Glucocorticoid “nintedanib” particles and their use
Inventors
BALTEZOR, Michael • MCCLOREY, Matthew • FARTHING, Joseph S. • Williams, Mark • SITTENAUER, Jacob
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-11931368-B2
Publication Date
2024-03-19
Expiration Date
Abstract
Disclosed herein are particles of at least 95% by weight of a glucocorticoid that have a specific surface area of at least 10 m2/g, methods for making, such particles, and methods for their use as therapeutics. Also disclosed herein are particles of at least 95% by weight of an indolinone that have a specific surface area of at least 10 m2/g, methods for making such particles, and methods for-their use as therapeutics.
Core Innovation
The invention relates to compositions comprising nintedanib particles, or pharmaceutically acceptable salts thereof. The nintedanib particles are at least 99% nintedanib by weight and are not bound to or conjugated to any other substance, with a defined specific surface area (SSA) and a controlled volume-mean particle size.
The described compositions position nintedanib particles with increased SSA and controlled particle size for pulmonary delivery formats. The disclosed formats include dry powder for inhalation and suspension formulations, and the particle physicochemical properties are used to characterize the therapeutic particle composition, including SSA measured by Brunauer-Emmett-Teller (BET) and particle size distributions using Dv values and mass median aerodynamic diameter (MMAD).
Claims Coverage
Independent claim clm-00001 defines a nintedanib particle composition by purity, lack of binding or conjugation, and specified ranges of SSA and volume-mean particle size. Dependent claims refine the nintedanib salt form and the pulmonary formulation format, and add narrower SSA and aerosol/droplet aerodynamic size ranges.
Highly pure, unbound nintedanib particle composition with defined SSA and volume-mean size
A composition comprising nintedanib particles, wherein the nintedanib particles are at least 99% nintedanib by weight, or a pharmaceutically acceptable salt thereof, wherein the nintedanib particles have a specific surface area (SSA) of between 9 m2/g and about 20.14 m2/g, wherein the nintedanib particles are not bound to or conjugated to any other substance, and wherein the nintedanib particles have a volume-mean particle size between about 0.5 μm and about 5.0 μm.
Nintedanib esylate particle composition
The composition wherein the nintedanib component is nintedanib esylate.
Suspension with pharmaceutically acceptable aqueous carrier
The composition formulated as a suspension containing a pharmaceutically acceptable aqueous carrier.
Dry powder for inhalation
The composition formulated as a dry powder intended for inhalation.
SSA constrained nintedanib particles (narrow SSA subrange)
The composition including nintedanib particles having a specific surface area (SSA) between 9.94 m2/g and 20.14 m2/g.
Aerosolized nintedanib with MMAD-defined droplet size
A composition in which nintedanib particles are aerosolized such that aerosol droplets containing the nintedanib particles have a MMAD between about 0.5 μm to about 6 μm diameter.
Across the independent claim and its dependents, the coverage is centered on nintedanib particles that are highly pure, not bound or conjugated, and characterized by defined SSA and volume-mean particle size, with additional claim support for salt form, formulation format, tighter SSA subranges, and MMAD-defined aerosol/droplet size.
Stated Advantages
Documented Applications
No documented applications found
Interested in licensing this patent?