Euro-celtique S.a.

Steve Whitelock

Hassan Mohammad

Malcolm Walden

Geoffrey Gerard Hayes

Harjit Tamber

Deborah Phyllis Harding

Carl David Turner

Derek Allan Prater

Vincenzo Martinelli

Helen Kathleen Danagher

The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein Rand Rare independently Calkyl and * represents a stereocentre.

Dihydroetorphines and their preparation

The invention relates to a process for preparing a controlled release pharmaceutical extrudate using a melt extruder,

Extrusion

Extrusion of a mix containing a pharmaceutically active agent can be achieved using a plasticizing excipient in an amount sufficient to act as plasticizer and also act as lubricant, thereby avoiding the need for inclusion of a lubricant. The invention provides multiparticulates with controlled release properties, substantially free of lubricant. The present invention is preferably directed to extruded multiparticulates containing an opioid such as oxycodone, an ammonium methacrylate copolymer such as Eudragit&#xae; RSPO, a plasticizing excipient such as preferably stearyl alcohol and a water permeability modifier such as preferably Eudragit&#xae; RLPO. The obtained multiparticulates show a release rate profile which is pH-independent.

Multiparticulates

A neutral poly(ethyl acrylate, methyl methacrylate) copolymer is employed as a carrier in the manufacture of pharmaceutical formulations containing an active ingredient. The formulations are preferably made by melt extrusion, and can have rubbery characteristics and can exhibit tamper resistance.

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Cambridge, United Kingdom

Steve Whitelock