Pulmonary delivery of polyene antifungal agents
AssigneeNektar Therapeutics
InventorsMichael Weickert, Marc S. Gordon, Sandeep Kumar, Bing Yang, Razaq Sarwar
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Abstract
The present invention provides spray-dried polyene compositions for oral inhalation to the lung. The polyene antifungal compositions demonstrate superior aerosol properties, do not exhibit appreciable degradation of the polyene upon spray-drying, and are useful in the treatment and prophylaxis of both pulmonary and systemic fungal infections.
Claims60
A method for preparing a spray-dried polyene powder suitable for oral inhalation to the lung, said method comprising:
- (i) dissolving a polyene antifungal compound in an acidified solvent to form an acidic polyene-containing solution, and
- (ii) spray drying said polyene-containing solution to form an inhaleable dry powder containing no more than about 10% polyene degradation products and characterized by an emitted dose greater than 60%.
A method for preparing a spray-dried polyene powder suitable for oral inhalation to the lung, said method comprising:
- (i) suspending a polyene antifungal compound in an aqueous solvent to form a suspension,
- (ii) wet milling the suspension from (i) to form a wet-milled suspension, and
- (iii) spray drying the wet milled suspension to produce an inhaleable dry powder containing no more than about 10% polyene degradation products and characterized by an emitted dose greater than about 60%.
A spray-dried powder composition suitable for oral inhalation to the lung comprising a therapeutically effective amount of a polyene antifungal compound, wherein the composition comprises no more than about 10% polyene degradation products and is characterized by an emitted dose greater than about 60%.
A spray-dried powder composition suitable for oral inhalation to the lung comprising a therapeutically effective amount of a polyene antifungal compound and a leucyl-containing excipient comprising from 1 to 3 amino acid residues.
An aerosolized, spray-dried powder composition suitable for oral inhalation to the lung comprising a therapeutically effective amount of a polyene antifungal compound, wherein the composition comprises no more than about 10% polyene degradation products and is characterized by an emitted dose greater than about 60%.
In a method for preparing an inhaleable spray-dried powder comprising the steps of spray drying a solution or suspension containing an active agent to form particles having a particular MMAD, the improvement comprising exposing said powder either during or after spray drying to moisture in an amount effective to reduce the MMAD of the particles from that of the particles formed in the absence of said exposing step.
Dependencies are inferred from the claim text.