CN112118739A - 包含一种或多种具有9-21个碳原子的驱虫脂肪酸的驱虫组合物 - Google Patents
包含一种或多种具有9-21个碳原子的驱虫脂肪酸的驱虫组合物 Download PDFInfo
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- CN112118739A CN112118739A CN201980023347.9A CN201980023347A CN112118739A CN 112118739 A CN112118739 A CN 112118739A CN 201980023347 A CN201980023347 A CN 201980023347A CN 112118739 A CN112118739 A CN 112118739A
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- insect repellent
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- repellent composition
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Abstract
本发明涉及一种驱虫组合物,其包含:‑包含一种或多种具有9‑21个碳原子的脂肪酸的驱虫成分;‑非水性溶剂;‑小于1%重量的水。
Description
技术领域
本发明涉及一种驱虫组合物,其包含一种或多种具有9-21个碳原子的脂肪酸。
本发明特别适用于对有害昆虫具有驱除功能的组合物,所述有害昆虫例如是刺或咬类嗜血昆虫,如蚊子。
背景技术
这样的组合物通常旨在通过如下方式被使用:直接施用到受试者的皮肤上,或者间接地施用到空气中或其他表面上,这例如借助于喷雾器、球形施涂器或其他施用方式来实施。
例如,由文献US-5 594 029已知一种旨在局部施用到人或动物受试者的皮肤上或衣物上的组合物,所述组合物包含因其驱虫性能而被使用的椰子油脂肪酸。
同样,由文献WO-00/72676已知一种组合物,该组合物尤其旨在施用到受试者的皮肤和/或衣物上,其中月桂酸(或十二烷酸)被用作蜱的驱除剂。
这些组合物通常包含主要由水组成的溶剂,这类溶剂易于获得,但需要添加表面活性剂才能真正有效地用作驱虫成分的溶剂。
另外,这些解决方案并不完全令人满意,因为随着时间的推移它们不再具有足够的效力。因此,它们需要定期重新施用,这可能是令人厌倦的并导致保护中断。
发明内容
本发明旨在通过特别提出一种驱虫组合物来完善现有技术,所述驱虫组合物具有改善的随时间的效力,同时易于施用到受试者的皮肤上。
为此,本发明提供了一种驱虫组合物,该驱虫组合物包含:
-包含一种或多种具有9-21个碳原子的脂肪酸的驱虫成分;
-非水性溶剂;
-小于1%重量的水。
附图说明
参考附图,本发明的其他特性和优点将在随后的各种特定实施方案的描述中显现,在附图中:
-图1a和1b是显示在实验室中对包含两种不同浓度的根据本发明的相同驱虫脂肪酸的组合物的样品进行的第一系列比较测试的结果的图,所述样品还包含水,特别是水性溶剂(“对照”样品),或者不含水,特别是非水性溶剂(“测试”样品),以凸显使用脂肪酸和非水性溶剂的无水驱虫组合物随时间的效力;
-图2是显示在包含相同浓度的根据本发明的驱虫脂肪酸以及非水性溶剂的无水样品之间的第二系列比较测试的结果的图,所述样品中的一些还包含额外的驱虫成分,以凸显使用非水性溶剂的无水驱虫组合物中该脂肪酸与所述额外成分之间的协同作用;
-图3是显示图2中给出的结果的图,其通过用根据与上述第二系列相同的方案进行的第三系列比较测试中的其他四个样品获得的结果进行补充而得到。
具体实施方式
本发明涉及一种驱虫组合物,其包含含有一种或多种具有9-21个碳原子的脂肪酸的驱虫成分。特别地,该驱虫组合物可包含具有9-21个碳原子的单一脂肪酸或脂肪酸的混合物。
这样的脂肪酸特别对有害昆虫具有驱除性能,所述有害昆虫例如是刺或咬类嗜血昆虫,如蚊子。
碳原子数大于21的脂肪酸并不适合于局部施用于受试者的皮肤上,因为它们使组合物呈糊状构造,从而使所述施用变得困难。此外,这种组合物在受试者的皮肤上留下难以去除的脂肪层,这是不希望的。
同样,碳原子数小于9的脂肪酸使组合物具有令人不悦的气味,这也是不希望的,特别是对于皮肤施用而言。
该驱虫脂肪酸可包含羧酸,特别选自壬酸,癸酸,十一烷酸,十二烷酸,十三烷酸,十四烷酸,十五烷酸,十六烷酸,十七烷酸,十八烷酸,十九烷酸,二十烷酸,二十一烷酸,十一碳烯酸,香茅酸,香叶酸或这些化合物中至少两种的混合物。
根据一种特别有效的实施方案,该驱虫脂肪酸具有12个碳原子和/或为饱和或不饱和脂肪酸。
有利地,该驱虫脂肪酸包括月桂酸(或十二烷酸)。
该驱虫脂肪酸还可包含选自以下组的酸:ω-羟基-15-甲基棕榈酸,ω-羟基植烷酸,(2E,6E,10E)-香叶基香叶酸,(2E,6E,10E,14E)-ω-羟基香叶基香叶酸。
该驱虫脂肪酸还可基于以下的脂肪酸:
-具有甲基分支的脂肪酸,特别选自以下组:(2S)-2-甲基十七烷酸,(E)-11-甲基十二烷-2-烯酸,10-甲基十二烷酸,10-甲基十一烷酸,12-甲基十八烷酸,12-甲基十五烷酸,13-甲基十五烷酸,14-甲基十六烷酸,14-甲基十五烷酸,16-甲基十七烷酸,16-甲基十八烷酸,17-甲基十八烷酸,18-甲基二十烷酸,18-甲基十九烷酸,2-甲基丁-2-烯酸,2-甲基十六烷酸,20-甲基二十二烷酸,20-甲基二十一烷酸;和/或
-具有丙基分支的脂肪酸,特别选自以下组:2-正丙基-2-戊烯酸,2-正丙基-3-戊烯酸,2-正丙基-4-戊烯酸,2-丙基-2,4-戊二烯酸,2-丙基-2-戊烯酸。
该驱虫脂肪酸还可衍生自至少一种水解植物油,所述植物油特别选自椰子(coco)油、棕榈油、摩洛哥坚果油、杏仁油、蓖麻油、鳄梨油、小麦胚芽油或者这些油中至少两种的混合物。
特别地,该组合物包含按重量计5%-50%、特别是12.5%-37.5%的驱虫脂肪酸。
该组合物还包含非水性溶剂,这使得能够改善其随时间的效力。
特别地,该组合物包含小于1%重量的水,这个量对应于形成所述组合物的各种成分中存在的任何可能的残余水剂量。
但是,该组合物优选不含水,以进一步改善其随时间的效力。
该非水性溶剂可包含至少一种选自以下组的成分:醇,酸,烷烃,烯烃,醛,胺,酰胺,酮,酯,醚,内酯,有机硅,硅氧烷,有机硫化合物(organosoufrés),有机磷化合物,矿物油,植物油,蜡,萜烯,精油或者这些成分中至少两种的混合物。
该非水性溶剂可包含至少一种选自以下组的醇:甲醇,乙醇,丙醇,丁醇,戊醇,己醇,1,3-丁二醇,单丙酸酯,2-丁基辛-1-醇,1-辛醇,2-丁基苯甲酸酯,环己醇,(1,7,7-三甲基双环[2.2.1]庚-2-基)-(1,7,7-三甲基双环[2.2.1]庚-2-基)环己-1-醇,氧基双丙二醇,癸二醇,己三醇,丁二醇,己二醇,戊二醇,二甲基辛二醇,丁基环己基丁醇,己烯醇,甲氧基丁醇,乙酸戊酯,苯甲酸戊酯,苄基二醇,苄醇,1,4:3,6-二氢-2,5-二-O-甲基-D-葡萄糖醇,1,1’-氧基二丙-2-醇,氧基二丙-2-醇,羟丙氧基丙醇,2-乙基己烷-1,3-二醇,2,6,10-十二碳三烯-1-醇,3,7,11-三甲基甘油,乙烷-1,2-二醇,己-1-醇,2-己基癸-1-醇,具有环氧乙烷(1:2)的聚合物,己基癸醇,具有环氧乙烷(1:20)的聚合物,3-甲基丁烷-1-醇,1-异丁氧基丙烷-2-醇,3-甲基丁烷-1,2-二醇,异丙醇,1-甲氧基丙烷-2-醇,3-甲氧基-3-甲基-1-丁醇,甲基醇,2-甲基-1,3-丙二醇,丁-1-醇,2,2-二甲基-1,3-丙二醇,2-辛基十二烷-1-醇,1,2-二羟基戊烷,1-苯氧基丙烷-2-醇,3-苯基丙-1-醇,聚(1,2-丁二醇)-6丙二醇,丙-1-醇,丙二醇,1-丁氧基丙-2-醇,1-丙氧基丙-2-醇,1-(1,1-二甲基乙氧基)-2-丙醇,1-甲基丙醇,2-甲基丙-2-醇,四氢糠醇,3,4-噻吩二醇,4,4’,4”-(1-甲基丙-3-叉基)三[6-叔丁基-间甲酚]2,2,4-三甲基-1,3-戊二醇,3,5,5-三甲基己-1-醇,2-乙基-2-羟甲基-1,3-丙二醇,3,5,5-三甲基己-1-醇。
该非水性溶剂可包含至少一种选自壬酸和/或D-葡糖酸的酸。
该非水性溶剂可包含至少一种选自以下组的烷烃或烯烃:戊烷,己烷,庚烷,辛烷,壬烷,癸烷,芳烃,环烷烃,椰子烷烃,环己烷,十氟戊烷,二苯甲烷,1-十二烯,异链烷烃,庚烷,1-十六烯,5-嘧啶胺,三甲基十二烷,十五烷,7-亚甲基,2,2,4-三甲基戊烷,2-甲基丁烷,1,3,5-三甲基苯,2-甲基丁烯,里格罗因十八烷,1-十八烯,辛烷,1-辛烯,石蜡油,1,1,1,3,3-五氟丙烷,戊烷,1-溴-1,1,2,2,3,3,4,4,5,5,6,6,7,7,8,8,8-十七氟辛烷,九氟(三氟甲基)环戊烷,全氟十二氢芴,2-[二氟(十一氟环己基)甲基]-1,1,2,3,3,4,4,4a,5,5,6,6,7,7,8,8,8a-十七氟十氢化萘,石油馏出物,丙基苯,1-十四碳烯,甲苯,1,1,1-三氯乙烷,1,2,4-三甲基苯,二甲基苯,十二烷,十一烷,十三烷,C13-15烷烃。
特别地,该非水性溶剂可包含烷烃或烯烃,其选自氢化烃,特别选自以下以其CAS(化学文摘社)号及其括号中的英文全称表示的那些:
-CAS 93685-81-5(《hydrocarbons,C4,1,3-butadiene-free,polymd.,triisobutylene fraction,hydrogenated》);
-CAS 93685-80-4(《Hydrocarbons,C4,1,3-butadiene-free,polymd.,tetraisobutylene fraction,hydrogenated》);
-CAS 93685-79-1(《hydrocarbons,C4,1,3-butadiene-free,polymd.,pentaisobutylene fraction,hydrogenated》)。
该非水性溶剂可包含至少一种选自苯甲醛和/或2-糠醛的醛。
该非水性溶剂可包含至少一种选自以下组的酮:丙酮,庚基环戊酮,环己酮,4-羟基-4-甲基戊-2-酮,1-乙基吡咯烷-2-酮,N-乙基吡咯烷酮,十一烷酸-4-内酯,4-羟甲基-1,3-二氧杂戊环-2-酮,丁酮,4-甲基戊-2-酮。
该非水性溶剂可包含至少一种选自以下组的胺或酰胺:油胺,羧甲基己酰基壳聚糖,N,N-二甲基癸酰胺,1-甲基吡咯烷酮,N,N’-(聚(氧四氟乙烯,氧二氟亚甲基)双(二氟亚甲基)双十八酰胺,聚(亚氨基-1,2-乙二基),α-氢-ω-氨基-乙氧基化的(氮丙啶的平均摩尔比为1000摩尔),聚(亚氨基-1,2-乙二基),α-氢-ω-氨基-乙氧基化的,多羟基硬脂酰胺基丙基二甲基胺。
该非水性溶剂可包含至少一种选自以下组的酯:壬酸乙酯,乳酸乙酯,丙酮酸乙酯,乙酸丁基环己酯,双-(1-甲基庚基)-2-丁烯二酸酯,苯甲酸,2-羟基-2-丁基辛基酯,己二酸,双(2-庚基十一烷基)酯,乙酸苄基酯,苯甲酸苄酯,乳酸丁酯,乙酸正丁酯,苯甲酸烷基酯,丁酸正辛酯,乙酸丁基环己酯,丁烯二酸,双(C12-15-烷基)酯(E),1,3-二乙酸甘油酯,己二酸二丁酯,草酸二丁酯,癸二酸二丁酯,丁二酸酯,羟基-双(2-丁基辛基),马来酸二辛基酯,双(2-乙氧基乙基)丁二酸酯,天冬氨酸,N-乙酰基-二乙酯,草酸二乙酯,癸二酸二乙酯,琥珀酸二乙酯,2,6-萘二甲酸二辛酯,己二酸双(2-乙基己基)酯,癸二酸双(2-乙基己基)酯,琥珀酸双(2-乙基己基)酯,己二酸二己酯,己二酸,二己基癸酯,癸二酸,双(2-己基癸基)酯,己二酸二异丁酯,草酸二仲丁酯,己二酸双(2-己基癸基)酯,己二酸二异癸酯,双(1-甲基庚基)酯,己二酸二异丙酯,己二酸二异癸酯,癸二酸二异丙酯,碳酸,二甲基酯,马来酸二甲酯,草酸二甲酯,邻苯二甲酸二甲酯,琥珀酸二甲酯,癸二酸酯,双(2-辛基十二烷基),己二酸二丙酯,草酸二丙酯,异十八烷酸,与2,2’-(氧双亚甲基)双[2-羟甲基-1,3-丙二醇]的戊酸酯,己二酸双(十三烷基)酯,3-羟基-1,2,4-丁三基三(2-乙基己酸)酯,乙酸乙酯,乙基乙缩醛乙酰丙酸酯,乙基甘油乙缩醛乙酰丙酸酯,丙酸,2-羟乙基酯,肉豆蔻酸乙酯,[2-(1-乙氧基乙氧基)乙基]苯,苯乙酸乙酯,乙酸2-乙基己酯,苯甲酸2-乙基己酯,1,2,3-丙三基三[乙酰氧基十八烷酸酯],1,2,3-丙三基三[(R)-12-(乙酰氧基)油酸酯],月桂酸己酯,2-羟基苯甲酸,2-己基十二烷基酯,2-甲基戊烷-2,4-二醇,乙酸异戊酯,乙酸异丁酯,苯甲酸异丁酯,苯甲酸,2-羟基-异十六烷基酯,异丙醇胺羊毛脂酸酯,乙酸异丙酯,肉豆蔻酸异丙酯(MIL),棕榈酸异丙酯,聚(氧-1,2-乙二基)聚(氧-1,2-丙二基),α-异癸基-ω-羧基甲氧基-1-甲基乙基酯,亚麻籽油的聚甘油-4酯,2-甲氧基-1-甲基乙基乙酸酯,乙酸甲酯,月桂酸/肉豆蔻酸的甲酯,油酸/棕榈酸/亚油酸/硬脂酸的甲酯,棕榈仁油的聚甘油-4酯,月桂酸/癸二酸的聚甘油-4酯,辛酸/癸酸的聚甘油-6酯,聚丙二醇,丙二醇,二辛酸丙二醇酯,乙酸丙酯,苯甲酸丙酯,碳酸亚丙酯,苯甲酸十八烷基酯,1,1-二甲基乙基乙酸酯,丙酸十四烷基酯,乙酸四氢糠酯,乙酸四氢糠酯,三醋精,柠檬酸三丁酯,十三烷酯甘油酯,三辛酸甘油酯,丙烷-1,2,3-三基2-乙基己酸酯,1,2,3-丙三基三(12-羟基十八烷酸酯),丙烷-1,2,3-三基3,5,5-三甲基己酸酯,柠檬酸三异丙酯,1,2,3-丙三基三异十八烷酸酯,三月桂酸甘油酯,丙烷-1,2,3-三基三[(9Z,12Z)-十八碳-9,12-二烯酸酯],三肉豆蔻酸甘油酯,1,2,3-丙三基三油酸酯,三棕榈酸甘油酯,三硬脂酸甘油酯,丙烷-1,2,3-三基三(十一烷酸)酯,碳酸亚乙酯,二氢-5-戊基-2(3H)-呋喃酮,柠檬酸三乙酯,十一碳烯酸庚酯(heptyl undecelynate),异壬酸异壬酯,异壬酸乙基己酯,二辛酰基醚,碳酸二辛酰基酯,乙酰基柠檬酸三丁酯(tributyl acetyl citrate),琥珀酸二辛酯,琥珀酸二辛酰基酯,琥珀酸二异辛酯,月桂酸异戊酯,辛酸椰油酯,辛酸癸酸椰油酯(coco caprylatecaprate)。
该非水性溶剂可包含至少一种选自以下组的醚:乙醇,2-(2-丁氧基乙氧基)-,1-乙酸酯,2-(2-丁氧基乙氧基)乙醇,2-丁氧基乙醇,乙酸2-丁氧基乙酯,1,1’-[亚甲基双(氧基)]二丁烷,二辛基醚,二甘醇二乙醚,二(3-甲基丁基)羟基丁二酸酯,二甲醚,戊二酸二甲酯,1,3-二氧戊环,二丙二醇二甲醚,二丙二醇异冰片醚,2-(2-乙氧基乙氧基)乙醇,2-(2-乙氧基乙氧基)乙酸乙酯,乙烷,1,1’-氧基双,1-乙氧基-1,1,2,2,3,3,4,4,4-九氟丁烷,丙烷,2-(乙氧基二氟甲基)-1,1,1,2,3,3,3-七氟,2-乙基己基-6-苄基-2,5-二氧杂哌嗪-3-基乙酸酯,聚(氧基-1,2-乙二基),α-(四氢-2-呋喃基)甲基-ω-羟基-,异辛基乳油(lactoil)妥尔油酸酯,异辛基妥尔油酸酯,1-甲氧基己烷,1,1,1,2,3,3,3,4,4-九氟-4-甲氧基丁烷,2-(二氟甲氧基甲基)-1,1,1,2,3,3,3-七氟丙烷,1-甲基吡咯烷酮,二甲氧基甲烷,聚丙烯酸酯-10的交联聚合物,叔丁基甲醚,2,2’-(亚乙基氧基)二乙醇,三甲基戊醇羟乙基醚,聚甘油-10异硬脂基醚。
特别地,该非水性溶剂可包含至少一种选自以下组的醚:聚乙二醇醚(PEG)和/或聚丙二醇醚(PPG),特别选自以下组:甲氧基PEG-25,甲氧基PEG-7,PEG-10,PEG-12,PEG-12亚油酸甘油酯,PEG-16,PEG-14,PEG-18,PEG-135,PEG-150,PEG-20,PEG-200,PEG-2苄基醚,PEG-200氢化棕榈酸甘油酯,PEG-220,PEG-3甲醚,PEG-32,PEG-33,PEG-350,PEG-4,PEG-45,PEG-4甲醚,PEG-40,PEG-45,PEG-500,PEG-55,PEG-6,PEG-7,PEG-8,PEG-9,PEG-80,PEG-90,PEG-6甲醚,PEG-7甲醚,PEG-80氢化棕榈酸甘油酯,PEG/PPG-1/2共聚物,PEG/PPG-10/30共聚物,PEG/PPG-10/65共聚物,PEG/PPG-10/70共聚物,PEG/PPG-116/6共聚物,PEG/PPG-12/35共聚物,PEG/PPG-125/30共聚物,PEG/PPG-15/15乙酸酯,PEG/PPG-150/35共聚物,PEG/PPG-16/17共聚物,PEG/PPG-160/30共聚物,PEG/PPG-160/31共聚物,PEG/PPG-17/6共聚物,PEG/PPG-18/4共聚物,PEG/PPG-19/21共聚物,PEG/PPG-20/20共聚物,PEG/PPG-20/60共聚物,PEG/PPG-20/65共聚物,PEG/PPG-20/9共聚物,PEG/PPG-200/40共聚物,PEG/PPG-200/70共聚物,PEG/PPG-22/25共聚物,PEG/PPG-23/17共聚物,PEG/PPG-23/50共聚物,PEG/PPG-240/60共聚物,PEG/PPG-25/30共聚物,PEG/PPG-26/31共聚物,PEG/PPG-28/30共聚物,PEG/PPG-3/17共聚物,PEG/PPG-30/35共聚物,PEG/PPG-30/33共聚物,PEG/PPG-30/35共聚物,PEG/PPG-30/55共聚物,PEG/PPG-35/40共聚物,PEG/PPG-35/9共聚物,PEG/PPG-38/8共聚物,PEG/PPG-4/2共聚物,PEG/PPG-5/30共聚物,PEG/PPG-5/35共聚物,PEG/PPG-50/40共聚物,PEG/PPG-6/2共聚物,PEG/PPG-7/50共聚物,PEG/PPG-8/17共聚物,PEG/PPG-8/55共聚物,PPG-10丁二醇,PPG-10辛酰基醚,PPG-10月桂基醚,PPG-2甲醚,PPG-2乙酸甲醚,PPG-2丙基醚,PPG-2丙基醚,PPG-3辛醚,PPG-3甲醚,PPG-4甲醚,PPG-5辛醚,PPG-55甘油基醚,PPG-6辛醚,SORBETH-20,SORBETH-30,SORBETH-40,SORBETH-6,STEARETH-12。
该非水性溶剂可包含至少一种选自D-葡萄糖酸-1,5-内酯和/或丁内酯的内酯。
该非水性溶剂可包含至少一种选自以下组的有机硅或硅氧烷:聚合物环状甲基乙氧基硅氧烷,十四甲基环七硅氧烷,十二甲基环六硅氧烷,环聚二甲基硅氧烷,十甲基环五硅氧烷,八甲基环四硅氧烷,六甲基环三硅氧烷,丙基聚三甲基硅氧烷。
该非水性溶剂可包含至少一种有机硫化合物,例如二甲基砜,和/或至少一种有机磷化合物,例如磷酸三乙酯。
该非水性溶剂可包含至少一种选自以下组的矿物油和/或植物油和/或蜡:大西洋鲱油(拉丁文为brevoortia tyrannus)的氢化油,橄榄树(拉丁文为olea europaea)的果实或豆荚的油,东方罂粟(拉丁文为papaver orientale)籽油,普通蓖麻(拉丁文为ricinuscommunis)籽油,鲨鱼肝油,妥尔油,大风子油,玉米油,羊毛脂油,荷荷芭油。
该非水性溶剂可包含至少一种选自以下组的萜烯和/或精油:柠檬烯,萜烯和类萜,octea quixos的叶油,松油醇。
特别地,该非水性溶剂可包含:
-乙醇,尤其是比率为该组合物的总重量的15%-80%,更特别地为31.25%-43.75%;和/或
-肉豆蔻酸异丙酯(MIP),尤其是比率为该组合物的总重量的10%-80%,更特别地为31.25%-43.75%。
该非水性溶剂还可包含:
-琥珀酸异辛酯,尤其是比率为该组合物的总重量的50%-90%,更特别地为64.80%-79.80%;和或
-椰子烷烃(coconut alkanes)、辛酸和癸酸的椰油酯(coco caprylate et decaprate)的混合物,尤其是比率为该组合物的总重量的10%-30%,更特别地为16.20%。
该组合物还可包含额外的驱虫成分,其能够与驱虫脂肪酸协同作用,以进一步改善其随时间的效力,并且可能将其驱虫性能扩展到更多种类的有害昆虫。
特别地,该组合物可包含按重量计0.1%-20%、尤其是3%-4%的额外的驱虫成分。
该额外的驱虫成分可选自对薄荷烷-3,8-二醇(PMD)和包含它的所有活性剂,N,N-二乙基-3-甲基苯甲酰胺(DEET),埃卡瑞丁,丁基乙酰氨基丙酸乙酯(IR3535),N,N-二乙基苯基乙酰胺(DEPA),萜烯,类萜,植物油,醋,柠檬苦素,类苯基丙烷,精油,拟除虫菊酯,天然除虫菊酯,内酯,胡椒基衍生物,胡椒碱,苯甲醇,马拉硫磷,林丹,或者这些成分中至少两种的混合物。
特别地,对薄荷烷-3,8-二醇(PMD)是衍生自植物的成分,其对于驱除刺或咬类嗜血昆虫如蚊子是特别有效的。
该额外的驱虫成分可尤其包含至少一种精油,尤其选自爪哇香茅、天竺葵、玫瑰草、醒目薰衣草(lavandin)、薰衣草、薄荷、丁香、茴香和肉桂的精油。
该额外的驱虫成分还可包含至少一种选自以下组的成分:
-萜烯或类萜,例如为香茅醛、香叶醇、芳樟醇、薄荷醇、橙花叔醇、萜品-4-醇、葛杜宁、苦木素或诺卡酮类型的;
-植物油,例如印度楝树油或酸渣树油;
-醋,例如苦木醋;
-柠檬苦素:例如印楝素或Andirobine;
-类苯基丙烷,例如丁子香酚或肉桂醛;
-内酯,例如荆芥内酯(nepetolactone),δ-癸内酯或δ-十一内酯类型的;
-胡椒基衍生物,例如乙酸胡椒酯、胡椒基丙酮、胡椒基醛、胡椒基醇(芝麻酚)、莳萝油脑或荜茇酰胺类型的;
-胡椒碱,例如简单胡椒碱、四氢胡椒碱、比坦维林、布托哌林和/或其盐或者哌嗪类型的;
-其他类型的成分,例如十一烷酮,6-甲基-5-庚-2-酮,聚二甲基硅氧烷或1,2-辛二醇。
该组合物还可包含稳定化成分,该稳定化成分包括不饱和脂肪酸,特别是基于油酸的不饱和脂肪酸。
实施例
在实验室进行的测试方案中,制备了多个驱虫组合物样品,以测试其随时间的效力。
为此,在对样品进行评价之前,将大约50只的多个种类的蚊子(尤其是虎斑蚊(拉丁文为Aedes albopictus)的成年雌性样本封装在尺寸为50x50x30(cm)的有机玻璃笼中,然后通过将未涂驱虫组合物的所谓“对照”前臂放入笼中三十秒来测试所述样本的攻击性。在这个测试结束时,观察到至少十次尝试在前臂上降落和/或刺咬。
然后,根据相同的实验方案依次测试样品,其步骤在下面说明。特别地,所使用的方案符合题为《Guidelines for efficacy testing of mosquito repellents for humanskin-WHO/HTM/NTD/WHOPES/2009.4》的WHO文件《Topical Guidelines(WHOPES 2009)》。
首先,将一定剂量的待测试样品施用到所谓“测试”前臂上,尤其以约1g/600cm2的密度。
然后,将“测试”前臂放入装有蚊子的笼子中,进行九个在1小时间隔之后重复的每个3分钟的测试周期P0、P1、P2、P3、P4、P5、P6、P7、P8(初始周期P0对应于施用本身的时刻,并且最终周期P8对应于所述施用之后的第8个小时),这不进行样品的重新施加。在每个测试周期P0-P8期间,通过计算“测试”前臂和“对照”前臂之间降落和/或刺咬次数的抑制百分比PI来评价样品的效力。
实施例1
在第一系列测试中,制备了四个驱虫组合物样品,其中:
-两个“对照”样品WW1、WW3(水性溶剂),各自包含87.25%重量的水和0.25%重量的基于十二烷基硫酸钠(SLS)的表面活性剂,以及:
ο对于样品WW1:12.5%重量的月桂酸;
ο对于样品WW3:37.5%重量的月桂酸;
-两个“测试”样品WL1、WL3(非水性溶剂),包含:
ο对于样品WL1:43.75%重量的乙醇,43.75%重量的肉豆蔻酸异丙酯(MIL)和12.5%重量的月桂酸;
ο对于样品WL3:31.25%重量的乙醇,31.25%重量的肉豆蔻酸异丙酯(MIL)和37.5%重量的月桂酸。
特别地,“测试”样品包含约0%重量的水,从而使得它们各自形成无水组合物。
根据上述实验方案测试了这四个样品WW1、WW3、WL1、WL3中的每一个,并且在图1a(对于样品WW1、WL1)和图1b(对于样品WW3和WL3)的图上列出了在每个周期P0-P8获得的PI百分比。
对于“对照”样品WW1、WW3,在初始时期P0期间,起始效力相对较低,其中对于样品WW1来说PI百分比为61.45%,并且对于样品WW3来说PI百分比为21.70%。另外,这种效力随着时间的推移迅速降低,因为对于样品WW1来说从第三周期P2开始PI百分比已降至0%,并且对于包含更高月桂酸浓度的WW3样品来说甚至从第二周期开始P1百分比已降至0%。
相反,对于“测试”样品WL1、WL3,在九个周期P0-P8期间均保持非常高的效力,其中对于具有12.5%月桂酸的样品WL1来说,PI百分比大于90%,甚至大于95%。特别地,在最后测试周期P8结束时,样品WL1、WL3具有分别为96.87%和93.56%的PI百分比。
因此,此第一系列测试中获得的结果使得能够凸显出,相比于使用月桂酸与水性溶剂的组合物来说,将月桂酸与非水性溶剂(并且尤其无水)组合的驱虫组合物的随时间的效力显著提高。
实施例2
在第二系列测试中,制备了七个驱虫组合物样品,每个样品均不含水,并且包含:
-包含月桂酸的驱虫成分和/或另外类型的驱虫成分;
-非水性溶剂,其包含:
ο乙醇(占组合物总重量的41.75%-48%);和
ο肉豆蔻酸异丙酯(MIL)(占组合物总重量的41.75%-48%)。
在这些样品中,提供了四个“对照”样品WL1、W4、W11、W8,每个样品都包含单一类型的驱虫成分。因而:
-样品WL1,与第一系统测试期间制备的样品类似,包含月桂酸(12.5%重量);
-样品W4,包含对薄荷烷-3,8-二醇(PMD)(3%重量);
-样品W11,包含N,N-二乙基-3-甲基苯甲酰胺(DEET)(3%重量);
-样品W8,包含醒目薰衣草精油(4%重量)。
另外,提供了三个“测试”样品WL4、WL11、WL8,每个样品包含与样品WL1相同比例的月桂酸(12.5%重量),分别与样品W4、W11、W8中存在的三种其他类型的驱虫成分之一混合,采用与相应样品W4、W11、W8中相同的比例。因而:
-样品WL4包含3%重量的PMD;
-样品WL11包含3%重量的DEET;
-样品WL8包含4%重量的醒目薰衣草精油。
根据上述实验方案测试这七个样品中的每一个,并且它们的完全保护时间(CPT,对应英文的“complete protection time”)(对应于上述PI百分比大于或等于99%的小时数)已列在图2的图中。
对于“对照”样品WL1、W4、W11、W8,完全保护时间被证明很短(对于仅有“PMD”的样品W4来说为大约3小时,对于仅有“DEET”的样品W11来说为4小时),甚至为零(对于“仅有月桂酸”的样品WL1来说,在初始周期P0的PI百分比仅为97.9%)。
相反,对于“测试”样品WL4、WL11、WL8,完全保护时间被证明更长。实际上,对于将月桂酸分别与PMD和醒目薰衣草精油混合的样品WL4、WL8来说,这个时间甚至达到了8小时,这与仅包含这些驱虫成分中的一种的相应“对照”样品WL1、WL4、WL8相比代表了效力的非常显著的提高。
实施例3
在第三系列测试中,制备了四个驱虫组合物样品,每个样品均不含水,并且包含:
-包含月桂酸的驱虫成分和/或另外类型的驱虫成分;
-非水性溶剂,其包含:
ο琥珀酸异辛酯(占组合物总重量的64.80%-79.80%);和
ο椰子烷烃、辛酸和癸酸的椰油酯的混合物(占组合物总重量的16.20%)。
在这些样品中,提供两个“对照”样品ASPF07、W12,每个样品均包含单一类型的驱虫成分。因而:
-样品ASPF07包含丁基乙酰氨基丙酸乙酯(IR3535)(4%重量);
-样品W12包含埃卡瑞丁(4%重量)。
此外,提供两个“测试”样品ASPF08、WL12,每个样品均包含与样品WL1相同比例的月桂酸(12.5%重量),分别与样品ASPF07、W12中存在的两种其他类型的驱虫成分之一混合,采用与相应样品ASPF07、W12中相同的比例。因而:
-样品ASPF08包含4%重量的IR3535;
-样品WL12包含4%重量的埃卡瑞丁。
根据上述实验方案测试这四个样品中的每一个,并且它们的完全保护时间(CPT,对应英文的“complete protection time”)(对应于上述PI百分比大于或等于99%的小时数)已列在图3的图中,图3还包括了在第二系列测试时获得并且在图2中示出的结果。
对于这四个样品,获得的结果与在第二系列测试中观察到的结果类似,即:
-对于“对照”样品ASPF07、W12来说完全保护时间很短,该完全保护时间被证明是短的(对于仅有“IR3535”的样品ASPF07来说为大约3小时,对于仅有“埃卡瑞丁”的样品WL11来说为4小时);
-对于“测试”样品ASPF08、WL12来说完全保护时间更长,即对于将月桂酸与IR3535混合的样品ASPF08来说为5小时,对于将月桂酸与埃卡瑞丁混合的样品WL12来说甚至为7小时。
因而,此第二和第三系列测试中获得的结果使得能够凸显出在包含非水性溶剂的组合物(特别是无水)中根据本发明的脂肪酸与额外成分的驱虫性能之间的协同作用,与仅包含脂肪酸或另一种类型的驱虫成分的组合物相比,所述效果导致驱虫组合物的随时间的效力显著提高。
Claims (16)
1.驱虫组合物,其包含:
-包含一种或多种具有9-21个碳原子的脂肪酸的驱虫成分;
-非水性溶剂;
-小于1%重量的水。
2.根据权利要求1的驱虫组合物,其特征在于,该驱虫脂肪酸具有12个碳原子。
3.根据权利要求1或2之一的驱虫组合物,其特征在于,该驱虫脂肪酸包含羧酸,特别是月桂酸。
4.根据权利要求1-3中任一项的驱虫组合物,其特征在于,该驱虫脂肪酸包含饱和或不饱和脂肪酸。
5.根据权利要求1-4中任一项的驱虫组合物,其特征在于,该驱虫组合物不含水。
6.根据权利要求1-5中任一项的驱虫组合物,其特征在于,该驱虫脂肪酸衍生自至少一种水解植物油,所述植物油特别选自椰子油、棕榈油、摩洛哥坚果油、杏仁油、蓖麻油、鳄梨油、小麦胚芽油或者这些油中至少两种的混合物。
7.根据权利要求1-6中任一项的驱虫组合物,其特征在于,该组合物包含按重量计5%-50%、特别是12.5%-37.5%的驱虫脂肪酸。
8.根据权利要求1-7中任一项的驱虫组合物,其特征在于,该非水性溶剂包含至少一种选自以下组的成分:醇,酸,烷烃,烯烃,醛,胺,酰胺,酮,酯,醚,内酯,有机硅,硅氧烷,有机硫化合物,有机磷化合物,矿物油,植物油,蜡,萜烯,精油或者这些成分中至少两种的混合物。
9.根据权利要求8的驱虫组合物,其特征在于,该非水性溶剂包含乙醇,尤其是比率为所述组合物的总重量的15%-80%,更特别地为31.25%-43.75%。
10.根据权利要求8或9之一的驱虫组合物,其特征在于,该非水性溶剂包含肉豆蔻酸异丙酯,尤其是比率为所述组合物的总重量的10%-80%,更特别地为31.25%-43.75%。
11.根据权利要求8-10中任一项的驱虫组合物,其特征在于,该非水性溶剂包含琥珀酸异辛酯,尤其是比率为该组合物的总重量的50%-90%,更特别地为64.80%-79.80%。
12.根据权利要求8-11中任一项的驱虫组合物,其特征在于,该非水性溶剂包含椰子烷烃(coconut alkanes)、辛酸和癸酸的椰油酯的混合物,尤其是比率为该组合物的总重量的10%-30%,更特别地为16.20%。
13.根据权利要求1-12中任一项的驱虫组合物,其特征在于,该驱虫组合物包含能够与该驱虫脂肪酸协同作用的额外的驱虫成分。
14.根据权利要求13的驱虫组合物,其特征在于,该驱虫组合物包含按重量计0.1%-20%、尤其是3%-4%的额外的驱虫成分。
15.根据权利要求13或14之一的驱虫组合物,其特征在于,该额外的驱虫成分选自对薄荷烷-3,8-二醇,N,N-二乙基-3-甲基苯甲酰胺,埃卡瑞丁,丁基乙酰氨基丙酸乙酯,N,N-二乙基苯基乙酰胺,萜烯,类萜,植物油,醋,柠檬苦素,类苯基丙烷,精油,尤其是醒目薰衣草精油,拟除虫菊酯,天然除虫菊酯,内酯,胡椒基衍生物,胡椒碱,苯甲醇,马拉硫磷,林丹,或者这些成分中至少两种的混合物。
16.根据权利要求1-15中任一项的驱虫组合物,其特征在于,该驱虫组合物包含稳定化成分,该稳定化成分包括不饱和脂肪酸,特别是基于油酸的不饱和脂肪酸。
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2019
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Also Published As
Publication number | Publication date |
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BR112020020425A2 (pt) | 2021-01-12 |
CA3095975A1 (fr) | 2019-10-10 |
IL277788B1 (en) | 2023-05-01 |
WO2019193561A2 (fr) | 2019-10-10 |
EP3772952A2 (fr) | 2021-02-17 |
CN115812710A (zh) | 2023-03-21 |
EP3772952A4 (fr) | 2022-03-02 |
CN112118739B (zh) | 2023-01-10 |
AU2019249372A1 (en) | 2020-10-15 |
KR20200142024A (ko) | 2020-12-21 |
IL277788B2 (en) | 2023-09-01 |
FR3079716A1 (fr) | 2019-10-11 |
IL277788A (zh) | 2020-12-31 |
WO2019193561A3 (fr) | 2019-11-28 |
MX2020010394A (es) | 2020-10-22 |
JP2021520359A (ja) | 2021-08-19 |
US20210144995A1 (en) | 2021-05-20 |
RU2020132017A (ru) | 2022-05-05 |
FR3079716B1 (fr) | 2020-04-24 |
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