The United States of America, as Represented by the Secretary, Department of Health and Human Services

Ascent Pharmaceuticals, Inc.

S Esmail Tabibi

B Rao Vishnuvajjala

Shanker Gupta

Emmanuel I Ezennia

Robert W Mendes

Nitin P Pathak

The present invention provides a drug delivery system comprising a water-insoluble drug, a water-miscible organic solvent for the water-insoluble drug, a surfactant, and water, as well as a process for preparing the same. This invention further provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and such a drug delivery system. In addition, the present invention provides a method of delivering a drug to a host by administering to the host the drug delivery system of the present invention.

Water-insoluble drug delivery system

A controlled release aqueous emulsion is disclosed, as are its method of manufacture and use as a vehicle for delivering medicaments in liquid form. A contemplated emulsion comprises an oil-in-water emulsion having an average oil particle size of about 100 nm to about 250 nm, a pH value of about 4.5 to about 8.0 and a viscosity at 20.degree.-25.degree. C. of 1 to about 1000 cps. The water phase constitutes at least 25 weight percent of the total composition. The oil phase is a wax matrix that is a wax having a melting point of about 40.degree. to about 80.degree. C. and is present in an amount of about 3 to about 30 percent of the total composition. A pharmaceutically effective amount of a pharmacologically active compound that is free from decomposition at a temperature below about 90.degree. C. is dissolved or dispersed in the wax matrix. The oil and water phases are emulsified by an emulsifying agent that provides freedom from phase separation at a pH value of about 4.5 to about 8, while also providing phase separation at a pH value below about 2.0. The emulsifier, based on lecithin, is present at about 2 to about 20 weight percent of the total composition. The composition can also contain zero to about 35 weight percent additional excipient.

Controlled release aqueous emulsion

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Rockville, MD, United States of America

S Esmail Tabibi