TWI433680B - 新化妝品及/或藥學組合物與其應用 - Google Patents
新化妝品及/或藥學組合物與其應用 Download PDFInfo
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Description
本發明係有關於新組合物與使用該等組合物於化妝品及/或應用於醫藥。
文獻曾記載某些化妝品及/或藥學組合物包括新鮮洋蔥,碘鹽,檸檬酸及檸檬汁。這些組合物係特別用作為化妝品以促進毛髮再生,或具有療效於某些適應症,以增進血管新生,刺激膠原蛋白合成及刺激肥大細胞增生與活化,甚至治療某些癌症。於此列舉一些相關文獻,如法國專利申請號第2 875 403號,第2 877 219號,第2 877 224號,第2 877 576號,及第2 877 408號,或瑞士專利申請號第682 217 A號。
本案申請人曾針對適合用於化妝品或人體治療之新組合物進行研究,上述新組合物顯示優異活性與高度穩定性,且不會有文獻中所述的缺點。
因此,本發明之目的係提供新組合物,其特徵在於包括一蔥屬(Allium species
)之萃取物,一橘屬(Citrus species
)之萃取物,及以下之一:-保利藤屬(Paullinia species
)之萃取物及可可屬(Theobroma species
)之萃取物,-或柳屬(Salix species
)之萃取物及硫酸鋅。
上述定義的組合物中,更感人興趣的組合物,其特徵在於包括一蔥屬之水-醇萃取物,一橘屬之水-醇萃取物,及-保利藤屬之水-醇萃取物(原子化或未原子化)及可可屬之水-醇萃取物原子化或未原子化),-或柳屬(原子化或未原子化)之萃取物及硫酸鋅。本發明之上述組合物之中,最感人興趣的組合物,包括65%至93%之蔥屬水-醇粹取物,5%至33%之橘屬水-醇萃取物,0.25%至2.5%之保利藤屬水-醇萃取物(原子化或未原子化),以及0.25%至2.5%之可可屬水-醇萃取物(原子化或未原子化),特別是包括65%至93%之洋蔥(Allium cepa
,)水-醇萃取物,5%至33%之檸檬(Citrus lemon
)水-醇萃取物,0.25%至2.5%保利藤屬水-醇萃取物(原子化或未原子化),以及0.25%至2.5%之可可屬水-醇萃取物(原子化或未原子化)。
用語蔥屬(Allium species
)萃取物或蔥屬之水-醇萃取物特別指涉由所有蔥屬(genus Allium
)(百合科(familyLiliaceae
))中之種,特別是洋蔥(Allium cepa
.),取得之水-醇萃取物及天然萃取物。
橘屬(Citrus species
)之萃取物或橘屬之水-醇萃取物特別指涉由所有橘屬(genus Citrus
)(芸香料(familyRutaceae
))中之種,特別是檸檬(Citrus lemon
),取得之水-醇萃取物及天然萃取物。
保利藤屬(Paullinia species
)之萃取物(原子化或未原子化)或保利藤屬之水-醇萃取物(原子化或未原子化)特別指涉由所有保利藤屬(genusPaullinia
)(無患子科(familySapindaceae
))中之種,特別是瓜拿納(Paullinia cupana
),取得之水-醇萃取物及天然萃取物。
可可屬(Theobroma species
)之萃取物(原子化或未原子化)或可可屬之水-醇萃取物(原子化或未原子化)特別指涉由所有可可屬(genusTheobroma
)(錦葵科(familyMalvaceae
))中之種,特別是可可樹(Theobroma cacao
),取得之水-醇萃取物及天然萃取物。
根據本發明上述定義之組合物中,最感人興趣的組合物包括65%至93%之蔥屬水-醇萃取物,5%至33%之橘屬水-醇萃取物,0.25%至2.5%之柳屬(Salix species
)水萃取物(原子化或未原子化),以及0.1%至1%之硫酸鋅,其中特別是該組合物包括65%至93%之洋蔥(Allium cepa
)水-醇萃取物,5%至33%之檸檬(Citrus lemon
)水-醇萃取物,0.25%至2.5%之柳屬水萃取物(原子化或未原子化),以及0.1%至1%之六水合硫酸鋅。
柳屬(Salix species
)萃取物或柳屬之水萃取物(原子化或未原子化)係指涉由所有柳屬(genusSalix
)(楊柳科(familySalicaceae
)),特別是白柳(Salix alba
),取得之水萃取物。
根據本發明之組合物所使用的硫酸鋅可以為無水鹽或多水合,特別是六水合鹽。
根據本發明之最適組合物為:-該組合物含有約87%之洋蔥水-醇萃取物,約12%之檸檬水-醇萃取物,約0.5%之瓜拿納水-醇萃取物,以及約0.5%之可可樹水-醇萃取物(原子化或未原子化),-以及該組合物含有約87%之洋蔥水-醇萃取物,約12%之檸檬水-醇萃取物,約0.5%之白柳水萃取物(原子化或未原子化),以及0.2%之六水合硫酸鋅。
本發明之另一目的為提供一種上述組合物之製備方法,包括製備一原型溶液(master solution),其含有蔥屬與橘屬之萃取物,以及將該溶液與以下其一混合,保利藤屬萃取物與可可屬萃取物,或或柳屬萃取物與硫酸鋅,以得到所欲組合物。
根據本發明製備方法之較佳樣態,上述方法之特徵為,上述原型溶液係經由挑選、清洗並磨製上述蔥屬及橘屬,於醇類浸泡數小時,與過濾,並調整該醇類萃取物,以及與其它成份混合。
根據本發明之組合物的製備方法,由上述組成份製備原型溶液之建議步驟為,挑選、清洗並磨製上述蔥屬及橘屬,與96°酒精混合,於低溫浸泡48小時,經由0.22-微米濾膜過濾上述原型溶液,以得到一水-醇萃取物,其具有低含量之粒子,以及接著調整上述萃取物以得到30°醇。上述原型溶液可進行後續處理,經由與以下兩者之一簡單混合,與保利藤屬及可可屬之萃取物(原子化或未原子化)混合,或與柳屬萃取物(原子化或未原子化)及硫酸鋅混合。
上述組合物顯示感人興趣的特性,而使其適用於化妝品。
在化妝品應用上,上述組合物可特別用於控制及/或穩定任何影響皮膚、頭皮或其他體表之狀態,且特別可減緩毛髮損失,刺激毛髮生長,增加毛髮密度,減少頭皮屑,補償頭皮老化的症狀,以及治療指甲任何失調症狀。
在局部應用時,上述組合物可直接施用於皮膚或頭皮,以每日一至三次、溶液或濃縮乳液形式施用,例如,可以5至30%之濃度,較佳約20%濃度。
用於化妝品時,上述組合物可以顆粒、有彈性的膠囊或飲品方式作為食物添加劑投與;依照所需最後形式,除使用水-醇溶液形式之產品外,較佳可使用上述溶液之乾燥形式為產品,例如將上述水-醇溶液進行原子化,冷凍乾燥,濃縮或以超臨界二氧化碳進行二次萃取。
上述組合物也顯示感人興趣之藥理特性。
因此,上述組合物可投與至人體或動物,作為醫藥,特別是治療性或預防性藥物。
特別是,上述組合物可用於治療皮膚病,及更特別地,治療各種表皮細菌與病毒感染之皮膚病,皮膚老化,脫色或漂白皮膚,白斑病,肢端皮炎,光致(光化(actinic))皮膚老化,及種種與太陽光線有關之症狀(光照性皮膚病),任何原因的痤瘡(尋常痤瘡(青春痘),感染或丘疹性膿疤),玫瑰痤瘡,紅斑狼瘡,敏感性皮膚,昆蟲螫咬,油性或乾性皮膚,脂溢性失調症,任何原因之無毛症,毛髮喪失,頭皮糠疹(pityriasis capitis),斑禿(pelada),敏感性頭皮,油性髮質,牛皮癬及頭皮之類牛皮癬,汗泡症,疣及雞眼,疥瘡,口角炎與水腫,或任何侵襲指甲之疾病。
治療上,上述組合物也對傷口、任何原因的感染、燙傷、色斑、貝西氏症(Behcet’s disease)、皮膚卟啉症、血管瘤及惡性轉移有微血管化作用與傷口癒合作用。
上述組合物亦可用於治療角質化失調,角質受損,過度角質,包括角皮症、毛囊角化症(Darier’s disease)、角化不全、魚鱗病、濕疹、神經性皮炎、紅皮病(erythroderma)、苔癬樣硬化(lichenification)、麟狀皮症(scaly dermatosis)、結節性癢疹(prurigo)、疤痕過多(cheloids)及膿皰病(pustulosis)。
上述組合物上可用於治療循環與血管舒縮失調症,特別是痔區壓力、血栓性感染症、與靜脈淋巴功能不全、重腿(heavy legs)及異感症(paresthesia)相關症狀等功能性失調。
上述組合物可單獨或與一或多種其他化合物之混合物形式投與,可為醫藥組合物,包含有效劑量之活性成分,及標準醫藥上惰性賦形劑及/或添加物。
上述醫藥組合物可經口腔、胃腸道或靜脈途徑給藥,皮膚與黏膜之局部給藥、或如皮下等注射給藥。
上述醫藥品也可經口服投與,如以錠劑、膜衣錠、膜衣型式、顆粒、膠囊、軟膠囊、溶液、糖漿、乳化劑、懸浮液或噴霧混合物等形式給藥。如上述,根據所需給藥形式,最佳為使用水-醇溶液形式或乾燥形式的產品。
也可經由直腸途徑給藥,例如以栓塞劑型式,或經由靜脈途徑給藥,如以注射液或點滴輸液、微膠囊或植入物等型式,經由表皮給藥,如軟膏、溶液、或色膏,經皮(貼片)給藥,或經由其他途徑,如以噴霧或鼻噴霧等型式者。
上述醫藥組合物可經常規方法製備,其中可加入醫藥上惰性、有機或無機賦形劑至上述之本發明組合物。
因此,上述組合物可為固態或液態,以任何慣常使用於人類醫藥的形式,如以常規方法製備之素片或糖衣錠、藥丸、喉片、膠囊、滴劑、顆粒、注射劑、軟膏、乳霜或凝膠。
為製備素片或糖衣錠、膜衣錠及硬明膠膠囊,可使用例如乳糖、玉米澱粉或其衍生物,滑石粉及硬脂酸或其鹽。
對於軟明膠膠囊或栓塞劑之適當載體包括,如脂肪、蠟、半固態或液態多元醇、天然或改質油等。對於製備如注射液、乳化劑或糖漿等溶液之適當載體包括,例如水、醇類、甘油、多元醇、蔗糖、惰性糖、葡萄糖、蔬菜油等。對於微膠囊或植入物之適當載體包括,例如乙醛酸與乳酸之共聚物。
上述定義之活性成分可與通常用於醫藥組合物之賦形劑攪拌混合,如與滑石粉、***膠、乳糖、澱粉、硬脂酸鎂、可可油、水性或非水性載體、動物或植物來源之脂肪成分、石蠟衍生物、甘油、各種濕潤劑、分散劑或乳化劑及防腐劑等混合。
除上述定義之活性成分與賦形劑,上述醫藥組合物也可包含添加劑,例如,稀釋劑、分散劑、結合劑、潤滑劑、濕潤劑、穩定劑、乳化劑、防腐劑、甘味劑、色素、香料、增稠劑、緩衝劑、及亦可添加溶劑或溶化劑、延緩劑、調整等張之鹽、包覆劑或抗氧化劑。
本發明亦包括一種醫藥組合物,其包含至少一上述定義之藥劑作為活性成分。
當使用根據本發明之上述組合物時,劑量可在相當廣範圍之內調整,且須依受治療個體及其狀況而給藥。上述醫藥組合物通常包括0.2至500 mg,較佳為1至200 mg,之乾萃取物形式的上述活性成份。口服給藥時,每日劑量通常介於0.05至10 mg/kg之間,較佳為0.1至8 mg/kg,更佳為0.1至6 mg/kg。例如,對於成人而言適當的每日劑量可介於5至500 mg。
靜脈給藥時,每日劑量為約0.05至6 mg/kg,較佳為0.1至5 mg/kg。
每日劑量可分次給與,特別是當給與大量活性成分時。
以下所示之實施例僅作為例示本發明之應用,而非用於限定本發明。依本發明產品之特性,顯然可在使用液態或固態形式時佐以香料。
實施例1:
製備含有以下成分之組合物:-洋蔥之水-醇萃取物:87.04%-檸檬之水-醇萃取物:11.96%-原子化之瓜拿納水-醇萃取物:0.50%-原子化之可可水-醇萃取物:0.50%
上述洋蔥之水-醇萃取物之製備係經由挑選、清洗與磨碎洋蔥,冷浸泡於96°之酒精48小時以泡軟洋蔥,經0.22-微米濾膜過濾,收集酒精過濾液並調整為30°酒***。
上述檸檬之水-醇萃取物之製備係經由挑選、清洗與磨碎檸檬,冷浸泡於96°之酒精48小時,再經0.22-微米之濾膜過濾,收集酒精過濾液並調整為30°酒***。
包含洋蔥與檸檬之水-醇萃取物原型溶液之製備係經簡單混合上述兩溶液,再加入原子化之瓜拿納與可可之水-醇萃取物,以得到所需組合的萃取物。
實施例2:
製備含有以下成分之組合物:-洋蔥之水-醇萃取物:87.30%-檸檬之水-醇萃取物:12.00%-原子化之白柳水萃取物:0.50%-六水合硫酸鋅:0.20%
上述洋蔥之水-醇萃取物的製備係經由挑選、清洗與磨碎洋蔥,將之冷浸泡於96°酒精48小時,經0.22-微米之濾膜過濾,收集酒精過濾液並調整為30°酒***。
上述檸檬之水-醇萃取物的製備係經由挑選、清洗與磨碎檸檬,冷浸泡於96°酒精48小時,經0.22-微米之濾膜過濾後,收集酒精過濾液並調整為30°酒***。
包含洋蔥與檸檬之水-醇萃取物原型溶液之製備係經簡單混合上述兩溶液,再加入白柳之水萃取物及六水合硫酸鋅,以得到所需組合的萃取物。
實施例3:
製備含有以下成分之食品添加劑:-洋蔥之乾萃取物:87.04%-檸檬之乾萃取物:11.96%-瓜拿納之乾萃取物:0.50%-可可之乾萃取物:0.50%
將實施例1所得之組合物添加香料,並冷凍乾燥該混合物以得到一粉末,可直接作為食品添加劑。
實施例4:
製備含有以下成分之化妝乳液或頭皮護理液:-由實施例1所得之組合物:21 ml-足量賦形劑(包括香料):100 ml
乳液之製備係經簡單混合實施例1所得組合物與賦形劑。
實施例5:
製備含有以下成分之頭皮護理醫藥乳液:-實施例2所得組合物:40 ml-足量賦形劑(包括香料):100 ml
乳液之製備係經簡單混合實施例2所得組合物與賦形劑。
實施例6:
製備含有以下配方之錠劑:-實施例3所得組合物:100 mg-足量賦形劑(包括香料):300 mg(賦形劑含有:乳糖、滑石粉、澱粉、硬脂酸鎂)
實施例7:
製備含有以下成分之藥膏:-實施例3所得組合物:5 ml-足量賦形劑(包括香料):100 gl.
1).研究抗落髮效果係使用自動數位影像計數(phototrichogram)方法,於正常狀態下治療頭髮連續12週。
將20位男性志願者,其年齡介於35-55歲且具有依漢氏評量(Hamilton scale)為第II級至第IV級之輕微至中度禿頭,以實施例4之組合物處理(漢氏評量:第1級:輕微髮線後退,第II級:髮線向顳骨方向後退且頭頂區域毛髮變薄,第III級:髮線後退至顳骨且頭頂有禿髮區,第IV級:除顳骨外之禿髮,第V級:頭頂禿髮)。
療程如下述:第1天:顳骨位置定位、頭皮落髮區之頭髮橫截面、研究區域之自動數位影像計數。
第1-2天:不施用產品,也不洗髮。
第3天:在第1天相同區域做自動數位影像計數,並開始治療。
第3-42天:一天兩次施用產品至頭皮(每次治療噴灑2-3次)。
第42天:毛髮與皮膚之耐受性評估,顳骨位置定位,頭皮落髮區之頭髮橫截面,研究區域之自動數位影像計數。
第42-43天:不施用產品,也不洗髮。
第44:在第1天相同區域重做自動數位影像計數。
第44-84天:一天兩次施用產品至頭皮(每次治療噴灑2-3次),施用於頭皮落髮區之頭髮橫截面。
第84天:毛髮與皮膚之耐受性評估,顳骨位置定位,頭皮落髮區之頭髮橫截面,研究區域之自動數位影像計數。
第84-85天:不施用產品,也不洗髮。
第86天:在第1天相同區域重做自動數位影像計數。
研究結果顯示:-6週治療後有顯著抗落髮效果:統計上顯著增加A/T比(毛法初生期(anagenic)/休止期(telogenic)比率)+44.91%。
-12週治療後有顯著抗落髮效果:統計上顯著增加A/T比(毛法初生期(anagenic)/休止期(telogenic)比率)+46.78%。
-良好臨床耐受性:皮膚學檢查時未觀察到皮膚反應。
-良好主觀自覺臨床耐受性:然有一名志願者表示感到皮膚不適。
2).評估實施例1與2之組合物的血管新生作用
對本發明之產品以血管新生套組盤(Angiokit plates)進行測試。使用習知測試法,檢驗與纖維母細胞同時培養之內皮細胞的發生情形,並觀察毛細結構(小管結構)之形成。將不同濃度之受測產品注入測試盤中之某些孔。某些孔另接受活化物(血管內皮生長因子(VEGF)),而其他孔接受抑制物(蘇拉明(Suramine))。某些孔則作為對照組。
在第3、4、7、10及12天換培養基,並在第15天結束實驗。
觀察第15天之結果顯示本發明之產品具有顯著血管新生活性。
Claims (8)
- 一種組合物,其特徵在於包括以下成份做為活性成分,一洋蔥(Allium cepa )萃取物、一檸檬(Citrus lemon )萃取物、一瓜拿納(Paullinia cupana )萃取物、及一可可樹(Theobroma cacao )萃取物。
- 如申請專利範圍第1項所述之組合物,其特徵在於包括一洋蔥之水-醇萃取物,一檸檬之水-醇萃取物,一瓜拿納水-醇萃取物原子化或未原子化及一可可樹水-醇萃取物原子化或未原子化。
- 如申請專利範圍第1或2項所述之組合物,其特徵在於包括65%至93%之洋蔥水-醇萃取物,5%至33%之檸檬水-醇萃取物,0.25%至2.5%之瓜拿納原子化或未原子化水-醇萃取物,以及0.25%至2.5%之可可樹原子化或未原子化水-醇萃取物。
- 如申請專利範圍第3項所述之組合物,其特徵在於包括87%之洋蔥水-醇萃取物,12%之檸檬水-醇萃取物,0.5%之瓜拿納(Paullinia cupana )原子化水-醇萃取物,以及0.5%之可可樹原子化水-醇萃取物。
- 一種組合物的製備方法,製備如申請專利範圍第1項之組合物,其特徵在於:製備一原型溶液,該原型溶液包括洋蔥與檸檬之萃取物,以及接著將該原型溶液與一瓜拿納萃取物與可可樹萃取物混合以得到所需組合物。
- 如申請專利範圍第5項之製備方法,其中該原型溶液係經由挑選、清洗、磨碎、及數小時浸泡洋蔥與檸檬於 醇類,過濾該混合物,調整該醇萃取物,以及與其它成份混合。
- 一種化妝品組合物,用於減緩毛髮喪失,刺激毛髮生長,增加毛髮濃度,包括申請專利範圍第1項之組合物。
- 一種醫藥品,含有如申請專利範圍第1項之組合物,其特徵在於:該醫藥品預期可刺激並促進毛髮再生。
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US10682299B2 (en) | 2017-11-06 | 2020-06-16 | Chih-Tseng WU | Nano composite materials and use thereof |
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