CN1233184A - 具有抗微生物活性的药品和化妆品制剂 - Google Patents

具有抗微生物活性的药品和化妆品制剂 Download PDF

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CN1233184A
CN1233184A CN97198872A CN97198872A CN1233184A CN 1233184 A CN1233184 A CN 1233184A CN 97198872 A CN97198872 A CN 97198872A CN 97198872 A CN97198872 A CN 97198872A CN 1233184 A CN1233184 A CN 1233184A
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CN1114436C (zh
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E·鲍姆巴戴利
P·默拉佐尼
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    • 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)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/005—Antimicrobial preparations
    • 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)
    • 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)
    • A61K36/38—Clusiaceae, Hypericaceae or Guttiferae (Hypericum or Mangosteen family), e.g. common St. Johnswort
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin

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Abstract

本发明涉及新的具有抗微生物活性的药品和化妆品制剂,其含有a)克雷默属植物亲水性提取物,或得自该提取物的纯化合物,和b)铁力木亲水性提取物。

Description

具有抗微生物活性的药品和化妆品制剂
本发明涉及新的具有抗微生物活性的药品和化妆品制剂，其含有a)克雷默属植物亲水性提取物，或得自该提取物的纯化合物，和b)铁力木亲水性提取物。
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EP0464297B1所述，可以用色谱技术从这些提取物中回收纯净组分Eupomatenoid6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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
本发明涉及一种组合物，其中含有具有抗微生物活性的--克雷默属植物，优选Krameria triandra亲水性提取物，或来自所述提取物的纯化合物，和--铁力木(Mesua ferrea)亲水性提取物。
“来自克雷默提取物的纯化合物”是指亲木脂体如Eupomatenoid6和2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃。
本发明人意外地发现所述组合物在1∶10至10∶1的比例范围优选1∶1的比例，能够起到单个提取物的抗微生物活性的协同作用，这是预先未能想见的。
本发明的组合物也可作为防腐剂用于食品和化妆品工业。因此，本发明还涉及食品或化妆品制剂，其含有作为防腐剂的：
a)克雷默属植物，优选Krameria triandra亲水性提取物，或来自
所述提取物的纯化合物，和
b)铁力木亲水性提取物。
本发明还涉及：a)克雷默属植物，优选Krameria triandra亲水性提取物，或来自所述提取物的纯化合物，和b)铁力木亲水性提取物用作食品或化妆品制剂的防腐剂的用途。
下表显示了两种例举的提取物的体外抗微生物活性的平均值，提取物分别由Krameria triandra和铁力木制得，以1∶1的比例组合而成。
所述活性以M.I.C.表示，用本领域熟炼技术人员已知的常规方法进行测定。表--Krameria triandra和铁力木标准化提取物的体外抗微生物活性。微生物菌株                      M.I.C.μg/ml
                        Ⅰ    Ⅱ   Ⅲ   Ⅳ金黄色葡萄球菌MPR5          6.1   4    2    1金黄色葡萄球菌ATCC6538      12    7    3    0.5金黄色葡萄球菌F2ISF3        9     15   4    --表皮葡萄球菌HCF Berset C    10    8    4    --表皮葡萄球菌CPHL            8     6    3    1feaecalis葡萄球菌LEP Br       10     6    2    16大肠杆菌CNUR1                ＞128 ＞128  32   0.51乙酸钙不动杆菌OSMPV           6.2    4    2    2铜绿假单胞菌CNUR4             6      4.3  1    32须发癣菌193                   128    61   12   2白假丝酵母ATCC10231           62.5   128  12   2脆弱拟杆菌                    26     16   4    32疮疱丙酸杆菌                  4      4    1    32Ⅰ=按实施例2制备的Krameria triandra提取物，Ⅱ=按实施例1制备的铁力木提取物，Ⅲ=Krameria friandra和铁力木的1∶1组合物，Ⅳ=芦氟沙星(抗细菌)，咪康唑(抗真菌)。
因此，本发明涉及含有上述组合成分的可局部施用的具有微生物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 Pharmaceuti cal 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。
下列实施例将更详细地介绍本发明。实施例1--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。实施例2--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％Eupematenoid6和14％2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃。实施例3--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；合并已烷提取物，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。

Claims (10)

1．具有抗微生物活性的药品和化妆品制剂，其含有：a)克雷默属植物，优选Krameria triandra亲水性提取物，或来自所述提取物的纯化合物，和b)铁力木亲水性提取物。
2．根据权利要求1的制剂，其中克雷默提取物与铁力木提取物的比例是1∶10至10∶1。
3．根据权利要求2的制剂，其中的比例是1∶1。
4．根据权利要求1的制剂，其中来自克雷默提取物的纯化合物是Eupomatenoid6和2-(2,4-二羟基苯基)-5-丙烯基-苯并呋喃。
5．a)克雷默属植物，优选Krameria triandra亲水性提取物，或来自所述提取物的纯化合物，和
b)铁力木亲水性提取物用于制备具有抗微生物活性的药物的用途。
6．根据权利要求5的用途，其中来自克雷默提取物的纯化合物是Eupomatenoid6或2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃。
7．食品或化妆品制剂，其中含有作为防腐剂的a)克雷默属植物，优选Krameria triandra亲水性提取物，或来自所述提取物的纯化合物，和b)铁力木亲水性提取物。
8．根据权利要求7的制剂，其中来自克雷默提取物的纯化合物是Eupomatenoid6或2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃。
9．a)克雷默属植物，优选Krameria triandra亲水性提取物，或来自所述提取物的纯化合物，和
b)铁力木亲水性提取物用作食品或化妆品制剂的防腐剂的用途。
10．根据权利要求9的用途，其中来自克雷默提取物的纯化合物是Eupomatenoid6或2-(2,4-二羟基苯基)-5-丙烯基苯并呋喃。
CN97198872A 1996-10-17 1997-10-08 具有抗微生物活性的药品和化妆品制剂 Expired - Fee Related CN1114436C (zh)

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ITMI96A002148 1996-10-17
IT96MI002148A IT1284970B1 (it) 1996-10-17 1996-10-17 Formulazioni farmaceutiche e cosmetiche ad attivita' antimicrobica

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NO991740D0 (no) 1999-04-13
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DK0932408T3 (da) 2002-04-22
HUP9904679A2 (hu) 2000-05-28
CZ133099A3 (cs) 1999-08-11
JP2000507609A (ja) 2000-06-20
KR20000049164A (ko) 2000-07-25
SI0932408T1 (en) 2002-04-30
PL332870A1 (en) 1999-10-25
WO1998017294A1 (en) 1998-04-30
NO321146B1 (no) 2006-03-27
AU717765B2 (en) 2000-03-30
CA2268914C (en) 2004-02-10
EP0932408B1 (en) 2002-01-02
ITMI962148A1 (it) 1998-04-17
DE69709886T2 (de) 2002-08-22
HUP9904679A3 (en) 2001-11-28
PL187940B1 (pl) 2004-11-30
ES2170374T3 (es) 2002-08-01
RU2196599C2 (ru) 2003-01-20
IT1284970B1 (it) 1998-05-28
DE69709886D1 (de) 2002-02-28
CA2268914A1 (en) 1998-04-30
CN1114436C (zh) 2003-07-16
SK282410B6 (sk) 2002-01-07
EP0932408A1 (en) 1999-08-04
KR100324860B1 (ko) 2002-02-28
NO991740L (no) 1999-06-10
HK1022278A1 (en) 2000-08-04
CZ289845B6 (cs) 2002-04-17
SK49599A3 (en) 2000-03-13
JP3279321B2 (ja) 2002-04-30

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