Science-Based Technology Selection & Formulation Development for Oral Bioavailability Enhancement

Capsugel Dosage Form Solutions White Paper

Authors: Hywel Williams, Michael Morgen, Eduardo Jule, Jan Vertommen, Hassan Benameur, Dwayne Friesen and David Vodak


The increasing fraction of poorly water-soluble compounds in pharmaceutical discovery is leading to significant growth in the use of enabling technologies to improve oral drug absorption and bioavailability (BA). Commonly used technologies in this area have been extensively reviewed (1) and include salt selection, cocrystals, amorphous solid dispersions, particle size reduction, cyclodextrins, amorphous/lipid micro- and nanoparticulates, adsorbents and lipid-based technologies. Many of these technologies have been shown to enhance drug BA, with most commercial products utilizing solid amorphous dispersion, nanocrystalline drug or lipid-based technologies. Examples include Neoral® (cyclosporine, Abbott), a lipid-based liquid-filled capsule; Incivek® (teleprevir, Vertex), an amorphous drug dispersion produced by spray drying; Kaletra® (lopinavir and ritonavir, Abbott) an amorphous drug dispersion produced by hot-melt extrusion (HME); and Emend® (aprepitant, Merck), a nanocrystal-containing tablet. Click here to download/view the whitepaper.