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Thomas Rades: Amorphous drugs and formulations

Amorphous drugs and formulations

Thomas Rades1*

1 Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, DENMARK

The low water solubility of many low molecular weight drugs continues to be a challenge in the development of oral drug formulations, since low water solubility can lead to low or variable bioavailability. Amongst the various enabeling formulations that are conceived to tackle this challenge, a very promising approach to increase not only the dissolution rate but also the apparent solubility of drugs, if the conversion of the crystalline drug material into an amorhous form. In this presentation, we will initially discuss the prerequisites for the drug material itself to be successfully converted into an amorphous form. The criteria amorphization ability, supersaturation propensity and physical stability will be defined and key experiments to address these critical quality attributes will be described. In the second part of the presentation, we will discuss amorphous drugs in amorphous solid dispersions with polymers and as co-amorphous systems together with another low molecular weight partner molecule (co-former). Specifically we will address the questions: how much drug can be loaded into a polymeric amorphous solid dispersion and how to find the right co-former molecule and drug to co-former ratio.

Selected references for further reading:

Liu J et al. Pharmaceutics 13: 389 (2021)

Kissi EO et al. Journal of Physical Chemistry B 122: 2803 – 2808 (2018)

Blaabjerg LI et al. International Journal of Pharmaceutics 538: 243 – 249 (2018)

Ruggiero MT et al. Phys Chem Chem Phys 19: 30039 – 30047 (2017)

Blaabjerg L et al. Molecular Pharmaceutics 13: 3318 - 3325 (2016)

Rask MB et al. European Journal of Pharmaceutical Sciences 85: 10-17 (2016)

Keywords: poorly water soluble drugs, amorphous, amorphous solid dispersions, co-amorphous, supersaturation