Lyophilized injectable formulations containing paclitaxel or other taxoid drugs - Patent Pending

United States Patent Application 20030099674
Kind Code A1
Chen, Andrew X. May 29, 2003
Lyophilized injectable formulations containing paclitaxel or other taxoid drugs
Abstract
A stable and porous lyophilized cake or powder is disclosed, which contains paclitaxel or another water-insoluble taxoid drug. This preparation is created by dissolving a taxoid drug in oil and a surfactant, with each component selected to provide a final product that will be benign and gentle, compared to the harsher and more toxic carriers used in paclitaxel emulsions today. An alcohol can also be used during the drug mixing step, but it should be removed before subsequent processing. The oily solution is mixed with an aqueous solution containing an non-proteinous anti-adhesion agent with a collapse temperature preferably in a range of about -25.degree. C. to about -35.degree. C., such as sucrose. The mixture is processed to form an emulsion, with oil droplets averaging less than about 2 microns (and preferably less than 1 micron) in diameter. This emulsion is passed through a sterilization filter and loaded into vials, and is lyophilized to form a porous cake or powder which is stable and can be stored for long periods without refrigeration. The cake or powder can be reconstituted with water shortly before use, to form an injectable emulsion or suspension which does not contain harsh and potentially toxic solubilizing agents or surfactants, and which contains oil droplets with very small diameters.
Inventors: Chen, Andrew X.; (San Diego, CA)
Correspondence Name and Address: Patrick D. Kelly
11939 Manchester #403
St. Louis
MO
63131
US
Serial No.: 218083
Series Code: 10
Filed: August 12, 2002
U.S. Current Class: 424/400; 514/27; 514/449
U.S. Class at Publication: 424/400; 514/449; 514/27
Intern'l Class: A61K 031/7048; A61K 031/337; A61K 009/00