Immediate release formulations of 1-aminocyclohexane compounds, memantine and neramexane

US8834924B2 · kind B2 · utility

Assignee

• FOREST LABORATORIES HOLDINGS LIMITED · US

Inventors

• Yan Yang · Suzhou, CN
• Rajiv Janjikhel · Owings Mills, US
• Niranjan Rao · Monroeville, US
• Antonia Periclou · Jersey City, US
• Wattanaporn Abramowitz · Plainsboro, US
• Mahendra G. Dedhiya · Pomona, US
• Erhard Seiller · Nidderau, DE
• Bernhard Hauptmeier · Gelnhausen, DE

Key dates

• Filing date: Jun 8, 2011
• Grant date: Sep 16, 2014
• Expiry date: Jun 8, 2031

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to an immediate release solid oral dosage form containing 1-aminocyclohexanes, preferably memantine or neramexane, and optionally a pharmaceutically acceptable coating, wherein the active ingredient exhibits dose proportionality and is released at a dissolution rate of more than about 80% within about the first 60 minutes following entry of said form into a use environment. The dosage form is direct compressed and has a hardness within the range of between about 3 and about 40 Kp, exhibits an average Tmax within the range of about 2 to about 8 hours with an active ingredient load within the range of about 2.5 to about 150 mg. The formulation allows for dose-proportional compositions for once daily or b.i.d. dosing, while maintaining a steady average range of Tmax.