Sanofi-aventis

Sanofi-synthelabo

Nanosystems L.l.c.

Sanofi Pharmaceuticals, Inc.

Nancy M Franson

William L Rocco

Sharon M Laughlin

Irwin C Jacobs

John D Higgins

Micael Guillot

Khawla Abdullah Abu-Izza

Micael A Guillot

Donald R Snyder

John D c/o Sanofi-Aventis Département De Brevets Higgins

Disclosed are amorphous solid dispersion formulations comprising 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide.

Amorphous solid dispersions

A method for preparing pharmaceutical formulations of poorly soluble drug substances in the form of concentrated solutions for filling soft gelatin capsules and solid dispersions and suspensions for filling hard gelatin capsules and compressing into tablets is provided. Pharmaceutical formulations of poorly soluble drug substances are also disclosed. The formulations include the sodium salt of the poorly soluble drug substance, a conversion aid such as PEG, polysorbate, a sugar alcohol (e.g. mannitol or xylitol), propylene glycol or transcutol, and, in some cases an excipient, such as dicalcium phosphate dihydrate, lactose monohydrate, or microcrystalline cellulose.

Pharmaceutical formulations containing poorly soluble drug substances

A pharmaceutical formulation comprising ##STR1## as the active ingredient, polyethylene glycol, NaOH, and water, wherein the mole equivalents of NaOH per mole equivalent of active ingredient is at least about 1.1, is suitable for soft gelatin capsule filling.

Pharmaceutical formulation

Dispersible particles consisting essentially of crystalline NSAID having hydroxypropyl cellulose adsorbed on the surface thereof in an amount sufficient to maintain an effective average particle size of less than about 1000 nm. Pharmaceutical compositions containing the particles exhibit unexpectedly reduced gastric irritation following oral administration and/or hastened onset of action.

Milled naproxen with hydroxypropyl cellulose as a dispersion stabilizer

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Collegeville, PA, United States of America

Nancy M Franson