Compositions of particulate coformulation

Abstract

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:
 an active substance and an additive, which is a solid dispersion of one component in the other, but which has a finite gradient in the relative additive concentration, which concentration increases radially outwards from the core to the surface of the particles, so that the particles have an additive-rich surface region but do not possess separate core and coating layers with a distinct physical boundary between them, wherein the coformulation is or comprises a pharmaceutical or nutraceutical agent or a foodstuff.   
     
     
         2 . The composition of  claim 1 , wherein the active substance:additive ratio, at the particle surfaces, is sufficiently low for the additive to form a protective surface layer around the active substance. 
     
     
         3 . The composition of  claim 1 , wherein the additive is a taste masking agent or an odor masking agent. 
     
     
         4 . The composition of  claim 2 , wherein the additive is a taste masking agent or an odor masking agent. 
     
     
         5 . The composition of  claim 1 , wherein the active substance is present in a crystalline form and the additive is present in an amorphous form, and wherein differential scanning calorimetry analysis or X-ray diffraction analysis of the coformulation indicates reduced active substance crystallinity compared to that of the active substance alone. 
     
     
         6 . The composition of  claim 1 , wherein the relative additive concentration is up to about 60% by weight. 
     
     
         7 . The composition of  claim 2 , wherein the relative additive concentration is up to about 60% by weight. 
     
     
         8 . The composition of  claim 4 , wherein the relative additive concentration is up to about 60% by weight. 
     
     
         9 . A composition of a particulate coformulation, comprising:
 particles comprising:
 an active substance, the active substance comprising a pharmaceutical agent, a nutritional agent, an herbicidal agent, a pesticidal agent, or combinations thereof; and 
 an additive, wherein each particle comprises a relative additive concentration increasing radially outwards from a particle center to a particle surface along a finite gradient, and wherein both the active substance and the additive comprise different pharmaceutically active substances for co-administration. 
   
     
     
         10 . The composition of  claim 9 , wherein the particle surface is an additive-rich surface without a distinct physical boundary between the particle center and the particle surface. 
     
     
         11 . The composition of  claim 10 , wherein the relative additive concentration has a continuous rate of change across the finite gradient. 
     
     
         12 . The composition of  claim 10 , wherein an active substance:additive ratio of the particle surface is sufficiently low to form a protective surface layer around the active substance. 
     
     
         13 . The composition of  claim 10 , wherein the particle surface is free of the active substance. 
     
     
         14 . The composition of  claim 9 , wherein the particle surface comprises a concentration of about 5% or less by weight of the active substance. 
     
     
         15 . The composition of  claim 14 , wherein the concentration of the active substance is about 2% or less by weight. 
     
     
         16 . The composition of  claim 15 , wherein the concentration of the active substance is about 1% or less by weight. 
     
     
         17 . The composition of  claim 16 , wherein the concentration of the active substance is about 0.5% or less by weight. 
     
     
         18 . The composition of  claim 17 , wherein the concentration of the active substance is about 0% by weight. 
     
     
         19 . The composition of  claim 9 , wherein a central region of each particle comprises a concentration of about 90% or greater by weight of the active substance. 
     
     
         20 . The composition of  claim 19 , wherein the concentration of the active substance is about 95% or greater by weight.