Lapatinib particles and uses thereof
AssigneeCrititech, Inc.
InventorsJacob SITTENAUER, Joseph FARTHING, Mark WILLIAMS, Michael BALTEZOR, Gere DIZEREGA, Aranza Barreda ABARCA, Shelby CLARK
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Abstract
The disclosure provides particles of at least 95% by weight of lapatinib, or a pharmaceutically acceptable salt thereof, wherein the particles have a specific surface area (SSA) of at least 10 m2/g and have a mean particle size by volume distribution of between about 0.7 μm and about 8 μm.
Claims28
A composition, comprising particles comprising at least 95% by weight of lapatinib, or a pharmaceutically acceptable salt thereof, wherein the particles have a specific surface area (SSA) of at least 10 m2/g and have a mean particle size by volume distribution of between about 0.7 μm and about 8 μm.
The method of 12, wherein the tumor is a breast tumor, pancreatic carcinoma, prostate carcinoma, bladder carcinoma, lung carcinoma, ovarian carcinoma, gastrointestinal tumor, or renal cell tumor.
A method for making lapatinib particles, comprising:
- (a) introducing (i) a solution comprising at least one solvent selected from the group consisting of acetone and DCM, or combinations thereof, and at least one solute comprising lapatinib or a pharmaceutically acceptable salt thereof into a nozzle inlet, and (ii) a compressed fluid into an inlet of a vessel defining a pressurizable chamber;
- (b) passing the solution out of a nozzle orifice and into the pressurizable chamber to produce an output stream of atomized droplets, wherein the nozzle orifice is located between 2 mm and 20 mm from a sonic energy source located within the output stream, wherein the sonic energy source produces sonic energy with an amplitude between 10% and 100% during the passing, and wherein the nozzle orifice has a diameter of between 20 μm and 125 μm;
- (c) contacting the atomized droplets with the compressed fluid, to cause depletion of the solvent from the atomized droplets, to produce compound particles comprising at least 95% lapatinib or a pharmaceutically acceptable salt thereof, wherein the particles have a specific surface area (SSA) of at least 10 m2/g and have a mean particle size by volume distribution of between about 0.7 μm and about 8 μm,
- wherein steps (a), (b), and (c) are carried out under supercritical temperature and pressure for the compressed fluid.
Dependencies are inferred from the claim text.