CN101442908B - 配制的壁虱和昆虫驱除组合物 - Google Patents
配制的壁虱和昆虫驱除组合物 Download PDFInfo
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- CN101442908B CN101442908B CN200780016796.8A CN200780016796A CN101442908B CN 101442908 B CN101442908 B CN 101442908B CN 200780016796 A CN200780016796 A CN 200780016796A CN 101442908 B CN101442908 B CN 101442908B
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- IFIDXBCRSWOUSB-UHFFFAOYSA-N potassium;1,3-dichloro-1,3,5-triazinane-2,4,6-trione Chemical compound [K+].ClN1C(=O)NC(=O)N(Cl)C1=O IFIDXBCRSWOUSB-UHFFFAOYSA-N 0.000 description 1
- MQOCIYICOGDBSG-UHFFFAOYSA-M potassium;hexadecanoate Chemical compound [K+].CCCCCCCCCCCCCCCC([O-])=O MQOCIYICOGDBSG-UHFFFAOYSA-M 0.000 description 1
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- MCJGNVYPOGVAJF-UHFFFAOYSA-N quinolin-8-ol Chemical compound C1=CN=C2C(O)=CC=CC2=C1 MCJGNVYPOGVAJF-UHFFFAOYSA-N 0.000 description 1
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- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicon dioxide Inorganic materials O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 229920002545 silicone oil Polymers 0.000 description 1
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- FJOLTQXXWSRAIX-UHFFFAOYSA-K silver phosphate Chemical compound [Ag+].[Ag+].[Ag+].[O-]P([O-])([O-])=O FJOLTQXXWSRAIX-UHFFFAOYSA-K 0.000 description 1
- 229940019931 silver phosphate Drugs 0.000 description 1
- 229910000161 silver phosphate Inorganic materials 0.000 description 1
- 230000037075 skin appearance Effects 0.000 description 1
- 230000036556 skin irritation Effects 0.000 description 1
- 231100000475 skin irritation Toxicity 0.000 description 1
- 238000002791 soaking Methods 0.000 description 1
- 239000000429 sodium aluminium silicate Substances 0.000 description 1
- 235000012217 sodium aluminium silicate Nutrition 0.000 description 1
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 description 1
- 235000010378 sodium ascorbate Nutrition 0.000 description 1
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- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
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- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 description 1
- MSXHSNHNTORCAW-GGLLEASOSA-M sodium;(2s,3s,4s,5r,6s)-3,4,5,6-tetrahydroxyoxane-2-carboxylate Chemical compound [Na+].O[C@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O MSXHSNHNTORCAW-GGLLEASOSA-M 0.000 description 1
- VRVKOZSIJXBAJG-ODZAUARKSA-M sodium;(z)-but-2-enedioate;hydron Chemical compound [Na+].OC(=O)\C=C/C([O-])=O VRVKOZSIJXBAJG-ODZAUARKSA-M 0.000 description 1
- CITBNDNUEPMTFC-UHFFFAOYSA-M sodium;2-(hydroxymethylamino)acetate Chemical compound [Na+].OCNCC([O-])=O CITBNDNUEPMTFC-UHFFFAOYSA-M 0.000 description 1
- GGXKEBACDBNFAF-UHFFFAOYSA-M sodium;hexadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCC([O-])=O GGXKEBACDBNFAF-UHFFFAOYSA-M 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
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- 238000005507 spraying Methods 0.000 description 1
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- 238000003892 spreading Methods 0.000 description 1
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- 229940071209 stearoyl lactylate Drugs 0.000 description 1
- 239000004575 stone Substances 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 238000005728 strengthening Methods 0.000 description 1
- 229910000018 strontium carbonate Inorganic materials 0.000 description 1
- 229940086735 succinate Drugs 0.000 description 1
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- 150000003456 sulfonamides Chemical class 0.000 description 1
- 229960000368 sulisobenzone Drugs 0.000 description 1
- 235000007586 terpenes Nutrition 0.000 description 1
- 150000005622 tetraalkylammonium hydroxides Chemical class 0.000 description 1
- HBPNTDBLHQHPLH-UHFFFAOYSA-N tetradecyl 16-methylheptadecanoate Chemical compound CCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC(C)C HBPNTDBLHQHPLH-UHFFFAOYSA-N 0.000 description 1
- 235000019818 tetrasodium diphosphate Nutrition 0.000 description 1
- 239000004577 thatch Substances 0.000 description 1
- 239000004308 thiabendazole Substances 0.000 description 1
- 235000010296 thiabendazole Nutrition 0.000 description 1
- WJCNZQLZVWNLKY-UHFFFAOYSA-N thiabendazole Chemical compound S1C=NC(C=2NC3=CC=CC=C3N=2)=C1 WJCNZQLZVWNLKY-UHFFFAOYSA-N 0.000 description 1
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- 230000008719 thickening Effects 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- YODZTKMDCQEPHD-UHFFFAOYSA-N thiodiglycol Chemical compound OCCSCCO YODZTKMDCQEPHD-UHFFFAOYSA-N 0.000 description 1
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- NBOMNTLFRHMDEZ-UHFFFAOYSA-N thiosalicylic acid Chemical compound OC(=O)C1=CC=CC=C1S NBOMNTLFRHMDEZ-UHFFFAOYSA-N 0.000 description 1
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- 230000000699 topical effect Effects 0.000 description 1
- CRDAMVZIKSXKFV-UHFFFAOYSA-N trans-Farnesol Natural products CC(C)=CCCC(C)=CCCC(C)=CCO CRDAMVZIKSXKFV-UHFFFAOYSA-N 0.000 description 1
- LOIYMIARKYCTBW-OWOJBTEDSA-N trans-urocanic acid Chemical compound OC(=O)\C=C\C1=CNC=N1 LOIYMIARKYCTBW-OWOJBTEDSA-N 0.000 description 1
- LOIYMIARKYCTBW-UHFFFAOYSA-N trans-urocanic acid Natural products OC(=O)C=CC1=CNC=N1 LOIYMIARKYCTBW-UHFFFAOYSA-N 0.000 description 1
- UWHZIFQPPBDJPM-BQYQJAHWSA-N trans-vaccenic acid Chemical compound CCCCCC\C=C\CCCCCCCCCC(O)=O UWHZIFQPPBDJPM-BQYQJAHWSA-N 0.000 description 1
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- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- SZHOJFHSIKHZHA-UHFFFAOYSA-N tridecanoic acid Chemical compound CCCCCCCCCCCCC(O)=O SZHOJFHSIKHZHA-UHFFFAOYSA-N 0.000 description 1
- 229940087291 tridecyl alcohol Drugs 0.000 description 1
- 125000002889 tridecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229940029614 triethanolamine stearate Drugs 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 description 1
- HTJNEBVCZXHBNJ-XCTPRCOBSA-H trimagnesium;(2r)-2-[(1s)-1,2-dihydroxyethyl]-3,4-dihydroxy-2h-furan-5-one;diphosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.OC[C@H](O)[C@H]1OC(=O)C(O)=C1O HTJNEBVCZXHBNJ-XCTPRCOBSA-H 0.000 description 1
- LINXHFKHZLOLEI-UHFFFAOYSA-N trimethyl-[phenyl-bis(trimethylsilyloxy)silyl]oxysilane Chemical compound C[Si](C)(C)O[Si](O[Si](C)(C)C)(O[Si](C)(C)C)C1=CC=CC=C1 LINXHFKHZLOLEI-UHFFFAOYSA-N 0.000 description 1
- 229940048102 triphosphoric acid Drugs 0.000 description 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- SOBHUZYZLFQYFK-UHFFFAOYSA-K trisodium;hydroxy-[[phosphonatomethyl(phosphonomethyl)amino]methyl]phosphinate Chemical compound [Na+].[Na+].[Na+].OP(O)(=O)CN(CP(O)([O-])=O)CP([O-])([O-])=O SOBHUZYZLFQYFK-UHFFFAOYSA-K 0.000 description 1
- 239000010681 turmeric oil Substances 0.000 description 1
- QFKMMXYLAPZKIB-UHFFFAOYSA-N undecan-1-amine Chemical compound CCCCCCCCCCCN QFKMMXYLAPZKIB-UHFFFAOYSA-N 0.000 description 1
- MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
- FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
- 235000012141 vanillin Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- ZFNVDHOSLNRHNN-UHFFFAOYSA-N xi-3-(4-Isopropylphenyl)-2-methylpropanal Chemical compound O=CC(C)CC1=CC=C(C(C)C)C=C1 ZFNVDHOSLNRHNN-UHFFFAOYSA-N 0.000 description 1
- PHXATPHONSXBIL-UHFFFAOYSA-N xi-gamma-Undecalactone Chemical compound CCCCCCCC1CCC(=O)O1 PHXATPHONSXBIL-UHFFFAOYSA-N 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 239000004246 zinc acetate Substances 0.000 description 1
- 239000001841 zingiber officinale Substances 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
- A01N43/04—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
- A01N43/14—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom six-membered rings
- A01N43/16—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom six-membered rings with oxygen as the ring hetero atom
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
- A01N43/42—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
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Abstract
本发明涉及含有二氢荆芥内酯,荆芥内酰胺,二氢荆芥内酰胺和/或它们的各自衍生物,以及一种或多种添加剂的壁虱或昆虫驱除用配制组合物的领域,该添加剂提供了按照使用者希望的方式输送组合物并输送到使用者希望的部位的一种有用和有效手段。
Description
本申请要求了2006年5月10日提交的美国临时申请No.60/799,277的权益,对于全部目的来说后者以全部内容被引入作为本申请的一部分。
技术领域
本发明涉及含有一种或多种植物派生的壁虱和/或昆虫驱除活性成分的配制组合物。
发明背景
美国04/127,553,对于所有目的以全部内容被引入这里作为本发明的一部分,公开了由荆芥内酯的氢化所衍生的二氢荆芥内酯(DHN)非对映异构体,和它的组合物,它们作为抵抗壁虱和/或对人特别感兴趣的几种昆虫类(其中包括蚊科和厩蝇)的有效驱虫剂。
美国申请序列号11/314,672,它对于所有目的以全部内容被引入这里作为本发明的一部分,公开了荆芥内酰胺非对映异构体,和它的组合物,作为有用的壁虱和/或昆虫驱除剂;和美国申请序列号11/314,385,它对于所有目的以全部内容被引入这里作为本发明的一部分,公开二氢荆芥内酰胺非对映异构体,和它的组合物,作为有用的壁虱和/或昆虫驱除剂。
然而仍然需求所有这些材料的配制组合物,它允许消费者容易地将它们用于壁虱和/或昆虫驱除目的。
概述
本发明的一个实施方案是物质组合物,或引入该组合物的制品,它们含有选自二氢荆芥内酯,二氢荆芥内酯的衍生物,荆芥内酰胺,N-取代的荆芥内酰胺,二氢荆芥内酰胺,N-取代的二氢荆芥内酰胺中的两种或多种组分。
本发明的附加实施方案是配制的壁虱和/或昆虫驱除剂组合物,或引入了该组合物的制品,它们含有作为驱虫活性成分的选自二氢荆芥内酯,二氢荆芥内酯的衍生物,荆芥内酰胺,N-取代的荆芥内酰胺,二氢荆芥内酰胺,N-取代的二氢荆芥内酰胺,和它们的混合物中的组分。当从它的此类驱虫活性成分制造时,组合物和/或制品也可具有令人所需的芳香特性。
尤其,本发明进一步提供皮肤用局部处理剂,如香料或芳香剂,或壁虱和/或昆虫的驱除剂,它们包括如上所述的驱虫活性成分。
本发明的另一个实施方案是用于制造壁虱和/或昆虫驱除组合物或壁虱和/或昆虫驱除制品的方法,这通过提供作为组合物或制品形式的如上所述驱虫活性成分或通过在组合物或制品中引入如上所述的驱虫活性成分来实现。
本发明的又一个实施方案是如上所述的驱虫活性成分或它的组合物用作壁虱和/或昆虫驱除剂,因此还包括一种实施方案,其中在驱除壁虱和/或昆虫的方法中,该壁虱和/或昆虫暴露于如上所述的驱虫活性成分或它的组合物。尤其,本发明提供了通过在壁虱和/或昆虫的宿主的表面上,如宿主的皮肤、兽皮、头发、毛皮或羽毛上,施用如上所述的驱虫活性成分来驱除壁虱和/或昆虫的方法。
在本发明的附加实施方案中,驱虫活性成分是天然的,植物来源的物质。在又一个实施方案中,该驱虫活性成分可以与典型用于化妆品工业中的一种或多种助剂或改性剂掺混。
详细说明
在一个实施方案中,本发明提供组合物,它含有选自二氢荆芥内酯或它的衍生物,荆芥内酰胺,N-取代的荆芥内酰胺,二氢荆芥内酰胺和N-取代的二氢荆芥内酰胺中的一种或多种组分。在优选的实施方案中,二氢荆芥内酯,荆芥内酰胺,二氢荆芥内酰胺,或各自衍生物,或它们的混合物,在组合物中用作壁虱和/或昆虫驱除活性成分。
该术语“二氢荆芥内酯”和“DHN”应该被理解为包括二氢荆芥内酯的任何立体异构体,或该立体异构体的任何结合物,以及它们的可以进一步包括DHN衍生物(如下所述的那些)的结合物。DHN的立体异构体示于图1中。特别理想的是:
(1S,9S,5R,6R)-5,9-二甲基-3-氧杂双环[4.3.0]壬烷-2-酮,
(1S,5S,9S,6S)-5,9-二甲基-3-氧杂双环[4.3.0]壬烷-2-酮,
(1S,9S,6S,5R)-5,9-二甲基-3-氧杂双环[4.3.0]壬烷-2-酮,
(9S,5S,1R,6R)-5,9-二甲基-3-氧杂双环[4.3.0]壬烷-2-酮,和
(9S,1R,5R,6R)-5,9-二甲基-3-氧杂双环[4.3.0]壬烷-2-酮。
适合于本发明的实施中的DHN或它的衍生物是由通式(I)表示的:
其中R1,是氢,C1~C20烷基或C6~C20芳基,和
R2是氢或C1~C20烷基。R1和/或R2的代表性值除氢之外还可以包括直链或支化的C1~C20烷基如仲丁基或新戊基,和优选是直链C1~C12烷基如甲基,乙基,丙基,丁基,戊基或己基;或R1和/或R2可以是取代或未取代的C6~C20苯基,和优选是未被取代的或间-或对-取代的苯基,其中在苯基上的取代基可以是直链C1~C12烷基或烷氧基,或卤素。在衍生物中,R1和/或R2最优选是甲基或乙基,苯基,或对-或间-甲苯基。
通式(I),它没有标明立体化学,在这里应该包括DHN的任何立体异构体,和DHN的衍生物的任何立体异构体,DHN立体异构体的任何结合物,DHN衍生物的立体异构体的任何结合物,以及DHN的一种或多种异构体与DHN的衍生物的一种或多种异构体的任何结合物。
DHN可以通过直接合成法制备,从各种天然来源物中分离出来,或通过荆芥内酯的催化氢化制备。荆芥属(假荆芥)植物的香精油或从该植物提取的荆芥内酯的氢化是DHN制备的优选方法。荆芥内酯大量存在于荆芥属植物叶片的香精油中,并且容易从中提纯获得。这会生产出可获取DHN的一种高度令人想望的天然产物。
荆芥内酯至DHN的催化氢化可以根据在Regnier,F.E.等人,Phytochemistry,6:1281~1289(1967)中的方法来进行,其中催化剂如担载在碳酸锶上的氧化铂和钯将以24-90%收率得到二氢荆芥内酯。优选地,DHN是根据在共同未决的美国专利申请序列号10/405,444中的方法,由催化氢化制得,该专利对于所有目的以其全部内容被引入这里作为本申请的一部分。这一方法包括下列成分的使用:催化金属如钌,铼,铑,铱,它们的化合物,和它们的结合物,以及,当使用时,载体如碳,氧化铝,硅石,硅石-氧化铝,二氧化钛,二氧化钛-氧化铝,二氧化钛-硅石,钡,钙,它们的化合物,和它们的结合物。
DHN也可通过荆芥内酯与碱水溶液接触来制备。合适的碱包括碱金属,碱土金属,和氢氧化铵。钠,钾,锂,钙,镁,铵,和氢氧化四烷基铵是优选的。在形成碱性混合物的步骤之后是用酸进行酸化形成荆芥酸的步骤。如上所述的提取的水溶液在这一步骤中进行逐渐酸化,至低于约4的pH,优选至约3或更低的pH。酸化优选通过使用强的无机酸,如盐酸,硝酸或硫酸来进行。
如上所述制得的荆芥酸进行去质子化,和进行从它的产物至DHN的还原反应。为此目的,在一个实施方案中,荆芥酸可以在0℃至约25℃范围内的温度下与无水的碱如氢化物接触进行去质子化。也用于去质子化的是胺类,特别地三乙胺。在去质子化步骤之后,所得的盐与还原剂接触而形成DHN产物。合适的还原剂包括硼氢化物和二烷基硼烷类。在优选的实施方案中,单独的去质子化步骤可通过使用过量的还原剂(如NaBH4)而省去-也就是说,使用大于1当量,优选使用稍微大于两个当量的还原剂,在单个步骤中同时进行去质子化和还原。DHN的附加描述,它的用途和制备它的方法已公开在共同未决的美国申请序列号11/017,254中,它对于所有目的以其全部内容被引入这里作为本申请的一部分。
从天然来源制得的HN必然代表立体异构体的混合物,这些立体异构体可以被分离成其组分或不被分离成其组分,这取决于具体应用的要求。已经观察到,在组成上的变化将在不同种类的荆芥属之间各不相同;在某些种类中,在相同种类的植物之间也会在组成上有所不同。后面的种类是起始原料的不太优选的来源。
分馏已经发现在本发明的实施中同时是从香精油中提纯荆芥内酯以及分离从香精油制得的非对映DHN对的有效方法。色谱分离也是合适的。
根据任何方法制得的DHN,它可以是单种立体异构体、非对映的配对或异构体的混合物的形式,可以通过在通式(I)中所示的4位上的取代被转化成它的衍生物。在通式(I)中的C-4位上的取代可通过格利雅试剂亲核加成到亲电子的荆芥酸(荆芥内酯的水合形式)来形成。荆芥酸在去质子化步骤中用无水的碱处理,形成羧酸盐。在一个实施方案中,例如,荆芥酸用碱金属氢化物(优选KH)处理。在这一实施方案中,在去质子化步骤之后是用格利雅试剂处理形成DHN衍生物。在附加的实施方案中,荆芥酸用大于1当量的格利雅试剂,和优选至少两个当量的格利雅试剂处理,形成衍生物。这一方法省去了首先用单独的无水的碱如碱金属氢化物处理荆芥酸的步骤。格利雅试剂以稍微超过两个当量的量使用可以确保高转化率转化成所需产物。
典型的格利雅试剂包括,但不限于,由金属镁与有机氯化物、溴化物或碘化物的结合制得,通常在醚的存在下和在水完全不存在的情况下。适合用于该方法中的是可与醛反应的任何格利雅试剂,其中包括但不限于烷基化氯镁,烷基溴化镁,芳基氯化镁,和芳基溴化镁。也包括的是二烷基锌,二芳基锌和烷基锂和芳基锂。可以在合适的格利雅试剂上存在的代表性取代基包括甲基,乙基,正丙基,丁基,戊基,己基苯基,对-和间-取代的苯基(包括对-和间-甲苯基,和对-甲氧基-苯基)。DHN的衍生物的附加描述,它们的用途和制备它们的方法已公开在共同未决的美国申请序列号10/997,279中,它对于所有目的以其全部内容被引入这里作为本申请的一部分。
DHN可以通过在通式(I)的C-1位上的取代来另外或进一步衍生化,这可通过内酯的烯醇化物(亲核试剂)用烷基化试剂如碘代甲烷(亲电子试剂)的烷基化,在桥头引入非氢取代基来实现。一般,碱如二异丙胺锂(lithium diisopropylamine)或LDA用于烯醇化物产生,但是许多碱是合适的,这取决于反应的具体要求。烷基化剂如烷基卤是优选的,但是许多烷基化剂都是合适的,这取决于具体反应的要求。
在这里适合用作驱虫活性成分的荆芥内酰胺,和它的衍生物如N-取代的荆芥内酰胺可以由通式(III)用示意图方式表示:
其中R是链烷烃,链烯烃,炔烃或芳族烃。
在各种实施方案中,在通式(III)中的R可以选自:1)H或C2H5,2)C3-C20直链,支化或环状链烷烃或链烯烃,3)包括选自O、N和S中的杂原子的C3-C20直链,支化或环状链烷烃或链烯烃,4)未被取代的或被取代的C6-C20芳族烃,其中该取代基选自C1-C12直链,支化或环状链烷烃或链烯烃,和5)包括选自O、N和S中的杂原子的未被取代的或被取代的C6-C20芳族烃,其中该取代基选自C1-C12直链,支化或环状链烷烃或链烯烃。通式(III)的取代或未被取代的荆芥内酰胺化合物可以是单种化合物的单种立体异构体,可以是单种化合物的立体异构体的混合物,或可以是其中R不相同的那些化合物的立体异构体的混合物。
如上所述的荆芥内酰胺可通过荆芥内酯与无水氨接触来制备,根据由Eisenbraun等人在J.Org.Chem.,53:3968-3972(1988)中描述的方法。N-取代的荆芥内酰胺然后通过荆芥内酰胺与合适的金属氢化物反应形成荆芥内酰胺盐,随后让荆芥内酰胺盐与合适的烷基化剂接触形成N-取代的荆芥内酰胺而最终形成。荆芥内酰胺和N-取代的荆芥内酰胺的进一步叙述,它们的用途和制备它们的方法已公开在共同未决的美国临时申请序列号60/639,945中,该专利申请对于所有目的被引入这里作为本申请的一部分。
在这里适合用作驱虫活性成分的二氢荆芥内酰胺,和它的衍生物如N-取代的二氢荆芥内酰胺可以由通式(IV)用示意图方式表示:
其中R是链烷烃,链烯烃,炔烃或芳族烃。
在各种实施方案中,在通式(IV)的化合物中的R可以选自:1)H或C2H5,2)C3-C20直链,支化或环状链烷烃或链烯烃,3)包括选自O、N和S中的杂原子的C3-C20直链,支化或环状链烷烃或链烯烃,4)未被取代的或被取代的C6-C20芳族烃,其中该取代基选自C1-C12直链,支化或环状链烷烃或链烯烃,和5)包括选自O、N和S中的杂原子的未被取代的或被取代的C6-C20芳族烃,其中该取代基选自C1-C12直链,支化或环状链烷烃或链烯烃。通式(IV)的取代或未被取代的荆芥内酰胺化合物可以是单种化合物的单种立体异构体,可以是单种化合物的立体异构体的混合物,或可以是其中R不相同的那些化合物的立体异构体的混合物。
如上所述的二氢荆芥内酰胺可通过荆芥内酰胺的烷基化、随后氢化来制备,或通过二氢荆芥内酰胺的烷基化来制备。荆芥内酰胺可以根据以上提及的Eisenbraun描述的方法,通过荆芥内酯与无水氨接触来制备。N-取代的二氢荆芥内酰胺是通过荆芥内酰胺氢化成二氢荆芥内酰胺、随后进行内酰胺氮的烷基化来合成,或通过荆芥内酰胺的烷基化、随后进行N-取代的荆芥内酰胺的氢化来合成的。荆芥内酰胺的氢化可以在合适的活性金属加氢催化剂存在下进行,如在Augustine,HeterogeneousCatalysisfortheSynthetic Chemist,Marcel Decker,New York,N.Y.(1996)中所述。
N-取代的二氢荆芥内酰胺也可以通过让二氢荆芥内酰胺与合适的金属氢化物反应形成二氢荆芥内酰胺盐,然后让二氢荆芥内酰胺盐与合适的烷基化剂接触形成N-取代的二氢荆芥内酰胺来最终形成。金属氢化物用于产生二氢荆芥内酰胺的酰胺-金属盐。合适的金属氢化物包括,但不限于,氢化钾和氢化钠。适合于二氢荆芥内酰胺盐的N-烷基化的烷基化剂包括链烷基,链烯基,炔基或芳基氯化物,溴化物,碘化物,硫酸酯,甲磺酸酯,甲苯磺酸酯和三氟甲磺酸酯。二氢荆芥内酰胺和N-取代的二氢荆芥内酰胺的进一步叙述,它们的用途和制备它们的方法已公开在共同未决的美国临时申请序列号60/640,129中,该专利申请对于所有目的被引入这里作为本申请的一部分。
在由本发明提供的组合物中,二氢荆芥内酯,荆芥内酰胺,二氢荆芥内酰胺或各自衍生物可以是一种化合物的单种立体异构体,一种化合物的立体异构体类的混合物,两种或多种单独化合物的各自单种立体异构体,或两种或多种单独化合物的立体异构体类的各自混合物的掺混物。
在由本发明提供的组合物中,二氢荆芥内酯,荆芥内酰胺,二氢荆芥内酰胺,和各自衍生物,是用于许多目的的全部化合物,如以有效量用于各种昆虫或节肢动物种类的驱除之目的的驱虫活性成分,或用作芳香剂组合物中的香料化合物,或用作皮肤的局部处理剂。例如,这些化合物能够以局部施用方式被施加在昆虫或节肢动物的人或动物宿主的皮肤、兽皮、头发、毛皮或羽毛上,或施加在非动物宿主如正在生长的植物或作物上,赋予昆虫或节肢动物排斥性或一种令人愉快的气味或芳香。非动物宿主也包括受到昆虫感染的任何制品,如建筑物,家具等等。典型地,这些制品被认为是壁虱/昆虫可接受的食品来源或壁虱/昆虫-可接受的栖息地。
驱虫剂或驱虫剂组合物指驱除昆虫或节肢动物远离它们的优选宿主或远离适合于壁虱/昆虫生存的制品的一种化合物或组合物。大部分已知的驱虫剂根本不是活性的毒药,但通过让昆虫/节肢动物食物来源或生活条件变得无吸引力或讨厌可防止损害人,动物,植物和/或制品。典型地,驱虫剂是化合物或组合物,它们能够局部施加于宿主上,或能够被引入到壁虱/昆虫易感的制品中,阻止昆虫/节肢动物靠近或保留在有宿主或制品存在的邻近3-维空间中。在任一种情况下,驱虫剂的作用是驱除昆虫/节肢动物远离或排斥:(1)宿主,因此最大程度减少“咬”宿主的频率,或(2)制品,因此保护该制品免受虫害。驱虫剂可以是气体(嗅觉),液体,或固体(尝味)的形式。
对于总体驱虫有效性来说比较重要的一种性能是表面活性,因为许多驱虫剂在它们的结构中同时含有极性和非极性的区域。第二种性能是挥发性。驱虫剂构成了不平常类型的化合物,其中活性成分从宿主皮肤或其它表面上,或从壁虱/昆虫排斥性制品上的蒸发,是有效性所必需的,这可通过保护宿主免受昆虫咬或保护制品免受损害来测量。
对于施加于宿主的皮肤、兽皮、头发、羽毛或毛皮上的局部用昆虫/节肢动物驱虫剂,驱虫剂的效力的一个方面是直接在所施加的表面之上的空气空间中驱虫剂足以驱除该昆虫/节肢动物的浓度的大小。驱虫剂的所希望水平的浓度是在空气空间中主要从蒸发获得的,但是蒸发速率受到吸收进入到皮肤或其它表面中的速率之影响,以及穿透进入和通过该表面的方式因此通常是驱虫剂从该表面上损失的不希望有的模式。对于含有驱虫剂或在其中引入了驱虫剂的制品有类似的考虑,因为驱虫剂的最低浓度是在包围制品本身的三位空气空间中获得预期保护水平所需要的。
在选择用作昆虫/节肢动物驱除活性成分的物质时,固有的挥发性因此是重要的因素。然而,各种策略都是可行的,当为了试图增加活性物的持久性,同时不降低和优选提高挥发性所需要时。例如,该活性物能够用聚合物和惰性成分配制以增加在所施加的表面上或在制品内的持久性。然而,惰性成分在配制剂中的存在会稀释在所施加的配制剂中的活性物,并且从不希望的快速蒸发所导致的损失因此必须加以平衡,以便抵消由于简单地施加太少的驱虫活性成分以致于变得不太有效的风险。另外地,该驱虫活性成分可以包含在微胶囊中以控制从表面或制品上的损失速率;在表面上或在制品中缓慢地崩解的前体分子可用于控制驱虫活性成分的释放速率;或增效剂可用来连续地刺激驱虫活性成分从组合物中的蒸发。
驱虫活性成分的释放可通过例如亚微米包封层来完成,其中活性成分被包封(包围)在富含蛋白质的表面内,就象空气被截留在气球内一样。该蛋白质能够以例如约20%浓度使用。一种剂型含有许多的这些蛋白质胶囊,这些胶囊被悬浮在水性的洗液中或喷洒用的水中。在与皮肤或其它表面接触之后,该蛋白质胶囊开始破裂,释放出包封的驱虫活性成分。随着各微小胶囊变贫化该过程继续进行,然后相继被一个接触到皮肤或其它表面的新胶囊所替代并且释放它的驱虫活性成分。该过程对于一种应用可以花费长达24小时。因为蛋白质非常有效地粘附于表面如皮肤上,这些配制剂非常耐受汗(出汗)和其它来源的水。
如上所述的驱虫活性成分的独特优点中的一个是它们全部以相对挥发度来表征,使得它们适合用于在如上所述的表面或制品之上、上方和周围获得驱虫活性成分的令人想望地高水平的浓度。这些化合物中的一种或多种典型地用于此目的作为组合物中的驱虫活性成分,在该组合物中化合物与稀释剂或载体掺混,该稀释剂或载体适合于组合物以例如液体,气溶胶,凝胶,气凝胶,泡沫体或粉末(如可喷雾的粉末或细粉)的形式湿法或干法施加于任何表面上。合适的稀释剂或载体包括各种商购有机和无机液体,固体,或半固体稀释剂或载体或者它们的可用于配制皮肤用产品或壁虱/昆虫驱除产品的配制剂当中的任何一种。当配制皮肤用产品或局部壁虱/昆虫驱除剂时,优选的是选择皮肤局部可接受的稀释剂或载体。
驱除昆虫和/或节肢动物的局部用组合物或制品的令人想望的性能包括低毒性,抵抗由于水浸泡或发汗所引起的损失,低的或没有气味或至少有令人愉快的气味,施用的容易性,和在宿主皮肤或其它表面上干的无粘性表面膜的快速形成。为了获得这些性能,局部施用的驱虫剂或驱虫制品所用的配制剂应该允许感染了昆虫和/或节肢动物的动物(例如有蚤虱的狗,有虱子的家禽,有螫蝇或壁虱的母牛,和人)用驱虫活性成分(包括它的组合物)处理,这通过此类人或动物的皮肤、兽皮、头发、毛皮或羽毛或其它表面与有效量的用于从人或动物宿主中驱除昆虫或节肢动物的驱虫剂接触来进行。
有效量的驱虫活性成分在受到昆虫侵蚀的表面(如皮肤,兽皮,头发,毛皮,羽毛或植物或农作物表面)上的施用可通过将驱虫活性成分分散到空气中或将驱虫活性成分分散为液体雾或引入到粉末或粉尘中来进行,这将允许驱虫活性成分降落在所预期的宿主表面上。还希望通过将驱虫活性成分与易消失的赋形剂掺混来配制驱虫活性成分的组合物以便以喷雾剂的形式施用。此类组合物可以是气溶胶,可喷雾的液体或可喷雾的粉末组合物,它们适合于利用压缩气体或机械泵喷雾将驱虫活性成分分散到大气中。同样地,液体/半固体/固体组合物以湿或干燥形式(例如作为易粉碎的固体)在宿主上的直接散布是让宿主的表面与有效量的驱虫活性成分接触的有效方法。
此外,还希望将一种或多种的这里所述的驱虫活性成分与已知具有昆虫驱除性能的一种或多种其它化合物掺混在组合物中,实现可从该掺混得到的协同效应。为此目的可掺混的已知具有昆虫驱除性能的合适化合物包括但不限于一种或多种下列物质:
二氢荆芥内酯,苯偶酰,苯甲酸苄酯,2,3,4,5-双(丁基-2-烯)四氢糠醛,丁氧基聚丙二醇,N-乙酰丁苯胺,6,6-二甲基-5,6-二氢-1,4-吡喃酮-2-羧酸正丁基酯,己二酸二丁酯,邻苯二甲酸二丁酯,琥珀酸二正丁基酯,N,N-二乙基-间-甲苯酰胺,卡百酸二甲酯(驱蚊灵),邻苯二甲酸二甲酯,2-乙基-2-丁基-1,3-丙二醇,2-乙基-1,3-已二醇,异辛可布酸二正丙基酯,2-苯基环己醇,N,N-二乙基琥珀酰胺酸正丙基酯,对-甲烷-3,8-二醇,IR-3535和picaridin。
除以上所述的一种或多种的驱虫活性成分外,壁虱/昆虫驱除组合物还可包括一种或多种香精油和/或香精油的活性成分。“香精油”被定义为从植物获得的具有植物的香味和其它属性的任何类型的挥发油。有用香精油的例子包括一种或多种的下列物质:苦杏仁油,茴香油,罗勒油,月桂油,页蒿子油,小豆蔻油,雪松油,芹菜油,春黄菊油,肉桂油,香茅油,丁香油,芫荽油,枯茗油,莳萝油,桉叶油,小茴香油,姜油,葡萄柚油,柠檬油,酸橙油,薄荷油,香芹油,薄荷油,胡椒油,玫瑰油,留兰香油(醇),甜橙油,麝香草油,姜黄油,和冬青油。香精油中活性成分的例子是:香茅醛,水杨酸甲酯,水杨酸乙酯,水杨酸丙酯,香茅醇,黄樟素,和苎烯。
可被本发明所提供的化合物和/或组合物驱除的昆虫和节肢动物包括较大组的无脊椎动物中的任何一种,该动物在成虫状态(非成虫状态包括幼虫和蛹)通过将身体分成头,胸,和腹部,三对的腿,和,常常(但不总是)两对的膜翼来表征。这一定义因此包括壁虱和各种蛰咬昆虫(例如蚂蚁,蜜蜂,恙螨,蚤虱,蚊子,黄蜂),蛰咬苍蝇[例如墨蚊,牛虻蝇,厩蝇,螫蝇(扰血蝇)],钻木昆虫(例如白蚁),有害昆虫(例如家蝇,蟑螂,虱子,蟑螂,木虱),和居家害虫(例如面粉和豆鞘翅目昆虫,尘螨类,蛾,蠹虫,象鼻虫)。
希望驱除壁虱或昆虫的宿主可以包括被壁虱或昆虫影响的任何植物或动物(包括人)。典型地,宿主被认为是壁虱/昆虫可接受的食品来源或壁虱/昆虫-可接受的栖息地。例如,人和动物成为吸血昆虫和节肢动物如蛰咬苍蝇,恙螨,蚤虱,蚊子,壁虱和虱子的食物来源宿主。
在另一个实施方案中,在这里描述的化合物可用作香料化合物或用作香料组合物中的活性物,并且以局部方式施用于人或动物皮肤或其它表面上以赋予令人喜欢的香味,就象在人或宠物用的皮肤洗液和芳香剂中一样。
特别因为与这里所述的化合物有关的令人愉快的芳香味,本发明的附加实施方案是这样一个实施方案,其中一种或多种的这些化合物被配制到组合物之中,该组合物用作有其它基本目的的产品。这些产品的香味将因为一种或多种的化合物在其中的存在而得到增强,该化合物迄今仅仅针对其作为驱虫活性成分的价值进行描述。此类产品包括,没有限制,科隆香水,洗液,喷雾剂,霜剂,凝胶剂,软膏,浴液和淋浴凝胶剂,泡沫产品(例如剃泡沫),粉底,除臭药,洗发剂,发用瓷漆/头发漂洗剂,和个人皂组合物(例如洗手皂和浴皂/淋浴皂)。化合物当然被引入此类产品中简单地赋予令人喜欢的芳香味,但是附加的有益效果是它们还具有壁虱/昆虫驱除性质。
各种以上讨论产品的相应方面是本发明的附加备选实施方案,它是通过提供作为组合物的或引入到组合物、皮肤处理剂或制品中的如上所述一种或多种化合物来制造物质组合物、皮肤的局部处理剂或制品的方法。此类产品,以及如上所述的方法和工艺,举例说明这些化合物作为香味化合物或芳香剂的用途,或在香料组合物或配制剂中的用途,或在皮肤用局部处理剂中的用途,或在制品中的用途。在制造物质组合物时,例如,组合物能够作为可喷雾液体剂,气溶胶,泡沫体,霜剂,软膏,凝胶剂,糊剂,粉末剂或易粉碎的固体剂来制得。在此情况下制造方法因此包括将活性成分与合适的稀释剂或载体或其它惰性成分掺混以促进以所述的物理形式输送,如容易喷雾的液体载体;气溶胶或泡沫剂的推进剂;霜剂,软膏,凝胶剂或糊剂的粘稠载体;或粉末剂或易粉碎的固体剂的干燥或半固体载体。
作为昆虫/节肢动物驱除剂,芳香产品,皮肤处理剂或其它个人护理产品制得的含有一种或多种以上所述化合物作为活性成分的组合物也可含有典型地在个人护理工业中使用的其它治疗或化妆活性助剂或辅助成分。这些的例子包括杀真菌剂,防晒剂,阳光遮蔽剂,维生素类,鞣剂,植物提取物,消炎药,抗氧化剂,自由基清除剂,类视黄醇,α-醇酸,防腐剂,抗生素,抗菌剂,抗组胺剂;助剂如增稠剂,缓冲剂,螯合剂,防腐剂,凝胶剂,稳定剂,表面活性剂,润肤剂,着色剂,库拉索芦荟提取物,蜡;以及这些中的任何两种或多种的混合物。
为了制备适合于如上所述的用途的组合物,典型地希望制备由驱虫活性成分和经过选择在该组合物中有特定的有益目的的一种或多种组分组成的配制组合物。这些类型的组分以及各组分的合适选择的例子的叙述在下面给出。现有技术中已知的任何混合方式可用于制备该配制组合物。
在本发明中,用于以上公开的活性成分化合物的各种稀释剂都能够使用。稀释剂使得该配制剂被调节到该活性成分化合物的有效浓度。当配制局部用的壁虱/昆虫驱除剂时,该活性成分化合物优选被混合在皮肤局部用可接受的稀释剂中。稀释剂可以进一步提供拒水性,防止皮肤刺激性,和/或安慰和调理皮肤。当对于壁虱/昆虫驱除剂的任何配制剂选择稀释剂时的考虑因素包括市场上有供应,成本,排斥性,蒸发速度,气味和稳定性。该载体,另外,应该优选也是对环境没有害的载体。一些载体能够本身具有驱虫性能。
在这里适合使用的稀释剂的例子包括水,和液体脂肪族烃(例如,戊烷,己烷,庚烷,壬烷,癸烷和它们的类似物)和液体芳族烃。其它液烃的例子包括由煤的蒸馏和各种类型和等级的石油化工原料的蒸馏所生产的油,其中包括由石油的分馏所获得的煤油。其它石油包括一般称作农业喷雾油的那些(例如,所谓的轻质和中等质量喷雾油,它由在石油的蒸馏中的中间馏分组成并且它们仅仅是轻微挥发性的)。此类油通常是高度精制的并且可以含有仅仅少量的不饱和化合物。此类油,另外,一般是链烷烃油和因此能够用水和乳化剂加以乳化,稀释到更低的浓度,并用作喷雾剂。从木质纸浆的硫酸盐消化获得的乇尔油,象链烷烃油,能够类似地使用。其它有机液体稀释剂能够包括液体萜烃和萜烯醇如α-蒎烯,二聚戊烯,萜品醇,等等。
仍然其它合适的稀释剂包括有机溶剂如脂肪族和芳族醇类,酯类,醛类,和酮类。脂肪族一元醇包括甲醇,乙醇,正丙醇,异丙醇,正丁醇,仲丁醇,和叔丁醇。合适的醇包括二醇(如乙二醇和丙二醇)和频哪醇。合适的多羟基醇包括甘油,阿拉伯糖醇,赤藓醇,山梨糖醇,等等。最终,合适的环状醇包括环戊基醇和环己基醇。
普通的芳族和脂族酯,醛和酮能够用作载体,并且偶而与上述醇相结合使用。仍然其它液体载体包括较高沸点的石油产品如矿物油和高级醇(如十六烷醇)。
适合用于本发明的组合物中的其它载体,除水或乙醇之外,包括一种或多种下列物质:丙酮,甲基乙基酮,四氢呋喃,环己烷,C6~C20线性、支化或环状的链烷烃,链烷醇或链烷烃多元醇,C6~C400聚乙二醇,C30~C150聚丙二醇,烷氧基化醇(如C4~C60醇的聚氧化乙烯醚和/或聚氧化丙烯醚;或酯,作为戊基、苄基、丁基、十六烷基、癸基、乙基、己基、甲基、辛基、丙基的乙酸酯,己二酸酯,苯甲酸酯,戊二酸酯,月桂酸酯,马来酸酯,肉豆蔻酸酯,草酸酯,棕榈酸酯,邻苯二甲酸酯,水杨酸酯,癸二酸酯,硬脂酸酯或琥珀酸酯来制得。
本发明提供的组合物还可含有在个人护理产品配制剂的现有技术中已知的助剂或改性剂,如增稠剂,缓冲剂,螯合剂,防腐剂,香料,抗氧化剂,凝胶剂,稳定剂,表面活性剂,润湿剂,着色剂,库拉索芦荟提取物,蜡,其它穿透增强剂和它们的混合物,以及治疗或化妆用活性剂。
另外,本发明的组合物也可含有其它助剂或改性剂,如一种或多种治疗或化妆用活性成分。可用于本发明的组合物中的举例性的治疗或化妆用活性成分包括杀真菌剂,防晒剂,阳光遮蔽剂,维生素类,鞣剂,植物提取物,消炎药,抗氧化剂,自由基清除剂,类视黄醇,α-醇酸,润肤剂,防腐剂,抗生素,抗菌剂或抗组胺剂,并且是以有效实现预期的治疗或化妆效果的用量存在。
另外,本发明的组合物可含有典型用于化妆品工业中的一种或多种其它助剂,改性剂或添加剂,如抗氧化剂,乳液稳定剂,防腐剂,推进剂,润肤剂,防晒剂,表面活性剂,乳化剂,增溶剂和/或紫外线吸收剂。可用作此类添加剂的材料的例子在下面进行阐述。
本发明的组合物可以包括可用作抗氧化剂的一种或多种材料,如还原剂和自由基清除剂。可用作抗氧化剂的合适材料包括一种或多种下列物质:乙酰半胱氨酸,抗坏血酸,叔丁基氢醌,半胱氨酸,二戊基氢醌,异抗坏血酸,阿魏酸,氢醌,对-羟基茴香醚,羟胺硫酸盐,抗坏血酸镁,抗坏血酸基磷酸镁,氰双苯丙烯酸辛酯,均苯三酚,抗坏血酸基生育酚基磷酸钾,亚硫酸钾,芸香苷,抗坏血酸钠,亚硫酸钠,巯基乙酸钠,硫二甘醇,硫二甘醇酰胺,巯基乙酸,硫代水杨酸,生育酚,醋酸生育酚,亚油酸生育酚酯,亚磷酸三(壬基苯基)酯。
本发明的组合物也可包括用作乳液稳定剂的一种或多种材料。这些材料不起着主乳化剂的作用,但是防止或减少已乳化液滴的凝聚。这能够例如通过电荷排斥改善该乳液的连续相或分散相,从粘度的变化,或从液滴表面上的薄膜形成来实现。可用作乳液稳定剂的合适材料包括一种或多种下列物质:C15~C18二醇;H(OCH2CH2)nOH,其中n=350-160,000;C10~C50醇如十六烷醇,月桂醇,肉豆蔻醇,硬脂醇,牛油醇;C10~C50线性,支化或环状脂肪族或芳族醇类;铝的山萮酸盐,辛酸盐,二亚油酸盐,二肉豆蔻酸盐,二硬脂酸盐,异硬脂酸盐,羊毛脂酸盐,月桂酸盐,肉豆蔻酸盐,棕榈酸盐,硬脂酸盐,或三硬酯酸盐;角叉菜胶钙;钙的月桂酸盐,肉豆蔻酸盐或硬脂酸盐;羟基硬脂酰基硬脂酸C18~C38烷基酯,羧甲基羟乙基纤维素,羧甲基羟丙基瓜尔胶,纤维素胶,十六烷基羟乙基纤维素,胆固醇,葡萄糖五乙酸酯,甘醇十六烷十八烷酸酯,甘醇羟基硬脂酸酯,褐煤酸酯,油酸酯,棕榈酸酯,蓖麻醇酸酯或硬脂酸酯;羟基丁基甲基纤维素,羟乙基纤维素,羟乙基乙基纤维素,羟基丙基纤维素,羟丙基瓜尔胶,羟丙基甲基纤维素,甲基纤维素,甲基羟乙基纤维素,微晶纤维素,果胶,藻酸钾,钾角叉菜胶,钠丙烯酸聚合物,钠羧甲基葡聚糖,钠角叉菜胶,纤维素硫酸钠,环糊精硫酸钠,硬脂基乙烯基醚/马来酸酐(“MA”)共聚物,苯乙烯/MA共聚物,聚乙酸乙烯酯,和黄原酸胶。
本发明的组合物还包括可用作防腐剂的一种或多种材料,它们防止或妨碍微生物生长和因此保护组合物(或从其制备的产品)免受损坏或免受在使用过程中消费者的偶然污染。可用作防腐剂的合适材料包括一种或多种下列物质:
·铵苯甲酸盐或丙酸盐
·对羟基苯甲酸异丁基酯
·对羟基苯甲酸异癸基酯
·苯甲酸
·异丙基甲酚,对羟基苯甲酸酯或山梨酸酯
·苯并三唑
·苯甲酸镁
·对羟基苯甲酸苄基酯
·丙酸镁
·水杨酸镁
·苯甲酸丁酯
·二甲基羟甲基吡唑
·对羟基苯甲酸丁酯
·二羟甲基环亚乙基硫脲
·钙苯甲酸盐,水杨酸盐,山梨酸盐,对羟基苯甲酸盐或丙酸盐
·二甲基噁唑烷
·甲基羟基乙内酰脲
·甲基二溴戊二腈
·甲基异噻唑啉酮
·甲基,乙基,丙基或苯基对羟基苯甲酸酯
·双氯苯双胍己烷双乙酸盐,二葡萄糖酸盐或二盐酸化物
·戊二醛
·乙二醛
·氯乙酰胺
·己氧苯脒
·氯丁醇
·己氧苯脒双(对羟基苯甲酸酯)
·苯酚
·己氧苯脒对羟基苯甲酸酯
·辛基,月桂基,肉豆蔻基,棕榈基或硬脂基水杨酸酯
·辛基,月桂基,肉豆蔻基,棕榈基或硬脂基苯甲酸酯
·氯吩(Chlorophene)
·4-羟基苯甲酸
·对羟基苯甲酸苯氧基乙基酯
·对-氯苯酚
·苯氧基异丙醇
·氯代百里酚
·苯甲酸苯酯
·钾水杨酸盐,山梨酸盐,苯甲酸盐,对羟苯甲酸丙酯,对羟基苯甲酸丁酯,对羟基苯甲酸乙酯,对羟基苯甲酸甲酯,对羟基苯甲酸(酯),酚盐,邻-苯基苯酚盐或丙酸盐
·丙酸
·苯甲酸丙酯
·硼硅酸银
·磷酸银镁铝
·山梨酸
·羟甲基甘氨酸钠,对羟基苯甲酸甲酯,对羟基苯甲酸酯,苯酚磺酸盐,酚盐,邻-苯基苯酚盐,丙酸盐,对羟苯甲酸丙酯,1-氧-2-巯基吡啶,水杨酸盐,山梨酸盐,苯甲酸盐,对羟基苯甲酸丁酯,对-氯-间甲酚,脱水乙酸酯(Dehydroacetate),对羟基苯甲酸乙酯,甲酸盐或羟基甲烷磺酸盐
·氧巯基吡啶锌
本发明的组合物还可包括用作推进剂的一种或多种材料,它们是用于从增压容器中逐出产物的化学品(气溶胶)。推进剂的功能取决于在环境温度下它的蒸气压和它的压缩性。液体或气体都能够用作推进剂,只要在容器内产生的压力在正常贮存和使用条件下安全地低于容器的爆裂压力就行。用作推进剂的合适材料包括一种或多种下列物质:氮气,二氧化碳,CH3CF2,CH3CClF2,CH3CHF2,一氧化二氮,二甲醚,丁烷,异丁烯,戊烷,乙烷,异戊烷,和丙烷。
本发明的组合物也可包括用作润肤剂的一种或多种材料,它是保持皮肤的柔软、光滑和柔顺性外观的化妆成分。润肤剂的目的是保留在皮肤表面上或保留在层状角质中用作润滑剂,减少剥落,和改善皮肤外观。这些主要是属于化学品类别的疏水性材料,这些化学品被描述为烃类(例如矿物油,聚异丁烯和聚α-烯烃);酯类(例如棕榈酸异丙酯,棕榈酸辛基酯和苯甲酸C12~C15烷基酯);三酸甘油酯(例如三辛酸/癸酸甘油酯,和植物油如芝麻油);聚氧化丙烯/聚氧化乙烯聚合物;和聚硅氧烷类如二甲基聚硅氧烷,环戊硅氧烷(cyclopentasiloxane)和苯基三甲基硅氧烷。也可用作润肤剂的合适材料包括一种或多种下列物质:
·乙酰化羊毛脂或羊毛脂醇
·双苯基六甲基硅氧烷
·辛酸/癸酸甘油酯
·辛酸/癸酸/琥珀酸三酸甘油酯
·乙酰化蔗糖二硬脂酸酯
·乙酰基柠檬酸三己基酯
·丁基异硬脂酸酯,肉豆蔻酸酯,油酸酯或硬脂酸酯
·辛酰基甘醇
·乙酰基柠檬酸三辛基酯
·十六烷基十八烷基辛酸酯或棕榈酸酯
·杏仁油(Prunus armenlaca Kernel Oil)
·十六烷基乙酸酯,辛酸酯,乳酸酯,月桂酸酯,辛酸酯或油酸酯
·C14~C15醇
·C10~C30羧酸类的C4~C20线性或支化脂族基酯
·Argania Spinosa Oil
·C12~C28烷基乙酸酯,苯甲酸酯或乳酸酯或辛酸酯
·油梨油
·C24~C28烷基甲基硅氧烷
·C12~C13烷基辛酸酯
·十六烷基二醇,甘醇异硬脂酸酯或甘醇棕榈酸酯
·十二烷酸苄酯
·异硬脂基醇,肉豆蔻基醇,月桂基醇,异十六烷基醇,十五烷基醇,油醇,十三烷基醇或十一烷醇
·异硬脂基甘油基醚
·异硬脂基苯甲酸酯,乳酸酯,新戊酸酯,辛酸酯,棕榈酸酯或肉豆蔻酸酯
·麝香蔷薇种子油
·月桂酸异戊基酯
·异丁基肉豆蔻酸酯,棕榈酸酯,壬酸酯或硬脂酸酯
·异丙基月桂酸酯,肉豆蔻酸酯,棕榈酸酯或硬脂酸酯
·肉豆蔻基异硬脂酸酯,乳酸酯,新戊酸酯,辛酸酯或丙酸酯
·中华猕猴桃种子油
·异十六烷基异癸酸酯,棕榈酸酯或硬脂酸酯
·羊毛脂,羊毛脂油或羊毛脂蜡
·异癸基柠檬酸酯,羟基硬脂酸酯,月桂酸酯,肉豆蔻酸酯,新戊酸酯,棕榈酸酯或硬脂酸酯
·乙酸壬酯
·月桂基二醇
·月桂基异硬脂酸酯或乳酸酯
·辛基癸醇或辛基十二烷醇
·辛基,月桂基,肉豆蔻基,棕榈基或硬脂基苯甲酸酯
异十六烷
·异己基新戊酸酯,棕榈酸酯或月桂酸酯
·羟基硬脂酸辛基酯,月桂酸酯,异棕榈酸酯,异硬脂酸酯,肉豆蔻酸酯,新戊酸酯,油酸酯,棕榈酸酯或硬脂酸酯
·异丙基·羟基十六烷基醚
·异丙基羟基硬脂酸酯,异硬脂酸酯,羊毛脂酸酯,月桂酸酯,亚油酸酯,肉豆蔻酸酯或油酸酯
·油基乙酸酯,乳酸酯或油酸酯
·甲基羟基硬脂酸酯,月桂酸酯,异硬脂酸酯,肉豆蔻酸酯,油酸酯,棕榈酸酯或壬酸酯
·棕榈酸异丙酯,或硬脂酸异丙基酯
·异山梨糖醇月桂酸酯
·西番莲油(Passiflora Eduls Oil)
·聚乙二醇甘油酯
·聚甘油基油基醚
·聚乙二醇蓖麻油
·季戊四醇基二油酸酯,二硬脂酸酯,硬脂酸酯,四苯甲酸酯或三油酸酯
·丙二醇羟基硬脂酸酯硬脂酸酯,月桂酸酯,亚油酸酯,肉豆蔻酸酯,蓖麻醇酸酯,硬脂酸酯,油酸酯,大豆脂肪酸酯或辛酸酯
·丙二醇肉豆蔻基醚或肉豆蔻基醚乙酸酯
·聚丙二醇月桂基,十六烷基,硬脂基,油基或季戊四醇基醚
·硬脂基乙酸酯,苯甲酸酯或乳酸酯
·硬脂基二醇异硬脂酸酯或柠檬酸酯
·聚丙二醇/聚乙二醇
·三羟甲基丙烷或丙烯
·三(三丁氧基硅氧基)甲基硅烷。
本发明的组合物还可包括用作防晒剂的一种或多种材料。在58Fed.Reg.28194(1993年5月12日),防晒活性成分被定义为“吸收至少85%的在290-320纳米的波长下的UV范围中的辐射,但透射或不透射波长比320纳米长的辐射的成分。用作防晒剂的合适材料包括一种或多种下列物质:氨基苯甲酸(“PABA”),氨基苯甲酸甘油基酯(对氨基苯甲酸甘油基酯),氧苯酮(二苯甲酮-3),对甲氧基肉桂酸乙氧乙酯,胡莫柳酯,对-二甲基氨基-苯甲酸辛基酯,二乙醇胺甲氧基肉桂酸酯,2-乙基己基、月桂基、肉豆蔻基、棕榈基或硬脂基4-甲氧基肉桂酸酯;苯基苯并咪唑磺酸,氨基苯甲酸基酯,双棓酰(digalloyl)三油酸酯,氰双苯丙烯酸辛酯,磺异苯酮(二苯甲酮-4),二羟基二苯甲酮(二苯甲酮-8),甲氧基肉桂酸辛基酯,二氧化钛,4-[双(羟丙基)]氨基苯甲酸乙基酯(二羟基丙基对氨基苯甲酸乙基酯),水杨酸辛基酯,和三乙醇胺水杨酸酯。
本发明的组合物还可包括用作乳化剂和/或也可用作表面活性剂或增溶剂的一种或多种材料。此类材料可用来降低表面张力,在乳化液滴的表面上形成复合膜,在乳化液滴上产生排斥性阻隔层以防止它们的凝聚,在贮存期间延迟在乳液中的物理变化或引起溶质变成由表面活性剂所形成的胶束的一部分。
这里适合使用的乳化剂包括具有疏水性和亲水性结构部分的阴离子乳化剂,其中疏水性(亲油性)结构部分具有负电荷。这些类型的乳化剂一般是:
脂肪酸皂,其中疏水性部分一般由具有C8~C20碳链的有机酸组成,和亲水性部分一般由钠,钾,三乙醇胺,或氨基甲基丙醇组成,例如三乙醇胺硬脂酸盐或硬脂酸钠;
磷酸酯和硫酸酯类,其中疏水性部分一般由具有C8~C20碳链的有机醇组成,和亲水性部分一般由从磷酸或硫酸衍生的磷酸根或硫酸根组成,并用碱中和,例如十六烷基磷酸二乙醇胺盐或十二烷基硫酸钠。
在这里适合使用的乳化剂也包括具有疏水性和亲水性结构部分的非离子型乳化剂,其中疏水性(亲油性)结构部分通常是脂肪酸(或二脂肪酸),脂肪醇,聚丙二醇,C6~C20醇,或聚硅氧烷(例如二甲基聚硅氧烷)。典型的非离子型乳化剂包括:脂肪酸酯,其中该亲水性部分是聚乙二醇(其中乙二醇基团的数量能够是2~150(n=2-150)),并且能够与酸如月桂酸或硬脂酸形成酯。
脂肪族醚,其中该亲水性部分是聚氧化乙烯(其中环氧乙烷基团的数量能够是2~150),并且能够从醇如月桂醇或硬脂醇形成。
嵌段共聚物,如从聚氧化乙烯(POE)和聚氧化丙烯(PPO)反应得到的那些。
这里适合使用的乳化剂也包括具有疏水性和亲水性结构部分的那些,其中疏水性(亲油性)结构部分具有来自“季铵化”氮基团的净正电荷。该季铵化铵基团能够具有作为它的阴离子的氯,乙基硫酸根或甲基硫酸根。疏水性基团能够是属于具有C8~C22碳链的脂肪醇和脂肪酸或硅油的物质组中的单、二或三脂肪族基团,例如二十二烷基三甲基氯化铵。
这里适合用作乳化剂的合适材料还包括一种或多种下列物质:
·C6~C400聚乙二醇,
·C30~C150聚丙二醇,
·烷氧基化醇(如C4~C60醇的聚氧化乙烯和/或聚氧化丙烯醚);
·C50~C650线性或支化的二羟基聚氧化乙烯/聚氧化丙烯嵌段共聚物
·乙二胺的C50~C650支化的多羟基聚氧化乙烯/聚氧化丙烯嵌段共聚物
·C12~C330乙氧基化烷基苯酚
·C12~C60醇的C16~C140聚乙二醇醚
·C12~C330乙氧基化烷基苯酚的羧酸酯
·C12~C40羧酸和C8~C40聚乙二醇的酯
·辛酸或癸酸三酸甘油酯和C8~C40聚乙二醇的酯
·C12~C330乙氧基化烷基苯酚的磷酸酯
·C12~C60醇的C16~C140聚乙二醇醚的磷酸酯和二酯
·枞酸
·硬脂酰基乳酸钙
·乙基硫酸十六烷基聚氧乙烯醚基(Cetethyl)吗啉鎓盐
·十六烷基三甲基铵溴化物,氯化物,甲基硫酸盐或甲苯磺酸盐
·十六烷醇
·十六烷基聚二甲基硅氧烷共聚物多元醇
·十六烷基甘油基醚/甘油共聚物
·十六烷基磷酸酯
·十六烷基十八烷基葡糖苷
·糊精山萮酸酯,月桂酸酯,肉豆蔻酸酯,棕榈酸酯或硬脂酸酯
·双十六烷基磷酸酯
·二乙基氨基乙基月桂酸酯或硬脂酸酯
·二甲基辛炔二醇
·肉豆蔻基磷酸酯
·甘油基花生酸酯,山萮酸酯,辛酸酯,癸酸酯,椰油酸酯,芥酸酯,氢化松脂酸酯,羟基硬脂酸酯,异棕榈酸酯,异硬脂酸酯,异十三烷酸酯/硬脂酸酯/己二酸酯,羊毛脂酸酯,月桂酸酯,油酸酯,亚油酸酯,亚麻酸酯,油酸酯,褐煤酸酯,肉豆蔻酸酯,棕榈酸酯,硬脂酸酯,棕榈酸油酸酯,蓖麻醇酸酯或十一碳烯酸酯
·甘醇辛酸酯
·氢化卵磷脂
·氢化棕榈酸甘油酯
·羟基十六烷基磷酸酯
·羟乙基甘油基油酸酯和/或硬脂酸酯
·羊毛脂
·月桂基三甲基铵氯化物
·月桂基磷酸酯
·卵磷脂
·一缩甘露醇月桂酸酯或油酸酯
·肉豆蔻酰基甲基丙氨酸
·棕榈酸
·辛氧基甘油基山萮酸酯或棕榈酸酯
·壬酸
·季戊四醇基硬脂酸酯
·磷脂酰胆碱
·钾月桂酸盐,肉豆蔻酸盐,油酸盐,月桂基羟丙基磺酸盐,十六烷基磷酸盐,月桂基硫酸盐,棕榈油酸盐(Palmate),棕榈酸盐,蓖麻醇酸盐或硬脂酸盐
·钠棕榈油酸盐,棕榈酸盐,邻苯二甲酸盐硬脂基酰胺,蓖麻醇酸盐,硬脂酸盐,硬脂基硫酸盐,十三烷基聚氧化乙烯醚硫酸盐,十三烷基硫酸盐,十一碳烯酸盐,月桂酰基乳酸盐,月桂基磷酸盐,肉豆蔻酸盐,油酸盐,油酰基乳酸盐,山萮酰基乳酸盐,己酰基乳酸盐,辛酸盐,异硬脂酰基乳酸盐或月桂酸盐
·丙二醇山萮酸酯,辛酸酯,羟基硬脂酸酯,异硬脂酸酯,月桂酸酯,亚油酸酯,unolenate,肉豆蔻酸酯,油酸酯,蓖麻醇酸酯或硬脂酸酯
·脱水山梨糖醇辛酸酯,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,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,三油酸酯或三硬酯酸酯
·蜜里三糖油酸酯
·硬脂酸
·硬脂酰基乳酸
·硬脂醇
·蔗糖二月桂酸酯,二硬脂酸酯,月桂酸酯,肉豆蔻酸酯,油酸酯,棕榈酸酯,多月桂酸酯,多亚油酸酯,多油酸酯,多棕榈油酸酯或多硬脂酸酯
·山萮醇的C32~C82聚乙二醇醚
·十六烷醇的C20~C106聚乙二醇醚
·十六烷基醇或油醇的C28~C80聚乙二醇醚
·十六烷基醇和/或硬脂醇的C20~C70聚乙二醇醚
·胆固醇的C20~C80聚乙二醇醚
·癸醇的C16~C24聚乙二醇醚
·二氢胆甾醇的C40~C80聚乙二醇醚
·异十六烷基醇的C20~C60聚乙二醇醚
·异癸醇的C18~C30聚乙二醇醚
·异月桂醇的C18~C40聚乙二醇醚
·异硬脂基醇的C20~C120聚乙二醇醚
·甘油癸酸酯,辛酸酯,月桂酸酯,肉豆蔻酸酯,油酸酯,棕榈酸酯或硬脂酸酯的C12~C120聚乙二醇醚
·月桂醇的C14~C100聚乙二醇醚
·肉豆蔻醇的C16~C24聚乙二醇醚
·油醇的C20~C70聚乙二醇醚
·丁醇的C10~C100聚乙二醇/聚丙二醇醚
·十六烷醇的C20~C106聚乙二醇/聚丙二醇醚
·癸醇的C20~C100聚乙二醇/聚丙二醇醚
·月桂醇的C14~C100聚乙二醇/聚丙二醇醚
·异硬脂基醇的C20~C120聚乙二醇醚的羧酸酯
·月桂醇的C14~C100聚乙二醇醚的羧酸酯
·肉豆蔻醇的C16~C24聚乙二醇醚的羧酸酯
·月桂醇的C14~C100聚乙二醇醚的柠檬酸二酯
·异丙基月桂酸酯,肉豆蔻酸酯,棕榈酸酯或硬脂酸酯
·山梨糖醇的C30~C120聚乙二醇醚的月桂酸酯
·辛基,月桂基,肉豆蔻基,棕榈基或硬脂基水杨酸酯
·十六烷醇的C20~C106聚乙二醇醚的磷酸酯
·异硬脂基醇的C20~C120聚乙二醇醚的磷酸酯
·月桂醇的C14~C100聚乙二醇醚的磷酸二酯
·油醇的C20~C70聚乙二醇醚的磷酸酯和/或二酯
·甘油的C15~C30聚乙二醇醚的硬脂酸酯
·异十六烷基醇的C20~C60聚乙二醇醚的硬脂酸酯
·异硬脂基醇的C20~C120聚乙二醇醚的硬脂酸酯
·十六烷醇的C20~C106聚乙二醇醚的磷酸酯的二乙醇胺盐
·十六烷基醇和/或硬脂醇的C20~C70聚乙二醇醚的磷酸酯的二乙醇胺盐
·油醇的C20~C70聚乙二醇醚的磷酸酯的二乙醇胺盐
·月桂醇的C14~C100聚乙二醇醚的柠檬酸酯的二钠盐
·月桂醇的C14~C100聚乙二醇醚的磷酸酯的二钠盐
·油醇的C20~C70聚乙二醇醚的磷酸酯的二钠盐
·十六烷基醇和/或硬脂醇的C20~C70聚乙二醇醚的磷酸酯的单乙醇胺盐
·山萮酸,癸酸,辛酸,月桂酸,油酸,辛酸,棕榈酸或硬脂酸的C12~C120聚乙二醇二酯
·C6~C40甘油聚合物和山萮酸,癸酸,辛酸,月桂酸,油酸,辛酸,棕榈酸或硬脂酸的聚酯。
本发明的组合物还可包括用作紫外光吸收剂的一种或多种材料,它保护从组合物制得的产品免受由紫外光诱导的化学或物理损害。UV吸收剂,象防晒剂,能够将入射的紫外线辐射转化成较少损害性的红外辐射(热)。可用作紫外线吸收剂的合适材料包括一种或多种下列物质:
·3-苄叉基莰酮
·均二苯乙烯二磺酸盐
·尿囊素对氨基苯甲酸盐
·亚苄基酞
·磺酰胺
·二苯甲酮
·苄叉基莰酮磺酸
·二羟基丙基对氨基苯甲酸乙基酯
·被选自羟基,烷氧基,烷基,卤素和磺酸酯中的一个或多个基团取代的二苯甲酮
·水杨酸苄酯
·布美三唑
·对氨基苯甲酸乙基酯
·丁基甲氧基二苯甲酰基甲烷
·对氨基苯甲酸丁基酯
·对甲氧基肉桂酸乙氧乙酯
·阿魏酸
·甘油基辛酸酯二甲氧基肉桂酸酯
·二叔丁基羟基苄叉基莰酮
·对氨基苯甲酸甘油基酯
·水杨酸甘醇酯
·二异丙基甲基肉桂酸酯
·对-甲氧基肉桂酸异戊基酯
·水杨酸异丙基苄基酯
·异丙基二苯甲酰基甲烷
·辛基三嗪酮
·甲氧基肉桂酸异丙基酯
·PABA(氨基苯甲酸)
·基氨基苯甲酸酯或水杨酸酯
·二甲基对氨基苯甲酸戊基酯
·对苯二亚甲基二缩莰酮磺酸
·4-甲基苄叉基莰酮
·苯基苯并咪唑磺酸
·二氧化钛
·氰双苯丙烯酸辛酯
·三对氨基苯甲酸(TriPABA)泛酰醇
·辛三唑(Octrizole)
·甲氧基肉桂酸钾
·尿刊酸
·二甲基对氨基苯甲酸辛基酯
·苯基苯并咪唑磺酸钾
·甲氧基肉桂酸辛基酯或水杨酸辛基酯
·苯基苯并咪唑磺酸钠
本发明的组合物还包括用作螯合剂与金属离子配位的一种或多种材料。此举将有助于钝化金属离子,以防止它们对于所配制组合物的稳定性或外观有不利影响。适合用于本发明的组合物中的螯合剂包括一种或多种下列物质:氨基三亚甲基膦酸,β-丙氨酸二乙酸,乙二胺四乙酸二钠钙,柠檬酸,环糊精,环己烷二胺四乙酸,柠檬酸二铵,EDTA二铵,EDTA二钾,氮杂环庚烷二磷酸二钠,EDTA二钠,焦磷酸二钠,EDTA(乙二胺四乙酸),葡糖酸,HEDTA(羟乙基乙二胺三乙酸),甲基环糊精,三磷酸五钾,氨基三亚甲基膦酸五钠,三磷酸五钠,戊烯酸(penteticacid),植酸,柠檬酸钾,葡糖酸钾,柠檬酸钠,二亚乙基三胺五亚甲基膦酸钠,二羟基乙基甘氨酸钠,葡糖酸钠,偏磷酸钠,偏硅酸钠,植酸钠,三乙醇胺(“TEA”)-EDTA,TEA-聚磷酸盐,四羟丙基乙二胺,焦磷酸四钾,EDTA四钠,焦磷酸四钠,EDTA三钾,EDTA三钠,HEDTA三钠,和磷酸三钠。
本发明的组合物还可以包括用作生物杀伤剂的一种或多种材料。生物杀伤剂用于抑制微生物(如细菌、真菌或酵母)的增长或破坏微生物并提供消毒剂。适合用于本发明的组合物中的生物杀伤剂包括一种或多种下列物质:
·苯酚磺酸铝
·苯酚磺酸铵
·新洁尔灭或洁尔灭
·苯甲酰喹啉
·双(1-氧-2-巯基吡啶)
·硼酸
·莰酮苯甲烃铵甲基硫酸盐
·十六烷基二甲基苄基氯化铵
·十六烷基乙基二甲基铵溴化物
·十六烷基三甲基铵溴化物,氯化物,甲基硫酸盐,糖精酸盐,或甲苯磺酸盐
·十六烷基吡啶鎓氯化物
·双氯苯双胍己烷
·双氯苯双胍己烷双乙酸盐
·双氯苯双胍己烷二葡萄糖酸盐
·双氯苯双胍己烷二盐酸化物
·对-氯-间甲酚
·氯吩(Chlorophene)
·对-氯苯酚
·氯代百里酚
·氯二甲苯酚
·煤焦油
·胶体状硫
·克菌定乙酸盐
·克菌定氯化物
·二氯苄基醇
·二氯吩
·二氯-间-二甲苯酚
·二碘甲基甲苯基砜
·二羟甲基环亚乙基硫脲
·二苯甲基哌嗪基苯并咪唑
·磺基琥珀酰基十一碳烯酸盐
·度米芬
·7-乙基双环噁唑烷
·甲醛
·戊二醛
·双三氯酚
·己氧苯脒
·己氧苯脒diisothionate,二(对羟基苯甲酸盐),或对羟基苯甲酸盐
·双辛氢啶
·过氧化氢
·羟甲基二氧代氮杂双环辛烷
·异丙基甲酚
·溴或氯月苯氧铵
·月桂基三甲基铵溴化物或氯化物
·月桂基吡啶鎓氯化物
·氧化汞
·乌洛托品氯化物
·甲苄乙氧胺氯化物
·壬苯聚醇-9碘
·壬苯聚醇-12碘
·Olealkonium Chloride
·羟基喹啉
·喹啉苯酸
·羟基喹啉盐
·苯酚
·邻苯基苯酚
·水杨酸苯酯
·苯酚钾
·邻-苯基苯酚钾
·水杨酸钾
·二氯异氰尿酸钾
·丙酸
·苯酚磺酸钠
·苯酚钠
·邻-苯基苯酚钠
·噻唑苯并咪唑
·2,2’-硫代双(4-氯苯酚)
·二硫化四甲秋兰姆
·甘油三乙酸酯
·三氯二苯脲
·三氯苯氧氯酚
·硼酸三辛基十二烷基酯
·十一碳烯酸
·乙酸锌
·天冬氨酸锌
本发明的组合物还可包括用作成膜剂的一种或多种材料,它在施用该组合物的表面上促进连续膜的产生(在干燥之后)。适合用于本发明的组合物中的成膜剂包括一种或多种下列物质:蛋白,藻酸铵,加拿大香脂(香脂冷杉),秘鲁香脂(秘鲁香脂树),塔鲁香脂(叶鲁香脂树),苯偶姻(安息香苯偶姻)胶,丁氧基脱乙酰壳多糖,丁基化的聚氧化亚甲基脲,角叉菜胶钙,羧甲基脱乙酰壳多糖,羧甲基葡聚糖,羧甲基羟乙基纤维素,乙酸纤维素,乙酸丁酸纤维素,纤维素胶,脱乙酰壳多糖,脱乙酰壳多糖己二酸酯,脱乙酰壳多糖乳酸酯,火棉胶,乙基纤维素,羟基丁基甲基纤维素,羟乙基纤维素,羟丙基脱乙酰壳多糖,羟丙基瓜尔胶,麦芽糖糊精,硝化纤维,聚β-丙氨酸,血清清蛋白,虫胶,钠丙烯酸聚合物,钠羧甲基壳多糖,钠角叉菜胶,和玉米溶蛋白;和含有从化合物衍生的单体单元的聚合物和共聚物,该化合物具有一种或多种的下面官能团或由于聚合反应而提供一种或多种的下列官能团:丙烯酰胺,(甲基)丙烯酸酯,乙烯基吡咯烷酮,(甲基)丙烯酸,己二酸,马来酸酐,新戊二醇,偏苯三酸酐,二甘醇,二亚乙基三胺,富马酸,邻苯二甲酸,间苯二酸,硬脂酸烯丙基酯,乙酸乙烯酯,苯乙烯,氨基甲基丙醇,苯甲酸,邻苯二甲酸酐,季戊四醇,丁二烯,丙烯腈,乙烯,表氯醇,哌嗪,十六烷基十八烷基醇,乙烯醇,乙酸乙烯酯,丙烯,异丁烯,马来酸钠,十八碳烯,邻苯二甲酸酐,苯甲酸,三羟甲基丙烷,对苯二甲酸丁二醇酯,对苯二甲酸乙二醇酯,谷氨酸乙基酯,异丁烯,亚甲基氧化物,蜜胺,戊烯,乙烯基丁缩醛,乙烯基咪唑鎓乙酸盐,月桂酸乙烯基酯,乙烯基·甲基醚,十八烷基乙烯基醚,衣康酸,丙烯酸钠,马来酸,烯丙基醚,乙烯基醚,苯甲酸烯丙酯,邻苯二甲酸苄基酯,和马来酸丁基酯;
本发明的组合物还包括用作触变剂的一种或多种材料,以便增稠所提供的组合物的含水部分。触变剂发挥这一功能的能力包括它的水溶性,或亲水性。主要的触变剂能够来自于各种化学类型:以黄原胶,纤维素,角叉菜,或瓜耳树胶为基础的天然增稠剂;或合成材料,如以例如羧基乙烯基化合物(例如丙烯酸聚合物),丙烯酸,丙烯酸酯或丙烯酰胺为基础的聚合物。适合用于本发明的组合物中的触变剂还包括一种或多种下列物质:
金合欢胶
乙酰胺单乙醇胺(“MEA”)
丙烯酸,丙烯酰胺,丙烯腈和/或丙烯酸酯聚合物和共聚物
琼脂
褐藻酸
藻酸
氢氧化铝/氢氧化镁硬脂酸盐
藻酸铵,氯化铵,或硫酸铵
支链淀粉
花生醇
花生基二醇
凹凸棒石
山萮酸酰胺二乙醇胺(“DEA”)
山萮酸酰胺MEA
山萮酰胺基丙基甜菜碱
二十二烷基甜菜碱
膨润土
丁氧基脱乙酰壳多糖
海藻酸钙,角叉菜胶钙,或氯化钙
硬脂酸C20~C40烷基酯
C6~C400聚乙二醇
癸酰胺DEA
羧甲基壳多糖
羧甲基脱乙酰壳多糖
羧甲基葡聚糖
羧甲基羟乙基纤维素
肉毒碱
角叉菜胶(鹿角菜)
纤维素胶
十六烷基十八烷基醇
十六烷醇
鲸蜡基甜菜碱
十六烷基二醇
十六烷基羟乙基纤维素
椰油基-甜菜碱
椰油基-羟基磺基甜菜碱
椰子醇
椰油基/油酰胺基丙基甜菜碱
癸醇
癸基甜菜碱
糊精
二亚苄基山梨糖醇
芥酸酰胺基丙基羟基磺基甜菜碱
明胶
洁冷胶
藻酸甘油基酯
瓜耳树(Cyanopsis TetragonolOba)胶
瓜耳树胶羟丙基三甲基铵氯化物
透明质酸
水合氧化硅
氢化牛油
羟基烷基纤维素
羟丙基脱乙酰壳多糖
羟丙基瓜尔胶
羟基硬脂酰胺MEA
异丁烯/马来酸钠共聚物
异硬脂酰胺DEA,MEA,或单异丙醇胺(“MIPA”)
海藻(Kelp)
乳酰胺MEA
羊毛脂酸酰胺DEA
月桂酰胺DEA
月桂酰胺MEA
月桂酰胺/肉豆蔻酰胺DEA
月桂酰胺基丙基甜菜碱
月桂醇,甜菜碱,羟基磺基甜菜碱,或磺基甜菜碱
卵磷脂酰胺DEA
亚麻酸酰胺DEA,MEA,或MIPA
硅酸锂镁
硅酸镁铝
硅酸镁
甲基纤维素
甲基羟乙基纤维素
蒙脱土
肉豆蔻酰胺DEA,MEA,或MIPA
肉豆蔻酰胺基丙基甜菜碱
肉豆蔻醇
肉豆蔻基甜菜碱
燕麦(Avena Sativa)粉
燕麦(Avena Sativa)淀粉
油酰胺DEA,MEA,或MIPA
油酰胺基丙基甜菜碱
油基甜菜碱
棕榈酰胺DEA,MEA,或MIPA
棕榈酸酰胺DEA
棕榈酸酰胺MEA
棕榈酰胺基丙基甜菜碱
棕榈仁醇
棕榈仁酰胺DEA,MEA,或MIPA
棕榈仁酰胺基丙基甜菜碱
花生(Arachis Hypogaea)粉
果胶
聚环戊二烯
聚甲基丙烯酸
聚乙烯醇
藻酸钾
角叉菜胶钾
氯化钾
棕榈酸钾
聚丙烯酸钾
硫酸钾
土豆(Solanum Tuberosum)淀粉
海藻酸丙二醇酯
蓖麻油酸酰胺DEA,MEA,或MIPA
蓖麻油酸酰胺基丙基甜菜碱
(甲基)丙烯酸钠共聚物
钠丙烯酸聚合物
钠羧甲基壳多糖
钠羧甲基葡聚糖
角叉菜胶钠
纤维素硫酸钠
氯化钠
环糊精硫酸钠
钠异辛烯/马来酸酐共聚物
氟硅酸钠镁
油酸钠
棕榈酸钠
聚苯乙烯磺酸钠
铝硅酸钠
硬脂酸钠
硫酸钠
大豆酸酰胺DEA
大豆酸酰胺基丙基甜菜碱
硬脂酰胺氨基甲基丙醇(“AMP”),DEA,二异丁基胺(“DIBA”),MEA,或MIPA
硬脂酸酰胺基丙基甜菜碱
硬脂醇
硬脂基甜菜碱
牛油酰胺DEA
牛油醇
牛油酰胺DEA
牛油酰胺MEA
牛油酰胺基丙基甜菜碱
牛油胺氧化物
牛油甜菜碱
TEA-盐酸盐
黄芪(Astragalus Gummi fer)胶
十三烷醇
硅酸三甲胺镁铝
十一烷醇
十一烷基酰胺DEA,或MEA
小麦(Triticum Vulgare)面粉
小麦(Triticum Vulgare)淀粉
黄原酸胶
酵母β-葡聚糖
酵母多糖。
本发明的组合物还可以包括用作湿润剂的一种或多种材料。湿润剂被添加到组合物中以延迟在使用过程中的水分损失,该效果一般通过在其中存在吸湿性材料来实现。适合用于本发明的组合物中的湿润剂包括一种或多种下列物质:C6~C400聚乙二醇,C6~C12线性或支化脂肪族多元醇,二甘油,赤藓醇,果糖,葡萄糖,甘油,甘醇,1,2,6-己烷三醇,蜂蜜,氢化蜂蜜,肌醇,乳酸,乳糖醇,麦芽糖醇,麦芽糖,甘露糖醇,聚甘油基山梨糖醇,丙二醇,葡糖醛酸钠,山梨糖醇,山梨糖醇的C6~C400聚乙二醇醚,蔗糖,尿素,脲-d-葡糖醛酸,和木糖醇。
本发明的组合物还可包括用作香料组分的一种或多种材料,以赋予所配制的组合物以令人愉快的香味或芳香味。适合用于本发明的组合物中的香料包括一种或多种下列物质:
乙醛
乙酰基六甲基四氢萘
戊基苯甲酸酯,β-苯丙烯醛,或水杨酸酯
茴香脑
茴香(Illicium Verum)油
p-茴香酸
薄荷香脂(Melissa Officinalis)油
罗勒(Ocimum Basilicum)油
蜡果杨梅(Myrica Cerifera)蜡
月桂叶(Pimenta Acris)油
香蜂花(Monarda Didyrna)油
苯甲醛
苯偶姻(Styrax Benzoin)胶
苄基乙酸酯,醇,苯甲酸酯,肉桂酸酯,或水杨酸酯
香柠檬(Citrus Aurantium Bergamia)油
桦树(Betula Alba)油
苦杏仁(Prunus Amygdalus Amara)油
苦橙(Citrus Aurantium Amara)油或果皮提取物
乙酸2-叔丁基环己基酯
2-叔丁基环己基氧基丁醇
洋蔷薇(Rosa Centifolia)油
洋蔷薇(Rosa Centifolia)水
金盏花油
莰酮
莰基环己醇
藏茴香(Carum Carvi)油
丁香烷
丁香烯
白豆蔻(Elettaria Cardamomum)油
香芹酮
雪松木油
北非雪松油
甘菊(Anthemis Nobilis)油
β-苯丙烯醛
肉桂(Cinnamomum Cassia)油
乙酯肉桂酯
肉桂醇
柠檬醛
香茅(Cymbopogon Nardus)油
香茅醛
香茅醇
香茅醇乙酸酯
香紫苏(Salvia Sclarea)油
丁子香(Eugenia Caryophyllus)油
丁子香叶(Eugenia Caryophyllus)油
芫荽(Coriandrum Sativum)油
香豆素
枯茗(Cuminum Cyminum)提取物
仙客来醛
地中海柏木(Cupressus Sempervirens)油
苯并二氢吡喃酮
二氢茉莉酮酸酯
二羟吲哚
十三烷二酸二甲基酯
2,4-二甲基-3-环己烯羧醛
二甲基六氢萘基二羟基甲基缩醛
二甲基八氢-2-萘醛
2,6-二甲基-7-辛烯-2-醇
二聚戊烯
犬蔷薇(Rosa Canina)枳子油
苯甲酸乙酯
环己基丙酸乙基酯
乙基烷羧酰胺
乙基苯乙基缩醛
苯基乙酸乙酯
乙基香兰素
桉油醇
柠檬桉油
蓝桉树油
丁子香酚
金合欢醇
乙酸金合欢基酯
茴香(Foeniculum Vulgare)油
糠醛
古蓬香(Ferula Galbaniflua)油
栀子油
香叶醇
老鹳草(Geranium Maculatum)油
乙酸香叶酯
姜(Zingiber Officinale)油
葡糖酸内酯
柚子(Citrus Grandis)油
天芥菜精
2-庚基环戊酮
3-己烯醇
律草烷
律草烯
羟基香茅醛
刺戴尔(Dalea Spinosa)油
乙酸异戊酯
异丁基甲基四氢吡喃醇
异戊基环己酮
苯甲酸异丙酯
异丙基苯基丁醛
茉莉花(Jasminum Officinale)油
欧洲刺柏油
刺柏焦油
铅笔柏油
月桂树(Laurus Nobilis)油
杂熏衣草(Lavandula Hybrida)油
熏衣草(Lavandula Angustifolia)油
柠檬(Citrus Medica Limonum)油
柠檬香草(Cymbopogon Schoenanthus)油
Lesquerella fendleri油
酸柠檬(Citrus Aurantifolia)油
乙酸里哪醇酯
心叶椴(Tilia Cordata)油
圆叶当归(Levisticum Officinale)油
蜜柑(Citrus Nobilis)油
马索桂皮油
母菊(Chamomilla Recutita)油
对烷-7-醇
醇
烷氧基丙二醇
基乙酸酯,乳酸酯,或水杨酸酯
甲氧基二氢化茚
对-甲基乙酰苯
6-甲基香豆素
甲基二异丙基丙酰胺
3-甲基间二羟苯甲酸甲基酯
摩洛哥春黄菊油
麝香酮
麝香蔷薇(Rosa Moschata)油
没药树(Commiphora Myrrha)香脂
没药树(Commiphora Myrrha)油
桃金娘(Myrtus Communis)油
挪威云杉(Picea Excelsa)油
肉豆蔻(Myristica Fragrans)油
栎扁枝衣(Evernia Prunastri)提取物
乳香
乳香(Boswellia Carterii)提取物
乳香(Boswellia Serrata)提取物
桔子(Citrus Aurantium Dulcis)提取物
桔子(Citrus Aurantium Dulcis)花提取物
桔子(Citrus Aurantium Dulcis)花油
桔子(Citrus Aurantium Dulcis)花水
桔子(Citrus Aurantium Dulcis)油
桔子(Citrus Aurantium Dulcis)皮提取物
鸢尾(IrisFlorentina)提取物
香根鸢尾(Iris Pallida)提取物
玫瑰草(Cymbopogon Martini)油
欧芹(Carum Petroselinum)种子油
广藿香(Pogostemon Cablin)油
天竺葵(Pelargonium Graveolens)油
薄荷油(Mentha Pulegium)油
十五烷酸内酯(Pentadecalactone)
辣薄荷(Mentha Piperita)提取物
辣薄荷(Mentha Piperita)油
乙酸苯基乙基酯
苯乙醇
苯氧基乙醇
苯甲酸苯酯
松树(Pinus Palustris)油
松树(Pinus Palustris)煤焦油
阿月浑子(Pistacia Vera)果仁油
苯甲酸丙酯
迷迭香(Rosmarinus Officinalis)油
玫瑰油
红木(Aniba Rosaedora)油
圆丹参(Salvia Officinalis)油
檀香(Santalum Album)油
美洲擦树油
欧洲冷杉(Abies Pectinata)油
马郁兰(Origanum Maiorana)油
香堇菜(Viola Odorata)油
茶树(Melaleuca Alternifolia)油
萜品醇
萜品醇乙酸酯
四甲基环戊烯丁烯醇
麝香草(Thymus Vulgaris)油
麝香草酚
γ-十一烷酸内酯
香子兰(Vanilla Planifolia)
香子兰(Vanilla Tahitensis)
香草醛
岩兰草(Vetiveria Zizanoides)油
蓍草(Achillea Millefolium)油
衣兰香精(Cananga Odorata)油。
在本发明的附加实施方案中,驱虫活性成分化合物被引入制品中以产生昆虫/节肢动物驱除效果。在本实施方案中考虑的制品包括制成品,其中包括纺织品如衣服,户外或军事装备如蚊帐,天然产品如木材,或昆虫易损坏植物的叶子。
在本发明的另一个实施方案中,这里所述的活性成分被引入到制品中以产生令人喜欢的香味,或施用于物体表面上以赋予香味。施用的具体方式将取决于所述的表面和为了赋予所需要的香味强度而需要的浓度。在这些实施方案之内考虑的制品包括制成品,其中包括纺织品,空气清新剂,蜡烛,各种带香味的制品,纤维,片材,纸,漆,油墨,粘土,木材,家具(例如庭院和甲板),地毯,卫生用品,塑料,聚合物,等等。壁虱/昆虫驱除性也因为在这些制品内存在了这里所述的活性成分化合物而被赋予这些制品。
在这里描述的化合物与其它组分(如上所述)一起被掺混在组合物中,其用量对于具体目的的应用是有效的,如昆虫/节肢动物驱除剂、香料或其它皮肤处理剂。在组合物中所含的活性化合物的量一般不超过最终产物重量的约80wt%,然而,在某些应用中可以使用更大量,并且这一用量没有限制。更优选,化合物的合适量将是至少约0.001%(按重量)和优选约0.01%至约50%按重量;和更优选,约0.01wt%到约20%wt%,基于总组合物或制品的总重量。具体的组成将取决于预期的用途。
一种或多种载体,助剂和/或添加剂的所配制混合物可以选自在以上所列的表中包含的各个组的那些成员。它们也可以选自于通过从以上列表中列出的整个组中省去任何一个或多个成员所形成的前述列表中的成员小组。结果,载体,助剂和/或添加剂的混合物在此类情况下不仅从一个或多个成员(它选自于由以上列表给出的整个组中的各个成员的全部各种不同组合所形成的任何大小的任何小组)制成,而且也可以在已经从整个组中省去而形成小组的那些成员不存在的情况下制成。另外,通过从以上列表中的整个组中省去各种成员所形成的小组可以是整个组的各个成员,使得在除所选择的单个成员之外的该整个组的全部其它成员不存在的情况下提供载体、助剂和/或添加剂。
本发明提供的组合物的其它用途或配方已公开在US2003/062,357;US2003/079,786;和US2003/191,047,这些文献中的每一个以其全部内容被引入作为本申请的一部分。
本发明进一步在下列特定的实施方案中叙述但不限于它们,这些实施方案举例说明引入了如上所述的驱虫活性成分,以及如上所述的某些助剂、改性剂和/或添加剂的各种配制剂的制造。
一般程序
与活性成分和配制剂的制备有关的全部反应和操作是在标准实验室通风橱中在标准实验室玻璃器皿中进行的。配制剂浓度被报道为重量/重量百分数。驱虫活性成分的分析是通过GC/MS分析来进行,并且浓度是相对于作为内标物的1,2-二溴苯来报道的。
实施例1,15%w/w活性成分洗液
将驱虫活性成分引入到表1中所示的油-水乳液配制剂中。在A和B相中的成分单独在75℃下掺混,然后两相通过混合均匀来进行掺混。A和B两相的所得混合物被冷却至40℃。然后在快速混合搅拌下经过30分钟缓慢地添加C相(活性成分)。最终,添加防腐剂(D相),和最终的乳液然后被冷却至室温,在此温度下贮存它们。
表1.实施例1洗液配制剂的成分
相 | 成分 | 功能 | INCI命名 | 供应商 | %(重量) |
A | 水 | 稀释剂 | 水(Aqua) | 58.35 | |
A | Na2EDTA | 螯合剂 | 二钠EDTA | Akzo | 0.05 |
A | Jeechem Bugl | 湿润剂 | 丁二醇 | Jeen Int′l | 2.5 |
A | MP二醇 | 湿润剂 | 甲基丙二醇 | Lyondell | 1.5 |
A | 甘油96% | 湿润剂 | 甘油 | Cognis | |
B | Crodacol C S50 | 乳液稳定剂 | 十六烷基十八烷基醇 | Croda | |
B | Brij721 | 乳化剂 | 硬脂基聚氧乙烯醚(Steareth)-21 | Uniqema | 0.5 |
B | Jeechem Op | 润肤剂 | 棕榈酸乙基己基酯 | Jeen Int′l | 5 |
B | Ceraphyl41 | 润肤剂 | 乳酸C12-15烷基酯 | ISP Sutton | 3 |
B | 多元醇预聚物14 | 成膜剂 | PEG-51/Smdi共聚物 | Barnet | 5 |
B | Finsolv TN | 润肤剂 | 苯甲酸C12-15烷基酯 | Finetex | 3 |
B | Cerasynt Q | 乳化剂 | 硬脂酸甘油基酯SE | Isp | 2.5 |
B | Emulsiphos S | 乳化剂 | 十六烷基磷酸钾氢化棕榈酸甘油酯 | Symrise | 1 |
B | Rapithix A60 | 增稠剂 | 聚丙烯酸钠氢化聚癸烯十三烷基聚氧乙烯醚(Trideceth-6) | ISP | 1.6 |
C | 驱虫活性剂 | 驱虫剂 | DuPont | 15 | |
D | Germazide PMP | 防腐剂 | 苯氧基乙醇氯酚醚对羟基苯甲酸甲酯羟苯丙酯 | 1 |
实施例2,15%w/w活性成分洗液
将驱虫活性成分引入到表2中所示的油-水乳液配制剂中。在A和B相中的成分单独在75℃下掺混,然后两相通过混合均匀来进行掺混。A和B两相的所得混合物被冷却至40℃。然后在快速混合搅拌下经过30分钟缓慢地添加C相(活性成分)。最终,添加防腐剂(D相),和最终的乳液然后被冷却至室温,在此温度下贮存它们。
表2.洗液实施例2配制剂的成分
相 成分 功能 INCI命名 供应商 %(重量)(商品名) |
A 水 稀释剂 水(Aqua) 49.65A Na2EDTA 螯合剂 EDTA二钠 Akzo 0.05A Jeechem Bugl 湿润剂 丁二醇 Jeen Int′l 5A MP Diol 湿润剂 甲基丙二醇 Lyondell 1.5A 甘油96% 湿润剂 甘油 CognisB Crodacol C S50 乳液稳 十六烷基十八烷基醇 Croda定剂B Brij721 乳化剂 硬脂基聚氧乙烯醚 Uniqema 0.7(Steareth)-21B Jeechem Op 润肤剂 棕榈酸乙基己基酯 Jeen Int′l 5B Ceraphyl41 润肤剂 乳酸C12-15烷基酯 ISP Sutton 3B 多元醇预聚物14 成膜剂 PEG-51/Smdi共聚物 Barnet 5B Finsolv TN 润肤剂 苯甲酸C12-15烷基酯 Finetex 5B CerasyntQ 乳化剂 硬脂酸甘油基酯 SEIsp 2.5B Emulsiphos S 乳化剂 十六烷基磷酸钾 Symrise 4氢化棕榈酸甘油酯B Rapithix A60 增稠剂 聚丙烯酸钠 ISP 1.6氢化聚癸烯十三烷基聚氧乙烯醚(Trideceth-6)C 驱虫活性剂 驱虫剂 DuPont 15D Germazide PMP 防腐剂 苯氧基乙醇 1氯酚醚对羟基苯甲酸甲酯羟苯丙酯 |
实施例3,15%w/w活性成分洗液
将驱虫活性成分引入到表3中所示的油-水乳液配制剂中。在A和B相中的成分单独在75℃下掺混,然后两相通过混合均匀来进行掺混。A和B两相的所得混合物被冷却至40℃。然后在快速混合搅拌下经过30分钟缓慢地添加C相(活性成分)。最终,添加防腐剂(D相),和最终的乳液然后被冷却至室温,在此温度下贮存它们。
表3.洗液实施例3配制剂的成分
相 成分 功能 INCI命名 供应商 %(重量)(商品名) |
A 水 稀释剂 水(Aqua) 43.15A Na2EDTA 螯合剂 EDTA二钠 Akzo 0.05A Jeechem Bugl 湿润剂 丁二醇 Jeen Int′l 3A MP Diol 湿润剂 甲基丙二醇 LyondellA Glycerin96% 湿润剂 甘油 Cognis 10B Crodacol C S50 乳液稳定剂 十六烷基十八烷基醇 Croda 1B Brij721 乳化剂 硬脂基聚氧乙烯醚 Uniqema 0.7(Steareth)-21B Jeechem Op 润肤剂 棕榈酸乙基己基酯 Jeen Int′l 5B Ceraphyl41 润肤剂 乳酸C12-15烷基酯 ISP Sutton 3B 多元醇预聚物 成膜剂 PEG-51/Smdi共聚物 Barnet 514B Finsolv TN 润肤剂 苯甲酸C12-15烷基酯 Finetex 5B Cerasynt Q 乳化剂 硬脂酸甘油基酯 SEIsp 2.5B Emulsiphos S 乳化剂 十六烷基磷酸钾 Symrise 4氢化棕榈酸甘油酯B Rapithix A60 增稠剂 聚丙烯酸钠ISP 1.6氢化聚癸烯十三烷基聚氧乙烯醚(Trideceth-6)C 驱虫活性剂 驱虫剂 DuPont 15D Germazide PMP 防腐剂 苯氧基乙醇 1氯酚醚对羟基苯甲酸甲酯对羟基苯甲酸丙酯 |
实施例4,15%w/w活性剂的醇基溶液
将驱虫活性成分引入液体醇溶液中,随后一次一个地添加在表4中所列的其它成分。在每次添加后,在添加下一种成分之前让溶液变均匀。
表4.液体实施例4配制剂的成分
成分 功能(商品名) INCI命名 供应商 %(重量) |
SD醇402 稀释剂200Proof SD醇40 Equastar 57.00驱虫活性剂 驱虫剂 DuPont 15.00Zenicone XX 润肤剂 PEG-8 聚二甲基硅氧烷PEG-8 蓖麻醇酸酯 Zenitech 500Jeesilc CPS312 润肤剂 环戊硅氧烷 Jeen Int′l 1500多元醇预聚物15 成膜剂 PEG-8/SMDI共聚物 Barnet 3.00Eutanol G 润肤剂 辛基十二烷醇 Cognis 5.00 |
实施例5,15%w/w活性剂的醇基溶液
将驱虫活性成分引入液体醇溶液中,随后一次一个地添加在表5中所列的其它成分。在每次添加后,在添加下一种成分之前让溶液变均匀。
表5.液体实施例5配制剂的成分
成分(商品名) | 功能 | INCI命名 | 供应商 | %(重量) |
SD醇402200Proof | 稀释剂 | SD醇40 | Equastar | 42.00 |
驱虫活性剂 | 驱虫剂 | DuPont | 1500 | |
Jeechem Bugl | 湿润剂 | 丁二醇 | Jeen Int′l | 5.00 |
MP二醇 | 湿润剂 | 甲基丙二醇 | Lyondell | 500 |
丙二醇 | 湿润剂 | 丙二醇 | Arco | 500 |
Zenicone XX | 润肤剂 | PEG-8聚二甲基硅氧烷PEG-8蓖麻醇酸酯 | Zenitech | 500 |
Jeesilc CPS312 | 润肤剂 | 环戊硅氧烷 | Jeen Int′l | 15.00 |
Polyolprepolymer15 | 成膜剂 | Peg-8/Smdi共聚物 | Barnet | 300 |
Eutanol G | 润肤剂 | 辛基十二烷醇 | Cognis | 5.00 |
实施例6,15%w/w活性剂的醇基溶液
将驱虫活性成分引入液体醇溶液中,随后一次一个地添加在表6中所列的其它成分。在每次添加后,在添加下一种成分之前让溶液变均匀。表6.液体实施例6配制剂的成分
与如上所述的那些类似的配制剂对于受试验的人测试在野外和在实验室的网笼(arm-in-cage)试验中针对蚊子的驱虫功效;并在野外试验中测试针对蚋的驱虫功效。全部试验结果表明,该配制剂提供了令人想望地高水平的驱虫保护作用。
这里的配制组合物可以包括在以上公开的总组中的不同类型的化妆品助剂,改性剂和添加剂中的任何一种或多种或全部。然而,该助剂,改性剂和添加剂也可以是在这里公开的助剂、改性剂和添加剂的总组的一个小组中的任何一种或多种的这些成员,其中该小组是通过从总组中排除任何一种或多种其它成员所形成的。结果,在此情况下助剂、改性剂和添加剂不仅是在任何大小的任何小组(它选自该总组,按照总组的各个成员的全部各种不同组合)中的任何一种或多种的助剂、改性剂和添加剂,而且在任何小组中的成员因此可以在总组的一个或多个成员(已经被排除而形成小组)不存在的情况下使用。通过从助剂、改性剂和添加剂的总组中排除各成员所形成的该小组另外可以是该总组的各个成员,使得该助剂、改性剂或添加剂是在排除所选择各成员之后的总组的全部其它成员不存在的情况下使用。
对于具体的化妆品助剂,改性剂或添加剂,这里的配制组合物可以包括在如上所述可提供该助剂、改性剂或添加剂的所需性能或功能的总组中的不同类型材料中的任何一种或多种或全部。然而,该材料也可以是在这里对于具体助剂、改性剂或添加剂所公开的材料总组的一个小组的那些成员中的任何一种或多种,其中该小组是通过从总组中排除任何一种或多种其它成员所形成的。结果,在此情况下这些材料不仅是在任何大小的任何小组(它选自该总组,按照总组的各个成员的全部各种不同组合)中的任何一种或多种的助剂/改性剂/添加剂材料,而且在任何小组中的成员因此可以在总组的一个或多个成员(已经被排除而形成小组)不存在的情况下使用。通过从材料总组中排除各成员所形成的该小组另外可以是该总组的各个成员,使得该助剂/改性剂/添加剂是在排除所选择各成员之后的总组的全部其它成员不存在的情况下使用。
本发明的某些特征已描述在实施方案的叙述内容中,该实施方案将各种此类特征结合在一起,不论描述在本公开物中或在一个实施例中。然而,本发明的范围不限于在任何具体实施方案中的仅仅某些特征的叙述,而且本发明还包括(1)比任何所述实施方案的全部特征更少的子组合,该子组合体现特征于所省去特征的不存在而形成子组合;(2)每一个特征分别地包括在所述实施方案的组合中;和(3)从所述实施方案的一个或多个或全部特征与本文其它地方公开的其它特征一起形成的其它特征组合。
在本说明书中,除非另外明确地声称或由使用背景有相反指示,否则,当本发明的实施方案被声称或描述为包括(comprising),包括(including),含有(containing),具有(having),某些特征或要素,由某些特征或要素组成或构成,除了明确声称或描述的这些之外的一个或多个特征或要素可以存在于实施方案中。然而,本发明的备选实施方案可以声称或描述为主要由某些特征或要素组成,在该实施方案中显著地改变实施方案的操作原理或区别特征的特征或要素在其中不存在。本发明的的附加备选实施方案可以声称或被描述为由某些特征或要素组成,在该实施方案中或在该实施方案的无实质变化的形式中,只有具体地声称或描述的特征或要素存在。
Claims (12)
1.一种配制的驱除昆虫组合物,包括:
(a)49.65wt%的水;
(b)15wt%的二氢荆芥内酯或二氢荆芥内酯的立体异构体混合物;
(c)0.05wt%的乙二胺四乙酸二钠;
组分(d),其包括5wt%的1,3-丁二醇和1.5wt%的甲基丙二醇的混合物;
组分(e),其包括下列物质的混合物:(I)0.7wt%的Steareth-21、(II)2.5wt%的硬脂酸甘油酯SE,和(III)4wt%的具有与Emulsiphos相同组成的十六烷基磷酸钾和氢化棕榈酸甘油酯的混合物;
组分(f),其包括5wt%的棕榈酸乙基己基酯和3wt%的乳酸C12-15烷基酯的混合物;
(g)5wt%的PEG-51/Smdi共聚物;
(h)1.6wt%的具有与Rapithix A-60相同组成的聚丙烯酸钠、氢化聚癸烯和Trideceth-6的混合物;
(i)1wt%的具有与Germazide PMP相同组成的苯氧基乙醇、氯酚醚、对羟基苯甲酸甲酯和对羟基苯甲酸丙酯的混合物;和
(j)5wt%的苯甲酸C12-15烷基酯。
2.一种配制的驱除昆虫组合物,包括:
(a)58.35wt%的水;
(b)15wt%的二氢荆芥内酯或二氢荆芥内酯的立体异构体混合物;
(c)0.05wt%的乙二胺四乙酸二钠;
组分(d),其包括2.5wt%的1,3-丁二醇和1.5wt%的甲基丙二醇的混合物;
组分(e),其包括下列物质的混合物:(I)0.5wt%的Steareth-21、(II)2.5wt%的硬脂酸甘油酯SE,和(III)1wt%的具有与Emulsiphos相同组成的十六烷基磷酸钾和氢化棕榈酸甘油酯的混合物;
组分(f),其包括5wt%的棕榈酸乙基己基酯和3wt%的乳酸C12-15烷基酯的混合物;
(g)5wt%的PEG-51/Smdi共聚物;
(h)1.6wt%的具有与Rapithix A-60相同组成的聚丙烯酸钠、氢化聚癸烯和Trideceth-6的混合物;
(i)1wt%的具有与Germazide PMP相同组成的苯氧基乙醇、氯酚醚、对羟基苯甲酸甲酯和对羟基苯甲酸丙酯的混合物;和
(j)3wt%的苯甲酸C12-15烷基酯。
3.一种配制的驱除昆虫组合物,包括:
(a)43.15wt%水;
(b)15wt%二氢荆芥内酯或二氢荆芥内酯的立体异构体混合物;
(c)0.05wt%的乙二胺四乙酸二钠;
组分(d),其包括3wt%的1,3-丁二醇和10wt%的甘油96%的混合物;
(e)1wt%的十六烷基十八烷基醇;
组分(f),其包括下列物质的混合物:(I)0.7wt%的Steareth-21、(II)2.5wt%的硬脂酸甘油酯SE,和(III)4wt%的具有与Emulsiphos相同组成的十六烷基磷酸钾和氢化棕榈酸甘油酯的混合物;
组分(g),其包括5wt%的棕榈酸乙基己基酯、3wt%的乳酸C12-15烷基酯和5wt%的苯甲酸C12-15烷基酯的混合物;
(h)5wt%的PEG-51/Smdi共聚物;
(i)1.6wt%的具有与Rapithix A-60相同组成的聚丙烯酸钠、氢化聚癸烯和Trideceth-6的混合物;和
(j)1wt%的具有与Germazide PMP相同组成的苯氧基乙醇、氯酚醚、对羟基苯甲酸甲酯和对羟基苯甲酸丙酯的混合物。
4.一种配制的驱除昆虫组合物,包括:
(a)57wt%的SD乙醇40 2 200 Proof;
(b)15wt%的二氢荆芥内酯或二氢荆芥内酯的立体异构体混合物;
组分(c),其包括(I)5wt%的具有与Zenicone XX相同组成的PEG-8聚二甲基硅氧烷和PEG-8蓖麻醇酸酯、(II)15wt%的环戊硅氧烷和(hI)5wt%的辛基十二烷醇的混合物;和
(d)3wt%的PEG-8/Smdi共聚物。
5.一种配制的驱除昆虫组合物,包括:
(a)42wt%的SD乙醇40 2 200 Proof;
(b)15wt%的二氢荆芥内酯或二氢荆芥内酯的立体异构体混合物;
组分(c),其包括5wt%的1,3-丁二醇、5wt%的甲基丙二醇和5wt%的丙二醇的混合物;
组分(d),其包括(I)5wt%的具有与Zenicone XX相同组成的PEG-8聚二甲基硅氧烷和PEG-8蓖麻醇酸酯、(II)15wt%的环戊硅氧烷和(III)5wt%的辛基十二烷醇的混合物;和
(e)3wt%的PEG-8/Smdi共聚物。
6.一种配制的驱除昆虫组合物,包括:
(a)37wt%的SD乙醇40 2 200 Proof;
(b)15wt%的二氢荆芥内酯或二氢荆芥内酯的立体异构体混合物;
组分(c),其包括15wt%的1,3-丁二醇、5wt%的甲基丙二醇和10wt%的甘油96%的混合物;
组分(d),其包括(I)5wt%的具有与Zenicone XX相同组成的PEG-8聚二甲基硅氧烷和PEG-8蓖麻醇酸酯、(II)5wt%的环戊硅氧烷和(III)5wt%的辛基十二烷醇的混合物;和
组分(e),其包括3wt%的PEG-8/Smdi共聚物。
7.驱除一种或多种壁虱或昆虫的方法,该方法包括让壁虱和/或昆虫接触到根据权利要求1-6中任一项的组合物。
8.根据权利要求7的方法,该方法包括将根据权利要求1或2的组合物施加于壁虱和/或昆虫的宿主的表面上。
9.根据权利要求7的方法,该方法包括将根据权利要求3的组合物施加于壁虱和/或昆虫的宿主的表面上。
10.根据权利要求7的方法,该方法包括将根据权利要求4的组合物施加于壁虱和/或昆虫的宿主的表面上。
11.根据权利要求7的方法,该方法包括将根据权利要求5的组合物施加于壁虱和/或昆虫的宿主的表面上。
12.根据权利要求7的方法,该方法包括将根据权利要求6的组合物施加于壁虱和/或昆虫的宿主的表面上。
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CA2648270A1 (en) | 2007-11-22 |
HK1132627A1 (zh) | 2010-03-05 |
US20070264297A1 (en) | 2007-11-15 |
CN101442908A (zh) | 2009-05-27 |
US8771718B2 (en) | 2014-07-08 |
WO2007133683A2 (en) | 2007-11-22 |
EP2040555A2 (en) | 2009-04-01 |
BRPI0710434A2 (pt) | 2011-08-09 |
WO2007133683A3 (en) | 2008-11-27 |
CA2648270C (en) | 2014-07-08 |
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