CN100566734C - 用于治疗蜂窝组织疾病的口服组合物 - Google Patents
用于治疗蜂窝组织疾病的口服组合物 Download PDFInfo
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- CN100566734C CN100566734C CNB2004800267572A CN200480026757A CN100566734C CN 100566734 C CN100566734 C CN 100566734C CN B2004800267572 A CNB2004800267572 A CN B2004800267572A CN 200480026757 A CN200480026757 A CN 200480026757A CN 100566734 C CN100566734 C CN 100566734C
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Abstract
本发明涉及用于治疗蜂窝组织疾病的包含游离形式或者与磷脂的复合体形式的葡糖提取物、雷公根三萜和二聚银杏类黄酮化合物的口服药物组合物和美容组合物。
Description
本发明涉及用于治疗蜂窝组织疾病(cellulite)的包含植物来源的成分的药物和美容组合物。
更具体而言,本发明涉及用于治疗蜂窝组织疾病的包含作为活性成分的葡糖(Vitis vinifera)提取物、二聚性银杏(Ginkgo biloba)类黄酮化合物和雷公根(Centella asiatica)三萜的药物和美容组合物。
本发明的活性成分为游离形式或者与磷脂复合的形式。
蜂窝组织疾病困扰着很大一部分西方人口并且受其影响人群的百分比日益增加,尤其是女性,包括许多没有肥胖情况的具有正常体重的成年妇女。蜂窝组织疾病指的是一种脂膜病(panniculopathy),其特征为外周循环差、水肿、纤维化和脂细胞代谢改变,并且理想的治疗方法应当考虑所有这些方面。
目前在市场上可以获得许多用于治疗蜂窝组织疾病的药物组合物或美容组合物:其通常是以植物来源的活性成分如常春藤、马栗树(horse-chestnut)或可乐果树(雷公根)提取物、咖啡因、β-肾上腺素能神经刺激物、甲基黄嘌呤等等为基础的。但是,迄今为止,没有证明这些组合物中的任何组合物真的有效并且得到的改善常常是由于通常与使用该组合物有关的饮食方案所导致的,而不是该组合物本身所导致的。
申请人发现,本发明的目的的包含植物来源活性成分的组合的口服药物和/或美容组合物使得可以在蜂窝组织疾病的治疗中获得最佳结果,其显著降低了皮下脂肪的沉积和“橙皮”样皮肤,正是由于采用各种组分不同活性的组合,从而更好地发挥了抗水肿、抗磷酸二酯酶解(antiphosphodiesterasis)和血管运动活性(vasokinetic activity),并且促进了胶原产生。还证明本发明的组合物可有效治疗下肢的静脉机能不全。
本发明组合物中所有的活性成分都是已知的并且已经被用于药物和/或化妆品中;但是,应当注意的是,这些组分表现出协同作用并且单独使用单一活性物质的活性远远低于联合使用这些活性物质所获得的活性。
本发明的组合物每单位剂量可以包含10至500mg葡萄标准化提取物、10至500mg二聚性银杏类黄酮化合物和10至500mg雷公根或等同数量的相应磷脂复合体。
游离形式的组分a)-c)是可通过商业途径获得的。
在欧洲专利275.224中公开了葡糖标准化提取物的磷脂复合体(也被称为“组分a”)。所说的由葡糖籽中所包含的poliphenols组成的提取物包含没食子酸、游离形式或者被没食子酸酯化的儿茶素和表儿茶素单体、二聚物、三聚体、四聚物、五聚物、六聚物和八聚物(eptamers)。
体外和体内研究已经证明,该提取物的抗氧化活性很高(根据实验模型,比维生素E高10至200倍),其使得可以消除大多数活性游离基并抵销其有害作用。此外,该提取物还能抑制黄嘌呤-氧化酶和螯合Cu++和Fe+++,从而防止了组织中酶催化的自由基产生。最后,该葡萄提取物抑制了胶原酶和其它蛋白酶,从而保护了***和皮肤不受皮肤接受UV辐射时和炎性应答过程中所释放出来的蛋白水解酶的有害影响;此外,该提取物还对皮肤和循环结构如微血管(microvessells)和毛细管有选择性亲合力,从而也对循环组织具有保护作用。
在EP 0275005中所述的二聚性银杏类黄酮化合物与磷脂的复合体(也被称为“组分b”)具有与游离形式银杏黄酮二聚物活性相同的活性,但是其使得活性成分的释放延长并且具有更好的生物利用度。由于银杏类黄酮化合物二聚物可以抑制组胺和cAMP磷酸二酯酶从肥大细胞的释放,所以它们是十分有效的作用于血管的活性剂。具体而言,cAMP磷酸二酯酶的抑制使得cAMP水平增加;因为cAMP能激活脂细胞代谢,所以这些复合体发挥了分解脂肪的作用并且改善了微血管灌注和皮肤营养性。
在EP 0283713中对雷公根标准化提取物的磷脂复合体(也被称为“组分c”)进行了描述。这种提取物包含三种对胶原代谢具有高活性的不同分子:积雪草苷、积雪草酸(asiatc acid)和羟基积雪草酸(madecassic acid)的4∶3∶3的混合物。这些分子改善了胶原结构中成纤维细胞对氨基酸的吸收,所说的氨基酸主要是L-脯氨酸和L-羟基脯氨酸,无论从性质还是从数量的观点来看,这两种氨基酸都是胶原结构中最重要的氨基酸。胶原生物合成的改善涉及被降解的老纤维被新纤维的替代加快。
本发明的组合物将以适宜制剂的形式经口服给药,其可以为液体(如糖浆、溶液、混悬液)或固体(如片剂、糖衣小丸、胶囊、咀嚼片)形式。这些制剂将根据常规方法来进行制备,如可以用在“Remington′sPharmaceutical Handbook“,Mack Publishing Co.,NY,USA中所公开的那些方法,使用适宜的赋形剂来进行制备。
在下文给出了一些本发明组合物的实施例。
实施例I:片剂
磷脂复合体葡萄提取物 240mg
二聚性银杏类黄酮化合物的磷脂复合体 100mg
雷公根三萜的磷脂复合体 60mg
交联羧甲基纤维素钠 28mg
二氧化硅 8mg
滑石粉 4mg
实施例II:
葡萄提取物 150mg
银杏二聚类黄酮化合物 100mg
雷公根三萜 10mg
磷酸二钙二水合物 150mg
微晶纤维素 100mg
交联羧甲基纤维素钠 28mg
二氧化硅 8mg
硬脂酸镁 9mg
滑石粉 3mg。
Claims (6)
1.用于治疗蜂窝组织疾病和下肢静脉机能不全的口服组合物,其每单位剂量包含:
a)10-500mg葡萄标准化提取物或其与磷脂的复合体;
b)10-500mg二聚性银杏类黄酮化合物或其与磷脂的复合体;
c)10-500mg雷公根或其与磷脂的复合体,
以及常规的赋形剂和载体。
2.如权利要求1所述的组合物,其中所说的组分a)-c)为游离形式。
3.如权利要求1所述的组合物,其中所说的组分a)-c)是与磷脂的复合体形式。
4.一种下列物质的组合在制备用于治疗蜂窝组织疾病的口服药物或美容组合物中的用途:
a)10-500mg葡萄标准化提取物或其与磷脂的复合体;
b)10-500mg二聚性银杏类黄酮化合物或其与磷脂的复合体,和
c)10-500mg雷公根或其与磷脂的复合体。
5.一种下列物质的组合在制备用于治疗下肢静脉机能不全的药物中的用途:
a)10-500mg葡萄标准化提取物或其与磷脂的复合体;
b)10-500mg二聚性银杏类黄酮化合物或其与磷脂的复合体,和
c)10-500mg雷公根或其与磷脂的复合体。
6.如权利要求1-3中任意一项所述的口服组合物在制备用于治疗蜂窝组织疾病的药物中的用途。
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CN104906153A (zh) * | 2015-06-09 | 2015-09-16 | 邳州鑫源生物制品有限公司 | 一种高效提取银杏黄酮的工艺方法 |
CN104940253A (zh) * | 2015-06-29 | 2015-09-30 | 兰捷 | 一种从银杏叶中提取高纯度总黄酮的方法 |
KR20200115927A (ko) * | 2019-03-29 | 2020-10-08 | 주식회사 유니베라 | 포도잎 추출물 및 병풀 추출물을 포함하는 정맥순환 장애 개선용 조성물 |
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IT1201151B (it) | 1987-01-14 | 1989-01-27 | Indena Spa | Complessi fosfolipidici con estratti da vitis vinifera,procedimento per la loro preparazione e composizioni che li cntengono |
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KR20060101456A (ko) | 2006-09-25 |
DE602004005603D1 (de) | 2007-05-10 |
US7691422B2 (en) | 2010-04-06 |
DK1663267T3 (da) | 2007-07-30 |
IL174353A0 (en) | 2006-08-01 |
AU2004273598A1 (en) | 2005-03-31 |
AU2004273598B2 (en) | 2009-10-08 |
CA2539229C (en) | 2015-07-21 |
ATE357925T1 (de) | 2007-04-15 |
US20060292249A1 (en) | 2006-12-28 |
EP1663267A1 (en) | 2006-06-07 |
DE602004005603T2 (de) | 2008-01-24 |
EP1663267B1 (en) | 2007-03-28 |
KR20110047280A (ko) | 2011-05-06 |
PL1663267T3 (pl) | 2007-08-31 |
PT1663267E (pt) | 2007-06-25 |
ITMI20031789A1 (it) | 2005-03-20 |
KR101186096B1 (ko) | 2012-09-25 |
WO2005027947A1 (en) | 2005-03-31 |
JP2007505850A (ja) | 2007-03-15 |
CN1852726A (zh) | 2006-10-25 |
NO334499B1 (no) | 2014-03-17 |
NO20061223L (no) | 2006-04-19 |
SI1663267T1 (sl) | 2007-06-30 |
ES2285528T3 (es) | 2007-11-16 |
RU2355389C2 (ru) | 2009-05-20 |
CY1106561T1 (el) | 2012-01-25 |
RU2006108386A (ru) | 2006-09-10 |
CA2539229A1 (en) | 2005-03-31 |
JP5537764B2 (ja) | 2014-07-02 |
NZ545972A (en) | 2009-04-30 |
HK1093901A1 (en) | 2007-03-16 |
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