Jeroen Van Renterghem

Laboratory of Pharmaceutical Process Analytical Technology

Ottergemsesteenweg 460
B-9000 Gent (Belgium)
Tel.: +32-9-264.80.39
Fax: +32-9-222.82.36
E-mail: Jeroen.VanRenterghem@UGent.be
Education: Pharmacist (Master in Drug Development)

Pharmaceutical hot-melt extrusion: significance and influence of cooling

The development of oral formulations for new small drug molecules is characterized by two major challenges. (i) More than 90% of the new molecules in drug development suffers from poor water solubility; (ii) traditional oral drug delivery systems are often subject to fluctuations in drug plasma concentrations, which is caused by the periodic drug delivery.

Hot-melt extrusion (HME) is a production technology that makes it possible to formulate products that (i) improve the dissolution rate and bioavailability of poorly water-soluble drugs (i.e., immediate release formulations), and (ii) show drug release over a longer time (i.e., sustained release formulations).

Hot-melt extrusion is one of the most widely applied processing technologies in the plastic, rubber and food industry, and has significant potential as a continuous process in the pharmaceutical industry. Extrusion is the process of converting a raw material into a product of uniform shape and density by forcing it through a die under controlled conditions. Hot-melt extrusion offers several advantages over traditional processing techniques for pharmaceutical applications. The process is anhydrous and requires no solvents, entails a continuous operation necessitating fewer processing steps, requires no compression of the actives, offers the possibility of the formation of solid dispersions and solid solutions and improves bioavailability of poorly soluble drugs.

The purpose of this research is to examine the influence of cooling after HME on the solid state, stability, drug release and processability of melt extruded pharmaceutical formulations.