TW201733567A - 包括親脂性組成物的水性配方 - Google Patents

包括親脂性組成物的水性配方 Download PDF

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TW201733567A
TW201733567A TW106100369A TW106100369A TW201733567A TW 201733567 A TW201733567 A TW 201733567A TW 106100369 A TW106100369 A TW 106100369A TW 106100369 A TW106100369 A TW 106100369A TW 201733567 A TW201733567 A TW 201733567A
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weight
aqueous formulation
lipophilic composition
formulation according
mixture
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TW106100369A
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尼可拉斯 維達爾
尚法蘭索瓦 勒斯加爾達斯
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長榮置地有限公司
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    • 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
    • A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
    • A01N25/02—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
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    • A61K36/185—Magnoliopsida (dicotyledons)
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    • A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
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Abstract

本發明涉及一種包含0.1重量%與50重量%之間的親脂性組成物的水性配方，所述配方進一步包含： - 0.1重量%與10重量%之間的包含至少微晶纖維素的均質組分； - 0.01重量%與2重量%之間的黏土； - 在水中的剩餘物。

Description

包括親脂性組成物的水性配方
本發明涉及一種包含0.1重量%與50重量%之間的親脂性組成物，例如精油或精油混合物的水性配方。
本發明特別適用於化妝品及/或藥物用途的水性配方，因此親脂性組成物(例如精油或精油混合物)具有對應於所尋求的化妝品及/或藥物效果的特性，例如對有害動物的驅避功能、治療及/或預防功能，例如意欲減輕有害動物的叮咬或咬傷的舒緩功能、抗紅腫功能、癒合功能、鬆弛功能或消炎功能，或健康功能，諸如加香功能、除臭功能、殺生物功能、殺菌功能或殺真菌功能。
此類配方大體意欲藉由直接施用於受試者的皮膚，或間接地施用在空氣中或在其他表面上，例如藉由霧化器、球施加器或其他施用模式來使用。
由於水及親脂性組成物是不混溶的液體，已知使用乳化劑，特別是合成的乳化劑用於提供其混合物的穩定性，當親脂性組成物濃度高時更是如此。
然而，該等乳化劑的合成性質造成了問題，特別是在所述配方的化妝品及/或藥物用途的情境中。實際上，該等乳化劑在配方中的存在可能改變親脂性組成物的特性，特別是加香特性，但亦會在某些受試者中引起不良皮膚反應，特別是刺激或過敏。
為了克服該等缺點，從文件JP-S55/162710中已知一種用於化妝品用途的水性配方，其包含水及高濃度(高達85重量%)的一或多個油，以及特別包含微晶纖維素的均質混合物，視情況補充有例如基於羧甲基纖維素的水溶性聚合物，以便儘可能地限制合成乳化劑的使用。
然而，此種配方不能完全令人滿意，因為其不能使水-油混合物完全穩定。因此，此種配方可能在一定時間長度之後在水與油之間表現出相分離，此可能導致由所述一或多個油形成的活性元素在所述配方的容器內及/或在施用所述配方的受試者身體的一部分上分佈的問題，並因此損害所述配方的功效。
為了改善包含高濃度的一或多個油的水性配方的特別是時間穩定性，文件FR-2 974 312提出將纖維素奈米晶體添加到此種的配方中，但是此方案證明實施起來相對複雜。
此外，從文件EP-1 699 429中已知用於化妝品用途的水性配方，其包含水及基於一或多個加香油，特別是一或多個精油的高濃度(至少30重量%)親脂性組成物，以及少量(0.1重量%與4重量%之間)的纖維素衍生物，特別是羧甲基纖維素，及/或黏土，特別是膨潤土。
然而，在此文件中，添加膨潤土及/或纖維素衍生物主要目的在於增稠配方，而水性配方的穩定是藉由添加乳化劑來獲得的。此外，增稠劑的量使得配方難以施用，特別是藉由霧化器施用。
本發明意欲藉由特別提出一種包含水及高濃度親脂性組成物的水性配方來改進現有技術，其中水及親脂性組成物的混合物具有隨時間改善的均勻性及穩定性，同時易於施用，特別是藉由霧化器或球施加器，施用到受試者的皮膚，所述配方亦易於製造。
為此，本發明提出一種包含0.1重量%與50重量%之間的親脂性組成物的水性配方，所述配方亦包含：
- 0.1重量%與10重量%之間的包含至少微晶纖維素的均質組分；
- 0.01重量%與2重量%之間的黏土；
- 在水中的剩餘物。
本發明的其他特徵及優點將在以下對各個特定實施方案的描述中出現。
本發明涉及一種包含0.1重量%與50重量%之間的親脂性組成物的配方，所述親脂性組成物特別包含至少一種油，並且更特別地包含精油或精油混合物。具體地說，本發明涉及一種包含高濃度，特別是大於20重量%的親脂性組成物的配方。
本發明特別適用於化妝品及/或藥物用途的水性配方，因此親脂性組成物具有對應於所尋求的化妝品及/或藥物效果的特性。
具體地說，親脂性組成物可以對有害動物具有驅避功能。為此，親脂性組成物可例如包含對-薄荷烷-3,8-二醇(PMD)，其是特別有效地阻止刺痛或刺激諸如蚊子或蜱的吸血昆蟲的天然成分。根據一個實施方案，在親脂性組成物中存在至少10重量%，並且特別是大於40重量%的PMD。
例如，親脂性組成物可包含衍生自檸檬味的桉樹或香茅油的精油，諸如以商標Citrepel®及Citriodiol®銷售的精油，此類油構成對-薄荷烷-3,8-二醇的已知天然來源。
親脂性組成物亦可以具有其他功能，特別是治療及/或預防功能，諸如意欲減輕有害動物的叮咬或咬傷的舒緩功能、抗紅腫、癒合、鬆弛或消炎功能，或健康功能，諸如加香、除臭、殺生物、殺菌或殺真菌功能。
水性配方亦包含0.1重量%與10重量%之間，並且特別是0.1重量%與2重量%之間的包含至少微晶纖維素的均質組分，以便改善親脂性組成物在水中的分佈。
具體地說，微晶纖維素是天然來源的成分，特別是來自木材的成分，其在宏觀上被組織叢集。此外，其不溶於水，並且當其被添加到水性配方中時藉由在水與親脂性組成物之間產生固體-固體鍵而形成凝膠。
根據一個實施方案，均質組分亦包含羧甲基纖維素、黃原膠或該等化合物的混合物，黃原膠尤其具有增稠及膠凝特性。具體地說，當製造均質組分時，微晶纖維素可以與羧甲基纖維素及/或黃原膠共同處理。
特別有利地，均質組分包含微晶纖維素與羧甲基纖維素及/或黃原膠的混合物，所述混合物特別包含75重量%與95重量%之間的微晶纖維素及5重量%與25重量%之間的羧甲基纖維素及/或黃原膠。
此外，水性配方包含0.01重量%與2重量%之間，特別是小於1重量%，並且更特別是小於0.5重量%的黏土，以便隨時間穩定水及親脂性組成物的混合物，並且因此防止相分離以及由此可能產生的親脂性組成物的均勻性及分佈的問題，特別是在將所述配方施用於受試者皮膚期間。此外，少量的黏土允許限制配方的增稠，並且因此促進其施用，特別是藉由標準霧化器或球施用器的施用。
具體地說，黏土可以包括蒙皂石，特別是藉由包括膨潤土，或其他黏土類，諸如高嶺石、伊利石、綠泥石、蛭石、海泡石或綠坡縷石。黏土可以有利地包含純度接近100質量%，並且含有小於10重量%的總結晶二氧化矽的膨潤土。
水性配方亦可以包含其他成分，特別是為了在其上賦予另外的特性。
因此水性配方可以包含0.1重量%與50重量%之間，特別是5重量%與20重量%之間的加香組成物。具體地說，加香組成物可以包含精油或精油混合物，或特別地從精油中提取的其他成分(諸如酯或萜烯)。
例如，加香組成物可基於Iceberg 57656®或RS57656®。
此外，所述配方亦可以包含：
- 小於20重量%的防腐劑，例如0.4重量%與5重量%之間的量的天然來源的苯乙醇；
- 小於10重量%的抗氧化劑，例如小於1重量%的量的維生素E；
- 小於2重量%的pH調整劑，特別是基於檸檬酸，用於在3與7之間，優選接近皮膚的pH的範圍內調節所述配方的pH；
- 3重量%與50重量%之間，特別是小於10重量%的一或多個溶劑，所述一或多個溶劑與親脂性組分或表面活性劑不可同化，並且特別選自醇、酸及/或酸式鹽。具體地說，一或多個溶劑可以選自乙醇、異丙醇、亞甲基二醇、乙二醇、丙二醇、甘油、丁二醇、戊醇、異戊二醇、己醇、己二醇以及苯二醇。
最後，無論水性配方的組成如何，特別是關於親脂性組成物、均質混合物、黏土以及其他可能成分的量，所述配方的其餘部分為100%是水，特別是軟化水。
具體地說，可以根據提供以下步驟的簡單方法來製備水性配方：
- 將親脂性組成物、均質組分、最終加香的黏土、防腐劑、抗氧化劑及/或pH調整劑混合；
- 機械攪拌所述混合物，特別是借助於以3000 rpm的速度運行的轉子-定子，持續約10分鐘的一段時間；
- 將獲得的配方靜置10與30分鐘之間的一段時間。
此外，若要獲得的水性配方亦包含溶劑，則製造方法可以在上述靜置之後提供以下補充步驟：
- 將所述溶劑添加到所述配方中；並且
- 機械攪拌所述配方，特別是借助於以3000 rpm的速度運行的轉子-定子，持續約5分鐘的一段時間。
實施例
在實驗室中進行的試驗程式期間，特別是根據上述方法製備九個水性配方樣品，並且所述樣品全部包含軟化水，以及：
- 26重量%的Citrepel®類型的檸檬味的桉樹精油；
- 13重量%的Iceberg 57656®類型的加香組成物；
- 3.5重量%的甘油；
- 0.25重量%的維生素E，以商標Bioxan®銷售；
- 高達0.02重量%的檸檬酸。
此外，該等樣品各自包含：
- 對於樣品1，對應於本發明提出的配方的試驗樣品；
○ 樣品1a：1重量%的微晶纖維素及0.2重量%的膨潤土；
○ 樣品1b：基於微晶纖維素與羧甲基纖維素共處理的1重量%的均質混合物及0.2重量%的膨潤土，所述均質混合物包含約85重量%的微晶纖維素及約15重量%的羧甲基纖維素；
- 對於樣品2：0.2重量%的膨潤土；
- 對於樣品3：基於微晶纖維素及羧甲基纖維素的1重量%的均質混合物；
- 對於樣品4：1重量%的黃原膠及0.2重量%的膨潤土；
- 對於樣品5：1重量%的羧甲基纖維素；
- 對於樣品6：1重量%的羧甲基纖維素及0.2重量%的膨潤土；
- 對於樣品7：基於微晶纖維素及黃原膠的1重量%的均質混合物；
- 對於樣品8：基於微晶纖維素及羧甲基纖維素的11重量%的均質混合物及2.5重量%的膨潤土，所述均質混合物包含約85重量%的微晶纖維素及約15重量%的羧甲基纖維素。
接下來，該九個樣品全部進行功效試驗，以便分別評估其各者隨時間的穩定性，特別是藉由在54℃下相分離試驗24小時，以及藉由霧化分配。
在該等試驗之後，獲得的結果如下：
- 關於相分離試驗，僅試樣1a、1b具有令人滿意的結果；
- 關於藉由霧化分配的試驗，僅試樣1a、1b、2及3具有令人滿意的結果。
因此由於藉由樣品1a、1b獲得的良好結果，該等試驗證明瞭同時添加膨潤土及基於微晶纖維素的均質混合物的功效，並且用適當的量以保證包含高濃度親脂性化合物的水性配方隨時間的穩定性以及良好的霧化分配。
實際上，試驗樣品1a、1b在隨時間的穩定性及霧化分配兩個方面的良好結果顯示微晶纖維素及膨潤土的組合存在在富含親脂性組成物的水性配方中的功效，特別是與由含有1%的羧甲基纖維素，並且特別是不含膨潤土及微晶纖維素的樣品5獲得的結果相比。
此外，由含有對應於本發明的比例(0.2%)的膨潤土但不含微晶纖維素的樣品2獲得的結果顯示，儘管在富含一或多個精油的水性配方中單獨以此類比例存在膨潤土可能在霧化分配方面獲得令人滿意的結果，然而其不足以保證隨時間的良好穩定性，因為此種配方在相分離試驗後，在水與親脂性組成物之間顯示出相對顯著的相分離。
同樣地，由含有對應於本發明的比例(1%)的微晶纖維素及羧甲基纖維素的混合物但不含膨潤土的樣品3獲得的結果顯示，儘管在富含親脂性組成物的水性配方中單獨以此類比例存在所述混合物亦可能像在僅含有膨潤土的樣品2中那樣，在霧化分配方面獲得良好的結果，但其亦不足以保證隨時間的良好穩定性。
此外，與由亦含有0.2%的膨潤土，但1%的均質混合物僅基於羧甲基纖維素的樣品6獲得的結果相比，由含有1%的微晶纖維素/羧甲基纖維素混合物及0.2%的膨潤土的試驗樣品1b獲得的結果顯示以明智選擇的比例添加微晶纖維素的增加的功效，以及在霧化分配及隨時間的穩定性方面增加的功效。
此外，藉由與由樣品6獲得的結果相比，由含有1%的僅基於微晶纖維素的均質混合物及0.2%的膨潤土的試驗樣品1a獲得的結果顯示微晶纖維素及膨潤土的簡單組合的功效，以及明智選擇的比例在霧化分配及隨時間的穩定性兩個方面的功效。
此外，由含有與除微晶纖維素(黃原膠)以外的成分包含的膨潤土的樣品4獲得的結果，以及由含有與除膨潤土(黃原膠)以外的成分包含的微晶纖維素的樣品7獲得的結果顯示，與該等成分中的一種或另一種與其他類型成分的組合存在相比，膨脹土及微晶纖維素的組合存在在隨時間的穩定性及霧化分配兩個方面的增加的功效。
最後，由與試驗樣品1a、1b一樣，含有膨潤土及基於微晶纖維素兩者的均質混合物，但是比例不同並且特別是高於所述樣品比例(基於微晶纖維素的混合物為11%，並且膨潤土為2.5%)的樣品8獲得的結果顯示，在富含親脂性組成物的水性配方中該兩種成分的組合存在本身不足以保證隨時間的良好穩定性，亦不能藉由霧化良好分配，並且該兩種成分必須以明智選擇的比例添加以保證良好的結果。
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Claims (21)

  1. 一種水性配方，其包含0.1重量%與50重量%之間的親脂性組成物，所述配方的特徵在於其亦包含： - 0.1重量%與10重量%之間的包含至少微晶纖維素的均質組分； - 0.01重量%與2重量%之間的黏土； - 在水中的剩餘物。
  2. 如請求項1之水性配方，其特徵在於所述均質組分亦包含羧甲基纖維素、黃原膠或該等化合物的混合物。
  3. 如請求項1或2中任一項所述的水性配方，其特徵在於所述黏土包括蒙皂石，特別是膨潤土。
  4. 如請求項1或2中任一項所述的水性配方，其特徵在於所述黏土包括高嶺石、伊利石、綠泥石、蛭石、海泡石或綠坡縷石。
  5. 如請求項1或2中任一項所述的水性配方，其特徵在於其包含大於20重量%的親脂性組成物。
  6. 如請求項1或2中任一項所述的水性配方，其特徵在於所述親脂性組成物包含至少一種油，特別是精油或精油混合物。
  7. 如請求項1或2中任一項所述的水性配方，其特徵在於所述親脂性組成物對有害動物具有驅避功能。
  8. 如請求項6之水性配方，其特徵在於所述親脂性組成物包含對-薄荷烷-3,8-二醇(PMD)。
  9. 如請求項1或2中任一項所述的水性配方，其特徵在於所述親脂性組成物具有選自以下的至少一種功能：治療及/或預防功能，特別是意欲減輕有害動物的叮咬或咬傷的舒緩功能、抗紅腫、癒合、鬆弛及消炎功能，以及健康功能，特別是加香、除臭、殺生物、殺菌以及殺真菌功能。
  10. 如請求項1或2中任一項所述的水性配方，其特徵在於其包含0.1重量%與2重量%之間的均質組分。
  11. 如請求項1或2中任一項所述的水性配方，其特徵在於所述均質組分包含微晶纖維素及羧甲基纖維素的混合物。
  12. 如請求項1或2中任一項所述的水性配方，其特徵在於其包含小於1重量%，特別是小於0.5重量%的黏土。
  13. 如請求項1或2中任一項所述的水性配方，其特徵在於其包含0.1重量%與50重量%之間，特別是5重量%與20重量%之間的加香組成物。
  14. 如請求項13之水性配方，其特徵在於所述加香組成物包含精油或精油混合物。
  15. 如請求項1或2中任一項所述的水性配方，其特徵在於其亦包含小於20重量%的防腐劑。
  16. 如請求項15之水性配方，其特徵在於所述防腐劑包含天然來源的苯乙醇，特別是以所述配方的0.4重量%與5重量%之間的量。
  17. 如請求項1或2中任一項所述的水性配方，其特徵在於其亦包含小於10重量%的抗氧化劑。
  18. 如請求項17之水性配方，其特徵在於所述抗氧化劑包含維生素E，特別是以所述配方的小於1重量%的量。
  19. 如請求項1或2中任一項所述的水性配方，其特徵在於其亦包含小於2重量%的pH調整劑，特別是基於檸檬酸。
  20. 如請求項1或2中任一項所述的水性配方，其特徵在於其亦包含3重量%與50重量%之間，特別是小於10重量%的一或多個溶劑，特別是選自醇、酸及/或酸式鹽。
  21. 如請求項20之水性配方，其特徵在於所述一或多個溶劑選自乙醇、異丙醇、亞甲基二醇、乙二醇、丙二醇、甘油、丁二醇、戊醇、異戊二醇、己醇、己二醇以及苯二醇。
TW106100369A 2016-01-08 2017-01-06 包括親脂性組成物的水性配方 TW201733567A (zh)

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AR030412A1 (es) * 2000-03-22 2003-08-20 Fmc Corp Proceso novedoso para preparar formulaciones acuosas
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DE10354564B3 (de) * 2003-11-21 2005-07-07 Henkel Kgaa Emulgierte Parfümöle
US20090317437A1 (en) * 2005-12-06 2009-12-24 Albert Mihranyan Cellulose gel formulations
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PL2335675T3 (pl) * 2009-12-10 2015-08-31 Neubourg Skin Care Gmbh & Co Kg Wolne od emulgatorów, stabilizowane polimerem formulacje pianki
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EP2608794A4 (en) * 2010-08-26 2014-01-22 Univ Northeastern METHODS AND COMPOSITIONS FOR THE PREVENTION OR TREATMENT OF OBESITY
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US11090350B2 (en) 2021-08-17
IL249719B (en) 2020-07-30
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AU2016277701B2 (en) 2022-06-23
JP2017160184A (ja) 2017-09-14
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CN107028794A (zh) 2017-08-11
FR3046540B1 (fr) 2018-03-02
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EP3189827B1 (fr) 2018-11-21
CA2953772A1 (fr) 2017-07-08
US20170196925A1 (en) 2017-07-13
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KR20170083489A (ko) 2017-07-18
AU2016277701A1 (en) 2017-07-27

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