Abstract
This comprehensive research delves into the formulation optimization, concentrating on the development and characterization of amorphous solid dispersions (ASDs) and abuse-deterrent formulations (ADFs). Acyclovir and acetaminophen were used as the model
drugs and the hot melt extrusion technique as the key formulation approach.
The study initiates with the development and validation of a robust High-Performance
Liquid Chromatography (HPLC) method for the quantitation of both drugs, thereby
providing a solid foundation for the subsequent formulation development.
This study further introduces an interdisciplinary approach by developing a novel web-based application that aids in optimizing ADFs. This combined approach of
complementing pharmaceutical sciences and digital technology underscores the innovative
quotient of this research, setting a precedent for current pharmaceutical research
methodologies.
A key segment of this thesis is the in-depth exploration of ASDs. Despite their theoretical
potential to enhance the bioavailability of poorly soluble drugs, the formulated ASDs,
employing Kollicoat® Protect and Kollicoat® IR as polymers, did not show a significant
improvement in dissolution. This underlines the intricate factors, including drug-polymer
interactions, drug-polymer ratio, and specifics of the preparation methodology, which
impact the performance of ASDs.
Simultaneously, the study pivots to develop effective ADFs by incorporating 4% (w/w)
xanthan gum into the ADFs. Comprehensive in vitro analyses, such as drug extraction in
different solvents, particle size reduction, scanning electron microscopy (SEM),
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dissolution tests, moisture uptake, and thermal analysis, affirm that the incorporation of
xanthan gum notably enhances the abuse-deterrent properties of these formulations.
When extrapolated to a global scale, these findings signify the potential of ADFs in
addressing the escalating crisis of prescription drug abuse. This could translate to
influencing regulatory policies, reducing the burden on healthcare systems, and improving
societal wellbeing through decreased drug-related crimes and increased productivity.
In conclusion, this research illuminates the complexities and untapped potential within
pharmaceutical formulation optimization, focusing on ASDs and ADFs. Despite the unmet
expectations with ASDs, the study emphasizes the continued need for research in this
domain. The exploration of ADFs presents promising solutions to tackle prescription drug
misuse, influencing global healthcare policies, regulatory guidelines, and socio-economic
challenges.