CN104721066B - 用多羟基烷基醇使芦丁增溶的方法 - Google Patents
用多羟基烷基醇使芦丁增溶的方法 Download PDFInfo
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- CN104721066B CN104721066B CN201310703023.4A CN201310703023A CN104721066B CN 104721066 B CN104721066 B CN 104721066B CN 201310703023 A CN201310703023 A CN 201310703023A CN 104721066 B CN104721066 B CN 104721066B
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- rutin
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- hydroxy alkyl
- premix
- alkyl alcohol
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Abstract
本发明总体涉及提高芦丁溶解度的口腔护理组合物,其包含芦丁和至少一种多羟基烷基醇。本发明还涉及使用和制备所述口腔护理组合物的方法。
Description
背景技术
口腔炎症与包括例如牙周炎在内的常见口腔疾病有关。牙龈炎是牙龈疾病的初期阶段。牙龈炎的原因是牙菌斑,其是在牙齿和牙龈上形成的柔软、粘性、无色的细菌膜。牙菌斑,如果置之不理,产生可以使牙龈组织发炎或感染而导致牙龈炎的毒素。未处理的牙龈炎最终可从牙龈扩散至支撑牙齿的韧带和骨,可导致牙周炎。
芦丁(IUPAC名称: 2-(3,4-二羟基苯基)-5,7-二羟基-3-[α-L-吡喃鼠李糖基-(1→6)-β-D-吡喃葡萄糖基氧基]-4H-色烯-4-酮; [153-18-4])是由黄酮醇槲皮素和二糖芦丁糖形成的糖苷,具有以下结构:
芦丁见于多种植物,包括芸香(Ruta graveolens)、桑叶、鱼腥草(Houttuynia cordata Thunb)、中国槐(Sophora japonica L.)、某些荞麦品种、柑橘和苹果。芦丁抑制血小板聚集,据信具有抗氧化和抗炎特性。但是,芦丁只微溶于水(溶解度约13 mg/100mL),这种特性明显限制其在口腔护理制剂中的递送和功效。
发明简述
我们评估了芦丁在牙膏中作为抗牙龈炎药的用途,例如用于中和自由基以便保护口腔黏膜细胞免受氧化损伤,以及减轻炎症。但是,证明芦丁难以配制,因为它疏水且可溶性差。由于口腔环境含水,所以对牙齿的有效递送受到限制。我们已经发现要成为有效的抗氧化剂,芦丁必须溶于水相。越多芦丁溶于水相,抗氧化效能越强。
我们用许多物质进行了实验以提高芦丁的溶解度,其中大部分都证明无效。但是,我们惊奇地发现以特定比率和浓度添加一种或更多种多羟基烷基醇,大大地增加芦丁的水溶性。
因此,在一个方面本发明涉及包含芦丁和至少一种或更多种多羟基烷基醇的口腔护理组合物。多羟基烷基醇降低芦丁的疏水性,帮助其溶于水中。
本发明涵盖组合物1.0——一种包含芦丁和至少一种多羟基烷基醇的口腔护理组合物,其中多羟基烷基醇与芦丁的重量比为至少5:1,如至少10:1,例如5:1至50:1,如约10:1。
例如,在多个方面本发明涵盖:
1.1 组合物1,其中组合物通过或可通过形成包含芦丁和多羟基烷基醇的预混合物获得,其中使芦丁基本溶于预混合物,然后将预混合物与组合物中其它成分合并。
1.2 组合物1.1,其中多羟基烷基醇选自丙二醇、山梨醇、甘油及其混合物。
1.3 组合物1.1或1.2,其中多羟基烷基醇与芦丁在预混合物中的比率为约10:1。
1.4 任何上述组合物,其中多羟基烷基醇包含100%丙二醇。
1.5 上述组合物1.1至1.3中的任何一种,其中多羟基烷基醇包含丙二醇和甘油,其中丙二醇与甘油的比率选自10%:90%至90%:10%;15%:85%至85%:15%,15%:85%至25%:75%,45%:55%至55%:45%,85%:15%至75%:25%,80%:20%,50%:50%和20%:80%。
1.6 上述组合物1.1至1.3中的任何一种,其中多羟基烷基醇包含丙二醇和山梨醇,其中丙二醇与山梨醇的比率选自70%:30%至90%:10%,75%:25%至85%:15%和80%。
1.7 任何上述组合物,其中芦丁在组合物中的量是有效减轻炎症和/或对口腔软组织的氧化损伤的量。
1.8 任何上述组合物,其中芦丁在组合物中的量是0.05-5%,例如0.1-1%,例如约0.5%。
1.9 任何上述组合物,其中在组合物中溶解芦丁的量占组合物中总芦丁的至少20%,例如其中可通过高效液相层析(HPLC)检测组合物中溶解芦丁的量,例如其中在实施HPLC之前将组合物以约5:1的水:组合物比率稀释在水中。
1.10 任何上述组合物,其中组合物进一步包含一种或更多种另外的植物提取物,例如其中植物提取物来自选自以下的属:牛至属(Origanum)、百里香属(Thymus)、薰衣草属(Lavandula)、鼠尾草属(Salvia)、蜜蜂花属(Melissa)、孜然芹属(Cuminum)、欧芹属(Pelroselinum)、金盏花属(Calendula)、万寿菊属(Tageles)、乳香属(Boswellia)、接骨木属(Sambucus)、骨湃香脂树属(Copaifera)、姜黄属(Curcuma)、葱属(Allium)、聚合草属(Symphylum)、石榴属(Punica)、埃塔棕属(Eulerpe)、槐属(Sophora)、大黄属(Rheum)、荞麦属(Fagopyrum)、茶属(Camellia)、黄连属(Coplis)、北美黄连属(Hydraslis)、十大功劳属(Mahonia)、黄檗属(Phellodendron)、小檗属(Berberis)、黄根树属(Xanthorhiza)、忍冬属(Lonicera)、越橘属(Vaccinium)、樟属(Cinnamomum)、葡萄属(VlZlS)、榄仁属(Terminalia)、松属(Pinus)、合欢属(Albizia)、楝属(Melia)、刺茉莉属(Salvadora)、泡林藤属(Paullinia)、胡椒属(Piper)、蒲桃属(Syzygium)、没药属(Commiphora)、胡桃属(Juglans)、黄芩属(Sculellaria)和木兰亚属(Magnolia)。
1.11 任何上述组合物,其进一步包含选自橙皮素、橙皮苷、圣草酚、槲皮素、万寿菊黄素和万寿菊苷的化合物。
1.12 任何上述组合物,其包含选自以下的抗菌剂:卤代二苯基醚(如三氯生)和草药提取物和精油(如迷迭香提取物、茶提取物、木兰提取物、麝香草酚、薄荷醇、桉树脑、香叶醇、香芹酚、柠檬醛、日柏酚、儿茶酚、水杨酸甲酯、表没食子儿茶素没食子酸酯、表没食子儿茶精、没食子酸、米斯瓦克(miswak)提取物、沙棘提取物)。
1.13 任何上述组合物,其中组合物通过形成包含芦丁和丙二醇的预混合物制备,其中使芦丁基本溶于预混合物,然后将预混合物与组合物中其它成分合并,其中预混合物进一步包含一种或更多种微溶物,如调味剂、抗菌剂或植物提取物,如其选自在1.7、1.8或1.9列出的化合物。
1.14 任何前述组合物,其在(如通过刷牙)应用于口腔后,有效减轻或抑制牙龈炎,减轻或抑制对口腔软组织的损伤,和/或促进口腔溃疡或伤口的愈合。
1.15 一种组合物,其通过或可通过将如任何上述组合物列出的成分合并获得。
1.16 任何上述组合物,其中组合物是牙膏或漱口水。
1.17 任何上述组合物,其中组合物是牙膏,任选进一步包含一种或更多种水、研磨剂、表面活性剂、发泡剂、维生素、聚合物、酶、湿润剂、增稠剂、抗微生物剂、防腐剂、调味剂、着色剂和/或其组合。
1.18 任何上述组合物,其中组合物是通过或可通过形成包含芦丁和多羟基烷基醇的预混合物的过程获得的牙膏,其中使芦丁基本溶于预混合物,然后将预混合物与牙膏基质合并,例如包含一种或更多种水、研磨剂、表面活性剂、发泡剂、维生素、聚合物、酶、湿润剂、增稠剂、抗微生物剂、防腐剂、调味剂、着色剂和/或其组合的牙膏基质。
1.19 段落1.18的过程,其中首先混合芦丁和丙二醇,接着与山梨醇混合。
本发明还涵盖方法2.0——一种改善有需要的受试者的口腔健康例如治疗、减轻或抑制牙龈炎、治疗、减轻或抑制对口腔软组织的损伤和/或促进口腔溃疡或伤口的愈合的方法,所述方法包括将有效量的与丙二醇组合的芦丁应用于有需要的受试者的口腔,例如将组合物1及其下列组合物中的任何一种口腔组合物应用于有需要的受试者的口腔。
在另一个实施方案中,本发明提供丙二醇提高芦丁在口腔护理制剂中的溶解度的用途。
在一方面本发明部分涉及制备口腔护理组合物(如牙膏)如组合物1及其下列组合物中的任何一种的方法或过程,其中口腔护理组合物包含芦丁和一种或更多种多羟基烷基醇,所述方法或过程包括形成包含芦丁和一种或更多种多羟基烷基醇的预混合物,其中使芦丁基本溶于预混合物,然后将预混合物与组合物中其它成分合并。例如,在一个实施方案中,所述过程包括:
● 合并芦丁与一种或更多种多羟基烷基醇;
● 加温包含芦丁和一种或更多种多羟基烷基醇的组合,同时混合该组合,例如在约60℃水浴中加温和混合约10分钟(如使用IKA架空混合器),以形成预混合物;和
● 冷却预混合物,如冷却至约室温;
● 混合预混合物与口腔护理基质如牙膏基质。
本领域技术人员将清楚本发明的其它实施方案。
发明详述
如用于本文,本文描述的所有测量水平都是按总组合物的重量计,除非另外指示。另外,本文引用的所有参考文献都通过引用以其整体结合到本文中。但是,在本公开内容的任何定义与引用的参考文献的那些定义之间冲突的情况下,以本公开内容为准。
“安全和有效的量”如用于本文意指足够治疗口腔如减少牙菌斑、牙龈炎和/或色斑且不损害口腔组织和结构的量。
如用于本文,“清洁”一般指除去靶表面上的污染物、灰尘、杂质和/或异物。例如,在其中表面是牙釉质的口腔表面的背景下,清洁可除去至少一些膜或色斑,比如牙菌斑生物膜、表膜或牙石。
术语“口腔组合物”在本文中用于指明这样的制品,其在正常使用过程中在口腔内保持足以接触基本上所有牙齿表面的时间并且故意不吞下。此类制品包括例如洁牙剂比如牙膏和凝胶、漱口水、口香糖和锭剂。
多种植物提取物含有活性化合物芦丁,据信其清除超氧自由基、螯合金属离子、调节中性粒细胞爆发、抑制脂质过氧化、维持生物学抗氧化剂还原型谷胱甘肽和还原型Fenton反应(其产生活性氧物质)。因此,芦丁具有抗氧化、抗炎、抗癌、抗血栓形成、细胞保护和血管保护活性,这对口腔组合物有益。
如用于本文,所有百分数都以总组合物重量的重量%计,除非另外指示。
本发明的口腔组合物(如组合物1及其下列组合物中的任何一种)还可包含本领域已知的牙齿增白或牙齿漂白组合物。合适的增白和漂白组合物包括过氧化物、金属亚氯酸盐、过硫酸盐。过氧化物包括氢过氧化物、过氧化氢、碱金属和碱土金属的过氧化物、有机过氧化合物、过氧酸及其混合物。碱金属和碱土金属的过氧化物包括过氧化锂、过氧化钾、过氧化钠、过氧化镁、过氧化钙、过氧化钡及其混合物。其它过氧化物包括过硼酸盐、过氧化脲及其混合物。合适的金属亚氯酸盐可包括亚氯酸钙、亚氯酸钡、亚氯酸镁、亚氯酸锂、亚氯酸钠和亚氯酸钾。根据选择的试剂,可加入有效量例如基于组合物总重量计约1%至约20%重量的此类试剂。
口腔组合物(如组合物1及其下列组合物中的任何一种)任选包含防牙垢组合物,例如在Gaffar等的美国专利号5,292,526中讨论的一种或更多种防牙垢组合物。在各种实施方案中,防牙垢组合物包含一种或更多种聚磷酸盐。防牙垢组合物可包含以有效防牙垢的量存在于口腔组合物中至的少一种全部或部分中和的碱金属或铵三聚磷酸盐或六偏磷酸盐。防牙垢活性物还可包括至少一种有效防牙垢量的水溶性、线性、分子脱水的聚磷酸盐。防牙垢活性物还可包括钾盐和钠盐的混合物,所述盐中的至少一种作为聚磷酸盐防牙垢剂以有效防牙垢量存在。防牙垢活性剂还可含有有效防牙垢量的存在于钠盐和钾盐的混合物中的线性分子脱水聚磷酸盐防牙垢剂。钾与钠在组合物中的比率可高达小于3:1。聚磷酸盐可以各种量存在于口腔组合物中,所述量比如为以下量:其中聚磷酸根离子与抗菌剂的重量比范围为从超过0.72:1至小于4:1,或者其中抗菌增强剂与聚磷酸根离子的重量比范围为约1:6至约2.7:1,或者其中抗菌增强剂与聚磷酸盐的重量比范围为约1:6至约2.7:1。其它有用的防牙垢剂包括聚羧酸盐聚合物和聚乙烯甲基醚/马来酸酐(PVM/MA)共聚物,比如GANTREZ®。
本发明的口腔护理组合物(如组合物1及其下列组合物中的任何一种)还可任选包含一种或更多种能够与细菌细胞壁中存在的钙络合的螯合剂。这种钙的结合削弱细菌细胞壁,增进细菌溶解,减少牙菌斑的形成。这些防牙垢剂可以例如包含聚磷酸盐,如焦磷酸盐、三聚磷酸盐或六偏磷酸盐,如采用钠或钾盐形式。可用于本发明的一类螯合剂是可溶性焦磷酸盐。用于本发明组合物的焦磷酸盐可以是任何碱金属焦磷酸盐。在某些实施方案中,盐包括四碱金属焦磷酸盐、二碱金属二酸焦磷酸盐、三碱金属单酸焦磷酸盐及其混合物,其中碱金属是钠或钾。水合和非水合形式的盐都可使用。可用于本发明组合物的焦磷酸盐的有效量为至少0.1 重量%,如约0.5 重量%至约5 重量%,约1 重量%至约3 重量%,或者约2%。
本发明的口腔护理组合物(如组合物1及其下列组合物中的任何一种)还可任选包含一种或更多种酶。有用的酶包括任何可获得的蛋白酶、葡聚糖水解酶、内切糖苷酶、淀粉酶、齿斑葡聚糖酶(mutanases)、脂肪酶和粘蛋白酶或其可相容性混合物。在某些实施方案中,酶是蛋白酶、葡聚糖酶、内切糖苷酶和齿斑葡聚糖酶。在另一个实施方案中,酶是木瓜蛋白酶、内切糖苷酶或者葡聚糖酶和齿斑葡聚糖酶的混合物。在本发明中几种可相容性酶的混合物的酶在一个实施方案中占约0.002%至约2.0%,或者在另一个实施方案中占约0.05%至约1.5%,或者在又一个实施方案中占约0.1%至约0.5%。
在制备口腔护理组合物(如组合物1及其下列组合物中的任何一种)时,可能需要加入一些增稠材料以提供期望的粘稠度或者稳定或提高制剂的性能。在某些实施方案中,增稠剂是羧基乙烯基聚合物、角叉菜胶、羟乙基纤维素和纤维素醚的水溶性盐比如羧甲基纤维素钠和羧甲基羟乙基纤维素钠。还可掺入天然树胶比如刺梧桐树胶、阿拉伯胶和西黄蓍胶。胶体硅酸镁铝或者精细分开的二氧化硅可用作增稠组合物的组分以进一步改善组合物的质地。在某些实施方案中,使用占总组合物重量约0.05%至约10%的量的增稠剂,如约0.1%至约7%,约0.5%至约5%,或者约1%、2%,或者小于约2%。用于口腔组合物的其它增稠剂包括天然和合成的树胶和胶体,比如角叉菜胶(爱尔兰苔藓(Irish moss))、黄原胶、羧甲基纤维素钠、淀粉、聚乙烯吡咯烷酮、羟乙基丙基纤维素、羟丁基甲基纤维素、羟丙基甲基纤维素和羟乙基纤维素。在一些实施方案中,聚合物可另外促进活性剂的递送,此类组合物可包括聚合物比如聚乙烯甲基醚马来酸共聚物,例如以商品名Gantrez销售的聚乙烯甲基醚马来酸共聚物。
本发明的口腔护理组合物(如组合物1及其下列组合物中的任何一种)还可任选包含一种或更多种表面活性剂,如非离子、阳离子或两性离子表面活性剂,或其组合。例如,在一些实施方案中,组合物可包含至少一种选自月桂基硫酸钠、椰油酰胺丙基甜菜碱及其组合的表面活性剂。在一些实施方案中,组合物包含阴离子表面活性剂,如其选自:脂肪酸单甘油酯单硫酸盐、高级烷基硫酸盐(如月桂基硫酸钠);高级烷基芳基磺酸盐(如线性十二烷基苯磺酸钠),高级烯烃磺酸盐(如高级烯烃磺酸钠),高级烷基碱金属磺基乙酸盐(如月桂基磺基乙酸钠);1,2-二羟基丙磺酸盐的高级脂肪酸酯;低级脂族氨基羧酸碱金属盐的基本饱和的高级脂族酰胺(如在脂肪酰基基团中具有12至16个碳原子),高级烷基聚-低级烷氧基(10至100个烷氧基)硫酸钠,椰子油和牛油的高级脂肪酸钠和钾皂。在一些实施方案中,组合物可包含阴离子表面活性剂,如其选自月桂基硫酸钠、月桂醇聚醚硫酸钠及其混合物;如可包含占组合物重量0.5-3%的量的月桂基硫酸钠。
本发明的组合物(如组合物1及其下列组合物中的任何一种)还可包含本领域技术人员已知的一种或更多种调味剂或着色剂。用于实施本发明的调味剂包括但不限于精油以及各种调味的醛、酯、醇和类似的材料。精油的实例包括留兰香、薄荷、冬青、黄樟、丁香、鼠尾草、桉树、马郁兰、肉桂、柠檬、莱檬、葡萄柚和橙的油。还有用的化学物是比如薄荷醇、香芹酮和茴香脑等化合物。某些实施方案采用薄荷和留兰香的油。将调味剂以约0.1至约5%重量和约0.5至约1.5%重量的浓度掺入口腔组合物中。
通过以下非限制性实施例进一步说明本发明。
实施例
实施例1-在水相的芦丁水平与其抗氧化功效的相关性
使芦丁溶于水中以制备一定范围不同水平的芦丁溶液。通过细胞染色法测量芦丁溶液的保护功效(ΔE*a,b值越大,保护功效越强)。结果如下:
表1-芦丁的保护功效
这些结果显示溶于水溶液的芦丁越多,ΔE*a,b值越大,由此它可提供越强的抗氧化功效。因此,将芦丁简单加至牙膏制剂中是不够的。为了使芦丁起效,制剂必须为芦丁提供最佳溶解度。
通过将芦丁与不同物质混合,并评估芦丁是否溶解(如通过溶液的相对清晰度所见),初步评价增溶剂。意外地发现丙二醇(PG)是溶解芦丁的最有效的溶剂湿润剂。例如,在被评价的多元醇湿润剂材料中——丙二醇、PEG-40氢化蓖麻油、甘油、PEG 600和山梨醇——其中将0.5%芦丁加至10 g每种测试增溶剂,被评价的湿润剂的溶解度能力按以下顺序排列,其中丙二醇最好,山梨醇最差。
丙二醇>>甘油> PEG600 ≈ PEG-40氢化蓖麻油>山梨醇
进一步设计实验以优化用于芦丁溶解度的湿润剂浓度。表2列出用预混合物和牙膏基质调配的9种原型,其中预混合物含有芦丁和丙二醇、甘油和山梨醇中的一种或更多种。
如下通过混合芦丁和各种增溶剂制备预混合物:
1) 将配方量的一种或多种增溶剂加入容器内;
2) 将配方量的芦丁加入装有湿润剂的容器内;
3) 使用60℃水浴,将内容物加温并在用IKA架空混合器不断搅拌的情况下混合10分钟;
4) 使预混合物冷却至室温后,将内容物转移至牙膏混合器并与牙膏基质以表2显示的比率混合10分钟。
表2-使芦丁在预混合物A中增溶的湿润剂的配方设计
表3说明包含如表2所述芦丁预混合物的牙膏的牙膏基质制剂。
表3
实施例2
通过高效液相层析评估最终制剂中的可溶性芦丁,所述层析使用a)具有自动采样器的HPLC装置(Waters 2695);b)柱:Agilcnt Zorbax SB-CN, C 18, 5um, 250×4.6 mm;和c) UV检测器Waters 2489。测试条件如下:a)流动相:甲醇/H2O/H3PO4 (550:450:1.8);b)流速:1 ml/min;c)检测波长:256nm d)运行时间:12分钟。程序如下:a)将5g牙膏样品放在玻璃烧杯中,加入5ml水并搅拌30分钟;b)将浆料转移至离心管并用水稀释至25ml,离心5分钟(8000 rmp);c)过滤并通过HPLC。
表4证明具有丙二醇(PG)的牙膏组合物在牙膏组合物中表现更高的可溶性芦丁浓度。与只含有甘油或山梨醇的组合物相比,包含丙二醇和甘油的组合物也表现更高的可溶性芦丁浓度。对含有5%甘油或5%山梨醇的预混合物见到最佳溶解度,但是只发现分别为0.08%和0.04%的可检测的可溶性芦丁。
在丙二醇与甘油或山梨醇的组合中,结果显示在配方中丙二醇含量越高,在牙膏中的可溶性芦丁越高。在预混合期间引入山梨醇至丙二醇内实质上降低芦丁的溶解度。
表4-在牙膏中的可溶性芦丁测试结果(通过HPLC方法)
实施例3
重复上文实施例2中关于样品2描述的可溶性芦丁的测试,但是代替如在样品2中首先混合丙二醇和山梨醇,然后将芦丁加至混合物并继续混合这些步骤的是,首先使芦丁溶于丙二醇,然后将山梨醇加至混合物并继续混合(在下表5中的样品10)。
表5证明山梨醇的添加顺序导致检测的芦丁量增加75% (0.14-0.08/0.08×100%= 75%)。
表5-在牙膏中的可溶性芦丁测试结果(通过HPLC方法)-不同添加顺序
如本领域技术人员将理解,可在不脱离本发明精神的情况下对本文所述实施方案进行多种改变和修饰。所有此类变更旨在落在随附权利要求的范围内。
Claims (11)
1.一种口腔护理组合物,其包含:(a)由溶于至少一种多羟基烷基醇的芦丁组成的预混合物,所述至少一种多羟基烷基醇为丙二醇和山梨醇,其中多羟基烷基醇与芦丁的重量比为5∶1-50∶1;和(b)包含甘油和山梨醇的口腔护理基质,其中所述口腔护理组合物包含0.05-5%的芦丁;其中先使芦丁溶于丙二醇,然后将山梨醇加至混合物并继续混合。
2.权利要求1的组合物,其中所述多羟基烷基醇与芦丁的比率为10∶1。
3.权利要求1的组合物,其中芦丁在组合物中的量为0.5%。
4.权利要求1的组合物,其中溶解的芦丁在组合物中的量占组合物中总芦丁的至少20%。
5.权利要求1的组合物,其中所述组合物是牙膏,其进一步包含水、研磨剂、表面活性剂、发泡剂、维生素、聚合物、酶、湿润剂、增稠剂、抗微生物剂、防腐剂、调味剂、着色剂和/或其组合中的一种或更多种。
6.权利要求1的组合物在制备用于改善有需要的受试者口腔健康的制剂中的用途,其中所述制剂应用于有需要的受试者的口腔,以减轻炎症、对口腔软组织的氧化损伤和/或促进口腔溃疡或伤口的愈合。
7.权利要求6的用途,其中减轻的炎症是牙龈炎。
8.至少一种多羟基烷基醇提高芦丁在权利要求1所述口腔护理组合物中的溶解度的用途,其中所述至少一种多羟基烷基醇为丙二醇和山梨醇。
9.一种用于制备权利要求1的口腔护理组合物的方法,其包括形成包含芦丁和至少一种多羟基烷基醇的预混合物,其中使芦丁溶于所述预混合物,然后将所述预混合物与组合物中的其它成分合并。
10.权利要求9的方法,其中所述预混合物在60℃的温度下制备。
11.权利要求9的方法,其中所述预混合物通过混合10分钟来制备。
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