Drug – bio-affecting and body treating compositions – In vivo diagnosis or in vivo testing – X-ray contrast imaging agent
Patent
1995-01-10
1997-09-02
Hollinden, Gary E.
Drug, bio-affecting and body treating compositions
In vivo diagnosis or in vivo testing
X-ray contrast imaging agent
424489, 424490, 424488, 424 95, A61K 914, A61K 4904
Patent
active
056628838
ABSTRACT:
It has been known that administration of pharmaceutical agents (both diagnostic and therapeutic) with poor water solubility in the form of particles less than 400 nm in diameter produces agent formulation with increased bioavailibility. Bioavailability being proportional to the surface area, increases with reduction of particle size of the dispersed agent. We have discovered that chemical derivatization of certain photographic coupler molecules with chemical moiety that are capable of functioning as pharmaceutical agents (both diagnostic and therapeutic) is amenable to the preparation of nanoparticulate pharmaceutical agent dispersions via a process that comprises the dissolution of the said pharmaceutical agent in an alkaline solution and then neutralizing the said solution with an acid in the presence of a suitable surface-modifying, surface-active agent to form an ultra fine particle dispersion of the said pharmaceutical agent. The composition and process of this invention leads to particles of Z-average diameters as small as up to 10 nm as measured by photon correlation spectroscopy. The composition and process schemes of this invention are suitable for large-scale manufacture of these micro-nanoparticulate pharmaceutical agent dispersions.
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Bagchi Pranab
McIntire Gregory L.
Minter John R.
Stewart Robert C.
Hartley Michael G.
Hollinden Gary E.
NanoSystems L.L.C.
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