Rapamycin formulation for IV injection

US5530006A · kind A · utility

Assignee

• Amerimas Home Products, Inc. · US

Inventors

• Robert P. Waranis · Chazy, US
• Maureen M. Harrison · Queensbury, US
• Thomas W. Leonard · Plattsburgh, US
• Robin Enever · Rouses Point, US

Key dates

• Filing date: Mar 7, 1994
• Grant date: Jun 25, 1996
• Expiry date: Mar 7, 2014

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P37/06
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.