US2012070498A1PendingUtilityA1

Submicron Particles of Antineoplastic Agents

43
Individually held — no corporate assignee on recordPriority: Dec 22, 2000Filed: Sep 23, 2011Published: Mar 22, 2012
Est. expiryDec 22, 2020(expired)· nominal 20-yr term from priority
Inventors:Mahesh V. ChaubalJane WerlingBarrett Rabinow
A61P 35/00A61K 9/1271A61K 9/10A61K 9/146A61K 31/12A61K 31/337A61K 31/55A61K 31/495A61K 9/1688A61K 31/496A61K 31/573A61K 9/14A61K 9/145A61K 9/127A61Q 7/00A61K 2800/82A61K 2800/412A61K 8/65A61K 8/0241
43
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Claims

Abstract

The present invention is concerned with the formation of submicron particles of an antineoplastic agent, particularly paclitaxel, by precipitating the antineoplastic agent in an aqueous medium to form a pre-suspension followed by homogenization. Surfactants with phospholipids conjugated with a water soluble or hydrophilic polymer such as PEG are used as coating for the particles. The particles produced generally have an average particle size of less than about 1000 nm and are not rapidly soluble.

Claims

exact text as granted — not AI-modified
1 .- 34 . (canceled) 
     
     
         35 . A pharmaceutical composition of submicron particles of precipitated paclitaxel or docetaxel comprising a suspension of precipitated small particles of an active agent, a phospholipid conjugated with a water-soluble or hydrophilic polymer, and a copolymer of oxyethylene and oxypropylene, the precipitated small particles having an average effective particle size of less than 1000 nm, and the active agent consisting of paclitaxel or docetaxel. 
     
     
         36 . The composition of  claim 35 , wherein the phospholipid is natural or synthetic. 
     
     
         37 . The composition of  claim 35 , wherein the phospholipid is phosphatidylcholine, phosphatidylethanolamine, diacyl-glycero-phosphoethanolamine, phosphatidylserine, phosphatidylinositol, phosphatidylglycerol, phosphatidic acid, lysophospholipids, egg or soybean phospholipid or a combination thereof. 
     
     
         38 . The composition of  claim 37 , wherein the diacyl-glycero-phosphoethanolamine is selected from the group consisting of: dimyristoyl-glycero-phosphoethanol-amine (DMPE), dipalmitoyl-glycero-phosphoethanolamine (DPPE), distearoyl-glycero-phosphoethanolamine (DSPE), and dioleolyl-glycero-phosphoethanolamine (DOPE). 
     
     
         39 . The composition of  claim 35 , wherein the water-soluble or hydrophilic polymer conjugated with the phospholipid is polyethylene glycol (PEG). 
     
     
         40 . The composition of  claim 39 , wherein the PEG is selected from the group consisting of PEG 350, PEG 550, PEG 750, PEG 1000, PEG 2000, PEG 3000, and PEG 5000. 
     
     
         41 . The composition of  claim 35 , wherein the water-soluble or hydrophilic polymer conjugated with the phospholipid is selected from the group consisting of: dextran, hydroxypropyl methacrylate (HPMA) and polyglutamate. 
     
     
         42 . The composition of  claim 35 , wherein the copolymer of oxyethylene and oxypropylene is a block copolymer. 
     
     
         43 . The composition of  claim 35 , wherein the copolymer of oxyethylene and oxypropylene is poloxamer. 
     
     
         44 . The composition of  claim 35 , wherein the small particles have an average effective particle size of less than 400 nm. 
     
     
         45 . The composition of  claim 35 , wherein the small particles have an average effective particle size of less than 200 nm. 
     
     
         46 . The composition of  claim 35 , wherein the small particles have an average effective particle size of less than 150 nm. 
     
     
         47 . The composition of  claim 35 , wherein the composition is sterile. 
     
     
         48 . The composition of  claim 35 , wherein the composition is formulated for administration by a route selected from the group consisting of: parenteral, oral, pulmonary, topical, ophthalmic, nasal, buccal, rectal, vaginal, and transdermal. 
     
     
         49 . The composition of  claim 35 , wherein the particles do not aggregate under stressed conditions or upon storage. 
     
     
         50 . A pharmaceutical composition of submicron particles of precipitated paclitaxel or docetaxel comprising a dry powder of precipitated small particles of an active agent, a phospholipid conjugated with a water-soluble or hydrophilic polymer, and a copolymer of oxyethylene and oxypropylene, the precipitated small particles having an average effective particle size of less than 1000 nm, and the active agent consisting of paclitaxel or docetaxel. 
     
     
         51 . The composition of  claim 50  further comprising a diluent. 
     
     
         52 . The composition of  claim 51 , wherein the diluent is suitable for parenteral administration of the particles.

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