Sonus Pharmaceuticals, Inc.

Shire Laboratories, Inc.

Alexander K Tustian

Panayiotis P Constantinides

Karel J Lambert

Steven C Quay

Edward M Rudnic

Beth A Burnside

Richard Alan Couch

Charlotte M McGuinness

Xiaodi Guo

Nagesh Palepu

Dean R Kessler

Andrew M Nienstedt

A method of making an emulsion of tocopherol incorporating a co-solvent and, stabilized by biocompatible surfactants, as a vehicle or carrier for therapeutic drugs, which is substantially ethanol free and which can be administered to animals or humans by various routes, is disclosed. Also included in the emulsion is PEGylated vitamin E. PEGylated &#x3b1;-tocopherol includes polyethylene glycol subunits attached by a succinic acid diester at the ring hydroxyl of vitamin E and serves as a primary surfactant, stabilizer and a secondary solvent in emulsions of &#x3b1;-tocopherol.

Emulsion vehicle for poorly soluble drugs

The present invention provides methods for administering a taxane composition for the treatment of cancer. In one aspect, the compositions are not diluted prior to administration. Some embodiments provide methods for administering a taxane as a bolus injection or an intravenous infusion in less than about 30 minutes. In other aspects, the invention provides methods for administering a taxane to provide high concentrations of the taxane in blood or in tumors. Another aspect provides methods for administering a taxane to provide anti-tumor activities against solid tumors. In some embodiments, the methods provide anti-tumor activities against tumors that were resistant to conventional taxane administration methods. In some embodiments, the methods provide anti-tumor activities against colorectal tumors.

Method for treating colorectal carcinoma using a taxane/tocopherol formulation

Disclosed is a beadlet comprising (i) a hydrophobic long chain fatty acid or ester material; (ii) a surfactant; and (iii) a therapeutic agent which in admixture form a solid solution at room temperature. The hydrophobic material preferably has a melting point of about 40 to about 100&deg; C., and is most preferably glyceryl behenate. The surfactant is preferably a polyglycolyzed glyceride, polyoxyethylene sorbate, ethylene or propylene block copolymer or combinations thereof, and is most preferably polyoxyethylene 20 sorbitan monolaurate.

Solid solution beadlet

An emulsion of tocopherol incorporating a co-solvent and, stabilized by biocompatible surfactants, as a vehicle or carrier for therapeutic drugs, which is substantially ethanol free and which can be administered to animals or humans by various routes is disclosed. Also included in the emulsion is PEGylated vitamin E. PEGylated &agr;-tocopherol includes polyethylene glycol subunits attached by a succinic acid diester at the ring hydroxyl of vitamin E and serves as a primary surfactant, stabilizer and a secondary solvent in emulsions of &agr;-tocopherol.

Compositions of tocol-soluble therapeutics

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Bothell, WA, United States of America

Alexander K Tustian