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WO2004087182A1 - Combinaisons de principes actifs d'huiles vegetales contenant des acides gras $g(v)3 et d'extraits vegetaux contenant des isoprenoides et utilisation desdites combinaisons - Google Patents

Combinaisons de principes actifs d'huiles vegetales contenant des acides gras $g(v)3 et d'extraits vegetaux contenant des isoprenoides et utilisation desdites combinaisons Download PDF

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Publication number
WO2004087182A1
WO2004087182A1 PCT/EP2004/003402 EP2004003402W WO2004087182A1 WO 2004087182 A1 WO2004087182 A1 WO 2004087182A1 EP 2004003402 W EP2004003402 W EP 2004003402W WO 2004087182 A1 WO2004087182 A1 WO 2004087182A1
Authority
WO
WIPO (PCT)
Prior art keywords
active ingredient
combination according
ingredient combination
oil
plant extract
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.)
Ceased
Application number
PCT/EP2004/003402
Other languages
German (de)
English (en)
Inventor
Egon Koch
Karl-Heinz Stumpf
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.)
Bioplanta Arzneimittel GmbH
Original Assignee
Bioplanta Arzneimittel GmbH
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 Bioplanta Arzneimittel GmbH filed Critical Bioplanta Arzneimittel GmbH
Priority to EP04724590A priority Critical patent/EP1608389A1/fr
Publication of WO2004087182A1 publication Critical patent/WO2004087182A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/55—Linaceae (Flax family), e.g. Linum
    • 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)
    • A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
    • A61K36/535—Perilla (beefsteak plant)
    • 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)
    • A61K36/72—Rhamnaceae (Buckthorn family), e.g. buckthorn, chewstick or umbrella-tree
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

  • the present invention relates to active ingredient combinations of ⁇ 3 fatty acid-containing vegetable oils and isoprenoid-containing plant extracts with improved tolerability and their use for lowering an elevated blood cholesterol level, for the prevention or treatment of atherosclerosis or coronary heart disease and for the prevention or treatment of a sex hormone-dependent disease.
  • perilla oil contains a very high content of polyunsaturated essential fatty acids. With a share of about 50-60%, the ⁇ -linolenic acid, which belongs to the ⁇ 3 fatty acids, is predominant. It is known from clinical and experimental studies that fatty acids of this type have numerous positive nutritional properties. By feeding perilla oil to rats, the incidence of breast, small and colon cancer was reduced. Anti-inflammatory and anticoagulant effects are also known. A decrease in triglyceride and cholesterol levels in the blood observed in human subjects and an antihypertensive effect are presumably significantly involved in the reduced rate of cardiovascular diseases.
  • perilla oil improves the function of the immune system and increases the ability to learn. Similar positive effects are also for other ⁇ 3-fatty vegetable oils, such as. B. oils from Borago officinalis (borage oil), Oenothera biennis (evening primrose oil) or Ribes nigrum (currant seed oil) as well as for fish oil and linseed oil.
  • Essential fatty acids such as linolenic acid are structural components of numerous cell membranes. Since these fatty acids cannot be synthesized by mammals themselves, they must be supplied with food.
  • eating perilla oil or other vegetable oils containing ⁇ 3 fatty acids can lead to dyspeptic complaints such as belching, bloating, abdominal pain and diarrhea.
  • Another object of the present invention is to provide agents which have an improved cholesterol-lowering effect compared to the use of vegetable oils containing only ⁇ 3 fatty acid. These agents should preferably also have a carminative and taste-correcting effect and promote the secretion of digestive juices.
  • Isoprenoids are a large group of plant substances that are characterized by a common biosynthetic pathway.
  • the basic structure of these secondary metabolites is the isoprene molecule, a C5 body, from which larger molecules such as terpenes and steroids, which are characterized by a wide range of biological effects, are formed by linking.
  • terpenes are the monoterpenes (composed of two isoprene components), such as thymol, menthol or carvone, sesquiterpenes (composed of three isoprene components), diterpenes (composed of four isoprene components), triterpenes (composed of six isoprene components), such as the phytosterols (ß- Sitosterol, Kampesterol, Stigmasterol) and the tetraterpenes (made up of eight isoprene building blocks), like the carotenes.
  • Sesquiterpenes form the largest terpene class and occur in about 50 different structure types. These substances often taste bitter and are contained in numerous plant extracts for the treatment of indigestion. Among other things, they improve gastric juice secretion and increase the formation of bile and the flow of bile. A common cause of bile complaints is an excessively high-fat diet, whereby the need for bile exceeds the stock.
  • Preferred isoprenoid-containing plant extracts according to the present invention are sesquiterpene-containing plant extracts, e.g. B. Extracts from Achillea millefolium (yarrow herb), Artemisia absinthium (wormwood herb), Cnicus benedictus (Benedictine herb), Cynara scolymus (artichoke leaves) and Taraxacum officinale (dandelion).
  • Phytosterols e.g. B. ß-sitosterol, campestrol or stigmasterol, which represent an important subgroup of isoprenoid derivatives, are ingredients of vegetable oils, nuts, seeds, grains, fruits and vegetables. ß-Sitosterol is known to competitively inhibit enteral cholesterol intake from food, thereby lowering blood cholesterol. In people with hypercholesterolemia, existing hypercholesterolemia can therefore be improved by increasing the intake of phytosterols. In addition, the increased consumption of phytosterol-containing products can prevent a pathological increase in blood cholesterol levels.
  • Another aspect of the present invention is therefore to increase the cholesterol-lowering effect by combining ⁇ 3-fatty acid-containing plant extracts, such as perilla oil, with isolated ß-sitosterol or an ß-sitosterol-containing extract, since this combination enables both cholesterol synthesis as well as the cholesterol absorption in the intestine is reduced. Extracts from Hypoxis rooperi, Sabal serrulatum (Serenoa repens) or Cyperus rotundus can preferably be used as plant extracts containing ⁇ -sitosterol.
  • ⁇ 3-fatty acid-containing plant extracts such as perilla oil
  • Extracts from Hypoxis rooperi Sabal serrulatum (Serenoa repens) or Cyperus rotundus
  • ⁇ -sitosterol can preferably be used as plant extracts containing ⁇ -sitosterol.
  • cardiovascular diseases such as B. Atherosclerosis or coronary artery disease is from lowering the Cholesterol levels are
  • Plasma LDL and HDL are the primary source of cholesterol as a precursor to the synthesis of steroid hormones. Lowering the plasma cholesterol level is therefore also expected to have a beneficial effect of the above combination on sex hormone-dependent diseases such as benign prostatic hyperplasia or tumor diseases of the mammary gland, uterus or prostate.
  • Monoterpenes e.g. limonene, perillyl alcohol or geraniol
  • HMG-CoA 3-hydroxy-3-methylglutaryl coenzyme A reductase
  • ⁇ 3-fatty acid-containing vegetable oils can therefore also be combined with monoterpene-containing plant extracts in order to increase the cholesterol-lowering effects of ⁇ 3-fatty acid-containing vegetable oils.
  • Plant extracts are extracts from Acorus calamus (calamus root), Carum carvi (caraway), Cinnamomum aromaticum (cinnamon bark), Crocus sativus (saffron), Curcuma longa (turmeric), Elettaria cardamomum (cardamom), Eucalyptus globulus (eucalyptus vulgaris), Foeniculum ), lllicium verum (star anise), Juniperus communis (juniper berries), Lavandula angustifolia (lavender),
  • Active substance combinations which contain one of the following combinations are preferred: extract from Cynara scolymus and perilla seed oil, extract from Sabal serrulatum and linseed oil, extract from Lavendula angustifolia and linseed oil, extract from Achillea millefolium and borage oil, extract from Cnicus benedictus and borage oil, extract from Zingiber officinale and evening primrose seed oil, extract from Artemisia absinthium and evening primrose seed oil, extract from Salvia officinalis and fish oil, extract from Hypoxis rooperi and fish oil, extract from Cyperus rotundus and currant seed oil, extract from Mentha crispa and currant seed oil, extract from Cinnamomucum oil extract, and perinomalum oil extract globulus and perilla seed oil, extract from Taraxacum officinale and perilla seed oil, extracts from Cynara scolymus (extract containing sesquiterpene) and Sabal serrul
  • antioxidants or radical scavengers such as. B. Vitamin C and E or polyphenol-containing plant extracts to the combinations according to the invention are recommended.
  • the active compound combinations according to the invention are well suited for filling in capsules. If necessary, other substances such.
  • B. partially or fully hydrogenated vegetable oils, beeswax, lecithin, neutral oil, hard fat and highly disperse Siiiciumdioxid be added to the capsule filling mass to adjust the consistency of the mixtures and to prevent segregation of the liquid component and solid plant extract.
  • To the To accelerate the dissolution of the capsule contents released from the capsule can also amphiphilic, surface-active substances and emulsifiers such.
  • B. Sorbitan monooleate can be added.
  • the extracts can be prepared in a variable composition with solvents such as e.g. B. water, methanol, ethanol, 2-propanol, acetone, etc. and their mixtures at temperatures from room temperature to 100 ° C with gentle to vigorous mixing or by percolation within 10 minutes to 24 hours under normal pressure or elevated pressure become.
  • solvents such as e.g. B. water, methanol, ethanol, 2-propanol, acetone, etc.
  • further concentration steps can be carried out, e.g. B. liquid-liquid distribution with z. B. 1-butanol / water or ethyl acetate / water, adsorption-desorption on ion exchanger, LH20, HP20 and other resins or chromatographic separations via RP18, silica gel, etc.
  • the further processing to dry extracts is carried out according to methods known per se by removing the solvent at elevated temperature and / or reduced pressure.
  • a plant extract is mixed with an oil containing ⁇ 3 fatty acids and, if appropriate, with the addition of auxiliaries such as. B. stabilizers, fillers, etc., filled into capsules.
  • auxiliaries such as. B. stabilizers, fillers, etc.
  • the plant extract is mixed with the oil (both according to the table below) and the flowable suspension obtained is filled into capsules using a suitable method.
  • the combination described in the previous example is distinguished by the fact that it maintains the positive physiological effects of the ⁇ 3-fatty acid-containing oil and by the presence of the sesquiterpene-containing oil. extract may counteract possible dyspeptic complaints when this product is taken orally by an increased production of bile.
  • the combination described in the previous example is distinguished by the fact that the inhibitory effect of the ⁇ 3-fatty acid-containing oil on the synthesis of gholesterin and the inhibitory effect of the sitosterol-containing extract on the intestinal absorption of gholesterin have an increased cholesterol-lowering effect compared to the individual components is achieved.
  • the combination described in the preceding example is characterized in that the inhibitory effect of the ⁇ 3-fatty acid-containing oil and the monoterpene-containing plant extract on the synthesis of gholesterin results in an increased cholesterol-lowering effect compared to the individual components.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biotechnology (AREA)
  • Medical Informatics (AREA)
  • Epidemiology (AREA)
  • Mycology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Microbiology (AREA)
  • Botany (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La présente invention concerne des combinaisons de principes actifs d'huiles végétales contenant des acides gras omega 3 et d'extraits végétaux contenant des isoprénoïdes présentant une compatibilité améliorée et l'utilisation desdites combinaisons dans l'abaissement d'une cholestérolémie élevée, dans la prévention ou le traitement d'une athérosclérose ou d'une cardiopathie coronaire ainsi que dans la prévention ou le traitement d'une maladie associée à une hormone sexuelle.
PCT/EP2004/003402 2003-04-02 2004-03-31 Combinaisons de principes actifs d'huiles vegetales contenant des acides gras $g(v)3 et d'extraits vegetaux contenant des isoprenoides et utilisation desdites combinaisons Ceased WO2004087182A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP04724590A EP1608389A1 (fr) 2003-04-02 2004-03-31 Combinaisons de principes actifs d'huiles vegetales contenant des acides gras omega-3 et d'extraits vegetaux contenant des isoprenoides et utilisation desdites combinaisons

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10315024.2 2003-04-02
DE10315024A DE10315024A1 (de) 2003-04-02 2003-04-02 Wirkstoffkombination aus ω3-fettsäurehaltigen Ölen mit isoprenoidhaltigen Pflanzenextrakten und deren Verwendung

Publications (1)

Publication Number Publication Date
WO2004087182A1 true WO2004087182A1 (fr) 2004-10-14

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PCT/EP2004/003402 Ceased WO2004087182A1 (fr) 2003-04-02 2004-03-31 Combinaisons de principes actifs d'huiles vegetales contenant des acides gras $g(v)3 et d'extraits vegetaux contenant des isoprenoides et utilisation desdites combinaisons

Country Status (3)

Country Link
EP (1) EP1608389A1 (fr)
DE (1) DE10315024A1 (fr)
WO (1) WO2004087182A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104707105A (zh) * 2015-03-11 2015-06-17 范志民 一种治疗乳腺增生病的中药制剂及其制备方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104187627B (zh) * 2014-08-11 2016-03-02 无限极（中国）有限公司 一种降血脂组合物及其在制备具有降血脂功能的保健食品中的应用

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US67706A (en) * 1867-08-13 baumann
US964538A (en) * 1910-03-31 1910-07-19 Thomas W Nichols Composition of matter for making soft soap.
GB455978A (en) * 1935-04-30 1936-10-30 Hidezo Kimura Preparation of a remedy for skin diseases and other purposes
GB487855A (en) * 1936-09-21 1938-06-21 Thurstan Wyatt Dickenson Improvements in and relating to stable emulsions of water with liquid or liquefiablesubstances which are immiscible with water, and to preparations comprising the same,and to methods of making the said emulsions and preparations, and to applications ofthe said emulsions and preparations, and to articles of manufacture, or structures, when comprising, or treated with, the said emulsions or preparations
WO1999062356A1 (fr) * 1998-06-03 1999-12-09 Wayne Coates Supplement dietetique pour l'homme
WO2001042455A1 (fr) * 1999-12-08 2001-06-14 California Institute Of Technology Evolution dirigee de voies de biosynthese et de biodegradation
US20040038952A1 (en) * 2000-12-13 2004-02-26 Janos Feher Pharmaceutical compositions for treatment of digestive disorders and associated diseases

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US67706A (en) * 1867-08-13 baumann
US964538A (en) * 1910-03-31 1910-07-19 Thomas W Nichols Composition of matter for making soft soap.
GB455978A (en) * 1935-04-30 1936-10-30 Hidezo Kimura Preparation of a remedy for skin diseases and other purposes
GB487855A (en) * 1936-09-21 1938-06-21 Thurstan Wyatt Dickenson Improvements in and relating to stable emulsions of water with liquid or liquefiablesubstances which are immiscible with water, and to preparations comprising the same,and to methods of making the said emulsions and preparations, and to applications ofthe said emulsions and preparations, and to articles of manufacture, or structures, when comprising, or treated with, the said emulsions or preparations
WO1999062356A1 (fr) * 1998-06-03 1999-12-09 Wayne Coates Supplement dietetique pour l'homme
WO2001042455A1 (fr) * 1999-12-08 2001-06-14 California Institute Of Technology Evolution dirigee de voies de biosynthese et de biodegradation
US20040038952A1 (en) * 2000-12-13 2004-02-26 Janos Feher Pharmaceutical compositions for treatment of digestive disorders and associated diseases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Health supplement food comprises galenicals, dioscoreae, radix, coix seed, cinnamon, carthamus, polygonati rhizoma and/or perilla extract and die saw, persicae semen, hawthorn, turmeric, ginger and/or liquorice", DERWENT, 2000, XP002191379 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104707105A (zh) * 2015-03-11 2015-06-17 范志民 一种治疗乳腺增生病的中药制剂及其制备方法

Also Published As

Publication number Publication date
EP1608389A1 (fr) 2005-12-28
DE10315024A1 (de) 2004-10-14

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