| As a growing number of new active compounds exhibit a very low solubility in biological media, the pharmaceutical industry is facing a major challenge to find routes to formulate such compounds in order to reach an “acceptable” bio-availability: More than one third of the drugs listed in the US Pharmacopoeia are considered as poorly-soluble, and a recent study stated that 41% of failures in new drug development in seven UK-owned companies have been attributed to poor biopharmaceutical properties, including water insolubility. In fact, it has been shown that, for most poorly-soluble compounds orally administered, the bio-absorption process is rate-limited by the dissolution in gastro-intestinal fluids; in the case of parenteral administration, the effective bio-availability of compounds is also limited by dissolution issues (risk of precipitation at the injection point, slow dissolution in serum,…). Many parameters related to solid morphology influences the dissolution rate of a compound, among which the particle size and the crystal habit and crystal pattern have a key-role. On two posters, we review literature and present some of our own results on the dissolution rate enhancement of poorly-soluble active ingredients by using supercritical fluid (SCF) processes in order to micronize these compounds into neat nano-/micro-particles, or to formulate them by micro-encapsulation, cyclodextrin (CD) inclusion and impregnation. |