Highly loaded amorphous efavirenz composition and process for preparing the same

• Main Authors: LESTER JAMES DAVID, DURIG THOMAS, BULL RANDY, RAHMAN MOHAMMED ABDUL, BI YUNXIA
• Format: Patent
• Language: English
• Published: 25.08.2015
• Subjects: AFTER-TREATMENT OF THE SHAPED PRODUCTS, e.g. REPAIRING; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PERFORMING OPERATIONS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SHAPING OF MATERIAL IN A PLASTIC STATE, NOT OTHERWISE PROVIDEDFOR; SHAPING OR JOINING OF PLASTICS; TRANSPORTING; WORKING OF PLASTICS; WORKING OF SUBSTANCES IN A PLASTIC STATE, IN GENERAL

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.