Vitamin A aerosol-inhalant preparations and method

• US 5,556,611 A
• Filed: 04/21/1995
• Issued: 09/17/1996
• Est. Priority Date: 05/04/1988
• Status: Expired due to Fees

• Current Assignee: Hermes Fabrik Pharmazeutischer Praparate
• Original Assignee: Hermes Fabrik Pharmazeutischer Praparate
• Inventors: Biesalski, Hans K.
• Primary Examiner(s): AZPURU, CARLOS A
• Application Number:
  US08/426,344
• Time in Patent Office: 515 Days
• Field of Search: 424/45, 424/46, 514/725
• US Class Current: 424/46
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/07 Retinol compounds, e.g. vitamin A retinoic acids A61K31/203
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/22 of acyclic acids, e.g. pravastatin
• CPC Class Codes: A61K 31/23 of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

A pharmaceutical preparation consisting of retinoic acid and/or an ester of retinoic acid and/or an ester of retinol as active substances, which are present in the preparation form of aerosol, is advantageously suitable for topical treatment of mucosal diseases in man and animal.

Claims

1. A method for preventing and treating mucosal diseases of the epithelia of the tracheobronchial tract, said epithelia being susceptible to treatment with vitamin A, in a human or animal subject, said method comprising topically applying to the mucosal site of the epithelia of a subject suffering from said disease a therapeutically effective amount of a pharmaceutical preparation in the form of an aerosol inhalate comprising at least one active substance selected from the group consisting of an ester of retinoic acid and an ester of retinol for those in need thereof, with solid or liquid particles distributed in the formed inhalate of about 10^-7 to 10^-1 cm in diameter.

2. A method for preventing and treating a condition selected from functional anomalies, diseases and pathological changes in the mucous membranes of the respiratory epithelium, the epithelia of the tracheal tract, or the epithelia of the deep bronchial tract, said epithelia being susceptible to treatment with vitamin A, of humans and animals, said method comprising topically applying to said mucous membranes of a subject suffering from said condition a therapeutically effective amount of a pharmaceutical preparation in the form of an aerosol inhalate comprising at least one active substance selected from the group consisting of an ester of retinoic acid and an ester of retinol for those in need thereof, with solid or liquid particles distributed in the formed inhalate of about 10^-7 to 10^-1 cm in diameter.

3. A method for preventing and treating a condition selected from cellular differentiation disturbances of the mucous membranes of the tracheobronchial tract, squamous metaplasia irrespective of the genesis, neoplastic changes, restricting activity of the ciliary epithelium, and dysfunction of mucigenous cells irrespective of the genesis, said method comprising topically applying to said mucous membranes of a subject suffering from said condition a pharmaceutical preparation in the form of an aerosol inhalate comprising at least one active substance selected from the group consisting of an ester of retinoic acid and an ester of retinol for those in need thereof, with solid or liquid particles distributed in the formed inhalate of about 10^-7 to 10^-1 cm in diameter.

4. An adjuvant in the therapy of a condition selected from bronchial carcinomas, acute and chronic bronchitis, acute and chronic functional disturbances due to reversible impairment of the tracheobronchial epithelium following inhalation of dusts and gases damaging the mucous membranes, and bronchopulmonary dysplasia of newborn children, said method comprising topically applying to a subject suffering from said condition a therapeutically effective amount of a pharmaceutical preparation in the form of an aerosol inhalate comprising at least one active substance selected from the group consisting of an ester of retinoic acid and an ester of retinol for those in need thereof, with solid or liquid particles distributed in the formed inhalate of about 10^-7 to 10^-1 cm in diameter.