Sterling Winthrop Inc.

Elan Pharma International Limited

Nanosystems L.l.c.

Sterling Wintrhop Inc.

Mary E Roberts

Stephen B Ruddy

Gregory L McIntire

Eugene Rex Cooper

Gary G Liversidge

Sui-Ming Wong

David A Engers

Shuqian Xu

Edward R Bacon

Carl R Illig

John L Toner

Brent D Douty

W Mark Eickhoff

Kimberly G Estep

Thomas J Caulifield

The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HIV-2) protease inhibitors are described.

Methods of treating mammals using nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors

The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HV-2) protease inhibitors are described.

Methods of making nanocrystalline formulations of human immunodeficiency

The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increase rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HIV-2) protease inhibitors are described.

Nanocrystalline formulations of human immunodeficiency virus (HIV)

There is described a composition comprised of nanoparticles of a therapeutic agent having a surface modifier adsorbed on the surface thereof. The present composition is characterized in that the therapeutic agent is ibuprofen or fenoprofen which is substantially enriched in the R(-) enantiomer.

Nanoparticles containing the R(-)enantiomer of ibuprofen

Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising nanoparticles of a barium salt having associated with its surface non-ionic and anionic stabilizers; and methods for their use in diagnostic radiology of the gastrointestinal tract.

Barium salt formulations stabilized by non-ionic and anionic stabilizers

Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkanes and iodophenyl ethers as the x-ray producing agents in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

Compositions of iodophenoxy alkanes and iodophenyl ethers and

Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkylene ethers and pharmaceutically acceptable clays in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

Compositions of iodophenoxy alkylene ethers and pharmaceutically

Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodobenzoic acid derivatives as the x-ray producing agents in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

Compositions of iodobenzoic acid derivatives and pharmaceutically

Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a nonionic x-ray producing agent in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

X-ray contrast compositions containing iodophenoxyalkanes and

Disclosed are x-ray contrast compositions of the formula ##STR1## wherein X is ##STR2## or --SO.sub.2 --; Z is H, halo, methyl, ethyl, n-propyl, C.sub.4 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups; R is C.sub.1 -C.sub.25 alkyl, cycloalkyl or aryl each of which may be optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl; lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy; n is 1-5; y is 0-4; and w is 1-4; in combination with a pharmaceutically acceptable clay; and method for their use in diagnostic radiology of the gastrointestinal tract.

Compositions of iodophenyl esters and iodophenyl sulfonates and

Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an iodoaniline derivative as the x-ray producing agent in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

X-ray contrast compositions containing iodoaniline derivatives and

Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a crystalline organic constrast agent in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

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Downingtown, PA, United States of America

Mary E Roberts