INCREASED AMORPHOUS STABILITY OF POORLY WATER SOLUBLE DRUGS BY NANOSIZING

摘要

Disclosed is a population of nanoparticles, together with methods of making a population of nanoparticles, wherein one or more of the nanoparticles includes: an amorphous drug core having an effective diameter less than or equal to about 2.0 microns, wherein the amorphous drug core is substantially free of dopant, and wherein the amorphous drug core comprises a drug with properties that satisfy the following relationships: a glass transition temperature greater than or equal to about 30 Deg. C.; and water solubility at 25 Deg. C. less than or equal to about 1 mg/ml; and at least one stabilizer adsorbed on a surface of the amorphous drug core; and wherein the at least one stabilizer is present in an amount effective to provide an amorphous stability of the population of nanoparticles that is approximately equal to or greater than an amorphous stability of an amorphous bulk drug substance comprising the drug, as measured over a period of at least four months.