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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
  • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
  • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• • 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
  • A61P11/00—Drugs for disorders of the respiratory system
  • A61P11/02—Nasal agents, e.g. decongestants

Definitions

• Part of the active ingredients La - 1.j and 1.1 - 1.101 contains a hydrolysis-sensitive ester or lactone group.
• substantially anhydrous dosage forms and application forms are selected for these compounds.
• nasal administration is preferably as a powder for intranasal deposition.
• the adjuvants used in nasal powders are carriers (which carry a finely micronized active), gelling agents (which promote the removal of the Slow down active agent from the nasal cavity), fillers (to bring low-dose drugs to a manageable volume) or enhancers (which improve the absorption of the drug), where an excipient can also perform several functions at the same time.
• Cyclodextrins and derivatives for example ⁇ -, ⁇ - or ⁇ -cyclodextrin, dimethyl- ⁇ -cyclodextrin, hydroxypropyl- ⁇ -cyclodextrin;
• candidate excipients are: human serum albumin, polyalcohols (e.g., mannitol, sorbitol, xylitol), trehalose, amino acids, monosaccharides (e.g., glucose or arabinose), casein, salts (e.g., sodium chloride, calcium carbonate) or mixtures of these excipients with each other.
• polyalcohols e.g., mannitol, sorbitol, xylitol
• trehalose amino acids
• monosaccharides e.g., glucose or arabinose
• casein casein
• salts e.g., sodium chloride, calcium carbonate
• the propellant-containing aerosols which can be used in the context of the use according to the invention can dissolve the active substance or the active substance combination in the propellant gas or contain it in dispersed form.
• the propellant gases which can be used to produce the aerosols are known from the prior art. Suitable propellant gases are selected from the group consisting of hydrocarbons such as n-propane, n-butcine or isobutane and halohydrocarbons such as preferably fluorinated derivatives of methane, ethane, propane, butane, cyclopropane or cyclobutane.
• the abovementioned propellant gases can be used alone or in mixtures thereof.
• Particularly preferred propellant gases are fluorinated alkane derivatives selected from TG134a (1,1,1,2-tetrafluoroethane), TG227 (1,1,1,3,3,3,3-heptafluoropropane) and mixtures thereof.
• the propellant-containing aerosols which can be used in the context of the use according to the invention can also contain further constituents, such as co-solvents, stabilizers, surfactants, antioxidants, lubricants and agents for aerosols Adjustment of pH included. All of these ingredients are known in the art.
• the nasal application of the active ingredient according to the invention or the active ingredient combination in the form of propellant-free solutions or suspensions come as a solution or suspending aqueous, oily or alcoholic, for example ethanolic solutions into consideration.
• the solvent may be water only or it may be a mixture of water and ethanol.
• sterile aqueous solutions of the corresponding pharmaceutically acceptable salts may be used.
• solutions or suspensions of the active compounds in aqueous propylene glycol, in sesame or peanut oil into consideration.
• Aqueous solutions should be suitably buffered if necessary and the liquid diluent made isotonic with, for example, sufficient salt or glucose.
• the formulations described in Examples 1-5 and 7 contain any active ingredient selected from Group 1.
• the formulation of Example 6 contains an active ingredient selected from Group 1 which has no hydrolysis-sensitive group, such as an ester or lactone group.
• the active ingredient and any excipient present are each micronised using conventional techniques, optionally spheronised and sieved, and optionally then mixed in the desired ratio.
• an average particle size (aerodynamic diameter) lying between 5 and 200 ⁇ m is set, for example in the range between 10 to 25 ⁇ m, the average particle size of the excipient is expediently selected in the range 10 to 350 ⁇ m, for example between 15 to 80 ⁇ m.
• Method of preparation The active ingredient in the form of a physiologically acceptable salt and the excipients are dissolved in water and filled into a corresponding container.
• the active ingredient is dissolved in sesame oil and filled into a corresponding container.

Landscapes

• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Epidemiology (AREA)
• General Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Pulmonology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Otolaryngology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Plural Heterocyclic Compounds (AREA)
• Medicinal Preparation (AREA)

Applications Claiming Priority (3)

Publications (1)

Family

ID=36228798

Family Applications (1)

Country Status (14)

Families Citing this family (8)

Family Cites Families (5)

• 2006
  • 2006-01-16 BR BRPI0607358-1A patent/BRPI0607358A2/pt not_active IP Right Cessation
  • 2006-01-16 KR KR1020077020172A patent/KR20070108889A/ko not_active Application Discontinuation
  • 2006-01-16 AU AU2006210175A patent/AU2006210175A1/en not_active Abandoned
  • 2006-01-16 CA CA002601740A patent/CA2601740A1/en not_active Abandoned
  • 2006-01-16 MX MX2007009265A patent/MX2007009265A/es not_active Application Discontinuation
  • 2006-01-16 EP EP06707722A patent/EP1845992A1/de not_active Withdrawn
  • 2006-01-16 JP JP2007553578A patent/JP2009523700A/ja active Pending
  • 2006-01-16 WO PCT/EP2006/050215 patent/WO2006082129A1/de active Application Filing
  • 2006-01-16 EA EA200701619A patent/EA200701619A1/ru unknown
  • 2006-02-02 US US11/275,903 patent/US20060178364A1/en not_active Abandoned
  • 2006-02-03 TW TW095103840A patent/TW200638937A/zh unknown
  • 2006-02-03 AR ARP060100386A patent/AR055029A1/es unknown
• 2007
  • 2007-06-18 NO NO20073097A patent/NO20073097L/no not_active Application Discontinuation
  • 2007-08-02 IL IL184997A patent/IL184997A0/en unknown

Non-Patent Citations (1)

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