CN107735106A - 用于递送疏水物质的水性多层组合物 - Google Patents
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- CN107735106A CN107735106A CN201680033675.3A CN201680033675A CN107735106A CN 107735106 A CN107735106 A CN 107735106A CN 201680033675 A CN201680033675 A CN 201680033675A CN 107735106 A CN107735106 A CN 107735106A
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Abstract
一种用于递送疏水物质的水性多层组合物,其包含:(i)约50重量%至约80重量%的苯乙醇和/或苯丙醇;(ii)(a)约10重量%至约20重量%的聚甘油‑4‑月桂酸酯/癸二酸酯和(b)约10重量%至约20重量%的聚甘油‑6‑辛酸酯/癸酸酯的混合物;(iii)约10重量%至约20重量%的辛烷‑1,2‑二醇;(iv)任选约10重量%至约20重量%的1,3‑丙二醇;和(v)约5.0重量%至约80重量%的水。还描述了所述组合物的使用和制备方法。
Description
发明领域
本申请涉及多层组合物,更具体而言,涉及用于递送诸如苯乙醇和/或苯丙醇等疏水物质的水性多层组合物。
发明背景
苯乙醇和苯丙醇是个人护理、家用、工业和制药产品等的典型香味物质组分。这些物质具有防腐剂和/或抗微生物增效作用。然而,使用苯乙醇和苯丙醇物质限制了制剂师,难点在于,例如,其在水中的溶解性差,在蒸发和分配到包装材料时的活性损失,以及由于其高蒸气压引起的强烈气味。
鉴于上述,仍然需要找到增加溶解度、防止活性损失和降低苯乙醇和苯丙醇的蒸气压的方法。
因此,本申请的主要目的是提供一种解决方案,以提高难溶性苯乙醇和苯丙醇香味物质的水溶性。
本申请的另一个目的是降低苯乙醇和苯丙醇化合物的蒸气压。
本申请的另一个目的是防止苯乙醇和苯丙醇化合物的活性损失。
本申请的另一个目的是使用完全天然和环保认证的表面活性剂体系来制备多层囊泡组合物。
WO2013105047A2公开了通过保护和修复真皮细胞外基质(ECM),将花姜酮(zerumbone)用于皮肤紧致的非治疗性化妆局部治疗,其中,所述局部施用的治疗使用了zemea(丙二醇)和NatraGem S140(聚甘油-4-月桂酸酯/癸二酸酯(和)聚甘油-6辛酸酯/癸酸酯(和)水。
WO2012055855A1公开了1-60重量%的月桂酰赖氨酸乙酯(LAE)的浓缩制剂,其包含(i)1-99重量%的至少一种选自于苯氧基乙醇,苄醇,癸二醇,己二醇,戊二醇,十二醇,甘油的脂肪酸单酯,所述脂肪酸选自于辛酸,癸酸,十一碳烯酸和月桂酸,聚甘油的单酯(聚甘油-3-辛酸酯),苯乙醇,苯丙醇和乙基己基甘油,条件是当苯氧基乙醇作为所述至少一种溶剂或表面活性剂存在时,其浓度应为2-99重量%;(ii)任选0-20重量%的一种或多种具有抗菌活性的有机酸;(iii)任选0-10重量%的一种或多种具有抗菌活性的天然提取物;(iv)任选0-10重量%的一种或多种螯合剂;(v)任选0-10重量%的一种或多种抗氧化剂;和(vi)任选0-50重量%的一种或多种没有抗菌活性的溶剂或表面活性剂。这些浓缩物可以作为防腐剂添加到个人护理用的化妆品组合物中。
发明概述
本申请的主要目的是提供苯乙醇和/或苯丙醇的有效递送体系,苯乙醇和苯丙醇是与个人护理、家用、清洁以及工业和机构产品有关的许多终端用户应用的典型香味物质组分。
本申请的另一个目的是提供用于递送疏水物质的水性多层组合物,其包含:(i)约50重量%至约80重量%的苯乙醇和/或苯丙醇;(ii)(a)约10重量%至约20重量%的聚甘油-4-月桂酸酯/癸二酸酯和(b)约10重量%至约20重量%的聚甘油-6-辛酸酯/癸酸酯的混合物;(iii)约10重量%至约20重量%的辛烷-1,2-二醇;(iv)任选约10重量%至约20重量%的1,3-丙二醇;和(v)约5.0重量%至约80重量%的水。
本申请的另一方面是提供一种多层组合物,其包含苯乙醇和/或苯丙醇,其能够抑制或杀死酵母、霉菌孢子、革兰氏(+)菌菌株、革兰氏(-)菌菌株、引起痤疮的菌株、或引起气味的菌株。
本申请的另一方面是提供了一种制备水性多层组合物的方法,其中所述方法包括混合:(i)约50重量%至约80重量%的苯乙醇和/或苯丙醇;(ii)(a)约10重量%至约20重量%的聚甘油-4-月桂酸酯/癸二酸酯和(b)约10重量%至约20重量%的聚甘油-6-辛酸酯/癸酸酯的混合物;(iii)约10重量%至约20重量%的辛烷-1,2-二醇;(iv)任选约10重量%至约20重量%的1,3-丙二醇;和(v)约5.0重量%至约80重量%的水。
本申请的另一方面涉及杀死细菌、真菌、霉菌、酵母和病毒或抑制其在那些易于生长微生物的化妆品、个人护理、家用、清洁、和/或工业和机构产品中的生长的方法。
本申请的一个重要方面是提供了当本申请的疏水性物质被并入化妆品或个人护理或清洁,工业和机构产品中时,用于受控地或周期性递送本申请的疏水性物质的方法。
本发明的详细说明
虽然本说明书以权利要求作为结论,所述权利要求特别指出并明确要求了被认为是属于本发明的事项,但是可以预期,通过阅读本发明的下述详细说明和研究所包括的实施例,可以更容易地理解本发明。
术语“包含”在本文中是指各种可用于本文的组合物中的任选的、相容成分,条件是,重要成分以合适的形式和浓度存在。因此,术语“包含”涵盖并包括更加限制性的术语“由...组成”和“基本上由...组成”,其可用于表征所述多层组合物的必需成分,如苯乙醇,苯丙醇,聚甘油月桂酸酯/癸二酸酯,聚甘油-6-辛酸酯/癸酸酯,辛烷-1,2-二醇,和1,3-丙二醇。
除非另有说明,否则本文所用的所有百分比、份数、比例和比率均基于整个组合物的重量。所有与所列成分有关的这些重量均基于活性成分的含量,因此,除非另有说明,否则不包括可能包含在市售材料中的溶剂或副产物。
对本发明的单数特征或限制的所有引用应包括相应的复数特征或限制,反之亦然,除非在所引用的文中另有说明或有明确相反的暗示。
本文使用的数值范围旨在包括在该范围内所包含的每个数值和每个数值子集,无论是否具体公开。此外,这些数值范围应被解释为支持针对该范围内的任何数值或数值子集的权利要求。
如本文所用,词语“优选”和变体是指在某些情况下提供某些益处的本发明的实施方案。然而,在相同或其它的情况下,其它的实施例也可以是优选的。此外,对一个或多个优选实施例的叙述并不意味着其它实施方案不是有用的,并不旨在将其它实施方案排除在本发明的范围之外。
本文中的“一个实施方案”,“一个方面”或“一个版本”或“一个目的”的引用包括一个或多个这样的实施方案、方面、版本或目的,除非文中另有明确规定。
出于所有目的,本文所引用的所有出版物、文章、论文、专利、专利出版物和其它参考文献与本文公开内容相一致的程度全部内容在此并入本文。
本文所用的术语“防腐剂”或“抗微生物剂”应理解为是指,例如,杀菌剂,杀真菌剂,杀藻剂,除水生植物剂,除草剂,杀虫剂,农药,植物生长调节剂等的试剂,其被用于抑制细菌,真菌,藻类,毛虫,昆虫,幼虫,霉菌,啮齿动物,蜘蛛,蠕虫等生物和/或微生物物种的生长和/或杀死它们。
术语“防腐”是指防止或延缓由于微生物侵袭而引起的任何消费产品的变坏。防腐剂是阻碍可能存在于任何消费品,主要是水基的消费品中的细菌和真菌菌株生长或杀死它们的活性成分。因此,任何消费品的防腐作用都是通过使用单一防腐剂或防腐剂混合物来进行的,以具有广谱抗菌活性。
如本文和权利要求中所述的术语“广谱”是指本申请的防腐组合物具有抑制或杀死广泛范围的微生物的能力,这些微生物会腐败或破坏任何容易受到微生物攻击的消费品。
如本文所使用的,“稳定”和“稳定性”是指在暴露于合理预期的运输、储存及其在终端用户应用中的使用条件下,化学性质、物理均匀性和/或颜色不显著受到影响的组合物。稳定性可以通过经验观察或通过本领域技术人员已知的适当化学和/或物理检验方法来确定。
本文所描述的是用于递送疏水物质的水性多层组合物,其包含:(i)约50重量%至约80重量%的苯乙醇和/或苯丙醇;(ii)(a)约10重量%至约20重量%的聚甘油-4-月桂酸酯/癸二酸酯和(b)约10重量%至约20重量%的聚甘油-6-辛酸酯/癸酸酯的混合物;(iii)约10重量%至约20重量%的辛烷-1,2-二醇;(iv)任选约10重量%至约20重量%的1,3-丙二醇;和(v)约5.0重量%至约80重量%的水。
本申请的难溶于水/难与水混溶的疏水性物质,苯乙醇和苯丙醇,是广泛用于许多个人护理,清洁,家庭,工业和机构产品中的香味物质,其中所述疏水性物质可以提高或增强所述防腐/抗菌活性。
根据本申请的一个重要实施方案,预期使用至少一种苯基烷基醇化合物,其可以作为适用的疏水物质用作香水或香味物质,其中所述烷基具有C1-C20的碳链长度。
本申请中所使用的苯基烷基醇或苯乙醇或苯丙醇的量为约50重量%至约55重量%,约56重量%至约60重量%,约61重量%至约65重量%,约66重量%至约70重量%,约71重量%至约75重量%,约76重量%至约80重量%。
根据本申请的另一个重要实施方案,所述疏水物质可以以多层结构的形式递送,从而以受控或周期性释放的方式释放所述疏水物质。此外,所述多层结构能够通过增加它们在油/水界面的分配,使最大部分进入水相,从而增加所包含的疏水性物质的水溶性。此外,所述多层结构使其易于并入到最终产物制剂中,并且促进在油水界面处活性物质的递送,这又提高了它们的功效并提高了活性物质如苯乙醇和苯丙醇的稳定性。在所述界面的受控和有针对性的递送有助于以更快的速度和更好的效果杀死生物。
此外,层状囊泡结构保持香味组分缓慢释放,降低高强度的香味,并以控制的方式在油/水界面处递送活性物质。通过优化所述囊泡层状结构来控制活性物质向所述油/水界面的递送。
包含苯乙醇和/或苯丙醇的多层组合物能够降低苯乙醇和苯丙醇化合物的蒸发,从而降低活性损失。因此,所述多层组合物还可以降低苯乙醇和苯丙醇的蒸气压,进而降低强烈或刺激性气味。
在本申请的一个实施方案中,所述多层结构可以是多层泡囊或多层脂质体或多层泡囊的形式。这种多层结构在递送活性物质方面可以提供诸如稳定性、包埋性、功效性和更好的生物活性等优点。
此外,预期采用其它可能的递送体系,例如单层囊泡/脂质体/泡囊,微粒,纳米颗粒,微粒,纳米颗粒,微乳液,纳米乳液,纳米球,纳米胶囊,固体-脂质纳米颗粒(SLN),纳米结构的脂质载体,包封方法,大囊泡,胶束,反胶束或层状液晶结构。
在优选的实施方案中,本申请的多层组合物如果并入其中则不会使最终用户产品产生任何显著的颜色变化。
根据本申请的另一个实施方案,选择包含至少两种非离子表面活性剂的混合物以形成本申请的多层囊泡体系。优选的实施方案包括两种非离子表面活性剂的混合物,其中第一非离子表面活性剂的HLB值为约8至12,第二非离子表面活性剂的HLB值为约14至17。另一相关实施方案采用HLB值为约10至12的第一非离子表面活性剂和HLB值为约14至16的第二非离子表面活性剂。此外,第一与第二非离子表面活性剂的比例为约1:10至约10:1。
一个重要的实施方案使用(a)约10重量%至约20重量%的聚甘油-4-月桂酸酯/癸二酸酯,第一非离子表面活性剂和(b)约10重量%至约20重量%的聚甘油-6-辛酸酯/癸酸酯,第二非离子表面活性剂。本申请的表面活性剂可从Croda Personal Care作为NatragemS140NP商购获得。其是100%的天然产物,并由Ecocert批准为天然的。可用的其它非限制性商业产品包括NatraGemTM E145和NatraGemTM S150。此外,NatraGem S140是被(良好的环境选择),Nordic Ecolabelling(Swan)和EU Ecoflower(2014/893/EU)广泛接受的。
此外,考虑使用其它聚甘油脂肪酸酯作为本申请的非离子表面活性剂,包括但不限于,脂肪酸的聚甘油酯,例如C3至C22脂肪酸,如丙酸,丁酸,戊酸,己酸,庚酸,辛酸,壬酸,癸酸,十一烷酸,月桂酸,十三烷酸,肉豆蔻酸,十五烷酸,棕榈酸,十七烷酸,硬脂酸,十九烷酸,二十烷酸,二十一烷酸,二十二烷酸,二十三烷酸,二十四烷酸,二十五烷酸,蜡酸,二十七烷酸,二十九烷酸,二十九烷酸,三十烷酸,三十一烷酸,三十二烷酸,三十三酸,三十四酸,三十五烷酸,三十六烷酸,三十七酸,三十八酸,α-亚麻酸,十八碳四烯酸,二十碳五烯酸,二十二碳六烯酸,亚油酸,γ-亚麻酸,Dihomo-γ-亚麻酸,花生四烯酸,肾上腺酸,棕榈油酸,异油酸,二十烯酸和油酸。
聚甘油酯的一些非限制性实例是聚甘油-4-癸酸酯,聚甘油-2-癸酸酯,聚甘油-4-辛酸酯,聚甘油-6-辛酸酯,聚甘油-6-癸酸酯,聚甘油-4-辛酸酯/癸酸酯,聚甘油-6辛酸酯/癸酸酯,聚甘油-3-椰油酸酯,聚甘油-4-椰油酸酯,聚甘油-10-十亚油酸酯,聚甘油-10-十油酸酯,聚甘油-10-十硬脂酸酯,聚甘油-3-二癸酸酯,聚甘油-3二椰油酸酯,聚甘油-10-二癸酸酯,聚甘油-2-二异硬脂酸酯,聚甘油-3-二异硬脂酸酯,聚甘油-10-二异硬脂酸酯,聚甘油-4-二月桂酸酯,聚甘油-2-二油酸酯,聚甘油-3-二油酸酯,聚甘油-6-二油酸酯,聚甘油-10-二油酸酯,聚甘油-6-二棕榈酸酯,聚甘油-10-二棕榈酸酯,聚甘油-2-二聚羟基硬脂酸酯,聚甘油-2-二硬脂酸酯,聚甘油-6-二硬脂酸酯,聚甘油-10-二硬脂酸酯,聚甘油-10-七油醇酯,聚甘油-10-七硬脂酸酯,聚甘油-6-六油酸酯,聚甘油-10-六油酸酯,聚甘油-2-异棕榈酸酯,聚甘油-2-异硬脂酸酯,聚甘油-4-异硬脂酸酯,聚甘油-5-异硬脂酸酯,聚甘油-6-异硬脂酸酯,聚甘油-10-异硬脂酸酯,聚甘油-2-月桂酸酯,聚甘油-3-月桂酸酯,聚甘油-4-月桂酸酯,聚甘油-4-月桂酸酯/癸二酸酯,聚甘油-4-月桂酸酯/琥珀酸酯,聚甘油基-5-月桂酸酯,聚甘油-6-月桂酸酯,聚甘油-10-月桂酸酯,聚甘油-3-肉豆蔻酸酯,聚甘油-10-肉豆蔻酸酯,聚甘油-2-油酸酯,聚甘油-3-油酸酯,聚甘油-4-油酸酯,聚甘油-5-油酸酯,聚甘油-6-油酸酯,聚甘油-8-油酸酯,聚甘油-10-油酸酯,聚甘油-3-棕榈酸酯,聚甘油-6-棕榈酸酯,聚甘油-10-五月桂酸酯,聚甘油-10-五亚油酸酯,聚甘油-4-五油酸酯,聚甘油-10-五油酸酯,聚甘油-3-五蓖麻酸酯,聚甘油-10-五蓖麻酸酯,聚甘油-4-五硬脂酸酯,聚甘油-6-五硬脂酸酯,聚甘油-10-五硬脂酸酯,聚甘油-3-聚蓖麻油酸酯,聚甘油-6-聚蓖麻油酸酯,聚甘油-3-蓖麻油酸酯,聚甘油-2-倍半异硬脂酸酯,聚甘油-2-倍半油酸酯,聚甘油-2-倍半硬脂酸酯,聚甘油-3-硬脂酸酯,聚甘油-2-硬脂酸酯,聚甘油-4-硬脂酸酯,聚甘油-8-硬脂酸酯,聚甘油-10-硬脂酸酯,聚甘油-2-四异硬脂酸酯,聚甘油-6-四油酸酯,聚甘油基-10-四油酸酯,聚甘油-2-四硬脂酸酯,聚甘油-2-三异硬脂酸酯,聚甘油-3-三异硬脂酸酯,聚甘油-10-三油酸酯,聚甘油-4-三硬脂酸酯,聚甘油三硬脂酸酯,聚甘油-10-三硬脂酸酯。
类似地,可用作表面活性剂的脂肪酸,例如C3至C22脂肪酸的聚乙二醇酯包括但不限于丙酸,丁酸,戊酸,己酸,庚酸,辛酸,壬酸,癸酸,十一烷酸,月桂酸,十三烷酸,肉豆蔻酸,十五烷酸,棕榈酸,十七烷酸,硬脂酸,十九烷酸,二十烷酸,二十一烷酸,二十二烷酸,二十三烷酸,二十四烷酸,二十五烷酸,蜡酸,二十七烷酸,二十九烷酸,二十九烷酸,三十烷酸,三十一烷酸,三十二烷酸,三十三酸,三十四酸,三十五烷酸,三十六烷酸,三十七酸,三十八酸,α-亚麻酸,十八碳四烯酸,二十碳五烯酸,二十二碳六烯酸,亚油酸,γ-亚麻酸,Dihomo-γ-亚麻酸,花生四烯酸,肾上腺酸,棕榈油酸,异油酸,二十烯酸和油酸。
此外,非磷脂两亲成分也可用于形成囊泡,且这些成分通常是在引入水或极性溶剂如醇时会水合形成层状物,然后自身闭合以形成泡罩或囊的两亲性脂质。这种两亲性油脂可以包括烷氧基化脂肪羧酸的单、二或三酯;烷氧基化甘油脂肪酸的单酯、二酯或三酯,磺化脂肪酸的单酯、二酯或三酯等。烷氧基化脂肪酸酯的实例包括具有约2至500个烷氧基或乙氧基的那些化合物。实例包括具有2-500个重复环氧乙烷单元的PEG(聚乙二醇)。所述脂肪酸酯可以是单、二或三酯,如果是二或三酯,其是与烷氧基化和甘油化部分反应的。在一个优选的实施方案中,所述烷氧基化脂肪酸酯或烷氧基化甘油脂肪酸酯,其中所述脂肪酸是约4-30个碳原子的脂族碳链。这种脂肪酸酯的实例包括但不限于PEG和脂肪羧酸的单酯,PEG和脂肪羧酸的二酯,或PEG和脂肪羧酸的三酯;PEG,甘油和脂肪羧酸的二酯;PEG,甘油和脂肪羧酸的三酯。这些分子的实例包括PEG丁酸酯,PEG异丁酸酯,PEG戊酸酯,PEG己酸酯,PEG二己酸酯,PEG庚酸酯,PEG二庚酸酯,PEG辛酸酯,PEG二辛酸酯,PEG壬酸酯,PEG二壬酸酯,PEG十二烷酸酯,PEG硬脂酸酯,PEG二硬脂酸酯,PEG异硬脂酸酯,PEG二异硬脂酸酯,PEG月桂酸酯,PEG二月桂酸酯,PEG肉豆蔻酸酯,PEG二肉豆蔻酸酯,PEG山嵛酸酯,PEG油酸酯,PEG二油酸酯,PEG亚油酸酯,PEG二亚油酸酯等。还可以使用甘油、PEG和脂肪羧酸的酯,例如PEG甘油二丁酸酯,PEG甘油二戊酸酯,PEG甘油二己酸酯,PEG甘油二庚酸酯,PEG甘油二辛酸酯,PEG甘油二壬酸酯,PEG甘油二癸酸酯,PEG甘油二硬脂酸酯,PEG甘油二异硬脂酸酯,PEG甘油二月桂酸酯,PEG甘油二肉豆蔻酸酯,PEG甘油二山嵛酸酯,PEG甘油二油酸酯,PEG甘油二亚油酸酯等。在上述实施例中,重复环氧乙烷部分的数目可以为1-500(如PEG1-500),如果需要,甘油部分的数量可以为1-500,但所述分子应包含足够的环氧乙烷和/或甘油部分,以赋予所述分子的至少一部分必要的亲水性。
在一个实施方案中,脱水山梨糖醇衍生物被认为是形成非磷脂囊泡的适用试剂。适用的脱水山梨糖醇衍生物包括脱水山梨糖醇的酯或醚,其是通过山梨糖醇脱水形成的杂环醚。脱水山梨糖醇可以通过羟基的乙氧基化和/或酯化衍生。适用于酯化的酸包括具有约4-30个碳原子的脂肪羧酸,更优选具有6-22个碳原子的脂肪羧酸。可用于形成囊泡的适用脱水山梨糖醇衍生物的实例包括脱水山梨糖醇的PEG衍生物,其中重复环氧乙烷单元的数量为2-200,如PEG脱水山梨糖醇蜂蜡,PEG脱水山梨醇羊毛脂酸酯,PEG脱水山梨糖醇月桂酸酯,PEG脱水山梨糖醇油酸酯,PEG脱水山梨糖醇棕榈酸酯,PEG脱水山梨糖醇全异硬脂酸酯,PEG脱水山梨糖醇全油酸酯,PEG脱水山梨糖醇硬脂酸酯,PEG脱水山梨糖醇四油酸酯,甘油/山梨糖醇/油酸酯/羟基硬脂酸酯,PEG脱水山梨糖醇椰油酸酯,PEG脱水山梨糖醇二异硬脂酸酯,PEG脱水山梨糖醇异硬脂酸酯,PEG脱水山梨糖醇四硬脂酸酯,PEG脱水山梨糖醇三异硬脂酸酯;还适用是聚山梨酸酯,其是由脱水山梨糖醇得到的聚合物。例如,聚山梨酸酯20至85或聚山梨醇酯20至85乙酸酯是适用的,数字20至85是指重复的脱水山梨糖醇部分的数目。脱水山梨糖醇酯,如脱水山梨糖醇辛酸酯,椰油酸酯,二异硬脂酸酯,二油酸酯,二硬脂酸酯,异硬脂酸酯,月桂酸酯,油酸酯,橄榄酸酯,棕榈酸酯,倍半异硬脂酸酯,倍半油酸酯,倍半硬脂酸酯,硬脂酸酯,三异硬脂酸酯,三油酸酯等也可用于形成囊泡。
根据本申请的一个重要实施方案,辛烷-1,2-二醇或辛二醇被用作用来制备本申请的多层组合物的辅助表面活性剂。辛二醇的量为约10重量%至约20重量%。其它范围包括约10重量%至约12重量%,约12重量%至约14重量%,约14重量%至约16重量%,约16重量%至约18重量%,或约18重量%至约20重量%。
本申请中使用的适用的溶解度增强剂选自于基于烷基二醇或二醇的化合物。可用于本申请的基于烷基二醇的化合物含有至少两个碳原子,其中,烷基二醇化合物的饱和脂族烃的任何两个氢原子被羟基取代,并且其中,所述烷基二醇的羟基(-OH)可以是伯、仲或叔羟基。在一个实施方案中,公开了两个羟基官能团可以彼此相邻(邻近),或者可以作为-OH基团存在于它们的末端位置,或者随机存在于C2-20碳链的任何两个碳原子上。结构I显示了本申请的所需烷基二醇,其中,R1、R2、R3、R4独立地是氢、C1-20烷基/环烷基、C1-20取代烷基/环烷基、烃基官能团。此外,“A”可以是直接键合,独立地是氢、C1-20烷基/环烷基,C1-20取代烷基/环烷基、和烃基官能团。术语“烃基”是指可进一步含有一个或多个杂原子的取代或未取代的烷基、烯基、环烷基、环烯基或芳烷基、单、二或多官能基团。然而,本申请的优选的烷基二醇是1,3-丙二醇,其中丙二醇的量为约10重量%至约20重量%。其它范围包括约10重量%至约12重量%,约12重量%至约14重量%,约14重量%至约16重量%,约16重量%至约18重量%,或约18重量%至约20重量%。
使用水来制备本申请的水性多层组合物。所述水可以是去离子水,双重或三重蒸馏水,反渗透水或易于在市场上获得的任何纯水。制备所述多层组合物所需的量为约5.0重量%至约80重量%。
在适用的实施方案中,考虑使用本申请的多层组合物与至少一种选自于由下述化合物所组成的组中的防腐化合物的组合:三氯沙,2-甲基-4-异噻唑啉-3-酮(MIT),1,2-苯并异噻唑啉-3-酮(BIT),5-氯-2-甲基-4-异噻唑啉-3-酮(CMIT),2-辛基-4-异噻唑啉-3-酮(OIT),3-碘代-2-丙炔基丁基-氨基甲酸酯(IPBC),3-碘丙炔基-N-苯基氨基甲酸酯(IPPC),吡啶硫酮锌(ZnPy),溴硝醇,季铵化合物,对羟基苯甲酸酯,对羟基苯甲酸烷基酯,氯苯甘油醚,苄醇,有机酸,山梨酸及其盐,苯甲酸及其盐,水杨酸及其盐,山梨酸钾,苯甲酸钠,苯氧基乙醇,重氮烷基脲,咪唑烷基脲,羟甲基甘氨酸钠,乙内酰脲,吡啶硫酮钠,苯乙醇,苯丙醇,苯扎铵季铵化合物,脂肪酸及其盐,α-羟基酸及其盐,β酸及其盐盐,甘油,己基甘油,环庚三烯酚酮,倍半萜烯,天然防腐剂,和/或乙基己基甘油。
包含苯乙醇和苯丙醇的本申请多层组合物能够抑制或杀死酵母,霉菌孢子,革兰氏(+)菌株,革兰氏(-)菌株,引起痤疮的菌株,或产生气味的菌株,其中,所述微生物菌株包括但不限于热带假丝酵母(Candida tropicalis),白色念珠菌(Candida albicans),异常汉森酵母(Hansenula anomala),酿酒酵母(Saccharomyces cerevisiae),接合酵母(Torulaspora delbreuckii),拜耳接合酵母(Zygosaccharomyces bailii),鲁氏接合酵母(Zygosaccharomyces rouxii),枯草杆菌(Bacillus subtilis),蜡样芽孢杆菌(Bacilluscereus),金黃色葡萄球菌(Staphylococcus aureus),表皮葡萄球菌(Staphylococusepidermidis),大肠杆菌(Escherichia coli),鼠伤寒沙门氏菌(Salmonellatyphimurium),肠炎沙门氏菌(Salmonella enteritidis),绿脓假单胞菌(Pseudomonasaeruginosa),黑曲霉(Aspergillus niger),黄曲霉(Aspergillus flavus),岛青霉(Penicillium islandicum),桔青霉(Penicillium citrinum),产黄青霉(Penicilliumchrysogenum),尖孢镰刀菌(Fusarium oxysporum),禾谷镰孢(Fusarium graminearum),茄病镰刀菌(Fusarium solani),互生交链孢霉(Alternaria alternata),巴曲霉(Aspergillus brasiliensis),洋葱伯克霍尔德氏菌(Burkhodelia cepacia),产气肠杆菌(Enterobacteraerogenes),阴沟肠杆菌(Enterobacter cloacae),格高菲肠杆菌(Enterobacter gergoviae),克雷波氏肺炎菌(Klebsiella pneumoniae),普通变形杆菌(Proteus vulgaris),螢光假單胞菌(Pseudomonas fluorescens),恶臭假单胞菌(Pseudomonas putida),嗜松青微菌(Penicillium pinophilum),藤黄微球菌(Micrococcus luteus),细枝状杆菌(Corynebacterium minutissimum),结膜干燥棒状杆菌(Corynebacterium xerosis),杰氏棒杆菌(Corynebacterium jeikeium),痤疮丙酸杆菌(Propionibacterium acnes)和/或总状毛霉(Mucor racemosus)。
所述水性多层组合物在室温下储存至少2年是稳定的。当温度在每24小时内从50℃循环至-24℃时,所述组合物在至少5次冷冻/融化循环中是稳定的,或在约45℃下稳定至少4周。
根据本申请的另一个实施方案,所述水性多层组合物可以用于水性和非水性的最终用户应用中,包括化妆品,盥洗品,个人护理产品,口腔护理产品,护肤品,头发护理产品,家用和清洁用品,肥皂和沐浴用品,工业和机构清洁产品,消毒产品,伤口护理,卫生产品,农业组合物,纺织工业,涂料工业和/或洗涤产品。用于水性和非水性最终用户产品/组合物中的组合物的量通常为所述总组合物的约0.01重量%至约5.0重量%。
在另一个实施方案中,本申请提供了制备上述水性多层组合物的方法,其中所述方法包括混合:(i)约50重量%至约80重量%的苯乙醇和/或苯丙醇;(ii)(a)约10重量%至约20重量%的聚甘油-4-月桂酸酯/癸二酸酯和(b)约10重量%至约20重量%的聚甘油-6-辛酸酯/癸酸酯的混合物;(iii)约10重量%至约20重量%的辛烷-1,2-二醇;(iv)任选约10重量%至约20重量%的1,3-丙二醇;和(v)约5重量%至约80重量%的水。
包含本申请的水性多层组合物的个人护理,家庭,清洁,和/或工业和机构产品需要使用有效量的所述组合物,所述有效量为0.01重量%至5.0重量%的所述产品的总质量。
本申请的一个实施方案涉及杀死细菌,真菌,霉菌,酵母和病毒或抑制其在易于微生物生长的化妆品,个人护理,家庭,清洁,和/或的工业和机构产品中的生长的方法。
本申请的另一个实施方案提供了一种用于受控或周期性递送并入到化妆品或个人护理或家庭,清洁,工业和机构产品中的本申请的疏水性物质的方法。
此外,通过下述实施例详细说明了本发明的某些方面。本文给出的实施例目的在于说明,不旨在限制本发明。
实施例1:
实施例2:
实施例3:
实施例4:
实施例5:
实施例6:
实施例1-6的上述组合物为澄清至浅黄色的溶液,在45℃下稳定1个月,并通过5次冻/融循环。
实施例7:
水性多层组合物的功效数据表明其可以杀死革兰氏(+)和革兰氏(-)的细菌菌株,酵母和真菌。
如下所述的标准筛选乳液组合物包含实施例1和2的组合物,其在C相中含有1重量%的防腐剂或不含防腐剂作为参比。
然后在28天的双重接种试验后,将含有具有1%或不具有防腐剂(参比)的实施例1或2或3的组合物的标准乳液进行用各种微生物挑战试验,其中,所述样品用革兰氏(+)细菌(金黄色葡萄球菌6538),革兰氏(-)细菌(大肠杆菌8739,绿脓假单胞菌9027和洋葱伯克霍尔德菌25416)的复合物接种,而所述细菌在第0天和第21天接种至最终浓度约10^6-7cfu/ml,所述真菌复合物在第0天和第21天接种至最终浓度约10^5-6孢子/ml。接种的样品在第2、7、14、21和28天进行铺板。回收培养基是用于细菌的Letheen琼脂(Letheen Agar)和用于真菌的马铃薯葡萄糖琼脂(Potato Dextrose agar)。在每个时间间隔下回收的微生物如下表1所示:
表1:标准筛选乳液制剂的PET挑战测试
如表1所示,含有具有1重量%的实施例1或2或3的组合物之一的标准筛选乳液显著降低了接种微生物的水平并阻止了它们的生长。
虽然已经参考某些优选实施例详细描述了本发明,但是应当理解的是,本发明不限于那些精确的实施方案。相反,鉴于本公开,在不脱离本发明的范围和精神的情况下,许多修改和变化都将呈现于本领域技术人员。
Claims (17)
1.用于递送疏水物质的水性多层组合物,其包含:
i.约50重量%至约80重量%的苯乙醇和/或苯丙醇;
ii.(a)约10重量%至约20重量%的聚甘油-4-月桂酸酯/癸二酸酯和(b)约10重量%至约20重量%的聚甘油-6-辛酸酯/癸酸酯的混合物;
iii.约10重量%至约20重量%的辛烷-1,2-二醇;
iv.任选约10重量%至约20重量%的1,3-丙二醇;和
v.约5.0重量%至约80重量%的水。
2.根据权利要求1的水性多层组合物,其中所述苯乙醇和苯丙醇是香味物质和/或防腐剂/抗微生物活性增强物质。
3.根据权利要求1的水性多层组合物,其中所述多层结构能够以受控或周期性释放的方式递送疏水物质。
4.根据权利要求1的水性多层组合物,其中所述非离子表面活性剂的混合物选自(a)至少一种HLB值为8-12的表面活性剂和(b)至少一种HLB值为14-17的表面活性剂,其中,(a)和(b)的混合物的比例为约1:10至约10:1。
5.根据权利要求1的水性多层组合物,其中通过增加疏水物质在油/水界面的分配使最大部分进入到水相中,所述多层结构能够提高疏水物质的水溶性。
6.根据权利要求1的水性多层组合物,其中所述多层结构能够降低疏水物质的蒸气压,从而控制苯乙醇和苯丙醇的刺激性气味的释放。
7.根据权利要求1的水性多层组合物,其中所述组合物与至少一种选自以下组中的防腐化合物组合:三氯沙,2-甲基-4-异噻唑啉-3-酮(MIT),1,2-苯并异噻唑啉-3-酮(BIT),5-氯-2-甲基-4-异噻唑啉-3-酮(CMIT),2-辛基-4-异噻唑啉-3-酮(OIT),3-碘代-2-丙炔基丁基-氨基甲酸酯(IPBC),3-碘丙炔基-N-苯基氨基甲酸酯(IPPC),吡啶硫酮锌(ZnPy),溴硝醇,季铵化合物,对羟基苯甲酸酯,对羟基苯甲酸烷基酯,氯苯甘油醚,苄醇,有机酸,山梨酸及其盐,苯甲酸及其盐,水杨酸及其盐,山梨酸钾,苯甲酸钠,苯氧基乙醇,重氮烷基脲,咪唑烷基脲,羟甲基甘氨酸钠,乙内酰脲,吡啶硫酮钠,苯乙醇,苯丙醇,苯扎铵季铵化合物,脂肪酸及其盐,α-羟基酸及其盐,β酸及其盐,甘油,己基甘油,环庚三烯酚酮,倍半萜烯,天然防腐剂,和/或乙基己基甘油。
8.根据权利要求1的水性多层组合物,其中所述组合物能够抑制或杀死酵母、霉菌孢子、革兰氏(+)细菌菌株、革兰氏(-)细菌菌株、引起痤疮的菌株、或引起气味的菌株。
9.根据权利要求1的水性多层组合物,其中所述组合物能够抑制或杀死热带假丝酵母(Candida tropicalis)、白色念珠菌(Candida albicans)、异常汉森酵母(Hansenulaanomala)、酿酒酵母(Saccharomyces cerevisiae)、接合酵母(Torulasporadelbreuckii)、拜耳接合酵母(Zygosaccharomyces bailii)、鲁氏接合酵母(Zygosaccharomyces rouxii)、枯草杆菌(Bacillus subtilis)、蜡样芽孢杆菌(Bacilluscereus)、金黃色葡萄球菌(Staphylococcus aureus)、表皮葡萄球菌(Staphylococusepidermidis)、大肠杆菌(Escherichia coli)、鼠伤寒沙门氏菌(Salmonellatyphimurium)、肠炎沙门氏菌(Salmonella enteritidis)、绿脓假单胞菌(Pseudomonasaeruginosa)、黑曲霉(Aspergillus niger)、黄曲霉(Aspergillus flavus)、岛青霉(Penicillium islandicum)、桔青霉(Penicillium citrinum)、产黄青霉(Penicilliumchrysogenum)、尖孢镰刀菌(Fusarium oxysporum)、禾谷镰孢(Fusarium graminearum)、茄病镰刀菌(Fusarium solani)、互生交链孢霉(Alternaria alternata)、巴曲霉(Aspergillus brasiliensis)、洋葱伯克霍尔德氏菌(Burkhodelia cepacia)、产气肠杆菌(Enterobacter aerogenes)、阴沟肠杆菌(Enterobacter cloacae)、格高菲肠杆菌(Enterobacter gergoviae)、克雷波氏肺炎菌(Klebsiella pneumoniae)、普通变形杆菌(Proteus vulgaris)、荧光假单胞菌(Pseudomonas fluorescens)、恶臭假单胞菌(Pseudomonas putida)、嗜松青微菌(Penicillium pinophilum),藤黄微球菌(Micrococcus luteus),细枝状杆菌(Corynebacterium minutissimum),结膜干燥棒状杆菌(Corynebacterium xerosis),杰氏棒杆菌(Corynebacterium jeikeium),痤疮丙酸杆菌(Propionibacterium acnes)和/或总状毛霉(Mucor racemosus)。
10.根据权利要求1的水性多层组合物,其中所述组合物在室温下储存稳定至少2年。
11.根据权利要求1的水性多层组合物,其中当温度在每24小时从50℃循环至-24℃时,所述组合物至少在5个冻/融循环是稳定的,或者在约45℃下至少稳定4周。
12.根据权利要求1的水性多层组合物,其中组合物可以用于基于水性和非水性的最终用户应用中,包括化妆品,盥洗品,个人护理产品,口腔护理产品,护肤品,头发护理产品,家用和清洁用品,肥皂和沐浴用品,工业和机构清洁产品,消毒产品,伤口护理,卫生产品,农业组合物,纺织工业,涂料工业和/或洗涤产品。
13.根据权利要求1的水性多层组合物,其中所述组合物在基于水性和非水性最终用户产品/组合物中的用量为整个组合物的约0.01重量%至约5.0重量%。
14.制备根据权利要求1的水性多层组合物的方法,其中,所述方法包含混合:
i.约50重量%至约80重量%的苯乙醇和/或苯丙醇;
ii.(a)约10重量%至约20重量%的聚甘油-4-月桂酸酯/癸二酸酯和(b)约10重量%至约20重量%的聚甘油-6-辛酸酯/癸酸酯的混合物;
iii.约10重量%至约20重量%的辛烷-1,2-二醇;
iv.任选约10重量%至约20重量%的1,3-丙二醇;和
v.约5.0重量%至约80重量%的水。
15.个人护理、家用、清洁、和/或工业和机构产品,其包含相对于所述产品的总质量约0.01重量%至5.0重量%的权利要求1的水性多层组合物。
16.一种杀死细菌、真菌、霉菌、酵母和病毒或抑制其在易于生长微生物的化妆品、个人护理、家用、清洁和/或工业和机构产品中的生长的方法,其包含掺入约0.01重量%至5.0重量%的权利要求1的防腐组合物。
17.一种受控或周期性递送疏水物质至化妆品或个人护理或家庭、清洁和/或工业和机构产品中的方法,其包含向所述产品中掺入约0.01重量%至5.0重量%的权利要求1的防腐组合物。
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PCT/US2016/024704 WO2016164205A1 (en) | 2015-04-09 | 2016-03-29 | An aqueous multilamellar composition for delivering hydrophobic substances |
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CN113647387A (zh) * | 2021-09-02 | 2021-11-16 | 山东国仓健生物科技有限公司 | 苯乙醇在防治小麦赤霉病中的应用 |
CN115768262A (zh) * | 2020-04-23 | 2023-03-07 | 阿奇英国生物灭杀剂有限公司 | 具有聚甘油酯的协同作用杀生物剂组合物 |
CN115942871A (zh) * | 2020-04-23 | 2023-04-07 | 阿奇英国生物灭杀剂有限公司 | 具有聚甘油酯的协同作用防腐剂/个人护理组合物 |
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CN111050736A (zh) * | 2017-08-28 | 2020-04-21 | 株式会社Adeka | 抗菌抗霉组合物 |
ES2870500T3 (es) * | 2017-12-14 | 2021-10-27 | Clariant Int Ltd | Vesículas para la administración retardada de fragancia, su preparación y uso de las mismas |
JP2022520109A (ja) * | 2019-02-15 | 2022-03-28 | サンコー・エナジー・インコーポレイテッド | 殺虫剤として使用するための光増感剤及びキレート剤の組み合わせ |
WO2021008696A1 (de) * | 2019-07-16 | 2021-01-21 | Symrise Ag | Riechstoffmischung enthaltend 1,3-propandiol |
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CA2982338A1 (en) | 2016-10-13 |
BR112017021668B1 (pt) | 2023-03-14 |
MX2017012958A (es) | 2018-05-22 |
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