CN1726007A - 除去咖啡因的咖啡豆提取物在制备通过口服给药用于刺激皮肤皮脂功能的组合物中的用途 - Google Patents
除去咖啡因的咖啡豆提取物在制备通过口服给药用于刺激皮肤皮脂功能的组合物中的用途 Download PDFInfo
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- CN1726007A CN1726007A CNA2003801059661A CN200380105966A CN1726007A CN 1726007 A CN1726007 A CN 1726007A CN A2003801059661 A CNA2003801059661 A CN A2003801059661A CN 200380105966 A CN200380105966 A CN 200380105966A CN 1726007 A CN1726007 A CN 1726007A
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Abstract
本发明涉及除去咖啡因的咖啡豆提取物在制备通过口服给药用于刺激皮肤皮脂功能的组合物中的用途，并且尤其能够调节与干性皮肤有关的病症。本发明尤其涉及通过口服途径给药来刺激皮肤的皮脂功能的美容的，营养的或药物的组合物。本发明也涉及用于治疗干性皮肤的美容方法。
Description
本发明涉及除去咖啡因的咖啡豆提取物在制备通过口服给药用于刺激皮肤皮脂功能的组合物中的用途，并且尤其用于校正与干性皮肤有关的病症。本发明尤其涉及通过口服途径给药来刺激皮肤的皮脂功能的美容的，营养的或药物的组合物。本发明也涉及用于治疗干性皮肤的美容方法。
皮脂不足的干性皮肤以皮脂的分泌和排泄不足为特征。按照惯例，在前额测量的皮脂浓度低于100μg/cm2被认为是这种干性皮肤的特征。
干性皮肤经常并发脱屑，面色暗淡，皮肤组织无活力。微炎性症状，尤其是皮炎，对于干性皮肤更加经常发生。
有干性皮肤的病人经常感觉脸部有不舒服的感觉如间歇性抽搐。
所有这些疾病随着年龄的增大而发展，因为逐渐老化通常伴有皮脂附件功能的丧失。
另一方面，普遍认为正常的多脂的皮肤比干性皮肤改善老化的写照。这种作用可能归咎于通过皮脂途径分泌维生素E的事实(Thiele等，J.Invest.Dermatol.1999；113；1006-10)。
皮脂是构成毛囊皮脂腺单元附件的皮脂腺的天然产物。与汗液一起，由外分泌腺或顶浆分泌腺产生，它构成表皮的天然水化剂。
皮脂分泌受不同神经原点传入纤维的控制。Cartlidge等(Br.J.Dermatol-1972；86(1)，61-63)确定了皮脂溢胆碱能系统(淋巴管周围)的调节剂作用。并且，已知的，多巴胺能系统，当失去稳定性时，在帕金森综合征的情况下，导致可被L-DOPA校正的高皮脂溢(JCVillares等，Acta Neurol Scand，80(1)，5Z-63)。也知道胆碱能系统，通过毒蕈碱性受体亚型媒介，拮抗多巴胺的释放(Pharmacologie，M.Schorderét等，p 71，Ed.Frison-Roche，ISBN 2-05-100910-4)。
多巴胺能系统的激活和/或胆碱能系统的抑制(通过毒蕈碱性受体)因而可能导致脂肪生成的衰退和/或皮脂的分泌。
另一方面，多巴胺能刺激的限制和/或胆碱能系统的激活(通过毒蕈碱性受体)可能导致皮脂分泌和/或生产的增加。除去咖啡因或未除去咖啡因(undecaffeinated)咖啡豆的乙醇部分被发现具有毒蕈碱型拟胆碱活性(SY Tse，J.Pharm Sci.，1991，80(7)，665-669和SY Tse，J.Pharm Sci.，1992，81(7)，449-452)。
本发明源于对以下事实的证明，口服给药含有除去咖啡因咖啡豆提取物的组合物可能对刺激皮肤的皮脂功能有有益的作用。
咖啡树是一种具有光滑边缘，多年生，皮质的，有光泽叶子(10-15×4-6cm)的小树。叶腋的螺纹处簇生白色、芳香的花朵。果实是绿色核果，成熟时变红，通常含有两个平面-凸面的浆果，这两个浆果通过它们的平面相毗邻。虽然只有两个品种的咖啡供应咖啡市场的基本需求(小果咖啡C.Arabica和中果咖啡C.canephora)，东非的热带丛林中存在着许多品种的野生咖啡树。
浆果是卵形的(10-15×6-8mm)，背面凸起，腹面平坦，腹面有纵沟穿过，即种脐。硬的并且呈绿色，没有气味。绿色咖啡粉末镜检可见源自外皮和胚乳细胞的梭状纤维：多面的，象珠子样的结构，壁是珍珠光泽和不规则厚度的；含有小油滴。
通过湿的途径(发酵，清洗)或干的途径(干燥后，机械剥皮)从咖啡“浆果”，也就是核果获得咖啡“豆”。除去红色外果皮和肉质的中果皮得到果肉，这就是咖啡的“剥皮”。剥皮后(除去木质内果皮)得到咖啡“浆果”(或豆)。
绿色咖啡浆果多于50％的干燥物以碳水化合物为代表，基本上是多糖。蛋白质占该质量的10至12％，脂类10至18％。天然脂类的不皂化部分是很大的(多于10％)：除了甾醇，烃类，维生素E，还观察到游离状态的二萜醇类(咖啡醇，咖啡白脂和kauranic衍生物)，尤其是，以脂肪酸酯形式存在的。咖啡浆果含有大约5％的酚酸类：奎尼酸，咖啡酸，绿原酸。咖啡因的含量是变量：从0.6至2％，对于特定的中果咖啡(robusta品种)多于3％。
在干燥过程中，浆果的结构和成分有显著变化。水含量减少，浆果膨胀，多糖被分解(尤其形成可溶的产物)，色素形成(缩聚呋喃)和非常复杂气味的产生(几百种化合物：乙醇，酚，醛，呋喃和吡咯衍生物，烃，噻吩等。)
据申请人所知，从未有过关于下述的提示：除去咖啡因的咖啡豆提取物被用于制备口服给药和刺激皮肤皮脂功能的组合物，尤其是用于干性皮肤的治疗。
因此本发明的目的是除去咖啡因的咖啡豆提取物在制备用于刺激皮肤皮脂功能组合物中的用途，所述制备的组合物用于口服给药。
本文下述的“咖啡豆”必须被理解为是咖啡“浆果”通过湿的途径(发酵，清洗)或干的途径(干燥后，机械剥皮)获得的咖啡豆，剥皮后如上所述。
“提取物”必须被理解为是从原料的乙醇或水合乙醇提取获得的所有化合物，原料是除去咖啡因的咖啡豆，烤过或没烤过的。
皮肤皮脂的产生量能根据所谓皮脂测量方法的标准、通过测量皮脂的量来确定，例如，在L′Oreal专利FR2368708或FR2404845中有记载。
“刺激皮肤皮脂功能”意思是皮肤皮脂量的显著刺激。
在组合物中使用的用于咖啡豆提取物制备的咖啡树品种有利地选自咖啡属的品种。
在一个具体实施例中，咖啡豆提取物选自小果咖啡(Coffeaarabica)，中粒种咖啡(Coffea robusta)，中果咖啡(Coffea canephora)或大果咖啡(Coffea iberica)。提取物可以从烤过的咖啡豆获得。也能从没烤过的咖啡豆获得。
根据本发明的用途，咖啡豆的提取物是去除咖啡因的。
尤其地，咖啡豆提取物能够通过水合醇或醇提取咖啡豆来获得，并且优选用甲醇，乙醇或丙醇提取。优选地，不含非极性溶剂提取的咖啡豆部分。
S.Y.H.Tse(见上)描述了去除咖啡因咖啡提取物的制备方法，下述实施例中也有记载。
本发明也涉及含有去除咖啡因的咖啡豆提取物、用于刺激皮肤的皮脂功能、适于口服给药的美容、营养或药用的组合物。尤其地，根据本发明的组合物旨在用于干性皮肤或皮肤老化的治疗和/或预防。除去咖啡因的咖啡豆提取物在组合物中的比例将显然由需要的刺激皮肤皮脂功能的作用和组合物的给药形式决定。
通过口服途径给药的组合物可以被制备成任何的适合这种给药形式的草本制剂形式，例如刻字或未刻字的片剂，颗粒剂，胶囊剂，明胶胶囊，溶液，悬浮液或含有适当赋形剂的溶液。
组合物可以是任意的口服应用的食品或药用产品，或美容产品。食品或药用载体的例子是牛奶，酸奶，凝乳，乳酪，发酵牛奶，牛奶为主的发酵产品，冰淇淋，发酵谷类为主的产品，奶粉为主的产品，婴儿或宠物食品，或片剂，液体细菌混悬液，干的口服补充剂，湿的口服补充剂，干的管饲或湿的管饲剂。
优选地，根据本发明的组合物是营养补充剂，以片剂，颗粒剂，胶囊剂，明胶胶囊固体组合物的形式出现，含有上述的除去咖啡因的咖啡豆提取物，并且至少含有一种适于口服给药的辅料。
在这方面，口服组合物尤其地对于食物补充剂的辅料对于专业人员来说是已知的。其中也可以提及一下，纯粹出于解释的目的，润滑剂例如硬脂酸镁，迅速溶解剂，凝胶制剂，增稠剂，润湿剂，脂肪的和/或水性化合物，防腐剂，填充(texturizing)剂，矫味剂和/或包衣衣料，抗氧化剂和食品中常用的着色原料。
根据本发明的组合物可以另外含有脂类，多酚，氨基乙磺酸，原生微生物，维生素和/或微量元素。如果原生物被使用，可以包括活性状态，半活性状态或失活状态，例如，作为冻干粉末。培养的超浮游物微生物也可以被包含在组合物中。它们可以选自包括乳酸菌在内的类群，尤其是乳酸杆菌和/或双歧杆菌并且更优选约翰逊乳杆菌(Lactobacillus johnsonii)，罗伊乳杆菌(Lactobacilus reuteri)，鼠李糖乳杆菌(Lactobacillus rhamnosus)，副干酪杆菌(Lactobacillus paracasei)，干酪乳杆菌(Lactobacillus casei)，两歧双歧杆菌(Bifidobacterium bifidum)，短双歧杆菌(Bifidobacterium breve)，动物双歧杆菌(Bifidobacteriumanimalis)，婴儿双歧杆菌(Bifidobacterium infantis)，青春双歧杆菌(Bifidobacterium dolescentis)和假链状双歧杆菌(Bifidobacterium pseudocatenulatum)。使用的最优选的具体的菌株是约翰逊乳杆菌(Lal)，根据布达佩斯条约于1992年6月30日存放于巴斯德研究所(Institute Pasteur)，保藏号是CNCM I-1225或者副干酪杆菌(ST11)根据布达佩斯条约于1999年1月12日存放于巴斯德研究所(Institute Pasteur)，得到保藏号CNCM I-2116。下述化合物可以例如单独或组合被使用：锌和它的盐包括硫酸锌和葡萄糖二酸锌，维生素B5，B6，B8，C，E或PP，β-胡萝卜素和类葫萝卜素，大蒜提取物尤其是硫化烯丙或大蒜油的形式，硒，姜黄素，姜黄木脂素类(curcuminoids)，烟酸，紫草酸(lithospermic acid)和腺苷。下述可以被理解：专业技术人员将选择这些活性化合物并且，可能时，通过阻止目的状态的预期活性被抑制或消弱，以某种方式将它们组合以改善本发明目的的组合物的预期作用。
旨在口服给药的组合物包含占组合物重量0.1％至80％的除去咖啡因的咖啡豆提取物并且优选占组合物重量的1％至50％。
绿原酸是自然存在于某些咖啡豆提取物中的酚类化合物，与干性皮肤的治疗无关。根据本发明，绿原酸不是治疗和/或预防干性皮肤的组合物中的活性因子。
如前所述，在一个具体实施例中，绿原酸存在于含有除去咖啡因的咖啡豆提取物的组合物中，其量低于或等于组合物总重量的0.1％。
本发明也涉及预防和/或治疗干性皮肤的美容方法，或涉及预防和/或美容治疗皮肤老化的方法，它包括通过口服途径给予含有咖啡豆提取物的组合物，如上所述。
治疗干性皮肤，通过口服途径给予除去咖啡因的咖啡豆提取物的每日剂量优选为0.01至5000mg/天。优选地，根据本发明存在于组合物中的咖啡豆提取物的允许给药的量是0.5至1000mg/天。
以上提及的本发明的特点通过下述实施例将变得更加清楚。
实施例
实施例1：中粒种咖啡烘烤提取物的制备
0.5kg烘烤过的咖啡豆被制成粉末，通过在4℃时(冰浴)用Turrax机械在24000转/分钟条件下研磨1分钟。
得到的粉末在pH 8.5时与5升0.05M磷酸盐缓冲剂混合。全部混合物在4℃下搅拌30分钟，然后在4℃下10000G离心。超浮游物通过0.22μm的过滤器过滤(无菌滤过)。
为了避免氧化现象，提取物然后被通过缝匠肌型膜的超滤法被分级。
然后提取物被冻干。得到被叫作“冻干提取物”的29.5克的活性提取物。
然后通过超临界层析法去除咖啡因(CO2被用作载气)。得到25.5克的被叫作“除去咖啡因的冻干提取物”的活性提取物。
实施例2：解释本发明配方的实施例和尤其是根据本发明的组合物。
通过不同组分的简单混合得到这些组合物。
组合物1：软胶囊
赋形剂：
大豆油…………………………………………………………40mg
麦芽油…………………………………………………………85mg
大豆卵磷脂……………………………………………………25mg
维生素：
天然维生素E………………………………………………… 3mg
维生素C棕榈酸盐…………………………………………… 150mg
组分：
除去咖啡因的中粒种咖啡冻干提取物………………………15mg
琉璃苣油………………………………………………………200mg
黑醋栗种子油……………………………………………………150mg
组合物2：软胶囊
赋形剂：
大豆油……………………………………………………………40mg
麦芽油……………………………………………………………85mg
大豆卵磷脂………………………………………………………25mg
维生素：
天然维生素E…………………………………………………… 3mg
组分：
除去咖啡因的中粒种咖啡冻干提取物…………………………150mg
琉璃苣油…………………………………………………………200mg
月见草油…………………………………………………………200mg
组合物3：软胶囊
赋形剂：
大豆油……………………………………………………………40mg
麦芽油……………………………………………………………85mg
大豆卵磷脂………………………………………………………25mg
维生素：
天然维生素E…………………………………………………… 3mg
组分：
除去咖啡因的中粒种咖啡冻干提取物…………………………50mg
琉璃苣油…………………………………………………………200mg
月见草油…………………………………………………………200mg
冻干乳酸杆菌……………………………………………………200mg
组合物4：软胶囊
赋形剂：
大豆油……………………………………………………………40mg
麦芽油……………………………………………………………5mg
大豆卵磷脂……………………………………………………25mg
维生素：
天然维生素E………………………………………………… 3mg
组分：
除去咖啡因的中粒种咖啡冻干提取物………………………150mg
琉璃苣油………………………………………………………200mg
月见草油………………………………………………………200mg
维生素C……………………………………………………… 50mg
葡萄糖二酸钙…………………………………………………200mg
硬脂酸镁………………………………………………………400mg
冻干乳酸杆菌…………………………………………………300mg
Claims (12)
1.用于刺激皮肤皮脂功能的组合物，其特征在于它含有除去咖啡因的咖啡豆提取物，所述组合物被配制用于口服给药。
2.根据权利要求1的组合物，其特征在于提取物源自选自小果咖啡，中粒种咖啡，中果咖啡或大果咖啡品种的咖啡豆。
3.根据权利要求1或2的组合物，其中提取物源自烘烤过的咖啡豆。
4.根据权利要求1至3任一的组合物，其中咖啡豆提取物是通过水合醇或醇提取来获得的。
5.根据权利要求1至4的组合物，其为可以通过口服途径以固体形式给予的组合物，其中含有至少一种适用于口服给药的辅料。
6.根据权利要求1至5任一的组合物，其中咖啡豆提取物占组合物总重量的0.1％至80％。
7.根据权利要求6的组合物，其中咖啡豆提取物占组合物总重量的1％至50％。
8.治疗和/或预防干性皮肤或治疗和/或预防皮肤老化的美容方法，包括口服给予含有根据权利要求1至7之一的除去咖啡因的咖啡豆提取物的组合物。
9.除去咖啡因的咖啡豆提取物在制备通过口服给药用于刺激皮肤皮脂功能的组合物中的用途。
10.根据权利要求9的用途，其中提取物源自选自小果咖啡，中粒种咖啡，中果咖啡或大果咖啡品种的咖啡豆。
11.根据权利要求9或10的用途，其中提取物源自未烘烤的咖啡豆。
12.根据权利要求9至11任一的用途，其中咖啡豆提取物是通过水合醇或醇提取来获得的。
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR02/15867 | 2002-12-13 | ||
| FR0215867A FR2848448B1 (fr) | 2002-12-13 | 2002-12-13 | Utilisation d'un extrait de grains de cafe decafeine dans la preparation d'une composition destinee a stimuler la fonction sebacee de la peau par administration orale |
| US60/441,734 | 2003-01-23 |
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| Publication Number | Publication Date |
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| CN1726007A true CN1726007A (zh) | 2006-01-25 |
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| Country | Link |
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| JP (1) | JP2006511603A (zh) |
| CN (1) | CN1726007A (zh) |
| FR (1) | FR2848448B1 (zh) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007128191A1 (fr) * | 2006-05-09 | 2007-11-15 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Inhibiteur du virus de l'hépatite b et son utilisation |
| CN103068360A (zh) * | 2010-07-30 | 2013-04-24 | 雀巢产品技术援助有限公司 | 烘焙咖啡豆和生咖啡豆的混合物用于调节皮肤色素沉着的用途 |
| CN103517699A (zh) * | 2010-07-30 | 2014-01-15 | 雀巢产品技术援助有限公司 | 烘焙咖啡豆用于调节皮肤色素沉着的用途 |
| CN103616426A (zh) * | 2013-12-02 | 2014-03-05 | 中国科学院上海应用物理研究所 | 一种用于快速生化分析的集成式的微流控电化学生物传感系统及其使用方法 |
| CN107106479A (zh) * | 2014-12-18 | 2017-08-29 | 纽璀克斯技术公司 | 改善皮肤的脂肪团外观的组合物 |
| CN111616995A (zh) * | 2020-04-14 | 2020-09-04 | 云南英格生物技术有限公司 | 一种咖啡银皮提取物及其制备方法和应用 |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008503563A (ja) * | 2004-06-23 | 2008-02-07 | ロレアル | 敏感及び／又は乾燥肌の予防及び／又は処置に有用な方法及び組成物 |
| FR2872047B1 (fr) * | 2004-06-23 | 2007-06-15 | Oreal | Composition pour peaux sensibles associant cation mineral et probiotique(s) |
| FR2920304B1 (fr) | 2007-09-04 | 2010-06-25 | Oreal | Utilisation cosmetique de lysat bifidobacterium species pour le traitement de la secheresse. |
| FR2920305B1 (fr) | 2007-09-04 | 2010-07-30 | Oreal | Utilisation d'un lysat de bifidobacterium species pour le traitement de peaux sensibles. |
| FR2942719B1 (fr) | 2009-03-04 | 2011-08-19 | Oreal | Utilisation de microorganismes probiotiques pour limiter les irritations cutanees |
| EP2598102A2 (en) * | 2010-07-30 | 2013-06-05 | Nestec S.A. | Use of green coffee beans for regulating skin pigmentation disorders |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR1533371A (fr) * | 1967-06-07 | 1968-07-19 | Produits dermo-cosmétiques à base d'extraits de caféier | |
| US3660107A (en) * | 1970-01-23 | 1972-05-02 | Meyer Lab Inc | Effervescent beverage powder and tableted beverage compositions |
| DE3920209A1 (de) * | 1989-06-21 | 1991-03-28 | Nolde Sylvia | Kaffee-pralinen (-riegel,-tafeln u.ae.m.), coffeinfrei |
| EP0534024B1 (en) * | 1991-09-23 | 1995-04-19 | Kraft Foods, Inc. | Decaffeinated coffee products with reduced potassium content |
| EP0582147A3 (en) * | 1992-08-03 | 1994-08-24 | Nestle Sa | Anti-urease cosmetic or dermatologic composition |
| IT1290806B1 (it) * | 1997-03-21 | 1998-12-11 | Universal Flavors S R L | Estratti decaffeinati di mate' |
| US20020160067A1 (en) * | 2001-04-25 | 2002-10-31 | Oncology Science Corporation | Therapeutic preparation and method for producing a therapeutic preparation using coffee beans as a substrate |
-
2002
- 2002-12-13 FR FR0215867A patent/FR2848448B1/fr not_active Expired - Fee Related
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2003
- 2003-12-12 CN CNA2003801059661A patent/CN1726007A/zh active Pending
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007128191A1 (fr) * | 2006-05-09 | 2007-11-15 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Inhibiteur du virus de l'hépatite b et son utilisation |
| CN103068360A (zh) * | 2010-07-30 | 2013-04-24 | 雀巢产品技术援助有限公司 | 烘焙咖啡豆和生咖啡豆的混合物用于调节皮肤色素沉着的用途 |
| CN103517699A (zh) * | 2010-07-30 | 2014-01-15 | 雀巢产品技术援助有限公司 | 烘焙咖啡豆用于调节皮肤色素沉着的用途 |
| CN103068360B (zh) * | 2010-07-30 | 2015-11-25 | 雀巢产品技术援助有限公司 | 烘焙咖啡豆和生咖啡豆的混合物用于调节皮肤色素沉着的用途 |
| CN103616426A (zh) * | 2013-12-02 | 2014-03-05 | 中国科学院上海应用物理研究所 | 一种用于快速生化分析的集成式的微流控电化学生物传感系统及其使用方法 |
| CN103616426B (zh) * | 2013-12-02 | 2016-05-11 | 中国科学院上海应用物理研究所 | 一种用于快速生化分析的集成式的微流控电化学生物传感系统及其使用方法 |
| US11045806B2 (en) | 2013-12-02 | 2021-06-29 | Hangzhou Jinchengyibang Technology Co. Ltd | Integrated type microfluidic electrochemical biosensor system and method for rapid biochemical analysis |
| CN107106479A (zh) * | 2014-12-18 | 2017-08-29 | 纽璀克斯技术公司 | 改善皮肤的脂肪团外观的组合物 |
| CN111616995A (zh) * | 2020-04-14 | 2020-09-04 | 云南英格生物技术有限公司 | 一种咖啡银皮提取物及其制备方法和应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| FR2848448A1 (fr) | 2004-06-18 |
| FR2848448B1 (fr) | 2007-04-06 |
| JP2006511603A (ja) | 2006-04-06 |
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