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Project

The influence of compression forces on the phase behavior of amorphous solid dispersions

The number of new drugs with low aqueous solubility is extremely high and as a consequence, their therapeutic effectiveness is also low. There exist a number of formulation strategies to increase the solubility and the formulation of low solubility compounds as an amorphous solid dispersion (this is a solid product that is made up of a non-crystalline polymer in which the drug is chaotically dispersed - comparable to a solution). However, it is known that unfavorable storage conditions (temperature and humidity) alter the structure of these materials leading to ineffective medication. We recently discovered as the first research group ever that the structure of amorphous solid dispersions can also change as a consequence of compressional forces that are applied during tablet manufacturing. This is an important finding because it points to an additional factor that can compromise the therapeutic value of the tablets. Also, it points to a missing link in the development chain of solid dispersions since until now, the impact of the transformation of amorphous solid dispersions from powders to tablets has not been studied. The objectives of this project are therefore to understand the physics behind the compression induced structural changes (phase separation) and to provide a solution to prevent this. In depth studies of the deformation behavior of selected amorphous solid dispersions upon compression as well as advanced solid state characterization will be undertaken for this purpose.

Date:1 Jan 2013 →  31 Dec 2016
Keywords:Dispersies, Amorfe, Compressiekrachten
Disciplines:Biomarker discovery and evaluation, Drug discovery and development, Medicinal products, Pharmaceutics, Pharmacognosy and phytochemistry, Pharmacology, Pharmacotherapy, Toxicology and toxinology, Other pharmaceutical sciences