European Journal of Pharmaceutics and Biopharmaceutics,
Journal Year:
2024,
Volume and Issue:
203, P. 114463 - 114463
Published: Aug. 27, 2024
This
work
studies
the
formation
of
deep
eutectic
solvents
formed
by
one
active
pharmaceutical
ingredient
(quinine,
pyrimethamine,
or
2-phenylimidazopyridine)
and
a
second
component
potentially
acting
as
an
excipient
(betaine,
choline
chloride,
tetramethylammonium
thymol,
menthol,
gallic
acid,
vanillin,
acetovanillone,
4-hydroxybenzaldehyde,
syringaldehyde,
propyl
gallate,
propylparaben,
butylated
hydroxyanisole),
aiming
to
address
challenges
regarding
drug
solubility,
bioavailability,
permeability.
A
preliminary
screening
was
carried
out
using
thermodynamic
model
COSMO-RS,
narrowing
down
search
three
promising
excipients
(thymol,
hydroxyanisole).
Nine
solid-liquid
equilibrium
(SLE)
phase
diagrams
were
experimentally
measured
combining
drugs
with
screened
excipients,
combination
visual
melting
method
differential
scanning
calorimetry.
Negative
deviations
from
ideality
observed
in
all
nine
systems.
Furthermore,
total
four
new
cocrystals
found,
powder
single
crystal
X-ray
diffraction
techniques
being
employed
verify
their
unique
patterns.
In
modelling
SLE
diagrams,
two
COSMO-RS
parametrizations
(TZVP
TZVPD-FINE)
also
applied,
though
neither
consistently
delivered
better
description
over
other.
