American Home Products Corporation

Maureen M Harrison

Gerald L Reuter

Thomas W Leonard

Robert P Waranis

Robin P Enever

Mark E Coons

Christian L Ofslager

The present invention comprises oral rapamycin formulations which contain, per 100 ml of the formulation, from about 0.01 to about 10.0 grams per 100 ml of rapamycin, from about 0.1 to about 10 ml of surfactant, from about 0.1 to about 25 ml of N,N-dimethylacetamide, and from about 65 to about 99.8 ml of a lecithin or phospholipid solution.

Rapamycin formulations for oral administration

Disclosed herein is an aqueous, injectable rapamycin solution comprising 0.1 to 10 percent of a concentrate solution of rapamycin in N,N-dimethylacetamide, at concentrations of rapamycin ranging from 0.25 mg/ml to 100 mg/ml, in combination with a diluent solution consisting of 0.1 to 10 weight percent of one or more polyoxyethylene sorbitan esters, 10 to 60 weight percent of either polyethylene glycol 200 or 300 or both and 30 to 90 volume percent water, wherein the concentration of rapamycin in he combined solution ranges from 0.05 mg/ml to 5.0 mg/ml. Also disclosed is an aqueous, injectable solution of rapamycin, said solution comprising rapamycin in 0.1 to 10 weight percent N,N-dimethylacetamide, 0.09 to 7.5 weight percent of one or more polyoxyethylene sorbitan esters, 9 to 60 weight percent of either polyethylene glycol 200 or 300 or both and 30 to 90 volume percent of water, wherein the concentration of rapamycin in the solution ranges from 0.05 mg/ml to 5.0 mg/ml. Preferred aqueous, injectable rapamycin solutions are those wherein one polyoxyethylene sorbitan ester is present and the polyethylene glycol present is polyethylene glycol 300.

Rapamycin formulation for IV injection

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St. Albans, VT, United States of America

Maureen M Harrison