CN1136859C - 含有克雷默或铁力木植物提取物的药品或化妆品抗痤疮制剂 - Google Patents
含有克雷默或铁力木植物提取物的药品或化妆品抗痤疮制剂 Download PDFInfo
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Abstract
本发明涉及新的具有抗痤疮活性的药品或化妆品制剂,其含有:a)克雷默属植物的抗微生物亲水提取物,或来自所述提取物的纯化合物,和/或铁力木的抗微生物亲水提取物;b)西门木烯酸和/或月桂酸;c)从铁青树、欧洲七叶树、积雪草、榄仁树、洋甘草提取的抗炎性皂甙。
Description
本发明涉及新的具有抗痤疮活性的药品和化妆品制剂,其含有:
a)克雷默属(Krameria)植物特别是垂安达克雷默(Krameria triandra)的抗微生物亲水提取物,或来自所述提取物的纯化合物,和/或铁力木(Mesua ferrea)的抗微生物亲脂提取物;
b)西门木烯酸(Ximeninic acid),其中可以加入或不加入月桂酸;
c)从铁青树(Olax dissitiflora)、欧洲七叶树(Aesculushippocastanum)、积雪草(Centella asiatica)、榄仁树(Terminaliasericea)、洋甘草(Glycyrrhiza glabra)提取的抗炎性皂甙。
先有技术:
从文献(Martindale,“增补药典”(extrapharmacopeia),第28版(1982);Cannizaro,Boll.Soc.Ital.Biol.Sperim、1.22,1964;V.Hoppe,Drogenkunde Bdl Walter De Gruyter Ed.,1975;以及英国专利2.184.353A)中可知用氯代溶剂、脂族醚、酮以及脂族和芳族酯提取富含新木脂体(neolignanes)(特别是Eupomatenoid 6和2-(2,4-二羟基苯基)-5-丙烯基-苯并呋喃)的各种克雷默属植物(优选Krameriatriandra)的根、树皮和叶获得的提取物对革兰氏阳性菌、革兰氏阴性菌、真菌和厌氧菌菌株具有抗微生物活性。
尽管这些提取物可通过用即使是质子性溶剂提取获得,由于其活性化合物的酚类性质,它们实际上是亲水性的。
如EP0464297 B1所述,可以用色谱技术从这些提取物中回收纯净组分欧泊玛替诺(Eupomatenoid)6和2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃。
用非质子溶剂如己烷、二氯甲烷提取铁力木的花,特别是芽,或更好是在二氧化碳存在下在严格的条件下,例如在35-65℃的温度范围,优选于45℃,在110-260bar的压力下,主要是在200bar,提取植物材料,产生一种亲脂性提取物,其含有取代的香豆素和山酮,所得到的提取物特别是对革兰氏阳性菌、革兰氏阴性菌和厌氧菌菌株具有活性,其活性可与从克雷默属Krameria triandra制备的提取物的活性相比拟。
本发明公开
本发明人意外地发现,将某些实际上具有抗微生物活性的植物提取物[所述提取物是从各种克雷默属植物(优选Krameria triandra)、铁力木提取的提取物或纯化合物]与例如西门木烯酸等物质以及皂甙(例如那些可从铁青树、欧洲七叶树、积雪草、榄仁树、洋兰草中提取的皂甙)联合使用,其中可加入或不加入低分子量脂肪酸(如月桂酸、豆蔻酸、异豆蔻酸等),对于治疗痤疮具有很高活性。
这些抗微生物剂与西门木烯酸以及具有抗炎活性的天然化合物的混合物的联合使用能够使痤疮几乎完全消失并能有效地防止痤疮的发展。一个具体的证明有效的联合应用的例子是抗微生物剂与西门木烯酸、月桂酸(塞润榈的亲脂性提取物的主要成分之一)以及皂甙(选自那些可从铁青树、欧洲七叶树、积雪草、榄仁树、洋甘草提取的皂甙,优选从欧洲七叶树和积雪草提取的皂甙)合用。药理学研究
在各种测定联合应用的实例中,表现出的临床效果最好的是混合物中含有0.1-0.5%克雷默属植物Krameria triandra提取物,优选0.2%;0.1-0.5%铁力木提取物,优选0.25%;0.2-1%西门木烯酸,优选0.6%;0.1-0.4%月桂酸,优选0.2%;以及0.35-1%七叶皂苷,优选0.5%。
抗痤疮活性是对30名18岁至35岁的男女患者进行测试而确定的,用0.5cm制剂每天2次连续45天对患者进行处理。用未经处理的面部作为对照。处理结束后,计算丘疹、脓疱、粉刺的数目(A),皮脂浓度(B),脓疱和粉刺渗出物中疮疱丙酸杆菌的存在(C)。
所得结果见下表:治疗 下降%
A B C无 5 2.3 0制剂1(实施例4) 70 13.1 80制剂2(实施例V) 50 12.4 70制剂3* 20 4 20*3制剂中含有西门木烯酸和七叶皂苷β-谷固醇。
因此,本发明涉及含有上述组合成分的可局部施用的具有抗痤疮活性的药品或化妆品制剂(凝胶、软膏、洗剂、乳剂和固体制剂)。所述制剂可按照制药技术领域已知的常规方法制备,如“雷明顿药物手册(Remington’s Pharmaceutical Handbook)”所述,Mack出版公司,美国,纽约;其中可添加适当的赋形剂,特别是抗氧化剂。
下例实施例将更详细地介绍本发明。实施例I——制备铁力木亲脂性提取物。
在5升提取器中,在CO2存在的严格条件下提取1kg研细的铁力木小芽;第一次提取是在34℃和90bar的压力下进行的,使用了约25升二氧化碳;倾析所得的提取物,将植物材料进行第2次提取,将温度升至45℃,压力升至220bar。得到了15.6g非常粘稠的桔黄色油状物。该油状物可就这样直接使用,或用常规化学分离技术进行进一步分离。优选就这样使用提取物。实施例II——制备克雷默属植物Krameria triandra提取物
将2kg研细的Krameria triandra的根皮用丙酮提取3次,每次5升;合并提取物并将其浓缩至小体积,将浓缩液溶于0.8升丙酮∶水1∶1(体积/体积)中。所得悬浮液用0.5升二氯甲烷提取2次,用无水硫酸钠干燥二氯甲烷相,然后浓缩至干。得到85g类红色固体,其含有约26%Eupomatenoid 6和14%2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃。实施例III--用己烷制备铁力木提取物
将1kg研细的铁力木小芽用3升己烷在回流下提取4次;合并己烷提取物,用活性炭(5g)脱色并真空浓缩成油状物。得到14.5g提取物,其可不经进一步分离而使用。实施例IV——制备水/硅乳剂铁力木 0.25g克雷默属植物Krameria triandra 0.2g西门木烯酸 0.60g月桂酸 0.20g18-β甘草次酸 0.50g丙二醇 5.0g可可基(Coccoyl)谷氨酸钠25%溶液 2.0g矿物油和羊毛脂醇 2.5g辛酸辛酯 5.0g豆蔻酸十八烷酯 7.5g十六烷基二甲酮(Dimethycone)共聚醇 2.5g环甲酮(Cyclomethicone)四聚体 5.0g氯化钠 2.0g甘油 2.5gImidurea 0.3g对羟基苯甲酸甲酯 0.1g纯水 适量加重
100.0g实施例V--制备油/水乳剂克雷默属植物Krameria Triandria 0.20g七叶皂苷β谷固醇fitosomaR 0.50g西门木烯酸 0.50g月桂酸 0.20g单硬脂酸甘油酯 3.00gC12-苯果酸烷基酯 7.00g硅油 0.50g聚羧乙烯制剂 0.50g丙烯酸/C10-30丙烯酸烷基酯交联共聚物 0.20g月桂基硫酸钠 1.00g丙二醇 5.00g10%氢氧化钠溶液 1.50gImidurea 0.3g对羟基苯甲酸甲酯 0.1g纯水 适量加至
100.0g实施例VI--油/水乳剂克雷默属植物Krameria Triandria 0.25g七叶皂苷β-谷固醇fitosomaR 0.50g月桂酸 0.20g8-五硬脂酸聚甘油酯和山萮醇和硬脂酸钠月桂酸酯(Nikkhomulese 41-Nikkho) 2.50g山萮醇 1.50g角鲨烷(Squalane) 7.00gTrioctanoine 6.00gPPG-12/SMDI 2.00g丁二醇 5.00g呫吨胶 0.30g防腐剂 适量纯水 适量加至
100.00g
Claims (3)
1.具有抗痤疮活性的药品或化妆品制剂,其含有:
a)用质子性溶剂提取获得的克雷默属植物垂安达克雷默的抗微生物亲水提取物,或来自所述提取物的纯化合物,和/或用非质子性溶剂提取获得的铁力木的抗微生物亲脂提取物;其中得自克雷默提取物的纯化合物是欧泊玛替诺6和2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃;
b)西门木烯酸和月桂酸;
c)从欧洲七叶树提取的抗炎性皂甙;
其中各成分含量如下:--0.1-0.5%的克雷默属植物垂安达克雷默提取物,--0.1-0.5%的铁力木提取物,--0.2-1%的西门木烯酸,--0.1-0.4%的月桂酸,--0.35-1%的七叶皂甙。
2.根据权利要求1的制剂,其含有:--0.2%的克雷默属植物垂安达克雷默提取物,--0.25%的铁力木提取物,--0.6%的西门木烯酸,--0.2%的月桂酸,--0.5%的七叶皂甙。
3.包含下列所有组分的组合物用于制备具有抗痤疮活性的药物的用途:
a)用质子性溶剂提取获得的克雷默属植物垂安达克雷默的抗微生物亲水提取物,或来自所述提取物的纯化合物,和/或用非质子性溶剂提取获得的铁力木的抗微生物亲脂提取物;其中得自克雷默提取物的纯化合物是欧泊玛替诺6和2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃;
b)西门木烯酸,其中可以加入或不加入月桂酸;
c)从欧洲七叶树提取的抗炎性皂甙。
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ITMI96A002149 | 1996-10-17 | ||
IT96MI002149A IT1284971B1 (it) | 1996-10-17 | 1996-10-17 | Formulazioni farmaceutiche e cosmetiche ad attivita' antiacne |
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HK (1) | HK1022277A1 (zh) |
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---|---|---|---|---|
WO2001007031A1 (fr) * | 1999-07-26 | 2001-02-01 | Shionogi & Co., Ltd. | Derives de benzene, compositions immunostimulantes ou agents de retablissement de la pharmacosensibilite les contenant |
KR20010097631A (ko) * | 2000-04-25 | 2001-11-08 | 김국남 | 스킨로션 조성물 |
FR2813194A1 (fr) * | 2000-08-22 | 2002-03-01 | Oreal | Utilisation d'une sapogenine pour traiter les desordres lies a une suractivite de la 5a-reductase |
JP4611565B2 (ja) * | 2001-03-30 | 2011-01-12 | 株式会社ナリス化粧品 | 脂肪合成促進剤および化粧料 |
DE10121090A1 (de) * | 2001-04-26 | 2002-10-31 | Beiersdorf Ag | Wirkstoffkombinationen aus Tetrahydrocurcuminoiden und Sericosid und/oder Pflanzenextrakten |
DE10121092A1 (de) * | 2001-04-26 | 2002-10-31 | Beiersdorf Ag | Kosmetische oder dermatologische Formulierungen mit einem Gehalt an Sericosid und/oder Pflanzenextrakten, dasselbe enthaltend |
DE10232774B4 (de) * | 2002-07-18 | 2004-07-15 | Cognis Deutschland Gmbh & Co. Kg | Kosmetische Zubereitungen mit antibakteriellen Eigenschaften |
EP1402787A1 (en) | 2002-09-27 | 2004-03-31 | Loders Croklaan B.V. | Ximenynic acid |
JP4589663B2 (ja) * | 2004-06-16 | 2010-12-01 | 株式会社マンダム | 抗男性ホルモン剤原料 |
JP5665276B2 (ja) * | 2008-02-27 | 2015-02-04 | 花王株式会社 | 皮膚老化予防又は改善剤 |
EP2268276A1 (en) * | 2008-04-24 | 2011-01-05 | Indena S.p.A. | Compositions for the treatment and prevention of infections of the oral cavity |
DE102008052520A1 (de) * | 2008-10-21 | 2010-04-22 | Cognis Ip Management Gmbh | Kosmetische und/oder pharmazeutische Zubereitungen |
SG185694A1 (en) * | 2010-05-24 | 2012-12-28 | Indena Spa | Tamarind seed polysaccharide for use in the treatment of inflammatory diseases |
CN104203229A (zh) | 2012-03-12 | 2014-12-10 | 皮拉马尔企业有限公司 | 治疗痤疮的方法和抗痤疮制剂 |
CN102949461B (zh) * | 2012-10-25 | 2014-06-11 | 北京华夏众芳生物科技有限公司 | 治疗结节型痤疮的外用中药组合物、制剂及其制备方法 |
JP6815006B2 (ja) * | 2016-11-01 | 2021-01-20 | 株式会社桃谷順天館 | アクネ菌株選択的抗菌剤 |
CN108272740B (zh) * | 2018-03-28 | 2019-03-12 | 湖南御家化妆品制造有限公司 | 组合物及含有该组合物的痤疮修复化妆品 |
CN109010390A (zh) * | 2018-08-20 | 2018-12-18 | 林爵文 | 一种提高男性性功能和治疗性功能障碍的保健品 |
KR102253095B1 (ko) | 2020-11-06 | 2021-05-17 | 주식회사 허브테라피 | 여드름 피부 개선 화장료, 이의 제조방법 및 이를 포함하는 여드름 피부 개선 기능성 화장품 |
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Publication number | Priority date | Publication date | Assignee | Title |
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JPS62126128A (ja) * | 1985-11-27 | 1987-06-08 | Sato Seiyaku Kk | 抗菌剤 |
IT1203515B (it) * | 1987-02-26 | 1989-02-15 | Indena Spa | Complessi di saponine con fosfolipidi e composizioni farmaceutiche e cosmetiche che li contengono |
IT1223290B (it) * | 1987-07-27 | 1990-09-19 | Indena Spa | Acidi poliinsaturi ad azione vasocinetica e relative formulazioni farmaceutiche e cosmetiche |
DK0464297T3 (da) * | 1990-07-05 | 1995-10-09 | Indena Spa | Komplekser af neolignanderivater med phospholipider, anvendelsen deraf samt farmaceutiske og kosmetiske formuleringer indeholdende disse |
GB2274058B (en) * | 1992-11-26 | 1997-06-25 | Eladevi Shah | Herbal Compositions |
JPH0812565A (ja) * | 1994-06-29 | 1996-01-16 | Shiseido Co Ltd | 皮膚外用剤 |
-
1996
- 1996-10-17 IT IT96MI002149A patent/IT1284971B1/it active IP Right Grant
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1997
- 1997-10-07 EP EP97911191A patent/EP0930888B1/en not_active Expired - Lifetime
- 1997-10-07 ES ES97911191T patent/ES2177953T3/es not_active Expired - Lifetime
- 1997-10-07 CA CA002268908A patent/CA2268908C/en not_active Expired - Fee Related
- 1997-10-07 HU HU9904667A patent/HU228300B1/hu not_active IP Right Cessation
- 1997-10-07 RU RU99109992/14A patent/RU2194524C2/ru not_active IP Right Cessation
- 1997-10-07 AT AT97911191T patent/ATE218357T1/de active
- 1997-10-07 CZ CZ19991329A patent/CZ289844B6/cs not_active IP Right Cessation
- 1997-10-07 AU AU48655/97A patent/AU717760B2/en not_active Ceased
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- 1997-10-07 JP JP51888798A patent/JP3725557B2/ja not_active Expired - Fee Related
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- 1997-10-07 PL PL97332861A patent/PL189441B1/pl not_active IP Right Cessation
- 1997-10-07 SK SK496-99A patent/SK282435B6/sk not_active IP Right Cessation
- 1997-10-07 KR KR1019997003258A patent/KR100325317B1/ko not_active IP Right Cessation
- 1997-10-07 WO PCT/EP1997/005510 patent/WO1998017293A1/en active IP Right Grant
- 1997-10-07 CN CNB971988714A patent/CN1136859C/zh not_active Expired - Fee Related
- 1997-10-07 PT PT97911191T patent/PT930888E/pt unknown
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1999
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2000
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