Compositions of particulate coformulation
View Patent ↗Embodiments of the invention provide a composition of a particulate coformulation which includes particles containing an active substance and an additive, wherein each particle contains a relative additive concentration increasing radially outwards from a particle center to a particle surface along a finite gradient. In one example, the particle surface is an additive-rich surface without a distinct physical boundary between the particle center and the particle surface. The relative additive concentration may have a continuous rate of change across the finite gradient. In some examples, an active substance: additive ratio of the particle surface is sufficiently low to form a protective surface layer around the active substance. Generally, the particle surface is free of the active substance.
1. A composition of a particulate coformulation, comprising:
particles comprising a solid dispersion of an active substance and an additive throughout each particle of the particulate coformulation, wherein each particle comprises:
a particle surface having a surface concentration within a range from about 0% to about 10% by weight of the active substance;
a particle core having a central region concentration within a range from about 90% to about 100% by weight of the active substance; and
an additive concentration increasing radially outwards through the particle core to the particle surface along a finite gradient, wherein each particle lacks a distinct physical boundary between the particle core to the particle surface, is spherical or substantially spherical, and has a volume mean diameter within a range from about 0.5 μm to about 100 μm, wherein the active substance is in crystalline form and the additive is in amorphous form.
2. A composition of a particulate coformulation, comprising:
particles comprising a solid dispersion of an active substance and an additive throughout each particle of the particulate coformulation, wherein each particle comprises:
a particle core having a central region concentration within a range from about 90% to about 100% by weight of the active substance;
a particle surface having a surface concentration within a range from about 0% to about 5% by weight of the active substance; and
an additive concentration increasing radially outwards through the particle core to the particle surface along a finite gradient, wherein each particle lacks a distinct physical boundary between the particle core to the particle surface, wherein the particulate coformulation is or comprises a pharmaceutical agent or a nutraceutical agent, wherein the active substance is in crystalline form and the additive is in amorphous form.
3. A composition of a particulate coformulation, comprising:
particles comprising a solid dispersion of an active substance and an additive throughout each particle of the particulate coformulation, wherein each particle comprises:
a particle core having a central region concentration within a range from about 80% to about 100% by weight of the active substance;
a particle surface having a surface concentration within a range from about 0% to about 10% by weight of the active substance; and
an additive concentration increasing radially outwards through the particle core to the particle surface along a finite gradient, wherein each particle lacks a distinct physical boundary between the particle core to the particle surface, wherein both the active substance and the additive comprise different pharmaceutically active substances for co-administration.
4. A composition of a particulate coformulation, comprising:
particles comprising a solid dispersion of an active substance and an additive throughout each particle of the particulate coformulation, wherein each particle comprises:
a particle core having a central region concentration within a range from about 80% to about 100% by weight of the active substance;
a particle surface having a surface concentration within a range from about 0% to about 10% by weight of the active substance; and
an additive concentration increasing radially outwards through the particle core to the particle surface along a finite gradient, wherein each particle lacks a distinct physical boundary between the particle core to the particle surface, wherein the active substance is in crystalline form and the additive is in amorphous form.