Cocrystals as an alternative to combination drugs: cocrystallization, physico-chemical characterization and structural determination of cocrystallized active pharmaceutical ingredients

Project: Research

Description

Cocrystallization is a technique which has taken tremendous importance in
the last decade. It aims to combine two (or more) chemical entities to form
new crystalline materials. Cocrystals are interesting in many areas and
particularly in the pharmaceutical field. They can indeed allow for the
optimization of solubility and dissolution properties of poorly soluble
pharmaceutical compounds while maintaining therapeutic properties.
Cocrystallization could be an alternative to combination drugs (combination
of two (or more) active compounds in a single tablet) avoiding problems
during the formulation phase (solubility, stability, …). Up to now, a very
limited number of multidrug cocrystals have been reported.
The principal aim of this research project is to form and characterize new
cocrystals of active pharmaceutical compounds. Within the frame of this
PhD, two systems have been selected: combined antituberculosis agents
(isoniazid and pyrazinamide) and anti-Parkinsionian drugs (levodopa and
benserazide).
Throughout our project, crystal molecular engineering and solid-state
synthesis will be applied to optimally arrange complementary chemical
functions (synthons) of drug molecules in order to modulate major physicochemical
properties of the resulting crystalline solids, in particular stability,
solubility and dissolution rate.
This crystal engineering approach should also contribute to a fundamental
knowledge of the principles underlying formation of ternary cocrystals and to
a systematic approach of expected synergetic effects of combination of
multiple drugs on their solubility and dissolution rate.
Once validated with the selected candidates, our approach, if successful,
could be generalized to a wide variety of systems.
Short titleCO-DRUGS
StatusFinished
Effective start/end date1/10/1726/09/19

Attachment to an Research Institute in UNAMUR

  • NARILIS
  • NISM