Enhancing the bioavailability of hydrophobic drugs using hot melt extrusion

Abstract

Many existing drugs (as well as new revelations) in the pharmaceutical industry bear a distinct disadvantage in the sense that they are not water soluble, displaying low bioavailability values and consequently a reduced invitro effect. Hot melt extrusion (HME) is one technique currently being used to increase the solubility of hydrophobic compounds. The current study examined the feasibility of enhancing the bioavailability of poorly soluble veterinary anthelmintics using melt extrusion. It was demonstrated that melt extrusion changed the morphology of the API,converting it from a crystalline (insoluble) to an amorphous (soluble) state. Subsequent dissolution trials demonstrated the concept dosage forms to greatly enhance the solubility of the API.