CN118139622A - 尼古丁口香糖 - Google Patents
尼古丁口香糖 Download PDFInfo
- Publication number
- CN118139622A CN118139622A CN202280070662.9A CN202280070662A CN118139622A CN 118139622 A CN118139622 A CN 118139622A CN 202280070662 A CN202280070662 A CN 202280070662A CN 118139622 A CN118139622 A CN 118139622A
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- Prior art keywords
- chewing gum
- nicotine
- coating
- powder core
- powder
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- 229960002715 nicotine Drugs 0.000 claims abstract description 78
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Abstract
本发明涉及一种尼古丁口香糖,该尼古丁口香糖给予尼古丁的立即释放和吸收以及尼古丁的延长释放和吸收。本发明还描述了此类口香糖调配物的合适制造方法,以及该口香糖用于治疗患有烟草和/或电子烟依赖渴求的人的用途。
Description
技术领域
本发明涉及一种尼古丁口香糖,该尼古丁口香糖给予尼古丁的立即释放和吸收以及尼古丁的延长释放和吸收,以及涉及此类口香糖调配物的合适制造方法。本发明还涉及此类口香糖用于治疗患有烟草和/或电子烟依赖渴求的人的用途。
背景技术
据世界卫生组织(WHO)称,尽管市场上存在帮助吸烟者戒烟的产品(药物),诸如例如包含尼古丁的口香糖、锭剂、喷剂和透皮贴剂等产品,但每年仍有约六百万人死于吸烟相关的疾病。
生产尼古丁口香糖的传统方式是产生尼古丁与阳离子交换树脂的复合物并将该复合物添加到口香糖调配物。
此类口香糖多年来一直可在市场上购得,例如以商标售卖。然而,有些消费者正在寻找可提供更快的渴求缓解、更接近香烟渴求缓解的尼古丁产品(药物),并且因此,仍然有机会开发可满足使用任何形式的尼古丁(包括烟草和电子烟)的该人群的需求的新型尼古丁口香糖。
市场上有一种产品给出更快渴求缓解,它是NicoretteTMQuickMistTM,这是一种待施用于口腔粘膜的口腔喷剂,尼古丁化合物容易从口腔粘膜吸收到血流中,从而给予快速渴求缓解。在NicoretteTMQuickMistTM产品中,尼古丁是游离形式,并且由于系统的缓冲能力,尼古丁快速通过粘膜以给予快速的渴求缓解。
因此,对于本领域的技术人员而言,制造一种介于液体QuickMistTM喷剂与口香糖之间的混合物是显而易见的。然而,此类产品会产生许多问题,包括尼古丁的稳定性(即尼古丁作为液体不稳定)、制造和储存问题。如果试图制备一种内部具有液体的口香糖,则口香糖将缓慢地溶解,并且存在于液体和口香糖内的组分将混合,从而引起不合适的化学反应。
包含尼古丁的口香糖需要被咀嚼并与唾液混合,以通过口腔粘膜释放尼古丁。喷剂(比如QuickMistTM)使用包含尼古丁的液体以及一种或多种缓冲剂来增加经粘膜吸收的速度。
对于本领域的技术人员而言,提出一种具有液体芯的口香糖是显而易见的。然而,此类产品的缺点在于存在许多问题,包括QuickMistTM中通常使用的游离形式的尼古丁的稳定性。
因此,需要找到一种另选的尼古丁替代产品,其与口香糖一样便利并且具有与QuickMistTM所提供的尼古丁吸收一样快的尼古丁吸收,同时还保持令人愉快的口感。
WO2007/133141公开了一种尼古丁口香糖,其具有包含任何形式的尼古丁的固体芯以及用氨丁三醇缓冲的至少一个包衣层。WO2007/133141公开了一种包含口香糖基础剂的口香糖芯,然而它没有关于液体芯的记载。
WO2020/012009公开了一种在口香糖上具有圆点的尼古丁口香糖,其中该圆点应当给予尼古丁的立即释放和快速渴求缓解以及口香糖的延长释放。该发明的问题是不可能制造该产品,并且能量需求非常高。存在于圆点中的成分在被置于口香糖上时需要处于液相,这需要能量。另外,此类方法对于生产工厂中的人而言是危险的,因为液体尼古丁是有毒的,并且尼古丁和缓冲剂不能一起存在。本方法存在的问题是,尼古丁将在圆点固化之前恢复到其游离形式。
本发明要解决的问题是提供一种产品,该产品给予令人愉快且可接受的口感,提供尼古丁的快速吸收以及尼古丁的延长吸收以帮助人员停止吸烟。通过提供此类产品,首次有可能提供一种给予立即和延长渴求缓解的产品,以及提供一种能够制造和储存而无稳定性问题的产品。
发明内容
发明人一直在探索产生引起尼古丁的立即释放和吸收以及延长释放和吸收的口香糖的可能性,该口香糖仍然具有良好的味道和适口性,包括能够被制造。为了提供尼古丁口香糖产品的立即释放和吸收,发明人的方法是以更容易获得的尼古丁盐形式来施用尼古丁,诸如尼古丁酒石酸氢盐或尼古丁二酒石酸盐二水合物,其被包含在作为粉末存在于口香糖内的芯中。然而,使芯具有粉末还意味着消费者在咀嚼口香糖时将暴露于粉末,这通常不是令人愉快的感觉。然而,本发明的粉末被设计成以快速立即方式溶解,并且因此给予令人愉快的味道和感觉。
尼古丁的pKa为大约7.8。众所周知,与尼古丁盐或呈带正电荷的酸形式的尼古丁相比,不带电荷(游离碱形式)的尼古丁可更容易且更快地进入生物膜,诸如口腔粘膜。更容易且更快地渗透通过生物膜会导致更快的全身吸收。
人类唾液的平均pH通常仅为约6-7.5。
通过选择某些成分并将其添加到口香糖粉末芯中,将发生进入粘膜的快速立即吸收,而没有粉末在口中的任何不合适的感觉。这将导致粉末芯中的近似约90%的尼古丁将在粉末在唾液中的崩解和溶解之后转化为其游离碱形式,以容易地吸收到全身循环中,以提供更快的渴求缓解。该粉末在消费者咀嚼口香糖时将在至多约30秒内溶解并且被吸附到粘膜内以提供快速的渴求缓解,诸如15秒-30秒、10秒或20秒。粉末溶解的速度取决于消费者咀嚼口香糖的强烈程度。
尼古丁游离碱形式不适合直接配制成半固体或固体剂型,因为尼古丁游离碱形式在正常条件下呈高度挥发性液体形式。为了避免该问题,例如,在尼古丁为其盐形式的情况下,粉末是优选的。通过使用盐,其更容易控制以及在制造产品时更容易。
为了能够提供瞬时和合适的pH增加,使用缓冲系统(诸如一种或多种不同缓冲剂(缓冲剂种类))是有益的。通常,缓冲系统的味道并不好,因此需要仔细选择并通过例如甜味剂和风味剂掩盖味道。此外,一种缓冲剂(缓冲剂种类)的缓冲能力可能不足够。
为了提供尼古丁从尼古丁口香糖包衣的延长释放,使用结合到树脂(诸如尼古丁离子交换树脂)的尼古丁是合适的。尼古丁离子交换树脂通常用于可在市场上购得的药用口香糖中。此类药用口香糖将在高达约20分钟至45分钟的时间内提供延长释放,这取决于使用。然而,在使用的前5分钟-10分钟期间,从这些口香糖的释放和吸收在某种程度上是有限的,现在通过使用具有尼古丁盐的粉末芯来解决该问题,这将给予快速吸收。
与市场上可购的其它当前可用的商业化尼古丁口香糖产品相比,本发明的尼古丁口香糖在同一产品中提供新特征。
在第一方面,本发明涉及一种尼古丁口香糖,该尼古丁口香糖包括:
i.粉末芯,该粉末芯包含至少尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物、甜味剂、缓冲剂和基于多元醇的填充剂;和
ii.口香糖包衣,该口香糖包衣包含至少尼古丁离子交换树脂,其中来自粉末芯的尼古丁被立即释放并且来自口香糖包衣的尼古丁被延长释放。
本发明还涉及一种尼古丁口香糖,该尼古丁口香糖包括:
i.粉末芯,该粉末芯包含至少尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物、甜味剂、缓冲剂和基于多元醇的填充剂;和
ii.口香糖包衣,该口香糖包衣包含至少口香糖基础剂和尼古丁离子交换树脂,
其中来自粉末芯的尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物具有立即释放并且来自口香糖包衣的尼古丁离子交换树脂具有延长释放。
任选地,至少一个基于多元醇的硬包衣包覆口香糖,该至少一个基于多元醇的硬包衣包含至少一种糖醇或糖醇的混合物。
具体实施方式
定义
在本专利申请和发明的上下文中,以下定义适用:
术语“尼古丁”是指呈任何盐形式或结合到任何载体的一定量(mg)的尼古丁,以每块口香糖对应游离碱的量计算。
术语“缓冲剂”是指一种或两种不同种类的缓冲剂种类,也区分缓冲剂系统的对应酸碱对。
如本文所用,术语“延长释放”(“ER”)是指特征在于存在于口香糖芯中的尼古丁将在通常20分钟至45分钟(消费者或患者咀嚼(使用)口香糖的时间)的延长时间段内释放的调配物。释放特征可使用所属领域的技术人员已知的技术通过体外溶解来估计(EuropeanPharmacopeia 9.0,General chapters,method of analysis,2.9.25Dissolutionformedication chewing gums,apparatus B)。
如本文所用,术语“立即释放”(“IR”)旨在意指包含在口香糖的粉末芯中的尼古丁的释放,其可用于快速口腔粘膜吸收。尼古丁的释放速率不是通过控释基质手段或其它此类手段进行持续的,而是取决于咀嚼时口香糖芯的崩解和溶解以及尼古丁盐的水溶性。如本文所述,“立即释放”是指尼古丁释放在开始咀嚼口香糖后约30秒内开始,这取决于消费者咀嚼口香糖的强烈程度,并且也可能短于30秒。
术语“粉末”旨在意指含有细干颗粒的粉末,这些细干颗粒不聚集并且保持稳定的粉末形式,并且具有小于310μm的平均粒度,以粉末中存在的最大赋形剂来计算。
术语“口香糖包衣”旨在意指包覆整个粉末芯并且保护粉末免于暴露于湿气的口香糖包衣;并且通过这样做,粉末芯在口香糖被咀嚼之前保持稳定。在咀嚼口香糖时,粉末芯暴露于唾液并如上文所定义的那样快速溶解,并且引起快速的渴求缓解。
术语“口感”是指由食物或饮料在口中引起的生理感觉,在这种情况下是咀嚼口香糖,不同于味道。它是一种基本的感官属性,其与味道和气味一起决定了口香糖的整体风味和质地。它被用来描述通过咀嚼对腭的感觉。
对存在于口香糖芯中的尼古丁的量的计算是计算作为并且最常表示为对应游离碱形式的尼古丁。
口香糖
在一个实施方案中,本发明涉及一种尼古丁口香糖,该尼古丁口香糖包括:粉末芯,该粉末芯包含至少尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物、甜味剂、缓冲剂和基于多元醇的填充剂;和口香糖包衣,该口香糖包衣包含至少尼古丁离子交换树脂,其中来自粉末芯的尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物被立即释放并且来自口香糖包衣的尼古丁离子交换树脂被延长释放。该口香糖包衣将该粉末包封在该芯中并且保护该粉末不受湿气影响直到在该口香糖上发生咀嚼为止。在咀嚼时,粉末被释放并快速溶解,并且发生快速渴求缓解。
本发明还涉及一种尼古丁口香糖,该尼古丁口香糖包括:粉末芯,该粉末芯包含至少尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物、甜味剂、缓冲剂和基于多元醇的填充剂;和口香糖包衣,该口香糖包衣包含至少口香糖基础剂和尼古丁离子交换树脂,其中来自粉末芯的尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物具有立即释放并且来自口香糖包衣的尼古丁离子交换树脂具有延长释放。
尼古丁口香糖还可包括至少一个基于多元醇的硬包衣,该至少一个基于多元醇的硬包衣包覆口香糖包衣的外部。
任选地,基于多元醇的硬包衣包覆口香糖,该基于多元醇的硬包衣包含至少一种糖醇或糖醇的混合物。
本领域技术人员众所周知的是如何生产传统的口香糖。
一个示例是US 3,877,468中公开的方法。已在WO2006/124366中公开了包衣口香糖,其中描述了基于多元醇的硬包衣与包含一种或多种甜味剂和/或风味剂的内部聚合物包衣组合以改善口香糖的味道和感官接受度。
粉末芯包含尼古丁。口香糖粉末芯中存在的尼古丁(以游离碱计算)可为按每块口香糖计算的约0.5mg至约5.0mg、约2.0mg至约4.0mg,诸如0.5、1.0、1.25、1.5、1.75、2.0、2.25、2.5、2.75、3.0、3.25、3.5、3.75、4.0、4.25、4.5或5.0。当使用者咀嚼口香糖时,尼古丁将从粉末芯中释放出来,并且该释放将立即发生,例如在约30秒内,诸如10秒或20秒内。
适合使用的缓冲剂选自由以下项组成的组:碳酸钠、碳酸氢钠、碳酸钾、碳酸氢钾、氨丁三醇碱(Tris碱)或氨丁三醇的对应的共轭酸(诸如氨丁三醇盐酸盐(Tris HCl))、磷酸三钠、磷酸氢二钠、磷酸二氢钠、磷酸三钾、磷酸氢二钾、磷酸二氢钾以及它们的混合物。根据一个实施方案,缓冲剂可选自由以下项组成的组:碳酸钠、碳酸氢钠、氨丁三醇碱(Tris碱)或氨丁三醇的对应的共轭酸(诸如氨丁三醇盐酸盐(Tris HCl))以及它们的混合物。在一些具体实施方案中,使用碳酸钠和/或碳酸氢钠。
芯中的尼古丁需要与大气隔绝,并且通过这样做,没有湿气会与干粉接触,因此尼古丁将是干燥和稳定的。
粉末芯的总量可为至多80mg,诸如10mg-80mg,诸如10mg、15mg、20mg、25mg、30mg、35mg、40mg、45mg、50mg、55mg、60mg、65mg、70mg、75mg或80mg,诸如20mg至60mg。限制是当粉末的溶解太慢且适口性不太令人愉快时。粉末的粒度取决于成分。如果芯中粉末的量为80mg,则口香糖包衣需要为约950mg以能够负载如此高量的粉末。然而,如果芯中的粉末为40mg,则475mg的口香糖包衣应当是足够的。
粉末芯和/或口香糖包衣或膜包衣中的缓冲剂可按以下总量存在:约1.0mg至约8.0mg(按每块口香糖计算),诸如约1.0mg至约6.0mg,诸如约2.0mg至约6.0mg,或约2.0mg至约5.0mg,或约3.0mg至约6.0mg,或约3.0mg至约5.0mg,诸如1.0mg、1.25mg、1.5mg、1.75mg、2.0mg、2.25mg、2.5mg、2.75mg、3.0mg、3.25mg、3.5mg、3.75mg、4.0mg、4.25mg、4.5mg、4.75mg、5.0mg、5.25mg、5.5mg、5.75mg、6.0mg、6.25mg、6.5mg、6.75mg、7.0mg、7.25mg、7.5mg或8.0mg。
本发明还涉及一种尼古丁口香糖,其中粉末芯包含量为每块口香糖约0.5mg至约5.0mg的尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物(以游离碱计算),并且口香糖包衣包含量为约0.25mg至约6.0mg的尼古丁离子交换树脂(以游离碱计算)。
粉末芯中尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物的量以及口香糖包衣中尼古丁离子交换树脂的量可被计算为尼古丁游离碱的当量,并且以每块口香糖的mg表示。
根据本发明的口香糖包衣中的口香糖基础剂为总口香糖包衣的约15重量%-80重量%,并且优选地为至少约40重量%。
当使用尼古丁本身时或当使用吸收形式时,针对最期望的尼古丁缓慢释放采用的口香糖基础剂的量通常在较高的范围内。口香糖基础剂可以是本领域已知的任何常规性质。例如,其可包含易于从商业来源获得的天然或合成来源的口香糖基础剂。天然口香糖基础剂包括例如糖胶树胶(chicle)、节路顿胶(jelutong)、莱卡胶(lechi de caspi)、索合胶(soh)、塞克胶(siak)、卡陶胶(katiau)、索瓦胶(sorwa)、巴拉塔胶(balata)、盘塔胶(pendare)、马来胶(malaya)和桃胶(peach gum)、天然生橡胶和天然树脂(诸如达玛胶和乳香)。合成口香糖基础剂是以下项的混合物:
-弹性体(聚合物、塑炼物质);
-增塑剂(树脂、弹性体、溶剂、疏水性树脂);
-填料(调质剂、水不溶性助剂)、软化剂(脂肪);
-乳化剂;
-蜡;
-抗氧化剂;和
-防粘剂(乙烯基聚合物、亲水性树脂)。口香糖基础剂的其它示例是树胶,包括琼脂、藻酸盐、阿拉伯树胶、角豆胶、角叉菜胶、茄替胶、瓜尔胶、刺梧桐树胶、果胶、黄蓍胶、刺槐豆胶、结冷胶和黄原胶。
口香糖基础剂和尼古丁离子交换树脂可存在于两个不同的层中,所述两个层构成了口香糖包衣。含有尼古丁离子交换树脂的层可以是口香糖包衣的内部部分,即含有尼古丁离子交换树脂的层可与粉末芯接触。另选地,含有口香糖基础剂的层可以是口香糖包衣的内部部分,即含有口香糖基础剂的层可与粉末芯接触。口香糖包衣可包含尼古丁离子交换树脂和口香糖基础剂的混合物;这两者均可与粉末芯接触。
口香糖基础剂可不存在于粉末芯中。
基于多元醇的填充剂和/或基于多元醇的硬包衣可以是基于赤藓糖醇、麦芽糖醇、木糖醇、乳糖醇、异麦芽酮糖醇、甘露糖醇、阿拉伯糖醇和山梨糖醇或它们的混合物。基于多元醇的填充剂和/或基于多元醇的硬包衣可优选地是木糖醇。
基于多元醇的填充剂可以是基于赤藓糖醇、麦芽糖醇、木糖醇、乳糖醇、异麦芽酮糖醇、甘露糖醇、阿拉伯糖醇和山梨糖醇或它们的混合物。基于多元醇的填充剂可优选地是木糖醇。
基于多元醇的硬包衣可以是基于赤藓糖醇、麦芽糖醇、木糖醇、乳糖醇、异麦芽酮糖醇、甘露糖醇、阿拉伯糖醇和山梨糖醇或它们的混合物。基于多元醇的硬包衣可优选地是木糖醇。
在具有粉末芯的尼古丁口香糖的一个实施方案中,粉末芯可包含尼古丁酒石酸氢盐(NHT)、碳酸钠、碳酸氢钠、木糖醇和纽甜。
尼古丁口香糖可用基于多元醇的外部硬包衣进行包衣,并且还可包括一个或多个基于聚合物的膜包衣。
单独的膜包衣可以具有约20μm至约200μm,诸如20μm至约100μm,诸如20μm至60μm,诸如30μm的厚度。
成膜聚合物可在以下项中选择:羟丙基甲基纤维素(HPMC)、甲基羟乙基纤维素(MHEC)、羟丙基纤维素(HPC)、羟乙基纤维素(HEC)、甲基丙烯酸共聚物-C型、羧基甲基纤维素钠、羟丙基甲基纤维素苯二甲酸酯(HPMCP)、乙基羟乙基纤维素(EHEC)和其它成膜聚合物,诸如聚右旋糖、聚乙二醇、丙烯酸酯聚合物、聚乙烯醇-聚乙二醇接枝共聚物、聚乙烯吡咯烷酮(PVP)的复合物诸如聚维酮、聚乙烯醇(PVOH或PVA)、微晶纤维素、角叉菜胶、预胶化淀粉、聚乙二醇、以及它们的组合。
在一个实施方案中,成膜聚合物在羟丙基甲基纤维素(HPMC)、甲基羟乙基纤维素(MHEC)、羟丙基纤维素(HPC)、羟乙基纤维素(HEC)、乙基羟乙基纤维素(EHEC)以及聚乙烯醇(PVOH或PVA)中选择。
如果施加两种基于聚合物的膜包衣,则可以在单独的包衣中使用相同以及不同的聚合物以及它们的混合物。在一个实施方案中,两种膜包衣(也称为膜层)均可以是基于羟丙基甲基纤维素(HPMC)。在另一个实施方案中,一个膜层是基于羟丙基甲基纤维素(HPMC),并且另一个膜层是基于另一种成膜聚合物(诸如聚乙烯醇(PVOH或PVA))。成膜聚合物可以显示稍微不同的特性。例如,PVA被认为对pH升高更具有抗性,因此当目标是高pH时,其可能适合用于含有缓冲剂的膜包衣。
HPMC提供了良好的适口性,并且能够在施用于硬包衣尼古丁口香糖时提供延长的风味剂和甜味剂增强。
口香糖或膜包衣外部的基于多元醇的硬包衣可包含至少一种糖醇或其混合物。糖醇可以是赤藓糖醇、麦芽糖醇、木糖醇、乳糖醇、异麦芽酮糖醇、甘露糖醇、阿拉伯糖醇、异麦芽酮糖醇以及山梨糖醇或它们的混合物。基于多元醇的硬包衣可以具有约350μm至约750μm诸如500μm的厚度。在一个实施方案中,基于多元醇的硬包衣是木糖醇与麦芽糖醇的混合物或者仅含有木糖醇。
调味剂/风味剂的示例包括水果和浆果风味剂诸如酸橙、橙、柠檬、黑加仑、血橙、越橘、云莓、枸杞莓、树莓、草莓、野生草莓、沙棘、樱桃、甜瓜、猕猴桃、番木瓜、菠萝、西番莲果、椰子,以及其他风味剂诸如蜂蜜、草本、茴芹、水草、柠檬草、凉爽剂、生姜、咖啡、桉树、山竹、胡椒薄荷、留兰香、冬青、蜜饯、肉桂、可可/可可粉、香草、甘草、盐、胡椒、辣椒、薄荷醇、八角或它们的混合物。调味剂/风味剂可以是天然提取物以及合成和半合成型式以及风味剂的混合物。风味剂可以相同或不同,并且可存在于粉末芯、口香糖包衣、膜包衣和/或基于多元醇的硬包衣中。风味剂的合适示例是薄荷科风味剂、水果和浆果风味剂。
此外,口香糖可具有存在于粉末芯和/或口香糖包衣中的至少一种人工甜味剂。至少一种人工甜味剂可存在于口香糖包衣、粉末芯、膜包衣和/或基于多元醇的硬包衣中。人工甜味剂的示例为糖精、糖精钠、天冬甜素、乙酰磺胺酸钾、纽甜、索马甜(thaumatin)、甘草素、三氯蔗糖、环己氨基磺酸盐、二氢查耳酮、阿力甜、爱德万甜(advantame)、非洲奇果蛋白和应乐果甜蛋白以及它们的混合物。
口香糖包衣中的尼古丁盐可按以下量存在:约0.25mg至约6mg,诸如0.5mg至约1mg或者0.25mg、0.5mg、0.75mg、1.0mg、1.25mg、1.5mg、1.75mg、2.0mg、2.25mg或2.5mg。
此外,口香糖包衣可具有至少一种人工甜味剂。该至少一种人工甜味剂可存在于粉末芯和/或口香糖包衣中。人工甜味剂的示例为糖精、糖精钠、天冬甜素、乙酰磺胺酸钾、纽甜、索马甜、甘草素、三氯蔗糖、环己氨基磺酸盐、二氢查耳酮、爱德万甜、阿力甜、非洲奇果蛋白和应乐果甜蛋白以及它们的混合物。纽甜充当掩味剂和甜味剂,并且适于掩盖尼古丁的令人不快的味道。
最后,本发明涉及以上所定义的尼古丁口香糖用于治疗患有烟草依赖和/或电子烟依赖渴求的人的用途。
本发明涉及以上所定义的尼古丁口香糖,该尼古丁口香糖用于在治疗患有烟草依赖和/或电子烟依赖渴求的人时使用。
实施例
本发明的具体实施方案通过以下实施例来示出。本发明并不受限于在这些实施例中列出的具体限制。
成分的量在实施例中以不同方式表达,并且不与最终的口香糖一致。然而,对于本领域的技术人员而言,如何重新计算并开发根据本公开的口香糖是显而易见的。
实施例1:用于尼古丁口香糖的芯的粉末混合物。
具有不同量的尼古丁和不同量的缓冲剂、基于多元醇的填充剂以及甜味剂的表。
NHT=尼古丁酒石酸氢盐
NRC=尼古丁树脂酸盐复合物
所有量均以mg/口香糖计
将所有成分进行混合并通过710μm的筛网过筛,以确保粉末混合物的良好分布而没有团块/聚集物。
实施例2:口香糖基础剂以及新型尼古丁口香糖的生产
根据本发明的尼古丁口香糖可通过常规口香糖制造方法来生产:
口香糖基础剂从商业口香糖基础剂生产商获得。具有尼古丁离子交换树脂的口香糖基础剂的制备是根据US 3,877,468中公开的一个或多个方法/实施例来进行。
具有粉末芯的口香糖的制备是使用常规糖果机根据US 5,976,581中公开的一个或多个方法/实施例来进行。
WO2006/124366公开了配制和制备尼古丁口香糖的方法,该尼古丁口香糖具有包含在基于多元醇的硬包衣内部的基于聚合物的膜。
实施例3:具有根据实施例1的粉末芯的尼古丁口香糖的评估。
5名受试者评估来自实施例1的粉末混合物样品1-7,其中粉末存在于根据实施例2制备的口香糖内。测量渴求缓解的时间,并发现介于10秒至30秒之间,这取决于受试者如何咀嚼尼古丁口香糖。
此外,受试者必须针对口感和其是否能感觉到粉末而对不同产品进行评分(低评分为1并且高评分为5)。高评分5意味着适口性良好并且无粉末感。
所有受试者对样品1-7给出评分5。使用木糖醇或甘露糖醇、不同的缓冲剂或甜味剂均没有区别。为了获得统计学意义,这需要在更大的受试者群体中进行重复,但给出了指示。
Claims (10)
1.一种尼古丁口香糖,所述尼古丁口香糖包括:
i.粉末芯,所述粉末芯包含至少尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物、甜味剂、缓冲剂和基于多元醇的填充剂;和
ii.口香糖包衣,所述口香糖包衣包含至少口香糖基础剂和尼古丁离子交换树脂,
其中来自所述粉末芯的所述尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物具有立即释放,并且来自所述口香糖包衣的所述尼古丁离子交换树脂具有延长释放。
2.根据权利要求1所述的尼古丁口香糖,其中所述粉末芯以至多80mg的量存在,并且所述口香糖包衣以约950mg的量存在。
3.根据权利要求1至2所述的尼古丁口香糖,其中所述粉末芯以约20mg至约60mg的量存在。
4.根据权利要求1至3所述的尼古丁口香糖,所述尼古丁口香糖还包括至少一个基于多元醇的硬包衣,其包覆所述口香糖包衣的外部。
5.根据权利要求1至4所述的尼古丁口香糖,其中所述甜味剂选自由以下项组成的组:糖精、糖精钠、天冬甜素、乙酰磺胺酸钾、纽甜、索马甜、甘草素、三氯蔗糖、环己氨基磺酸盐、二氢查耳酮、爱德万甜、阿力甜、非洲奇果蛋白和应乐果甜蛋白以及它们的混合物。
6.根据权利要求1至5所述的尼古丁口香糖,其中所述缓冲剂选自由以下项组成的组:碳酸钠、碳酸氢钠、碳酸钾、碳酸氢钾、氨丁三醇碱(Tris碱)或氨丁三醇的对应的共轭酸,诸如氨丁三醇盐酸盐(Tris HCl)、磷酸三钠、磷酸氢二钠、磷酸二氢钠、磷酸三钾、磷酸氢二钾、磷酸二氢钾以及它们的混合物。
7.根据权利要求6所述的尼古丁口香糖,其中所述缓冲剂是碳酸钠和/或碳酸氢钠。
8.根据权利要求1至7所述的尼古丁口香糖,其中所述基于多元醇的填充剂和/或所述基于多元醇的硬包衣选自由以下项组成的组:木糖醇、赤藓糖醇、乳糖醇、甘露糖醇、麦芽糖醇、异麦芽酮糖醇、阿拉伯糖醇和山梨糖醇或它们的混合物。
9.根据前述权利要求中任一项所述的尼古丁口香糖,其中所述粉末芯包含量为每块口香糖约0.5mg至约5.0mg的尼古丁酒石酸氢盐和/或尼古丁二酒石酸盐二水合物(以游离碱计算),并且所述口香糖包衣包含量为约0.25mg至约6.0mg的尼古丁离子交换树脂(以游离碱计算)。
10.根据权利要求1至9中任一项所述的尼古丁口香糖用于治疗患有烟草和/或电子烟依赖渴求的人的用途。
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