Ph-modulated formulations for pulmonary delivery

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/72 (2006.01) A61K 31/496 (2006.01)

Patent

CA 2752296

An aerosolizable formulation comprised of a drug, a carrier and pH affecting component is disclosed. The drug is dissolved in the formulation at a concentration above which it remains in solution at neutral pH. This increases the concentration of the drug in solution making it possible to administer larger amounts of drug with the same or a smaller volume of formulation. When the formulation is aerosolized to small particles and inhaled into human lungs in small volumes (e.g. 0.05 to 0.5 mL) the fluids in the lungs neutralize the formulation causing the drug to participate out of solution. This results in the drug being delivered at a controlled rate below the rate at which drug is administered from a formulation initially at a neutral pH.

La présente invention concerne une formulation pouvant être aérosolisée composée d'un médicament, d'un support et d'un composant affectant le pH. Le médicament est dissous dans la formulation à une concentration au-dessus de laquelle il demeure en solution à pH neutre. Ceci augmente la concentration du médicament en solution, rendant possible l'administration de quantités plus importantes de médicament avec le même volume ou un volume plus petit de formulation. Lorsque la formulation est aérosolisée en petites particules et inhalée dans des poumons humains dans des petits volumes (par exemple, 0,05 à 0,5 ml), les liquides dans les poumons neutralisent la formulation, provoquant la précipitation du médicament hors de la solution. Ceci entraîne l'administration du médicament à une vitesse contrôlée inférieure à laquelle le médicament est administré à partir d'une formulation initialement à pH neutre.

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