CN101119642A - 预防紫外线损伤的口服组合物 - Google Patents
预防紫外线损伤的口服组合物 Download PDFInfo
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- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
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Abstract
本发明涉及用于预防紫外线损伤的口服组合物,特别是基于橄榄提取物制备的口服组合物,所述橄榄提取物是通过对压榨橄榄所得的植物水用有机溶剂提取或使用水和/或有机溶剂对橄榄饼进行提取得到的。
Description
发明领域
本发明涉及用于预防紫外线损伤的口服组合物,特别是基于橄榄提取物制备的口服组合物,所述橄榄提取物是通过对压榨橄榄所得的植物水用有机溶剂提取或使用水和/或有机溶剂对橄榄饼(即,橄榄压榨后剩余的固体相,也被称为果渣或残渣)进行提取得到。
现有技术
当皮肤暴露于紫外线下时,会出现各种皮肤损伤,例如红斑、浮肿和光老化现象,例如皮肤增厚、弹性丧失、皱纹形成和皮肤暗化。反复暴露于强烈紫外线下已知可增加皮肤癌的患病危险。为预防紫外线损伤,通常使用防晒霜;但是,防晒霜的使用可能很麻烦,例如为了提供足够的保护,防晒霜需要多次使用,特别是在游泳和大量出汗后。因此,仍需要一种方便有效的预防紫外线损伤的方法。
已进行了各种研究以发现对紫外线皮肤损伤有保护作用的可口服使用的生理成分。例如,已证明口服使用类胡萝卜素或维生素E能够抑制紫外线导致的皮肤炎症(红斑)(实验生物学和医学学会报告(Proceedings ofSociety of Experimental Biology&Medicine),223卷,170-174页,2000;美国临床营养学杂志(American Journal of Clinical Nutrition),71卷,795-798页,2000)。
橄榄提取物(木樨榄)也被证实具有抗氧化特性,能够抑制过量黑色素的生成和肿瘤细胞增殖并能清除肿瘤细胞(JP-A第09-78061号;WO01/45514,JP-A第2002-18645号)。
专利申请JP-A第2000-319161号、JP-A第2001-206822号和JP-A第2001-252054号公开了含有从橄榄果实得到的植物水的皮肤化妆品、头发营养品和口服组合物。同时也发现当将橄榄植物水或橄榄饼的提取物给大鼠口服使用时,激发了血浆的抗氧化活性并降低了由测流烟诱发的DNA氧化损伤标志物(Free Rad.Res.,34卷,301-305页,2001;Circulation,102卷,2169-2171页,2000)。
但是,得自橄榄压榨残渣的橄榄提取物对于暴露于紫外线的人类皮肤的作用还未被评估。
发明描述:
现已发现,由橄榄压榨所得植物水和橄榄饼得到的提取物(在下文中称为“橄榄果实提取物”)在口服使用时,能够预防紫外线损伤,特别是当它们口服使用时,能预防红斑、水肿、皮肤增厚、弹性消失、皱纹形成及皮肤暗化。
因此,本发明涉及橄榄果实提取物在制备用于预防紫外线损伤的口服组合物中的用途。根据本发明的宗旨,“橄榄果实提取物”指通过对橄榄压榨所得植物水用有机溶剂提取或使用水和/或有机溶剂对橄榄饼进行提取所得到的产物。
“橄榄果实提取物”在口服组合物中的含量为干重的0.01至70%(重量);为抑制紫外线辐射导致的皮肤损伤,施用的组合物应该可以提供剂量为每天0.05至1.0克(干重)的橄榄果实提取物。
本发明中的橄榄果实提取物可获自任何种类橄榄果实的橄榄压榨残渣,不考虑它们的产地或计划用途(食物橄榄或油料橄榄)。但是,科拉蒂(Coratina)品种为特别优选。橄榄压榨残渣通常被废弃,因此,它们相对便宜。
提取物可获自全果(果皮、果肉和种子)的残渣,也可在去除果皮和果肉后,只获自果肉。
植物水是从橄榄压榨制备橄榄油的副产品,为水溶液。植物水本身可直接应用;但是,优选通过过滤和/或离心方法去除其所含的脂质、含纤维的物质和种子壳。此外,为了抑制细菌污染及去除异味,在植物水中加入亲水性醇和多羟基醇例如乙醇、异丙醇、1,3-丁二醇和丙二醇,优选加入总重的5至80%(重量),更优选的范围是总重的10至40%(重量),然后进行过滤和离心。另外,植物水,无论是其本身还是在经过过滤离心或者加入乙醇进行处理后,均可进行浓缩或干燥。
“橄榄饼”指橄榄压榨后得到的固体相。
本发明的提取物通过对植物水用有机溶剂提取或使用水和/或有机溶剂对橄榄饼提取获得。优选的溶剂是醇,亲水性醇和多羟基醇例如乙醇、异丙醇、1,3-丁二醇和丙二醇。另外,也可使用水和有机溶剂的溶剂混合物。所得提取物可直接使用,或在分离和纯化步骤后浓缩和干燥。
根据上述提取方法从固体相得到的提取物可以同从水相提取得到的提取物,及从水和固体两相提取得到的提取物同样使用。
本发明的提取物可加入其它活性物质,例如维生素类如维生素C、维生素E、维生素B2、维生素B6和烟酰胺;矿物质例如镁、锌和铬;大花紫薇、匙羹藤、芦荟、罗汉果、茭白、桑树叶、枇杷叶、荷花、五层龙属、红景天、不吸收性糊精、Echevaria glauca、绿茶多酚、茶氨酸、组氨酸、人参、海藻、蛇马草、甘薯或啤酒酶。此外,还可加入乳化剂、分散剂、助悬剂、扩展剂、渗透剂、增湿剂和稳定剂。本发明的口服组合物可以是固态或液态形式,例如片剂、颗粒剂、胶囊、饮料、果冻、口香糖、糖果和片状糖果。
“橄榄果实提取物”的含量随着最终的给药形式而变化。但是,一般说来,依据干重,橄榄提取物的含量优选为组合物总重的0.01至70%(重量)并且更优选的含量范围是总重的0.01至50%(重量)。提取物含量低于0.01%时,经常不能提供有效的预防紫外线损伤的效果。
本发明的口服组合物的服用量应当可以提供每天0.05至1.0克,优选0.08至0.5克“橄榄果实提取物”(干重)的剂量。在此剂量,有足够的紫外线损伤预防效果并且组合物服用方便;疗程根据个体的需要,通常持续一个星期或更长时间。
图标简述
图1显示了在持续服用实施例1的片剂前后,最小红斑剂量(MED)的变化。
现通过一些实施例来更加详细地说明本发明。
实施例
制备例1-橄榄果实压榨后,水溶液和其浓缩物的制备
向从科拉蒂橄榄果实生产橄榄油的过程中所得的8升水溶液中,加入2升纯乙醇。获得的水-乙醇溶液在4℃以10,000转每分钟的速度离心15分钟,得到1.5千克固相和8.5升水相。水相根据标准方法在硅藻土上过滤,得到8.5升浅棕色水溶液(“制备例1的水溶液”)。将5升该溶液根据标准方法浓缩得到220克浓缩物(“制备例1的浓缩物”)。
制备例2-自橄榄压榨得到的水溶液中,制备干燥的固体物质
冷冻干燥74.8克“制备例1的浓缩物”,得到34.84克干燥固体物质(“制备例2的干燥固体物质”)。
制备例3-自橄榄压榨所得的水相和固相中制备提取物
压榨两千克科拉蒂品种橄榄果实并用含水乙醇提取两次。所得提取物根据传统程序浓缩,获得100克干燥的固体物质(“制备例3的干燥固体物质”)。
实施例1-含有制备例3的干燥固体物质的片剂
含有制备例3的干燥固体物质及下面列出的成分的片剂根据标准方法制备。
成分 | 含量(重量%) |
(1)“制备例3的干燥固体物质” | 7.0 |
(2)糊精 | 33.0 |
(3)还原型麦芽糖淀粉糖浆粉末*1 | 30.0 |
(4)结晶纤维素 | 23.0 |
(5)琼脂粉末 | 4.0 |
(6)香料 | 1.0 |
(7)蔗糖脂肪酸酯 | 2.0 |
*1商品名:Malbit,NIKKEN Fine Chemical Co.Ltd生产。
实施例2-预防紫外线照射诱发的红斑的实验
实验程序
1.13名健康男性用紫外线照射其背部并测得每人的最小红斑照射剂量(MED)。选择10块7.5mmx 7.5mm的区域作为紫外线照射部位。用紫外线发射装置(商品名:M-DMR-100,Clinical Supply Corp.生产)照射紫外线,UVB:FL20S/E(TOREX CORP.生产)和UVA:S/BL(TOREX Corp.生产)平行排列。紫外线强度用紫外线强度计(商品名:UVR-305/360-D(II),TOREX Corp.生产)测量并且测得UVB的强度为0.45mW/cm2。用紫外线以不同的周期照射紫外线照射部位,并且在照射24小时后测定每一个体的MED值。
2.13位受试者随机分为两组,分别为10人和3人;10人组服用(每天12片,服用4个星期)根据实施例1制备的口服片剂(200毫克/片)。服用时间和方法由每一个体自行决定(每目的“制备例3的干燥固体物质”的剂量是0.168克)。对照组3人不进行任何处置,以确认MED在实验过程中没有变化。在实验结束时,MED根据上述方法测量。
实验结果
实验结果见图1。对照组实验前后的MED没有差异,而服用根据实施例1制备的片剂4个星期的实验组中,MED有显著性增加(p<0.01),即,对紫外线的抵抗性增加并且有炎症预防效果。
下列各实施例涉及其它含有本发明提取物的口服制剂。
实施例3-片剂
成分 | 含量(重量%) |
(1)“制备例3的干燥固体物质” | 50.0 |
(2)糊精 | 20.0 |
(3)结晶纤维素 | 23.0 |
(4)琼脂粉末 | 4.0 |
(5)香料 | 1.0 |
(6)蔗糖脂肪酸酯 | 2.0 |
将各成分充分混合并根据标准程序制成片剂。
实施例4-颗粒剂
成分 | 含量(重量%) |
(1)“制备例3的干燥固体物质” | 20.0 |
(2)淀粉 | 30.0 |
(3)乳糖 | 49.0 |
(4)结晶纤维素 | 1.0 |
将各成分充分混合并根据标准程序制成颗粒剂。
实施例5-软胶囊
成分 | 含量(重量%) |
(1)“制备例1的浓缩物” | 30.0 |
(2)大豆油 | 25.0 |
(3)维生素E | 20.0 |
(4)麦胚油 | 15.0 |
(5)甘油脂肪酸酯 | 5.0 |
(6)蜂蜡 | 5.0 |
将各成分充分混合并根据标准程序制成软胶囊。
实施例6-硬胶囊
成分 | 含量(重量%) |
(1)“制备例2的干燥固体物质” | 30.0 |
(2)糖粉 | 45.0 |
(3)糊精 | 24.0 |
(4)甘油脂肪酸酯 | 1.0 |
将各成分充分混合并根据标准程序制成硬胶囊。
例7-可饮用制剂
成分 | 含量(重量%) |
(1)“制备例3的干燥固体物质” | 1.5 |
(2)还原型麦芽糖淀粉糖浆 | 20.0 |
(3)赤藓醇 | 10.0 |
(4)柠檬酸 | 1.0 |
(5)纯水 | 适量 |
将各成分混合并根据标准程序制成可饮用制剂。
实施例8-果冻
成分 | 含量(重量%) |
(1)“制备例3的干燥固体物质” | 0.1 |
(2)糊精 | 24.0 |
(3)帕拉金糖 | 5.0 |
(4)明胶 | 1.0 |
(5)果胶 | 0.5 |
(6)肌醇 | 5.0 |
(7)柠檬酸 | 0.8 |
(8)维生素C | 3.0 |
(9)烟酰胺 | 0.01 |
(10)纯水 | 适量 |
将各成分混合并根据标准程序制成果冻。
实施例9-口香糖
成分 | 含量(重量%) |
(1)“制备例2的干燥固体物质” | 5.0 |
(2)胶基 | 25.0 |
(3)麦芽糖醇 | 45.0 |
(4)甘露醇 | 20.0 |
(5)山梨醇 | 5.0 |
(6)香料 | 1.0 |
(7)纯水 | 适量 |
将各成分根据标准程序制成口香糖。
实施例10-(软糖果)
成分 | 含量(重量%) |
(1)“制备例3的干燥固体物质” | 5.0 |
(2)砂糖 | 34.0 |
(3)淀粉糖浆 | 30.0 |
(4)明胶 | 10.0 |
(5)柠檬酸 | 0.5 |
(6)酒石酸 | 0.3 |
(7)香料 | 1.0 |
(8)纯水 | 适量 |
将各成分充分研磨和混合,并根据标准程序制成胶状糖果。
Claims (4)
1.一种预防紫外线损伤的活性剂,其含有压榨橄榄果实所得的含水部分。
2.一种预防紫外线损伤的活性剂,其含有一种通过使用水和/或有机溶剂对压榨橄榄果实所得的含水部分和固体部分进行提取得到的提取物。
3.一种用于口服给药的组合物,其含有根据权利要求1或2的预防紫外线损伤的活性剂。
4.根据权利要求3的组合物,其中通过使用水和/或有机溶剂对压榨橄榄果实所得的含水部分及固体部分进行提取得到的提取物的含量范围是饮料组合物干重的0.01至70%(重量)。
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US3723487A (en) * | 1970-07-14 | 1973-03-27 | R Couche | Process for extracting oil from palm fruits and olives |
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FR2712463B1 (fr) * | 1994-03-03 | 1996-03-22 | Arkopharma Laboratoires | Jus et suspension de fruits, leur procédé de préparation et leurs applications. |
ES2220090T3 (es) * | 1998-07-23 | 2004-12-01 | Creagri, Inc. | Extracto de aceituna soluble en agua. |
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JP3820218B2 (ja) * | 2000-09-01 | 2006-09-13 | クレアグリ, インコーポレイテッド | 植物水からヒドロキシチロソール富化組成物を得る方法 |
WO2002043736A1 (fr) * | 2000-11-30 | 2002-06-06 | The Nisshin Oillio, Ltd. | Aliments et boissons embellissants et preparations perorales embellissantes |
FR2825022B1 (fr) * | 2001-05-23 | 2005-01-14 | Seppic Sa | Composition de polyphenols d'olives.utilisation comme actif cosmetique et dietetique |
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FR2867071B1 (fr) * | 2004-03-02 | 2006-06-09 | Occitane L | Composition cosmetique ou dermatologique a base d'olive |
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