Hot-melt extrudable pharmaceutical formulation

• US 6,488,963 B1
• Filed: 03/02/1999
• Issued: 12/03/2002
• Est. Priority Date: 06/26/1996
• Status: Expired due to Term

• Current Assignee: University of Texas System
• Original Assignee: University of Texas System
• Inventors: McGinity, James W., Zhang, Feng
• Primary Examiner(s): Webman, Edward J.
• Application Number:
  US09/260,694
• Time in Patent Office: 1,372 Days
• Field of Search: 424/484, 424/486, 424/468, 424/457, 424/500, 424/422, 514/953, 514/964, 514/772.7
• US Class Current: 424/486
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00

Abstract

The present invention relates to pharmaceutical formulations comprising a hot-melt extrudable mixture of a therapeutic compound and a high molecular weight poly(ethylene oxide) in an essentially non-film like preparation. In some embodiments, the formulation further comprises poly(ethylene glycol). The present invention also includes efficient methods for hot-melt extruding pharmaceutical formulations in essentially non-film preparations.

Claims

1. A non-film controlled release pharmaceutical formulation comprising an effective amount of a therapeutic compound and a high molecular weight poly(ethylene oxide), wherein the poly(ethylene oxide) has a molecular weight of about 1,000,000 to about 10,000,000 Daltons, and wherein the poly(ethylene oxide) and the therapeutic compound comprise a ratio of poly(ethylene oxide) to therapeutic compound of from about 99.99:

.01 weight percent to about 50;

50 weight percent.

2. The non-film controlled release pharmaceutical formulation of claim 1 further comprising a plasticizer.

3. The non-film controlled release formulation of claim 2 wherein the plasticizer is selected from the group consisting of:

an oligomer, a copolymer, an oil, a organic molecule, a polyol having aliphatic hydroxyls, an ester-type plasticizer, a glycol ether, poly(propylene glycol), a multi-block polymer, a single block polymer, and a poly(ethylene oxide) having a molecular weight less than about 500,000 Daltons.

4. The non-film controlled release pharmaceutical preparation of claim 3, wherein the polyethythene oxide is further defined as polyethylene oxide having a molecular weight less than about 500,000 Daltons.

5. The non-film controlled release pharmaceutical formulation of claim 4, further comprising poly(ethylene glycol).

6. The non-film controlled release pharmaceutical formulation of claim 1 wherein said formulation is prepared by a process of hot-melt extrusion.