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)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P11/00—Drugs for disorders of the respiratory 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
• • 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
  • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
  • A61P25/16—Anti-Parkinson drugs
• • 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
• • 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
  • A61P31/12—Antivirals
• • 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
  • A61P31/12—Antivirals
  • A61P31/14—Antivirals for RNA viruses
• • 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
  • A61P31/12—Antivirals
  • A61P31/14—Antivirals for RNA viruses
  • A61P31/18—Antivirals for RNA viruses for HIV
• • 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
  • A61P35/00—Antineoplastic agents
  • A61P35/02—Antineoplastic agents specific for leukemia
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• the present invention relates to the use of extracts or extractives from guaiacum species, which extracts or these extractives cause a phosphodiesterase-4 inhibition, and a process for their recovery.
• the resin obtained by melting the heartwood from Guajacum officinale L. and Guajacum sanctum L. is used.
• the resin is used to prepare preparations based on a mother tincture and liquid HAB 1 dilutions.
• An allopathic reprocessing monograph of Commission E is based on guaiac wood; published in the Federal Gazette 76 of 23 April 1987.
• the area of application is the supportive treatment of rheumatic complaints.
• DE 101 31 036 A1 describes an elixir which contains per 100 grams 70 grams of an alcoholic macerate (15 vol.% Ethanol) of 50 grams of condoorango rind, 0.60 grams of guaiac wood, 0.40 grams of dandelion root with cabbage and 0 , Contains 40 grams of peppermint leaves.
• US Pat. No. 4,774,229 claims a method for the treatment of tumors of the skin of mammals.
• the tumors are treated topically with a novel mixture of a plant extract of the family Zygophyllaceae and a non-alkaline metal halide.
• this invention is based on the idea that, depending on the particular concentration, highly cytotoxic salts of antimony, cadmium, copper and zinc can be converted into complexes with phenolic compounds and thus better applied for the desired applications.
• a dry extract of plant parts of guaiac should be produced, which should be suitable for the supportive treatment of rheumatic complaints in accordance with Commission E's monograph.
• the addition and concentration must be such that during this process, such an alcohol and water concentration is maintained that neither the gum arabic precipitates nor separate the plant extractives contained in the extract.
• the dry extract can be obtained either by conventional spray drying, belt drying or paddle drying of the spissum extract, in particular the post-concentrated spissum extract.
• a fluid extract which was prepared with 80 m / m% ethanol, as a moderate inhibitor of cyclooxygenase I.
• the IC was 5 o value for COXl 30 ug / ml was found.
• Human leukocyte elastase HLE was 50% inhibited at 60 ⁇ g / ml.
• the release of interleukin-1 beta from human macrophages was 50% at 45 ug / ml to 'inhibited.
• the release of interleukin-6 was 50% inhibited at 5 ⁇ g / ml.
• the release of tumor necrosis factor- ⁇ was 50% inhibited at 7 ⁇ g / ml.
• the dry extract prepared according to the method according to the invention was additionally tested in the pharmacological in vitro test system of human phosphodiesterase-5, abbreviated to PDE5, to find out whether the extract has a specificity for one of the phosphodiesterases.
• dry extracts prepared according to the invention apparently inhibit phosphodiesterase-4, and apparently contain at least one extractive agent which inhibits phosphodiesterase-4.
• Sapwood with a cut size of about 1 mm to about 2 mm of Guajacum sanctum L. were extracted at a temperature between 30 0 C and 45 ° C for 2 hours with a mixture of 80 parts by weight of ethanol and 20 parts by weight of water with stirring.
• the weight ratio of drug to extractant mixture was 1: 7.
• the drug thus extracted was separated by stratified filtration.
• the remaining portion of the fluid extract was continuously added to the evaporator until the entire amount of the fluid extract was drawn in and concentrated.
• the spissum extract thus obtained had a light brown color, was free-flowing and of homogeneous consistency.
• This spissum extract was concentrated under vacuum (300 mbar to 20 mbar) and elevated temperature (40 0 C to 55 ° C) to a dry matter content of 45% to 55%.
• the resulting concentrated spissum extract (2 kg with 50% dry matter content) had a light brown color, was thick-flowing and of homogeneous consistency.
• This post-concentrated spissum extract was dried in a dryer under vacuum at a pressure of 150 mbar to 10 mbar and a temperature of 40 ° C to 55 ° C.
• the dry extract prepared according to the invention was dissolved in 90 v / v% ethanol and diluted so that a maximum concentration of 1 v / v% ethanol in Test system resulted.
• the extract thus dissolved was tested for its inhibitory effect in the following concentrations, calculated on the extract without adjuvant:
• Rolipram a specific PDE4 inhibitor
• the dry extract prepared according to the invention was dissolved in 90 v / v% ethanol and diluted so that a maximum concentration of 1 v / v% ethanol resulted in the test system.
• the extract thus dissolved was tested for its inhibitory effect in the following concentrations, calculated on the extract without adjuvant:
• sildenafil a specific PDE5 inhibitor, was comparatively tested for its inhibitory effect in the following concentrations:
• the dry extract or at least one extractant contained therein is suitable for treating diseases in which phosphodiesterase 4 inhibition is therapeutically desirable and effective is to be employed.

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• Health & Medical Sciences (AREA)
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• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
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• General Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Animal Behavior & Ethology (AREA)
• Engineering & Computer Science (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Natural Medicines & Medicinal Plants (AREA)
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• AIDS & HIV (AREA)
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• 2007
  • 2007-07-04 WO PCT/CH2007/000325 patent/WO2008003185A1/de active Application Filing
  • 2007-07-04 JP JP2009516852A patent/JP2009541366A/ja active Pending
  • 2007-07-04 EP EP07763932A patent/EP2035025A1/de not_active Withdrawn
  • 2007-07-04 KR KR1020087030746A patent/KR101170209B1/ko not_active IP Right Cessation
  • 2007-07-04 US US12/227,596 patent/US7914827B2/en not_active Expired - Fee Related

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