Microcapsule matrix microspheres, absorption-enhancing pharmaceutical compositions and methods

A pharmaceutical composition comprising microspheres, each having a surface and an interior, and comprising a pharmaceutically acceptable water insoluble organic matrix material, within which interior are distributed water-dispersable capsules consisting essentially of a core of a bioactive compound in a pharmaceutically effective amount, said core having a mean particle size of less than about ten microns in diameter and having a coating consisting essentially of an organic material having multiple charged groups, wherein said capsules are distributed homogenously within said microsphere.

A pharmaceutical composition comprising microspheres having a structure of an outer surface, and an interior comprising matrix of pharmaceutically acceptable water insoluble material and microcapsules of a hydrophobic bioactive compound coated with a pharmaceutically acceptable charged hydrophilic material, which particles are distributed homogenously within said interior region and are absent from said surface.

A process for the production of pharmaceutically acceptable microspheres comprising spraying, into a chilling zone, a flowable dispersion of bioactive micron-sized organic particles containing charged organic moieties in a water insoluble fluid matrix, under conditions that form droplets of said dispersion, and maintaining the fluidity of said droplets for a time sufficient to distribute homogenously said particles within said droplets, and allowing said droplets to solidify into said microspheres.

The process of claim 67 further comprising the step of first subjecting a dispersion of bioactive organic particles and a water soluble organic material containing charged organic moieties in a water insoluble fluid medium to sufficient high-pressure forces to form said flowable dispersion of bioactive micron-sized organic particles.