Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/19—Carboxylic acids, e.g. valproic acid
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/60—Salicylic acid; Derivatives thereof
• • 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
  • A61K9/20—Pills, tablets, discs, rods
  • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
  • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
  • A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P23/00—Anaesthetics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P23/00—Anaesthetics
  • A61P23/02—Local anaesthetics
• • 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
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

• the present invention relates to orally administrable pharmaceutical preparations containing a fixed combination of at least one locally acting analgesic with rapid onset of action and at least one systemically acting analgesic with long-lasting action.
• Local-acting analgesics with rapid onset of action are already known, which e.g. can be used in the form of sprays or lozenges. Such local anesthetics already show their effect after less than a minute, but they only have a short duration of action, so that frequent medication is required, which means an impairment of safety and "patient compliance".
• Particularly interesting local analgesics are e.g. called the benzocaine. They inhibit the formation and conduction of stimuli in nerves by blocking the sodium current.
• NSAIDS acetylsalicylic acid
• ASA acetylsalicylic acid
• Pain relief can be explained by the inhibition of prostaglandin synthesis. With most of these systemic analgesics, the maximum effectiveness is only reached after approx. 1-2 hours.
• the object of the present invention is to satisfy the long-standing
• active analgesics all active substances can be used which show a significant onset of activity in a period of up to 10 minutes, preferably 4 minutes, in particular 1 minute and very particularly 30 seconds.
• the locally acting analgesics are expediently used in amounts of 0.5 to 100 mg, preferably 1 to 60 mg and in particular 2 to 30 mg per individual form of administration.
• the combination according to the invention can be one or more local anesthetics
• ester-like local anesthetics such as benzocaine, amethocaine,
• anilide-like local anesthetics such as lidocaine, butainocaine, bainocaine Mepivacaine, oxethazain, prilocaine, ropivacaine, ethyl p-piperidinoacetyl aminobenzoate, tolycaine,
• Non-steroidal anti-inflammatory agents are preferably mentioned, e.g. Phenylacetic acid derivatives such as aceclofenac, alclofenac, bromfenac, diclofenac, fenclofenac etc., arylacetic acid derivatives such as acemetacin, amfenacsodium, bendazac, glucametacin, oxametacin etc., para
• Aminophenol derivatives such as acetanilide etc., propionic acid derivatives such as alminoprofen, ibuprofen, ketoprofen, flurbiprofen, naproxen, oxaprozin, salicylic acid derivatives such as acetylsalicylic acid (ASS), aluminum ASS and other salts, difiunisal.
• propionic acid derivatives such as alminoprofen, ibuprofen, ketoprofen, flurbiprofen, naproxen, oxaprozin
• salicylic acid derivatives such as acetylsalicylic acid (ASS), aluminum ASS and other salts, difiunisal.
• systemically active analgesics of element B are used according to the invention in amounts of 5 to 1500 mg, preferably 8 to 1000 mg, in particular
• Fast-acting local analgesics are preferably used as element A, the optimal duration of action of which lasts from 0.5 to 120 minutes, preferably from 2 to 60 minutes, in particular from 5 to 30 minutes.
• Systemic analgesics are preferably used as element B, the significant effect of which occurs after 15 minutes and lasts up to 24 hours, preferably those whose effect occurs after 20 minutes and lasts up to 12 hours, in particular up to 8 hours.
• Preferred systemic analgesics are those that have a duration of action of at least 3 hours.
• the combination according to the invention is particularly suitable for the treatment of inflammatory and / or painful diseases of the pharynx, in particular for the treatment of pharyngitis, laryngitis, tonsillitis, stomatitis, gingivitis of different etiology.
• the combination preparation according to the invention is expediently administered orally.
• the combination can be used in customary formulations, the local anesthetic being to be released first and the systemically acting analgesic possibly also being in depot form.
• Examples of such preparations include: kernel-coated tablets, lozenges, chewing gum, hard caramel with a liquid, semi-solid or solid core. They are manufactured using customary methods using common auxiliary substances.
• a tablet with the following composition may be mentioned as an example:
• ASS core tablet
• ASA 500 mg ASA combine with 30 mg ascorbic acid, 75 mg sucrose, 47 mg microcrystalline cellulose, 2 mg saccharin (550 times) and 6 ml orange juice aroma
• the tablet above shows a clear analgesic effect just 2 minutes after ingestion that lasts for more than 3 hours.
• a core tablet with 300 mg naproxen is coated with a coating syrup which contains 500 mg lidocaine.
• This combination preparation shows an effect after 2 minutes and an effect duration of more than 6 hours.

Landscapes

• Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Anesthesiology (AREA)
• Pain & Pain Management (AREA)
• Rheumatology (AREA)
• Biomedical Technology (AREA)
• Neurology (AREA)
• Neurosurgery (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Medicinal Preparation (AREA)

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Publications (1)

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Cited By (4)

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Citations (10)

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• 1997
  • 1997-04-15 DE DE19715594A patent/DE19715594A1/de not_active Withdrawn
• 1998
  • 1998-04-02 CA CA002285979A patent/CA2285979C/en not_active Expired - Lifetime
  • 1998-04-02 PL PL336154A patent/PL190863B1/pl unknown
  • 1998-04-02 HU HU0003636A patent/HU225601B1/hu not_active IP Right Cessation
  • 1998-04-02 ES ES98921419T patent/ES2210754T3/es not_active Expired - Lifetime
  • 1998-04-02 RS YUP-529/99A patent/RS49620B/sr unknown
  • 1998-04-02 AT AT98921419T patent/ATE253919T1/de not_active IP Right Cessation
  • 1998-04-02 CN CNB988041928A patent/CN1177589C/zh not_active Expired - Fee Related
  • 1998-04-02 YU YU52999A patent/YU52999A/sh unknown
  • 1998-04-02 RU RU99124179/15A patent/RU2218180C2/ru active
  • 1998-04-02 WO PCT/EP1998/001926 patent/WO1998046235A1/de not_active Ceased
  • 1998-04-02 DE DE59810166T patent/DE59810166D1/de not_active Expired - Lifetime
  • 1998-04-02 NZ NZ500262A patent/NZ500262A/en not_active Application Discontinuation
  • 1998-04-02 US US09/402,737 patent/US6929805B2/en not_active Expired - Lifetime
  • 1998-04-02 EP EP98921419A patent/EP0979087B1/de not_active Expired - Lifetime
  • 1998-04-02 JP JP54342398A patent/JP2002503221A/ja not_active Ceased
  • 1998-04-02 AU AU74286/98A patent/AU742622B2/en not_active Ceased
  • 1998-04-02 KR KR10-1999-7009433A patent/KR100532647B1/ko not_active Expired - Fee Related
  • 1998-04-02 BR BR9808875-0A patent/BR9808875A/pt not_active Application Discontinuation
  • 1998-04-02 PT PT98921419T patent/PT979087E/pt unknown
  • 1998-04-02 DK DK98921419T patent/DK0979087T3/da active
  • 1998-04-02 TR TR1999/02396T patent/TR199902396T2/xx unknown
  • 1998-04-14 AR ARP980101703A patent/AR012417A1/es active IP Right Grant
• 1999
  • 1999-09-24 NO NO19994663A patent/NO323022B1/no not_active IP Right Cessation

Patent Citations (11)

Non-Patent Citations (2)

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