CN1852726A - 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 PDF

Info

Publication number
CN1852726A
CN1852726A CNA2004800267572A CN200480026757A CN1852726A CN 1852726 A CN1852726 A CN 1852726A CN A2004800267572 A CNA2004800267572 A CN A2004800267572A CN 200480026757 A CN200480026757 A CN 200480026757A CN 1852726 A CN1852726 A CN 1852726A
Authority
CN
China
Prior art keywords
phospholipid
complex
itself
treatment
cellulite
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CNA2004800267572A
Other languages
English (en)
Other versions
CN100566734C (zh
Inventor
E·邦巴尔代利
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Indena SpA
Original Assignee
Indena SpA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Indena SpA filed Critical Indena SpA
Publication of CN1852726A publication Critical patent/CN1852726A/zh
Application granted granted Critical
Publication of CN100566734C publication Critical patent/CN100566734C/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/16—Ginkgophyta, e.g. Ginkgoaceae (Ginkgo family)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Biotechnology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)

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

用于治疗蜂窝组织疾病的口服组合物
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，从而保护了结缔组织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 0 275 005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EP0 283 713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.口服药物组合物，其包含：
a)葡萄标准化提取物或其与磷脂的复合体；
b)二聚性银杏类黄酮化合物或其与磷脂的复合体；
c)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和美容组合物中的用途：
a)葡萄标准化提取物或其与磷脂的复合体；
b)二聚性银杏类黄酮化合物或其与磷脂的复合体，和
c)雷公根或其与磷脂的复合体。
5.一种下列物质的组合在治疗下肢静脉机能不全中的用途：
a)葡萄标准化提取物或其与磷脂的复合体；
b)二聚性银杏类黄酮化合物或其与磷脂的复合体，和
c)雷公根或其与磷脂的复合体。
6.如权利要求1-3所述的美容组合物用于治疗蜂窝组织疾病的用途。
CNB2004800267572A 2003-09-19 2004-09-10 用于治疗蜂窝组织疾病的口服组合物 Expired - Fee Related CN100566734C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT001789A ITMI20031789A1 (it) 2003-09-19 2003-09-19 Composizioni farmaceutiche e cosmetiche per il trattamento
ITMI2003A001789 2003-09-19

Publications (2)

Publication Number Publication Date
CN1852726A true CN1852726A (zh) 2006-10-25
CN100566734C CN100566734C (zh) 2009-12-09

Family

ID=34362407

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB2004800267572A Expired - Fee Related CN100566734C (zh) 2003-09-19 2004-09-10 用于治疗蜂窝组织疾病的口服组合物

Country Status (22)

Country Link
US (1) US7691422B2 (zh)
EP (1) EP1663267B1 (zh)
JP (1) JP5537764B2 (zh)
KR (2) KR20110047280A (zh)
CN (1) CN100566734C (zh)
AT (1) ATE357925T1 (zh)
AU (1) AU2004273598B2 (zh)
CA (1) CA2539229C (zh)
CY (1) CY1106561T1 (zh)
DE (1) DE602004005603T2 (zh)
DK (1) DK1663267T3 (zh)
ES (1) ES2285528T3 (zh)
HK (1) HK1093901A1 (zh)
IL (1) IL174353A0 (zh)
IT (1) ITMI20031789A1 (zh)
NO (1) NO334499B1 (zh)
NZ (1) NZ545972A (zh)
PL (1) PL1663267T3 (zh)
PT (1) PT1663267E (zh)
RU (1) RU2355389C2 (zh)
SI (1) SI1663267T1 (zh)
WO (1) WO2005027947A1 (zh)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT104241B (pt) 2008-10-29 2012-03-06 Stargate Produtos Farmaceuticos Dieteticos E Nutricionais Lda Composições incorporando agentes redutores da celulite e inestetismos associados e formulações que as contêm
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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
IT1201149B (it) * 1987-01-14 1989-01-27 Indena Spa Complessi di bioflavonoidi con fosfolipidi,loro preparazione,uso e composizioni farmaceutici e cosmetiche
IT1203515B (it) 1987-02-26 1989-02-15 Indena Spa Complessi di saponine con fosfolipidi e composizioni farmaceutiche e cosmetiche che li contengono
JP2004517801A (ja) * 2000-04-18 2004-06-17 セテリス・ホールディング・ベスローテン・フェンノートシャップ−アムステルダム（オランダ）−スックルサーレ・ディ・ルガーノ 皮膚のしわの予防または治療に有用な天然抽出物に基づく組成物
AU2002258649A1 (en) 2001-03-30 2002-10-28 Rhodia Inc. Aqeuous suspension of nanoparticles comprising an agrochemical active ingredient
ITMI20011022A1 (it) 2001-05-17 2002-11-17 Indena Spa Composizioni farmaceutiche e cosmetiche contro l'invecchiamento cutaneo
ITMI20031427A1 (it) * 2003-07-11 2005-01-12 Indena Spa Combinazioni di agenti vasoattivi, loro uso in campo farmaceutico e cosmetico e formulazioni che li contengono

Also Published As

Publication number Publication date
KR101186096B1 (ko) 2012-09-25
JP5537764B2 (ja) 2014-07-02
ATE357925T1 (de) 2007-04-15
DE602004005603D1 (de) 2007-05-10
SI1663267T1 (sl) 2007-06-30
WO2005027947A1 (en) 2005-03-31
NO334499B1 (no) 2014-03-17
PL1663267T3 (pl) 2007-08-31
AU2004273598B2 (en) 2009-10-08
US20060292249A1 (en) 2006-12-28
US7691422B2 (en) 2010-04-06
HK1093901A1 (en) 2007-03-16
EP1663267B1 (en) 2007-03-28
DK1663267T3 (da) 2007-07-30
AU2004273598A1 (en) 2005-03-31
CA2539229C (en) 2015-07-21
CA2539229A1 (en) 2005-03-31
ITMI20031789A1 (it) 2005-03-20
EP1663267A1 (en) 2006-06-07
JP2007505850A (ja) 2007-03-15
CY1106561T1 (el) 2012-01-25
PT1663267E (pt) 2007-06-25
NO20061223L (no) 2006-04-19
ES2285528T3 (es) 2007-11-16
KR20060101456A (ko) 2006-09-25
KR20110047280A (ko) 2011-05-06
IL174353A0 (en) 2006-08-01
RU2006108386A (ru) 2006-09-10
CN100566734C (zh) 2009-12-09
NZ545972A (en) 2009-04-30
DE602004005603T2 (de) 2008-01-24
RU2355389C2 (ru) 2009-05-20

Similar Documents

Publication Publication Date Title
US8343557B2 (en) Compositions incorporating agents for reducing cellulite and unaesthetic appearance associated therewith and formulations containing them
AU776037B2 (en) An anti-oxidant preparation based on plant extracts for the treatment of circulation and adiposity problems
CN1293562A (zh) 减轻哺乳动物蜂窝炎的方法
ZA200604097B (en) Composition comprising an aqueous extract of red vine leaves and a blood circulation-improving agent for the treatment of chronic venous insufficiences
Maggioli Chronic venous disorders: pharmacological and clinical aspects of micronized purified flavonoid fraction
US20030157185A1 (en) Topical treatment of neuropathy
US7871647B1 (en) Topical treatment of neuropathy
CA2386770C (en) Composition for the prevention and/or treatment of circulatory disorders, comprising derivatives of l-carnitine and extracts of ginkgo biloba
CN100566734C (zh) 用于治疗蜂窝组织疾病的口服组合物
WO2021064132A1 (en) Treatment of menopausal syndrome and/or symptoms associated with menopause
US20050142235A1 (en) Composition comprising an aqueous extract of red vine leaves and an antithrombotic agent
ITTO20100888A1 (it) Composizioni comprendenti principi attivi di origine vegetale associati o meno a promotori e/o protettori di ossido nitrico per il trattamento e la prevenzione dei deficit erettili e dell'impotenza e per il potenziamento della performance sportiva
RU2414231C1 (ru) Антиоксидантное средство
RO123164B1 (ro) Compoziţie farmaceutică vasculoprotectoare şi utilizarea acesteia în terapia tulburărilor circulatorii

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1093901

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1093901

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20091209

Termination date: 20200910

CF01 Termination of patent right due to non-payment of annual fee