CN100413512C - 银杏提取物用于增加肌肉质量而减少脂肪质量的用途 - Google Patents
银杏提取物用于增加肌肉质量而减少脂肪质量的用途 Download PDFInfo
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Abstract
本发明涉及银杏提取物、特别是包含20%至30%黄酮苷、总量为2.5%至4.5%的银杏苦内酯A、B、C和J、2%至4%白果内酯、少于10%的原花色素和少于10ppm的烷基酚类化合物的银杏提取物在制备用于在试图通过饮食治疗和/或药物治疗来减轻或增加体重的患者中增加肌肉质量而减少脂肪质量的药物中的用途。
Description
本专利申请涉及银杏(Ginkgo biloba)提取物在制备用于增加肌肉质量而减少脂肪质量的药物中的用途。
肥胖是一个现实的公共健康问题。一些药物确实可刺激体重减轻或增加,但是这种治疗通常使那些体重减轻或增加常常是由肌肉质量与脂肪质量的比例下降而引起的患者变得虚弱。
申请人现已发现:对试图减轻或增加体重的个体施用银杏提取物具有增加肌肉质量而减少脂肪质量的有益效果。此外,申请人还能观察到所述施用可刺激被施用银杏提取物的过重个体体重减轻。
一般而言,本发明涉及银杏提取物在制备用于在试图增加体重和减轻体重的人中治疗体重问题的药物中的用途。
本发明特别涉及银杏提取物在制备用于减轻体重的药物中的用途。根据本发明,在所治疗的个体中,体重减轻为其总体重的至少4%或5%,更优选至少6%、8%或10%。
根据本发明的一个特定变形,银杏提取物可用于制备旨在在试图减轻或增加体重的患者中增加肌肉质量而减少脂肪质量的药物。这些患者可任选地接受饮食治疗和/或其它药物治疗。
换言之,根据本发明,当用银杏提取物联合其饮食治疗或其它药物治疗对试图增加或减轻体重的患者进行治疗时,比例R倾向于保持稳定或者在大多数情况下倾向于增加,所述的比例R等于患者的肌肉质量Mm除以其总体重Mt。优选在用银杏提取物治疗至少一个月的周期后所获得的增加大于或等于5%,更优选大于或等于6%或8%或10%。
可用于本发明的银杏提取物为至少包含黄酮苷和/或一种或多种银杏苦内酯的银杏提取物。优选地,黄酮苷和/或一种或多种银杏苦内酯在用于制备本发明的药物的银杏提取物中存在的浓度为以重量计至少25%,更优选浓度为以重量计至少30%,还更优选浓度为以重量计至少50%。此外,在本发明所用的银杏提取物中烷基酚类化合物的比例优选少于10ppm,更优选少于5ppm,还更优选少于1ppm。如果适宜,一种或多种银杏苦内酯可被其乙酰化同系物、其烷氧基化同系物或其糖基化同系物(如例如下述的通式(I)化合物)替换。
优选地,用于制备本发明的药物的银杏提取物富含黄酮苷和/或银杏苦内酯。其可以是例如EGb型提取物。根据本发明的另一个变形,用于制备本发明的药物的银杏提取物是任何含有黄酮苷、银杏苦内酯和白果内酯的银杏提取物,例如CP 401型提取物。
EGb型提取物意指其组成或多或少与标准EGb提取物的组成相同的提取物,所述的标准EGb提取物特别是在以下文章中被定义:K.Drieu,La presse médicale,31,1986年9月25日,专门讲述银杏提取物(EGb)的增刊,1455-1457;或欧洲专利EP 431535和EP 431536;因此EGb型提取物特别意指包含20%至30%黄酮苷、总量为2.5%至4.5%的银杏苦内酯A、B、C和J、2%至4%白果内酯、少于10%的原花色素(proanthocyanidine)和少于10ppm(优选少于5ppm,且还更优选少于1ppm)的烷基酚类化合物的银杏提取物,优选包含22%至36%黄酮苷、总量为2.5%至3.5%的银杏苦内酯A、B、C和J、2.5%至3.5%白果内酯、少于8%的原花色素和少于10ppm(优选少于5ppm,且还更优选少于1ppm)的烷基酚类化合物的银杏提取物,特别是包含约24%黄酮苷、总量为3.1%的银杏苦内酯A、B、C和J、2.9%白果内酯、6.5%原花色素和少于1ppm的烷基酚类化合物的银杏提取物。
CP 401型提取物所指的提取物如美国专利5,389,370中给出的那些提取物,特别是包含总量为5.5%至8%的银杏苦内酯A、B、C和J、40%至60%黄酮苷和5%至7%白果内酯的银杏提取物,优选包含总量为6.5%至7.5%的银杏苦内酯A、B、C和J、45%至55%黄酮苷和5.5%至6.5%白果内酯的银杏提取物,非常特别的是包含总量为约7%的银杏苦内酯A、B、C和J、50%黄酮苷和6%白果内酯的提取物。
根据本发明的一个变形,一种或多种银杏苦内酯中至少一部分可以被通式(I)化合物替换,
其中W、X、Y和Z独立地表示H、OH、直链或支链烷氧基或O-Gs基团,其中Gs-OH表示单糖或双糖,或者其衍生物或类似物之一,条件是:W、X、Y或Z中至少一个表示O-Gs基团。
优选地,上述通式(I)化合物为这样的化合物,其中:X表示OH或O-Gs基团,其中Gs-OH表示单糖或双糖,或者其衍生物或类似物之一,并且:
-W表示OH或O-Gs基团,Y表示H,且Z表示H;
-或者W表示OH或O-Gs基团,Y表示OH或O-Gs基团,且Z表示H;
-或者W表示OH或O-Gs基团,Y表示OH或O-Gs基团,且Z表示OH或O-Gs基团;
-或者W表示OH或O-Gs基团,Y表示H,且Z表示OH或O-Gs基团;
-或者W表示H,Y表示OH或O-Gs基团,且Z表示OH或O-Gs基团;
-或者W表示OH或O-Gs基团,Y表示直链或支链烷氧基,且Z表示H。
对于通式(I)化合物的制备,本领域技术人员可参考PCT专利申请WO98/52959或美国专利6.143.725。
根据本发明的一个方面,患者需减轻体重。在这种情况下,银杏提取物可以例如与含奥利司他的药物(例如)、含西布曲明或其可药用盐之一的药物(例如)、含绿茶的水醇提取物的药物(例如或)或含来自绿茶的水醇提取物的药物(例如)或者与任何其它用于刺激体重减轻的药物组合施用于患者。根据本发明,优选银杏提取物与含奥利司他的药物(例如)、含西布曲明或其可药用盐之一的药物(例如)组合施用。然而,当欲减轻的体重较少(例如小于或等于总体重的5%,或者小于或等于总体重的10%)时,患者可以除了接受为他开具的饮食治疗外仅接受银杏提取物。
因此,本发明还涉及包含至少一种以上所述的银杏提取物与至少一种选自奥利司他、西布曲明或其可药用盐之一、绿茶的或来自绿茶的水醇提取物的化合物的组合、在治疗体重过重中同时、分别或在一段时间中使用的产品。
同时治疗使用在本申请中意指以相同途径且在同一时间施用多种活性成分。分别使用在本申请中特别意指在大约相同的时间以不同的途径施用多种活性成分。在一段时间中治疗使用在本申请中意指在不同的时间施用多种活性成分,且特别意指其中活性成分之一的所有施用在其它一种或多种活性成分开始施用前进行的施用方法。因此,活性成分之一在施用其它一种或多种活性成分之前可施用数月。在这种情况下,不存在同时治疗。
根据本发明的另一方面,患者需增加体重。在这种情况下,银杏提取物可以与药物如胡芦巴(例如)或任何其它用于刺激体重增加的药物组合施用于患者。然而,当欲增加的体重较少(例如小于或等于总体重的5%,或者小于或等于总体重的10%)时,患者可以除了接受为他开具的饮食治疗外仅接受银杏提取物。
因此,本发明还涉及包含至少一种以上所述的银杏提取物与葫芦巴的组合、在治疗体重过轻中用于同时、分别或在一段时间中使用的产品。
根据本发明,需减轻或增加体重的患者可以是动物或人。在可使用本发明的动物中,可特别提及的是狗、猫、牛、羊、家禽(鸡、火鸡、鸭等)或马。优选患者为人。
包含银杏提取物的药物组合物可以是固体形式,例如散剂、颗粒剂、片剂、明胶胶囊剂、脂质体、栓剂或贴剂。适宜的固体载体可以是例如磷酸钙、硬脂酸镁、滑石粉、糖、乳糖、糊精、淀粉、明胶、纤维素、甲基纤维素、羧甲基纤维素钠、聚乙烯吡咯烷酮和蜡。
包含银杏提取物的药物组合物也可以是液体形式,例如溶液剂、乳剂、混悬剂或糖浆。适宜的液体载体可以是例如水、有机溶剂如甘油或乙二醇以及它们在水中各种比例的混合物。
本发明的药物的施用可通过局部、口服、胃肠外途径或通过注射(肌内、皮下、静脉内等)等进行。
根据提取物中活性成分的浓度和待治疗个体体重问题的严重程度,所拟定的银杏提取物的日剂量为0.1mg至10g。最终决定将由主治医生或兽医作出。
术语“约”是指所考虑的值附近的区间。本申请中所用的“约X”表示X-10%X至X+10%X的区间,优选X-5%X至X+5%X的区间。
除非特别指出,此处所用的所有技术和科学术语的含义与本发明所属领域的专业人员通常理解的含义相同。相似地,此处所提及的所有出版物、专利申请、所有专利和所有其它参考资料均引入作为参考。
为了证明在治疗体重问题中使用上述银杏提取物的益处,可进行下述试验。也可以进行其它旨在例如测定身体组成且特别是脂肪质量与非脂肪质量比例的试验(参见Chumlea等人,Nutrition,Health & Aging,1(1),7-12)以得到相同结果。
药理学部分
用或不用EGb 761治疗的老年大鼠体重发展的对比测定:
由于被豢养,老年试验大鼠有体重增加的自然趋势。组建两组老年(22个月)Wistar大鼠,一组由11只接受正常饮用水5周的大鼠组成,另一组由12只接受含75mg/kg标准银杏提取物EGb的饮用水的大鼠组成。在开始治疗前和治疗结束后将大鼠进行称重。
所得结果:
i)对大鼠体重进行测定产生以下结果:
未经治疗的老年大鼠 | 经治疗的老年大鼠 | |
22个月时的平均体重(g) | 605.64 | 594.10 |
22个月加5周时的平均体重(g) | 619.33 | 570.11 |
换言之,在几周时间内,未经治疗的大鼠体重增加了2.2%,而经治疗的大鼠体重减轻了4%。
ii)此外,最重要的是还观察到经治疗的大鼠肌肉重量与总体重的比例为0.53,而未经治疗的大鼠为0.42。
Claims (10)
1. 至少包含黄酮苷和/或一种或多种银杏苦内酯的银杏提取物在制备用于治疗体重问题的药物中的用途,其特征在于所制备的药物用于增加肌肉质量而减少脂肪质量。
2. 权利要求1的用途,其特征在于黄酮苷和/或一种或多种银杏苦内酯在用于制备药物的银杏提取物中存在的浓度为以重量计至少25%。
3. 权利要求1的用途,其特征在于银杏提取物包含以重量计为20%至30%的黄酮苷、以重量计总量为2.5%至4.5%的银杏苦内酯A、B、C和J、以重量计为2%至4%的白果内酯、以重量计少于10%的原花色素和少于10ppm的烷基酚类化合物。
5. 权利要求4的用途,其特征在于通式(I)化合物为这样的化合物,其中:X表示OH或O-Gs基团,其中Gs-OH表示单糖或双糖,或者其衍生物或类似物之一,并且:
-W表示OH或O-Gs基团,Y表示H,且Z表示H;
-或者W表示OH或O-Gs基团,Y表示OH或O-Gs基团,且Z表示H;
-或者W表示OH或O-Gs基团,Y表示OH或O-Gs基团,且Z表示OH或O-Gs基团;
-或者W表示OH或O-Gs基团,Y表示H,且Z表示OH或O-Gs基团;
-或者W表示H,Y表示OH或O-Gs基团,且Z表示OH或O-Gs基团;
-或者W表示OH或O-Gs基团,Y表示直链或支链烷氧基,且Z表示H。
6. 权利要求1的用途,其特征在于银杏提取物包含总量为5.5%至8%的银杏苦内酯A、B、C和J、40%至60%黄酮苷和5%至7%白果内酯。
8. 权利要求7的用途,其特征在于通式(I)化合物为这样的化合物,其中:X表示OH或O-Gs基团,其中Gs-OH表示单糖或双糖,或者其衍生物或类似物之一,并且:
-W表示OH或O-Gs基团,Y表示H,且Z表示H;
-或者W表示OH或O-Gs基团,Y表示OH或O-Gs基团,且Z表示H;
-或者W表示OH或O-Gs基团,Y表示OH或O-Gs基团,且Z表示OH或O-Gs基团;
-或者W表示OH或O-Gs基团,Y表示H,且Z表示OH或O-Gs基团;
-或者W表示H,Y表示OH或O-Gs基团,且Z表示OH或O-Gs基团;
-或者W表示OH或O-Gs基团,Y表示直链或支链烷氧基,且Z表示H。
9. 权利要求1至8之一的用途,其特征在于所制备的药物的预期使用患者为试图减轻体重的人。
10. 权利要求1至8之一的用途,其特征在于所制备的药物的预期使用患者为试图增加体重的人。
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FR02/08941 | 2002-07-16 | ||
FR0208941A FR2842425B1 (fr) | 2002-07-16 | 2002-07-16 | Utilisation d'extraits de ginkgo biloba pour favoriser la masse musculaire au detriment de la masse graisseuse |
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CN1668321A CN1668321A (zh) | 2005-09-14 |
CN100413512C true CN100413512C (zh) | 2008-08-27 |
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CN (1) | CN100413512C (zh) |
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KR100920648B1 (ko) * | 2007-10-22 | 2009-10-07 | 한림대학교 산학협력단 | 징코라이드 에이를 유효성분으로 포함하는 비만 치료 및 예방용 조성물 |
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EP0493151A1 (fr) * | 1990-11-28 | 1992-07-01 | L'oreal | Composition amincissante à base de ginkgo biloba en tant qu'alpha-2 bloqueurs |
CN1235784A (zh) * | 1999-01-18 | 1999-11-24 | 包德圻 | 心脑血康饮食 |
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DE3338995A1 (de) * | 1983-10-27 | 1985-05-09 | Dr. Willmar Schwabe GmbH & Co, 7500 Karlsruhe | Bilobalid enthaltende arzneimittel |
IT1239281B (it) * | 1989-10-27 | 1993-10-19 | Indena Spa | Composizioni per la riduzione dei depositi di grasso superfluo a base di principi attivi di origine vegetale ad attivita' agonista dell'adenilato ciclasi o/e ad attivita' antifosfodiesterasica |
DE3940094A1 (de) * | 1989-12-04 | 1991-06-06 | Montana Ltd | Wirkstoffkonzentrate und neue wirkstoff-kombinationen aus blaettern von ginkgo biloba, ein verfahren zu ihrer herstellung und die wirkstoff-konzentrate bzw. die wirkstoff-kombinationen enthaltenden arzneimittel |
DE3940091A1 (de) * | 1989-12-04 | 1991-06-06 | Schwabe Willmar Gmbh & Co | Extrakt aus blaettern von ginkgo biloba, verfahren zu seiner herstellung und den extrakt enthaltende arzneimittel |
FR2763592B1 (fr) * | 1997-05-20 | 1999-07-16 | Sod Conseils Rech Applic | Nouveaux derives glycosyles des ginkgolides, leur application en tant que medicaments et compositions pharmaceutiques les contenant |
US6340482B1 (en) * | 2000-05-18 | 2002-01-22 | Zhishin, Llc | Methods for inducing weight loss in a human with materials derived from Citrus varieties |
FR2788438B1 (fr) * | 1999-01-14 | 2003-10-03 | Arkopharma Laboratoires | Composition pour le traitement de l'obesite et procede de traitement esthetique |
IT1314199B1 (it) * | 1999-10-20 | 2002-12-06 | Ambros Pharma S R L | Composizioni contenenti sostanze ad attivita' adrenergica ed estrattivegetali per il trattamento del sovrappeso e obesita' |
JP4719372B2 (ja) * | 2000-06-21 | 2011-07-06 | 花王株式会社 | Ppar依存的遺伝子転写活性化剤 |
JP2003012527A (ja) * | 2001-06-29 | 2003-01-15 | Takeda Food Products Ltd | 過食抑制剤 |
FR2827518B1 (fr) * | 2001-07-17 | 2005-07-08 | Sod Conseils Rech Applic | Utilisation d'extraits de ginkgo biloba pour preparer un medicament destine a traiter la sarcopenie |
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2002
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- 2003-07-15 JP JP2004526943A patent/JP2005538127A/ja active Pending
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EP0493151A1 (fr) * | 1990-11-28 | 1992-07-01 | L'oreal | Composition amincissante à base de ginkgo biloba en tant qu'alpha-2 bloqueurs |
CN1235784A (zh) * | 1999-01-18 | 1999-11-24 | 包德圻 | 心脑血康饮食 |
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EP1523321B1 (fr) | 2009-12-02 |
NZ536917A (en) | 2006-08-31 |
FR2842425A1 (fr) | 2004-01-23 |
CA2492021A1 (fr) | 2004-02-19 |
RU2317094C2 (ru) | 2008-02-20 |
ATE450267T1 (de) | 2009-12-15 |
KR20050021479A (ko) | 2005-03-07 |
ES2336786T3 (es) | 2010-04-16 |
CN1668321A (zh) | 2005-09-14 |
FR2842425B1 (fr) | 2005-04-08 |
AU2003273444A1 (en) | 2004-02-25 |
AU2003273444B2 (en) | 2010-05-20 |
EP1523321A1 (fr) | 2005-04-20 |
RU2005104118A (ru) | 2005-08-10 |
CA2492021C (fr) | 2011-08-30 |
US20050202107A1 (en) | 2005-09-15 |
PL208255B1 (pl) | 2011-04-29 |
JP2005538127A (ja) | 2005-12-15 |
PL374841A1 (en) | 2005-11-14 |
DE60330345D1 (de) | 2010-01-14 |
PT1523321E (pt) | 2010-02-22 |
WO2004014405A1 (fr) | 2004-02-19 |
KR101118778B1 (ko) | 2012-03-20 |
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