Amorphous formulations

Research on amorphous materials focuses on improving dissolution properties of poorly soluble drugs. Majority of drug products (>80%) are tablets due to their ease of use. However, poor solubility of new drug substances compromises their formulation into e.g. tablets. Amorphization is one of the most efficient approaches to improve dissolution properties of poorly soluble drugs and it thus enables the use of such drug substances in tablet production.
The research at pharmaceutical technology focuses on amorphous mixtures of small molecule drugs (co-amorphous mixtures) and excipients and on solid polymer dispersions as approaches for improving drug dissolution and stability of the amorphous form. Selection of the excipients can be done systematically by in silico modeling and the amorphous materials are prepared by spray- or freeze drying or by mechanical activation. Suitability of the amorphous materials, prepared by mechanical activation, spray- or freeze-drying, for e.g. tablet preparations is evaluated by using research methods of physical pharmacy. These include investigating the dissolution and solid state properties by e.g. simultaneous dissolution/permeation testing and differential scanning calorimetry (TA DCS 2500, TA Instruments, USA), equipped also with an Optical Accessory kit for spectroscopic applications, a DSC Microscope Accessory for visual inspection and a LN2P liquid nitrogen cooler allowing operation at low temperatures (-180°C – +550°C) and fast cooling rates (to 140°C/min).