Highly loaded amorphous efavirenz composition and process for preparing the same

US9114170B2 · kind B2 · utility

Assignee

• ISP Investments LLC · US

Inventors

• Yunxia Bi · Westtown, US
• Mohammed Abdul Rahman · Columbia, US
• James David Lester · West Boylston, US
• Thomas Durig · Chadds Ford, US
• Randy A. Bull · Hopewell, US

Key dates

• Filing date: Mar 15, 2013
• Grant date: Aug 25, 2015
• Expiry date: Apr 9, 2033

Classification

• Technology area (CPC B): Performing Operations; Transporting
• CPC primary: B29C43/003
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A stable and high loading ternary solid dispersion composition comprising (a) about 50% wt. to about 90% wt. of amorphous Efavirenz; (b) about 10% wt. to about 50% wt. of polyvinyl pyrrolidone (PVP), a first polymer; (c) about 1% wt. to about 30% wt. of a water-soluble second polymer; and (d) optionally about 0.1% wt. to about 50% wt. of at least one pharmaceutically acceptable excipient. Also discloses a high loading ternary composition comprising (a) a solid dispersion composition comprising (i) about 50% wt. to about 90% wt. of amorphous Efavirenz; (ii) about 10% wt. to about 50% wt. of polyvinyl pyrrolidone, a first polymer; (b) about 1% wt. to about 30% wt. of a water-soluble second polymer blended with solid dispersion of composition of (a); and (c) optionally about 0.1% wt. to about 50% wt. of at least one pharmaceutically acceptable excipient. Additionally discloses a method for preparing solid dosage forms comprising (i) amorphous Efavirenz and (ii) polyvinyl pyrrolidone (PVP), a first polymer; (iii) a water-soluble second polymer; and (iv) optionally, at least one pharmaceutical excipients.