CN101827582A - 含有清凉剂的口腔组合物 - Google Patents

含有清凉剂的口腔组合物 Download PDF

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CN101827582A
CN101827582A CN200880111672A CN200880111672A CN101827582A CN 101827582 A CN101827582 A CN 101827582A CN 200880111672 A CN200880111672 A CN 200880111672A CN 200880111672 A CN200880111672 A CN 200880111672A CN 101827582 A CN101827582 A CN 101827582A
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preparation
endothermic
buccal tablet
endothermic cooler
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金斯利·伊奥阿
尼尔·缪尔
罗伯特·罗兹
奥尔登·罗德韦尔
大卫·迈克尔·瑟古德
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Reckitt Benckiser Healthcare UK Ltd
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Abstract

本发明涉及一种制剂，该制剂含有选自由木糖醇、山梨醇、甘露醇和赤藓糖醇组成的组并且热焓为-10cal/g至-100cal/g的吸热清凉剂，以及一种或多种活性剂，其中所述吸热剂在制剂中的存在量少于10重量％。

Description

含有清凉剂的口腔组合物
技术领域
本发明涉及一种含有清凉剂的口腔组合物。特别是，本发明涉及含有清凉剂的药剂。更特别是，本发明涉及一种含有木糖醇的用于治疗咽喉痛的药剂。
背景技术
清凉剂已经被用于诸如硬糖产品或口香胶等很多不同的制剂中以提供愉快的味道和清凉的感觉。例如，诸如薄荷醇或薄荷油等化合物已经被用于作为制剂的一部分或包衣的一部分，以便为使用者提供清凉的感觉。
清凉剂也被用于药物制剂以增强生理和/或感觉上的益处，例如缓解的速度或持续时间。这类试剂通常用于非处方止咳药。
咽喉痛通常使用含有治疗有效量的活性化合物的药物含片来治疗。适宜地，含片由需要该治疗的患者来吮吸，并且活性剂释放于口腔中并递送到疼痛的咽喉的表面(即黏膜)。
一些用于缓解咽喉痛相关症状的活性剂，例如非甾体抗炎药(NSAID)，当停留在口中时，会在口腔的后部带来不愉快的灼烧感。这是接受治疗的患者所不能接受的。因此，设计了含有诸如NSAID等活性剂的药物含片，由此所形成的含片可缓解咽喉痛的症状，但患者不会经历不能接受的灼烧感。
清凉剂也已经和甜味剂一起被用于咳嗽治疗用液体组合物中。液体受限的携带性限制了清凉剂在液体组合物中的使用，并且一些高强度的甜味剂，例如阿斯巴甜，在受热时会降解。
此外，如果在组合物中使用过高水平的清凉剂，其本身就会导致灼烧的效果。
通常可使用多元醇来获得口中的清凉效果或清凉感觉。该效果由所述多元醇在水中溶解的负热引起，并且也与它们的溶解速度有关。结晶木糖醇在这方面特别有效，因其赋予了最强的清凉感觉。山梨醇和赤藓糖醇具有比木糖醇略低的清凉效果。
木糖醇，又称为木糖或桦木糖(birch sugar)，是可用作糖替代物的五碳糖醇。它衍生自各种类型的纤维素产品，诸如木材、稻草、甘蔗浆、种壳和果壳。木糖醇是一种无气味的、甜味颗粒状固体(含有结晶的同等大小的颗粒)。木糖醇具有与糖相同的甜味水平。相对大的溶解负热和高溶解度的结合意味着木糖醇在口中提供被称为清新的清凉感觉。
山梨醇是可在许多食品中找到的常用主体甜味剂。除提供甜味外，它还是优良的湿润剂和调质剂。甘露醇是一种单糖多元醇。山梨醇和甘露醇通常都是稳定并且化学上惰性的。
木糖醇的主要缺点在于它是一种昂贵的成分。此外，普遍理解的是，只有当使用结晶木糖醇时才能获得清凉效果。因此，木糖醇经常被较廉价的无糖多元醇如山梨醇替换。
山梨醇的用途是公知的并且已有记载。很多专利公报公开了这样的用途，例如GB 2 115 672、US 4 317 838和US 4 753 790。
能够以较低的量应用木糖醇将是理想的。但是，制剂中少量木糖醇的存在被认为不能产生显著的清凉感。
发明内容
根据本发明的第一方面，提供了一种含有热焓为-10cal/g至-100cal/g的吸热清凉剂、以及一种或多种活性剂的制剂，其中该吸热剂在制剂中存在的量少于10重量％。
吸热清凉剂可以具有-10cal/g至-50cal/g的热焓。更优选的吸热清凉剂可以具有-20cal/g至-35cal/g的热焓。
吸热清凉剂可以在药剂中以1％～5％的量存在。优选的量是1％～3％。
吸热清凉剂可以是多元醇，优选选自由木糖醇、山梨醇、甘露醇和赤藓糖醇组成的组。
活性剂优选选自包括但不限于2，4-二氯苄基醇(DCBA)、戊基间甲酚(AMC)、己基间苯二酚、氟比洛芬、利多卡因、苯佐卡因、氯化十六烷基吡啶、地喹氯铵(dequalinium chloride)、薄荷醇、盐酸氨溴索、氢溴酸右美沙芬和愈创甘油醚的组。
该制剂可以是任何合适的形式，包括含片剂、凝胶剂、喷雾剂、胶囊剂、锭剂、口香糖或片剂。
当所述制剂是适合包衣的形式时，该试剂可以形成包衣的一部分。
优选地，所述制剂不含高强度甜味剂。
该制剂可以根据需要含有额外的赋形剂。典型的赋形剂包括但不限于酸度调节剂、遮光剂、着色剂、稳定剂、缓冲剂、甜味剂、调味剂和防腐剂。
根据本发明的第二方面，提供了热焓为-10cal/g至-100cal/g的吸热清凉剂在药剂中的应用，其中该吸热剂在药剂中存在的量少于10重量％。
吸热清凉剂可以具有-10cal/g至-50cal/g的热焓。更优选的吸热清凉剂可以具有-20cal/g至-35cal/g的热焓。
吸热清凉剂可以在药剂中以1％～5％的用量范围存在。优选的量是1％～3％。
吸热清凉剂可以是多元醇，优选选自由木糖醇、山梨醇、甘露醇和赤藓糖醇组成的组。
活性剂优选选自包含2，4-二氯苄基醇(DCBA)、戊基间甲酚(AMC)、己基间苯二酚、氟比洛芬、利多卡因、苯佐卡因、氯化十六烷基吡啶、地喹氯铵、薄荷醇、盐酸氨溴索、氢溴酸右美沙芬和愈创甘油醚的组。
该药剂可以是任何合适的形式，包括含片剂、凝胶剂、喷雾剂、胶囊剂、锭剂或口香糖。
当所述药剂是适合包衣的形式时，该试剂可以形成包衣的一部分。
优选药剂不含高强度甜味剂。
所述药剂可以根据需要含有额外的赋形剂。典型的赋形剂包括但不限于酸度调节剂、遮光剂、着色剂、稳定剂、缓冲剂、甜味剂、调味剂和防腐剂。
根据本发明的第三方面，提供了吸热清凉剂用于制备本发明第二方面的治疗咽喉痛的药剂的应用。
本发明的优选形式是固体形式，例如可以被吸吮或咀嚼从而在患者口中释放吸热清凉剂的含片。然后，所述清凉剂可以透过咽喉的表面并给患者提供缓解。
在本发明的上下文中，此处使用的术语“吸热清凉剂”是指诸如木糖醇等化合物，其实际上是由于具有显著的溶解负热而对身体进行局部冷却。相比之下，诸如薄荷醇等化合物通常基于它们可使身体感觉到较低的温度而被称为“生理清凉剂”(即使这通常是错误的)。
为免生疑问，如本发明第一方面所定义的制剂包括糖果、食品补充剂和食品、营养品、药品和非药物产品，其中非药物产品包括不被视为糖果的产品，例如用于治疗诸如咽喉痛等状况的非处方含片。
具体实施方式
现在说明本发明的一个示例实施方式。
实施例制剂
标准名称                     mg          ％
蔗糖/葡萄糖糖浆              2481.06     95.42％
木糖醇                       40          1.54％
调味剂                       18          0.70％
左薄荷醇Ph Eur Natural       8           0.31％
2，4-二氯苄基醇              1.2         0.05％
戊基间甲酚BP                 0.615       0.02％
桉树油Ph Eur                 0.5         0.02％
总量(包含理论上2％的水分)    2600
含片使用基于混合组分连续流的方法来制备，这对于高沸含片产品的高速制造是常规的。混合液体蔗糖和液体葡萄糖以形成糖浆，填入收纳容器。将糖浆随后从收纳容器泵入烹煮器系统，在这里水含量减少从而导致含片基质的形成。将含片基质从烹煮器中以连续的流引出并供应到混合室中；向含片本体(含有活性成分和调味剂)中以与含片基质流成比例的速率加入结晶木糖醇。这样形成了含片团。
随后，使含片团从混合室连续流到回火带上，在含片形成和进一步冷却前在那里变凉。
可选择的剂型，例如咀嚼固体剂型，可以使用本领域技术人员公知或已记载的方法制备。
为了证明含木糖醇的含片的局部物理清凉，在实验室制备了各种含片样品。
制备了下述含片：
1.纯的糖-葡萄糖含片
2.含有左薄荷醇(每2.6克含片中8mg)的糖-葡萄糖含片
3.含有木糖醇(每2.6克含片中40mg 1.5重量％)的糖-葡萄糖含片
4.含有木糖醇(每2.6克含片中40mg 4.6重量％)的糖-葡萄糖含片
试验中包括纯的糖-葡萄糖含片作为这种清凉的对比点。由于木糖醇通过与薄荷醇不同的机理提供清凉，因此含有薄荷醇的样品也包括在本试验中，以强调这种区别。
上述的含片样品(即1～4)由许多个体来品尝。
参与者被要求指出当含片与口的任意部分接触时，他们是否在含片的表面获得了清凉的感觉。参与者还被要求将含片的表面清凉从1到4(1最清凉～4最不清凉)分级。
下表显示了参与者如何在提供清凉方面对样品评分。1分被认为是最凉，而4分是最不凉。
  参与者  含片1  含片2  含片3  含片4
  1   4   3   2   1
  2   4   3   2   1
  3   4   3   1   2
  4   4   3   2   1
  5   4   3   2   1
解释
含片1-纯的糖-葡萄糖含片
含片2-含有左薄荷醇的糖-葡萄糖含片
含片3-含有木糖醇(每2.6克含片中40mg 1.5重量％)的糖-葡萄糖含片
含片4-含有木糖醇(每2.6克含片中120mg 4.6重量％)的糖-葡萄糖含片
每位参与者感觉到主要在含有木糖醇的含片中表现的表面清凉。大多数参与者可以将具有更高量木糖醇的含片确定为最清凉。
相应地，含片中存在低浓度(1.5重量％-4.6重量％)的木糖醇可导致含片显示出预料不到的强清凉性质。
一般来说，本发明可以使用任意的多元醇，因为它们具有甜味并且可以用于口腔中提供清凉效果。常用的多元醇包括木糖醇、甘露醇、山梨醇和赤藓糖醇。然而，本领域技术人员会认识到，可以使用许多种多元醇和使用多元醇的组合。
在替代的具体实施例中，活性组分DCBA和AMC可以被氟比洛芬、己基间苯二酚、利多卡因、苯佐卡因、氯化十六烷基吡啶、地喹氯铵、薄荷醇、盐酸氨溴索、氢溴酸右美沙芬或愈创甘油醚代替。
可以引入进一步的变型和改进而不背离本发明在此公开的范围。

Claims (11)

1.一种包含热焓为-10cal/g至-100cal/g的吸热清凉剂以及一种或多种活性剂的制剂，其中所述吸热剂在所述制剂中的存在量少于10重量％。
2.如权利要求1所述的制剂，其中所述吸热清凉剂具有-10cal/g至-50cal/g的热焓。
3.如权利要求2所述的制剂，其中所述吸热清凉剂具有-20cal/g至-35cal/g的热焓。
4.如前述权利要求中任一项所述的制剂，其中所述吸热清凉剂在所述制剂中的存在量为1％～5％。
5.如权利要求4所述的制剂，其中所述清凉剂的量是1％～3％。
6.如前述权利要求中任一项所述的制剂，其中所述吸热清凉剂选自由木糖醇、山梨醇、甘露醇和赤藓糖醇组成的组。
7.如前述权利要求中任一项所述的制剂，其中所述活性剂选自包含2，4-二氯苄基醇、戊基间甲酚、己基间苯二酚、氟比洛芬、利多卡因、苯佐卡因、氯化十六烷基吡啶、地喹氯铵、薄荷醇、盐酸氨溴索、氢溴酸右美沙芬和愈创甘油醚的组。
8.如前述权利要求中任一项所述的制剂，其中所述制剂是包括含片剂、凝胶剂、喷雾剂、胶囊剂、锭剂、口香糖或片剂的任何适合的形式。
9.如前述权利要求中任一项所述的制剂，其中所述制剂含有选自酸度调节剂、遮光剂、着色剂、稳定剂、缓冲剂、甜味剂、调味剂和防腐剂的一种或多种额外的赋形剂。
10.热焓为-10cal/g至-100cal/g的吸热清凉剂在药剂中的应用，其中所述吸热剂在所述药剂中的存在量少于10重量％。
11.热焓为-10cal/g至-100cal/g的吸热清凉剂在制备用于治疗咽喉痛的药剂中的应用。
CN200880111672A 2007-10-19 2008-10-17 含有清凉剂的口腔组合物 Pending CN101827582A (zh)

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