Inhalable compositions comprising macrocyclic immunosuppressants
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Publication Number
US-12303593-B2
Publication Date
2025-05-20
Expiration Date
Abstract
The present disclosure relates to a pharmaceutical composition comprising an inhalable immunosuppressive macrocyclic active ingredient for use in the prevention or treatment of a pulmonary disease or condition in a subject, wherein the pharmaceutical composition is administered to the subject by inhalation in form of an aerosol, and wherein the aerosol is generated by nebulization of the pharmaceutical composition using a nebulizer (100), the nebulizer comprising: a) an aerosol generator (101) comprising: —a fluid reservoir (103) for holding the pharmaceutical composition or an interface configured to connect a fluid reservoir, and—a vibratable membrane (110) having a plurality of apertures, the apertures being adapted to produce an aerosol comprising droplets having a mass median aerodynamic diameter (MMAD) of up to about 15 4.0 μm as measured with a 0.9% (w/v) aqueous solution of sodium chloride; b) a chamber (105) for temporarily accommodating the aerosol generated by the aerosol generator (101), the chamber having an inner lumen with a volume in the range of from about 50 to about 150 ml; and c) a mouthpiece (40) for delivering the aerosol supplied by the nebulizer (100) to the subject, the mouthpiece having an exhalation filter (30).
Core Innovation
The disclosure describes inhalable pharmaceutical compositions containing an inhalable immunosuppressive macrocyclic active ingredient, administered to a subject by inhalation in the form of an aerosol generated by nebulization. The aerosol generation uses a nebulizer that includes a vibratable membrane having a plurality of apertures, a chamber having an inner lumen volume, and a mouthpiece having an exhalation filter.
The pharmaceutical composition includes at least one disaccharide selected from saccharose, lactose and trehalose in the range of from about 5 to about 15 wt.-%, based on the total weight of the pharmaceutical composition. The disclosed compositions are also described as liposomally solubilized immunosuppressant formulations, including liposomally solubilized cyclosporine A (L-CsA) intercalated in unilamellar phospholipid bilayers.
The disclosure further describes aerosol characterization and breath simulation comparisons, including total output rate, delivered dose %, exhaled amount %, residue, respirable dose, MMAD, fine particle fraction, and end time. The stated approach targets droplet and aerosol properties such as MMAD up to about 4.0 m and delivered dose while minimizing exhaled fraction.
Claims Coverage
The partial content provides two independent claims covering a method of treating a pulmonary disease or condition using an inhalable immunosuppressive macrocyclic active ingredient with a specified disaccharide component and a specified membrane-based nebulizer architecture, and a corresponding kit that includes the pharmaceutical composition and the nebulizer. Both independent claims include the same core inventive structure: disaccharide-containing composition for inhalation together with an aperture vibratable membrane nebulizer delivering droplets with MMAD up to about 4.0 m, a chamber inner lumen volume of about 50 to about 150 ml, and a mouthpiece with an exhalation filter.
Disaccharide-containing inhalable immunosuppressive macrocyclic active ingredient for aerosol administration
The pharmaceutical composition comprises at least one disaccharide selected from saccharose, lactose and trehalose in the range of from about 5 to about 15 wt.-%, based on the total weight of the pharmaceutical composition, and includes an inhalable immunosuppressive macrocyclic active ingredient administered to treat a pulmonary disease or condition by inhalation in the form of an aerosol.
Vibratable membrane nebulizer producing droplets with MMAD up to about 4.0 m
The nebulizer comprises an aerosol generator having a vibratable membrane with a plurality of apertures adapted to produce an aerosol comprising droplets having a mass median aerodynamic diameter of up to about 4.0 m as measured with a 0.9% (w/v) aqueous solution of sodium chloride.
Chamber inner lumen volume of about 50 to about 150 ml
The nebulizer includes a chamber for temporarily accommodating the aerosol generated by the aerosol generator, the chamber having an inner lumen with a volume in the range of from about 50 to about 150 ml.
Mouthpiece with exhalation filter for aerosol delivery
The nebulizer includes a mouthpiece for delivering the aerosol to the subject, the mouthpiece having an exhalation filter.
Kit including disaccharide-containing inhalable immunosuppressive macrocyclic active ingredient and specified nebulizer
A kit comprising a pharmaceutical composition comprising an inhalable immunosuppressive macrocyclic active ingredient for use in the treatment of a pulmonary disease or condition, with at least one disaccharide selected from saccharose, lactose and trehalose in the range of from about 5 to about 15 wt.-%, and a nebulizer having an aerosol generator with a vibratable membrane producing droplets with MMAD up to about 4.0 m, a chamber with an inner lumen volume of about 50 to about 150 ml, and a mouthpiece having an exhalation filter.
Across the independent claims, the coverage centers on delivering an inhalable immunosuppressive macrocyclic active-ingredient pharmaceutical composition that contains saccharose, lactose and/or trehalose (about 5 to about 15 wt.-%) as an aerosol produced by a nebulizer with a vibratable membrane producing droplets with MMAD up to about 4.0 m, a chamber inner lumen volume of about 50 to about 150 ml, and a mouthpiece with an exhalation filter.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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