Niraparib particles and uses thereof
Inventors
SITTENAUER, Jacob • ABARCA, Aranza Barreda • Clark, Shelby • FARTHING, Joseph • Williams, Mark • DiZerega, Gere • BALTEZOR, Michael
Assignees
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Publication Number
US-11738014-B2
Publication Date
2023-08-29
Expiration Date
Abstract
Compositions of particles having at least 95% by weight of niraparib and a specific surface area (SSA) of at least 5 m2/g, methods for their use, and methods for their production are provided.
Core Innovation
The invention relates to niraparib particle compositions comprising particles that include at least 95% by weight of niraparib, or a pharmaceutically acceptable salt thereof. The particles are characterized by a specific surface area (SSA) of at least 5 m2/g, and the disclosed compositions include particles that can be uncoated.
The document states that increased SSA and lower bulk density improve dissolution and support tumor treatment. It further describes formulation forms that can include suspensions and aerosolizable compositions, including aerosolized suspensions and aerosolized dry powders, with particle or droplet properties described using mass median aerodynamic diameter (MMAD) ranges.
The invention also covers a method for making niraparib particles by introducing a solution comprising selected solvents and a solute comprising niraparib or a pharmaceutically acceptable salt into a nozzle inlet and introducing a compressed fluid into a vessel defining a pressurizable chamber. The solution passes out of a nozzle orifice to produce atomized droplets, and the atomized droplets contact the compressed fluid to deplete the solvent and produce particles under supercritical temperature and pressure.
Claims Coverage
The independent claims are directed to 2 inventive features: a niraparib particle composition and a method for making niraparib particles.
Niraparib particle composition with minimum SSA
A composition comprising particles comprising at least 95% by weight of niraparib, or a pharmaceutically acceptable salt thereof, wherein the particles have a specific surface area (SSA) of at least 5 m2/g.
Supercritical nozzle-atomization particle formation
A method for making niraparib particles comprising introducing a solution comprising at least one solvent selected from ethanol, methanol, hexafluoroisopropanol (HFIP), or combinations thereof and a solute comprising niraparib or a pharmaceutically acceptable salt thereof into a nozzle inlet; introducing a compressed fluid into a vessel defining a pressurizable chamber; passing the solution out of a nozzle orifice into the pressurizable chamber to produce atomized droplets; contacting the atomized droplets with the compressed fluid to cause depletion of the solvent; and carrying out the steps under supercritical temperature and pressure for the compressed fluid, to produce particles comprising at least 95% niraparib or a pharmaceutically acceptable salt thereof with SSA of at least 5 m2/g.
The claimed inventive coverage centers on a niraparib particle system defined by at least 95% by weight niraparib, or a pharmaceutically acceptable salt, together with SSA of at least 5 m2/g, and a manufacturing method that produces such particles by nozzle atomization followed by contacting with a compressed fluid under supercritical temperature and pressure.
Stated Advantages
Increased dissolution attributed to increased SSA and lower bulk density, supporting tumor treatment.
Documented Applications
Administration to a subject for tumor treatment using the defined niraparib particle compositions.
Formulation as aerosolized suspensions and aerosolized dry powder compositions, including MMAD-defined pulmonary or aerosol contexts.
Production of niraparib particles by supercritical nozzle atomization processing to obtain particles with at least 95% niraparib, or a pharmaceutically acceptable salt thereof, and SSA at least 5 m2/g.
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