Particle formation methods and their products
AssigneeNektar Therapeutics UK, Ltd.
InventorsMazen H. Hanna, Peter York
Life of this patent
Estimating the term…
Abstract
Preparation of particles of an active substance having a layer of an additive at the particle surfaces, by dissolving both the active substance and the additive in a vehicle to form a target solution, and contacting the target solution with an anti-solvent fluid using a SEDS™ particle formation process, to cause the active substance and additive to coprecipitate. The additive is typically a protective additive, in particular a taste and/or odour masking agent. Also provided is a particulate coformulation made by the method, which has a finite gradient in the relative additive concentration, which concentration increases radially outwards from the active-rich core to the additive-rich surface of the particles.
Claims60
A particulate coformulation of an active substance and an additive, which is a solid dispersion of one component in the other formed from a co-precipitation process containing a supercritical fluid, whererin each particle contains a particle core having a first concentration by weight of the active substance within a range from about 90% to about 100%, a particle surface having a second concentration by weight of the active substance within a range from about 0% to about 5%, a relative additive concentration increasing radially outwards along a finite gradient and the particles are spherical or approximately spherical particles having a volume mean diameter of less than 100 μm, or needle-like particles having a volume mean length within a range from about 5 μm to about 100 μm and a volume mean thickness within a range from about 0.5 μm to about 5 μm, or plate-like particles having a volume mean thickness within a range from about 0.5 μm to about 5 μm.
A particulate coformulation, comprising:
- an active substance and an additive contained within particulate formed from a co-precipitation process containing a supercritical fluid, wherein each particle contains a particle core having a first concentration by weight of the active substance within a range from about 90% to about 100%, a particle surface having a second concentration by weight of the active substance within a range from about 0% to about 5 %, an additive concentration having a finite gradient increasing radially from a center towards the particle surface and the particles are spherical or substantially spherical particles having a volume mean diameter of less than 100 μm.
A particulate coformulation, comprising:
- an active substance and a taste masking agent contained within particulate formed from a co-precipitation process containing a supercritical fluid, wherein each particle contains a particle core having a first concentration by weight of the active substance within a range from about 90% to about 100%, a particle surface having a second concentration by weight of the active substance within a range from about 0% to about 5%, an additive concentration having a finite gradient increasing radially from a center towards the particle surface and the particles are spherical or substantially spherical particles having a volume mean diameter of about 20 μm or less.
A particulate coformulation, comprising:
- an active substance and an additive contained within particulate formed from a co-precipitation process containing a supercritical fluid;
- and
- an additive concentration having a finite gradient increasing radially towards a particle surface of each particle within the particulate, wherein each particle contains a particle core having a first concentration by weight of the active substance within a range from about 90% to about 100% and the particle surface having a second concentration by weight of the active substance within a range from about 0% to about 5%.
Dependencies are inferred from the claim text.