EP1603582A1 - Petasite, extrait de petasite et / ou fractions d'extrait de petasite pour le traitement d'etats pathologiques aigus - Google Patents

Petasite, extrait de petasite et / ou fractions d'extrait de petasite pour le traitement d'etats pathologiques aigus

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Publication number
EP1603582A1
EP1603582A1 EP04719396A EP04719396A EP1603582A1 EP 1603582 A1 EP1603582 A1 EP 1603582A1 EP 04719396 A EP04719396 A EP 04719396A EP 04719396 A EP04719396 A EP 04719396A EP 1603582 A1 EP1603582 A1 EP 1603582A1
Authority
EP
European Patent Office
Prior art keywords
petasites
substance
extract
petasin
furanopetasin
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.)
Withdrawn
Application number
EP04719396A
Other languages
German (de)
English (en)
Inventor
Reiner Rittinghausen
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.)
Weber and Weber GmbH and Co KG
Original Assignee
Weber and Weber GmbH and Co KG
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 Weber and Weber GmbH and Co KG filed Critical Weber and Weber GmbH and Co KG
Publication of EP1603582A1 publication Critical patent/EP1603582A1/fr
Withdrawn legal-status Critical Current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)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps

Definitions

  • the present invention relates to the use of at least one substance and / or mixtures of substances selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) for the acute treatment of Diseases include pain, spasms, tension headache, migraines, asthma, colitis, gastrointestinal cramps, biliary colic, psycho-vegetative restlessness, tension, anxiety and / or depression.
  • Petasite extracts are usually isolated from the roots of butterbur and have an antispasmodic and analgesic effect. This effect of butterbur was already known to Hippocrates, Galen and Paracelsus.
  • DE-Al 198 38 848 discloses that petasite extracts are suitable for the treatment of gastrointestinal diseases, asthma, pollinosis, dysmenorrhea, eczema, migraines, psoriasis, high blood pressure and / or for use as an antispasmodic.
  • the pharmaceutical preparations from petasites extract currently used are, in particular, viscous extracts of Rhizoma petasites, i.e. Extracts from the butterbur rootstock, which have an unpleasant, bitter taste.
  • butterbur also contains eremophilans and pyrrolizidine alkaloids.
  • the pyrrolizidine alkaloids have in common the pyrrolizidine backbone. They are common in higher plants worldwide.
  • pyrrolizidine alkaloids and their N-oxides can be found in the genera of petasites.
  • the pyrrolizidine alkaloids contained in the plant parts of the genus Petasites are distinguished by considerable hepatotoxic, carcinogenic and mutagenic, but also cytostatic properties. The toxicity of the
  • SAM al fa Pyrrolizidine alkaloids are bound to certain structural groups, which have the following structural features:
  • Cyclic diesters have the highest toxicity and carcinogenicity.
  • the pyrrolizidine alkaloids are rapidly absorbed after oral intake, their N-oxides only after reduction by the intestinal flora.
  • the pyrrolizidine alkaloids are converted into very toxic pyrrole derivatives by mixed-function oxidases. These are very reactive and alkylate nucleophilic groups of the DNA, such as amino, thiol and hydroxy groups, under physiological conditions.
  • the object of the present invention is to provide new indications for the use of compositions containing petasites.
  • the subject matter of the present invention relates to the use of at least one substance and / or mixtures of substances selected from the group comprising petasin (s), Furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) for the acute treatment of disease conditions including pain conditions, convulsions, tension headache, migraines, asthma, colitis, gastrointestinal cramps, biliary colic, psychovegetables states, states of tension, anxiety and / or depression.
  • s petasin
  • Furanopetasin s
  • eremophilan lactone s
  • petasites extract s
  • s at least one petasites extract fraction
  • At least one substance and / or substance mixture selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) during acute treatment of disease states including pain, spasms, tension headache, migraines, asthma, colitis, gastrointestinal cramps, biliary colic, psychovegetative restlessness, tension, anxiety and / or depression are effective.
  • Acute treatment in the sense of this invention is the administration of at least one of the aforementioned substances and / or mixtures of substances selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least a petasite extract fraction (s) understood to achieve an advantageous pharmaceutical effect at the point in time shortly before, during or after the occurrence of the disease states, without the need for a previous long-term administration which is independent of disease states, ie over several days, weeks or months.
  • “acute treatment” in the sense of this invention the conditions of the disease are alleviated without the need for prophylactic administration and / or long-term treatment that is independent of the conditions of the disease and / or permanent treatment with the aforementioned substances and / or substance mixtures.
  • a “substance mixture” in the sense of this invention is understood to mean at least the combination of two individual substances, for example petasin and eremophilan lactone.
  • “substance mixtures” in the sense of this invention are a petasite extract or petasite extract fraction (s).
  • the administration of the substances and / or substance mixtures which can be administered according to the invention in the case of an acute treatment is a single and / or repeated, time-limited administration which, in contrast to a curative administration, does not have to be started before the crane conditions occur in order to achieve an effect.
  • Another advantage is that acute treatment eliminates permanent stress on the organism. It is furthermore advantageous that accidental effects that occur during long-term use and that can lead to an increase in the dose of the pharmaceutically active substances are reliably avoided by the acute treatment according to the invention.
  • At least one substance and / or substance mixture selected from the group comprising petasin (s), furanopetasin (e), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) can, according to the invention, advantageously be used for the acute treatment of tension headache, migraines, Asthma, colitis, gastrointestinal cramps, biliary colic, psycho vegetative unrulies and / or tension, anxiety, depression and / or seizures can be used. Preference is furthermore given to the use for acute treatment of cramped states of smooth muscles, such as cramps in the hamstring, and furthermore the acute treatment of psychovegetative states of tension.
  • At least one substance and / or substance mixtures are selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fracture action (s) according to the invention as an antispasmodic, spasmolytic and / or analgesic can be used for the acute treatment of disease states, including slime ores, convulsions, tension headaches, migraines, asthma, colitis, gastrointestinal cramps, biliary colic, psycho-vegetative restlessness, tension, anxiety and / or depression.
  • At least one substance and / or substance mixture is selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) for the acute treatment of joint and connective tissue disorders, Polyps, adenomas, gastrointestinal diseases and gastritis of all kinds, colitis, Crohn's disease, thromboembolic diseases as well coronary disease, 'peripheral arterial occlusive diseases, inflammatory coronary arteries, myocarditis, spinal syndrome, back pain, intervertebral disc disease, high blood pressure, headaches, migraines, asthma, allergic rhinitis, skin diseases, Alzheimer's disease, tuberculosis, dysmenorrhea, high blood pressure and / or general pain usable.
  • petasin s
  • furanopetasin s
  • eremophilan lactone s
  • petasites extract /
  • At least one substance and / or mixture of substances selected from the group comprising petasin (s), furanopetasin (e), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) can furthermore be used for the acute treatment of diseases of the joints and the Connective tissue such as arthritis, arthrosis, osteoarthritis, rheumatoid arthritis, chronic polyarthritis, coronary and thromboembolic diseases, for example inflammatory coronary arteries, myocarditis, myocardial infarction, unstable and stable angina pectoris, transient ischemic attack, apoplexy, reversible, defective, ischemic, ischemic, ischemic, ischemic, ischemic, ischemic, ischemic, ischemic, ischemic, ischemic, ischemic, deficit gastrointestinal diseases, for example ulcerative colitis, gastrointestinal
  • Ulcerations exogenous and endogenous damage to the gastrointestinal mucosa, adenomas, for example in the intestine, nose and / or sinuses, skin diseases such as psoriasis and / or eczema can be used.
  • Administration doses of 100 mg, 125 mg, 150 mg, 175 mg, 200 mg, 225 mg, 250 mg, 275 mg, 300 mg, 325 mg, 350 mg, 375 mg, 400 mg, 425 have an effect in the acute treatment of disease states mg 450 mg, 475 mg, 525 mg, 550 mg, 575 mg, 625 mg, 650 mg, 675 mg, 700 mg, 725 mg, 750 mg and / or 775 mg petasites extract and / or petasites extract fraction (s).
  • the doses of administration can also be higher.
  • the respective administration dose for acute treatment is at least 100 mg petasites extract and / or petasites extract fraction (s), preferably at least 150 mg petasites extract and / or petasites extract fraction (s), most preferably at least 200 mg petasites extract and / or petasites extract fraction (s). having.
  • An acute treatment which comprises 100 mg of petasites extract and / or petasites extract fraction (s) as the minimum starting amount as the first administration dose.
  • the minimum starting quantity can be divided into several individual servings. Administration in the form of a single portion is preferred.
  • the individual portions are preferably administered within a short time, preferably within the period of time which is required to swallow several individual portions, usually within a few minutes.
  • Administration doses of ⁇ 100 mg to ⁇ 125 mg,> 125 mg to ⁇ 150 mg,> 150 mg to ⁇ 175 mg, ⁇ 175 mg to ⁇ 200 mg,> 200 mg to ⁇ 225 also have an effect in the acute treatment of disease states mg,> 225 mg to ⁇ 250 mg,> 250 mg to ⁇ 275 mg,> 275mg to ⁇ 300 mg,> 300 mg to ⁇ 325 mg,> 325 mg to ⁇ 350 mg,> 350 mg to ⁇ 375 mg,> 375 mg to ⁇ 400 mg,> 400 mg to ⁇ 425 mg,> 425 mg to ⁇ 450 mg,> 450 mg to ⁇ 475 mg,> 525 mg to ⁇ 550 mg, ⁇ 550 mg to ⁇ 575 mg,> 625 mg up to ⁇ 650 mg,> 650 mg to ⁇ 675 mg,> 675 mg to ⁇ 700 mg, ⁇ 725 mg to ⁇ 750 mg and / or> 750 mg to ⁇ 775 mg petasite extract and / or petasite extract
  • the amounts given relate to an undiluted extract and / or petasite extract fraction (s) which are free from added solvent and / or
  • Extractant is.
  • An “undiluted petasite extract” is an extract which has l 1% by weight of solvent and / or extracting agent.
  • An administration dose is preferably a single dose, but can also be divided into two or more individual portions, wherein the individual portions can comprise the same or different proportions of the administration dose.
  • the aforementioned individual portions are administered according to the invention within a short period of time, preferably within four hours, preferably within two hours, more preferably within one hour and further preferably within 30 minutes.
  • the administration of a single dose is also advantageous.
  • an administration dose of, for example, 200 mg is divided into several individual servings, for example several capsules, the capsules contain, soften the
  • Administration dose is distributed, together the administration dose of at least 200 mg. Administration in the form of a single dose of, for example, 200 mg is also advantageous.
  • High administration doses of, for example, more than 300 mg, such as 450 mg or 650 mg, are preferably divided into two or more individual servings, the total
  • Administration dose is advantageously administered within four hours, preferably within two hours, more preferably within one hour.
  • the administration dose is particularly preferably administered within a few minutes.
  • An acute treatment which comprises 100 mg, 150 mg and / or 200 mg of petasites extract and / or petasites extract fraction (s) as the initial administration dose.
  • the initial administration dose can be divided into one or more individual servings. Administration in the form of a single portion is preferred. Preferably, several individual servings of an administration dose are administered within a short time, preferably within the period of time that is required to swallow several servings, usually within a few minutes. Higher doses, for example 300 mg or 400 mg, are also suitable as the initial administration dose when the disease states actually occur. A dose increase depends on the severity of the illnesses that occur.
  • Disease conditions are achieved when an administration dose of 200 mg petasites extract and / or petasites extract fraction (s) is divided into two individual portions, the first individual portion to be administered being 150 mg and the second individual portion being administered 50 mg, and both individual portions being two hours apart, preferably be administered at intervals of one hour.
  • a good effect in the acute treatment of disease states is also achieved if a single dose of 150 mg, 200 mg or 300 mg petasite extract and / or petasite extract fraction (s) is administered.
  • the administration of two or more administration units within a short time interval preferably at intervals of eight hours, six hours, four hours, three hours, two hours and / or one hour, has an effect in the acute treatment of disease states.
  • Several administration units can also be administered within a shorter period of time, for example within a few minutes.
  • Single doses of 100 mg, 125 mg, 150 mg, 175 mg, 200 mg, 225 mg, 250 mg, 275 mg and / or 300 mg petasite extract and / or petasite extract fraction (s) have an effect in the acute treatment of disease states.
  • the single dose can also be higher.
  • a single dose is understood to mean an administration unit of the substances and / or substance mixtures used according to the invention; a single dose corresponds, for example, to a tablet, a capsule or an individual Unit of administration of another form of preparation.
  • a daily dose is understood to mean the amount of the substances and / or substance mixtures used according to the invention, which is administered per day.
  • the particular single dose for acute treatment particularly advantageously has at least 100 mg petasites extract and / or petasites extract fraction (s), preferably at least 150 mg petasites extract and / or petasites extract fraction (s), most preferably at least 200 mg petasites extract and / or petasites extract fraction (s).
  • Single doses that have an effect in the acute treatment of disease states are> 100 mg to ⁇ 125 mg, ⁇ 125 mg to ⁇ 150 mg,> 150 mg to ⁇ 175 mg,> 175 mg to ⁇ 200 mg, 200 mg to ⁇ 225 mg, ⁇ 225 mg to ⁇ 250 mg,> 250 mg to ⁇ 275 mg and / or ⁇ 275 mg to ⁇ 300 mg petasite extract and / or petasite extract fraction (s). Higher single doses may also be suitable.
  • Daily doses of> 100 mg to ⁇ 225 mg,> 275 mg to ⁇ 475 mg,> 525 mg to ⁇ 575 mg,> 625 mg to ⁇ 750 mg, ⁇ 750 mg to ⁇ 825 mg have an effect in the acute treatment of disease states , ⁇ 825 mg to ⁇ 900 mg and / or> 900 mg to ⁇ 975 mg petasite extract and or petasite extract fraction (s). If necessary, the daily dose can also be higher.
  • Daily doses of 150 mg, 200 mg, 300 mg, 350 mg, 400 mg, 450 mg, 550 mg, 650 mg, 725 mg, 750 mg, 775 mg, 850 mg and / or 925 mg have an effect in the acute treatment of disease states Petasite extract and / or petasite extract fraction (s). If necessary, the daily dose can also be higher.
  • the daily dose for acute treatment of disease states advantageously has> 100 mg to ⁇ 225 mg petasites extract and / or petasites extract fraction (s), preferably> 275 mg to ⁇ 475 mg petasites extract and / or petasites extract fraction (s), particularly preferably> 525 mg to ⁇ 575 mg petasites extract and / or petasites extract fraction (s).
  • the administration dose for the acute treatment of disease states is at least 45 mg petasin (s) and / or furanopetasin (s), preferably at least 90 mg petasin (e) and / or furanopetasin (e), most preferably at least 135 mg petasin (e) and / or furanopetasin (e).
  • the doses of administration can also be higher.
  • High administration doses of petasin (s) and / or furanopetasin (s) of, for example, more than 150 mg can be divided into two or more individual servings.
  • An acute treatment is preferred which comprises 45 mg, 90 mg and / or 135 mg petasin (s) and / or furanopetasin (s) as the initial administration dose.
  • the initial administration dose can be divided into one or more individual servings. Administration in the form of a single portion is preferred.
  • the individual portions of an administration dose are preferably administered within a short time, preferably within the time period which is required to swallow several individual portions, usually within a few minutes.
  • Administration doses> 45 mg to ⁇ 60 mg, ⁇ 60 mg to ⁇ 75 mg,> 75 mg to ⁇ 90 mg,> 90 mg to ⁇ 105 mg,> 105 mg to ⁇ 125 mg have an effect in the acute treatment of disease states ,> 125 mg to ⁇ 150 mg, ⁇ 150 mg to ⁇ 175 mg, ⁇ 175 mg to ⁇ 200 mg, ⁇ 200 mg to ⁇ 225 mg and / or> 225 mg to ⁇ 250 mg petasin (s) and / or furanopetasin (e) have. Higher doses of administration may also be suitable.
  • An administration dose comprising petasin (s) and / or furanopetasin (e) is preferably a single dose, but can also be divided into two or more individual portions, wherein the individual portions can comprise the same or different proportions of the administration dose.
  • the individual doses can also be higher.
  • Single doses of> 45 mg to 60 mg, ⁇ 60 mg to ⁇ 75 mg,> 75 mg to ⁇ 90 mg,> 90 mg to ⁇ 105 mg, ⁇ 105 mg to ⁇ 125 mg, ⁇ 125 mg to ⁇ 150 mg, ⁇ 150 mg to ⁇ 175 mg, ⁇ have an effect in the acute treatment of medical conditions 175mg to ⁇ 200mg,> 200 mg to ⁇ 225 mg and / or ⁇ 225 mg to ⁇ 250 mg petasin (s) and / or furanopetasin (s).
  • the individual doses can also be higher.
  • the daily dose for acute treatment advantageously has> 45 mg to ⁇ 250 mg petasin (s) and / or furanopetasin (e), preferably ⁇ 90 mg to ⁇ 135 mg petasin (s) and / or furanopetasin (e). If necessary, the daily dose can also be higher.
  • Daily doses that are ⁇ 45 mg to ⁇ 60 mg,> 60 mg to ⁇ 75 mg,> 75 mg to ⁇ 90 mg,> 90 mg to ⁇ 105 mg,> 105 mg to ⁇ 125 mg,> 125 mg to ⁇ 150 mg, ⁇ 150 mg to ⁇ 175 mg have an effect in the acute treatment of disease states ,> 175mg to ⁇ 200mg,> 200 mg to ⁇ 225 mg and / or> 225 mg to ⁇ 250 mg petasin (s) and / or furanopetasin (s). If necessary, the daily dose can also be higher.
  • petasin (s) and / or furanopetasin (s) are petasin, isopetasin and / or eremophilan lactone (s).
  • An effect in the acute treatment of medical conditions shows an administration dose that> 45 mg to ⁇ 60 mg,> 60 mg to ⁇ 75 mg,> 75 mg to ⁇ 90 mg, ⁇ 90 mg to ⁇ 105 mg, ⁇ l 05 mg to ⁇ 125 mg, ⁇ 125mg to ⁇ 150mg, ⁇ 150mg to ⁇ 175mg, ⁇ l 75 mg to ⁇ 200 mg, ⁇ 200 mg to ⁇ 225 mg and / or ⁇ 225 mg to ⁇ 250 mg petasin, isopetasin and / or eremophilan lactone (s).
  • the doses of administration can also be higher.
  • the doses of administration can also be higher.
  • the respective administration dose for acute treatment advantageously has at least 45 mg petasin, isopetasin and / or eremophilan lactone (s), preferably at least 90 mg petasin, isopetasin and / or eremophilan lactone (s), most preferably at least 135 mg petasin, isopetasin and / or eremophilan lactone ( e) on.
  • Single doses ⁇ 45 mg to ⁇ 60 mg, ⁇ 60 mg to ⁇ 75 mg, ⁇ 75 mg to ⁇ 90 mg, ⁇ 90 mg to ⁇ 105 mg, ⁇ 105 mg to 125 g, ⁇ have an effect in the acute treatment of disease states 125 mg to ⁇ 150 mg, ⁇ 150 mg to ⁇ 175 mg, ⁇ 175 mg to ⁇ 200 mg,> 200 mg to ⁇ 225 mg and / or ⁇ 225 mg to ⁇ 250 mg petasin, isopetasin and / or eremophilan lactone (s) exhibit.
  • the individual doses can also be higher.
  • the respective individual dose for acute treatment advantageously has at least 45 mg petasin, isopetasin and / or eremophilan lactone (s), preferably at least 90 mg petasin, Isopetasin and / or eremophilan lactone (s), most preferably at least 135 mg petasin, isopetasin and / or eremophilan lactone (s).
  • the daily dose for acute treatment is also advantageously ⁇ 45 mg to ⁇ 250 mg petasin, isopetasin and / or eremophilan lactone (s), preferably ⁇ 90 mg to ⁇ 135 mg
  • Daily doses of ⁇ 45 mg to ⁇ 60 mg, ⁇ 60 mg to ⁇ 75 mg, ⁇ 75 mg to ⁇ 90 mg,> 90 mg to ⁇ 105 mg, ⁇ 105 mg to ⁇ 125 g have an effect in the acute treatment of disease states , ⁇ 125 mg to 150 mg, ⁇ 150 mg to ⁇ 175 mg, ⁇ 175 mg to ⁇ 200 mg,> 200 mg to ⁇ 225 mg and / or ⁇ 225 mg to ⁇ 250 mg petasin, isopetasin and / or eremophilan lactone (e ) exhibit. If necessary, the daily dose can also be higher.
  • the daily dose can also be higher if necessary.
  • the petasites extract or petasites extract extract (s) in the sense of this invention consist of a complex mixture of active ingredients.
  • the petasites extract or petasites extract fraction can comprise sesquiterpenes as active component.
  • the petasite extract which can be used according to the invention can be one or more
  • Petasite extract fractions at least one substance and / or substance mixtures selected from the group comprising petasin (s), furanopetasin (s) and / or eremophilan lactone (s) may be enriched.
  • the effect of the petasite extract by enrichment with certain Petasites extract fraction or petasites extract fractions, petasin (s), furanopetasin (s) and / or eremophilan lactone (s) can be improved.
  • the petasites extract and / or petasites extract fraction can in particular have petasins and / or furanopetasins.
  • Furanopetasin chemovarietusch with furanoeremophilanes such as furanoeremophilane, 9-hydroxy-furanoeremophilane, furanopetasin, 2-senecioyl-furanopetasol, 2-tigloyl-furanopetasol, 2-methlythioacryloyl-fu ⁇ -anophenol.
  • Petasin-Chemovariet with different petasins, which from esters of different acids, like esterified acids: u.a. Angelica acid, cis-3-methylthioacryloylic acid, methacrylic acid, 3-methylcrotonic acid, isobutyric acid with the three isomeric compounds petasol, isopetasol and / or neopetasol.
  • the petasins are preferably selected from the group comprising petasine esters, such as angelica acid, cis-3-methylthioacryloylic acid, methacrylic acid, 3-methylcrotonic acid, isobutyric acid, petasol, isopetasol and / or neopetasol.
  • petasine esters such as angelica acid, cis-3-methylthioacryloylic acid, methacrylic acid, 3-methylcrotonic acid, isobutyric acid, petasol, isopetasol and / or neopetasol.
  • Furanopetasins are preferably selected from the group comprising furanoeremophilanes, such as 9-hydroxy-furanoeremophilane, furanopetasine, 2-senecioyl-furanopetasol, 2-tigloyl-furanopetasol, 2-methylthioacryloyl-furanopetasol and / or eremophilane.
  • Petasite extracts or fractions thereof which can be used according to the invention can contain furanopetasins and little or no petasins. But it is also possible that Petasite extracts or fractions thereof which can be used according to the invention contain petasins and little or no furanopetasins.
  • a petasite extract can be preparatively separated using known separation processes, such as chromatography processes: a) via the molecular size b) via the polarity using adsorption chromatography, such as TLC or HPLC.
  • separation processes such as chromatography processes: a) via the molecular size b) via the polarity using adsorption chromatography, such as TLC or HPLC.
  • Chromatographic separation processes can be based on the chemical-physical
  • chromatographic processes use the adsorption properties of the combination of substances consisting of the separation mixture, mobile phase and adsorbent for separation.
  • the liquid mixture of substances is fractionated in a carrier phase due to the differently intense interaction of its components with an adsorbent, the chromatographic material.
  • the mobile phase flows through the adsorbent (inert or stationary phase).
  • a sample of the mixture is introduced into the mobile phase and transported through the adsorbent.
  • the substance component with the greater affinity for the chromatographic material is retained more strongly.
  • the mobile phase is chosen so that it on the one hand the flow through the adsorbent and others ensure that the adsorbed components are extracted from the chromatographic material.
  • Liquid chromatography is used to separate high-molecular compounds as well as chemically and physically labile, polar and non-volatile substances.
  • the petasite extract has so far been obtained from the rootstock of butterbur. According to WO 00/12107, the petasite extract from plants and / or
  • Parts of plants for example from the plant and / or parts of plants of the genus Petasites.
  • Petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or petasites extract fraction (s) which can be used according to the invention can be obtained from plants, parts of plants and / or plant cells.
  • the petasin (s), furanopetasin (e), eremophilan lactone (s), petasites extract (s) and / or petasites extract fraction (s) can preferably be obtained from plants and / or parts of plants from Petasites hybridus, Petasites albus, Petasites japonicus, Petasites paradoxus, Petasites formosanus , Petasites kablikianus, Petasites tricholobus, Petasites niveus, Petasites amplus, Petasites georgicus, Petasites fragrans and / or Petasites spurius can be obtained, the underground parts of the plants preferably being used to produce the extract.
  • Petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or petasites extract fraction (s) can also be obtained from a transformed plant, parts of plants, and / or plant cells, preferably cultures transformed with Agrobacterium rhizogen, in particular transformed Root hair cultures can be obtained.
  • Sterile shoots or other parts of plants e.g. transform juvenile flower parts of Petasites hybridus with Agrobacterium rhizogenes. This creates transformed root hair cultures. These are cultivated and propagated in a liquid nutrient medium, for example in a fermentor. The cultures release their ingredients, among other things, the desired petasins into the aqueous medium from which they were enriched.
  • the petasite extract obtained by a biogenetic production process can optionally contain pyrrolidine alkaloids and / or opines. It is therefore advantageous to select the culture which best produces the desired petasins and which has the least pyrrolidine alkaloids and / or opines.
  • petasins or generally sesquiterpenes or ingredients can be enhanced with so-called elicitors.
  • the processing i.e. Isolation and enrichment of the petasins from the nutrient medium is carried out by customary methods known to those skilled in the art.
  • Petasite extract (s), fraction (s) thereof, petasin (s) and / or furanopetasin (s) which can be used according to the invention should preferably be free from pyrrolizidine alkaloids and / or opines.
  • the petasite extract has between OO to ⁇ 5 ppm pyrrolizidine alkaloid (s), preferably ⁇ 1 ppm pyrrolizidine alkaloid (e), particularly preferably no pyrrolizidine alkaloid (s).
  • usable petasite extract (s) or fraction (s) thereof have no opines.
  • Opines are formed by various strains of Agrobacterium after transfection of the corresponding plants.
  • the petasite extract or fraction (s) thereof may contain opines.
  • the aim is that the extract which can be used according to the invention has ⁇ O to ⁇ 5% by weight of opine (s), preferably ll% by weight of opine (s), based on the total weight of the extractant-free petasite extract.
  • the petasin (s), furanopetasin (e) and / or eremophilan lactone (s) are obtained synthetically. It is advantageous that synthetically obtained petasin (s), furanopetasin (s) and / or eremophilan lactone (s) have a few, preferably no, pyrrolizidine alkaloids, opines and / or other contaminants.
  • At least one substance and / or substance mixtures are preferably selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) for producing a composition, in particular a pharmaceutical Composition, for the acute treatment of
  • compositions which can be used according to the invention and comprise at least one substance and / or substance mixtures selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or petasites extract fraction (s) can be further pharmaceutically and / or physiologically effective substances, such as trace elements, are added.
  • the pharmaceutical effect of the pharmaceutical composition comprising at least one substance and / or substance mixtures selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (e) and / or
  • petasite extract fraction (s) could also be obtained by adding at least one pharmaceutically and / or physiologically active substance, comprising at least one anti-logistics agent, analgesic, extracts of Chamomilla recutita, Rhizoma Curcumae longae, Rhizoma Curcumae xanthorrhizae, Curcumae xanthorrhiza, Cortex Salicurea, Cortex Salicurea, Salicis daphenoides, Tanacetum parthenium, trace elements, preferably salts of chromium, iron, iodine, copper, cobalt, magnesium, manganese, selenium, zinc, secretolytic, secretomotor, preferably extracts of licorice root, thyme herb, peppermint oil, bronchospasmolytic, preferably extracts of ivy leaves, calendula , Vitamin, preferably vitamin A, B, C, D, E, K, antioxidant, preferably ly
  • the absorption of the pharmaceutical composition according to the invention contained in the gastrointestinal tract can be increased if this composition has at least one emulsifier, such as sodium alkyl sulfate, alkyl sulfonate, alkyl carboxylate, alkyl alcoholate, preferably with an alkyl chain length of C 2 -C 18 ;
  • emulsifier such as sodium alkyl sulfate, alkyl sulfonate, alkyl carboxylate, alkyl alcoholate, preferably with an alkyl chain length of C 2 -C 18 ;
  • Polyethylene glycol fatty alcohol ether at least one ester and ether of polyethylene glycol with higher fatty acids or fatty alcohols and / or polyethylene glycol stearate, particularly preferably cetylstearyl alcohol and / or glycerol-polyethylene glycol ricinoleate. It is advantageous if the absorption is increased that an increased plasma concentration of the active compounds can be achieved within a short time, for example within a few hours, preferably within four hours, more preferably within two or very particularly preferably within one hour. A rapid increase in the plasma concentration leads to a very rapid availability of high concentrations of the active compounds for the organism and thus to the effectiveness of the acute treatment within a short period of time, preferably within four hours, preferably within two hours, more preferably within one hour.
  • a further advantageous embodiment comprises a pharmaceutical composition
  • a pharmaceutical composition comprising at least one substance and / or substance mixtures selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or petasites extract fraction (s) in which the Absorption in the gastrointestinal tract is delayed.
  • Such a composition has the advantage that a larger amount of petasite extract per unit dose can be administered, which is then absorbed over an extended period of time. This makes it possible to achieve a practically constant petasites drug blood plasma level of the pharmaceutically active ingredients of the petasitic extract over a period of at least 12-48 hours, preferably 24 hours, which allows the pharmaceutical composition to be administered twice, preferably once, per day.
  • Suitable substances for this include, in particular, the generally known substances which retard the absorption in the gastrointestinal tract for the release of lipophilic active substances.
  • the absorption-retarding substance selected from the group of paraffins is preferably a paraffin that is solid at room temperature, particularly preferably a hard paraffin.
  • an orally administrable dosage form according to the invention containing petasites extract can be provided with a gastric juice-resistant and / or absorption-delaying layer.
  • Oral administration forms are preferably coated with cellulose acetate phthalate.
  • Delayed dosage forms can be selected from the group comprising coated slow-release forms and / or microencapsulated individual substances, extracts or extract fractions from which the medicinal substance is released with a delay and / or medicinal substances stored in matrixes from which there is a delayed release.
  • a particular disadvantage of the petasite extract is its unpleasant, bitter taste.
  • a dosage form that partially or completely releases the active ingredient in the mouth / throat area is not possible because the taste of the petasitic extract is perceived as extremely unpleasant by the patient and sometimes causes immediate nausea.
  • the bitter, extremely unpleasant taste of petasites or petasites extract can be effectively masked by adding at least one taste-masking substance, the taste-masking substance preferably ethereal oils, essences, aromatic waters, oil sugar, fruit flavors such as strawberry aromas, lemon , Vanilla, and the like, aromatic drug extracts, artificial flavorings, sugar, sweetening polyols, neutral tasting thickeners, cyclodextrins and / or mixtures thereof.
  • the taste-masking substance preferably ethereal oils, essences, aromatic waters, oil sugar, fruit flavors such as strawberry aromas, lemon , Vanilla, and the like, aromatic drug extracts, artificial flavorings, sugar, sweetening polyols, neutral tasting thickeners, cyclodextrins and / or mixtures thereof.
  • the pharmaceutical composition usable according to the invention comprising at least one substance and / or substance mixture selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) can be in a liquid , solid and / or liposomal dosage form.
  • the dosage form is a spray, an aerosol, a foam, a phthalate, a powder, a tablet, a capsule, a soft gelatin capsule, a chewable tablet, a granulate, an ointment, a cream, a gel, a suppository or is a solution for injection.
  • the pharmaceutically active composition that can be used is a spray, an inhalate, a tablet, a capsule, a chewable tablet and / or a granulate.
  • Calendula tinctura / extraction
  • viola tinctura / extraction
  • vitamins preferably vitamin E
  • the oral administration of the substances and / or substance mixtures which can be used according to the invention is selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasite extract (s) and / or at least one
  • Petasite extract fraction (s) particularly preferred.
  • a dosage form of the substances and / or substance mixtures which can be used according to the invention in the form of a spray or an inhalation spray is preferred. It is advantageous with such a form of administration that a spray can be applied to the oral mucosa or an inhalation spray can be administered without having to swallow a solid form of administration. It is also particularly preferred if the pharmaceutical composition according to the invention is in the form of a tablet, capsule, chewable tablet or granulate which comprises the active ingredient in the form of microcapsules and / or is formed from microcapsules.
  • the pharmaceutically active composition that can be used is preferably in solid form, preferably in the form of granules, for oral administration, the substances and / or substance mixtures preferably being absorbed or adsorbed onto carriers.
  • the pharmaceutical composition in the form of granules is preferably easy to swallow without the need to dissolve in a liquid.
  • Such granules can be produced by customary methods known to the person skilled in the art, particularly preferably by means of spray technology.
  • a pharmaceutical composition comprising at least one substance and / or substance mixture selected from the group comprising petasin (s), furanopetasin (s), eremophilan lactone (s), petasites extract (s) and / or at least one petasites extract fraction (s) is very particularly suitable for Acute treatment of disease states including pain, spasms, tension headache, migraines, asthma, colitis, gastric daim cramps, biliary colic, psycho-vegetative restlessness, tension, anxiety and / or depression.
  • the amount of active ingredient of the pharmaceutical composition to be administered orally preferably comprises at least 100 mg petasites extract and / or petasites extract fraction (s), preferably at least 45 mg petasin (s) and / or furanopetasin (s), preferably at least 45 mg petasin, isopetasin and / or eremophilan lactone ( e).
  • s 100 mg petasites extract and / or petasites extract fraction
  • s preferably at least 45 mg petasin (s) and / or furanopetasin (s)
  • s preferably at least 45 mg petasin, isopetasin and / or eremophilan lactone
  • preparation forms given in the following examples have the usual auxiliaries used for the formulation of the respective preparation forms and / or further components customary in galenics in an amount appropriate to the amount of active substance.
  • auxiliaries used for the formulation of the respective preparation forms and / or further components customary in galenics in an amount appropriate to the amount of active substance.
  • the person skilled in the art will adapt these substances to the amount of active substance in the usual way.
  • Example 2 Soft gelatin capsule according to Example 1, with the difference that 125 mg extract from plant leaves are used.
  • Soft gelatin capsule according to Example 1 with the difference that 125 mg extract from extract from root hair cultures transformed with Agrobacterium rhizogen are used.
  • Example 5 corresponds to Example 1, except that 150 mg of extract are used.
  • Example 6 corresponds to Example 2 with the exception that 150 mg of extract are used.
  • Example 7 corresponds to Example 3 with the exception that 150 mg of extract are used.
  • Example 8 corresponds to Example 4 with the exception that 150 mg of extract are used.
  • Example 9 corresponds to Example 1 with the exception that 200 mg of extract are used.
  • Example 10 corresponds to Example 2 with the exception that 200 mg of extract are used.
  • Example 11 corresponds to Example 3 with the exception that 200 mg of extract are used.
  • Example 12 corresponds to Example 4 with the exception that 200 mg of extract are used.
  • Example 13 corresponds to Example 1 except that 45 mg of petasin and / or isopetasin are used.
  • Example 14 corresponds to Example 2 with the exception that 45 mg of petasin and / or isopetasin are used.
  • Example 15 corresponds to Example 3 with the exception that 45 mg of petasin and / or isopetasin extract are used.
  • Example 16 corresponds to Example 4 with the exception that 45 mg petasin and / or isopetasin
  • Extract can be used. Examples 17-20
  • Example 17 corresponds to Example 1, except that 135 mg petasin and / or isopetasin are used.
  • Example 18 corresponds to Example 2 except that 135 mg petasin and / or isopetasin are used.
  • Example 19 corresponds to Example 3 with the exception that 135 mg petasin and / or isopetasin
  • Extract can be used.
  • Example 20 corresponds to Example 4 except that 135 mg petasm and / or isopetasin
  • Extract can be used.
  • Table 1 shows a comparison of the effect of the administration of substances and / or substance mixtures selected from the group comprising petasites extract (s) and / or petasites extract fraction (s) in the acute treatment of migraines compared to a control group which has been given a cured continuous use of a daily dose of 75 for one year mg of petasite extract was administered. It can be seen from Table 1 that a significantly improved effect of petasites extract (s) and / or petasites extract fraction (s) is achieved in the acute treatment of migraines with an administration dose of at least 100 mg.

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Abstract

Utilisation d'au moins une substance et / ou de mélanges de substances choisies dans le groupe constitué par des pétasines, des furanopétasines, des érémophilanelactones, des extraits de pétasite et / ou au moins une fraction d'extrait de pétasite pour le traitement d'états pathologiques aigus comprenant les douleurs, les crampes, les céphalées de tension, les migraines, l'asthme, la colite, les crampes gastro-intestinales, les coliques hépatiques, les états d'agitation psychovégétatifs, les états de tension, l'angoisse et / ou la dépression.
EP04719396A 2003-03-14 2004-03-11 Petasite, extrait de petasite et / ou fractions d'extrait de petasite pour le traitement d'etats pathologiques aigus Withdrawn EP1603582A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10311651A DE10311651A1 (de) 2003-03-14 2003-03-14 Petasites, Petasitesextrakt und/oder Petasitesextraktfraktionen davon zur Akutbehandlung von Krankheitszuständen
DE10311651 2003-03-14
PCT/EP2004/002544 WO2004080472A1 (fr) 2003-03-14 2004-03-11 Petasite, extrait de petasite et / ou fractions d'extrait de petasite pour le traitement d'etats pathologiques aigus

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EP1603582A1 true EP1603582A1 (fr) 2005-12-14

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WO2011042469A1 (fr) * 2009-10-07 2011-04-14 Reiner Rittinghausen Utilisation d'une composition à base d' érémophilanolides
DE102022115137A1 (de) 2022-06-15 2023-12-21 Weber & Weber Gmbh Zusammensetzung mit hepatoprotektiver Wirkung

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EP0281656B1 (fr) * 1987-03-12 1992-01-29 Plantamed Arzneimittel GmbH Utilisation d'extraits de pétasites pour la préparation d'un médicament pour le traitement de maladies gastro-intestinales
CH690355A5 (de) * 1996-03-28 2000-08-15 Zeller Max Soehne Ag Verwendung von Extrakt aus Petasites hybridus sowie Verfahren und Vorrichtung zur Gewinnung des Extraktes.
DE19838848A1 (de) * 1998-08-26 2000-03-02 Weber & Weber Gmbh & Co Kg Pyrrolizidinalkaloidfreie Petasites enthaltende Zusammensetzung
DE10217939A1 (de) * 2002-04-22 2003-11-13 Weber & Weber Gmbh & Co Kg Verwendung von Petasites enthaltenden Zusammensetzungen zur Behandlung von Krankheitszuständen

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See references of WO2004080472A1 *

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