Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
  • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
  • A61K9/7007—Drug-containing films, membranes or sheets
• • 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
  • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
• • 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
  • A61P11/06—Antiasthmatics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P19/00—Drugs for skeletal disorders
  • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• • 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
  • A61P25/04—Centrally acting analgesics, e.g. opioids
• • 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
  • A61P25/06—Antimigraine agents
• • 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
  • A61P25/08—Antiepileptics; Anticonvulsants
• • 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
  • A61P25/28—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
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
  • A61P25/32—Alcohol-abuse
• • 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
  • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
  • A61P25/34—Tobacco-abuse
• • 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
  • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
  • A61P25/36—Opioid-abuse
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P27/00—Drugs for disorders of the senses
  • A61P27/02—Ophthalmic agents
  • A61P27/06—Antiglaucoma agents or miotics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect

Definitions

• Film-like mucoadhesive dosage forms for the administration of cannabxs active ingredients are provided.
• the present invention relates to film-like, mucoadhesive dosage forms which contain cannabis active ingredients and are suitable for the administration of cannabis active ingredients for therapeutic purposes.
• the invention further extends to the use of the dosage forms mentioned for the treatment of disease states in humans or animals.
• the ingredients of the Indian hemp plant (Cannabis sativa L.) have a variety of pharmacological effects, of which the psychotropic effect is best known.
• cannabis ingredients also have anti-emetic, anti-convulsive, muscle relaxant, analgesic, sedative, and appetite-increasing effects.
• cannabis ingredients with good efficacy can be used to treat insomnia, neuralgia, painful rheumatism and gastrointestinal disorders.
• a beneficial therapeutic effect of cannabis active ingredients has also been observed in the following indications:
• Painful conditions in cancer and as a result of chemotherapy Pain and wasting syndrome in AIDS; Nausea and vomiting as a side effect of chemotherapy, as well as with AIDS or hepatitis; Neuropathic pain; Anorexia or cachexia, especially in the case of AIDS or advanced cancer; Paralysis in multiple sclerosis or traumatic cross-sectional diseases; Dystonic movement disorders; Bronchial asthma; epileptic seizures or generalized epilepsy; Withdrawal symptoms with alcohol, benzodiazepine and opiate addiction; Parkinson disease; Dementia diseases, in particular Alzheimer's disease; Nausea; Arthritis; Glaucoma; Migraine; Dysmenorrhea.
• cannabis extracts and cannabis oils for therapeutic treatment purposes can also be considered. It is usually administered orally, e.g. in the form of capsules.
• Cannabis extracts or oils contain as pharmacologically active ingredients tetrahydrocannabinol (predominantly ⁇ -9-tetrahydro-cannabinol, to a lesser extent: ⁇ -8-tetrahydrocannabinol), cannabidiol, cannabinol and cannabichromes. These active ingredients are also referred to as cannabinoids (see overview "The Merck Index", 12th edition, 1996, p.285, No. 1794, and S.1573, No. 9349).
• This object is achieved by a film-like, mucoadhesive dosage form containing at least one active ingredient from the group of cannabis active ingredients according to claim 1; further preferred embodiments are described in the subclaims.
• the object is further achieved by using the film-like, mucoadhesive dosage forms according to the invention in the treatment of diseases or disease symptoms.
• the dosage forms according to the invention are applied to the oral mucosa, preferably in the form of thin sheets or wafer-shaped structures, where they remain adherent due to their mucoadhesive properties.
• the application on the oral mucosa is preferably sublingual or buccal.
• other mucosal surfaces can also be considered as the application site, e.g. B. the nasal mucosa.
• the cannabis active ingredient (s) contained in the dosage form is / are released to the surrounding saliva and subsequently resorbed by the oral mucosa (i.e. transmucosal).
• the active ingredient can also be released directly from the dosage form to the mucous membrane.
• the dosage form absorbs saliva and the active ingredient it contains is diffused to the outside.
• the active substance is released into the saliva after a very short delay, so that the saliva-active substance mixture can immediately reach all areas of the oral mucosa and be resorbed there.
• the amount of saliva in which the released active ingredient is dissolved or dispersed per unit of time is relatively small and there is no excessive salivation. flow, so that ingestion of the active ingredient (with the disadvantages of gastrointestinal absorption mentioned) is largely excluded.
• the dosage forms according to the invention also increase compliance, since a special discipline is not required for the application.
• the application of the film-like dosage forms is generally not perceived as disruptive by the people to be treated due to the small layer thickness.
• the dosage forms according to the invention have a polymer matrix which serves as an active substance reservoir and has mucoadhesive properties. At least one layer or at least one surface of the dosage form has mucoadhesive properties.
• the dosage form can consist of a single layer or comprise several layers. In the case of a multilayer structure, at least one of the layers contains active substance.
• a dosage form is made up of a mucoadhesive, preferably single-layer polymer matrix, which contains one or more cannabis active ingredients.
• the active ingredient (s) can be present in the dosage form in dissolved, dispersed or emulsified form.
• the polymer matrix preferably contains one or more polymers which are water-soluble and / or swellable in aqueous media.
• the choice of such polymers can influence the mucoadhesive properties and the release behavior.
• Polymers from the following group are particularly suitable as water-soluble or swellable polymers: starch and starch derivatives, dextran; Cellulose derivatives, such as carboxymethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl ethyl cellulose, sodium carboxymethyl cellulose, ethyl or propyl cellulose;
• the polymer content is preferably 5 to 95 wt. -5s, particularly preferably 15 to 75 wt.%, Based on the dry matter of a dosage form.
• the dosage forms according to the invention contain a cannabis extract or a cannabis oil, preferably in a proportion of 0.5 to 50% by weight, particularly preferably in a proportion of 1 to 30
• the invention also encompasses dosage forms of the type mentioned which contain at least one cannabinoid active ingredient from the group consisting of tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromes.
• Tetrahydrocannabinol in particular R- (6a, 10a) - ⁇ -9-tetrahydro-cannabinol, is particularly preferred as the active ingredient.
• the cannabinoid active ingredients can be of natural, semi-synthetic or synthetic origin.
• the active substance content is preferably 0.1 to 20% by weight, particularly preferably 0.5 to 10% by weight, based on the dry mass of a dosage form.
• a single presentation Form preferably contains 0.5 to 20 mg, particularly preferably 1 to 10 mg of active ingredient, e.g. B. Tetrahydrocannabinol.
• the dosage forms according to the invention can optionally contain one or more additives from the following groups: fillers, colorants, flavors, aromas, fragrances, emulsifiers, plasticizers, sweeteners, preservatives, permeation-promoting substances, pH regulators and antioxidants. Substances suitable for this are known in principle to the person skilled in the art.
• flavors, smells and aromas are particularly advantageous.
• the taste impression can be improved by adding a refreshing flavoring agent (eg menthol, eucalyptol).
• a refreshing flavoring agent eg menthol, eucalyptol.
• this enables the drug to be taken inconspicuously, since it smells like an ordinary refreshment candy. This also helps to improve compliance.
• the dosage forms according to the invention containing cannabis active ingredients are in film form, ie of thin and flat shape, for example in the form of thin platelets or small wafers (also referred to as “wafers”). These film-shaped platelets can have various geometrical shapes, for example circular, elliptical or elongated.
• the thickness is preferably 0.01 to 2 mm; it is particularly preferably in the range from 0.05 to 0.5 mm.
• the layer thickness should be as small as possible (preferably less than 0.2 mm).
• the dosage forms according to the invention can be constructed in two or more layers.
• the individual layers can differ with regard to one or more of the following parameters: polymer composition, active substance content, active substance concentration, content of additives.
• the dosage forms according to the invention containing cannabis active ingredients can advantageously be used in the treatment of diseases or symptoms of the disease, in particular in the case of: painful conditions in cancer and as a result of chemotherapy; Pain and wasting syndrome in AIDS; Nausea and vomiting, in particular nausea and vomiting as a side effect of chemotherapy, as well as in AIDS or hepatitis; Neuropathic pain; Anorexia or cachexia, particularly in the case of AIDS or advanced cancer; Symptoms of paralysis in multiple sclerosis or traumatic cross-sectional diseases; Dystonia movement disorders; Bronchial asthma; epileptic seizures or generalized epilepsy; Withdrawal symptoms of alcohol, benzodiazepine and opiate addiction; Parkinson disease; Dementia, especially Alzheimer's disease; Arthritis; Glaucoma; Migraine; Dysmenorrhea.

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• Health & Medical Sciences (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Neurosurgery (AREA)
• Neurology (AREA)
• Biomedical Technology (AREA)
• Addiction (AREA)
• Pain & Pain Management (AREA)
• Psychiatry (AREA)
• Epidemiology (AREA)
• Ophthalmology & Optometry (AREA)
• Hospice & Palliative Care (AREA)
• Pulmonology (AREA)
• Rheumatology (AREA)
• Nutrition Science (AREA)
• Physiology (AREA)
• Psychology (AREA)
• Reproductive Health (AREA)
• Endocrinology (AREA)
• Otolaryngology (AREA)
• Immunology (AREA)
• Orthopedic Medicine & Surgery (AREA)
• Physical Education & Sports Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)
• Medicines Containing Plant Substances (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

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• 2002
  • 2002-06-14 DE DE10226494A patent/DE10226494A1/de not_active Withdrawn
• 2003
  • 2003-05-08 CA CA002489106A patent/CA2489106A1/en not_active Abandoned
  • 2003-05-08 US US10/517,849 patent/US20060039959A1/en not_active Abandoned
  • 2003-05-08 AU AU2003227735A patent/AU2003227735B2/en not_active Ceased
  • 2003-05-08 WO PCT/EP2003/004807 patent/WO2003105800A2/de not_active Ceased
  • 2003-05-08 JP JP2004512706A patent/JP4526384B2/ja not_active Expired - Fee Related
  • 2003-05-08 CN CN038137291A patent/CN1658840A/zh active Pending
  • 2003-05-08 BR BR0311867-3A patent/BR0311867A/pt not_active IP Right Cessation
  • 2003-05-08 RU RU2005100953/15A patent/RU2324476C2/ru not_active IP Right Cessation
  • 2003-05-08 EP EP03725174A patent/EP1513494A2/de not_active Withdrawn
• 2004
  • 2004-12-13 IL IL16574404A patent/IL165744A0/xx unknown

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