Oral Pharmaceutical Compositions in a Solid Dispersion Comprising Preferably Posaconazole and HPMCAs
The present invention provides a solid molecularly dispersed composition comprising a poorly water soluble and weakly basic azole antifungal compound and a pH sensitive polymer, pharmaceutical compositions, comprising the solid molecularly dispersed composition of the invention and methods of treating and/or preventing a fungal infection in a patient in need thereof comprising orally administering a pharmaceutical composition comprising a composition of the invention to a patient in need thereof. Preferably the antifungal, compound is posaconazole, and the pH sensitive polymer is HPMCAS.
1 . A composition comprising a weakly basic and poorly-aqueous soluble azole molecularly dispersed in at least one pH sensitive polymer prepared by evaporating the solvent from a solution comprising the azole and said at least one pH sensitive polymer.
2 . A composition comprising posaconazole molecularly dispersed in hypromellose acetate succinate prepared by evaporating the solvent from a solution comprising posaconazole and the hypermellose acetate succinate polymer.
3 . A pharmaceutical composition suitable for oral administration comprising the composition of claim 2 .
4 . A method for the treatment or prevention of a fungal infection, the method comprising administering to a patient in need thereof an oral pharmaceutical composition comprising a solid molecular dispersion prepared by a spray-drying technique, wherein the solid molecular dispersion comprises:
(a) posaconazole; and
(b) hypromellose acetate succinate (HPMCAS).
5 . The method of claim 4 , wherein the fungal infection is an Aspergillus or a Candida infection, or is a fungal infection caused by a zygomycetes or a dermatophyte.