选用于本发明中的是购自Wilkinson Sword的WS-23即三甲基异丙基丁酰胺。
优选的生理暖和剂选自香草醇正丁醚、香草醇正丙醚、香草醇异丙醚、香草醇异丁醚、香草醇正氨基醚(vanillyl alcohol n-amino ether)、香草醇异戊醚、香草醇正己醚、香草醇甲醚、香草醇乙醚、姜醇、生姜酚、paradol、姜油酮、辣椒碱、二氢辣椒碱、去甲二氢辣椒碱、高辣椒碱、高二氢辣椒碱、乙醇、异丙醇、异戊醇、苄醇、氯仿、丁子香酚、肉桂油、肉桂醛或它们的磷酸酯。这些磷酸酯衍生物描述于WO97/02273中。该专利被引证而包括在这里。
按填充物的重量计，本发明的润喉糖也含有0.001-10％重量的发泡剂。该发泡剂用于形成分散在填充物中并包封喉痛缓解剂的泡。“泡”是指基本上球形的结构，它包括包封核芯的脂质双层。本发明中的泡可以是单或多个薄层，它的数均粒径约为1-100微米，更好约为5-50微米。该粒径可用连接于电子图象分析系统(如Linkam MS 100)的光学显微镜(如Nikon Optiphoto 2)测量。也可用视野中的刻度方格线测量。EP-A-534,823描述了遇水可形成泡的无水成形组合物(make-up composition)。该专利申请综合列举了可用于形成泡的两亲液体。对于本发明的润喉糖，当然优选使用食品级的物质。优选的发泡剂是天然磷脂，如蛋卵磷脂或大豆卵磷脂。本发明优选的磷脂是来源于植物的卵磷脂，特别大豆卵磷脂。大豆卵磷脂可用来在用量很少的条件下形成泡。按填充物的重量计，发泡剂的用量较好约为0.001-1％，更好约为0.005-0.1％，最好约为0.01-0.05％重量。在水和上述喉痛缓解剂的存在下进行充分的混合，卵磷脂形成包封喉痛缓解剂的泡。
现已发现，存在甘油可促进泡的形成。按填充物的重量计，甘油的用量约为5-25％，较好约为10-20％，更好约为12-18％。
如果该组合物还含有甜味填充剂(bulk sweetener)(如糖)，可大大地改善填充物的口味。按填充物的重量计，甜味剂的合适用量约为5-80％，较好约为50-75％(以干燥固体为基准)。优选的甜味剂原料是果糖含量高的玉米糖浆。市售的玉米糖浆含有85％的活性物质和余量的水。这种玉米糖浆也提供部分或全部含水填充物所需的水。
也可使用含有糖醇(如山梨醇)的无糖组合物。然而，较好是使用与甘油混合的糖醇，因为现已发现糖醇本身能抑制发泡。
本发明中的含水填充物也可包括增香剂。本发明中所用的术语“增香剂”是指主要为了使糖果剂产品具有香味而加入有香味的组合物中的香精以及等效的合成成分。它不包括上述的喉痛缓解剂。糖果剂领域中众所周知的增香剂可加入本发明的有香味的组合物中。这些增香剂可选自合成的香味液体和/或来源于植物叶、花、果实等的油或其混合物。代表性的增香剂包括人造、天然或合成水果香料(如柠檬、橙、香蕉、葡萄、酸橙、杏和柚子油)和水果香精(包括苹果、草莓、樱桃、橙、凤梨等)；来源豆类和坚果的香料(如咖啡、可可、可乐果、花生、杏仁等)；来源于根的香料(如甘草)。增香剂的用量一般根据所需香型、香基类型(basetype)和强度之类的因素而定。其用量一般可高达约4％重量，优选的用量约为0.1-1％。
可食用的壳可以是口香糖、硬或软糖，较好是硬糖。夹心口香糖例如在US-A-3,894,154中有描述。夹心硬糖在US-A-4,372,942和US-A-4,466,983中有描述。适用作硬糖壳的糖基料含有约30-85％葡萄糖浆和约15-70％蔗糖。或者可将无糖的基料用作这种壳。合适的无糖基料包括甜味填充剂，如异麦芽糖(isomalt)、麦芽糖醇(maltitol)和山梨醇。异麦芽糖和麦芽糖醇是优选的。该壳的内表面也可有一层分离的可食用内层，以防止或减少填充物与壳的相互作用。该可食用的壳还可含有上述的增香剂和喉痛缓解剂。在本发明优选的润喉糖中，可食用的壳和液体夹心都含有喉痛缓解剂。这样，消费者会感受到立即和长效的喉和鼻充血缓解。
含水填充物可用直接混合技术制得。用于制夹心糖果剂产品的常规技术可参见Silesia-Essenzenfabrik Gerhard Hanke K.G.，Abt.Fachbuecherei出版的“SilesiaConfiserie Manual No.3”。
本发明夹心润喉糖可用本领域中已知的淀积法、成丝(rope-forming)法或挤出法制备。挤出和成丝法是优选的。挤出法的一个实例描述于US-A-5,458,894中。挤出法的一个实例描述于US-A-5,002,791中。
以下实施例用于说明本发明的组合物和用途。然而，本发明并不局限于这些实施例。
实施例1
按如下的配方A和B制备液体夹心的润喉糖。将卵磷脂、色素溶液、香精油和/或清凉剂和暖和剂的预混合物加入到预热至82℃的高果糖玉米糖浆的混合物中，制备液体填充物。将这些组分混合2分钟，然后与分别制备的糖果基料共挤塑，制得夹心润喉糖。
    A     B
糖果基料(占润喉糖的80％重量)     ％重量     ％重量
蔗糖     58.12     49.37
葡萄糖浆(80％固体)     41.51     49.37
薄荷油     0.17     -
薄荷醇     0.17     0.08
柠檬油     -     0.27
柠檬酸     -     0.91
    100％     100％
液体填充物(占润喉糖的20％重量)     -     -
高果糖玉米糖浆1     84.38     84.306
甘油     15.0     15.0
卵磷脂     0.02     0.02
柠檬油     -     0.314
色素(％水溶液)     0.32     0.16
薄荷油     0.15     -
David Michael Heat2     0.125     0.20
香草醛     0.005     -
    100％     100％
1含85％糖固体，余量基本上为水
2购自David Michael&Co.，Inc.，Philadelphia，USA的暖和剂
将配方A和B的润喉糖给喉或鼻受刺激的人吮吸。这些人立刻会感受到缓解，反应为喉痛缓解或鼻通畅。当果糖壳破碎时，这种感觉会明显加强。缓解的感觉会延长到治疗后15分钟。

Claims (11)

1.一种润喉糖，其特征在于按润喉糖的重量计它含有60-95％可食用的壳和5-40％含水填充物，该填充物含有8-95％水和0.001-10％发泡剂，该发泡剂把喉痛缓解剂包封在分散在该填充物中的泡内。
2.如权利要求1所述的润喉糖，其特征在于按润喉糖的重量计该润喉糖含有75-85％可食用的壳和15-25％填充物。
3.如权利要求1或2所述的润喉糖，其特征在于该填充物含有8-20％，较好为10-15％的水。
4.如权利要求1-3中任一项所述的润喉糖，其特征在于该填充物含有5-25％，较好为10-20％，更好为12-18％的甘油。
5.如权利要求1-4中任一项所述的润喉糖，其特征在于该填充物含有5-80％，较好为50-75％的糖。
6.如权利要求5所述的润喉糖，其特征在于所述的糖由高果糖玉米糖浆提供。
7.如权利要求1-4中任一项所述的润喉糖，其特征在于所述的壳含有无糖基料。
8.如权利要求7所述的润喉糖，其特征在于所述的填充物含有糖醇，较好是与甘油混合。
9.如权利要求1-8中任一项所述的润喉糖，其特征在于所述的喉痛缓解剂选自生理清凉剂、生理暖和剂或它们的混合物。
10.如权利要求1-9中任一项所述的润喉糖，其特征在于所述的喉痛缓解剂含有选自薄荷醇、薄荷油、N-取代-p-烷-3-羧酰胺、无环叔和仲羧酰胺、3-1-氧基-1，2-丙二醇或它们混合物的生理清凉剂。
11.如权利要求1-10中任一项所述的润喉糖，其特征在于所述的喉痛缓解剂含有选自香草醇正丁醚、香草醇正丙醚、香草醇异丙醚、香草醇异丁醚、香草醇正氨基醚、香草醇异戊醚、香草醇正己醚、香草醇甲醚、香草醇乙醚、姜醇、生姜酚、paradol、姜油酮、辣椒碱、二氢辣椒碱、去甲二氢辣椒碱、高辣椒碱、高二氢辣椒碱、乙醇、异丙醇、异戊醇、苄醇、氯仿、丁子香酚、肉桂油、肉桂醛或它们的磷酸酯的生理暖和剂。
CN98804263A 1997-04-21 1998-04-14 减轻喉痛的组合物 Pending CN1252708A (zh)

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CN101001536B (zh) * 2004-08-11 2014-01-22 洲际大品牌有限责任公司 温热组合物和它的输送体系
CN108709788A (zh) * 2018-04-23 2018-10-26 河南科高中标检测技术有限公司 采用一测多评法测定姜药材提取物中姜辣素含量的方法

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CA2284753A1 (en) 1998-10-29
TR199902608T2 (xx) 2000-02-21
DE69818029D1 (de) 2003-10-16
CZ341299A3 (cs) 2000-01-12
CZ292693B6 (cs) 2003-11-12
CO4930321A1 (es) 2000-06-27
NO995110L (no) 1999-11-23
PE68999A1 (es) 1999-10-03
KR20010006285A (ko) 2001-01-26
EP0977553A1 (en) 2000-02-09
EP0977553B1 (en) 2003-09-10
HUP0001915A3 (en) 2003-05-28
US6432441B1 (en) 2002-08-13
KR100356082B1 (ko) 2002-10-12
CA2284753C (en) 2003-06-10
GB9707978D0 (en) 1997-06-11
ATE249203T1 (de) 2003-09-15
HUP0001915A2 (hu) 2000-10-28
BR9808947A (pt) 2000-10-03
WO1998047482A1 (en) 1998-10-29
AU734587B2 (en) 2001-06-21
JP2001526646A (ja) 2001-12-18
DK0977553T3 (da) 2004-01-12
NO995110D0 (no) 1999-10-20
DE69818029T2 (de) 2004-06-09

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