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
  • A61K31/13—Amines
  • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
  • A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
• • 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
  • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• • 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
  • A61K31/13—Amines
  • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
• • 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
  • A61K31/13—Amines
  • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
  • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/47—Quinolines; Isoquinolines
  • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
• • 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
  • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• • 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
  • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• • 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
  • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
• • 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]
  • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
• • 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
  • A61P31/20—Antivirals for DNA viruses
  • A61P31/22—Antivirals for DNA viruses for herpes viruses

Definitions

• the invention relates to the use of ambroxol and its pharmacologically acceptable salts for the manufacture of a medicament for the treatment of painful conditions in the mouth and throat.
• ambroxol trans-4- (2-amino-3,5-dibromobenzylamino) cyclohexanol
• ambroxol is a known expectorant and mucolytic. It is used in peroral forms such as juices, capsules, tablets, inhalation solutions, drops or lozenges.
• ambroxol in suitable doses or concentrations at local application in addition to a very good compatibility has a very good analgesic effect in the mouth and throat.
• the invention therefore relates to the use of ambroxol or one of its pharmacologically tolerable salts for the manufacture of a medicament for the treatment of pain in the oral and / or pharyngeal cavity, selected from the group consisting of acute sore throats, aphthae, gingivitis, periodontal diseases, prosthesis pressure points, pain after oro-pharyngeal interventions, mucosal lesions in the oropharynx and herpes simplex in the oropharynx, in particular aphthae, gingivitis, periodontal diseases, Denture pressure points, pain after oro-pharyngeal surgery, mucosal lesions in the mouth and throat and herpes simplex in the mouth and throat, particularly preferred for the treatment of acute sore throat.
• Acute sore throat means severe sore throat, for example sore throat with difficulty swallowing or burning in the throat.
• Another object of the invention is a pharmaceutical composition containing ambroxol or one of its pharmacologically acceptable salts and one or more active ingredients selected from the group consisting of
• Antiseptics vitamins, corticoids, antiphlogistics, antivirals, antibiotics,
• Suitable antiseptics are, for example, cetylpyridinium Cl, dequalinium Cl,
• Chlorhexidine digluconate, benzalkonium Cl or ethacridine lactate Suitable vitamins are, for example, dexpanthenol (pantothenic acid) or
• Suitable corticoids are, for example, triamcinolone or prednisolone acetate.
• Suitable antiphlogistics are, for example, benzydamine-Cl or choline-salicylate.
• Suitable antivirals are, for example, acyclovir or idoxuridine.
• Suitable antibiotics are, for example, thyrotricin or bacitracin.
• Suitable antimycotics are, for example, amphotericin B or nystatin.
• a suitable proteolytic enzyme is, for example, lysozyme.
• Suitable essential oils are, for example, peppermint oil, thyme or sage.
• Another object of the invention is a pharmaceutical composition containing ambroxol or one of its pharmacologically acceptable salts and one or more active ingredients selected from the group consisting of lysozyme hydrochloride, dipotassium glycyrrhizinat, ammonium glycyrrhizinat, cetylpyridinium chlorides, chlorpheniramine maleate, noscapine, dequalinium chlorides, dextromethorphan phenolphthalinate , Potassium guaiacol sulfonate, dl-methylephedrine hydrochloride, chlorhexidine hydrochloride, and potassium cresolsulfonate.
• Ambroxol is a metabolite of the secretolytic bromhexine. Both active ingredients represent a very well-tolerated active ingredient combination, which positively influences the dual action of ambroxol.
• Another object of the invention is therefore a pharmaceutical composition consisting of ambroxol, bromhexine or its pharmacologically acceptable salts and pharmaceutical excipients, preferably having an ambroxol: bromhexine ratio in a range from 4: 1 to 6: 1, particularly preferably 5: 1.
• compositions wherein the single dose contains 15 to 50 mg ambroxol, preferably 20 mg ambroxol.
• Another object of the invention is a solid, lutschbare or slowly dissolving dosage form of a pharmaceutical composition containing ambroxol and one or more active ingredients selected from the group consisting of antiseptics, vitamins, corticoids, anti-inflammatory drugs, antibiotics, antimycotics and proteolytic enzymes.
• Another object of the invention is the use of a pharmaceutical composition described above for the preparation of a
• Medicament for the treatment of pain in the mouth or pharynx selected from the group consisting of acute sore throats, aphthae, gingivitis, periodontal diseases, denture pressure points, pain after oropharyngeal interventions, mucosal lesions in the oropharyngeal area, and herpes simplex im Oral and pharyngeal area, particularly preferred for the treatment of acute sore throat.
• Another object of the invention is the use of a pharmaceutical composition consisting of ambroxol hydrochloride, a flavoring agent, a lubricant, a matrix material, a sweetener and a polyethylene glycol for the manufacture of a medicament for the treatment of pain in the mouth or / and pharynx selected from the group from acute sore throat, aphthous ulcers, gingivitis, periodontal disease, prosthesis pressure sores, pain after oro-pharyngeal surgery, mucosal Lesions in the oropharynx, and herpes simplex in the oropharynx, particularly preferred for the treatment of acute sore throat.
• Suitable flavorings are, for example, peppermint, eucalyptus or lemon, preferably peppermint flavor.
• Suitable matrix materials are, for example, calcium carbonate, calcium phosphate or sorbitol, preferably sorbitol.
• Suitable sweeteners are, for example, saccharin, saccharin sodium, cyclamate, glycerol or sugar, preferably saccharin sodium.
• Suitable tablet lubricants are, for example, polyethylene glycols, preferably Macrogol 6000.
• Suitable lubricants are, for example, talcum or magnesium stearate, preferably talcum.
• Another object of the invention is the use of an ambroxol-containing lozenge based on sugar alcohols as a matrix material characterized by a content of a pharmaceutically tolerable phyllosilicate and a polyethylene glycol optionally in addition to other pharmaceutical auxiliaries, flavorings for the preparation of a medicament for the treatment of pain in the Oral and / or pharyngeal cavity selected from the group consisting of acute sore throat, aphthous ulcers, gingivitis, periodontal disease, prosthesis pressure, pain after oro-pharyngeal surgery, mucosal lesions in the oropharynx and herpes simplex in the oropharynx, especially preferred for the treatment of acute sore throat.
• Another object of the invention is the use of ambroxol for the manufacture of a medicament having an analgesic effect over a period of at least 3 hours, preferably over 3 hours, after an application.
• the invention likewise relates to the use of a pharmaceutical composition containing ambroxol for the manufacture of a medicament having an analgesic action over a period of at least 3 hours, preferably over 3 hours, after an application. Preference is given to administering the pharmaceutical composition according to the invention 1 to 6 times, preferably 2 to 4 times daily.
• Suitable acids for sacculating ambroxol are, for example, hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, nitric acid, oxalic acid, malonic acid, fumaric acid, maleic acid, tartaric acid, citric acid, ascorbic acid and methanesulfonic acid, preferably hydrochloric acid.
• ambroxol according to the invention is to be illustrated by the following examples of clinical studies examining the efficacy of ambroxol lozenges of different strengths. These serve only to illustrate the invention and are not to be regarded as limiting.
• a multicentre, prospective, placebo-controlled, randomized, double-blind study was conducted over two days of treatment with up to 6 lozenges containing ambroxol hydrochloride per day.
• the intent-to-treat (ITT) population consisted of 208 patients (105 with ambroxol treatment and 103 with appropriate placebo administration); 196 patients formed the per-protocol (PP) population (97 with Verum and 99 with placebo, respectively).
• ITT intent-to-treat
• PP per-protocol
• Double-blind treatment with up to 6 lozenges per day, each containing either 20 mg ambroxol or a placebo (lozenge without the active ingredient, but also with a verum comparable - pronounced taste of peppermint)
• Endpoints the time-weighted average pain reduction during the first 3 hours after administration of the first lozenge, normalized to the degree of baseline pain (SPID norm ); furthermore, the evaluation of efficacy and tolerability by the patient at the end of each treatment day. Results: In both treatment groups, a reduction in pain intensity was observed; the mean SPID norm ( ⁇ SD) after the first one
• Lozenge was 0.39 ⁇ 0.27 for 20 mg ambroxol hydrochloride and 0.28 ⁇ 0.25 for placebo.
• Figure 1 shows the time course of the mean change in pain intensity (PID) for the period before ingestion (baseline) up to 3 hours after ingestion of the first lozenge with 20 mg ambroxol hydrochloride and placebo.
• Double-blind treatment with up to 6 lozenges per day containing either 20 mg or 30 mg ambroxol hydrochloride or a placebo (lozenge without the active substance but also with a pronounced peppermint flavor similar to the verum)
• Endpoints the time-weighted average pain reduction during the first 3 hours after administration of the first lozenge, normalized to the degree of baseline pain (SPID norm ); Furthermore, the assessment of efficacy and tolerability by the patient at the end of each treatment day. Results: All treatments resulted in a reduction of pain intensity, the mean ( ⁇ SD) SPID norm after ingestion of the first lozenge was 0.53
• Ambroxol may be used alone or in combination with other pharmacologically active substances.
• dosage forms all types of preparations that are suitable for local use can be used.
• compresses or candies based on sugar or sugar substitutes are suitable or pasty-like products with a gum arabic or gelatine base.
• Suitable semi-solid preparations for application to the oral mucosa are gels, in particular gels based on cellulose or acrylate.
• Suitable spraying, gargling and rinsing solutions are aqueous preparations, advantageously with the addition of viscosity-increasing substances, such as modified celluloses, acrylic acid derivatives or polyvinyl compounds.
• the semi-solid and liquid forms may contain sweeteners and humectants, for example glycols and sugar alcohols. All forms are usually flavored, e.g. by adding essential oils.
• the dosage forms can be prepared by methods known in the pharmaceutical art.
• Peppermint oil 6.0 mg light anhydrous silicic acid 1.0 mg talc 1.0 mg magnesium stearate 1.5 mg
• Cetylpyridinium chlorides 1.0 mg sucrose (purified) 869.7 mg peppermint flavor 16.0 mg corn starch 30.0 mg polyvinylpyrrolidone 20.0 mg

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• Health & Medical Sciences (AREA)
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• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
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• Chemical Kinetics & Catalysis (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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