EP1802320A1 - Composition pharmaceutique contenant canscora diffusa - Google Patents

Composition pharmaceutique contenant canscora diffusa

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Publication number
EP1802320A1
EP1802320A1 EP05794094A EP05794094A EP1802320A1 EP 1802320 A1 EP1802320 A1 EP 1802320A1 EP 05794094 A EP05794094 A EP 05794094A EP 05794094 A EP05794094 A EP 05794094A EP 1802320 A1 EP1802320 A1 EP 1802320A1
Authority
EP
European Patent Office
Prior art keywords
pharmaceutical composition
canscora
plant
disorders
composition according
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Withdrawn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
EP05794094A
Other languages
German (de)
English (en)
Inventor
Michael Barthel
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of EP1802320A1 publication Critical patent/EP1802320A1/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Withdrawn legal-status Critical Current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)
    • A61K36/51—Gentianaceae (Gentian family)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Definitions

  • the present invention relates to a pharmaceutical composition containing the plant Canscora diffusa, in the family Gentianaceae, a dosage form containing the composition and the use of the pharmaceutical composition.
  • Canscora decussata is used as a laxative, as a means of general health improvement, and as a general, unspecified nerve tonic.
  • Canscora lucidissima is reportedly used as a medicinal plant in China and Vietnam, but it does not specify what it is for diffusa, there is only one scientific work, in which the isolation of the active ingredient Diffutin, a Glycosyloxyflavan, is listed.
  • the active ingredient diffutin is assigned an "adaptogenic" effect. This is an effect against stress and against anxiety.
  • Canscora decussata contains xanthones C-glycosides, one of which, Magniferin, has anti-inflammatory and "CNS-lowering" effects, but it is not clear what the latter indication means, and it has a fungicidal and a weak effect It also has an anti-Mycobacterium tuberculosis effect and also spermicide in animal studies.
  • Ghosal, S. et al. describe the isolation of the active ingredient diffutin from the plant Canscora diffusa (Ghosal, S. et al .: "Diffutin, a novel adaptogenic glucosyloxyflavan from Canscora diffusa in Journal of Chemical Research, Synopses, 1983, page 330). Also referred to in this article is the "adaptogenic" (anti-stress and anti-anxiety) effect of this plant, which is called the main active ingredient of Canscora.
  • Object of the present invention is to propose new uses of substances or extracts of the plant of the genus Canscora diffusa, (family Gentianaceae).
  • Canscora diffusa is from the Gentianaceae family. It is a narrow, four-leaved annual plant that grows to a normal size of 15 to 60 cm.
  • the stems are quadrangular.
  • the leaves are arranged opposite, the lower ones are elliptical 4x1 cm in size, the upper ones are wider 2.5x1, 6 cm in size. They are dreinervig,
  • the flowers are purple-colored, numerous, two-sexed.
  • the petals are up to 1, 5 cm long. It can bloom all year round. (For more detailed botanical description, see attached copy of botanical books.) It grows well on moist rocks. It has a very wide distribution in tropical Africa, in the tropical areas of Asia, especially in Nepal, India, Sri Lanka, Vietnam, Laos, Thailand, Java, Philippines and tropical Australia.
  • the whole above-ground plant with stalk, leaf and flower without the root is used.
  • an alcoholic or aqueous / alcoholic solution mono-, di- or trihydric alcohols having 1 to 5 C atoms
  • the plant In order to be suitable for the production of the drug, the plant should be obtained from their natural occurrence. Alternatively, it can also be grown and then obtained.
  • the usual methods such. Cleaning, crushing and drying and stabilization method used.
  • drying methods lyophilization should be mentioned in particular.
  • stabilization methods the preservation with 96% ethanol should be mentioned.
  • the alcoholic extract or the trituration with lactose is preferably used at a concentration of 1 nanogram per single dose.
  • the dosage is given as a single dose at intervals of 1 to 12 months, preferably 2-4 months, according to stopping the improvement in the symptoms.
  • compositions containing Canscora diffusa or their use in the use according to the invention are carried out in the usual way by means of common pharmaceutical and technological processes.
  • the extract or the trituration with milk sugar is processed together with suitable pharmaceutically acceptable excipients and carriers to the drug forms suitable for the various indications and application sites.
  • An important systemic administration form is peroral administration as tablets, hard or soft gelatin capsules, dragees, powders, pellets, microcapsules, oblong compresses, granules, chewing gums. Lozenges, chewing gum, sachets or globules.
  • adjuvants for the preparation of pharmaceutical compositions for peroral administration for example, counter sticking and lubricating and release agents, dispersants, such as flame-dispersed silica, disintegrants, such as various types of starch, PVP, cellulose esters as granulating agents, such as waxy and or polymeric substances on Euthragit ® , cellulose or Cremophor ® base used.
  • dispersants such as flame-dispersed silica
  • disintegrants such as various types of starch, PVP
  • cellulose esters as granulating agents, such as waxy and or polymeric substances on Euthragit ® , cellulose or Cremophor ® base used.
  • Antioxidants sweeteners, such as sucrose, xylitol or mannitol, flavoring agents, flavorings, preservatives, ingredients, buffering agents, directing agents; such as microcrystalline cellulose, starch and starch hydrolysates (for example Celutab ®), lactose, polyethylene glycols, polyvinylpyrrolidone and Dicalcimphosphat, lubricants, fillers, such as Lact ⁇ se or starch, binders in the form of lactose.
  • Starches such as wheat or corn or rice starch, cellulose derivatives such as methylcellulose, hydroxypropylcellulose or silica, talc, stearates such as magnesium stearate, aluminum stearate, calcium stearate, talc, siliconized talc, stearic acid, cetyl alcohol, hydrogenated fats, may also be used.
  • Ais Hiifs- or carriers are recordable as sodium alginate as gelling agent for the preparation of a suitable basis or cellulose derivatives, such as guar or xanthan gum, inorganic gelling agents, such as aluminum hydroxides or bentonites (so-called thixotropic gel-forming agent), polyacrylic acid derivatives, such as Carbopol ®, polyvinylpyrrolidone, microcrystalline cellulose or carboxymethyl cellulose. Furthermore, amphiphilic lower and higher molecular weight compounds such as phospholipids come into consideration.
  • the gels can be present either as water-based hydrogels or as hydrophobic organelles, for example based on mixtures of low and high molecular weight paraffin hydrocarbons and vaseline.
  • Suitable emulsifiers are anionic, cationic or neutral surfactants, for example alkali soaps, metal soaps, amine soaps, sulfurized and sulfonated compounds, invert soaps, high coat alcohols, partial fatty acid esters of sorbitan and polyoxyethylene abitans, wool wax, lanolin or other syndthetic products for the preparation of the oil / water and / or or water / oil emulsions.
  • the hydrophilic organogels can be prepared, for example, based on high molecular weight polyethylene glycols. These gel-like shapes are washable.
  • lipids in the form of fatty and / or oil and / or waxy components for the preparation of ointments are vaseline, natural or synthetic waxes, fatty acids, fatty alcohols, fatty acid esters, for example as mono-, di- or triglydeides, paraffin oil or vegetable oils, hydrogenated castor oil or coconut oil, lard, synthetic fat, eg based on caprylic, capric, lauric and stearic acid, or triglyceride mixtures such as Miglycol® used.
  • osmatically effective acids and alkalis e.g. Hydrochloric acid, citric acid, caustic soda, potassium hydroxide, sodium hydrogen carbonate, and also buffer systems, e.g. Citrate, phosphate, Tris buffer or triethanolamine.
  • buffer systems e.g. Citrate, phosphate, Tris buffer or triethanolamine.
  • preservatives e.g. Methyl or Popylbenzoat- (parabens) or sorbic acid are added.
  • topically administrable forms include pastes, powders or solutions.
  • the pastes often contain lyophilic and hydrophilic excipients with a very high proportion of fat as the basis for consistency.
  • the powders or topically applied powders may be used to increase the dispersity and the flow and lubricity and to prevent agglomerates, such as starches, such as wheat or rice starch, flame-dispersed silica or silica, which also serve as a diluent.
  • Particularly suitable as tra ⁇ sdermale systems are patches which, based on various layers and / or mixtures of suitable excipients and carriers, are capable of delivering the active ingredient in a controlled manner over longer or shorter periods of time.
  • the membrane permeation enhancing substances or permeation promoters such as oleic acid, Arzone®, adipic acid derivatives, ethanol, urea, popyl glycol in addition to suitable auxiliaries and carriers, such as solvents, polymeric components , such as based on Eutragit®, into consideration.
  • the patches are preferably applied to the inside of the forearm.
  • injectables can also be administered. These are either in the form of ampoules or as so-called ready-to-use Injektabilia, e.g. as pre-filled syringes or disposable syringes, besides also in vials for multiple removal, prepared.
  • Administration of the injectables may be in the form of subcutaneous (s.c.), intramuscular (i.m.), intravenous (Lv.) Or intracutaneous (i. E.) Administration.
  • the respectively suitable injection forms can be used in particular as solutions, crystal suspensions, nanoparticulate or colloidally disperse systems, such as e.g. Hydrosols.
  • the injectable preparations can also be prepared as concentrates, which can be adjusted with aqueous isotonic diluents to the desired active ingredient dosage. Furthermore, they may also be used as powders, e.g. Lyophilisates are prepared, which are then preferably dissolved or dispersed immediately before administration with suitable diluents.
  • Suitable excipients and carriers in the preparation of the injectable preparations are acqua ste ⁇ lisata, the pH-influencing substances, such as organic and inorganic acids and bases, and their salts, buffer substances for adjusting the pH, isotonizing, such as sodium chloride, sodium bicarbonate , Glucose and fructose, surfactants or surface-active substances and emulsifiers, such as partial fatty acid esters of polyoxyethylene sorbitan (Tween®), or fatty acid esters of polyoxyethylene (Cremophor®), fatty oils, such as peanut oil, soybean oil and castor oil, synthetic fatty acid esters, such as ethyl oleate , Isopropyl myristate and neutral oil (Miglycol®), as well as polymeric auxiliaries, such as, for example, gelatin, dextran, polyvinylpyrrolidone, the solubility-increasing additives of organic solvents, such as,
  • Administration may also be perlingual.
  • Delayed release dosage forms may also be used.
  • composition of the present invention containing Canscora diffusa can be found in many disorders of the central nervous system (CNS), especially in impaired concentration, disturbed nerves, school impairments, school refusal, dyslexia, mental retardation and developmental retardation, speech development delay, confusion states, mental dementia and senile dementia , Alzheimer's disease, in memory impairment, in fragile (X) syndrome, in psychosis, depression, schizophrenia, in affective psychoses, in mania, in hyperkinetic behavioral disorders in children and adults, in hemucinations, in compulsive acts such as Compulsory washing, behavioral abnormalities, anorexia nervosa, listlessness, borderline syndrome, autism, bipolar mood disorders, mental disability, test lamp fever, nightmares, tics, lack of self-confidence.
  • CNS central nervous system
  • the pharmaceutical composition according to the invention with an extract of the plant Canscora diffusa was applied in 274 patients within about 6 to 7 years, of which 106 were female. Among these 274 patients, a clear subjective and objective improvement of the symptoms occurred at 183. For each of the 274 patients, one single dose was used. In the period of the effect of the single dose no other drugs (either internally or externally eg as ointments) were administered, no vitamins, trace elements, minerals, phytotherapeutics, etc., so that the effect alone is attributable to the drug used by Canscora diffusa.
  • the amount of active ingredient was always in the nanogram range or even lower, in the picogram range.
  • a single dose should be given no sooner than 7 weeks.
  • the longest duration of effect was 11 months, that is to say that the symptoms that led to the indication for Canscora diffusa did not return until after 11 months in these patients, so that only then was a single dose necessary.
  • the average duration of a single dose is two to three months.
  • the duration of action of a single dose depends on the severity of the disease. The need for repetition exists only with recurrence of the complaints.
  • the compliance is as high as in the case of the Canscora diffusa-containing pharmaceutical compositions according to the invention.
  • Canscora diffusa containing pharmaceutical composition are significantly lower than comparable psychotropic drugs, such as Ritalin ® (is about 4 to 6 times as expensive), Captagon ® (is about 4 times more expensive), Dogmatil ® (is about 5 times more expensive), Fluctin ® (is about 10 times as expensive), Ludiomil ® (is about 2 times as expensive).
  • comparable psychotropic drugs such as Ritalin ® (is about 4 to 6 times as expensive), Captagon ® (is about 4 times more expensive), Dogmatil ® (is about 5 times more expensive), Fluctin ® (is about 10 times as expensive), Ludiomil ® (is about 2 times as expensive).
  • the invention relates to a pharmaceutical composition containing an active substance obtained from a plant of the genus Canscora in the family Gentianaceae, particularly obtained an active ingredient from a plant "of the type Canscora diffusa.
  • composition of the invention with a content of Canscora can in many disorders in central nervous system, in particular in case of impaired concentration, learning disabilities, at school performance weakness, Schul elaboratesverweigemng, dyslexia, mental retardation and developmental retardation, speech development delay, Verwirmngszuenten, mental dementia and senile dementia, Alzheimer's disease, memory impairment, fragile (X) syndrome, psychosis , Depression, schizophrenia, affective psychoses, mania, anxiety and panic states, hyperkinetic behavioral disorders in children and adults, hallucinations, obsessional behavior such as washing compulsion, behavior sauf Wurkeiten be administered in anorexia nervosa, with listlessness in borderline syndrome, autism, "in bipolar affective disorders, mental disabilities, in fright, in nightmares, with tics, with lack of self-confidence.

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Mycology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une composition pharmaceutique contenant une substance active issue de la plante du genre Canscora dans la famille des Gentianaceae, en particulier une substance issue de la plante de l'espèce Canscora diffusa. La composition selon l'invention, qui présente une teneur en canscora, peut être administrée pour traiter de nombreux troubles du système nerveux central, en particulier des troubles de la concentration, des troubles de l'apprentissage, des difficultés scolaires, le rejet de l'école, la dyslexie, le retard mental, le retard de développement, le retard de développement du langage, les états confusionnels, la démence mentale, la démence sénile, le Morbus Alzheimer, les troubles de la mémoire, le syndrome de l'X fragile, les psychoses, les dépressions, les schizophrénies, les psychoses affectives, les manies, la peur et les états de panique, les troubles du comportement hyperkinétiques chez l'enfant et l'adulte, les hallucinations, les actes compulsifs, par exemple la compulsion de lavage, les comportements inhabituels, l'anorexie mentale, l'apathie, le syndrome borderline, l'autisme, les troubles affectifs bipolaires, les handicaps mentaux, le trac, les cauchemars, les tics, le manque de confiance en soi.
EP05794094A 2004-10-21 2005-10-21 Composition pharmaceutique contenant canscora diffusa Withdrawn EP1802320A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH01740/04A CH699169B1 (de) 2004-10-21 2004-10-21 Pharmazeutische Zusammensetzung, enthaltend Canscora.
PCT/CH2005/000620 WO2006042440A1 (fr) 2004-10-21 2005-10-21 Composition pharmaceutique contenant canscora diffusa

Publications (1)

Publication Number Publication Date
EP1802320A1 true EP1802320A1 (fr) 2007-07-04

Family

ID=34974975

Family Applications (1)

Application Number Title Priority Date Filing Date
EP05794094A Withdrawn EP1802320A1 (fr) 2004-10-21 2005-10-21 Composition pharmaceutique contenant canscora diffusa

Country Status (5)

Country Link
US (1) US20080193567A1 (fr)
EP (1) EP1802320A1 (fr)
JP (1) JP2008516997A (fr)
CH (1) CH699169B1 (fr)
WO (1) WO2006042440A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015127512A1 (fr) * 2014-02-26 2015-09-03 Deakin University Extraits de plante riches en xanthone ou composés dérivés de ceux-ci pour la modulation de maladies du système nerveux central et de troubles associés

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1092296A (zh) 1993-03-05 1994-09-21 吴振耀 一种治疗精神分裂症的中草药

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
SAINI K S ET AL: "NATURALLY OCCURRING FLAVANS UNSUBSTITUTED IN THE HETEROCYCLIC RING", PHYTOCHEMISTRY (OXFORD), vol. 23, no. 11, 1984, pages 2415 - 2422, ISSN: 0031-9422 *
See also references of WO2006042440A1 *

Also Published As

Publication number Publication date
CH699169B1 (de) 2010-01-29
WO2006042440A8 (fr) 2006-06-08
WO2006042440A1 (fr) 2006-04-27
US20080193567A1 (en) 2008-08-14
JP2008516997A (ja) 2008-05-22

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